2026-10-16T05:10:19Z https://pharmacia.pensoft.net/oai.php

10.3897/pharmacia.66.e35643 2019-05-14 pharmacia

Development of a chiral RP-HPLC method for identification of stereomers of newly synthesised xanthine-based hydrazide-hydrazone compound Peikova,Lily Tzankova,Diana Mateeva,Alexandrina Georgieva,Maya Zlatkov,Alexander xanthine-hydrazone isomers chiral RP-HPLC Pharmacia 66(1): 1-6 A reverse phase enantio-selective high performance liquid chromatographic method was developed for enantiomeric separation of 2-(1,3-dimethyl-2,6-dioxo-2,3-dihydro-1H-purine-7(6H)-yl)-N’-(3-fluorobenzylidene)-propanehydrazide isomers. The enantiomers of 2-(1,3-dimethyl-2,6-dioxo-2,3-dihydro-1H-purine-7(6H)-yl)-N’-(3-fluorobenzylidene)propanehydrazide were resolved on a ACE®Equivalence™ С18 (250 × 4.6 mm, 5 μm) column using a mobile phase system containing methanol, water, phosphate buffer рН 7.4 (50:46:4 v/v/v). The resolution between enantiomers was found to be more than 2.0. The sample solution and mobile phase were found to be stable for at least 48 h. The final optimised method was successfully applied to separate the (R)- and the (S)-enantiomers of 2-(1,3-dimethyl-2,6-dioxo-2,3-dihydro-1H-purine-7(6H)-yl)-N’-(3-fluorobenzylidene)-propanehydrazide and was proven to be reproducible and accurate. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35643 https://doi.org/10.3897/pharmacia.66.e35643 https://pharmacia.pensoft.net/article/35643/ https://pharmacia.pensoft.net/article/35643/download/pdf/ en

10.3897/pharmacia.66.e35293 2019-06-06 pharmacia

Antibacterial acticivity of extracts from Potentilla reptans L. Mincheva,Irena Zaharieva,Maya Batovska,Daniela Najdenski,Hristo Ionkova,Iliana Kozuharova,Ekaterina Potentilla reptans antibacterial activity mastitis traditional use Pharmacia 66(1): 7-11 Potentilla reptans is widely used in traditional medicine as an astringent, for treating diarrhoea, haemorrhoids and for bleeding gums. A recent ethnobotanical study has reported on the anti-mastitis effects of the aerial parts of P. reptans decoction. The aim of the present study is to evaluate the antibacterial potential of extracts and fractions, obtained from aerial parts of P. reptans against three strains of Staphylococcus aureus. The observed MICs were within the range of 0.325 – 2.5 mg/ml. Studied extracts and their fractions exerted mostly bacteriostatic effect, with the n-hexane fraction of hydroethanolic extract being the most active (MIC 0.313 mg/ml against S. aureus ATCC 6538 P). However, further investigations are necessary to reveal the precise mode of action of P. reptans against mastitis. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35293 https://doi.org/10.3897/pharmacia.66.e35293 https://pharmacia.pensoft.net/article/35293/ https://pharmacia.pensoft.net/article/35293/download/pdf/ en

10.3897/pharmacia.66.e35048 2019-06-06 pharmacia

The memory and learning enhancing effects of Atristamine Podolsky,Illya Shtrygol',Sergiy 2-methyl-3-(phenylaminomethyl)-1H-quinolin-4-one Atristamine the Morris water maze the memory enhancing effect Pharmacia 66(1): 13-18 The object of the present study, 2-methyl-3-(phenylaminomethyl)-1H-quinolin-4-one (Atristamine), has been deeply studied as a promising antidepressant with the unique spectrum of additional neuropharmacological properties. Previously, the memory-enhancing effects of Atristamine have already been studied in the passive-avoidance test after scopolamine-induced amnesia in mice. Thus, the study of the effects of Atristamine on the spatial learning and memory in the Morris water maze under physiological conditions was the next logical step of our research. According to the results obtained, Atristamine (100 mg/kg) has almost the same effect on the main markers of the memory-enhancing activity (the escape latency and distance moved) as Piracetam (300 mg/kg) and Phenibut (20 mg/kg) chosen as the well-studied and widely-used memory enhancers. The escape latency decreased in the Atristamine group by 3.2 times compared to the vehicle control group, whereas Piracetam and Phenibut caused a significant reduction of this indicator by 4.3 and 3.7 times, respectively. Moreover, the rats from the Atristamine group swam 5.1 times shorter distance to the platform in the probe trial compared to animals from the vehicle control group. The distance moved was 3-fold shorter in the Piracetam group and decreased by 5.2 times in the Phenibut group. All drugs used in this study caused considerable changes of inter-quadrant preferences of animals. Based on the analysis of the inter-quadrant behaviour of rats, it has been found that there are considerable differences in search strategies associated, probably, with distinct mechanisms of the memory and learning enhancing action of the drugs used. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35048 https://doi.org/10.3897/pharmacia.66.e35048 https://pharmacia.pensoft.net/article/35048/ https://pharmacia.pensoft.net/article/35048/download/pdf/ en

10.3897/pharmacia.66.e35083 2019-06-07 pharmacia

QSAR-analysis of 1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl]propyl)-2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one’s derivatives as potential antioxidants Drapak,Iryna Zimenkovsky,Borys Perekhoda,Lina Yeromina,Hanna Lipakova,Kateryna Demchuk,Inna Rakhimova,Maryna antioxidant activity molecular descriptors 1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl]propyl)-2 3-dihydro-1 3-thiazol-5-yl]ethane-1-one derivatives QSAR analysis Pharmacia 66(1): 33-40 Aim. The aim of study was to determine of the parameters of the molecular structure of new 1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl]propyl)-2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one derivatives and QSAR-analysis. The latter can be considered as the theoretical basis for de novo design of new potential antioxidants. Materials and methods. 14 new derivatives of 1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl] propyl)-2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one were involved in the study and their antioxidant activities were evaluated. Hyper-Chem 7.59 and BuildQSAR software were used for calculation of molecular descriptors and building the QSAR-models. Results. The calculation of number of molecular descriptors (electronic, steric, geometric, energy) was carried out for the tested compounds: 14 derivatives of 1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl] propyl) -2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one. For QSAR analysis, the compounds studied were divided into a training and test sample. The correlations between the antioxidant activity level and abovementioned molecular descriptors were shown in multivariate linear QSAR-model: Activity = ∑хіаі + bі, where xi – molecular descriptor. Based on the analysis of the obtained QSAR-models, it was found that antioxidant activity increases with decreasing of the area, molecular volume, lipophilicity, polarisation and increasing the magnitude of the dipole moment. The increase in the energy of the bonds, the energy of inter-nuclear interactions, the energy of the lower vacant molecular orbit and the reduction of the energy of hydration and energy of the higher vacant molecular orbitals also results in an increase in the antioxidant activity. The greatest effect of effective charges on atoms on the antioxidant activity was detected: the increase in the charge value on the morpholine cycle Oxygen and the decrease in the charge size on the Sulphur atom of the thiazole ring and the Oxygen atom of the acetyl group. QSAR models with better statistics were selected. QSAR models obtained are characterised by high predictive ability, determined both by internal and external validation and can be used for virtual screening of the antioxidant activity of substances of this class of compounds. Conclusions. 1). The study of the structure–activity relationships for 1-[2-(R-phenylimino)-4-methyl-3-(3- [morpholine-4-yl]propyl)-2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one derivatives were carried out. 2). QSAR analysis revealed the following: polarisation, dipole moment, lipophilicity, energy parameters as well as the size of the molecule and its branching possessed the most significant effect on antioxidant activity; the antioxidant activities of the compounds were increased with the increase in their hydrophilic and reductive properties; the molecules with small volume and surface area showed the higher level of antioxidant activity. 3). Obtained QSAR models are proposed for antioxidant activity prediction within the above-mentioned row of compounds and can be considered as a theoretical basis for de novo design of new potential antioxidants. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35083 https://doi.org/10.3897/pharmacia.66.e35083 https://pharmacia.pensoft.net/article/35083/ https://pharmacia.pensoft.net/article/35083/download/pdf/ en

10.3897/pharmacia.66.e35022 2019-06-07 pharmacia

Justification of technological parameters of the cream production with sapropel extract Strus,Oksana Polovko,Nataliia Yezerska,Oksana apropel extract o/w emulsion cream emulsification methods technology Pharmacia 66(1): 19-25 The aim of the research was to substantiate the technological parameters of cream production with the sapropel extract and work out the technological scheme for its production. In this study, extract of sapropel from the Prybych deposit, emulsion base, containing corn oil, emulsifier No.1, cetylstearyl alcohol, nisin, euxyl K 100 and purified water were employed. To carry out the research, a set of methods to analyse colloidal and thermal stability was used. Rheological properties of the samples were determined. The method of microscopic analysis was carried out to analyse the stability of the emulsion system. It was proved experimentally that, when producing the cream, it is appropriate to use the phase inversion method, and the emulsification needs to be carried out at 5000 r/m for 20 min. Size and shape of the sample drops, obtained at 5000 r/m, were monodisperse and more uniform, most of which range from 2 to 3 microns that indicates the system stability. The following parameters of technological process were determined: mixing temperature conditions, speed of homogenisation and mixing time. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35022 https://doi.org/10.3897/pharmacia.66.e35022 https://pharmacia.pensoft.net/article/35022/ https://pharmacia.pensoft.net/article/35022/download/pdf/ en

10.3897/pharmacia.66.e35131 2019-06-07 pharmacia

Synthesis of some new 4-iminothiazolidine-2-ones as possible antioxidants agents Chaban,Taras Ogurtsov,Volodymyr Chaban,Ihor Myrko,Iryna Harkov,Stefan Lelyukh,Maryan antioxidant activity 4-iminothiazolidine-2-ones synthesis Pharmacia 66(1): 27-32 Novel N3 substituted derivatives of 4-iminothiazolidine-2-one were synthesised under the reactions of [2+3]cyclocondensation, thionation and aminolysis. The functionalisation of 3-phenyl-4-imino-thiazolydine-2-one was carried out in its C5 position under condensation Knoevenagel and nitrosation reactions. The antioxidant activity of the synthesised compounds was evaluated in vitro by the method of their scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals. When compared with existing antioxidants, some of our compounds were found to be more potent. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35131 https://doi.org/10.3897/pharmacia.66.e35131 https://pharmacia.pensoft.net/article/35131/ https://pharmacia.pensoft.net/article/35131/download/pdf/ en

10.3897/pharmacia.66.e35139 2019-07-09 pharmacia

Ethnobotany and exploitation of medicinal plants in the Rhodope Mountains – is there a hazard for Clinopodium dalmaticum? Mincheva,Irena Jordanova,Michaela Benbassat,Niko Aneva,Ina Kozuharova,Ekaterina sustainable use medicinal plants plant collection herbal tea Clinopodium dalmaticum Pharmacia 66(2): 49-52 The present work summarises preliminary results of an ethnobotanical study in the Rhodope Mountains. The aim was to assess the traditional home use of medicinal plants for herbal tea by local people and to estimate the threats to the Balkan endemic Clinopodium dalmaticum. Semi-structured interviews with local informants from 15 localities in Central and Eastern Rhodope Mountains were performed in 2015 and 2018. As a result, the most used plant species were listed. The major source of plants was recorded as being gathered from the wild. The plants, known with the local names “wild mint” and “white mint”, were identified as Clinopodium dalmaticum from dried specimens presented by informants in Central Rhodopes. A frequent collection from wild populations of C. dalmaticum in Central Rhodope Mts. (Smoljan region) was revealed along with just a few cases of cultivation close to the studied sites. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35139 https://doi.org/10.3897/pharmacia.66.e35139 https://pharmacia.pensoft.net/article/35139/ https://pharmacia.pensoft.net/article/35139/download/pdf/ en

10.3897/pharmacia.66.e35023 2019-07-09 pharmacia

Analysis of diosgenin and phenol compounds in Tribulus terrestris L. Burda,Nadiia Zhuravel,Iryna Dababneh,Moeen F. Fedchenkova,Yulia caltrop herb TLC densitometry Pharmacia 66(2): 41-44 Caltrop (Tribulus terrestris L.) is a weed plant widely growing in warm climate. The crude caltrop has multidirectional pharmacological action favorable for the development of drug preparations. As in European countries caltrop is a non-officinal plant, it seems feasible to develop raw material standardization parameters for creation of novel drugs. In the course of thin layer chromatography research the following compounds were identified in caltrop herb purveyed during the fruiting season: rutin, chlorogenic acid, caffeic acid, diosgenin. Diosgenin content in this raw material was determined by densitometry to be min. 0,11%. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35023 https://doi.org/10.3897/pharmacia.66.e35023 https://pharmacia.pensoft.net/article/35023/ https://pharmacia.pensoft.net/article/35023/download/pdf/ en

10.3897/pharmacia.66.e35132 2019-07-09 pharmacia

Process optimization of preparation of pentoxifylline – extended release tablets Tzankov,Stanislav Tzankov,Borislav pentoxifylline tablets swelling index dissolution profiles Pharmacia 66(2): 45-48 The possibilities for correction of the rate of drug release by minimal changes in the technology process and by maintaining the quantitative and qualitative composition of the product pentoxifylline – extended release tablets were explored. Correction was made by addition of different quantity of HPMC (4000 cPs) to a granulating solution of PEG 6000. The main characteristics of the granules (compressibility index and density) were established. The swelling of the hydrogel tablets in water was determined in order more information on the release process to be obtained. Dissolution profiles of produced tablets were determined. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35132 https://doi.org/10.3897/pharmacia.66.e35132 https://pharmacia.pensoft.net/article/35132/ https://pharmacia.pensoft.net/article/35132/download/pdf/ en

10.3897/pharmacia.66.e35279 2019-07-09 pharmacia

Organisational and economic characteristics of the baby food products market in Ukraine and EU countries Krychkovska,Aelita Zayarnyuk,Nataliya Lobur,Ivanna Khomenko,Olena Lopatynska,Oksana Hubytska,,Iryna Novikov,Volodymyr nutrition support neonatal period infant nutrition baby food market Pharmacia 66(2): 59-65 This article presents the results of the study of problematic issues of organisational-and-economic character concerning the provision of children with baby food products in Ukraine and European Union countries. It is established that the marketing feature of baby food products in Ukraine is its sales from pharmacies. It has been proved that the cost of baby food products in EU countries and in Ukraine have no price gradation depending on the degree of economic development of the country. The dynamics of development of the Ukrainian market of baby food products, as well as the dynamics of the cost of baby food products in Ukraine, depending on their dispensing place, have been analysed. It is established that the cost of baby food products is somewhat lower in pharmacies. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35279 https://doi.org/10.3897/pharmacia.66.e35279 https://pharmacia.pensoft.net/article/35279/ https://pharmacia.pensoft.net/article/35279/download/pdf/ en

10.3897/pharmacia.66.e35162 2019-07-09 pharmacia

Predicting the outcomes and costs for a cohort of 426 patients with Chronic Obstructive Pulmonary Disease (COPD) in Bulgaria through a Markov model Tachkov,Konstantin Mitov,Konstantin Savova,Alexandra COPD Markov Model Pharmacotherapy Cost-effectiveness Pharmacia 66(2): 53-57 The aim was to estimate the economic burden, as well as rate of progression of COPD for a cohort of 426 patients for a 10-year period. A total of 426 patients from 19 regions with Chronic Obstructive Pulmonary Disease were enrolled in a representative, ambispective, national study for Bulgaria. Patients were recorded on disease stage, occupation, smoking habits and medication. Cost of treatment was calculated and a 10-year one-way Markov model was used by employing transition probabilities and quality of life data from available literature. Costs and outcomes were recorded and a cost-effectiveness acceptability curve (CEAC) was established. Out of all patients included in the study 288 were non-smokers with a mortality percentage after 10 years of 42.7%. Smokers showed faster transition rate with 139 of them transitioning to more severe states and mortality was 54.6%. The incremental cost-effectiveness ratio (ICER) was 863.75 BGN. Patients who smoked had a lower quality of life – cumulatively for the 10-year period QALY = 623.51 for smokers vs. 1557.51 for non-smokers, but also lower costs for treatment (538 007.52 BGN vs. 1 344 757.95 BGN) accounted by the high transition rate and mortality amongst that group. Relatively few non-smokers transitioned from a less severe to a more severe state (6%), while most of the very severe stage patients experienced a lethal outcome within 10 years (81%). Despite the higher costs associated with the disease, the Quality of Life and lower transition probability would enable patients to live a normal life. The ICER was well below the WHO threshold. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35162 https://doi.org/10.3897/pharmacia.66.e35162 https://pharmacia.pensoft.net/article/35162/ https://pharmacia.pensoft.net/article/35162/download/pdf/ en

10.3897/pharmacia.66.e36530 2019-07-23 pharmacia

Evaluation of the current status of the value-added pharmacy services and pharmacists’ attitude in Bulgaria Balkanski,Stefan Simeonova,Joana Gitev,Ivan Getov,Ilko Value-added pharmacy services pharmacists community pharmacy patient benefits Pharmacia 66(2): 79-83 Value-added pharmacy services (VAPS) are additional services to the traditional pharmacy activities, which do not include dispensing of medicinal products and professional consultation. Over 51% of the community pharmacies in Bulgaria offer VAPS but mainly measuring of blood pressure (67.4%) and blood glucose (12.9%). About 60% of community pharmacists in the country are willing to perform other VAPS. About 70% of them believe that patients would rate VAPS as useful. Younger pharmacists with professional experience less than 5 years (90.9%) tend to believe that VAPS would be positively rated by their patients. The study shows that VAPS different from consultation and dispensing of medicinal products have a potential for development in the community pharmacies in Bulgaria. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e36530 https://doi.org/10.3897/pharmacia.66.e36530 https://pharmacia.pensoft.net/article/36530/ https://pharmacia.pensoft.net/article/36530/download/pdf/ en

10.3897/pharmacia.66.e35976 2019-07-23 pharmacia

4-aminopyridine – the new old drug for the treatment of neurodegenerative diseases Kostadinova,Ivanka Danchev,Nikolai 4-aminopyridine multiple sclerosis neurodegenerative diseases Pharmacia 66(2): 67-74 In this review are described the preclinical and clinical pharmacological data as well as new therapeutic indications for the use of 4-aminopyridine. 4-aminopyridine is a potassium (K+) channel blocker that has a long history and various application areas. It is a chemical agent developed in 1963 as a bird poison. The first approval for clinical application of 4-aminopyridine was in 70’s in Bulgaria, since anesthetists in that country have confirmed its effect as reversal agent for nondepolarizing myorelaxants. The Bulgarian pharmaceutical company Sopharma commersialized 4-aminopyridine under the trade name Pymadin. Since then 4-aminopyridine was extensively studied and in 2010 is approved in the USA for the treatment of walking disabilities in patients with multiple sclerosis. In recent years, data from clinical trials indicated that K-channel blockade may prove to be an appropriate strategy to overcome disturbances in nerve impulses conduction associated with demyelination of the central nervous system. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35976 https://doi.org/10.3897/pharmacia.66.e35976 https://pharmacia.pensoft.net/article/35976/ https://pharmacia.pensoft.net/article/35976/download/pdf/ en

10.3897/pharmacia.66.e36143 2019-07-23 pharmacia

Kinesitherapeutic behaviour in conservative treatment of coxarthrosis – case report Becheva,Maria Petrova,Gergana Kirkova-Bogdanova,Angelina Atanasov,Petar coxarthrosis functional deficiency kinesitherapy Pharmacia 66(2): 75-77 Hip arthrosis is the main cause of disability of all degenerative joint diseases and therefore it is considered to be of social significance. The presented clinical case aims to confirm the efficacy of the applied kinesitherapeutic program in conservative treatment of 62-year-old patient with right-sided coxarthrosis. The kinesitherapeutic methods included right lower limb massage, suspension therapy, tractions and manual movements of the right hip joint, positional treatment, active exercisesinan openkinetic chain, postisometric relaxation and stretching for shortened muscles. The pain symptoms were reduced, the volume of movement in the right hip increased, the strength of the right hip joint stabilizer muscles partially improved. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e36143 https://doi.org/10.3897/pharmacia.66.e36143 https://pharmacia.pensoft.net/article/36143/ https://pharmacia.pensoft.net/article/36143/download/pdf/ en

10.3897/pharmacia.66.e37035 2019-10-10 pharmacia

Toxicity of cyanobacteria. Organotropy of cyanotoxins and toxicodynamics of cyanotoxins by species Ilieva,Viktoria Kondeva-Burdina,Magdalena Georgieva,Tzveta Pavlova,Vera cyanobacteria mechanism of action toxicity Pharmacia 66(3): 91-97 As a result of blooming, some cyanobacteria (Microcystis, Anabaena, Planktothrix, etc.) produce toxins at concentrations that are high enough to poison and even kill animals and humans. According to Annex II of the Framework Directive 2000/60/EC, transformed into the Bulgarian legislation, for the characterization of surface water, at this stage, there are no acceptable limit values for cyanotoxins. Cyanotoxins include some of the strongest natural poisons, including those that could cause rapid death due to respiratory failure. The aim of this publication is an overview of toxic cyanobacteria and toxicity mechanisms. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Review Article text/html info:doi:10.3897/pharmacia.66.e37035 https://doi.org/10.3897/pharmacia.66.e37035 https://pharmacia.pensoft.net/article/37035/ https://pharmacia.pensoft.net/article/37035/download/pdf/ en

10.3897/pharmacia.66.e37263 2019-10-10 pharmacia

Synthesis and preliminary hepatotoxicity evaluation of new caffeine-8-(2-thio)-propanoic hydrazid-hydrazone derivatives Mitkov,Javor Kondeva-Burdina,Magdalena Zlatkov,Alexander caffeine isolated rat liver microsomes pro-oxidant effects Pharmacia 66(3): 99-106 New series of caffeine-8-(2-thio)-propanoic hydrazid-hydrazone derivatives were designed and synthesized. The targed compounds were obtained in yields of 51 to 96% and their structures were elucidated by FTIR, 1H NMR, 13C NMR, MS and microanalyses. All of the compounds were found to be “drug-like” as they fulfill the criteria of drug-likeness, which includes the MDDR-like rule. The tested compounds were subjected to in silico prediction of substrate/metabolite specificity and Drug Induced Liver Injury (DILI). The prediction for indicated that the evaluated compounds would most probably act as CYP1A2 substrates. The performed in vitro studies didn’t reveal statistically significant hepatotoxicity of the tested compounds, probably due to the pro-oxidant effects expressed on sub-cellular (isolated rat liver microsomes) level. The obtained experimental results confirmed the predicted low hepatotoxicity for the tested structures. Based on these results the compounds may be considered as promising structures for design of future molecules with low hepatotoxicity. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e37263 https://doi.org/10.3897/pharmacia.66.e37263 https://pharmacia.pensoft.net/article/37263/ https://pharmacia.pensoft.net/article/37263/download/pdf/ en

10.3897/pharmacia.66.e35880 2019-10-10 pharmacia

Analysis of good distribution practice inspection deficiency data of pharmaceutical wholesalers in Bulgaria Stoimenova,Assena Kirilov,Bogdan Zaykova,Krassimira Good Distribution Practice (GDP) medicinal products non-conformities deficiencies supply chain compliance Bulgarian Drug Agency Pharmacia 66(3): 85-89 The current study analyses the regulatory inspection findings of the wholesalers in Bulgaria in 2017 and compares the results with the findings from some other EU member-states. In total, 48 GDP inspections were performed in 2017. 50% of the inspections were performed in relation with issuing an authorization for wholesale of medicines, the rest half were related to changes in already granted authorizations. During the inspections, 17 non-conformities (NCs) have been documented. The NCs were identified in 3 wholesalers and 6 deficiencies were classified as major. No critical deficiencies were found. NCs were found in 6.25% of the inspected companies. No critical NCs were identified and only 6 NCs were classified as major which demonstrated high level of compliance of distributions sites in Bulgaria with the requirements of GDP. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35880 https://doi.org/10.3897/pharmacia.66.e35880 https://pharmacia.pensoft.net/article/35880/ https://pharmacia.pensoft.net/article/35880/download/pdf/ en

10.3897/pharmacia.66.e38573 2019-10-10 pharmacia

Caffeic acid phenethyl ester (CAPE): pharmacodynamics and potential for therapeutic application Yordanov,Yordan Pharmacology therapeutic application selective inhibitor of nuclear export NF-κB activation inhibition Pharmacia 66(3): 107-114 Caffeic acid phenethyl ester (CAPE) is the major pharmacologically-active component of some propolis types, rich in polyphenols, such as poplar propolis types. CAPE has the potential to be applied as a pharmaceutical as it possesses most of the pharmacological activities of propolis, such as anti-proliferative, antioxidant, immunomodulatory, antidiabetic, anti-inflammatory and antimicrobial. Its advantage is that it lacks some of the downsides of total propolis extracts, such as inability for unified standardization, which is cornerstone for implementing its therapeutic potential as a drug. The current paper provides an overview on the pharmacodynamic principles of CAPE. We present literature search outcomes form ClinicalTrials.gov database and from scientific publications, available on Scopus and Crossref databases. We take a round view of CAPE’s potential therapeutic implications in light of approved drugs with related modes of action. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Review Article text/html info:doi:10.3897/pharmacia.66.e38573 https://doi.org/10.3897/pharmacia.66.e38573 https://pharmacia.pensoft.net/article/38573/ https://pharmacia.pensoft.net/article/38573/download/pdf/ en

10.3897/pharmacia.66.e35969 2019-11-07 pharmacia

Spectral characteristics of 5-hydroxymethylfurfural as a related substance in medicinal products containing glucose Hudz,Nataliia leontiev,Dmytro Wieczorek,Piotr P. 5-hydroxymethylfurfural spectrophotometric method molar absorption coefficient medicinal products containing glucose Pharmacia 66(3): 121-125 Objectives: To study 5-hydroxymethylfurfural (5-HMF) spectral characteristics aiming at their future application in analytical procedures and their validation for the determination of 5-HMF in liquid products containing glucose after sterilization. Method: Direct spectrophotometric method for the determination of 5-HMF using the molar absorption coefficient at the absorption maximum (284 nm). Results and discussion: aqueous 5-HMF solutions have strong absorption in the ultraviolet range below 310 nm and give two absorption maxima at wavelengths of 229–230 nm and 284 nm. An excellent linear relationship between absorbance and 5-HMF concentration was observed in the concentration range of 2.0–10.0 mg/l. The linear dependence passes through the origin. The molar absorption coefficients of 5-HMF were determined and found to be 3007 mol−1•L•cm−1at 229–230 nm and 16070 mol−1•L•cm−1at 284 nm. The use of the molar absorption coefficient of 5-HMF stated in the Pharmacopeia of the United States of America for determining 5-HMF in polydextrose (16830 mol−1·L·cm−1at 283 nm) gives recovery results for model solutions of reference substance of 5-HMF that are acceptable from the point of view of the requirements of the State Pharmacopeia of Ukraine for methods of quantitative determination of impurities. However, other values of the molar absorption coefficient (17000 and 22700 mol−1•L•cm−1) given in the scientific publications are unsuitable for the quantitative determination of 5-HMF as an impurity in medicinal products. Conclusion: The molar absorption coefficient (16830 mol−1•L•cm−1at 284 nm) may be used to quantify 5-HMF as an impurity in medicinal products containing glucose. For a specific medicinal product, a full validation of the analytical procedure of the 5-HMF determination is required taking into account the composition of this product. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Short Communication text/html info:doi:10.3897/pharmacia.66.e35969 https://doi.org/10.3897/pharmacia.66.e35969 https://pharmacia.pensoft.net/article/35969/ https://pharmacia.pensoft.net/article/35969/download/pdf/ en

10.3897/pharmacia.66.e37954 2019-11-07 pharmacia

Phytotherapeutic approaches to treatment and prophylaxis in pediatric practice Petkova,Valentina Hadzhieva,Bozhidarka Nedialkov,Paraskev phytotherapeutic alternative medicines pediatric medicinal plants Pharmacia 66(3): 115-119 Medicinal plants, their extracts and herbal medicinal products occupy a growing share of medicines in the pharmacy worldwide. Historically, the first medicines were products of plants, as well as some of the most important medicines still in use today. With the development of phytochemistry, as part of the pharmaceutical science, great progress has been made in the isolation and in determining the value of a number of biologically active substances (BAS). Many plants have yielded pure substances (or natural products) that are applied in modern medical practice. Other compounds are potentially useful or have toxic effects. Traditional medicine incorporating many herbal medicines remains an important (and in some cases, the only) form of treatment in some countries, with increasing use in medical practice. On the other hand, the fact that in pediatric patients there is a limitation, mainly moral and ethical, of the number of medications to be administered due to the difficulty of conducting clinical trials in children, stimulates the use of herbal medicines of proven quality, effectiveness and safety among this group of patients. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e37954 https://doi.org/10.3897/pharmacia.66.e37954 https://pharmacia.pensoft.net/article/37954/ https://pharmacia.pensoft.net/article/37954/download/pdf/ en

10.3897/pharmacia.66.e47035 2019-11-12 pharmacia

Development and validation of RP-HPLC method for stability evaluation of model hydrazone, containing a pyrrole ring Tzankova,Diana Peikova,Lily Vladimirova,Stanislava Georgieva,Maya pyrrole-hydrazide pyrrole-hydrazone stability RP-HPLC validation Pharmacia 66(3): 127-134 RP-HPLC method with UV detection was developed and validated for determination of the chemical stability and stability in close to physiological conditions of a model pyrrole hydrazone ethyl 5-(4-bromophenyl)-1-(1-(2-(4-hydroxy-3-methoxybenzylidene) hydrazineyl)-4-methyl-1-oxopentan-2-yl)-2-methyl-1H-pyrrole-3-carboxylate (D_5d), containing susceptible to hydrolysis hydrazone group. The evaluated substance was subjected to the influence of a variety of pH , representing the main physiological values of 37°C and corresponding pH values in the stomach (pH 2.0), blood (pH 7.4) and small intestine (pH 9.0). Chemical stability in a highly alkaline medium with a pH of 13.0 was also evaluated. The hydrazone I tested was found to be stable at pH 7.4 and pH 9.0 and 37 ° C and hydrolyzed under strong acidic (pH 2.0) and highly alkaline media (pH 13.0) and at the same temperature.The products of hydrolysis were identified to be the initial hydrazide and aldehyde, pointing the hydrazone group as most liable. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e47035 https://doi.org/10.3897/pharmacia.66.e47035 https://pharmacia.pensoft.net/article/47035/ https://pharmacia.pensoft.net/article/47035/download/pdf/ en

10.3897/pharmacia.66.e35075 2019-11-26 pharmacia

Public opinion study on the role of advertising in choice of non-prescription drugs for self-treatment Ryvak,Tetiana Denysiuk,Oksana drug advertising non-prescription drugs self-treatment questionnaire survey Pharmacia 66(3): 135-140 An assessment of the opinion of a certain cohort of the population on the role of drug advertising in the choice of non-prescription drugs for self-treatment was conducted. According to the questionnaire survey, it has been established that advertising affects the choice of drug for self-treatment 26.0% of the polled. Despite the fact that the majority of respondents indicate that there is no influence of drug advertising, 62.8% of them buy self-medication drug sabout which they learned from advertising. Thus, our scientific hypothesis about the presence of the direct influence of drug advertising on the commitment of patients to pharmacotherapy is confirmed. The majority of respondents (90.0%) do not consider advertising of drugs to be effective and safe, and 61.0% say that drug advertising contains contradictory and incomprehensible information. Almost all respondents (88.0%) are convinced that drug advertising is not always objective and fair. At the same time, according to 50.0% of respondents, the volume of drug advertising in Ukraine should be reduced, 22.0% of respondents believe that advertising of drugs should be prohibited. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35075 https://doi.org/10.3897/pharmacia.66.e35075 https://pharmacia.pensoft.net/article/35075/ https://pharmacia.pensoft.net/article/35075/download/pdf/ en

10.3897/pharmacia.66.e37739 2019-12-19 pharmacia

Nanomaterials for cancer medication: from individual nanoparticles toward nanomachines and nanorobots Loukanov,Alexandre Nikolova,Svetla Filipov,Chavdar Nakabayashi,Seiichiro Drug delivery nanosystems targeted nanotherapy nanomachines personalized nanomedicine Pharmacia 66(3): 147-156 The nanomaterials for cancer medication are already reality providing a wide range of new tools and possibilities, from earlier diagnostics and improved imaging to better, more efficient, and more targeted anticancer therapies. The purpose of this critical review is to focus on the current use of clinically approved nanoparticles for cancer theranostic, nanovaccines and delivery platforms for gene therapy. These include inorganic, metal and polymer nanoparticles, nanocrystals and varieties of drug delivery nanosystems (micelles, liposomes, microcapsules and etc.). The recent progress in cancer nanomedicine enables to combine the benefits of individual nanoparticles with biomolecules into a multifunction nanomachines and even highly advanced nanorobots for targeted therapies. Nowadays clinical trials with advanced anticancer nanomachines provide potential for more accurately and effective identification and destruction of the cancer cells present in the human body. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Review Article text/html info:doi:10.3897/pharmacia.66.e37739 https://doi.org/10.3897/pharmacia.66.e37739 https://pharmacia.pensoft.net/article/37739/ https://pharmacia.pensoft.net/article/37739/download/pdf/ en

10.3897/pharmacia.66.e38137 2019-12-19 pharmacia

Synthesis and anticonvulsant activity of 6-methyl-2-((2-oxo-2-arylethyl)thio)pyrimidin-4(3 H)-one derivatives and products of their cyclization Severina,Hanna I. Skupa,Olga O. Voloshchuk,Natalya I. Suleiman,Marharyta M. Georgiyants,Victoriya A. synthesis pyrimidine thiazolopyrimidine anticonvulsant activity Pharmacia 66(3): 141-146 The alkylation of 6-methyl-2-thioxo-2,3-dihydro-1H-pyrimidine-4-one phenacyl bromides under different conditions was investigated. It was found that during the reaction in the medium of DMF/K2CO3 a mixture of 2-(2-aryl-2-oxoethyl)thio-6-methyl-pyrimidine-4(3H)-one and 3-hydroxy-3-aryl-7-methyl-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-5-one was formed. The holding of the resulting mixture in the concentrated sulphuric acid leads to the formation of cyclization products - derivatives of 3-aryl-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one with high yields. Individual S-alkylated derivatives – 2-(2-aryl-2-oxoethyl)thio-6-methyl-pyrimidine-4(3H)-one - were obtained by reacting in methanol in the presence of sodium methoxide. Pharmacological screening of synthesized compounds for anticonvulsant activity on the model of pentylenetetrazole seizures in rats was carried out and some regularity “structure-activity” was established. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e38137 https://doi.org/10.3897/pharmacia.66.e38137 https://pharmacia.pensoft.net/article/38137/ https://pharmacia.pensoft.net/article/38137/download/pdf/ en

10.3897/pharmacia.66.e35186 2019-12-19 pharmacia

Clinical and economic estimation of children’s pharmacotherapy with meningococcial infections in Ukraine Bilyk,Iryna Fedyak,Iryna Ivaniulyk,Iryna Havryshchuk,Liubomyr ABC-analysis children frequency analysis meningococcal disease VEN-analysis Pharmacia 66(3): 157-160 A comprehensive study for assessment the appointments rationality for children with meningococcal infectious (MI) in Ukraine in real clinical practice has been conducted. The doctor’s appointment sheets from 184 inpatients medical cards have been processed by the integral ABC / VEN / frequency analysis. In average, children were in the hospital (14±7) bed-days, they were granted 2908 appointments of 191 drugs by the INN. It has been established that medicine for MI etiotropic therapy took the third place in the appointments frequency. At the same time, the ABC / VEN-analysis results revealed a rational approach to pharmacotherapy.The total treatment cost was estimated at USD 25,173.59 (for one child – USD 136.81).Since currently in Ukraine inpatient children treatment is mainly provided by parents, further medical prescriptions improvement is needed in order to increase the efficiency and minimize the childrenMI therapy cost. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35186 https://doi.org/10.3897/pharmacia.66.e35186 https://pharmacia.pensoft.net/article/35186/ https://pharmacia.pensoft.net/article/35186/download/pdf/ en

10.3897/pharmacia.66.e36620 2019-12-31 pharmacia

Analysis of primary outpatient data for off-label use of medicines in neurology Drenska,Maria Elitova,Savina Grigorova,Velina Naseva,Emilia Getov,Ilko off-label use neurology pharmacovigilance Pharmacia 66(4): 165-170 Introduction: The off-label use of medicines is a common practice that covers a wide range of therapeutic areas in both, adults and children. So far, the extent of off-label use among neurology patients in Bulgaria has not been studied. The aim of this study is to provide data on the off-label use in neurology patients in Bulgaria and to contribute to planning actions by the European Commission and EMA to provide a harmonized guideline and to regulate the off-label use of medicines within the European Union. Materials and methods: The data on prescriptions of 360 neurology outpatients, treated in a 1 – year period, were recorded and provided for analyses. The Summaries of Product Characteristics, were used as reference documents for assessment of prescriptions. Results: The results from this study show that most neurology patients (63%) were exposed to off-label use. Most of the medicines prescribed off-label (90%), were used for a therapeutic indication, other than the one listed in the authorized product information. Meloxicam is found to be the most commonly prescribed off-label medicine. Other medicines, like trasadone, pentoxyfylline and fupentixol / melitracen were prescribed less frequently, but deserve special attention, as they were found to be used off-label to a very large extent, some of them in 100% of prescriptions. Half of the top 10 medications, most commonly used off-label in neurology, were found to be non-steroidal anti-inflammatory drugs. Conclusion: The results reveal a big gap between the authorized medicines and the real medical needs. Further studies based on a larger number of medical centers are needed to establish more accurate data on off-label prescribing in neurology patients on a national level. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e36620 https://doi.org/10.3897/pharmacia.66.e36620 https://pharmacia.pensoft.net/article/36620/ https://pharmacia.pensoft.net/article/36620/download/pdf/ en

10.3897/pharmacia.66.e46687 2019-12-31 pharmacia

The knowledge and experience with the off-label use – results of a survey Drenska,Maria Naseva,Emilia Getov,Ilko off-label pharmacovigilance survey Pharmacia 66(4): 217-221 Introduction: The aim of this survey is to assess the current knowledge and experience of medical doctors in regard to off-label use and to determine whether it is legal, according to them, as the local current legislation on medicinal products does neither prohibit nor explicitly permit such use. Materials and methods: One hundred medical doctors from inpatient and outpatient medical care participated and answered 10 questions. The inclusion criteria were to have a degree in medicine and right to prescribe medications. Statistical analysis was performed using the SPSS v19.0 statistical program. Results: The results show that 8 out of 10 medical doctors have knowledge in regard to the meaning of the term “off-label”. More than half (62%) stated they have prescribed off-label medicine in their medical practice. Half of the respondents (49%) experienced some kind of trouble when prescribing off-label. In regard to whether the law allows this practice, opinions were divided. To a larger extent (88%), medical doctors support the introduction of clearer rules for off-label use in Bulgaria. Conclusion: Edical doctors have significant knowledge about off-label use, but feel uncertainty in their actions when they use medicines off-label. It is necessary to consider regulating this use at a national level, following the good examples of other European Union (EU) member states, until a harmonized solution within EU is found. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e46687 https://doi.org/10.3897/pharmacia.66.e46687 https://pharmacia.pensoft.net/article/46687/ https://pharmacia.pensoft.net/article/46687/download/pdf/ en

10.3897/pharmacia.66.e38571 2019-12-31 pharmacia

Caffeic acid phenethyl ester (CAPE): cornerstone pharmacological studies and drug delivery systems Yordanov,Yordan Caffeic acid phenethyl ester propolis pharmacological properties drug delivery systems Pharmacia 66(4): 223-231 Propolis is a natural product with a plethora of biological effects, utilized by traditional medicine since antiquity. However, its application as a pharmaceutical is hindered by its variable composition and difficult standardization. CAPE has been shown to be a major component of propolis, with a large contribution to its pharmacological effects, among which the anti-inflammatory, antioxidant and antineoplastic have been attracting most attention. The current review article aims to present the cornerstone pharmacological studies of CAPE throughout the years, following its discovery, which confirmed its primary importance among propolis constituents and opened the path to its intensive research as a potential pharmaceutical. We present the diversity of drug delivery systems of CAPE, which have been developed to improve its efficacy in in vitro and in vivo disease models and discuss their primary promises and weaknesses. The increased interest in recent years over more practical approaches of CAPE research such as its pharmaceutical formulation comes to show that it has a potential to become commercialized as a pharmaceutical. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Review Article text/html info:doi:10.3897/pharmacia.66.e38571 https://doi.org/10.3897/pharmacia.66.e38571 https://pharmacia.pensoft.net/article/38571/ https://pharmacia.pensoft.net/article/38571/download/pdf/ en

10.3897/pharmacia.66.e37706 2019-12-31 pharmacia

Clinical pharmacy in Ukraine according to the healthcare professionals’ assessment Zimenkovsky,Andriy Nastyukha,Yuliya Kostyana,Kateryna Devinyak,Oleg Zayats,Marta Koval,Andriy Denysiuk,Oksana Gorodnycha,Oksana Siatynia,Vitaliy clinical pharmacy clinical pharmacist healthcare professionals’ opinion Ukraine Pharmacia 66(4): 193-200 An anonymous questionnaire survey among healthcare professionals in Ukraine (n = 10737) showed contradictions in the attitude to the peculiarities of clinical pharmacy compared to a general pharmacy, the relation to the specialists who provide clinical pharmacy services, and the healthcare settings for them. The respondents considered the activity of clinical pharmacist necessary in 74.2%. The community pharmacies were identified as prior professional settings for clinical pharmacists in 55.3%; hospitals – 47.7%, hospital pharmacies – 45.0%. Among the directions of the clinical pharmacist’s activity at the hospital, monitoring of drug safety and efficacy was stated by 69.9%, provision of the pharmaceutical care – 50.5%, evaluation of pharmacotherapy – 42.1%, processing of the local drug formulary – 26.8%. The respondents saw prospects for the development of clinical pharmacy in Ukraine in 54.2%. Therefore, there were differences in views on the key issues of clinical pharmacy throughout Ukraine and the insufficient support for its prospects. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e37706 https://doi.org/10.3897/pharmacia.66.e37706 https://pharmacia.pensoft.net/article/37706/ https://pharmacia.pensoft.net/article/37706/download/pdf/ en

10.3897/pharmacia.66.e36808 2019-12-31 pharmacia

Search for angiotensin II receptor antagonists among 4-aryl-n-(aryl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imine derivatives Drapak,Iryna Zimenkovsky,Borys Perekhoda,Lina Suleyman,Мargarita Yeromina,Hanna Skaletska,Natalia Seredynska,Natalya Demchenko,Anatolii synthesis 4-aryl-N-(aryl)-3-(prop-2-en-1-yl)-2 3-dihydro-1 3-thiazol-2-imine derivatives molecular docking angiotensin receptor ІІ antagonists Pharmacia 66(4): 181-186 The aim of study was to find potential antihypertensive and cardiotropic drugs among new 4-aryl-N-(aryl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imines. Materials and methods: The target compounds were synthesized by condensation asymmetrical substituted thioureas with α-bromo-4-R1-acetophenones in ethanol medium. The structure and purity of the compounds synthesized were confirmed by 1H, 13C NMR-spectroscopy and elemental analysis. Docking studies of synthesized compounds to the active site of angiotensin receptor ІІ (PDB ID: 3R8A) were performed in order to find its potential inhibitors and to select promising compounds for experimental screening. Pharmacological studies of the influence on the cardiovascular system were performed. Results: The results of docking studies indicate a high affinity of all tested substances to the selected biotarget. The thermodynamic probability of binding of synthesized substances to protein 3R8A was confirmed by negative values of scoring functions. Hydrobromide of 4-(4-methoxyphenyl)-N-phenyl-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imine 3(1) and hydrobrmide of 4-(4-methoxyphenyl)-N-(4-bromphenyl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imine 3(3), which have the highest negative values of scoring functions, are recommended for in vivo pharmacological studies. Based on a complete analysis of the geometric location of the synthesized compounds (ligands) in the active site of the angiotensin II receptor, it was found that the complexes are formed with the involvement of Nitrogen atom of imino group, the 1,3-thiazole ring, the phenyl and alkyl moieties of the molecule form hydrogen bonds, intermolecular electrostatic and donor-acceptor interactions. The conducted pharmacological studies of the influence on the cardiovascular system have allowed to confirm the presence of antihypertensive effect inherent in compounds of this series (except for compound 3(2)). The most effective antihypertensive effect, which is similar in duration and strength of the effect of valsartan, was the effect of compound 3(5). Conclusions: In order to expand the arsenal of biologically active substances of cardiotropic action a systematic series of new 4-aryl-N-(aryl)-3-(prop-2-en-1-yl)-2,3-dihydro-1,3-thiazol-2-imine derivatives were synthesized. The structure and purity of the compounds synthesized were confirmed by 1H, 13C NMR-spectroscopy and elemental analysis. Based on the results of docking studies using Autodock 4.2.6 software, selected compounds with the best affinity for protein biomes (PDB codes: 3R8A) are promising for experimental studies of hypotensive and cardiotropic activity. The most effective antihypertensive effect, which is similar in duration and strength of the effect of valsartan, was the effect of compound 3(5). A comparative analysis of the results of molecular docking and in vivo results suggests that there is a positive correlation between scoring protein inhibition and experimental data. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e36808 https://doi.org/10.3897/pharmacia.66.e36808 https://pharmacia.pensoft.net/article/36808/ https://pharmacia.pensoft.net/article/36808/download/pdf/ en

10.3897/pharmacia.66.e36764 2019-12-31 pharmacia

Antioxidant properties of some novel derivatives thiazolo[4,5-b] pyridine Chaban,Taras Ogurtsov,Volodymyr Mahlovanyy,Anatoliy Sukhodolska,Natalia Chaban,Ihor Harkov,Stefan Matiychuk,Vasyl antioxidant activity 2 2 diphenyl-1-picrylhydrazyl synthesis thiazolo[4 5-b]pyridines Pharmacia 66(4): 171-180 The synthesis and determination of the antioxidant activity of some novel (5,7-dimethyl-2-oxo-thiazolo[4,5-b]pyridine-3-yl)-acetic acid hydrazide derivatives are described in this article. The transformation of the base heterocycle was carried out via the reactions of acylation, [2+3]cyclocondensation, Knoevenagel condencation and alkylation for the purpose to obtain substances with a satisfactory pharmacological profile. Antioxidant activity of the synthesized compounds was evaluated in vitro by means of the scavenging metod effect on 2,2 diphenyl-1-picrylhydrazyl (DPPH) radicals. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e36764 https://doi.org/10.3897/pharmacia.66.e36764 https://pharmacia.pensoft.net/article/36764/ https://pharmacia.pensoft.net/article/36764/download/pdf/ en

10.3897/pharmacia.66.e38976 2019-12-31 pharmacia

Application of the Folin-Ciocalteu method to the evaluation of Salvia sclarea extracts Hudz,Nataliia Yezerska,Oksana Shanaida,Mariia Pervaiz,Roomna Wieczorek,Piotr P. Salvia sclarea herb extract Folin-Ciocalteu reagent total phenolic content Pharmacia 66(4): 209-215 Polyphenols are valuable group of phytoconstituents due to their high antioxidant activity and healing properties. Antioxidant properties of sages are attributed mainly to a high level of phenolic compounds. The aim of the present study was to elaborate an analytical procedure for the evaluation of the content of secondary metabolites of the polyphenol nature in the herb of Clary Sage (Salvia sclarea L.). Four crude extracts of Salvia sclarea herb obtained with different technologies were used to develop an analytical procedure for the total phenolic content (TPC) assay by spectrophotometric method. The optimum conditions for the analysis (time of the reaction, wavelength, and reference substances) were chosen and experimentally justified (60–80 min, 760 nm, gallic acid and rutin, respectively). Under these conditions, the developed analytical procedure is robust in the indicated time and easy for performing in phytochemical or technological laboratories. The yield of TPC from the herb of Salvia sclarea was the highest in the extracts prepared by heating at a temperature of 36–46 °C and with using the ultrasonic bath. TPC was the highest in the extract in which solvent-to-herb ratio was the least (10:1) and particle size was in the range of 2–5 mm. As a result of the studies, the analytical procedure of the determination of TPC was developed and its parameters were justified. This methodology complies with the requirements for pharmaceutical analysis to ensure the reliability of results during pharmaceutical development and routine control of Salvia sclarea extracts. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e38976 https://doi.org/10.3897/pharmacia.66.e38976 https://pharmacia.pensoft.net/article/38976/ https://pharmacia.pensoft.net/article/38976/download/pdf/ en

10.3897/pharmacia.66.e37893 2019-12-31 pharmacia

Fatty acid composition of vegetable marrows and zucchini leaves Iosypenko,Olena Zhuravel,Iryna Omelchenko,Zinaida Burlaka,Iryna vegetable marrows zucchini leaves GC/MS fatty acids indices: atherogenicity thrombogenicity and health Pharmacia 66(4): 201-207 The qualitative composition and quantitative content of fatty acids in leaves of vegetable marrows (Cucurbita pepo L. var. giromontina Alef.), zucchini (Cucurbita pepo L. var. cylindrica Paris) yellow- and green-fruits varieties were determined by using GC/MS. 14 fatty acids were identified as the result of the experiment. Unsaturated fatty acids were found to be dominated in the raw plant material. The total content of unsaturated fatty acids amounted to 60.47% in vegetable marrows leaves, 64.35% yellow zucchini leaves and 68.85% green zucchini leaves, among which linoleic and linolenic acid dominated. The related health lipid indices (IA, atherogenicity, IT, thrombogenicity and IH, health) were determined. It is shown that the use of such biological resources is actual and expedient for the purpose of alimentary correction of the physiological condition of a person. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e37893 https://doi.org/10.3897/pharmacia.66.e37893 https://pharmacia.pensoft.net/article/37893/ https://pharmacia.pensoft.net/article/37893/download/pdf/ en

10.3897/pharmacia.66.e35194 2019-12-31 pharmacia

HPLC determination of phenolic compounds content in Parmelia sulcata and Parmelia vagans thalli Kyslychenko,Aleksandra Процкая,Viktoriia Zhuravel,Iryna HPLC lichen lichen acids Parmelia sulcata Parmelia vagans phenolic compounds Pharmacia 66(4): 161-164 The species of Parmelia genus have long been used in Indian folk medicine for the treatment of bronchitis, ulcers, furunculosis, cardiovascular diseases, urolithiasis, amenorrhea, and also at infectious and inflammatory diseases. In Ukraine, the most common lichens of the Parmelia genus are Parmelia sulcata Tailor and Parmelia vagans Nyl. At the same time, thalli of Parmelia genus lichens belong to the non-officinal and poorly studied types of raw material. The qualitative composition and the quantitative content of phenolic compounds in Parmelia sulcata and Parmelia vagans thalli was studied by HPLC. According to the results of the chromatographic analysis, salazinic, fumaroprotocetraric, usnic acids, chloratranorin and atranorin were identified in both types of raw material studied. In addition, protocetraric acid was identified in Parmelia sulcata thalli. According to the results of the experiment, the total content of identified phenolic compounds in Parmelia sulcata thalli was 2019.71±40.39 g/mol, and in Parmelia vagans thalli it comprised 1754.18±34.77 g/mol. In the thalli of both studied species of Parmelia genus, fumaroprotocetraric acid dominanted by the quantity. This substance was present in Parmelia sulcata thalli in the amount of 474.00±9.00 g/mol, and in Parmelia vagans thalli – 456.21±8.67 g/mol. In addition, a significant amount of chloratranorin (408.79±8.99 g/mol) was present in Parmelia sulcata thalli. Quite a high content of atranorin (393.34±8.65 g/mol) and usnic acid (375.31±7.53 g/mol) were defined in Parmelia vagans thalli. The results obtained can be used in the development of quality control methods for Parmelia sulcata and Parmelia vagans thalli, as well as medicines based on these types of raw materials. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e35194 https://doi.org/10.3897/pharmacia.66.e35194 https://pharmacia.pensoft.net/article/35194/ https://pharmacia.pensoft.net/article/35194/download/pdf/ en

10.3897/pharmacia.66.e37267 2019-12-31 pharmacia

Study of rheological behaviour of hydroxyethyl cellulose gels in the development of the composition and technology of the medicine with anti-inflammatory activity Postoy,Vladyslav Kukhtenko,Halina Kukhtenko Vyshnevska,Liliia Gladukh,Ievgenii Semchenko,Kateryna rheological paramets gel hydroxyethyl cellulose Pharmacia 66(4): 187-192 The aim of the research was to investigate the rheological behaviour of hydroxyethyl cellulose gels, which are used in the development of the composition and technology of the medicine with anti-inflammatory activity. The objects of research were hydroxyethyl cellulose gels in the concentration of 1.0%; 1.5%; 2.0%; 2.5% and 3.0%. Investigation of the rheological behavior of HEC gels (structural and mechanical properties) was performed using the Rheolab QC rheometer from Anton Paar (Austria) using the C-CC27 / SS Coaxial Cylinder System. The obtained results showed that excipients influence on the rheological behaviour in the following way: propylene glycol and polyethylene oxide 400 reduce rheoparameters, while PEG 40 hydrogenated castor oil increases these parameters. The further study of the rheological properties in comparison with medicines “Troxerutin” and “Thiotriazolinum” showed that the developed gel fully corresponds to technological and consumer requirements. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e37267 https://doi.org/10.3897/pharmacia.66.e37267 https://pharmacia.pensoft.net/article/37267/ https://pharmacia.pensoft.net/article/37267/download/pdf/ en

10.3897/pharmacia.66.e37997 2019-12-31 pharmacia

Neuroprotective and antioxidant activities of saponins’ mixture from Astragalus glycyphylloides in a model of 6-hydroxydopamine-induced oxidative stress on isolated rat brain synaptosomes Kondeva-Burdina,Magdalena Krasteva,Ilina Popov,Georgi Krasteva,Ilina Astragalus glycyphylloides saponins’ mixture synaptosomes neuroprotection antioxidant Pharmacia 66(4): 233-236 The aim of the study was to investigate the possible neuroprotective and antioxidant activity of purified saponins’mixture (PSM), isolated from Astragalus glycyphylloides (Fabaceae), in a model of 6-hydroxydipamine (6-OHDA)-induced oxidative stress on isolated rat brain synaptosomes. Synaptosomes were incubated with 3 different concentrations of PSM: 60 µg/mL; 6 µg/mL; 0.6 µg/mL. The effects of PSM were compared to those of silymarin (S), at the same concentrations. The main parameters, characterized functional and metabolic status of synaptosomes, were investigated: viability (MTT-test) and level of reduced glutathione (GSH). At isolated rat brain synaptosomes, in conditions of 6-OHDA-induced oxidative stress (150 μМ), PSM revealed statistically significant, concentration-dependent, neuroprotective and antioxidant effects, compared to those of silymarin. Effects were most prominent at concentration 60 µg/mL. These neuroprotective effects of PSM might be due to the possible activity as scavenger of reactive oxygen species (ROS), produced by p-quinone (toxic metabolite of 6-OHDA). info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2019 Research Article text/html info:doi:10.3897/pharmacia.66.e37997 https://doi.org/10.3897/pharmacia.66.e37997 https://pharmacia.pensoft.net/article/37997/ https://pharmacia.pensoft.net/article/37997/download/pdf/ en

10.3897/pharmacia.67.e37004 2020-05-13 pharmacia

HPLC method for simultaneous determination of impurities and degradation products in Cardiazol Drapak,Iryna Zimenkovsky,Borys Ivanauskas,Liudas Bezruk,Ivan Perekhoda,Lina Muzychenko,Volodymir Logoyda,Liliya Demchuk,Inna HPLC Cardiazol Impurities Degradation Products Pharmacia 67(1): 29-37 Aim. The aim of study was to develop a simple and accurate procedure that could be applied for the determination of impurities and degradation products in cardiazol. Materials and methods. Separation in samples was carried out with Acquity H-class UPLC system (Waters, Milford, USA) equipped with Acquity UPLC BEH C18 column (2.1 × 50 mm, 1.7 μm) (Waters, Milford, USA). Xevo TQD triple quadrupole mass spectrometer detector (Waters Millford, USA) was used to obtain MS/MS data. Mobile phase A: 0.1% solution of trifluoroacetic acid R in water R; Mobile phase B: acetonitrile R. Samples were chromatographed in gradient mode (Table 1). Flow rate of the mobile phase: 1 ml / min. Column temperature: 30 °С. Detection: at 240 nm wavelength. Injection volume: 10 μl. Results. The retention time of the main substance is about 18.5 minutes. The order of the peak, the retention times and relative retention times: impurity B (12.04, 0.65); impurity А (18.5; 0.98); Cardiazol (18.87; 1.00). The LOD and LOQ values obtained were in the range of 30 ng/mL to 100 ng/mL and 80 ng/mL to 310 ng/mL respectively (with respect to sample concentration of 2 mg/ml). Linearity was established in the range of LOQ level to 0.2% having regression coefficients in the range of 0.9996 to 0.9999. The change in the temperature of the column affects the degree of separation of cardiazol and the impurity A, and thus, with a decrease of 5 ° C, the degree of separation is (1.06), while with increasing this index (3.43). When changing the flow rate of the mobile phase, the degree of separation changes in the following order, with a decrease to 0.9 ml / min separation (1.90), with an increase in speed to 1.1 ml / min (2.45). When the number of mobile phase B decreases by 5%, the degree of separation varies by (2.65), with an increase of 5% (1.82). In comparison with the chromatogram of the tested solution, the substance is not resistant to the action of peroxide, alkaline and acid decomposition. Conclusion. 1) HPLC method was developed and validated for the simultaneous detection and quantitation of impurities formed during the synthesis of cardiazol. 2) The method proved to be sensitive, selective, precise, linear, accurate and stability-indicating. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e37004 https://doi.org/10.3897/pharmacia.67.e37004 https://pharmacia.pensoft.net/article/37004/ https://pharmacia.pensoft.net/article/37004/download/pdf/ en

10.3897/pharmacia.67.e36150 2020-05-13 pharmacia

Biochemical indexes of mineral metabolismin patients from the polluted regionaffected by chronic periodontitis Popovych,Zoryana Rozhko,Mykola Ostapyak,Iryna Oktysyuk,Yuriy biochemical indexes chronic periodontitis dental caries blood serum oral liquid Pharmacia 67(1): 23-28 To be living at the most advanced technological area in history is to exist and face pollution one of the most serious threats to all living things on the planet. It is a well known fact that industrial pollutions cause a considerable number of health problems and stomatological in particular. This article demonstrates the results of our study regarding investigation ofsome biochemical indexes in children and adults from the polluted area. We have examined 1236 scholars and 133 workers of Burstyn Thermoelectric Station. The findings suggest that the prevalence of stomatological disorders reaches up to 84,2–93,5% in all examined, the statistic shows also that 31,6 % of six year old children have decayed teeth, in 12 year old children this index is more than 76,8% and almost 92,3% in those aged15–17years. Symptoms of periodontal disorders were observed in 37,1–78,3% of children, the orthodontic pathology was diagnosed in 43,9–61,2% of all examined scholars. People that work at the Burstyn Thermoelectric Station are affected by periodontal pathology and demonstrated disordered mineral metabolism in the blood serum and oral liquid with decreased level of Calcium and increased amount of Phosphates. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e36150 https://doi.org/10.3897/pharmacia.67.e36150 https://pharmacia.pensoft.net/article/36150/ https://pharmacia.pensoft.net/article/36150/download/pdf/ en

10.3897/pharmacia.67.e35152 2020-05-13 pharmacia

Clinical study of the efficacy of si-containing polishing paste for the professional hygiene procedures in patients with periodontal disease Olha Ripetska,Olha Mahlovanyy,Anatoliy Hrynovets,Ihor Chaban,Taras Hrynovets,Volodymyr Buchkovska,Anna Harkov,Stefan Deneha,Ihor Pasko,Oksana Renka,Marta bleeding dental calculus dental plaque dental scaling generalized periodontitis Si-containing polishing paste Pharmacia 67(1): 17-22 Silicon-containing (Si-containing) polishing paste has been tested clinically in patients with chronic generalized periodontitis, I-st degree of severity. All patients have been examined for the presence of supra- and sub-gingival calculus and bleeding on probing on a six- month-testing time and within one year after conducting the professional hygienic procedures. It has been revealed that the proposed Si-containing polishing paste proved to be effective in the maintenance of gingival health in the lapse of time from 1 to 12 months after treatment. The majority of patients showed neither dental deposits nor bleeding on probing up in the interval from 1 to 12 months after dental scaling and polishing with Si-containing polishing paste. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e35152 https://doi.org/10.3897/pharmacia.67.e35152 https://pharmacia.pensoft.net/article/35152/ https://pharmacia.pensoft.net/article/35152/download/pdf/ en

10.3897/pharmacia.67.e35147 2020-05-13 pharmacia

Combination of general and local action drugs in treatment of patients with generalized periodontitis on the basis of the pathology of the hepatobilary system Furdychko,Anastasiya Buchkovska,Anna Petryshyn,Olga Hrynovets,Volodymyr Chaban,Taras Hrynovets,Ihor Harkov,Stefan Chaban,Ihor hepatobiliary pathology hepatoprotector prebiotic periodontitis thiotriazolin Pharmacia 67(1): 13-16 The pathology of the hepatobiliary system significantly affects the state of the organs of the oral cavity. A clinical and index study of the state of periodontal tissues in 122 patients was conducted, which showed the prevalence of periodontal disease in patients with chronic acalculous cholecystitis. The examined patients were divided into groups depending on the treatment method, and the result was evaluated before treatment, directly after treatment and 6 months following treatment. Antidysbiotic hepatoprotector and 2% thiotriazolin ointment were included in the combination therapy. Studies have shown that patients with hepatobiliary pathology have increased likelihood of periodontal diseases, and after treatment, periodontal indicators and the hygiene index are significantly reduced, especially in the group where the proposed scheme was used, and the long-term results were stable for 6 months. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e35147 https://doi.org/10.3897/pharmacia.67.e35147 https://pharmacia.pensoft.net/article/35147/ https://pharmacia.pensoft.net/article/35147/download/pdf/ en

10.3897/pharmacia.67.e35126 2020-05-13 pharmacia

Spectroscopic criteria for early diagnosis of changes in the mineral and organic matrix of hard dental tissues Dovhanyk,Viktoria Maglyovanyi,Anatoliy Harkov,Stefan Synytsa,Volodymyr Hrynovets,Volodymyr Hrynovets,Ihor Chaban,Ihor Lelyukh,Maryan infrared spectroscopy hydroxyapatite carbamide peroxide Pharmacia 67(1): 5-12 At the present stage of development of medical science, experimental and clinical dentistry is often used in scientific research, which allows diagnosing preclinical stages of manifestations of changes in tissues and organs of the oral cavity and biological fluids at the level of nanotechnology enabling to study the mechanisms of molecular transformation that lead to occurrence of pathological changes. One of the promising methods of research is infrared spectroscopy. The advantage of the method is that the absorption spectrum can be obtained with a small amount of the test substance (0.1–0.01 cm3) and under conditions of different aggregate states (solution, powder, liquid). Graphical abstract info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e35126 https://doi.org/10.3897/pharmacia.67.e35126 https://pharmacia.pensoft.net/article/35126/ https://pharmacia.pensoft.net/article/35126/download/pdf/ en

10.3897/pharmacia.67.e35117 2020-05-13 pharmacia

Correction of disordered mineral bone metabolism in patients affected by chronic periodontitis Yarmoshuk,Iryna bisphosphonates bone tissue chronic periodontitis synthetic osteoplastic material Pharmacia 67(1): 1-4 One of the main mechanisms in pathogenesis of chronic periodontitis is disordered bone metabolism that is accomplished by cortical plate’s resorption, destruction of the interdental septums and osteoporosis of the jaws. Administration of osteotropic agents will allow achieving efficient results in treatment of the patients affected by periodontal disorders, lower the tendency of bone resorption and stimulate the processes of regeneration. The article demonstrates the results obtained after the surgical treatment of the patients with osteopenia affected by chronic periodontitis of II–III degree that were administered simultaneously with synthetic osteoplastic material Tricalcium phosphate and a bone resorption inhibitor Ibandronic acid. It has been established the high efficiency of the recommended treatment that was proved by positive progress of biochemical markers of bone metabolism in blood serum and urine of the individuals from the main group taken 24 month after the beginning of the treatment. The study shows that the reis arise of osteocalcin by 11,5% in the blood serum of the main group patients 2 years after the research and the amount of desoxypiridynolin, on the other hand, was by 21,72% lower comparing with those from the main group (р < 0,05). info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e35117 https://doi.org/10.3897/pharmacia.67.e35117 https://pharmacia.pensoft.net/article/35117/ https://pharmacia.pensoft.net/article/35117/download/pdf/ en

10.3897/pharmacia.67.e50397 2020-07-31 pharmacia

Bioanalytical method development and validation for the determination of metoprolol and meldonium in human plasma Horyn,Mariana Logoyda,Liliya LC-MS/MS Metoprolol Meldonium Validation Human plasma Pharmacia 67(2): 39-48 Aim.The main purpose of this study was to develop a simple, precise, rapid and accurate method for the quantification of metoprolol and meldonium in human plasma. Materials and methods. The resolution of peaks of metoprolol was best achieved with Discovery C18, 50 × 2.1 mm, 5 μm column and meldonium - ZORBAX HILIC Plus, 50 × 2.1 mm, 3.5 μm column. Samples of metoprolol were chromatographed in a gradient mode (eluent A (acetonitrile – water – formic acid, 5 : 95 : 0.1 v/v), eluent B (acetonitrile – formic acid, 100 : 0.1 v/v)). The initial content of the eluent B is 0%, which increases linearly by 1.0 min to 100% and to 1.11 min returns to the initial 0%. The mobile phase was delivered at a flow rate of 0.400 mL/min into the mass spectrometer ESI chamber. The injection volume was 5μl. Samples of meldonium were chromatographed in a isocratic using mobile phase water – acetonitrile – ammonium formate buffer 200 мМ, 20 : 75 : 5 v/v). Results.The total chromatographic run time was 2.0 minutes and the elution of metoprolol, meldonium and IS occurred at ~1.39 and 1.18 minutes, respectively.A linear response function was established at 2 - 200 ng/mL for metoprolol and 50 -5000 ng/mL for meldonium in human plasma. The% mean recovery for metoprolol in LQC, MQC and HQC was 99.0%, 107.5% and 96.8%, for meldonium in LQC, MQC and HQC was 94.1%, 100.2% and 93.1% respectively. The lowest concentration with the RSD <20% was taken as LLOQ and was found to be 2.31 ng/mL for metoprolol, 47.70 ng/mL for meldonium. The % accuracy of LLOQ samples prepared with the different biological matrix lots were found 115.4% for metoprolol and 95.5% for meldonium, which were found within the range of 80.00–120.00% for the seven different plasma lots. % CV for LLOQ samples was observed as 12.8% and 7.7% respectively, which are within 20.00% of the acceptance criteria. Conclusion.A rapid method was developed for simultaneous determination of metoprolol and meldonium in human plasma. The method was strictly validated according to the ICH guidelines. Acquired results demonstrate that proposed strategy can be effortlessly and advantageously applied for routine examination of metoprolol and meldonium in human plasma. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e50397 https://doi.org/10.3897/pharmacia.67.e50397 https://pharmacia.pensoft.net/article/50397/ https://pharmacia.pensoft.net/article/50397/download/pdf/ en

10.3897/pharmacia.67.e38648 2020-07-31 pharmacia

Evaluation of physicochemical and antioxidant properties of nanosized copolymeric micelles loaded with kaempferol Yoncheva,Krassimira Hristova-Avakumova,Nadia Hadjimitova,Vera Traykov,Trayko Petrov,Petar copolymeric micelles nanosized systems kaempferol radical scavenging activity Pharmacia 67(2): 49-54 The study was focused on the evaluation of two copolymers as micellar carriers for kaempferol delivery. The copolymers comprised identical hydrophilic blocks of poly(2-(dimethylamino)ethyl methacrylate and different hydrophobic blocks of either poly(ε-caprolactone) (PDMAEMA9-b-PCL70-b-PDMAEMA9) or poly(propylene oxide) (PDMAEMA13-b-PPO69-b-PDMAEMA13). The calculation of Flory-Huggins parameters and determination of encapsulation efficiency showed that PDMAEMA-b-PCL-b-PDMAEMA copolymer possessed higher capacity for kaempferol loading. The diameter of the micelles before and after lyophilization was not changed, suggesting that the micelles could be lyophilized and redispersed before administration. The in vitro release of kaempferol from PDMAEMA-b-PPO-b-PDMAEMA micelles was faster than the release from PDMAEMA-b-PCL-b-PDMAEMA micelles, probably due to the higher affinity of kaempferol to this copolymer. Further, the higher affinity resulted in a retention of antioxidant activity of kaempferol in the presence of DPPH and KO2 radicals. Thus, PDMAEMA-PCL-PDMAEMA was considered more appropriate carrier because of the higher encapsulation efficiency and preservation of antioxidant activity of the drug. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e38648 https://doi.org/10.3897/pharmacia.67.e38648 https://pharmacia.pensoft.net/article/38648/ https://pharmacia.pensoft.net/article/38648/download/pdf/ en

10.3897/pharmacia.67.e48220 2020-07-31 pharmacia

Efficient validated method of HPLC to determine amlodipine in combinated dosage form containing amlodipine, enalapril and bisoprolol and in vitro dissolution studies with in vitro/ in vivo correlation Logoyda,Liliya Amlodipine High performance liquid chromatography Dissolution study Validation In vitro / in vivo correlation Pharmacia 67(2): 55-61 Aim. A rapid and reproducible HPLC method has been developed for the determination of amlodipine in experimental combined dosage forms containing amlodipine, bisoprolol and enalapril and for drug dissolution studies. Materials and methods. The separation was done using a column Phenomenex Polar Synergi, 5 μm, 4.6×50 mm and a mobile phase of methanol:phosphate buffer solution (65:35, v/v), flow-rate of 1.0 mL/min. The injection volume was 100 μL and the ultraviolet detector was set at 240 nm. Results. The method was validated as per ICH guidelines. Under these conditions, amlodipine was eluted at 1.89 min. Total run time was shorter than 2.5 min. The linearity of the method had a good correlation with concentration and peak area. The correlation coefficient of amlodipine was found to be not less than 0.9991, which indicates good linear relationship over concentration range 0.625 mg/mL–5.000 mg/mL (1.250 mg/mL–5.000 mg/mL at pH 4.5). The % RSD values in intra-day and inter-day precision study were found to be less than 0.267 for amlodipine, which indicate method was precise. Hence, the present developed method was said to be suitable for the analysis of drugs in their pharmaceutical dosage form. Also, in vitro dissolution of amlodipine containing tablets were performed to validate the suitability of the proposed method. The dissolution pattern complies with the FDA standards, indicating suitability of the proposed method for the dissolution study of amlodipine. It will allow conducting comparative studies in vitro to confirm the equivalence of tablets containing amlodipine. Conclusion. A simple and sensetive HPLC method was developed for the estimation of amlodipine in tablets containing amlodipine, enalapril and bisoprolol. The proposed method was applied successfully for quality control assay of amlodipine in experimental tablets and in vitro dissolution studies. In vitro / in vivo correlation of amlodipine has been conducted. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e48220 https://doi.org/10.3897/pharmacia.67.e48220 https://pharmacia.pensoft.net/article/48220/ https://pharmacia.pensoft.net/article/48220/download/pdf/ en

10.3897/pharmacia.67.e48896 2020-07-31 pharmacia

HPLC MS/MS method development for the quantitative determination of verapamil hydrochloride from Caco-2 cell monolayers Logoyda,Liliya Herasymiuk,Maksym Popovych,Dariya Pidruchna,Svitlana Hlushok,Vitaliy Herasymiuk,Nazar Zarivna,Nadiya HPLC-MS/MS Verapamil hydrochloride Caco-2 cells Recovery Bioavailability Pharmacia 67(2): 63-69 Aim. An understanding of the role that transporters, in particular P-glycoprotein (P-gp), can play in the absorption, distribution, metabolism and excretion (ADME) of candidate drugs, and an assessment of how these processes might impact on toxicity and the potential for drug-drug interactions in the clinic, is required to support drug development and registration. It is therefore necessary to validate preclinical assays for the in vitro evaluation of candidate drugs as substrates or inhibitors of human P-gp. 2. A simple, rapid HPLC MS/MS method was developed for determination of verapamil hydrochloride from confluent Caco-2 monolayers and from aqueous solution. Materials and methods. Chromatography was achieved on Discovery C18, 50 × 2.1 mm, 5 μm column. Samples were chromatographed in a gradient mode (eluent A (acetonitrile – water – formic acid, 5 : 95 : 0.1 v/v), eluent B (acetonitrile – formic acid, 100 : 0.1 v/v)). The initial content of the eluent B is 0%, which increases linearly by 1.0 min to 100% and to 1.01 min returns to the initial 0%. The mobile phase was delivered at a flow rate of 0.4 mL/min into the mass spectrometer ESI chamber. The sample volume was 5 μl. Results. Under these conditions, verapamil hydrochloride was eluted at 1.08 min. A linear response function was established at 1 – 100 ng/mL. The regression equation for the analysis was Y = 0.0162x + 0.00391 with coefficient of correction (R2) = 0.9992. According to the Caco-2 test results, verapamil showed low permeability. It should be noted that the recovery value for verapamil hydrochloride is 102.69%. The within-run coefficients of variation ranged between 0.336% and 0.617% for verapamil. The within-run percentages of nominal concentrations ranged between 98.82% and 100.62% for verapamil. The between-run coefficients of variation ranged between 0.334% and 0.612% for verapamil. The between-run percentages of nominal concentrations ranged between 98.97% and 101.76% for verapamil. The assay values on both the occasions (intra- and inter-day) were found to be within the accepted limits. Conclusion. From results of analysis, it can be concluded that developed method is simple and rapid for determination of verapamil hydrochloride from confluent Caco-2 monolayers and from aqueous solution. Acquired results demonstrate that proposed strategy can be effortlessly and advantageously applied for examination of verapamil hydrochloride from Caco-2 cell monolayers. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e48896 https://doi.org/10.3897/pharmacia.67.e48896 https://pharmacia.pensoft.net/article/48896/ https://pharmacia.pensoft.net/article/48896/download/pdf/ en

10.3897/pharmacia.67.e48319 2020-07-31 pharmacia

Ailanthus altissima and Amorpha fruticosa – invasive arboreal alien plants as cheap sources of valuable essential oils Kozuharova,Ekaterina Benbassat,Niko Berkov,Strahil Ionkova,Iliana essential oils pharmacological activity invasive plants Ailanthus altissima Amorpha fruticosa Pharmacia 67(2): 71-81 The high tolerance of various habitat conditions and potent propagation ability of Ailanthus altissima (Mill.) Swingle (Simaroubaceae) and Amorpha fruticosa L. (Fabaceae) promote their aggressive invasive behaviour. Additionally, they not only over-compete the local vegetation but suppress the seed development. In the newly invaded habitats they might not have suitable herbivores to control their populations. The aim of this review is to evaluate the potential of A. altissima and A. fruticosa, as cheap sources of valuable essential oils. The essential oils yield and compostion of both plant species vary significantly depending on plant parts, origin and time of collection. The main constituents of A. altissima essential oil are α-curcumene, α-gurjunene, γ-cadinene, α-humulene β-caryophyllene caryophyllene oxide, germacrene D etc. The main constituents of A. fruticosa are δ-cadinene, γ-cadinene, β-caryophyllene γ-muurolene +, ar-curcumene, myrcene etc. These essential oils have been reported to possess different activities such as antimicrobial, insect repellent, insecticidal and herbicidal activity. Due to the fact that these are aggressive invasive species, they can provide abundant and cheap resources. Additionally, future industrial exploitation of the biomass of these invasive plants for essential oils’ extraction might contribute to biodiversity conservation by relieving their destructive impact on the natural habitats. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Review Article text/html info:doi:10.3897/pharmacia.67.e48319 https://doi.org/10.3897/pharmacia.67.e48319 https://pharmacia.pensoft.net/article/48319/ https://pharmacia.pensoft.net/article/48319/download/pdf/ en

10.3897/pharmacia.67.e50159 2020-07-31 pharmacia

HPLC-MS/MS method development for the quantitative determination of nifedipine for Caco-2 permeability assay Logoyda,Liliya LC-MS/MS Nifedipine Caco-2 cells Recovery Bioavailability Pharmacia 67(2): 83-88 Aim. Poorly water-soluble drugs such as nifedipineoffer challenging problems in drug formulation as poor solubility is generally associated with poor dissolution characteristics and thus with poor oral bioavailability (BCS class II drugs). Methods of quantitative determination of nifedipine by methods of spectrophotometry and chromatography are described in the scientific literature. However, methods are not developedfor examination of nifedipine from Caco-2 cell monolayers. Caco-2 cell monolayers have been extensively used for years as a tool to test permeability, assess the oral absorption potential and study the absorption mechanism of compounds. Therefore, the aim of this study was to develop and validate an efficient HPLC MS/MS method for determination of nifedipine from Caco-2 cell monolayers. Materials and methods. Chromatography was achieved on DiscoveryC18, 50 × 2.1 mm, 5 μm column. Samples were chromatographed in a gradient mode (eluent A (acetonitrile – water – formic acid, 5 : 95 : 0.1 v/v), eluent B (acetonitrile – formic acid, 100 : 0.1 v/v)). The initial content of the eluent B is 0%, which increases linearly by 1.0 min to 100% and to 1.01 min returns to the initial 0%. The mobile phase was delivered at a flow rate of 0.4 mL/min into the mass spectrometer ESI chamber. The sample volume was 5 μl. Results. Under these conditions, nifedipine was eluted at 1.83 min. A linear response function was established at 1 – 100 ng/mL. The regression equation for the analysis was Y = 0.0323x-0.00121 with coefficient of correction (R2) = 0.9987. According to the Caco-2 test results, nifedipine showed high permeability. The within-run coefficients of variation ranged between 0.331% and 0.619% for nifedipine. The within-run percentages of nominal concentrations ranged between 98.80% and 100.63% for nifedipine. The between-run coefficients of variation ranged between 0.332% and 0.615% for nifedipine. The between-run percentages of nominal concentrations ranged between 98.98% and 101.71% for nifedipine. The assay values on both the occasions (intra- and inter-day) were found to be within the accepted limits. Conclusion. From results of analysis, it can be concluded that developed method is simple and rapid for determination of nifedipine from confluent Caco-2 monolayers and from aqueous solution. Acquired results demonstrate that proposed strategy can be effortlessly and advantageously applied for examination of nifedipine from Caco-2 cell monolayers. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e50159 https://doi.org/10.3897/pharmacia.67.e50159 https://pharmacia.pensoft.net/article/50159/ https://pharmacia.pensoft.net/article/50159/download/pdf/ en

10.3897/pharmacia.67.e48472 2020-07-31 pharmacia

Topical use of resveratrol: technological aspects Gugleva,Viliana Zasheva,Stanimira Hristozova,Maya Andonova,Velichka antioxidant activity biologically active compound drug delivery systems skin protection Pharmacia 67(2): 89-94 Resveratrol is a natural polyphenolic phytoalexin found in grapes, berry skins, roots of Japanese knotweed and is reputed as an excellent antioxidant, anti-inflammatory, neuro- and cardio- protective agent. Resveratrol has also beneficial effects in therapy of different skin conditions such as acne, exfoliative eczema, psoriasis and is known to provide a protection against ultraviolet radiation-mediated oxidative stress. However, its low oral bioavailability and short biological half- life compromise its beneficial therapeutic effects; therefore, its topical application is a practical approach in the treatment of various cutaneous disorders. Challenges associated with the development of topical resveratrol drug delivery systems and dosage forms include its low aqueous solubility as well as its poor UV-, pH- and temperature-dependent stability. The purpose of this article is to discuss the mechanism of action, therapeutic effect and physicochemical properties of resveratrol and to present recent technological approaches designed to improve its stability, bioavailability and therapeutic efficiency. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Review Article text/html info:doi:10.3897/pharmacia.67.e48472 https://doi.org/10.3897/pharmacia.67.e48472 https://pharmacia.pensoft.net/article/48472/ https://pharmacia.pensoft.net/article/48472/download/pdf/ en

10.3897/pharmacia.67.e50390 2020-07-31 pharmacia

Induction of flavonoid biosynthesis by in vitro cultivation of Astragalus glycyphyllos L. Popova,Pavlinka Zarev,Yancho Shkondrov,Aleksandar Krasteva,Ilina Ionkova,Iliana Astragalus glycyphyllos flavonoids in vitro cultures Pharmacia 67(2): 95-99 Establishment of in vitro cultures from Astragalus glycyphyllos, determination of biomass and analysis of total flavonoids, rutin and camelliaside A were performed. To increase flavonoid production various combinations of plant hormones and light/dark regimen were investigated. Suspension cultures with exogenous quercetin were evaluated for possible increase in flavonoid production. Shoots, calli and suspensions were successfully established. Rutin and camelliaside A were proved in highest amount in shoots. Calli, cultivated on modified G48 medium, with double amount of Ca2+ and Mg2+, achieved higher total flavonoid content (2.37 and 2.03 mg/g DW). Suspensions cultures, cultivated on modified G48 medium with 10, 20 and 30 mg/mL quercetin achieved higher total flavonoid content (0.09, 0.10 and 0.13 mg/mg DW). Biotransformation of quercetin to isoquercitrin was achieved. The highest concentration of isoquercitrin (56.73 ng/mg DW) was observed on suspensions cultures cultivated on modified G48 medium, with 20 mg/mL quercetin. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e50390 https://doi.org/10.3897/pharmacia.67.e50390 https://pharmacia.pensoft.net/article/50390/ https://pharmacia.pensoft.net/article/50390/download/pdf/ en

10.3897/pharmacia.67.e39045 2020-07-31 pharmacia

Kinesitheraphy in trimalleolar fracture – case report Becheva,Maria kinesitherapy trimalleolar fracture Pharmacia 67(2): 101-103 The purpose of the paper is to prove the efficacy of a kinesitherapeutic program intherecovery of a patient with trimalleolar fractureofthe left lower limb.We present a 42-year-old patient with a trimalleolar fracture and paresis of n. peroneus communis. Kinesitherapy was performed after thirteen weeks of surgery for ten consecutive days. The kinesitherapeuticmeans included: cryotherapy, lymphatic drainage massage, isometric contractions for the femur muscles, active exercises with and without resistance, active exercises with and on gymnastic apparatuses, post-isometric relaxation for the sciatic musculature and m. triceps surai, training in walking.As a result of the kinesitherapeutic exercises, the ankle swelling decreased.The volume of movement increased, pain was reduced as well as the muscle spasm in the ankle joint. The gait improved. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e39045 https://doi.org/10.3897/pharmacia.67.e39045 https://pharmacia.pensoft.net/article/39045/ https://pharmacia.pensoft.net/article/39045/download/pdf/ en

10.3897/pharmacia.67.e55257 2020-08-06 pharmacia

Analytical difficulties for determination of acesulfame K in chocolate products Petrova,Svetla Christova-Bagdassarian,Valentina chocolate and cocoa products Е 950 HPLC – UV synthetic sweeteners Pharmacia 67(2): 105-110 Sweeteners are substances used as a dietary supplement to replace sugar. Consumers are concerned about the high levels of sugar, calories and cariogenicity in confectionery products, which is why the popularity of the so-called. „Light“ products and „sugar-free“ products. Acesulfame K is a synthetic sweetener about 200 times sweeter than sugar. In the present work, an analysis of acesulfame K in cocoa and chocolate products was performed. For the determination of sweeteners acesulfame K, saccharin and aspartame in foodstuffs, a standardized reverse phase high performance liquid chromatography method with UV detection was used. A cocoa matrix-specific compound was observed in all chocolate products analyzed for acesulfame K. Interference did not correspond to acesulfame K on the UV spectrum and could not be removed by two-step purification. The comparison of the spectral characteristics allowed to avoid a misleading result for the presence of acesulfame K in chocolate and cocoa products. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e55257 https://doi.org/10.3897/pharmacia.67.e55257 https://pharmacia.pensoft.net/article/55257/ https://pharmacia.pensoft.net/article/55257/download/pdf/ en

10.3897/pharmacia.67.e50806 2020-08-20 pharmacia

In vitro analysis of the activity of human monoamine oxidase type B (hMAOB), treated with the cyanotoxin anatoxin-a: supposed factor of neurodegenerative diseases Ilieva,Viktoria Kondeva-Burdina,Magdalena Georgieva,Tzveta MAO-B activity neurodegenerative diseases anatoxin-a Pharmacia 67(2): 111-114 In this study, we investigated the hypothesis that an additional source of free radicals may be hydrogen peroxide formed by monoamino oxidase (MAO) -catalyzed deamination of catecholamines. Also, increased MAO-B activity in the brain has been linked to the development of some neurodegenerative diseases. The toxicant we used to treat recombinant human MAO-B enzyme is the cyanotoxin аnatoxin-a. For anatoxin-a is known that it’s an agonist of neuronal acetylcholine receptors with 20 times greater affinity to them compared to the natural neurotransmitter. In this study, we analyzed the effect of anatoxin at various selected concentrations on the activity of recombinant human MAO-B enzyme. The method we use is to analyze the activity of human MAO-B with the fluorimetric reagent Amplex UltraRed and the substrate tyramine hydrochloride. The aim of this study is to analyze the effect of anatoxin-a on the hMAO-B enzyme activity and its influence as a factor for the development and progression of neurodegenerative diseases. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e50806 https://doi.org/10.3897/pharmacia.67.e50806 https://pharmacia.pensoft.net/article/50806/ https://pharmacia.pensoft.net/article/50806/download/pdf/ en

10.3897/pharmacia.67.e52738 2020-08-25 pharmacia

Antithrombotic regimens in patients after coronary artery bypass grafting and coronary endarterectomy Kyuchukov,Dimitar Zheleva-Kyuchukova,Ivayla Nachev,Gencho dual antiplatelet therapy (DAPT) coronary endarterectomy (CEAE) coronary artery bypass grafting (CABG) Pharmacia 67(3): 115-120 Background: Coronary artery bypass grafting (CABG) remains the gold standard in the treatment of complex chronic forms of coronary heart disease (CHD). Coronary endarterectomy (CEAE) is a useful adjunctive technique to CABG in patients with diffuse coronary artery disease. In order to maintain the patency of the coronary arteries and graft conduits, various antithrombotic protocols have been introduced over the years, combining various antiplatelet and anticoagulant drugs, but still there is no consensus. Aim: The aim of the study is to compare results between two antithrombotic regimens after CEAE. The first one is a combination of acenocoumarol combined with acetylsalicylic acid (ASA), the second regimen is a dual antiplatelet therapy (DAPT) of clopidogrel combined with ASA. Material and methods: We retrospectively reviewed 56 consecutive patients (60 ± 8.2 years) undergoing isolated CABG in association with CEAE between January 2018 and December 2019. In the postoperative period, patients were divided into two groups according to the antithrombotic regimens described above. Twenty-four were in the ASA and acenocoumarol group (AA) and 32 were in the ASA and clopidogrel group (AC). Patients were followed up to 30 days after the operation and we access the mortality rate, new ECG changes, levels of myocardial fraction of creatinine phosphokinase (CPK-MB), left ventricular systolic function, pericardial or pleural effusions requiring drainage or revision for bleeding. Results: Operative mortality was 3,6 %. No differences in the antithrombotic efficacy of the two regimens. A significantly higher level of hemorrhagic complications was observed in the ASA + acenocoumarol treatment group. Conclusion: Dual antiplatelet therapy (DAPT) after CABG and coronary endarterectomy is an effective pharmacological regimen in regard to 30-day postoperative outcomes and is considerably safety in terms of bleeding complications. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e52738 https://doi.org/10.3897/pharmacia.67.e52738 https://pharmacia.pensoft.net/article/52738/ https://pharmacia.pensoft.net/article/52738/download/pdf/ en

10.3897/pharmacia.67.e53886 2020-08-28 pharmacia

Assessment of allergenicity of irradiated dairy products in a Balb/c mice model Miteva,Daniela Solak,Ayten Dyankova,Svetia Nacheva,Iliana Dimov,Krasimir Cow’s milk hypersensitivity murine model irradiation IgE ELISA Pharmacia 67(3): 129-133 The objective of the present in vivo study was to analyze the changes in the immune response of the sensitized Ваlb/c mice against milk allergens in lyophilized cow’s milk (LCM) and whey curd (LC) before and after gamma irradiation (10 kGy). The results showed lower levels of IgE in the group treated with irradiated LCM (ICM) compared to the group treated with non-irradiated LCM (NiCM). Hence, it could be suggested that gamma irradiation influenced the epitopes of the major milk proteins and was associated with lower allergenicity of the lyophilized irradiated milk. The gamma irradiation in the whey curd, however, did not significantly change the level of IgE antibodies in IC (treated with irradiated LC) compared to NiC (treated with non-irradiated LC) group. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e53886 https://doi.org/10.3897/pharmacia.67.e53886 https://pharmacia.pensoft.net/article/53886/ https://pharmacia.pensoft.net/article/53886/download/pdf/ en

10.3897/pharmacia.67.e38969 2020-08-28 pharmacia

Anti-inflammatory properties of some novel thiazolo[4,5-b]pyridin-2-ones Chaban,Taras Matiychuk,Vasyl Komarytsya,Olexandra Myrko,Iryna Chaban,Ihor Ogurtsov,Volodymyr Nektegaev,Ihor anti-inflammatory activity organic synthesis thiazolo[4 5-b]pyridines Pharmacia 67(3): 121-127 Synthesis of novel N3 and C5 substituted thiazolo[4,5-b]pyridin-2-ones was carried out on the basis of [3+3]-cyclocodensation, acylation and alkylation reactions. The structures of the obtained compounds were confirmed by 1H NMR spectroscopy, and elemental analysis. The anti-inflammatory action of novel thiazolo[4,5-b]pyridine-2-one derivatives was evaluated in vivo employing the carrageenan-induced rat paw edema method. When compared with Ibuprofen, some our compounds were found to be more potent. Graphical abstract info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e38969 https://doi.org/10.3897/pharmacia.67.e38969 https://pharmacia.pensoft.net/article/38969/ https://pharmacia.pensoft.net/article/38969/download/pdf/ en

10.3897/pharmacia.67.e52585 2020-09-14 pharmacia

HPLC study of phenolic compounds in Mirabilis jalapa raw material Sarray,Dhurgham Khalid Abed Sarray Horiacha,Liliia Zhuravel,Iryna Fedosov,Andriy Mirabilis jalapa four-o’clocks phenolic compounds HPLC Pharmacia 67(3): 145-152 Mirabilis jalapa is a popular decorative plant valued for its beautiful multicolored flowers. Folk medicine in various countries applies Mirabilis jalapa as anti-microbial, anti-inflammatory, diuretic, spasmolytic drug. Chemical composition of different types of Mirabilis jalapa has not yet been adequately studied which is an obstacle for its application in medicine. The qualitative composition and quantitative content of phenolic compounds were studied by the HPLC method. The performed experiment revealed presence of hydroxycinnamic acids, flavonoids, isoflavonoids and coumarins in tested herb. The content of phenolic compounds was the highest in Mirabilis jalapa flowers, counting as much as 2977.41 ± 59.55 µg/mg. Total content of phenolic compounds in Mirabilis jalapa herb was 304.25 ± 6.08 µg/mg, in fruits – 67.92 ± 1.36 µg/mg, and in roots – 12.44 ± 0.25 µg/mg. Quantitatively neochlorogenic acid dominated in flowers, chlorogenic acid in fruits, whereas Mirabilis jalapa herb mostly contained rutin and hyperoside. The obtained results will be useful in the development of quality control methods for Mirabilis jalapa herb and manufacture of drug preparations on its basis. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e52585 https://doi.org/10.3897/pharmacia.67.e52585 https://pharmacia.pensoft.net/article/52585/ https://pharmacia.pensoft.net/article/52585/download/pdf/ en

10.3897/pharmacia.67.e51812 2020-09-14 pharmacia

Determination of fatty acid composition content in the herbal antidiabetic collections Savych,Alona Marchyshyn,Svetlana Basaraba,Roksolana diabetes mellitus herbal antidiabetic collection GC/MS fatty acids Pharmacia 67(3): 153-159 It was determined the qualitative composition and the quantitative content of fatty acids in the herbal antidiabetic collection № 3, № 4, № 7, № 13, № 19, which are used in folk medicine for prevention and treatment of diabetes mellitus type 2 in Ukraine by GC/MS method. According to the results it was identified 8 fatty acids in the herbal antidiabetic collection № 3, 13 fatty acids in the herbal antidiabetic collection № 4, 12 fatty acids in the herbal antidiabetic collection № 7, 13 fatty acids in the herbal antidiabetic collection № 13 and 11 fatty acids in the herbal antidiabetic collection № 19. The saturated fatty acids were found to be dominated in the raw plant material. The results of the quantitative research showed that the herbal antidiabetic collection № 3 contains 16.13 mg/g of fatty acids, the herbal antidiabetic collection № 4 – 27.17 mg/g, the herbal antidiabetic collection № 7 – 31.98 mg/g, the herbal antidiabetic collection № 13 – 27.37 mg/g, the herbal antidiabetic collection № 19 – 18.79 mg/g. The GC/MS analysis of the fatty acid composition in the herbal antidiabetic collections has shown that this raw material has a lot of fatty acids, which can have a positive effect for the treatment and prevention of diabetes mellitus type 2. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e51812 https://doi.org/10.3897/pharmacia.67.e51812 https://pharmacia.pensoft.net/article/51812/ https://pharmacia.pensoft.net/article/51812/download/pdf/ en

10.3897/pharmacia.67.e52737 2020-09-14 pharmacia

Antiplatelet therapy after PCI in patients with high risk of bleeding Zheleva-Kyuchukova,Ivayla Gelev,Valeri percutaneous coronary interventions (PCI) dual antiplatelet therapy (DAPT) high bleeding risk (HBR) acetylsalicylic acid (ASA) Pharmacia 67(3): 135-143 The progress of percutaneous coronary interventions (PCI) over the last few decades facilitated treatment of increasingly complex patient populations. The introduction of drug-eluting stents (DESs) led to need of stronger and prolonged inhibition of platelets which in turn increased the incidence of bleeding complications. The identification and management of patients at high bleeding risk (HBR) during and after percutaneous coronary interventions (PCI) is still problematic in everyday clinical practice. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Review Article text/html info:doi:10.3897/pharmacia.67.e52737 https://doi.org/10.3897/pharmacia.67.e52737 https://pharmacia.pensoft.net/article/52737/ https://pharmacia.pensoft.net/article/52737/download/pdf/ en

10.3897/pharmacia.67.e52474 2020-09-15 pharmacia

Influence between NO and CO in guinea pig stomach fundus Kadinov,Boris Itzev,Dimitar Contraction guinea-pig hemin heme oxygenase histochemistry smooth muscle Pharmacia 67(3): 161-168 The interaction between carbon monoxide and nitric oxide and their role in modulation of stomach fundus excitability was studied. The presence and colocalization of heme oxygenase 1 (HO-1) and nitric oxide synthase (NOS) was verified in myentheric ganglia by immunohistochemistry. The role of inducible heme oxygenase isoenzyme was investigated after in vivo treatment of animals with CoCl2 (80 mg kg-1 b.w.) injected subcutaneously 24 hours before euthanasia. This treatment resulted in positive staining for the inducible isoform in stomach smooth muscle. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e52474 https://doi.org/10.3897/pharmacia.67.e52474 https://pharmacia.pensoft.net/article/52474/ https://pharmacia.pensoft.net/article/52474/download/pdf/ en

10.3897/pharmacia.67.e35080 2020-09-15 pharmacia

Prophylaxis of dental caries in children from polluted regions Avakov,Valentyn Oktysyuk,Yuriy Rozhko,Mykola dental caries xenobiotics alcohol dehydrogenase glutathione-S-transferase prophylaxis Pharmacia 67(3): 169-172 To be living at the most advanced technological area in history is to exist and face pollution one of the most serious threats to all living things on the planet. There is evidence that anthropogenic and technological pollutions cause a considerable number of health problems and stomatological in particular. This article demonstrates the results gained by administration of vitamin-macro element complex “Calcinova” and sorbent “Enterosgel” in correction of enzymes responsible for biotransformation of xenobiotics in blood serum of children from the polluted areas. It has been established the high efficiency of recommended scheme on caries prophylaxis that is proved by positive biochemical indexes in blood serum of this children observed 30 month after the beginning of the investigation. As a result of the introduced prophylaxis, we have noticed the significant improvement of biochemical indexes in children with tooth decay. The findings reflect a certain rise in activity of enzymes responsible for elimination of xenobiotics such as alcohol-dehydrogenase (ADH) and glutathione-S-transferase (GST) obtained from the blood serum of children from the main group comparing to the control group. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e35080 https://doi.org/10.3897/pharmacia.67.e35080 https://pharmacia.pensoft.net/article/35080/ https://pharmacia.pensoft.net/article/35080/download/pdf/ en

10.3897/pharmacia.67.e56788 2020-10-02 pharmacia

A geranylated chalcone with antiplatelet activity from the leaves of breadfruit (Artocarpus altilis) fakhrudin,nanang Pertiwi,Krisna Takubessi,Marce Susiani,Eka Nurrochmad,Arief Widyarini,Sitarina Sudarmanto,Ari Nugroho,Arief Wahyuono,Subagus Artocarpus communis 2-geranyl-2ʹ 3 3 4ʹ-tetrahydroxydihydrochalcone thrombosis P2Y12 P2Y1 Pharmacia 67(4): 173-180 Platelet plays a crucial role in cardiovascular diseases (CVDs) development. Abnormalities in platelet aggregation provokes thromboembolism, eventually leading to death. In Indonesia, breadfruit (Artocarpus altilis) leaf is traditionally used to treat CVDs. This study aimed to evaluate the antiplatelet activity of A. altilis leaf extract (AAE) and to identify its active compound. A. altilis leaves were extracted with ethanol, and the antiplatelet activity was assessed using ADP-induced platelet aggregation. The major compound was isolated with column chromatography followed by preparative TLC, and the structure was determined on the basis of UV, MS, IR, and NMR spectra. The binding mode of the active compound to platelet receptors was characterized in in silico study. AAE exhibited an antiplatelet activity (IC50 of 252.23 µg/mL). A geranylated chalcone, 2-geranyl-2ʹ,3,3,4ʹ-tetrahydroxydihydrochalcone (GTDC) was identified as the antiplatelet compound (IC50 of 9.09 µM). GTDC actions with P2Y12 platelet receptor involving three amino acid residues. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e56788 https://doi.org/10.3897/pharmacia.67.e56788 https://pharmacia.pensoft.net/article/56788/ https://pharmacia.pensoft.net/article/56788/download/pdf/ en

10.3897/pharmacia.67.e46586 2020-10-02 pharmacia

Determination of social and economic accessibility of drugs for treatment of Parkinson’s disease on the basis of modern approaches Kotvitska,Alla Prokopenko,Oleksii clinical protocol medicines index of retail prices neurological diseases Pharmacia 67(4): 215-221 In the context of the economic crisis, the availability of medicines for the population is one of the key issues facing pharmaceutical sector of healthcare system. Due to the fact of that, the purpose of the work was to study the social and economic accessibility of medicines, since such studies in the future may provide an opportunity for effective input of medicines costs reimbursement system, which will increase their availability, especially for socially vulnerable groups of population. The data analysis of the clinical protocols of Great Britain, Kazakhstan and Ukraine was conducted, and the indicators of social and economic availability within 2014–2018 were calculated. The obtained results indicate an adequate level of availability of medicines for the able-bodied population and, unfortunately, a low level of accessibility of medicines for people of retirement age with a tendency to further descension. These results point the necessity of the further research and development of government control systems and provision of pharmaceutical care for the population. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e46586 https://doi.org/10.3897/pharmacia.67.e46586 https://pharmacia.pensoft.net/article/46586/ https://pharmacia.pensoft.net/article/46586/download/pdf/ en

10.3897/pharmacia.67.e50458 2020-10-02 pharmacia

Cost analysis of neonates after prenatal corticosteroid prophylaxis of Respiratory Distress Syndrome Mihaylova,Anna A. Kasnakova,Petya Gueorguiev,Stanislav Petkova-Gueorguieva,Elina Peikova,Lily preterm birth prenatal corticosteroid prophylaxis health costs premature neonates RDS Pharmacia 67(4): 209-214 Preterm birth is a vital global health-economic problem. Health disorders provoked by it generate a high neonatal mortality rate. Prenatal corticosteroid prevention aims to reduce postnatal complications in premature infants. This survey covered two basic baby groups: work group of 89 premature infants that had been subjected to prenatal corticosteroid prophylaxis and a control group of 78 premature babies without prenatal prevention. The analysis of the pharmacoeconomic aspects of prenatal corticosteroid prevention enabled the comparison of clinical and therapeutic results, treatment costs, therapeutic expenditures, shortterm therapeutic effect, benefits and sequences from premature infants’ therapy. The analysis of clinical data obtained during this survey enabled the conclusion that when analyzing the combined effect of Dexamethasone prophylaxis, gestation week at birth and the age of the mother of premature infants with RDS, respiratory obstuction occurrence was mediated by the earlier gestation week at birth, older mother’s age and, at this background, it was restricted to a certain extent by prenatal corticosteroid administration. Conclusions: Prenatal corticosteroids cause reduction of premature infants’ treatment costs. The implementation of a smaller number of dexamethasone applications leads to smaller expenditures for premature infants’ treatment and care compared to those that have more dexamethasone applications. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e50458 https://doi.org/10.3897/pharmacia.67.e50458 https://pharmacia.pensoft.net/article/50458/ https://pharmacia.pensoft.net/article/50458/download/pdf/ en

10.3897/pharmacia.67.e55835 2020-10-02 pharmacia

Pharmacotherapy costs and medicines reimbursement policies of osteoporosis in the Republic of Bulgaria and Republic of North Macedonia Chakuleska,Lidija Simeonova,Rumiana Danchev,Nikolay bisphosphonate Health Insurance Fund reimbursement status Pharmacia 67(4): 199-207 The aim of the present study was to analyze and compare the number of health insured persons suffering from osteoporosis and antiosteoporotic drugs reimbursed by the National Health Insurance Funds (NHIF) in the Republic of Bulgaria (RBG) and Republic of North Macedonia (RNM) for the period 2015–2018. The reimbursement cost paid by the NHIF for the same period in both countries was surveyed. The results show an increase in both the number of patients with osteoporosis and the cost of the treatment. The most prescribed drug in R. Bulgaria is denosumab and it has the highest costs respectively, while in R.N. Macedonia the most prescribed and respectively the most expensive treatment is the bisphosphonate ibandronic acid, tablets of 150 mg. The trend of rising costs in both countries is likely to continue due to the increasing number of patients with osteoporosis. The number of patients and cost of pharmacotherapy in RNM and RBG are increasing but the reimbursement policy in RNM is more restrictive in terms of reimbursed medicines. On the other side, the RNM is with a higher level of reimbursement that might positively affect the cost of pharmacotherapy. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e55835 https://doi.org/10.3897/pharmacia.67.e55835 https://pharmacia.pensoft.net/article/55835/ https://pharmacia.pensoft.net/article/55835/download/pdf/ en

10.3897/pharmacia.67.e46865 2020-10-02 pharmacia

Prevention and treatment of osteoporosis Becheva,Maria Taneva,Daniela Osteoporosis prophylaxis medication treatment Pharmacia 67(4): 181-185 Osteoporosis is a generalized bone disease characterized by diminished bone strength with an increased risk of fractures. Osteoporosis is a major health concern, both because of the risk of potentially serious fractures and because its prevalence is increasing as the population ages. The treatment of the disease is complex and includes adherence to a particular diet, medications (hormone replacement therapy, calcium, vitamin D, etc.), kinesitherapy, physiotherapy and orthotics. To reduce osteoporosis, it is necessary to avoid the risk of fractures, to do regular physical activities, to eat bone-healthy foods, to lead a proper lifestyle with the avoidance of negative habits and to maintain a healthy weight. A person also needs to have knowledge of personal risk factors and to consult a doctor if medical treatment is to be applied. The classic therapeutic approach is with antiresorptive anti-osteoporosis agents. A promising therapeutic trend is the study of compounds with low toxicity and potential properties to influence the pathogenetic mechanisms of disease and oxidative stress, such as phytoestrogens and hormone replacement therapy, at the same time. The aim of the article is to familiarize the audience with the preventive measures and therapies applied to the treatment of osteoporosis. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Review Article text/html info:doi:10.3897/pharmacia.67.e46865 https://doi.org/10.3897/pharmacia.67.e46865 https://pharmacia.pensoft.net/article/46865/ https://pharmacia.pensoft.net/article/46865/download/pdf/ en

10.3897/pharmacia.67.e37433 2020-10-02 pharmacia

Identification and quantitative analysis of furostanol glycosides in caltrop Burda,Nadiia Zhuravel,Iryna Dababneh,Moeen F. Kotov,Andrii Kotova,Elina Popyk,Andrii caltrop herb TLC UV-vis spectrophotometry Pharmacia 67(4): 187-191 This study describes the identification and quantitative determination of furostanol glycosides in caltrop herb harvested in the fructification period. Furostanol glycosides were identified by thin-layer chromatography (TLC) and quantified by UV-vis spectrophotometry. The furostanol glycosides were visualized on the TLC plate as pink spots after treatment with dimethylamine benzaldehyde solution. UV-vis spectrophotometry quantified these substances to the amount of at least 0.4 %. The data on the identification and quantification of furostanol glycosides obtained in the course of this research was implemented in the development of the Ukrainian State Pharmacopoeia for caltrop herb. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e37433 https://doi.org/10.3897/pharmacia.67.e37433 https://pharmacia.pensoft.net/article/37433/ https://pharmacia.pensoft.net/article/37433/download/pdf/ en

10.3897/pharmacia.67.e54473 2020-10-02 pharmacia

Clinical observation of generalized sarcoidosis with damage of bones Chaplynska,Nataliia Rudnyk,Viktoriya Skrypnyk,Liubov Matkovska,Nataliia clinical case sarcoidosis bones of hands methylprednisolone Pharmacia 67(4): 193-197 Sarcoidosis is a multisystem disease of unknown etiology, at the basis of which there is an inflammatory granulation epithelioid process without a pronounced exudative reaction and without caseous necrosis. This disease has various manifestations. The aim of the study was to investigate the clinical case of generalized sarcoidosis with bone lesion in a patient M., born in 1987. There were performed X-ray examinations, computed tomography (CT), fibrobronchoscopy, determination of calcium levels, angiotensin converting enzyme (ACE), soluble IL-2 receptor in the blood. Dynamic observation was performed for 10 months. The patient started methylprednisolone therapy at a dose of 20 mg/day. Significant positive effect of this treatment was noted. Thus, when patients complain of the bone and joint system problems, examination plan should include radiological examination of thoracic organs, which will allow us to avoid late diagnosis of sarcoidosis or other multisystem diseases that may have similar clinical manifestations. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e54473 https://doi.org/10.3897/pharmacia.67.e54473 https://pharmacia.pensoft.net/article/54473/ https://pharmacia.pensoft.net/article/54473/download/pdf/ en

10.3897/pharmacia.67.e55437 2020-10-02 pharmacia

Immunomodulatory effect of melatonin supplementation in experimental diabetes Ivankiv,Yana Oleshchuk,Oleksandra M. experimental diabetes melatonin immune system Pharmacia 67(4): 223-228 Aim: To investigate the effect of melatonin on the immunomodulatory response in experimental type 1 and 2 diabetes mellitus. Methods: Experiments were performed on male rats (180–200 g), purchased from the Experimental Animal Holding,. Animals were maintained in standard diet conditions. Two pathological states were simulated on male rats: experimental type 1 and type 2 diabetes. Melatonin was introduced from 14 to 23 days of experiment intraperitoneally. Levels of immunoglobulin classes A, M and G (Ig A, M, G), circulating immune complexes (CIC), interleukin 1β (EE), interleukin 6 (IL-6), and tumor necrosis factor (TNF-a) were measured. Results: We demonstrated that melatonin in case of immune hyperactivity, can, provide a suppressive effect and is able to enhance immune reactivity under conditions of its limitation, indicating the immunostimulating activity. Furthermore, we found that administration of melatonin decreased inflammatory responses by mediating the levels of immunomodulatory factors, including TNF-α, IL-1β and IL-6. Conclusion: Melatonin is a positive regulator of immune system, may be a potential therapeutic agent, it has no reported side effects. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e55437 https://doi.org/10.3897/pharmacia.67.e55437 https://pharmacia.pensoft.net/article/55437/ https://pharmacia.pensoft.net/article/55437/download/pdf/ en

10.3897/pharmacia.67.e48634 2020-10-23 pharmacia

Bulgarian species of genus Astragalus as potential sources of mauritianin Shkondrov,Aleksandar Krasteva,Ilina Kozuharova,Ekaterina Zdraveva,Petranka Savev,Slavcho Astragalus mauritianin quantitative analysis flavonoids UHPLC-MS Pharmacia 67(4): 229-232 Mauritianin is a relatively rare flavonoid, but several studies revealed its pharmacological potential. In this study overground parts of ten Astragalus species were investigated for mauritianin content to find a reliable source of the compound. The quantity of the flavonoid in each extract was determined by a novel high performance liquid chromatography-high resolution mass spectrometry method. For the first time mauritianin is reported in A. cicer, A. onobrychis, A. glycyphyllos, A. glycyphylloides, A. corniculatus and A. ponticus. Only in A. depressus the compound was not found. Significant differences in mauritianin content (from 4 to 1642 ng/mg dry weight) of the samples were observed. Noteworthy, A. onobrychis var. chlorocarpus and A. cicer could be considered as a potential source of the compound, substituting the rare A. monspessulanus subsp. monspessulanus. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e48634 https://doi.org/10.3897/pharmacia.67.e48634 https://pharmacia.pensoft.net/article/48634/ https://pharmacia.pensoft.net/article/48634/download/pdf/ en

10.3897/pharmacia.67.e51304 2020-10-23 pharmacia

The pharmacological basis for application of cannabidiol in cancer chemotherapy Zhelyazkova,Margarita Kirilov,Bogdan Momekov,Georgi anticancer effect cannabidiol mechanism of action pharmacological interactions safety profile Pharmacia 67(4): 239-252 Chemotherapy is one of the therapeutic approaches for cancer treatment and has demonstrated great success with the introduction of selectively acting molecules against specific biomarkers of some types of tumors. Despite this success there is a large unmet need for novel therapies that provide effective control on the progression of advanced or drug-resistant cancer diseases. In this review, we briefly summarized our knowledge of cannabinoids and the endocannabinoid system, as possible agents for cancer therapy. We analyzed the anticancer properties and mechanism of action of cannabidiol (CBD), the main non-psychoactive cannabinoid received from hemp of Cannabis plant. Despite of data for pleiotropic effects of CBD, we here present the results for the efficacy of CBD in the modulation of different stages of cancer development. The analysis of the anticancer properties of CBD is made in relation to the proposed or newly discovered molecular targets of action. Thereafter, we consider the specific effects of CBD on primary tumors, their invasiveness and metastases, whether the influence on identified tumor markers in different types of tumors reflect the therapeutic potential of CBD. The studies reviewed herein indicate that CBD elicit activity through the cannabinoid receptor dependent and independent pathways. The processes such as ceramide production, ER-stress, autophagy and apoptosis, angiogenesis and matrix remodeling also appear to regulate the anticancer activity of CBD. So, the pharmacological basis for therapeutic application of CBD is constructed on the scientific data for its antitumor activity, extensively provided studies in vitro and in vivo in animal tumor models, and available data on the safety profile of clinically approved CBD products. We also try to reduce the deficits of our understanding in relation of pharmacological synergistic interactions of CBD with cytostatic drugs, where data remains limited. It is recognized that more studies for defining the specific molecular and signaling mechanisms of anticancer action of cannabinoids, particularly CBD, requires further evaluation. We believe that the therapeutic advantages of CBD are associated not only with its non-psychoactive behavior, but also are related to its influence on the important biochemical pathways and signal molecules, defining the genome instability and specific changes of the malignant tumor cells. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Review Article text/html info:doi:10.3897/pharmacia.67.e51304 https://doi.org/10.3897/pharmacia.67.e51304 https://pharmacia.pensoft.net/article/51304/ https://pharmacia.pensoft.net/article/51304/download/pdf/ en

10.3897/pharmacia.67.e58024 2020-10-23 pharmacia

The role of immunostimulants in the complex therapy of Covid 19 – a clinical case Kobakova,Yozlem Ali Kobakova,Yozlem Ali Atanasov,Petar Ivanova,Stefka Obreshkova,Danka immunomodulators proteolytics pneumonia SARS-CoV-2 treatment Pharmacia 67(4): 233-237 The aim of current study was the investigation of complex treatment including nutritional supplement with recognized antioxidant and immunomodulatory properties (malic, glycyrrhizic, ascorbic and folic acids, glucosamine, arginine, glycine, calcium pantothenate, cyanocobalamine, zinc sulfate, pyridoxal) and purely plant systemic protease supplement (Serrapeptase, Bromelaim, Boswellia, Uncaria tomentosa, Quercetin) as a strategy against Covid 19. A clinical case of a 33-year-old patient treated in Internal Clinic Diseases ”Pirogov” against atypical bilaterally viral pneumonia with RT-PCR proven coronavirus have been presented. A complex treatment strategy was applied: Doxycycline, Amikacin sulfate, food additive containing malic and glycyrhizic acids, aminoacids, B-vitamins, antioxidants, proteolytic agent, Methylprednisolone, anticoagulant: Nadroparin calcium, hepatoprotector: Ademethionine. After 16 days hospitalization and two negative RT-PCR tests the patient was discharged in improved condition and home treatment with Levofloxacin hemihydrate, vitamins, probiotics, immunomodulatory and proteolytic products for one month was recommended. Immunostimulating, proteolytic and other products have an important role in complex treatment. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Review Article text/html info:doi:10.3897/pharmacia.67.e58024 https://doi.org/10.3897/pharmacia.67.e58024 https://pharmacia.pensoft.net/article/58024/ https://pharmacia.pensoft.net/article/58024/download/pdf/ en

10.3897/pharmacia.67.e38078 2020-10-23 pharmacia

Efficacy of the N-acetylglucosamine in experimental therapy of chronic kidney disease Shebeko,Sergii Zupanets,Igor Otrishko,Inna chronic kidney disease intramuscular administration N-acetylglucosamine rats Pharmacia 67(4): 253-259 The efficacy of N-acetylglucosamine in rats with chronic kidney disease is described in this article. The results of the study show that N-acetylglucosamine significantly increased (p<0.05) the excretion of nitrogen compounds (creatinine by 100.4% and urea by 46.6%) and as a result de-creased the level of azotemia. The intensity of free radical oxidation was significantly decreased (p<0.05) (blood conjugated dienes by 32.9%, blood thiobarbituric acid reactive substances – by 14.1%, kidney conjugated dienes – by 40.1% and kidney thiobarbituric acid reactive substances – by 26.3%) and the balance of kidney antioxidant system was restored. N-acetylglucosamine was significantly superior (p<0.05) to comparator quercetin in renal excretory function and nitro-gen metabolism by the most of indicators and was not inferior to the influence on the free radical oxidation and kidney oxidative stress. Thus, N-acetylglucosamine is advisable to further experimental studies at i.m. administration as a chronic kidney disease treatment. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e38078 https://doi.org/10.3897/pharmacia.67.e38078 https://pharmacia.pensoft.net/article/38078/ https://pharmacia.pensoft.net/article/38078/download/pdf/ en

10.3897/pharmacia.67.e57134 2020-10-26 pharmacia

Pharmacovigilance: procedures for uniform assessment of periodic safety update reports and their implementation in national settings. Focus on analgesics Koleva,Kalina Todorova,Lyubina Marchev,Stanislav Vlaskovska,Mila Nikolov,Rumen NSAIDs opioids regulatory requirements discrepancies Pharmacia 67(4): 283-288 Pharmacovigilance activities are of vital importance for ensuring effective and safe medicinal products. In order to clarify to which extent marketing authorisation holders (MAHs) meet the requirements of the Law and the Directives related to this activities, we conducted a systematic search among the procedures submitted to the Bulgarian Drug Agency (BDA) related to the implementation of the decisions of the Pharmacovigilance Committee and the Co-ordination Group for Mutual Recognition and Decentralised Procedures – Human (CMDh) for a period of 6 years. The results of the study showed significant discrepancies between regulatory requirements and the behavior of the MAH at the national level. This could be a serious problem, as inadequate or late implementations of the PRAC (Pharmacovigilance Risk Assessment Committee)/CMDh/EC recommendations can lead to untimely informing of healthcare professionals and patients about potential safety concerns and risks related to the use of medicinal products. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e57134 https://doi.org/10.3897/pharmacia.67.e57134 https://pharmacia.pensoft.net/article/57134/ https://pharmacia.pensoft.net/article/57134/download/pdf/ en

10.3897/pharmacia.67.e56880 2020-10-26 pharmacia

Experimental research of garden spinach extract as a potential anabolic medicinal product Nykyforuk,Andriy Fira,Liudmyla Lykhatskyі,Petro Pyda,Victor spinach garden leaves dry extract food deprivation protein metabolism spontaneous diuresis oxidative stress rats Pharmacia 67(4): 277-282 Disorders of protein metabolism – one of the pathologies, the treatment of which is an urgent problem of modern medicine and pharmacy. The importance of the problem is stipulated due to the prevalence of diseases that are accompanied by a violation of protein metabolism in the body. Restoration of protein resources during such conditions requires adequate intake of structural components from the outside – proteins, amino acids and other biologically active substances-correctors of protein metabolism. In recent decades, much attention has been paid to the discoveries of anabolic agents of natural origin, especially from plants. We conducted research on the study of the anabolic and antioxidant properties of dry extract of spinach garden leaves on the model of food deprivation in rats. Established, that the dry extract at the dose of 100 mg/kg body weight of animals prevents the development of organic disorders of protein metabolism, oxidative stress, prevents a sharp decrease in body weight and slows down the generalized catabolism caused by starvation in rats. Under the influence of the extract on the model of food deprivation, the diuretic function of the kidneys is preserved at the physiological level. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e56880 https://doi.org/10.3897/pharmacia.67.e56880 https://pharmacia.pensoft.net/article/56880/ https://pharmacia.pensoft.net/article/56880/download/pdf/ en

10.3897/pharmacia.67.e57794 2020-10-26 pharmacia

The role of the State Drug Formulary of Ukraine in providing rational pharmacotherapy for elderly patients Nastyukha,Yuliya Kostyana,Kateryna Maksymovych,Maria Boretska,Olga elderly potentially inappropriate medication pharmaceutical care State Drug Formulary Pharmacia 67(4): 261-268 Applying the Classification for Drug-Related Problems (DRPs) of the Pharmaceutical Care Network Europe (V 9.00, 2019) allowed to systematize the information on the use of drugs in elderly patients given in the Annex of the State Drug Formulary of Ukraine. As a result of this work, special warnings and recommendations of the State Drug Formulary were presented together with the possible causes for potential DRPs, which they allow to prevent. The lists of potentially inappropriate medications (PIMs) for the elderly (n = 98), drugs the dosage of which in patients of this age group should be adjusted (n = 127), and drugs that need monitoring (n = 108) were formed. The obtained results can serve as a basis for the development of a specialized geriatric tool to ensure rational pharmacotherapy, in particular in the provision of pharmaceutical care. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e57794 https://doi.org/10.3897/pharmacia.67.e57794 https://pharmacia.pensoft.net/article/57794/ https://pharmacia.pensoft.net/article/57794/download/pdf/ en

10.3897/pharmacia.67.e55159 2020-10-26 pharmacia

The trends of assisted reproductive technologies and cost for ovarian stimulation protocols in Ukraine Zaliska,Olha Stasiv,Khrystyna Maksymovych,Nataliia Hrynkiv,Yaryna infertility assisted reproductive technologies cost ovarian stimulation affordability Pharmacia 67(4): 269-276 The prevalence of infertility has risen 2.9 times in recent years in Ukraine. The use of assisted reproductive technologies (ART) is needed. The State program for infertility treatment by budget funds was approved in Ukraine since 2004. However, funding for this program is enough only for 500–600 cycles per year, but ART centers conducted more than 27,000 cycles in 2018. This means that many women have to pay out-of-pockets. Our research has shown that between 2000 and 2018, the number of ART clinics and the number of cycles, pregnancies, and children born increased significantly in Ukraine. The rate of ART cycles per 1 million population in Ukraine has increased from 226.9 to 655.3, but it is lower than the WHO recommended rate 800–1000 cycles per 1 million population. Changes in the structure of ART cycles for 2000–2018, the increase of ICSI, and egg donation cycles are shown. It requires an adequate supply by hormonal drugs for ovarian stimulation in ART centers. Since 2004 Ministry of Health of Ukraine annually approved the list of medicines for State program of ART. Only 8 drugs were purchased by the state funds, which amounted for USD 227 438 in 2017, 2018. A retrospective analysis of drug prescriptions in short and long stimulation protocols was performed. The frequency of drug prescriptions according to the ATC-classification based on medical records was determined, all prescriptions were accordance with the requirements of ART treatment standards in Ukraine. The costs of the three hormonal stimulation schemes, which were the most prescribing in ART center, were calculated. It was found that costs for hormonal schemes increased by 22–54% during 2015–2020, it significantly reduces the availability and affordability of ART for the population in Ukraine. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e55159 https://doi.org/10.3897/pharmacia.67.e55159 https://pharmacia.pensoft.net/article/55159/ https://pharmacia.pensoft.net/article/55159/download/pdf/ en

10.3897/pharmacia.67.e54777 2020-11-03 pharmacia

The relevance of training specialists in the Health Technology Assessment in the world and Ukraine Kotvitska,Alla Nemchenko,Alla Nazarkina,Viktoria educational program health technology assessment training of specialists Pharmacia 67(4): 295-301 Based on generalization of the modern international experience the areas of development of the methodology for training specialists in Health Technology Assessment (НТА) system have been determined; they reflect the categories of information consumers, the goal, methods, organizers and intermediaries of knowledge transfer. The analysis of the market of educational services, educational curricula and Internet resources in the field of НТА has been conducted. Based on the results they are classified into 4 groups – academic programs, professional improvement and continuing education, short-term training and information for various target groups, online courses at the pre-graduate level and for postgraduate training. According to the all-Ukrainian survey the necessity for training specialists in the field of “expert in assessing health technologies” has been confirmed. Based on the information needs, requirements of stakeholders and international experts in НТА a qualification characteristic, and on its basis – the professional academic program, have been developed at the National University of Pharmacy, as well as training of the corresponding specialists has been started. In the future, it is planned to expand educational services and conduct short-term courses and workshops, as well as online training of specialists in НТА at the postgraduate level. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e54777 https://doi.org/10.3897/pharmacia.67.e54777 https://pharmacia.pensoft.net/article/54777/ https://pharmacia.pensoft.net/article/54777/download/pdf/ en

10.3897/pharmacia.67.e57752 2020-11-03 pharmacia

What does self-medication counseling in Bulgarian community pharmacies look like – a field study Lebanova,Hristina Balkanski,Stefan Naseva,Emilia Getov,Ilko self-medication pharmaceutical counseling over-the-counter medicines Pharmacia 67(4): 289-293 The aim of the study is to identify the current practices of self-medication in Bulgaria, estimate the extent patients are influenced by information about the safety of OTC products and pharmacists’ role and behavior in the process. An anonymous, questionnaire-based, descriptive study was carried out among 280 pharmacists. The majority of the patients (92.6%) ask for pharmacists’ advice before buying OTC products. Most often patients need OTC drugs for mild conditions (80.7%), to save time (63.9%), and because they are unable to consult a physician (61.9%). The medium duration of consultation for an OTC product is between 5 and 10 minutes. The main barriers hindering the process are unwillingness from the patient (72.5%), lack of time (27.5%), and lack of confidentiality (26.6%). OTC medicines are considered safer than prescription-only medicines by pharmacists. Pharmacists could substantially contribute to rational self-medication and alleviate the burden on healthcare systems. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e57752 https://doi.org/10.3897/pharmacia.67.e57752 https://pharmacia.pensoft.net/article/57752/ https://pharmacia.pensoft.net/article/57752/download/pdf/ en

10.3897/pharmacia.67.e47298 2020-11-06 pharmacia

Aryl hydrocarbon receptors as potential therapeutic targets Andreeva-Gateva,Pavlina Bakalov,Dimitar Sabit,Zafer Tafradjiiska-Hadjiolova,Radka dioxin indoles toxicology neuroprotection Pharmacia 67(4): 311-315 Aryl hydrocarbon receptors (AhR) are regulators of the expression of cytochrome P-450 isoforms, mediating a wide variety of the effects of substances from the endogenous or exogenous origin, including those produced from the microbiome. An exciting new aspect of their activity is their localization in the brain and their potential to modulate the action of the immune system. AhR is emerging as an essential toxicological and therapeutic target for neuromodulation. Further studies are needed for elucidating their utility as drug-targets. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Review Article text/html info:doi:10.3897/pharmacia.67.e47298 https://doi.org/10.3897/pharmacia.67.e47298 https://pharmacia.pensoft.net/article/47298/ https://pharmacia.pensoft.net/article/47298/download/pdf/ en

10.3897/pharmacia.67.e56511 2020-11-06 pharmacia

Elderly consumers’ satisfaction with the quality of community pharmacy services in Ho Chi Minh City, Vietnam: a Q-methodology study Tran,Van De Dorofeeva,Valeria V. Loskutova,Ekaterina E. Lagutkina,Tatyana P. Kosova,Irina V. Gribkova,Elena I. Galkina,Galina A. Pak,Tatiana V. Ibragimova,Alfia N. Le,Minh Hoang Cao,Thi Tai Nguyen community pharmacy elderly consumer Q-methodology satisfaction Vietnam Pharmacia 67(4): 303-309 Introduction: The purpose of this study was to understand elderly consumers’ satisfaction on the community pharmacy services in Ho Chi Minh City, Vietnam. Materials and methods: A sample of 32 consumers, aged over 60, was recruited in four pharmacies in Ho Chi Minh City, Vietnam, from December, 2017 to January, 2018. Q-methodology was used to identify the patterns of consumers’ satisfaction. Results: Two distinct patterns of elderly consumers’ viewpoints toward the community pharmacy services were identified. Elderly consumers in viewpoint 1 were satisfied with the geographic accessibility of community pharmacies. Elderly consumers in viewpoint 2 were satisfied with the affordability of medicines. However, consumers of both viewpoints expressed dissatisfaction with the pharmacy staff counseling on missed doses, storage, side effects, and interactions of medicines. Conclusion: The results from this study suggest that pharmacy staff need to spend more time for consultations on proper medication use with elderly consumers. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e56511 https://doi.org/10.3897/pharmacia.67.e56511 https://pharmacia.pensoft.net/article/56511/ https://pharmacia.pensoft.net/article/56511/download/pdf/ en

10.3897/pharmacia.67.e56112 2020-11-26 pharmacia

Toxicological and pharmacological profile of Amanita muscaria (L.) Lam. – a new rising opportunity for biomedicine Voynova,Maria Shkondrov,Aleksandar Kondeva-Burdina,Magdalena Krasteva,Ilina Amanita muscaria muscimol ibotenic acid Pharmacia 67(4): 317-323 Amanita muscaria, commonly known as fly agaric, is a basidiomycete. Its main psychoactive constituents are ibotenic acid and muscimol, both involved in ‘pantherina-muscaria’ poisoning syndrome. The rising pharmacological and toxicological interest based on lots of contradictive opinions concerning the use of Amanita muscaria extracts’ neuroprotective role against some neurodegenerative diseases such as Parkinson’s and Alzheimer’s, its potent role in the treatment of cerebral ischaemia and other socially significant health conditions gave the basis for this review. Facts about Amanita muscaria’s morphology, chemical content, toxicological and pharmacological characteristics and usage from ancient times to present-day’s opportunities in modern medicine are presented. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Review Article text/html info:doi:10.3897/pharmacia.67.e56112 https://doi.org/10.3897/pharmacia.67.e56112 https://pharmacia.pensoft.net/article/56112/ https://pharmacia.pensoft.net/article/56112/download/pdf/ en

10.3897/pharmacia.67.e35069 2020-11-27 pharmacia

Correction of disordered oral immunity in children affected by dental caries with herbal immune modulator “Esberitox” Cherepyuk,Olena Oktysyuk,Yuriy Bazalytska,Aleksandra Rozhko,Mykola children dental caries lysozyme oral liquid secretory immunoglobulin A Pharmacia 67(4): 347-350 Dental caries is the most prevalent pathological condition in the child population of Ukraine. Despite the achievements of medical science, dental caries in children remains one of the most actual problems nowadays. Epidemiological investigations conducted in different regions of Ukraine demonstrate that 62% of children have decay and in many parts of the country the statistic is even higher up to 96.5% when the intensity of carious damage fluctuates between 3.2 to 7.2 teeth. This article reflects the results of the study regarding correction of disordered oral immunity indexes by immune modulator “Esberitox” in children affected by different caries activity. We have confirmed the high efficiency of the recommended scheme of caries prophylaxis that is proved by positive dynamic of oral immunological indexes observed 24 month after the beginning of the research. There was a certain rise of lysozyme by about 21.1% and s-IgA has increased by 28% in children from prophylactic groups in comparison with control groups. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e35069 https://doi.org/10.3897/pharmacia.67.e35069 https://pharmacia.pensoft.net/article/35069/ https://pharmacia.pensoft.net/article/35069/download/pdf/ en

10.3897/pharmacia.67.e47528 2020-11-27 pharmacia

Study on the influence of technological factors on drug loading of poorly water-soluble drug on MCM-41 mesoporous carrier Popova,Teodora Voycheva,Christina Tzankov,Borislav drug loading indomethacin MCM-41 technological factors Pharmacia 67(4): 351-356 The present study explored solvent impregnation drug loading process of the poorly soluble non-steroid anti-inflammatory drug indomethacin on MCM-41 type mesoporous silica carrier. Different technological factors that can influence drug-loading process as time of reaction, temperature, use of non-solvent as well as different ratios between drug and MCM-41 were studied. TEM and DLS were used to characterize physicochemical properties of obtained particles. The influence of drug-loading rate on dissolution process were studied using in-vitro release tests. Our results established that changes in explored technological factors could lead to different indomethacin loading. Moreover, the in-vitro release tests proved that drug loading rate had a direct influence on indomethacin release from MCM-41 particles. Our finding suggested that by tuning the main technological factors it would be possible different drug delivery systems with different drug loading rate to be obtained. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e47528 https://doi.org/10.3897/pharmacia.67.e47528 https://pharmacia.pensoft.net/article/47528/ https://pharmacia.pensoft.net/article/47528/download/pdf/ en

10.3897/pharmacia.67.e54170 2020-11-27 pharmacia

Determination of the optimum extraction regime of reducing compounds and flavonoids of Primula denticulata Smith leaves by a dispersion analysis Budniak,Liliia Vasenda,Marjana Marchyshyn,Svitlana Kurylo,Khrystyna Primula denticulata Smith dispersion analysis flavonoids reducing compounds Pharmacia 67(4): 373-378 Herbal medicines are widely used in the complex treatment of various diseases. Therefore, theoretical and practical interest is the in-depth study of drumstick primrose (Primula denticulata Smith). The study aimed to determine the optimal extraction mode of flavonoids and reducing compounds of drumstick primrose leaves. The concentration of ethanol, the ratio of raw materials and extractant, and extraction method were studied by dispersion analysis. This allowed reducing the number of experiments from 64 to 16. To obtain the alcohol extract of drumstick primrose leaves with the highest content of reducing compounds and flavonoids, found that maceration is the optimal method of extraction, the ratio of raw materials to extractant should be 1 to 5 and 40% ethanol is the most appropriate extractant. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e54170 https://doi.org/10.3897/pharmacia.67.e54170 https://pharmacia.pensoft.net/article/54170/ https://pharmacia.pensoft.net/article/54170/download/pdf/ en

10.3897/pharmacia.67.e52262 2020-11-27 pharmacia

The study of pharmaceutical specialists’ thoughts concerning self-regulation of pharmaceutical activity in Ukraine Pankevych,Ostap Hromovyk,Bohdan Horilyk,Artem Bilushchak,Halyna Self-regulation pharmaceutical activities pharmaceutical practice pharmaceutical societies public organizations Ukraine Pharmacia 67(4): 379-382 The aim of our study was to investigate the views of pharmacists on understanding the nature and necessity of implementing the self-regulation of pharmaceutical practice in Ukraine. We conducted an anonymous questionnaire survey among pharmaceutical specialists (n = 827) from the majority (16 out of 25) of the regions controlled by the Ukrainian government during the period from October till December 2018. This survey revealed lack of pharmacists’ understanding the concept of self-regulation of pharmaceutical practice. On the one hand, most respondents do not oppose the implementing of self-regulation and don’t reject exclusive membership in self-regulated pharmaceutical organizations for only pharmaceutical specialists, but on the other hand the survey showed a low willingness voluntarily to become a member of such organizations and also low level of knowledge of self-regulation process. This indicates the need to update the self-regulation process through providing training activities for pharmacists, the development of legal framework and the government’s assistance of self-regulation of pharmaceutical practice. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e52262 https://doi.org/10.3897/pharmacia.67.e52262 https://pharmacia.pensoft.net/article/52262/ https://pharmacia.pensoft.net/article/52262/download/pdf/ en

10.3897/pharmacia.67.e58392 2020-11-27 pharmacia

In-vitro anti-diabetic activity and in-silico studies of binding energies of palmatine with alpha-amylase, alpha-glucosidase and DPP-IV enzymes Okechukwu,Patrick Sharma,Mridula Tan,Wei Hui Chan,Hor Kuan Chirara,Kavita Gaurav,Anand Al-Nema,Mayasah Alpha-glucosidase alpha-amylase dipeptidyl peptidase-IV diabetes mellitus palmatine Pharmacia 67(4): 363-371 Palmatine a protoberberine alkaloid has been previously reported to possess in vivo antidiabetic and antioxidant property. The aim of the experiment is to evaluate the in vitro antidiabetic activity and in-silico studies of the binding energies of Palmatine, acarbose, and Sitagliptin with the three enzymes of alpha-amylase, alpha-glucosidase, and dipeptidyl peptidase-IV (DPP-IV). The in vitro antidiabetic study was done by evaluating the inhibitory effect of palmatine on the activities of alpha-amylase, alpha-glucosidase, and DPP-IV. Acarbose, and sitagliptin was used as standard drug. The molecular docking study was performed to study the binding interactions of palmatine with alpha-glucosidase, a-amylase, and DPP-IV. The binding interactions were compared with the standard compounds Sitagliptin and acarbose. Palmatine with IC50 (1.31 ± 0.27 µM) showed significant difference of (< 0.0001) higher inhibiting effect on alpha-amylase and weak inhibiting effect on alpha-glucosidase enzyme with IC50 (9.39 ± 0.27 µM) and DPP-IV with IC50 (8.7 ± 1.82 µM). Palmatine possess inhibition effect on the three enzymes. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e58392 https://doi.org/10.3897/pharmacia.67.e58392 https://pharmacia.pensoft.net/article/58392/ https://pharmacia.pensoft.net/article/58392/download/pdf/ en

10.3897/pharmacia.67.e51334 2020-11-27 pharmacia

The invasive alien species Amorpha fruticosa in Bulgaria and its potential as economically prospective source of valuable essential oil Kozuharova,Ekaterina Benbassat,Niko Ionkova,Iliana Amorpha fruticosa chemical composition essential oil yield Pharmacia 67(4): 357-362 The high tolerance of various habitat conditions and potent propagation ability of Amorpha fruticosa L. (Fabaceae) promote its aggressive invasive behaviour. The aim of this study is to evaluate 1) several populations of this plant by the potential yield of the fruit, 2) the approximate yield of the essential oils, and 3) composition of the essential oil. The potential yield of fruit is evaluated based on extrapolations of weight and number of fruits per infrutescence, number of infrutescences per plant and number of individuals per population. Steam extraction of the essential oil was performed and GS/MS analysis of the composition of the essential oil. The populations on our key plots are big enough for harvesting with fruit/infrutescence 152 ±15 (n = 20) and infrutescences/shrub 436 ±157 (n = 20). The yield is 0.83 ml/100g. We identified 22 components with major constituents caryophyllene (17.64%) α-guaiene (14.70%), naphthalene (6.75%), γ-muurolene + (5.98%). info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e51334 https://doi.org/10.3897/pharmacia.67.e51334 https://pharmacia.pensoft.net/article/51334/ https://pharmacia.pensoft.net/article/51334/download/pdf/ en

10.3897/pharmacia.67.e57242 2020-11-27 pharmacia

Application of membrane filters in determination of the adsorption of tetracycline hydrochloride on graphene oxide Dedic,Mirza Gutic,Sanjin Gicevic,Armina Becic,Ervina Imamovic,Belma Markovic,Damir Ziga-Smajic,Nermina spectrophotometry antibiotics purifiers nanomaterial Pharmacia 67(4): 339-345 This paper shows the use of membrane filters in adsorption of solution of tetracycline hydrochloride on graphene materials. The adsorption process was monitored at different wavelengths, different pH values ​​at certain time intervals. The absorbances of the solutions were measured by UV-Vis spectrophotometry at two wavelengths (275 nm and 356 nm), and three pH values (pH 4, pH 7 and pH 10) every 90 minutes for 6 hours of monitoring, with constant stirring in an ultrasonic bath. The results showed decrease in absorbance at both wavelength and in all three pH values which proved the adsorption of tetracycline hydrochloride on GO and rGO. The largest decrease in absorbance was 98.1%. The most suitable pH value for adsorption was pH 4. This paper used a unique approach to filtration through membrane filters, which in the future could lead to the development of membrane filters based on graphene materials. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e57242 https://doi.org/10.3897/pharmacia.67.e57242 https://pharmacia.pensoft.net/article/57242/ https://pharmacia.pensoft.net/article/57242/download/pdf/ en

10.3897/pharmacia.67.e53842 2020-11-27 pharmacia

Antiviral properties of chalcones and their synthetic derivatives: a mini review Marinov,Radoslav Markova,Nadezhda Krumova,Stefka Yotovska,Kamelia Zaharieva,Maya Genova-Kalou,Petia antiviral effect chalcones in vitro synthetic derivatives Pharmacia 67(4): 325-337 Chalcones (natural or synthetic derivatives) are aromatic ketones possessing a central backbone that form a core for variety important compounds with different substitutions. Recent scientific advances show that chalcones exhibit different bio-medical activities, including antiviral, which is related to the variety substitutions. This review provides general information on the origin, sources, virucidal and direct antiviral properties of chalcones in vitro, as well as a brief overview of the possible application and molecular modes of action of these compounds. The antiviral effect of chalcones probably results from the disruption of the different stage of viral replication cycle, inhibition of viral or cell enzymes, induction of apoptosis and others. Structural requirements for antiviral activities vary according to the mechanisms of action. Based on the published information, it could be considered that synthetic chalcones are very perspective antiviral candidates and deserve further studies for elucidating of their pharmacological potential. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Review Article text/html info:doi:10.3897/pharmacia.67.e53842 https://doi.org/10.3897/pharmacia.67.e53842 https://pharmacia.pensoft.net/article/53842/ https://pharmacia.pensoft.net/article/53842/download/pdf/ en

10.3897/pharmacia.67.e57981 2020-11-27 pharmacia

Simple RP-HPLC method for Aceclofenac quantitative analysis in pharmaceutical tablets Sharmin,Suriya Sohrab,Md. Hossain Moni,Fatema Afroz,Farhana Rony,Satyajit Roy Akhter,Shammi Aceclofenac Octylsilyl column 10 mM Phosphate Buffer Method validation Robustness Pharmacia 67(4): 383-391 A reverse phase liquid chromatographic method for estimation of Aceclofenac in bulk drug and tablet dosage form was developed and validated. The chromatographic conditions to achieve the highest performance parameters using octylsilyl column with guard filter were optimized. The separation was carried out using a mobile phase containing 10 mM Phosphate Buffer, pH 2.1 and methanol (30:70% v/v) pumped at a flow rate of 1.0 mL/min with detection at 272 nm. The method was shown to be linear in 19.8–148.5 μg/mL concentration range (regression coefficient of 0.999). The limit of detection (LOD) and limit of quantification (LOQ) was found to be 0.0692 μg/mL and 0.2076 μg/mL, respectively. The accuracy of the method was assessed by adding fixed amount of pre-analyzed sample to different standard solutions (80%, 100%, and 120% of the tested concentration) in triplicate. The percentage mean recoveries were 97.91% to 100.39% with %RSD values of 0.64–0.79. The method was found to be precise with %RSD value of 1.13 and 1.60 for intraday and interday precision study, respectively. The method specificity and robustness were also established. New and sensitive HPLC method for estimation of Aceclofenac has been developed, in respect to the reviewed analytical methods. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e57981 https://doi.org/10.3897/pharmacia.67.e57981 https://pharmacia.pensoft.net/article/57981/ https://pharmacia.pensoft.net/article/57981/download/pdf/ en

10.3897/pharmacia.67.e59319 2020-11-27 pharmacia

Evaluation for the level of knowledge about herbal medicine use within people and university students in Mutah region Al-Nadaf,Afaf Awadallah,Areeg Awareness Attitude Herbal medicine Herb-Drug interaction Mutah. Pharmacia 67(4): 397-403 Background: Conventional medication; traditional or folk medicine as well as herbal medicines; have been widely used since ancient times. In Jordan traditional medicines are freely available and self-prescribed as well. No previous study has investigated believes and knowledge with regards to herb-drug interaction in Mutah geographical in Jordan. Objectives: This study aims to investigate and evaluate knowledge and attitude about self-medication using herbal medicine and its drug interaction among the public in Mutah. Materials and methods: A questionnaire-based survey conducted. Survey took place in different locations in the Mutah region in Al-Karak city from Jordan, during December 2017 and January 2018. Data analyzed by SPSS. Results: The majority of responders (82%) use self-prepared herbal preparation. While (56%) go for self-medication rather than visiting a physician. About (63%) participants responded that physicians didn’t ask them about if they use any herbal medication and about (50%) not willing to tell their physician about their self-medication. Knowledge about herbs gained from the family in the first place (38%); TV (21%) and friends (15%). Almost (79%) responders agree that herbs are safer and easier to be used compared to physician-prescribed medicine. Conclusion: A high belief in herbal therapy use. Responders gain their knowledge primarily from their families which they obtain their knowledge primarily from their tradition. They are not aware of their interaction with other therapies. Care-givers in this region should be aware of the high percentage of herbal medicine use and are encouraged to discuss potential use with their patients to avoid future complications. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e59319 https://doi.org/10.3897/pharmacia.67.e59319 https://pharmacia.pensoft.net/article/59319/ https://pharmacia.pensoft.net/article/59319/download/pdf/ en

10.3897/pharmacia.67.e52568 2020-11-27 pharmacia

Determination of Candida albicans proteins concentration by enzyme-linked immunosorbent assay method at subcutaneous introduction in candidiasis therapy Rybalkin,Mykola Khokhlenkova,Natalia Azarenko,Julia Diadiun,Tetiana Kovalenko,Svitlana antigen candidiasis dose immunity therapy vaccine Pharmacia 67(4): 393-396 Therapeutic effect of C. albicans proteins in concentrations 1, 2, 3, 4 and 5 mg/ml has been examined in white mice. Animals were infected i.p. with suspension of C. albicans strain CCM 335–867 in the amount of 20 million cells per 1 ml volume. After 5 days and repeatedly after 14 days mice were injected s.c. in the upper part of right hind paw with proteins of Candida cells of volume 0.2 ml. 14 days after each injection, the determination of the animal body protective functions has been carried out by the titer of specific antibodies during immunoassay. According to the data obtained, it has been found that in the s.c. administration, after the first and second injection with C. albicans protein of concentration 1, 2, 3, 4 and 5 mg/ml antibody titers increased 2 times, indicating that there is no stimulation of immune protection. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2020 Research Article text/html info:doi:10.3897/pharmacia.67.e52568 https://doi.org/10.3897/pharmacia.67.e52568 https://pharmacia.pensoft.net/article/52568/ https://pharmacia.pensoft.net/article/52568/download/pdf/ en

10.3897/pharmacia.68.e53631 2021-01-07 pharmacia

Novel HPLC-UV method for simultaneous determination of valsartan and atenolol in fixed dosage form; Study of green profile assessment Peleshok,Kateryna Piponski,Marjan Ajie,Elizabeth Adaeze Poliak,Olha Zarivna,Nadiya Denefil,Olha Logoyda,Liliya Valsartan Atenolol HPLC-UV Method Development Validation Green chemistry Pharmacia 68(1): 43-51 Aim of this work was to develop the first simple, rapid, green, economical and selective HPLC method for simultaneous quantification of the cited drugs in their challenging binary mixture. The work was motivated by the global trends towards sustainable chemistry in designing eco-friendly mobile system without affecting the analysis parameters. The proposed method was subjected to a greenness profiles using some metrics as Eco-scale. Materials and methods. This was accomplished under the following chromatographic conditions: HPLC column Discovery C18 (4.6 mm i.d. × 150 mm, 5 μm), column temperature 30 °C, flow rate 1.0 mL/min, mobile phase composed of 20% acetonitrile, 80% of 0.16% ammonium acetate and 0.2% of 1.5 M tetramethylammonium hydroxide (V/V) and signal monitoring at a wavelength of 225 nm and 237 nm. Results. A conventional mixture of acetonitrile and 0.16% ammonium acetate was tried in different ratios, but the drugs were not well separated. The shortest aliphatic chain cationic ion pair reagent tetramethylammonium hydroxide should not be exchanged with other type similar with this, like tetramethylammonium hydrogen sulfate, it did not work to our experiments. Increasing salt concentration, ammonium acetate, more than 0.2%, pushes the peak of atenolol closer to dead volume, which is negative. Atenolol in their methods for multicomponent mixtures elutes in dead volume, or when retained longer, much stronger, hydrophobic mobile phase should be used if valsartan should be seen in same chromatogram at dissent time. The 237 nm can be chosen as compromise signal for nearly equal peaks height with high sensitivity is not essential. The 225 nm signal shows much higher sensitivity for atenolol and less increase for valsartan peaks, which can be used when higher sensitivities will be essential. Linearity was examined and proven at different concentration levels in the range of working concentration of valsartan (0.16–0.96 mg/mL) and atenolol (0.2–1.20 mg/mL). The high value of recoveries obtained for valsartan and atenolol indicates that the proposed method was found to be accurate. The results of proposed method found to be an excellent green analysis with a score of 84. Conclusion. A new fast, simple and green, but selective, accurate, precise and robust HPLC-UV method for simultaneous determination of valsartan and atenolol in newly formulated dosage form was developed and many possible variations of the same were suggested. The developed method for the simultaneous quantification of valsartan and atenolol in their challenging binary mixture offers simplicity essential for quality control of a large number of samples in short time intervals, which is necessary for routine analysis. The method was subjected to greenness profile assessment. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2021 Research Article text/html info:doi:10.3897/pharmacia.68.e53631 https://doi.org/10.3897/pharmacia.68.e53631 https://pharmacia.pensoft.net/article/53631/ https://pharmacia.pensoft.net/article/53631/download/pdf/ en

10.3897/pharmacia.68.e52119 2021-01-07 pharmacia

Method development and validation for the determination of residual solvents in quinabut API by using gas chromatography. Message 2 Golembiovska,Оlena Voskoboinik,Oleksii Berest,Galina Kovalenko,Sergiy Logoyda,Liliya Gas Chromatography Quinabut Residual Solvents Validation Pharmacia 68(1): 53-59 Aim. The aim of study was to develop and validate a simple, precise and accurate method using gas chromatography for analysis of residual solvents – acetone and 2-propanol – in quinabut API. Materials and methods. All experiments were performed on a gas chromatographic system equipped with FID detector (Shimadzu GC System) using the DB-624 (30 m × 0.32 mm ID, 3.0 μm film sickness) column as stationary phase. Nitrogen was used as carrier gas with flow rate 7.5 mL/ min. Split ratio was 1:5, injector temperature was 140 °C, detector temperature was 250 °C, oven temperature was programmed from 40 °C (2 min) to 50 °C at 1 °C/min and then increased at a rate of 15 °C/min up to 215 °C; and maintained for 2 min. All solutions were prepared using water as diluent. Results. This proposed method is assessed for separation of residual solvent from quinabut with quantification. The obtained results are compared with the corresponding specified limits of ICH standard guidelines. The method validation was done by evaluating specificity, limit of detection (LOD) and limit of quantitation (LOQ), linearity, accuracy, repeatability, ruggedness, system suitability and method precision of residual solvents as indicated in the ICH harmonized tripartite guideline. The separation between acetone and 2-propanol peaks is 2.07. Hence method was found to be specific. The linear relationship evaluated across range of 15 to 180% for acetone and 2-propanol of ICH specified limit of residual solvents. The graphs of theoretical concentration versus obtained concentration are linear and the regression coefficients ‘R’ for residual solvents were more than 0.9968. The values of LOD and LOQ were much less than the lower limit of the concentration range and cannot affect the accuracy of the test. The technique was characterized by high intra-laboratory accuracy at concentrations close to the nominal acetone and 2-propanol concentration. All solutions were stable in water for at least 1 hour when stored at room temperature. Conclusion. A simple, specific, accurate, precise and rugged gas chromatography method was developed and validated for the quantification of residual solvents present in quinabut API through an understanding of the synthetic process, nature of solvents and nature of stationary phases of columns. The residual solvents acetone and 2-propanol were determined. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2021 Research Article text/html info:doi:10.3897/pharmacia.68.e52119 https://doi.org/10.3897/pharmacia.68.e52119 https://pharmacia.pensoft.net/article/52119/ https://pharmacia.pensoft.net/article/52119/download/pdf/ en

10.3897/pharmacia.68.e54581 2021-01-07 pharmacia

Prevalence of use of permitted pharmacological substances for recovery among athletes Omeragic,Elma Marjanovic,Aleksandra Djedjibegovic,Jasmina Turalic,Amila Dedic,Mirza Niksic,Haris Lugudic,Aida Sober,Miroslav athletes drugs food supplements OTC analgesic drugs sport Pharmacia 68(1): 35-42 Objectives: Food supplements and medicines which are not on the list of prohibited substances of the World Anti-Doping Agency are included in the group of permitted pharmacological agents for athlete’s recovery. The aim of this study was to describe qualitatively and quantitatively food supplements (FS) and over-the-counter drugs use among athletes in the last six month. Methods: This was a cross sectional study. Data on food supplements and the over-the-counter drugs, usage were collected during 2018 by self-administered, anonymous questionnaire. Results: A total of 112 athletes completed the survey. A total of 51.8% (n = 58) athletes reported the use of food supplements. The use of medical supplements was reported by 50.0% (n = 56) of athletes, 26.8% (n = 30) reported using ergogenic supplements, 1.8% (n = 2) using of sports food and 4.5% (n = 5) using other supplements. The use of over-the-counter drugs was reported by 35.7% (n = 40) of athletes. The over-the-counter analgesic drugs were used by 95% (n = 38) of over-the-counter drug users. Concomitant administration two or more over-the-counter drugs was reported by 40% (n = 16) athletes. Doctors and coaches had no advisory role in the use of food supplements or over-the-counter drugs. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2021 Research Article text/html info:doi:10.3897/pharmacia.68.e54581 https://doi.org/10.3897/pharmacia.68.e54581 https://pharmacia.pensoft.net/article/54581/ https://pharmacia.pensoft.net/article/54581/download/pdf/ en

10.3897/pharmacia.68.e56987 2021-01-07 pharmacia

Opportunities of information communication technologies for providing pharmaceutical care in the COVID-19 pandemic Kilova,Kristina Mihaylova,Anna A. Peikova,Lily health care pharmaceutical services pharmacist telemedicine telepharmacy Pharmacia 68(1): 9-14 This article discusses the opportunities of information and communication technologies for providing pharmaceutical care in the context of the COVID-19 pandemic. The global COVID-19 pandemic has necessitated a reorientation of the concept of providing health care to large-scale implementation of information technologies to improve the quality of medical and pharmaceutical services for the population. It had a significant impact on pharmacy, which necessitated changes in the management of pharmaceutical care for patients. Rapid and urgent measures were taken by the pharmacists, who found themselves at the forefront. Telepharmacy has proven to be a successful solution in the fight against the virus in the conditions of physical distance. The introduction of modern information and communication technologies worldwide will create significant advantages for more efficient use of resources and management of pharmaceutical care. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2021 Research Article text/html info:doi:10.3897/pharmacia.68.e56987 https://doi.org/10.3897/pharmacia.68.e56987 https://pharmacia.pensoft.net/article/56987/ https://pharmacia.pensoft.net/article/56987/download/pdf/ en

10.3897/pharmacia.68.e57819 2021-01-07 pharmacia

Quinolone resistance (qnrA) gene in isolates of Escherichia coli collected from the Al-Hillah River in Babylon Province, Iraq Al-Rafyai,Hawraa Alwash,Mourouge Al-Khafaji,Noor S.K. Aquatic environment Escherichia coli qnrA gene Quinolone resistance Pharmacia 68(1): 1-7 Aquatic environment contamination remains a foremost global public health hazards, and symbolizes a significant reservoir of releasing antibiotic resistant bacteria. The survival of Escherichia coli in aquatic environments serves as a potential reservoir of antibiotic resistance, encompassing but not restricted to a plasmid-mediated quinolone resistance (PMQR) mechanism. The current study aimed to detect the presence of the PMQR-qnrA gene in quinolone-resistant E. coli isolates. Sixty-one waterborne E. coli with known phylogroups/subgroups isolated from the Al-Hillah River in Babylon Province, Iraq, were screened for the phenotypic resistance to third-generation quinolones (levofloxacin and ofloxacin) and were further analysed for the presence of the qnrA gene using polymerase chain reaction (PCR). Fifty-seven (93.4%) of 61 E. coli isolates were levofloxacin-resistant, and 55 (90.2%) were ofloxacin-resistant. Among the 57 quinolone-resistant E. coli, 40 (65.57%) isolates were found to carry the PMQR-qnrA gene. Among the 40 qnrA-positive E. coli, 22 (36.1%) isolates were in phylogroup B2, followed by 8 (13.1%) isolates in phylogroup D, 6 (9.8%) isolates in phylogroup B1, and 4 (6.6%) isolates in phylogroup A. The presence of the PMQR-qnrA gene in E. coli belonging to phylogroup B2 and D reflects the need for routine monitoring of antibiotic resistance genes (ARGs) in the Al-Hillah River. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2021 Research Article text/html info:doi:10.3897/pharmacia.68.e57819 https://doi.org/10.3897/pharmacia.68.e57819 https://pharmacia.pensoft.net/article/57819/ https://pharmacia.pensoft.net/article/57819/download/pdf/ en

10.3897/pharmacia.68.e56715 2021-01-07 pharmacia

Analysis of carboxylic acids of Crambe cordifolia Steven Marchyshyn,Svitlana Slobodianiuk,Liudmyla Budniak,Liliia Skrynchuk,Olha Crambe cordifolia Steven fatty acids GC/MS HPLC organic acids Pharmacia 68(1): 15-21 Crambe cordifolia Steven is a perennial herb and contains many biologically active substances, including amino acids, quercetin and glycosides of kaempferol. In continuation of the investigation of these plant compounds, it is advisable to study the qualitative composition and quantitative contents of carboxylic acids. Using a HPLC method the quantitative content of the following organic acids was identified and determined: pyruvic (40.66 mg/g), isocitric (12.88 mg/g), citric (8.71 mg/g), succinic (38.03 mg/g) and malic (0.75 mg/g). Among fatty acids the saturated and unsaturated acids were determined by the GC/MS method. The content of polyunsaturated fatty acids of the total fatty acids was 56.97%, saturated – 38.53% and monounsaturated – 4.50%. Linolenic and palmitic acids dominated among the determined 7 fatty acids, their content was 9.68 mg/g (47.87%) and 4.88 mg/g (24.14%). The results of the study show that Crambe cordifolia Steven leaves is a source of carboxylic acids. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2021 Research Article text/html info:doi:10.3897/pharmacia.68.e56715 https://doi.org/10.3897/pharmacia.68.e56715 https://pharmacia.pensoft.net/article/56715/ https://pharmacia.pensoft.net/article/56715/download/pdf/ en

10.3897/pharmacia.68.e56543 2021-01-07 pharmacia

Synthesis of new series of pyrimidine nucleoside derivatives bearing the acyl moieties as potential antimicrobial agents Bulbul,Md Z.H. Chowdhury,Tasneem S. Mlisbah,Md M.H. Ferdous,Jannatul Dey,Sujan Hasan,Imtiaj Fujii,Yuki Ozeki,Yasuhiro Kawsar,Sarkar uridine synthesis antimicrobial anticancer SAR studies Pharmacia 68(1): 23-34 Nucleoside derivatives are important therapeutic drugs and are the focal point in the ongoing search for novel, more potent drug targets. In this study, a new series of pyrimidine nucleoside i.e., uridine (1) derivatives were synthesized via direct method and evaluated for their antimicrobial potential activity. The title compound uridine (1) was treated with triphenylmethyl chloride in pyridine to give the 5´-O-(triphenylmethyl)uridine derivative (2), which was subsequently derivatized to create a series of 2´,3´-di-O-acyl analogs containing a wide variety of functionalities in a single molecular framework. In vitro antimicrobial functionality tests were determined against both human and plant pathogens by disc diffusion and food poisoned techniques. The chemical structures of the synthesized compounds were confirmed on the basis of their spectral, analytical, physicochemical data. The antimicrobial results indicated that the synthesized derivatives exhibited moderate to good antibacterial and antifungal activity; in particular, they were found to be more effective against fungal phytopathogens than against human bacterial strains. Compounds 7, 9, and 14 were of particular interest as they exhibited noteworthy antifungal and antibacterial properties. In vitro MTT assays revealed that compound 9 was effective against Ehrlich’s ascites carcinoma (EAC) cells, resulting in 7.12% and 1.34% cell growth inhibition at concentrations of 200 and 6.25 µg/ml, respectively. The IC50 value for compound 9 was rather high and found to be 1956.25 µg/ml. Structure-activity relationship (SAR) studies were also conducted to predict structural and pharmacokinetic properties. The findings of this study indicate that the different uridine derivatives are potentially useful antimicrobial agents for the advancement of future pharmaceutical research. info:eu-repo/semantics/altIdentifier/eissn/2603-557X info:eu-repo/semantics/altIdentifier/pissn/0428-0296 info:eu-repo/semantics/openAccess CC BY 4.0 Bulgarian Pharmaceutical Scientific Society 2021 Research Article text/html info:doi:10.3897/pharmacia.68.e56543 https://doi.org/10.3897/pharmacia.68.e56543 https://pharmacia.pensoft.net/article/56543/ https://pharmacia.pensoft.net/article/56543/download/pdf/ en cGFnZT0xJnNldD1waGFybWFjaWEmZnJvbT0mdW50aWw9Jm1ldGFkYXRhX3ByZWZpeD1vYWlfZGM=