Pub Date : 2022-10-29DOI: 10.19163/2307-9266-2022-10-4-320-330
A. Giyoszoda, E. Stepanova, O. Veselova, S. E. Storozhenko
The comparative assessment results of the hypoglycemic activity of a combined preparation containing microcapsules with a phytocomposition consisting of Glycyrrhiza glabra L. extracts, a dry extract of Galega officinalis L., Mentha piperita L., and gliclazide, are discussed in the article. Methods for obtaining microcapsules with an original PEG-6000 shell are described.The aim of the study was to develop an optimal technology for obtaining microcapsules with a PEG-6000 shell containing a combined antidiabetic substance, and conduct its detailed pharmacological study on the model of type 2 diabetes mellitus, to conduct a detailed comparative pharmacological study of a microencapsulated antidiabetic composition with a shell based on PEG-6000, including gliclazide and a sum of phytoextracts on the model of type 2 diabetes mellitus.Materials and methods. As the main objects of the study, microcapsules with a PEG-6000 shell were obtained using methyl miristate as the base liquid. The capsules contained the amount of plant extracts in their composition: a dry extract of Glycyrrhiza glabra L., a dry extract of Galega officinalis L., a dry extract of Mentha piperita L., and gliclazide. The study of a hypoglycemic activity was carried out after a single administration of drugs to the animals with alloxan-induced type 2 diabetes mellitus. The cumulative effect assessment of the drugs was carried out within 14 days with a test for the resistance to oral glucose on days 7 and 14.Results. Microcapsules with the original shell were obtained by dispersion in a liquid-liquid system with the adjustment of some technological stages. The effect of the drugs under study on the glycemic profile in the rats with an experimental model of type 2 diabetes mellitus was investigated. A comparative evaluation of the pharmacological effect was carried out with a separate and combined use of microencapsulated preparations.Conclusion. The rationality of combining phytocomponents and a synthetic antidiabetic agent in microcapsules has been proven. The obtained results testify to the rationality of plant extracts combination and a synthetic hypoglycemic agent – gliclazide in microcapsules.
{"title":"DEVELOPMENT OF MICROCAPSULES BASED ON COMBINED ANTIDIABETIC SUBSTANCE: PHARMACOLOGICAL CHARACTERISTICS","authors":"A. Giyoszoda, E. Stepanova, O. Veselova, S. E. Storozhenko","doi":"10.19163/2307-9266-2022-10-4-320-330","DOIUrl":"https://doi.org/10.19163/2307-9266-2022-10-4-320-330","url":null,"abstract":"The comparative assessment results of the hypoglycemic activity of a combined preparation containing microcapsules with a phytocomposition consisting of Glycyrrhiza glabra L. extracts, a dry extract of Galega officinalis L., Mentha piperita L., and gliclazide, are discussed in the article. Methods for obtaining microcapsules with an original PEG-6000 shell are described.The aim of the study was to develop an optimal technology for obtaining microcapsules with a PEG-6000 shell containing a combined antidiabetic substance, and conduct its detailed pharmacological study on the model of type 2 diabetes mellitus, to conduct a detailed comparative pharmacological study of a microencapsulated antidiabetic composition with a shell based on PEG-6000, including gliclazide and a sum of phytoextracts on the model of type 2 diabetes mellitus.Materials and methods. As the main objects of the study, microcapsules with a PEG-6000 shell were obtained using methyl miristate as the base liquid. The capsules contained the amount of plant extracts in their composition: a dry extract of Glycyrrhiza glabra L., a dry extract of Galega officinalis L., a dry extract of Mentha piperita L., and gliclazide. The study of a hypoglycemic activity was carried out after a single administration of drugs to the animals with alloxan-induced type 2 diabetes mellitus. The cumulative effect assessment of the drugs was carried out within 14 days with a test for the resistance to oral glucose on days 7 and 14.Results. Microcapsules with the original shell were obtained by dispersion in a liquid-liquid system with the adjustment of some technological stages. The effect of the drugs under study on the glycemic profile in the rats with an experimental model of type 2 diabetes mellitus was investigated. A comparative evaluation of the pharmacological effect was carried out with a separate and combined use of microencapsulated preparations.Conclusion. The rationality of combining phytocomponents and a synthetic antidiabetic agent in microcapsules has been proven. The obtained results testify to the rationality of plant extracts combination and a synthetic hypoglycemic agent – gliclazide in microcapsules.","PeriodicalId":20031,"journal":{"name":"Pharmacology & Pharmacy","volume":"26 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75711723","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-10-29DOI: 10.19163/2307-9266-2022-10-4-308-319
O. D. Nemyatykh, I. I. Terninko, A. Sabitov, A. I. Lyashko, Z. Sakipova
A therapeutic plants potential is based on the pharmacological effects due to their phytochemical profile. Today, scientific interest in botanicals is increasing as a result of recent research that looks at the prospect of using these raw materials for the cosmetic industry as a means to protect the skin from the harmful effects of UV rays.The aim of the study was to evaluate a potential of plant-based UV-filters in modern concept view of skin photoprotection.Materials and methods. A systematic literature search was carried out using the electronic information arrays PubMed, Scopus, Google Scholar, eLibrary. The search depth was 10 years (the period from 2010 to 2021). The search was carried out by the following keywords: antioxidants, cosmetics, photoprotection, chemical composition, pharmacological action.Results. In the paper, modern principles of skin photoprotection based on the use of chemical or physical UV-filters are considered and scientifically substantiated A trend for the use of plant-based materials and their components in the formulation of photoprotectors was notified. That is associated with a wide activity spectrum, the absence of a xenobiotic effect, and a high bioavailability of organic plant compounds.Conclusion. The data analysis from scientific publications demonstrated a potential photoprotective activity of plant-based biologically active substances due to antioxidant, anti-inflammatory and anti-radical effects. The results of the study are a theoretical basis for a further comprehensive experimental study of plant objects in order to obtain a pool of evidence in the field of photoprotection in in vivo experiments.
{"title":"EVALUATION OF PLANT-BASED UV FILTERS POTENTIAL IN MODERN CONCEPT VIEW OF SKIN PHOTOPROTECTION","authors":"O. D. Nemyatykh, I. I. Terninko, A. Sabitov, A. I. Lyashko, Z. Sakipova","doi":"10.19163/2307-9266-2022-10-4-308-319","DOIUrl":"https://doi.org/10.19163/2307-9266-2022-10-4-308-319","url":null,"abstract":"A therapeutic plants potential is based on the pharmacological effects due to their phytochemical profile. Today, scientific interest in botanicals is increasing as a result of recent research that looks at the prospect of using these raw materials for the cosmetic industry as a means to protect the skin from the harmful effects of UV rays.The aim of the study was to evaluate a potential of plant-based UV-filters in modern concept view of skin photoprotection.Materials and methods. A systematic literature search was carried out using the electronic information arrays PubMed, Scopus, Google Scholar, eLibrary. The search depth was 10 years (the period from 2010 to 2021). The search was carried out by the following keywords: antioxidants, cosmetics, photoprotection, chemical composition, pharmacological action.Results. In the paper, modern principles of skin photoprotection based on the use of chemical or physical UV-filters are considered and scientifically substantiated A trend for the use of plant-based materials and their components in the formulation of photoprotectors was notified. That is associated with a wide activity spectrum, the absence of a xenobiotic effect, and a high bioavailability of organic plant compounds.Conclusion. The data analysis from scientific publications demonstrated a potential photoprotective activity of plant-based biologically active substances due to antioxidant, anti-inflammatory and anti-radical effects. The results of the study are a theoretical basis for a further comprehensive experimental study of plant objects in order to obtain a pool of evidence in the field of photoprotection in in vivo experiments.","PeriodicalId":20031,"journal":{"name":"Pharmacology & Pharmacy","volume":"66 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84012283","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-10-29DOI: 10.19163/2307-9266-2022-10-4-343-353
S. Adzhiakhmetova, D. Pozdnyakov, N. Chervonnaya, E. O. Kulichenko, E. Oganesyan
Antioxidants are widely used in practical medicine. Not only the search for new plant antioxidants, but also the study of the factors affecting their accumulation in plants, are relevant.The aim is to study the interrelation between the activity of mitochondrial enzymes and the antioxidant activity of the secondary polyphenolic nature metabolites in hemiparasite Viscum Album L. leaves.Materials and methods. The sampling material was Viscum album L. leaves, collected in winter from a host tree, Malus domestica Borkh. The extraction of biologically active substances was carried out with ethyl alcohol of various concentrations (90%, 70% and 50%), or purified water. The amount of total antioxidants was estimated by the amperometric method. The amount of total phenols was evaluated in the reaction with the Folin-Ciocalteu reagent. The concentration of total flavonoids was estimated by the change in the optical density of the rutin with aluminum (III) chloride complex. The antioxidant properties of the analyzed extracts were determined in vitro in the induced lipid peroxidation test. The activity of aconitase was assessed by a conjugated aconitase-isocitrate dehydrogenase reaction, citrate synthase – by changing the color intensity of the Ellman reagent solution, succinate dehydrogenase were determined in the reaction of succinate-dependent oxidation of 2,6-dichlorophenolindophenol.Results. The carried out study showed that the maximum amount of total phenols (2.39±0.05%) is observed in a 50% ethanol extract from Viscum album L. leaves, with the content of total flavonoids equal to 1.83±0.04%, and the antioxidants equal to 0.503±0.007 mg/g (a quercetin equivalent) and 0.322±0.006 mg/g (a gallic acid equivalent). A 50% ethanol extract suppressed lipid peroxidation in the model mixture with IC50=106.3±1.09 µg/ml. In Viscum album L. leaves, a high activity of aconitase which strongly correlated (r=0.88416) with changes in the concentration of flavonoids, has been notified.Conclusion. The optimal extractant for obtaining extracts with a high antioxidant activity is 50% ethyl alcohol. The analysis of the mitochondrial enzymes activity showed that in Viscum album L. leaves collected in winter, a high activity of aconitase strongly correlated with changes in the concentration of flavonoids (r=0.88416).
抗氧化剂在实际医学中应用广泛。不仅是寻找新的植物抗氧化剂，而且对其在植物体内积累的影响因素的研究也具有重要意义。目的是研究半寄生虫粘属植物叶片线粒体酶活性与次生多酚代谢产物抗氧化活性之间的相互关系。材料和方法。取样材料为冬季从寄主树海棠(Malus domestica Borkh)上采集的visum album L.叶片。用不同浓度的乙醇(90%、70%和50%)或纯净水提取生物活性物质。用安培法测定了总抗氧化剂的含量。用Folin-Ciocalteu试剂测定了总酚的含量。通过测定芦丁与氯化铝络合物的光密度变化来测定总黄酮的浓度。通过体外诱导脂质过氧化实验测定所分析提取物的抗氧化性能。采用共轭乌头酸-异柠檬酸脱氢酶反应测定乌头酸酶活性，通过改变elman试剂溶液颜色强度测定枸橼酸合酶活性，测定琥珀酸依赖2,6-二氯酚吲哚酚氧化反应中琥珀酸脱氢酶活性。研究结果表明，50%乙醇提取物中总酚含量最高，为2.39±0.05%，总黄酮含量为1.83±0.04%，抗氧化剂含量为0.503±0.007 mg/g(槲皮素当量)和0.322±0.006 mg/g(没食子酸当量)。50%乙醇提取物抑制模型混合物脂质过氧化，IC50=106.3±1.09µg/ml。结果表明，乌头酸酶活性较高，与黄酮浓度变化呈显著正相关(r=0.88416)。获得高抗氧化活性提取物的最佳萃取剂为50%乙醇。线粒体酶活性分析表明，冬采粘子叶片中乌头酸酶活性高与黄酮浓度变化呈极显著相关(r=0.88416)。
{"title":"INTERRELATION BETWEEN MITOCHONDRIAL ENZYME ACTIVITY AND ANTIOXIDANT ACTIVITY OF SECONDARY POLYPHENOL NATURE METABOLITES IN HEMIPARASITE VISCUM ALBUM L. LEAVES","authors":"S. Adzhiakhmetova, D. Pozdnyakov, N. Chervonnaya, E. O. Kulichenko, E. Oganesyan","doi":"10.19163/2307-9266-2022-10-4-343-353","DOIUrl":"https://doi.org/10.19163/2307-9266-2022-10-4-343-353","url":null,"abstract":"Antioxidants are widely used in practical medicine. Not only the search for new plant antioxidants, but also the study of the factors affecting their accumulation in plants, are relevant.The aim is to study the interrelation between the activity of mitochondrial enzymes and the antioxidant activity of the secondary polyphenolic nature metabolites in hemiparasite Viscum Album L. leaves.Materials and methods. The sampling material was Viscum album L. leaves, collected in winter from a host tree, Malus domestica Borkh. The extraction of biologically active substances was carried out with ethyl alcohol of various concentrations (90%, 70% and 50%), or purified water. The amount of total antioxidants was estimated by the amperometric method. The amount of total phenols was evaluated in the reaction with the Folin-Ciocalteu reagent. The concentration of total flavonoids was estimated by the change in the optical density of the rutin with aluminum (III) chloride complex. The antioxidant properties of the analyzed extracts were determined in vitro in the induced lipid peroxidation test. The activity of aconitase was assessed by a conjugated aconitase-isocitrate dehydrogenase reaction, citrate synthase – by changing the color intensity of the Ellman reagent solution, succinate dehydrogenase were determined in the reaction of succinate-dependent oxidation of 2,6-dichlorophenolindophenol.Results. The carried out study showed that the maximum amount of total phenols (2.39±0.05%) is observed in a 50% ethanol extract from Viscum album L. leaves, with the content of total flavonoids equal to 1.83±0.04%, and the antioxidants equal to 0.503±0.007 mg/g (a quercetin equivalent) and 0.322±0.006 mg/g (a gallic acid equivalent). A 50% ethanol extract suppressed lipid peroxidation in the model mixture with IC50=106.3±1.09 µg/ml. In Viscum album L. leaves, a high activity of aconitase which strongly correlated (r=0.88416) with changes in the concentration of flavonoids, has been notified.Conclusion. The optimal extractant for obtaining extracts with a high antioxidant activity is 50% ethyl alcohol. The analysis of the mitochondrial enzymes activity showed that in Viscum album L. leaves collected in winter, a high activity of aconitase strongly correlated with changes in the concentration of flavonoids (r=0.88416).","PeriodicalId":20031,"journal":{"name":"Pharmacology & Pharmacy","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72670118","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-10-29DOI: 10.19163/2307-9266-2022-10-4-331-342
V. Petrov, I. S. Anikeev, T. Zayachnikova, A. Strygin, A. M. Dotsenko
To control the concentration of drugs with a narrow therapeutic range, and to conduct effective and safe treatments, Therapeutic Drug Monitoring (TDM) is carried out. However, to date, the implementation of TDM is associated with various difficulties, for the solution of which more convenient and less invasive methods for collecting biological material are being developed.The aim of the study was to develop protocols for the collection and storage of “dried blood spot” (DBS) samples, as well as protocols for the validation methods for the quantitative determination of drugs in whole blood, using this technology for subsequent therapeutic drug monitoring.Materials and methods. To analyze a “dried blood spot” method in detail and to identify the characteristic features of taking and storing biosamples, a collection and analysis of scientific literature over the past 10 years has been conducted. The search for literature materials has been carried out from open and accessible sources located in the scientific libraries of institutions, in electronic databases and search engines: Elibrary, PubMed, Scopus, Cyberleninka, Medline, ScienceDirect, Web of Science, Google Scholar. Primary protocols for taking, storing and analyzing samples of the “dried blood drop” have been prepared. To obtain the adequate quality samples, the developed protocols have been tested and optimized at the stages of selection and storage. By high-performance liquid chromatography with mass spectrometric detection (HPLC-MS/MS), using a “dried blood drop” as a sample preparation, drug validation protocols have been optimized to ensure that acceptable validation characteristics were achieved, and subsequent Therapeutic Drug Monitoring was performed.Results. The features of the collection, storage and analysis of the “dried blood spot” samples have been revealed. Such characteristics as a spot volume effect, a hematocrit effect, a droplet uniformity, which can affect the results of a quantitative HPLC-MS/MS analysis, have been determined. For a successful use of the new methods, appropriate protocols for taking samples of “dried blood spot” from the finger of adult patients and from the heel of newborns, as well as protocols for validating methods for the quantitative determination of drugs from these samples, have been developed.Conclusion. The application of the “dried blood spot” method using newly developed protocols for taking, storing and analyzing biological samples, relieves the existing constraints in conducting TDM, and can later become a promising method for conducting preclinical and clinical studies.
治疗药物监测(therapeutic Drug Monitoring, TDM)是为了控制治疗范围较窄的药物浓度，进行有效、安全的治疗。然而，迄今为止，TDM的实施伴随着各种困难，为了解决这些困难，正在开发更方便和更少侵入性的生物材料收集方法。本研究的目的是制定“干血斑”(DBS)样本的收集和储存方案，以及全血中药物定量测定的验证方法的方案，并利用该技术进行后续治疗药物监测。材料和方法。为了详细分析“干血点”法，并确定生物样本采集和储存的特点，对近10年的科学文献进行了收集和分析。文献资料的搜索是从机构的科学图书馆、电子数据库和搜索引擎(图书馆、PubMed、Scopus、Cyberleninka、Medline、ScienceDirect、Web of Science、Google Scholar)中开放和可访问的资源中进行的。已经制定了采集、储存和分析“干血滴”样本的主要方案。为了获得足够质量的样品，在选择和储存阶段对所开发的方案进行了测试和优化。通过高效液相色谱-质谱检测(HPLC-MS/MS)，使用“干血滴”作为样品制备，优化了药物验证方案，以确保获得可接受的验证特性，并进行了后续的治疗药物监测。揭示了“干血斑”标本的采集、保存和分析特点。斑点体积效应、红细胞压积效应、液滴均匀性等特性会影响定量HPLC-MS/MS分析的结果，这些特性已经确定。为确保新方法的成功应用，已经制定了从成人患者手指和新生儿脚跟采集“干血斑”样本的适当方案，以及从这些样本中验证药物定量测定方法的方案。“干血斑”法采用新开发的生物样本采集、储存和分析方案，缓解了目前进行TDM的限制，以后可能成为进行临床前和临床研究的一种有前景的方法。
{"title":"ADAPTATION OF “DRIED BLOOD DROP” METHOD FOR THERAPEUTIC DRUG MONITORING","authors":"V. Petrov, I. S. Anikeev, T. Zayachnikova, A. Strygin, A. M. Dotsenko","doi":"10.19163/2307-9266-2022-10-4-331-342","DOIUrl":"https://doi.org/10.19163/2307-9266-2022-10-4-331-342","url":null,"abstract":"To control the concentration of drugs with a narrow therapeutic range, and to conduct effective and safe treatments, Therapeutic Drug Monitoring (TDM) is carried out. However, to date, the implementation of TDM is associated with various difficulties, for the solution of which more convenient and less invasive methods for collecting biological material are being developed.The aim of the study was to develop protocols for the collection and storage of “dried blood spot” (DBS) samples, as well as protocols for the validation methods for the quantitative determination of drugs in whole blood, using this technology for subsequent therapeutic drug monitoring.Materials and methods. To analyze a “dried blood spot” method in detail and to identify the characteristic features of taking and storing biosamples, a collection and analysis of scientific literature over the past 10 years has been conducted. The search for literature materials has been carried out from open and accessible sources located in the scientific libraries of institutions, in electronic databases and search engines: Elibrary, PubMed, Scopus, Cyberleninka, Medline, ScienceDirect, Web of Science, Google Scholar. Primary protocols for taking, storing and analyzing samples of the “dried blood drop” have been prepared. To obtain the adequate quality samples, the developed protocols have been tested and optimized at the stages of selection and storage. By high-performance liquid chromatography with mass spectrometric detection (HPLC-MS/MS), using a “dried blood drop” as a sample preparation, drug validation protocols have been optimized to ensure that acceptable validation characteristics were achieved, and subsequent Therapeutic Drug Monitoring was performed.Results. The features of the collection, storage and analysis of the “dried blood spot” samples have been revealed. Such characteristics as a spot volume effect, a hematocrit effect, a droplet uniformity, which can affect the results of a quantitative HPLC-MS/MS analysis, have been determined. For a successful use of the new methods, appropriate protocols for taking samples of “dried blood spot” from the finger of adult patients and from the heel of newborns, as well as protocols for validating methods for the quantitative determination of drugs from these samples, have been developed.Conclusion. The application of the “dried blood spot” method using newly developed protocols for taking, storing and analyzing biological samples, relieves the existing constraints in conducting TDM, and can later become a promising method for conducting preclinical and clinical studies.","PeriodicalId":20031,"journal":{"name":"Pharmacology & Pharmacy","volume":"26 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84287031","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-07-25DOI: 10.19163/2307-9266-2022-10-3-289-304
T. Demidova, M. Y. Izmailova, S. E. Ushakova, K. Zaslavskaya, A. Odegova, V. V. Popova, M. E. Nevretdinova, A. Verbovoy, P. A. Bely
The article presents clinical study results of the efficacy and safety of combination therapy with sibutramine and metformin (fixed combination) in comparison with sibutramine therapy with microcrystalline cellulose in patients with alimentary obesity.The aim is to evaluate the efficacy and safety of using the sibutramine+metformin fixed dose combination (Reduxin® Forte) and compare it with the sibutramine + microcrystalline cellulose combination (Reduxin®) in patients with alimentary obesity in the course of the obesity therapy.Materials and methods. Male and female patients (240 people) aged 18 to 65 years inclusive with alimentary obesity, meeting the inclusion criteria and not meeting the non-inclusion criteria, were randomized into 2 groups in a 1:1 ratio. One group (n=120) received sibutramine+ metformin p. o., 1 tablet (850 mg + 10 mg) once per day, the second group (n=120) received sibutramine+ microcrystalline cellulose (MCC) p. o., 1 capsule (10 mg + 158.5 mg) once per day in the morning. On day 30 ± 1, in the absence of a 2 kg weight loss compared to the first visit, the dose was increased in accordance with the medical instruction. The therapy period was 180 days. The randomization list was generated by the factory method of random numbers. The efficacy and safety were assessed by anthropometric, clinical and laboratory parameters and the SF-36 questionnaire. The proportion of patients who achieved a decrease in body weight by more than 5% in 6 months, the magnitude and dynamics of changes in body weight and body mass index, waist and hip measurements, their ratios, changes in lipid profile, blood pressure, as well as the total number of adverse events, their frequency and nature of occurrence were analyzed.Results. The both drugs have demonstrated efficacy in all parameters of the obesity therapy. At the same time, in a comparative analysis, a statistically significant advantage of therapy with sibutramine + metformin was demonstrated in relation to the proportion of patients who had achieved more than 5% weight loss (body weight dynamics). Significant benefits were shown in terms of the magnitude of the change in body mass index (BMI); there was a statistically significant increase in the proportion of the patients who had switched from one category of BMI to another. By the end of the study, the vast majority of patients had no longer met the criteria for the diagnosis of “Obesity”. There was also a statistically significant benefit of sibutramine + metformin in terms of lowering triglycerides and low-density lipoprotein levels. The analysis of the safety parameters of sibutramine + metformin confirms a high safety profile of the drug, a comparative statistical analysis of adverse events in terms of their presence, severity, causal relationship with therapy and outcome have not revealed intergroup differences. Adverse events were transient and did not require discontinuation of therapy.Conclusion. The results of the study showed th
{"title":"EVALUATION OF WEIGHT REDUCTION EFFICACY AND SAFETY OF SIBUTRAMIN-CONTAINING DRUGS IN PATIENTS WITH ALIMENTARY OBESITY","authors":"T. Demidova, M. Y. Izmailova, S. E. Ushakova, K. Zaslavskaya, A. Odegova, V. V. Popova, M. E. Nevretdinova, A. Verbovoy, P. A. Bely","doi":"10.19163/2307-9266-2022-10-3-289-304","DOIUrl":"https://doi.org/10.19163/2307-9266-2022-10-3-289-304","url":null,"abstract":"The article presents clinical study results of the efficacy and safety of combination therapy with sibutramine and metformin (fixed combination) in comparison with sibutramine therapy with microcrystalline cellulose in patients with alimentary obesity.The aim is to evaluate the efficacy and safety of using the sibutramine+metformin fixed dose combination (Reduxin® Forte) and compare it with the sibutramine + microcrystalline cellulose combination (Reduxin®) in patients with alimentary obesity in the course of the obesity therapy.Materials and methods. Male and female patients (240 people) aged 18 to 65 years inclusive with alimentary obesity, meeting the inclusion criteria and not meeting the non-inclusion criteria, were randomized into 2 groups in a 1:1 ratio. One group (n=120) received sibutramine+ metformin p. o., 1 tablet (850 mg + 10 mg) once per day, the second group (n=120) received sibutramine+ microcrystalline cellulose (MCC) p. o., 1 capsule (10 mg + 158.5 mg) once per day in the morning. On day 30 ± 1, in the absence of a 2 kg weight loss compared to the first visit, the dose was increased in accordance with the medical instruction. The therapy period was 180 days. The randomization list was generated by the factory method of random numbers. The efficacy and safety were assessed by anthropometric, clinical and laboratory parameters and the SF-36 questionnaire. The proportion of patients who achieved a decrease in body weight by more than 5% in 6 months, the magnitude and dynamics of changes in body weight and body mass index, waist and hip measurements, their ratios, changes in lipid profile, blood pressure, as well as the total number of adverse events, their frequency and nature of occurrence were analyzed.Results. The both drugs have demonstrated efficacy in all parameters of the obesity therapy. At the same time, in a comparative analysis, a statistically significant advantage of therapy with sibutramine + metformin was demonstrated in relation to the proportion of patients who had achieved more than 5% weight loss (body weight dynamics). Significant benefits were shown in terms of the magnitude of the change in body mass index (BMI); there was a statistically significant increase in the proportion of the patients who had switched from one category of BMI to another. By the end of the study, the vast majority of patients had no longer met the criteria for the diagnosis of “Obesity”. There was also a statistically significant benefit of sibutramine + metformin in terms of lowering triglycerides and low-density lipoprotein levels. The analysis of the safety parameters of sibutramine + metformin confirms a high safety profile of the drug, a comparative statistical analysis of adverse events in terms of their presence, severity, causal relationship with therapy and outcome have not revealed intergroup differences. Adverse events were transient and did not require discontinuation of therapy.Conclusion. The results of the study showed th","PeriodicalId":20031,"journal":{"name":"Pharmacology & Pharmacy","volume":"28 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78184491","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-07-24DOI: 10.19163/2307-9266-2022-10-3-232-243
G. S. Barkaev, T. I. Kabakova, A. Goryachev
The aim of the article is the structure and content specification of the subject area professional term “drug supply” in order to deepen and concretize the conceptual apparatus in the field of the pharmaceutical activity.Materials and methods. The review presents the analysis of 389 titles of scientific pharmaceutical publications for the periods of 1995–1998 and 2010–2019. The selection of publications was carried out by the random sampling based on the phrases: «drug provision», «medical care», «provision of medicines», «pharmaceutical care», «medicinal services», «drug supply» and their English-language counterparts in Russian and foreign electronic information sources. A methodological base of the study was a cluster analysis of the subject area concept of “drug supply” according to the methodology proposed by E.A. Korzhavykh and I.V. Voronovich. In this study, a cluster was interpreted as a set of publications in which a certain pair of terms was simultaneously cited with a preset frequency of co-citation.Results. When analyzing the publications, two clusters of the “drug supply” concept were formed for the time periods indicated above. The comparison of the clusters showed an increase in the activity of the scientific research to expand the structure and content of the subject area of the “drug supply” concept. For the modern cluster, 124 co – cited pairs of lexical units were selected. They were grouped into 9 hierarchy levels according to the strength of relationship between an interval of 10 units and mentioning frequencies of the “drug supply” term. At the final stage, a graphical model of the “drug supply” concept cluster was formed. It was established that the lexical units included from the first to the fifth level, are the cluster nucleus of the “drug supply” concept as the most stable part of the lexical array, which it is advisable to rely on when developing a definition for the concept under study.Conclusion. Thus, the subject field of the “drug supply” concept is characterized by the scientific research, reflecting the socio-economic significance of the objects under study in the field of pharmaceutical activities, and its content is characterized by a high level of pharmaceutical knowledge which describes the most stable elements that make it possible to formulate an adequate definition of the “drug supply” definition.
{"title":"CLUSTER ANALYSIS OF INTEGRATED “DRUG SUPPLY” CONCEPT","authors":"G. S. Barkaev, T. I. Kabakova, A. Goryachev","doi":"10.19163/2307-9266-2022-10-3-232-243","DOIUrl":"https://doi.org/10.19163/2307-9266-2022-10-3-232-243","url":null,"abstract":"The aim of the article is the structure and content specification of the subject area professional term “drug supply” in order to deepen and concretize the conceptual apparatus in the field of the pharmaceutical activity.Materials and methods. The review presents the analysis of 389 titles of scientific pharmaceutical publications for the periods of 1995–1998 and 2010–2019. The selection of publications was carried out by the random sampling based on the phrases: «drug provision», «medical care», «provision of medicines», «pharmaceutical care», «medicinal services», «drug supply» and their English-language counterparts in Russian and foreign electronic information sources. A methodological base of the study was a cluster analysis of the subject area concept of “drug supply” according to the methodology proposed by E.A. Korzhavykh and I.V. Voronovich. In this study, a cluster was interpreted as a set of publications in which a certain pair of terms was simultaneously cited with a preset frequency of co-citation.Results. When analyzing the publications, two clusters of the “drug supply” concept were formed for the time periods indicated above. The comparison of the clusters showed an increase in the activity of the scientific research to expand the structure and content of the subject area of the “drug supply” concept. For the modern cluster, 124 co – cited pairs of lexical units were selected. They were grouped into 9 hierarchy levels according to the strength of relationship between an interval of 10 units and mentioning frequencies of the “drug supply” term. At the final stage, a graphical model of the “drug supply” concept cluster was formed. It was established that the lexical units included from the first to the fifth level, are the cluster nucleus of the “drug supply” concept as the most stable part of the lexical array, which it is advisable to rely on when developing a definition for the concept under study.Conclusion. Thus, the subject field of the “drug supply” concept is characterized by the scientific research, reflecting the socio-economic significance of the objects under study in the field of pharmaceutical activities, and its content is characterized by a high level of pharmaceutical knowledge which describes the most stable elements that make it possible to formulate an adequate definition of the “drug supply” definition.","PeriodicalId":20031,"journal":{"name":"Pharmacology & Pharmacy","volume":"141 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80079985","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-07-24DOI: 10.19163/2307-9266-2022-10-3-267-277
V. Petrov, A. Ryazanova, N. S. Privaltseva, D. A. Nekrasov
The aim. To identify polypharmacy cases and develop the ways to optimize pharmacotherapy of patients with COVID-19 hospitalized in infectious disease facilities.Materials and methods. ATC/DDD analysis with calculation of DDDs/100 bed days and a sample analysis of 500 patients’ prescriptions were performed for presenting drug utilization statistics in the infectious disease facilities of Volgograd region, which had been reassigned to treat patients with COVID-19 in 2020 and 2021.Results. Five or more drugs were administered simultaneously in 96.8% of patients. Antibacterial drugs were in 74.3% of the analyzed prescriptions in 2020 and in 73.5% in 2021. The total consumption of antibiotics was 102.9 DDDs/100 bed-days in 2020 and 95.7 DDDs/100 bed-days in 2021. The cases of multiple administrations of biological disease modifying antirheumatic drugs and the use of cyclophosphamide have been identified. In 73.6% of prescriptions in 2020 and 85.4% of 2021, omeprazole at the dose of 40 mg per day was used (77.3 and 84.6 DDDs/100 bed-days, respectively). In 2021, there were cases of concomitant intravenous prescribing of acetylcysteine under the trade name of Fluimucil® with tableted forms of ambroxol and acetylcysteine under the name of ACC®. The cumulative consumption of hepatotoxic drugs was 269.2 DDDs/100 bed-days in 2020 and 401.5 DDDs/100 bed-days in 2021.Conclusion. Lack of drugs with proven effectiveness for treatment of COVID-19, worked-out treatment algorithms, a high mortality of patients in the hospitals led to polypragmasy, excessive prescribing of drugs in the hospitals. The prescription of antibacterial drugs, omeprazole, mucolytics, hepatotoxic drugs, immunosuppressors in infectious hospitals should be monitored by clinical pharmacologist.
{"title":"POLYPHARMACY IN MANAGMENT OF IN-PATIENTS WITH NOVEL CORONAVIRUS DISEASE (COVID-19)","authors":"V. Petrov, A. Ryazanova, N. S. Privaltseva, D. A. Nekrasov","doi":"10.19163/2307-9266-2022-10-3-267-277","DOIUrl":"https://doi.org/10.19163/2307-9266-2022-10-3-267-277","url":null,"abstract":"The aim. To identify polypharmacy cases and develop the ways to optimize pharmacotherapy of patients with COVID-19 hospitalized in infectious disease facilities.Materials and methods. ATC/DDD analysis with calculation of DDDs/100 bed days and a sample analysis of 500 patients’ prescriptions were performed for presenting drug utilization statistics in the infectious disease facilities of Volgograd region, which had been reassigned to treat patients with COVID-19 in 2020 and 2021.Results. Five or more drugs were administered simultaneously in 96.8% of patients. Antibacterial drugs were in 74.3% of the analyzed prescriptions in 2020 and in 73.5% in 2021. The total consumption of antibiotics was 102.9 DDDs/100 bed-days in 2020 and 95.7 DDDs/100 bed-days in 2021. The cases of multiple administrations of biological disease modifying antirheumatic drugs and the use of cyclophosphamide have been identified. In 73.6% of prescriptions in 2020 and 85.4% of 2021, omeprazole at the dose of 40 mg per day was used (77.3 and 84.6 DDDs/100 bed-days, respectively). In 2021, there were cases of concomitant intravenous prescribing of acetylcysteine under the trade name of Fluimucil® with tableted forms of ambroxol and acetylcysteine under the name of ACC®. The cumulative consumption of hepatotoxic drugs was 269.2 DDDs/100 bed-days in 2020 and 401.5 DDDs/100 bed-days in 2021.Conclusion. Lack of drugs with proven effectiveness for treatment of COVID-19, worked-out treatment algorithms, a high mortality of patients in the hospitals led to polypragmasy, excessive prescribing of drugs in the hospitals. The prescription of antibacterial drugs, omeprazole, mucolytics, hepatotoxic drugs, immunosuppressors in infectious hospitals should be monitored by clinical pharmacologist.","PeriodicalId":20031,"journal":{"name":"Pharmacology & Pharmacy","volume":"31 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73540274","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-07-24DOI: 10.19163/2307-9266-2022-10-3-278-288
I. Krysanov, E. Makarova, V. Ermakova
The aim of the study was to conduct a pharmacoeconomic evaluation of the atezolizumab, vemurofenib and cobimetinib (ATZ+VM+COB) combination and the nivolumab and ipilimumab (NIVO+IPI) combination for the treatment of BRAF-confirmed metastatic melanoma in adult patients.Materials and methods. With the help of mathematical modeling methods, a pharmacoeconomic “cost-effectiveness” analysis; a “budget impact” analysis; a sensitivity analysis to the changes in the initial parameters of the model, were carried out.Results. The analysis of literature sources made it possible to conclude that the combination of ATZ+VM+COB compared with the combination of NIVO+IPI (15.1 and 11.2 months, respectively) has a greater clinical efficacy in terms of a progression-free survival (PFS) in patients with metastatic melanoma. When choosing the ATZ+VM+COB combination, the total cost of treatment for one adult patient with metastatic melanoma per course was lower, compared to the NIVO+IPI combination (RUB 8 326 864.89 vs RUB 7 172 751.68); the difference amounted to 1 154 113.21 rubles. When calculating the “cost-effectiveness” ratio for a year of a progression-free survival, the advantage of the ATZ + VM + COB combination in comparison with the NIVO + IPI combination, remained (5 700 200.01 rubles vs 8 942 400.10 rubles); the difference amounted to 3 242 200.09 rubles. The sensitivity analysis demonstrated the developed model stability to an increase in the cost of the ATZ + VM + COB course up to + 16%, a decrease in the cost of the NIVO + IPI course to –13%, and a reduction in the PFS to –37% against the background of the ATZ + VM + COB course. The “budget impact” analysis showed the possibility of reducing costs by 8 655 849.11 rubles with an increase from 5% to 20% in the proportion of the patients administrated with the ATZ+VM+COB combination, and with a decrease from 95% to 80% in the proportion of the patients administrated with the NIVO+IPI combination.Conclusion. The results of the work have shown that within the healthcare system of the Russian Federation, the triple combination of ATZ+VM+COB is a clinically cost-effective option for the treatment of adult metastatic melanoma patients with a confirmed BRAF mutation.
{"title":"CLINICAL AND ECONOMIC EVALUATION OF ATEZOLIZUMAB + VEMURAFENIB + COBIMETINIB COMBINATION AND NIVOLUMAB + IPILIMUMAB COMBINATION: ADMINISTRATION IN METASTATIC MELANOMA TREATMENT WITH BRAF-CONFIRMED MUTATION IN ADULT PATIENTS","authors":"I. Krysanov, E. Makarova, V. Ermakova","doi":"10.19163/2307-9266-2022-10-3-278-288","DOIUrl":"https://doi.org/10.19163/2307-9266-2022-10-3-278-288","url":null,"abstract":"The aim of the study was to conduct a pharmacoeconomic evaluation of the atezolizumab, vemurofenib and cobimetinib (ATZ+VM+COB) combination and the nivolumab and ipilimumab (NIVO+IPI) combination for the treatment of BRAF-confirmed metastatic melanoma in adult patients.Materials and methods. With the help of mathematical modeling methods, a pharmacoeconomic “cost-effectiveness” analysis; a “budget impact” analysis; a sensitivity analysis to the changes in the initial parameters of the model, were carried out.Results. The analysis of literature sources made it possible to conclude that the combination of ATZ+VM+COB compared with the combination of NIVO+IPI (15.1 and 11.2 months, respectively) has a greater clinical efficacy in terms of a progression-free survival (PFS) in patients with metastatic melanoma. When choosing the ATZ+VM+COB combination, the total cost of treatment for one adult patient with metastatic melanoma per course was lower, compared to the NIVO+IPI combination (RUB 8 326 864.89 vs RUB 7 172 751.68); the difference amounted to 1 154 113.21 rubles. When calculating the “cost-effectiveness” ratio for a year of a progression-free survival, the advantage of the ATZ + VM + COB combination in comparison with the NIVO + IPI combination, remained (5 700 200.01 rubles vs 8 942 400.10 rubles); the difference amounted to 3 242 200.09 rubles. The sensitivity analysis demonstrated the developed model stability to an increase in the cost of the ATZ + VM + COB course up to + 16%, a decrease in the cost of the NIVO + IPI course to –13%, and a reduction in the PFS to –37% against the background of the ATZ + VM + COB course. The “budget impact” analysis showed the possibility of reducing costs by 8 655 849.11 rubles with an increase from 5% to 20% in the proportion of the patients administrated with the ATZ+VM+COB combination, and with a decrease from 95% to 80% in the proportion of the patients administrated with the NIVO+IPI combination.Conclusion. The results of the work have shown that within the healthcare system of the Russian Federation, the triple combination of ATZ+VM+COB is a clinically cost-effective option for the treatment of adult metastatic melanoma patients with a confirmed BRAF mutation.","PeriodicalId":20031,"journal":{"name":"Pharmacology & Pharmacy","volume":"4 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84907041","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-07-24DOI: 10.19163/2307-9266-2022-10-3-255-266
E. B. Sysuev, E. Stepanova, V. D. Noskova
In the group of fat-soluble vitamins, vitamin D is one of the most relevant objects, that is why the problem of its technology optimization is under consideration. In general, there is a number of ways to obtain this substance, although it is not produced in Russia yet.The aim of the study was to select optimal process conditions to increase the efficiency of protein transformation with the isolation of a fat fraction containing fat-soluble vitamin D.Materials and methods. Various types of fish and the vitamins contained in them are described as the main research models. Variants of technological solutions have been considered: the possibility of using extraction to obtain the vitamin D substance has been tested. Classical maceration and intensifying maceration have been used; the circulating extraction method and the alkaline hydrolysis method have been applied. The yield of the target product has been determined by HPLC.Results. Methods for obtaining the substance of fat-soluble vitamin D from fish raw materials have been considered in detail. The optimal technological characteristics of the vitamin release by alkaline hydrolysis with a 12.5% decrease in the concentration of the hydrolyzing alkaline component – potassium hydroxide – has been established; that concentration ensured the maximum yield of the fat fraction containing vitamin D.Conclusion. The use of the resulting substance makes it possible to develop domestic standard samples applicable both in the pharmaceutical field and in the field of technical regulation.
{"title":"OPTIMIZATION TECHNOLOGY OF FAT-SOLUBLE VITAMINS PRODUCTION BASED ON ALKALINE HYDROLYSIS","authors":"E. B. Sysuev, E. Stepanova, V. D. Noskova","doi":"10.19163/2307-9266-2022-10-3-255-266","DOIUrl":"https://doi.org/10.19163/2307-9266-2022-10-3-255-266","url":null,"abstract":"In the group of fat-soluble vitamins, vitamin D is one of the most relevant objects, that is why the problem of its technology optimization is under consideration. In general, there is a number of ways to obtain this substance, although it is not produced in Russia yet.The aim of the study was to select optimal process conditions to increase the efficiency of protein transformation with the isolation of a fat fraction containing fat-soluble vitamin D.Materials and methods. Various types of fish and the vitamins contained in them are described as the main research models. Variants of technological solutions have been considered: the possibility of using extraction to obtain the vitamin D substance has been tested. Classical maceration and intensifying maceration have been used; the circulating extraction method and the alkaline hydrolysis method have been applied. The yield of the target product has been determined by HPLC.Results. Methods for obtaining the substance of fat-soluble vitamin D from fish raw materials have been considered in detail. The optimal technological characteristics of the vitamin release by alkaline hydrolysis with a 12.5% decrease in the concentration of the hydrolyzing alkaline component – potassium hydroxide – has been established; that concentration ensured the maximum yield of the fat fraction containing vitamin D.Conclusion. The use of the resulting substance makes it possible to develop domestic standard samples applicable both in the pharmaceutical field and in the field of technical regulation.","PeriodicalId":20031,"journal":{"name":"Pharmacology & Pharmacy","volume":"25 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77036961","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-07-24DOI: 10.19163/2307-9266-2022-10-3-244-254
A. Mubinov, V. Kurkin, E. Avdeeva, S. D. Kolpakova, A. Zhestkov
Nigella sativa L. is a promising plant object, herbal medicinal raw materials of which can be comprehensively used for the development of drugs with an antimicrobial activity.The aim of the study was to screen and compare the antimicrobial activity of water-ethanolic extractions from the Nigella sativa L. herbs with a eucalyptus tincture of as a reference preparation.Materials and methods. Chromatograms of the extracts were obtained by thin layer chromatography in the system of chloroform – ethanol – water (26:16:3). The detection of adsorption zones was carried out in daylight, in the UV light at λ=254 nm and λ=365 nm, as well as by treatment with reagents – a 3% alcohol solution of aluminum chloride and a solution of diazobenzosulfonic acid in a 20% sodium carbonate solution. The next step was to determine the minimum inhibitory concentration by the method of double serial dilutions in Mueller-Hinton nutrient broth (Bio-Rad, USA). As test cultures, the strains of the American Type Culture Collection (ATCC) microorganisms were used: Staphylococcus aureus (ATCC 29213), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), as well as Candida albicans (a clinical strain). Simultaneously, an experiment to establish a “negative” control was carried out. For the comparative evaluation of the studied samples activity, its activity was compared with the reference preparation with a proven antimicrobial activity – a eucalyptus tincture.Results. For all water-ethanolic extractions and the Nigella sativa L. herb tincture, the adsorption zones characteristic of flavonoids with Rf1 = 0.28, Rf2 = 0.15, Rf3 = 0.11 were revealed, and under the action of an alcoholic solution of aluminum chloride, the fluorescence of the adsorption zones was also enhanced, which indicates the phenolic nature of these compounds.In the course of the study, it was found out that all water-ethanolic extractions from the Nigella sativa L. herbs have the greatest antimicrobial effect against the Pseudomonas aeruginosa strain. When compared with the reference preparation – a eucalyptus tincture, it was notified that the specified tincture of the Nigella sativa L. herbs has an advantage in the antimicrobial activity over the strain of Pseudomonas aeruginosa – the action at the 16-fold dilution vs the 4-fold dilution. The action on the Escherichia coli and Candida albicans strains is comparable for the both tinctures.Conclusion. The obtained results of phytochemical and microbiological analyses will be used as a rationale for the introduction of antimicrobial preparations based on the Nigella sativa herbs in medical and pharmaceutical practice.
{"title":"PHYTOCHEMICAL AND MICROBIOLOGICAL ASPECTS OF THE NIGELLA SATIVA L. HERBS STUDY","authors":"A. Mubinov, V. Kurkin, E. Avdeeva, S. D. Kolpakova, A. Zhestkov","doi":"10.19163/2307-9266-2022-10-3-244-254","DOIUrl":"https://doi.org/10.19163/2307-9266-2022-10-3-244-254","url":null,"abstract":"Nigella sativa L. is a promising plant object, herbal medicinal raw materials of which can be comprehensively used for the development of drugs with an antimicrobial activity.The aim of the study was to screen and compare the antimicrobial activity of water-ethanolic extractions from the Nigella sativa L. herbs with a eucalyptus tincture of as a reference preparation.Materials and methods. Chromatograms of the extracts were obtained by thin layer chromatography in the system of chloroform – ethanol – water (26:16:3). The detection of adsorption zones was carried out in daylight, in the UV light at λ=254 nm and λ=365 nm, as well as by treatment with reagents – a 3% alcohol solution of aluminum chloride and a solution of diazobenzosulfonic acid in a 20% sodium carbonate solution. The next step was to determine the minimum inhibitory concentration by the method of double serial dilutions in Mueller-Hinton nutrient broth (Bio-Rad, USA). As test cultures, the strains of the American Type Culture Collection (ATCC) microorganisms were used: Staphylococcus aureus (ATCC 29213), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), as well as Candida albicans (a clinical strain). Simultaneously, an experiment to establish a “negative” control was carried out. For the comparative evaluation of the studied samples activity, its activity was compared with the reference preparation with a proven antimicrobial activity – a eucalyptus tincture.Results. For all water-ethanolic extractions and the Nigella sativa L. herb tincture, the adsorption zones characteristic of flavonoids with Rf1 = 0.28, Rf2 = 0.15, Rf3 = 0.11 were revealed, and under the action of an alcoholic solution of aluminum chloride, the fluorescence of the adsorption zones was also enhanced, which indicates the phenolic nature of these compounds.In the course of the study, it was found out that all water-ethanolic extractions from the Nigella sativa L. herbs have the greatest antimicrobial effect against the Pseudomonas aeruginosa strain. When compared with the reference preparation – a eucalyptus tincture, it was notified that the specified tincture of the Nigella sativa L. herbs has an advantage in the antimicrobial activity over the strain of Pseudomonas aeruginosa – the action at the 16-fold dilution vs the 4-fold dilution. The action on the Escherichia coli and Candida albicans strains is comparable for the both tinctures.Conclusion. The obtained results of phytochemical and microbiological analyses will be used as a rationale for the introduction of antimicrobial preparations based on the Nigella sativa herbs in medical and pharmaceutical practice.","PeriodicalId":20031,"journal":{"name":"Pharmacology & Pharmacy","volume":"48 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83114963","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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