Vol 70, No 1 (2021)

Introduction. Pharmaceutical science requires that new highly effective nonsteroidal anti-inflammatory drugs (NSAIDs) should be sought because of different negative pharmacological properties of this group of drugs. Previous studies may suggest that further molecular design of novel anti-inflammatory structures should be carried out by varying with different alkyl substituents at 2 and 6 positions of the heterocyclic nucleus. Objective: to synthetize 2,6-dialkyl N-sulfonamide and N-diphenylsulfone derivatives of pyrimidine-4(1H)-one, which have a pronounced anti-inflammatory effect compared to that of the comparison drug. Material and methods. The targeted products were obtained by cyclocondensation of N-acyl-β-ketoamides with aromatic amines in acetic acid. The purity of the synthesized substances was determined by thin-layer chromatography (TLC); the structure of the synthesized compounds was confirmed by spectral studies. The synthesis of the predicted substances used 4-aminobenzenesulfonamide and 2-(4-aminobenzenesulfonamide)-thiazole and 4,4'-diaminodiphenylsulfone as primary aromatic amines. Their anti-inflammatory activity was investigated using a model of acute exudative inflammation according to the guidelines for the study of anti-inflammatory activity versus that of diclofenac, one of the most widely used NSAIDs. Results. The yield of 6-methyl-2-ethylpyrimidine-4(1H)-one derivatives was found to be higher than that of 2-methyl-6-ethylpyrimidine-4(1H)-one. The difference in the yields of the reaction products can be explained by the spatial structure of the starting carbonyl compound, which considerably affects its reactivity. The results of primary pharmacological screening for acute aseptic inflammation could reveal the leading compounds with anti-inflammatory activity at the level of the comparison drug diclofenac. Conclusion. Based on the spatial structure of N-acyl-β-ketoamides, the authors explained the yields of 2,6-dialkyl derivatives of pyrimidine-4 (1H)-one with fragments of 4-aminobenzenesulfonamide, 2-(4-aminobenzenesulfamide)-thiazole and 4,4'-diaminodiphenylsulfone. The investigation of the targeted compounds for anti-inflammatory activity could identify the most promising compounds among them, which had an effect commensurable with that of diclofenac.

Introduction. Currently, the number of highly effective drugs is growing on the global pharmaceutical market, and the requirements for methods for assessing the quality of medicinal substances are becoming more stringent. At the same time, there is a clear lag in domestic developments of new methods of analysis in comparison with foreign countries. Aim of the study. The aim of the study is to compare the pharmacopoeial requirements for assessing the quality of a fish oil substance in the USA and Great Britain, as well as to determine potential indicators of the quality of a fish oil substance and methods for their assessment that can be used by domestic manufacturers. Methods. Сomparative analysis of pharmacopoeial sources and regulatory documents that are freely available. Results. The analysis of pharmacopoeial requirements for assessing the quality of the substance of fish oil in the United States and the UK was provided. As a result of a comparison of requirements and standardization methods, it has been established that the regulatory documentation governing the assessment of the quality of the fish oil substance in the United States of America practically coincides with the requirements in the British Pharmacopoeia. This indicates close cooperation between Western countries in the development of new methods for assessing the quality of the fish oil substance and dosage forms based on it. Conclusion. Foreign experience in the use of modern methods of analysis of fish oil can be used to improve the relevant articles of the domestic pharmacopoeia, as well as in various regulatory documents.

Introduction. The term «job satisfaction» has a multifaceted meaning that is based on an employee's emotional and evaluative attitude to the duties performed. The level of job satisfaction contributes to the interest of pharmaceutical workers in forming the loyalty of visitors to a pharmacy organization and in enhancing its competitiveness. Objective: to identify factors that shape job satisfaction in pharmaceutical workers, as well as their quantitative assessment. Material and methods. The factors that form their influence on job satisfaction in pharmaceutical workers in the pharmacy organizations were investigated using content analysis that could identify 26 factors that affect job satisfaction; logical and structural analysis that grouped the identified factors into 6 groups; a sociological survey; economic and mathematical methods. Results. The authors identified groups of job satisfaction-shaping factors in pharmaceutical workers. Using the results of sociological surveys based on the analysis of a representative number of questionnaires (n=214), they calculated the average scores of the factors shaping the job satisfaction; defined a group indicator, and ranked factors, by determining the most influential one. The factors from the labor organization groups, a moral and material satisfaction group, and a working-conditions-in-the-organization group with total scores of 20.61; 20.2, and 19.81, respectively, had the maximum impact on job satisfaction in pharmaceutical workers. The group of factors that influence labor organization combines 5 positions. With the maximum score of 5 per factor, the «intensity of work activity» had an average score of 4.4; «the content of work performed» averaged 4.31 scores; and «work irregularity, a shift system» had 4.13 scores. When assessing the «working conditions», the «work and rest regime» was the most significant factor with an average score of 4.27. Conclusion. The findings suggest that to reasonably organize work and to ensure its conditions are important for the pharmaceutical worker, whereas an irrational organization lowers job satisfaction and can reduce the competitiveness of a pharmacy organization.

Introduction. Cefpirome is white to slightly yellow hygroscopic, crystalline powder, freely soluble in water. It belongs to the group of third-generation cephalosporin antibiotics and has a broad spectrum of action. Objective: to develop and validate procedures for determining cefpirome in biological material. Material and methods. Cefpirome was isolated with solvents of different chemical nature of the mixture models with liver tissue. The duration of isolation, its multiplicity, and the mass ratio of the isolating agent to the biological object were examined for its impact on the percentage of extraction of the test compound with an optimal isolating agent. Low-pressure macrocolumn reversed-phase liquid chromatography was used as a purification procedure. Identification and quantification were done by reverse-phase HPLC. The determination methods were validated according to well-known parameters. Results. An acetone-water (5:5) mixture was the most suitable isolating agent for extracting cefpirome from biological material. The necessary frequency of isolation of the analyte of ths mixture was 2; the duration of each contact of the isolating mixture with the biological object was 30 min; the isolating mixture/biomatrix ratio was 2:1. A procedure was developed to determine cefpirome in cadaveric organ tissues by reversed-phase HPLC, which involves preliminary isolation of the analyte with an acetone-water (5:5) mixture and its purification in a 150x10-mm macrocolumn containing Silasorb C8 sorbent with a particle size of 15 |im. The developed procedure was validated according to the criteria of specificity, linearity, accuracy, and precision. Conclusion. The results of the investigations make it possible to present the nature of isolation of cefpirome from biological material. The developed procedure provides extraction, purification, identification, and quantitative determination of cefpirome in biological material.