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DEVELOPMENT OF NITROFURAN DERIVATIVE: COMPOSITION AND TECHNOLOGY OF EFFERVESCENT TABLETS WITH SOLID DISPERSIONS 硝基呋喃衍生物的研制:固体分散泡腾片的组成与工艺
Pub Date : 2022-03-06 DOI: 10.19163/2307-9266-2022-10-1-55-68
A. Elagina, A. Belyatskaya, I. I. Krasnyuk (jr.), I. Krasnyuk, O. I. Stepanova, T. V. Fateeva, E. Smolyarchuk, S. V. Kozin, O. Plakhotnaya, O. V. Rаstopchina, J. Rau
Taking into account the current Product specification file, the aim of the work was to develop the composition and technology for obtaining effervescent tablets based on solid dispersions of furazolidone in the form of an aqueous solution for external use.Materials and methods. The used substances were: furazolidone, anhydrous sodium carbonate (chemically pure), polyvinylpyrrolidone-24000±2000 (chemically pure), malic acid (analytically pure), tartaric acid (chemically pure), citric acid (chemically pure), sodium benzoate (chemically pure), ethyl alcohol 96% (chemically pure), purified water. Preparation of granulates is separate wet granulation in a fluidized bed (Mycrolab, BOSCH, Germany). Obtaining tablets is the process of pressing on a manual hydraulic test press (“PRG”, VNIR, Russia). The dependence of disintegration, abrasion capacity and crushing resistance on compacting pressure was investigated. Technological parameters of granulates, еру obtained effervescent tablets, shelf life and storage conditions were investigated according to the State Pharmacopoeia of the Russian Federation XIVth ed.Results. Two compositions of effervescent tablets containing solid dispersions of furazolidone as an active substance were obtained, which, when dissolved in 100 ml of water at room temperature (20°C), form a solution of furazolidone with a concentration of 0.004% in less than 5 minutes. The method of quantitative determination of the furazolidone content in the effervescent tablets was validated. A complex of physicochemical methods for the analysis of tablets was carried out. Quality standards have been developed. The developed compositions stability of instant tablets during storage during accelerated and long-term tests has been experimentally confirmed. The preliminary shelf life and storage conditions have been determined.Conclusion. The result of technological and chemical-pharmaceutical research is the creation and evaluation of the quality of a new instant furazolidone dosage form as effervescent tablet formulations.
考虑到目前的产品规范文件,该工作的目的是开发基于呋喃唑酮固体分散体的水剂型外用泡腾片的组合物和技术。材料和方法。所用物质为:呋喃唑酮、无水碳酸钠(化学纯)、聚乙烯吡啶酮-24000±2000(化学纯)、苹果酸(分析纯)、酒石酸(化学纯)、柠檬酸(化学纯)、苯甲酸钠(化学纯)、乙醇96%(化学纯)、纯净水。颗粒的制备是在流化床中分离的湿制粒(Mycrolab, BOSCH,德国)。获得片剂是在手动液压压力机(“PRG”,VNIR,俄罗斯)上按压的过程。研究了复合材料的崩解性、耐磨性和抗破碎性与压实压力的关系。根据《俄罗斯联邦国家药典》第14版对颗粒剂、所得泡腾片的工艺参数、保质期和贮存条件进行了考察。制备了两种以呋喃唑酮固体分散体为活性物质的泡腾片组合物,在室温(20℃)下将其溶解于100ml水中,在不到5分钟的时间内形成浓度为0.004%的呋喃唑酮溶液。建立了泡腾片中呋喃唑酮含量的定量测定方法。采用综合理化方法对片剂进行了分析。制定了质量标准。实验证实了速溶片剂的成分在加速和长期贮存过程中的稳定性。初步确定了保鲜期和贮存条件。对呋喃唑酮泡腾片新型速溶剂型进行了工艺和化学药学研究,并对其质量进行了评价。
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引用次数: 2
FEATURES OF QUANTITATIVE ESTIMATION OF FLAVONOID CONTENT IN JUGLANS NIGRA L. BARKS PREPARATIONS 黑胡桃树皮制剂中类黄酮含量定量测定的特点
Pub Date : 2022-03-06 DOI: 10.19163/2307-9266-2022-10-1-31-43
V. Kurkin, N. I. Zimenkina
The aim of the research is the development of quantification procedures of flavonoids in Juglans nigra L. barks preparations using modern instrumental analytical techniques (spectrophotometry, high performance liquid chromatography).Materials and methods. The subjects of research were tincture and dry extract of Juglans nigra L. bark, the samples of which were prepared in March and April 2020 in the Botanical Garden of Samara State Medical University (Samara); the standard samples (SS) of myricitrin, myricetin. The registration of the electronic spectra was carried out with a spectrophotometer «Specord 40» (Analytik Jena, Germany). The chromatographic analysis was carried out by the method of reversed-phase HPLC on a microcolumn liquid chromatograph “Milichrom-6” (NPAO “Nauchpribor”, Russia).Results. Using differential spectrophotometry, methods for the quantitative determination of the total amount of flavonoids in terms of myricitrin in the tincture and dry extract of Juglans nigra L. bark, has been developed. It has been determined that the content of the total amount of flavonoids in terms of myricitrin in the tincture and dry extract of Juglans nigra L., is 0.84±0.07% and 12.38±0.24%, respectively. The error of a single determination of the total amount of flavonoids in terms of myricitrin in the tincture and dry extract of Juglans nigra L. bark with a confidence probability of 95%, is ± 8.91% and ± 2.10%, respectively. Methods for the quantitative determination of myricitrin in the tincture and dry extract of Juglans nigra L. bark by HPLC has been developed. The content of the dominant flavonoid – myricitrin (myricetin-3-O-α-L-rhamnopyranoside) – in the tincture and dry extract of Juglans nigra L., was 0.42±0.06% and 8.45±0.24%, respectively. The error of the single determination of myricitrin in the tincture and dry extract of Juglans nigra L. with a confidence probability of 95% is ± 15.04% and ±2.96%, respectively.Conclusion. The developed methods for the quantitative determination of flavonoids in the preparations of Juglans nigra L. barks L. can be used in solving the problems of standardization of Juglans nigra L. preparations.
本研究的目的是利用现代仪器分析技术(分光光度法、高效液相色谱法)建立黑核桃制剂中黄酮类化合物的定量分析方法。材料和方法。研究对象为黑胡桃树皮酊剂和干提取物,样品于2020年3月和4月在萨马拉国立医科大学(萨马拉)植物园制备;杨梅素、杨梅素的标准样品(SS)。电子光谱的登记使用分光光度计«Specord 40»(Analytik Jena,德国)进行。采用反相高效液相色谱法,在俄罗斯NPAO“Nauchpribor”公司的“Milichrom-6”微柱液相色谱仪上进行色谱分析。建立了用差示分光光度法定量测定黑胡桃树皮酊剂和干浸膏中杨梅三醇类黄酮总量的方法。测定了黑核桃酊剂和干浸膏中以杨桃苷为单位的总黄酮含量分别为0.84±0.07%和12.38±0.24%。用黑胡桃树皮酊剂和干浸出物中杨梅三醇含量测定黄酮类化合物总量的误差分别为±8.91%和±2.10%,置信概率为95%。建立了用高效液相色谱法定量测定核桃树皮酊剂和干浸膏中杨梅三苷含量的方法。杨梅苷(杨梅苷-3- o -α-L-鼠李糖吡喃苷)在黑核桃酊剂和干浸膏中的含量分别为0.42±0.06%和8.45±0.24%。测定黑核桃酊剂和干浸出物中杨桃苷含量的误差分别为±15.04%和±2.96%,置信概率为95%。所建立的方法可用于黑核桃制剂中黄酮类化合物的定量测定,为解决黑核桃制剂的标准化问题提供参考。
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引用次数: 1
APPLICATION OF MULTIVARIATE ANOVA AND GENERALIZED DESIRABILITY TO OPTIMIZE THE COMPOSITION AND TECHNOLOGY OF TABLETS CONTAINING N-BENZYL-N-METHYL-1-PHENYLPYRROLO [1,2-A] PYRAZINE-3-CARBOXAMIDE 应用多元方差分析和广义期望优化n -苄基- n -甲基-1-苯基吡咯[1,2- a]吡嗪-3-羧酰胺片剂的组成和工艺
Pub Date : 2022-03-06 DOI: 10.19163/2307-9266-2022-10-1-69-81
S. Tishkov, E. Blynskaya, K. Alekseev, V. Alekseev, D. I. Gavrilov
The creation of drugs with an anxiolytic activity, which do not have the main side effects characteristic of drugs of this group, is an important and socially significant task. For its implementation, within the framework of the development of an original drug with an anxiolytic activity, the composition and manufacturing of GML-1 tablets (N-benzyl-N-methyl-1-phenylpyrrolo [1,2-a] pyrazine-3-carboxamide) are being developed.The aim of this article is to study, using a four-factor analysis of variance, the influence of composition factors on the manufacturing properties of GML-1 tablets and the selection of the type, the amount, stage of the disintegrant addition and the type of lubricating excipients used in the technology of wet granulation of GML-1 tablets.Materials and methods. The materials used are: the substance – GML-1 (N-benzyl-N-methyl-1-phenylpyrrolo [1,2-a] pyrazine-3-carboxamide). Excipients: microcrystalline cellulose 101 (MCC 101); polyvinylpyrrolidone (PVP); crospovidone, croscarmellose sodium (CCS), sodium starch glycolate (SSG); magnesium stearate (MS), sodium stearyl fumarate (SSF). To obtain tablet mixtures, wet granulation and tableting with the study of their main pharmaceutical and technological properties was used.Results. Model compositions were developed and their pharmaceutical and technological properties were studied. These results have been analyzed, the degree of these factors’ influence and their interactions have been determined. In most of the cases considered, the interactions of the factors did not cause a significant change in the optimization criteria. With an increase in the amount of a disintegrant, the disintegration time decreased unevenly, so an increase in the amount of these excipients from 4 to 6 mg had a stronger effect than from 2 to 4 mg. Factor B affected the release degree non-linearly. Factor A influenced all the optimization criteria considered, especially a PS release. The best release and disintegration were observed with crospovidone, which was of a particular importance when processing the test results using a generalized desirability method.Conclusion. In view of the conflicting variance analysis results, for particular factors, the resulting values were additionally analyzed using the generalized desirability function. The use of this method made it possible to reduce the conflicting variance analysis results to the most optimal composition.
创造具有抗焦虑活性的药物,而不具有该组药物的主要副作用特征,是一项重要的和具有社会意义的任务。为了实施该计划,在开发具有抗焦虑活性的原始药物的框架内,正在开发GML-1片剂(n -苄基- n -甲基-1-苯基吡咯[1,2-a]吡嗪-3-carboxamide)的组成和制造。本文采用四因素方差分析方法,研究了各组成因素对GML-1片剂生产性能的影响,并对GML-1片剂湿制粒工艺中崩解剂的种类、用量、添加阶段和润滑辅料的选择进行了研究。材料和方法。所使用的材料是:物质- GML-1 (n -苄基- n -甲基-1-苯基吡咯[1,2-a]吡嗪-3-羧酰胺)。辅料:微晶纤维素101 (MCC 101);聚乙烯吡咯烷酮(PVP);交联维酮、交联棉糖钠(CCS)、淀粉乙醇酸钠(SSG);硬脂酸镁(MS),富马酸硬脂酰钠(SSF)。采用湿法造粒和压片法制备复方片剂,并对其主要药物性能和工艺性能进行了研究。研制了模型组合物,并对其药物性能和工艺性能进行了研究。对这些结果进行了分析,确定了这些因素的影响程度及其相互作用。在考虑的大多数情况下,这些因素的相互作用不会导致优化标准发生重大变化。随着崩解剂用量的增加,崩解时间的减少不均匀,因此,将这些赋形剂的用量从4毫克增加到6毫克比从2毫克增加到4毫克的效果更强。因子B对释放度有非线性影响。因素A影响了所考虑的所有优化标准,尤其是PS版本。在使用广义期望方法处理试验结果时,观察到交叉聚维酮的释放和崩解效果最佳,这一点尤为重要。鉴于方差分析结果存在冲突,针对特定因素,采用广义可取性函数对结果值进行附加分析。利用该方法,可以将相互冲突的方差分析结果减少到最优组合。
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引用次数: 1
PHARMACOTHERAPY POSSIBILITIES OF CARDIOVASCULAR AUTONOMOUS NEUROPATHY IN CHILDREN WITH TYPE 1 DIABETES MELLITUS AT THE PRECLINICAL STAGE 临床前阶段1型糖尿病患儿心血管自主神经病变的药物治疗可能性
Pub Date : 2022-03-06 DOI: 10.19163/2307-9266-2022-10-1-93-103
N. Malyuzhinskaya, I. Shishimorov, O. Magnitskaya, K. V. Stepanenko, O. V. Polyakova, G. Klitochenko, I. V. Petrova, S. A. Emelyanova, A. Skiba
The aim of the article is to evaluate the effectiveness of the thioctic acid preparation in the complex therapy of type 1 diabetes mellitus (T1DM) in children with cardiovascular autonomic neuropathy at the preclinical stage.Materials and methods. A design is a prospective randomized study. A clinical and instrumental examination of 64 children with preclinical stage signs of diabetic cardiovascular autonomic neuropathy (DCAN) was carried out. The cohort was divided into 2 groups: in the main and control groups, glycemic control was normalized by adjusting a dose of insulin therapy; in the main group, the children additionally received thioctic acid at the dose of 600 mg/day for 3 months. To control the effectiveness of the therapy, the technique of laser Doppler flowmetry was used.Results. After the pharmacological intervention, there was an improvement in the disease course, normalization of carbohydrate and lipid metabolism, increased vasomotor mechanisms of the regulation of the tissue blood flow due to an increase in endothelial and neurogenic kinds of activity in combination with a decrease in the intravascular tone and an increase in the effective perfusion in tissues. An increase in the heart rate variability was detected, positive dynamics of cardiovascular tests indicators according to D. Ewing, temporal (pNN50%, SDNN) and spectral indicators (VLF) were diagnosed. Achievement and maintenance of the target values of glycemic control indicators, as well as the absence of glycemic variability, turned out to be clinically significant for reducing the manifestations of neuropathy. The non-invasive technique of laser Doppler flowmetry is informative for the early diagnosis of DCAN in T1DM children.Conclusion. The carried out studies have demonstrated the effectiveness of the lipoic acid use at the dose of 600 mg/day for 3 months in the children with DCAN signs at the preclinical stage. The method of laser Doppler flowmetry for determining indications and monitoring the effectiveness of therapy makes it possible to implement a personalized approach to prescribing preventive treatment in T1DM children.
本文的目的是评价硫辛酸制剂在临床前阶段合并心血管自主神经病变的1型糖尿病(T1DM)患儿的综合治疗中的有效性。材料和方法。设计是一项前瞻性随机研究。对64例有糖尿病性心血管自主神经病变(DCAN)临床前阶段体征的患儿进行了临床和仪器检查。该队列分为两组:主组和对照组通过调整胰岛素治疗剂量使血糖控制正常化;主组患儿在对照组基础上给予硫辛酸600 mg/d治疗,疗程3个月。为了控制治疗效果,采用激光多普勒血流测量技术。药物干预后,病程改善,碳水化合物和脂质代谢正常化,由于内皮和神经源性活性增加,血管内张力降低,组织有效灌注增加,调节组织血流的血管舒缩机制增加。检测到心率变异性增加,根据D. Ewing诊断心血管试验指标,时间(pNN50%, SDNN)和频谱指标(VLF)的积极动态。血糖控制指标达到并维持目标值,血糖无变异性,对减轻神经病变的表现具有临床意义。无创激光多普勒血流法对T1DM患儿DCAN的早期诊断具有重要意义。已开展的研究表明,在临床前阶段有DCAN症状的儿童中,硫辛酸以600毫克/天的剂量连续使用3个月是有效的。激光多普勒血流法用于确定适应症和监测治疗的有效性,使得在T1DM儿童中实施个性化的预防性治疗处方成为可能。
{"title":"PHARMACOTHERAPY POSSIBILITIES OF CARDIOVASCULAR AUTONOMOUS NEUROPATHY IN CHILDREN WITH TYPE 1 DIABETES MELLITUS AT THE PRECLINICAL STAGE","authors":"N. Malyuzhinskaya, I. Shishimorov, O. Magnitskaya, K. V. Stepanenko, O. V. Polyakova, G. Klitochenko, I. V. Petrova, S. A. Emelyanova, A. Skiba","doi":"10.19163/2307-9266-2022-10-1-93-103","DOIUrl":"https://doi.org/10.19163/2307-9266-2022-10-1-93-103","url":null,"abstract":"The aim of the article is to evaluate the effectiveness of the thioctic acid preparation in the complex therapy of type 1 diabetes mellitus (T1DM) in children with cardiovascular autonomic neuropathy at the preclinical stage.Materials and methods. A design is a prospective randomized study. A clinical and instrumental examination of 64 children with preclinical stage signs of diabetic cardiovascular autonomic neuropathy (DCAN) was carried out. The cohort was divided into 2 groups: in the main and control groups, glycemic control was normalized by adjusting a dose of insulin therapy; in the main group, the children additionally received thioctic acid at the dose of 600 mg/day for 3 months. To control the effectiveness of the therapy, the technique of laser Doppler flowmetry was used.Results. After the pharmacological intervention, there was an improvement in the disease course, normalization of carbohydrate and lipid metabolism, increased vasomotor mechanisms of the regulation of the tissue blood flow due to an increase in endothelial and neurogenic kinds of activity in combination with a decrease in the intravascular tone and an increase in the effective perfusion in tissues. An increase in the heart rate variability was detected, positive dynamics of cardiovascular tests indicators according to D. Ewing, temporal (pNN50%, SDNN) and spectral indicators (VLF) were diagnosed. Achievement and maintenance of the target values of glycemic control indicators, as well as the absence of glycemic variability, turned out to be clinically significant for reducing the manifestations of neuropathy. The non-invasive technique of laser Doppler flowmetry is informative for the early diagnosis of DCAN in T1DM children.Conclusion. The carried out studies have demonstrated the effectiveness of the lipoic acid use at the dose of 600 mg/day for 3 months in the children with DCAN signs at the preclinical stage. The method of laser Doppler flowmetry for determining indications and monitoring the effectiveness of therapy makes it possible to implement a personalized approach to prescribing preventive treatment in T1DM children.","PeriodicalId":20031,"journal":{"name":"Pharmacology & Pharmacy","volume":"4 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84616704","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}
引用次数: 0
STUDY OF ORGANIC ACIDS PROFILE OF GENUS PERSICARIA MILL SPECIES 桃属植物有机酸谱的研究
Pub Date : 2022-03-06 DOI: 10.19163/2307-9266-2022-10-1-44-54
A. S. Chistyakova, A. Gudkova, A. Slivkin, E. Chupandina
The genus Persicaria Mill. species belonging to the buckwheat family (Polygonaceae Juss.) and widespread in Russia, are weeds. The chemical composition’s main components of the genus Persicaria Mill. species, are flavonoid glycosides (rutin, avicularin, hyperoside, etc.). The data concerning a comparative study of the organic acids in the herb representatives of genus Persicaria Mill., have not been detected in the available literature.The aim of the research is a comparative study of the organic acids qualitative and quantitative composition in the genus Persicaria Mill. species growing in the Voronezh region.Materials and methods. The objects of the study were dried herb samples of the genus Persicaria Mill. species. All the species were harvested in the Voronezh region during the blooming period. The quantitative content of ascorbic acid and the amount of organic acids in terms of malic (hydroxy-succinic) acid was carried out according to the titrimetric methods of the Russian Federation State Pharmacopeia, the XIVth ed. The study of the qualitative composition of the organic acids profile and their quantitative content assessment in the studied objects, the herbs, was carried out by the method of capillary electrophoresis (“Kapel”, St. Petersburg, Russia).Results. With the help of pharmacopoeial titrimetric methods, it was established that the highest content of the organic acids total amount is characteristic of the Persicaria maculosa Mill. herb (5,60%), the lowest one – of the Persicaria tomentósa (Schrank) E. P. Bicknell herb (4.03%). Persicaria maculosa S. F. Gray and Persicaria hydropiper (L.) Delarbre are the richest in ascorbic acid (0.17% and 0.15%, respectively). Using the method of capillary electrophoresis, the composition of the total amount of the studied organic acids has been established. It is represented by oxalic, formic, citric, malic, wine, propionic, lactic, benzoic and other acids.Conclusion. The study of the organic acids of the genus Persicaria Mill. species has been carried out. It has been established that in the studied species, the organic acids total amount in terms of malic acid and the amount of ascorbic acid are similar. By the method of capillary electrophoresis, a complete composition of organic acids has been studied, and the quantitative content of each component has been established. In all the studied Persicaria Mill. species, the predominance of oxalic, formic and malic acids has been revealed.
桃属植物。属于荞麦科(蓼科)的一种,广泛分布于俄罗斯,是杂草。木犀草属植物的主要化学成分。种类,均为黄酮类苷类(芦丁、木犀草苷、金丝桃苷等)。桃属代表性草本植物有机酸的比较研究。,在现有文献中未发现。对桃属植物中有机酸的定性和定量组成进行比较研究。生长在沃罗涅日地区的品种。材料和方法。本研究的对象是桃属的干草本样品。物种。所有的品种都是在开花期间在沃罗涅日地区收获的。根据俄罗斯联邦国家药典第十四版的滴定法测定抗坏血酸的定量含量和苹果酸(羟基琥珀酸)中有机酸的含量。采用毛细管电泳法(“Kapel”,俄罗斯圣彼得堡)对研究对象药材中有机酸谱的定性组成及其定量含量进行了研究。利用药典滴定法,确定了其有机酸总含量最高是桃皮药材的特征。(5.60%),最低的是百椒tomentósa (Schrank) e.p. Bicknell(4.03%)。maculosa s.f. Gray和Persicaria hydropiper (L.)Delarbre的抗坏血酸含量最高(分别为0.17%和0.15%)。采用毛细管电泳的方法,确定了所研究有机酸的总量组成。以草酸、甲酸、柠檬酸、苹果酸、酒酸、丙酸、乳酸、苯甲酸等酸为代表。桃属植物有机酸的研究。物种已经被执行。研究表明,在所研究的物种中,有机酸总量以苹果酸和抗坏血酸的总量计算是相似的。采用毛细管电泳的方法,研究了有机酸的完整组成,并确定了各组分的定量含量。在所有被研究过的木犀草中。在物种上,草酸、甲酸和苹果酸具有优势。
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引用次数: 1
OBESITY AS A REFLECTION OF PSYCHO-EMOTIONAL DISORDERS: FOCUS ON PHARMACOTHERAPY 肥胖是心理情绪障碍的反映:关注药物治疗
Pub Date : 2022-03-06 DOI: 10.19163/2307-9266-2022-10-1-19-30
V. Shishkova
Obesity is a vivid example of a multifactorial disease. In its development, not only the discrepancy between the energy intake and its expenditure but also various neurohumoral mechanisms, as well as external socio-economic and psychosocial factors, play important roles. One of the frequent options for combining psychoemotional disorders with obesity is the development of certain types of eating disorders in a patient. In this regard, the actual problem is to find the optimal therapeutic and prophylactic strategy in the management of such patients.The aim of the work is to analyze the literature data on the features of the pathogenetic mechanisms of the obesity development against the background of psychoemotional disorders that are realized through eating disorders, and to identify the possibilities of using sibutramine to carry out a pharmacological correction of these pathological conditions.Materials and methods. In the process of selecting materials for writing a review article, the following databases were uses: PubMed, Scopus, Web of Science, Google Scholar, ScienceDirect, etc. The search carried out, was based on the publications for the period from 2009 to 2020. The following words and phrases were chosen as parameters for the literature selection: obesity, psycho-emotional disorders, eating disorders, sibutramine.Results. This review summarizes the main pathogenetic aspects that unite both the development of psychoemotional and metabolic disorders. A modern classification of obesity, taking into account the latest domestic and international recommendations of professional communities, is given. Eating disorders are considered in detail, their socio-psychological and psychiatric classifications are given. The prospect of choosing a therapeutic and prophylactic strategy for managing such patients is assessed, depending on the presence of psycho-emotional and eating disorders.Conclusion. Thus, the combined drug containing sibutramine and metformin registered in the Russian Federation is effective, safe and can be used in patients with alimentary obesity and eating disorders, taking into account contraindications.
肥胖是多因素疾病的一个生动例子。在其发展过程中,除了能量摄入和能量消耗的差异外,各种神经体液机制以及外部社会经济和社会心理因素也起着重要作用。将心理情绪障碍与肥胖相结合的常见选择之一是患者出现某些类型的饮食失调。因此,在对这类患者的管理中,如何找到最佳的治疗和预防策略是实际问题。本工作的目的是分析通过饮食失调实现的心理情绪障碍背景下肥胖发展的发病机制特征的文献资料,并确定使用西布曲明对这些病理状况进行药物纠正的可能性。材料和方法。在撰写综述文章的材料选择过程中,使用了以下数据库:PubMed, Scopus, Web of Science, Google Scholar, ScienceDirect等。这项研究基于2009年至2020年期间的出版物。选择以下词和短语作为文献选择的参数:肥胖,心理情绪障碍,饮食失调,西布曲明。本文综述了结合心理情绪障碍和代谢障碍发展的主要发病方面。考虑到最新的国内和国际专业团体的建议,给出了一个现代的肥胖分类。详细考虑了饮食失调,并给出了其社会心理和精神分类。选择治疗和预防策略来管理这类患者的前景进行了评估,这取决于心理情绪和饮食失调的存在。因此,在俄罗斯联邦注册的含有西布曲明和二甲双胍的联合药物是有效、安全的,在考虑禁忌症的情况下,可用于患有食源性肥胖和饮食失调的患者。
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引用次数: 4
PHARMACOLOGICAL ACTIVITY OF EXTRACTS FROM PLANTS OF COSMOS BIPINNATUS CAV. SPECIES 山竹植物提取物的药理活性研究。物种
Pub Date : 2022-03-06 DOI: 10.19163/2307-9266-2022-10-1-82-92
E. O. Kulichenko, O. Andreeva, E. Sergeeva, S. S. Sigareva, A. Terekhov, E. Oganesyan, S. Y. Sidorskaya
The aim of the study is to determine antioxidant, anti-inflammatory and hypolipidemic activities of the extracts from Cosmos bipinnatus Cav. three varieties, obtained by the extraction with 70% ethyl alcohol.Materials and methods. The antioxidant effect was studied in vitro using a model of iron-induced lipid peroxidation in the lecithin liposome system. The study of the anti-inflammatory activity was carried out on 30 male rats of the “Wistar” line. Diclofenac was used as a reference drug (p. o., the dose of 13 mg/kg in terms of the weight of an adult). The substances were administered to animals in the form of an aqueous suspension stabilized with Tween-80. To simulate the inflammatory process, a model of “cotton granuloma” was created. A hypolipidemic activity of the extracts was studied on 36 white male rats of the “Wistar” line. To study the hypolipidemic activity of the studied extracts, a tween model was used to create a hyperlipidemic state in rats, the concentrations of total cholesterol and triglycerides was determined in the serum of the experimental animals.Results. The conducted model experiments made it possible to conclude that the alcohol extracts obtained from the dried inflorescences of the “Dazzler”, “Rosea” and “Purity” varieties of Cosmos bipinnatus Cav. have antioxidant, anti-inflammatory and hypolipidemic kinds of activities. It has been established that the extracts from the “Dazzler” and “Rosea” varieties (Cosmos bipinnatus Cav.) contribute to a better reduction in the accumulation of peroxide compounds, compared to the extract obtained from the “Purity” variety. The data analysis on the anti-inflammatory activity shows that all the studied objects significantly (p = 0.05) reduce the stage of exudation compared with the control group animals by 50% (the «Purity» variety), by 52% (the «Rosea» variety) and by 40% (the “Dazzler” variety).An experiment on the study of a hypolipidemic activity in the control group of the animals revealed a significant, in relation to the values of the intact group, increase in the cholesterol level of the blood serum by 78%, and in the level of triglycerides (TGCs) – by 64%.The administration of the extracts obtained from Cosmos bipinnatus Cav. “Purity”, “Rosea”, “Dazzler” varieties to the animals, led to a decrease in cholesterol in blood serum by 44%, 47%, 50%, and triglycerides by 52%, 52% and 57%, respectively. Both indicators reached the normal level and did not differ significantly from the values in healthy (intact) animals.Conclusion. According to the conducted studies, it can be concluded that alcohol extracts obtained from Cоsmos bipinnatus Cav., have pronounced antioxidant, anti-inflammatory and hypolipidemic kinds of effect.
本研究旨在测定双翅草提取物的抗氧化、抗炎和降血脂活性。三个品种,用70%乙醇提取得到。材料和方法。在体外建立卵磷脂脂质体系统铁诱导脂质过氧化模型,研究其抗氧化作用。对30只雄性“Wistar”系大鼠进行了抗炎活性研究。双氯芬酸作为对照药物(按成人体重计算,剂量为13mg /kg)。这些物质以吐温-80稳定的水悬浮液的形式给予动物。为了模拟炎症过程,我们建立了一个“棉花肉芽肿”模型。对36只“Wistar”系白种雄性大鼠进行了降血脂活性研究。为了研究所研究的提取物的降血脂活性,采用小鼠模型建立了高脂血症大鼠,测定了实验动物血清中总胆固醇和甘油三酯的浓度。所进行的模型实验可以得出结论,从“Dazzler”,“Rosea”和“Purity”三种Cosmos bipinnatus Cav的干燥花序中获得的酒精提取物。具有抗氧化、抗炎、降血脂等多种活性。已经确定,与从“纯度”品种中获得的提取物相比,从“炫乐”和“玫瑰”品种(Cosmos bipinnatus Cav.)中获得的提取物有助于更好地减少过氧化物化合物的积累。抗炎活性数据分析表明,与对照组相比,各研究对象的泌液期分别缩短50%(“纯度”品种)、52%(“玫瑰”品种)和40%(“炫目”品种)(p = 0.05)。一项研究动物的降血脂活动的实验显示,与未受影响的动物相比,对照组的血清胆固醇水平显著增加了78%,甘油三酯(TGCs)水平增加了64%。山参提取物的药理作用。“纯度”、“玫瑰”、“炫彩”品种的动物血清胆固醇分别下降44%、47%、50%,甘油三酯分别下降52%、52%和57%。两项指标均达到正常水平,与健康(完整)动物无显著差异。根据所进行的研究,可以得出的结论是,获得的醇提取物,从金盏花Cav。,具有显著的抗氧化、抗炎、降血脂等功效。
{"title":"PHARMACOLOGICAL ACTIVITY OF EXTRACTS FROM PLANTS OF COSMOS BIPINNATUS CAV. SPECIES","authors":"E. O. Kulichenko, O. Andreeva, E. Sergeeva, S. S. Sigareva, A. Terekhov, E. Oganesyan, S. Y. Sidorskaya","doi":"10.19163/2307-9266-2022-10-1-82-92","DOIUrl":"https://doi.org/10.19163/2307-9266-2022-10-1-82-92","url":null,"abstract":"The aim of the study is to determine antioxidant, anti-inflammatory and hypolipidemic activities of the extracts from Cosmos bipinnatus Cav. three varieties, obtained by the extraction with 70% ethyl alcohol.Materials and methods. The antioxidant effect was studied in vitro using a model of iron-induced lipid peroxidation in the lecithin liposome system. The study of the anti-inflammatory activity was carried out on 30 male rats of the “Wistar” line. Diclofenac was used as a reference drug (p. o., the dose of 13 mg/kg in terms of the weight of an adult). The substances were administered to animals in the form of an aqueous suspension stabilized with Tween-80. To simulate the inflammatory process, a model of “cotton granuloma” was created. A hypolipidemic activity of the extracts was studied on 36 white male rats of the “Wistar” line. To study the hypolipidemic activity of the studied extracts, a tween model was used to create a hyperlipidemic state in rats, the concentrations of total cholesterol and triglycerides was determined in the serum of the experimental animals.Results. The conducted model experiments made it possible to conclude that the alcohol extracts obtained from the dried inflorescences of the “Dazzler”, “Rosea” and “Purity” varieties of Cosmos bipinnatus Cav. have antioxidant, anti-inflammatory and hypolipidemic kinds of activities. It has been established that the extracts from the “Dazzler” and “Rosea” varieties (Cosmos bipinnatus Cav.) contribute to a better reduction in the accumulation of peroxide compounds, compared to the extract obtained from the “Purity” variety. The data analysis on the anti-inflammatory activity shows that all the studied objects significantly (p = 0.05) reduce the stage of exudation compared with the control group animals by 50% (the «Purity» variety), by 52% (the «Rosea» variety) and by 40% (the “Dazzler” variety).An experiment on the study of a hypolipidemic activity in the control group of the animals revealed a significant, in relation to the values of the intact group, increase in the cholesterol level of the blood serum by 78%, and in the level of triglycerides (TGCs) – by 64%.The administration of the extracts obtained from Cosmos bipinnatus Cav. “Purity”, “Rosea”, “Dazzler” varieties to the animals, led to a decrease in cholesterol in blood serum by 44%, 47%, 50%, and triglycerides by 52%, 52% and 57%, respectively. Both indicators reached the normal level and did not differ significantly from the values in healthy (intact) animals.Conclusion. According to the conducted studies, it can be concluded that alcohol extracts obtained from Cоsmos bipinnatus Cav., have pronounced antioxidant, anti-inflammatory and hypolipidemic kinds of effect.","PeriodicalId":20031,"journal":{"name":"Pharmacology & Pharmacy","volume":"38 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-03-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87211820","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}
引用次数: 2
EVALUATION OF ABCB1-PROTEIN INHIBITION PROSPECTIVENESS IN HEMATOENCEPHALIC BARRIER AS METHOD FOR INCREASING EFFICIENCY OF PHARMACOTHERAPY IN CEREBRAL ISCHEMIA 血脑屏障abcb1蛋白抑制作为提高脑缺血药物治疗效率方法的前景评价
Pub Date : 2022-03-06 DOI: 10.19163/2307-9266-2022-10-1-104-112
I. V. Chernykh, A. Shchulkin, M. V. Gatsanoga, E. Yakusheva
The aim of the article is to evaluate the ABCB1 protein inhibition in the blood-brain barrier to increase the effectiveness of neuroprotective therapy for focal and global cerebral ischemia.Materials and methods. The work was performed on 103 male Wistar rats. In the 1st group (n=33), the neuroprotective activity of the ABCB1 protein substrate, nimodipine (0.4 mg/kg), was analyzed in terms of reducing the area of the brain necrosis after a 1-hour occlusion of the middle cerebral artery with a 24-hour reperfusion (focal ischemia). In the 2nd group (n=60), the effectiveness of nimodipine was analyzed by reducing the lethality of rats and the neurological deficit (ND) level against the background of the bilateral occlusion of the common carotid arteries (global ischemia). In both groups, nimodipine was used alone or in the combination with omeprazole, the ABCB1 protein inhibitor (17.6 mg/kg). The drugs were administered intravenously.Results. The nimodipine administration to the 1st group led to the reduction of the necrosis focus by 28% compared with the control series. Omeprazole did not cause a change in the area of the necrosis. The combination of drugs caused a decrease in the area of the necrosis in relation to the control by 29%; there were no differences in comparison with the nimodipine series. Nimodipine reduced the rats’ lethality in the 2nd group against the background of the pathology (a tendency). Omeprazole alone did not change the mortality. The drug combination reduced the mortality compared to the control and nimodipine series. The administration of omeprazole alone did not reduce the neurological deficit score relative to the control. In the nimodipine series, ND was 88% lower than the control, after 24 hours. With the administration of the drugs combination, this indicator decreased in relation to the control by 88%, 80%, 88%, 87% and 86% after 4, 12, 24, 48 and 72 hours, respectively, and in relation to the nimodipine series it decreased by 60% and 67% after 4 and 48 hours.Conclusion. The ABCB1 protein inhibition is promising for increasing the effectiveness of neuroprotective therapy for global ischemia, but not for focal cerebral ischemia.
本文的目的是评估ABCB1蛋白在血脑屏障中的抑制作用,以提高局灶性和全局性脑缺血的神经保护治疗的有效性。材料和方法。这项工作在103只雄性Wistar大鼠身上进行。在第一组(n=33)中,分析ABCB1蛋白底物尼莫地平(0.4 mg/kg)在大脑中动脉闭塞1小时24小时再灌注(局灶性缺血)后减少脑坏死面积的神经保护活性。第二组(n=60)在双侧颈总动脉闭塞(全脑缺血)的背景下,通过降低大鼠的死亡率和神经功能缺损(ND)水平来分析尼莫地平的有效性。在两组中,尼莫地平单独使用或与ABCB1蛋白抑制剂奥美拉唑联合使用(17.6 mg/kg)。药物经静脉给药。第一组给予尼莫地平使坏死灶比对照组缩小28%。奥美拉唑没有引起坏死区域的改变。联合用药组坏死面积较对照组减少29%;与尼莫地平系列比较无差异。在病理背景下,尼莫地平降低了第二组大鼠的死亡率(一种趋势)。单独使用奥美拉唑对死亡率没有影响。与对照组和尼莫地平系列相比,联合用药降低了死亡率。与对照组相比,单独服用奥美拉唑并没有降低神经功能障碍评分。尼莫地平组24小时后ND比对照组低88%。在给药后4、12、24、48和72 h,该指标分别较对照组下降88%、80%、88%、87%和86%,与尼莫地平系列给药后4和48 h,该指标分别较对照组下降60%和67%。ABCB1蛋白抑制有望提高全脑缺血的神经保护治疗的有效性,但对局灶性脑缺血则不然。
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引用次数: 0
Induction of Sirtuin1 Activity in SH-SY5Y Cells by Cyanidin-3-O-Glucocide Induced 花青素-3- o -葡萄糖苷诱导SH-SY5Y细胞Sirtuin1活性的研究
Pub Date : 2022-01-01 DOI: 10.4236/pp.2022.132003
K. Yama, Yoshiki Hasebe, Ayuka Inomata, J. Miura, A. Konda
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引用次数: 1
Phytochemical Analysis and Antibacterial Activity of Azadirachta indica Leaf Extracts against Escherichia coli 印楝叶提取物对大肠杆菌的抑菌活性及植物化学分析
Pub Date : 2022-01-01 DOI: 10.4236/pp.2022.131001
C. Hikaambo, Luyando Kaacha, Steward Mudenda, Mutenta N Nyambe, Billy Chabalenge, M. Phiri, Luke Biete, T. M. Akapelwa, W. Mufwambi, Martha Chulu, M. Kampamba
Background: Traditional medicine has employed Azadirachta indica to treat a variety of ailments. However, there is little information on the use of this plant in Zambia. Objective: To evaluate the phytochemicals and antibacterial activity of Azadirachta indica leaf extracts against Escherichia coli. Materials and Methods: This was a laboratory-based experimental study in which ethanol and water were used for extraction by maceration. Phytochemical analysis was then done on the leaf extract. Using the disc diffusion method, varying concentrations of A. indica aqueous and ethanolic extracts were used to test the antibacterial activity of A. indica against Escherichia coli. The sensitivity of the tested microorganisms to aqueous and ethanolic leaf extracts was shown by zones of inhibition after incubation. Results: The phytochemical screening of the A. indica leaves revealed the presence of phenolics and tannins in both the ethanol and aqueous extract. Saponins, flavonoids and alkaloids were only present in the aqueous extract. While steroids were only present in the ethanol extract. The antibacterial activity of A. indica leaves extract was determined by zones of inhibition which showed that both aqueous and ethanol extracts had activity against E. coli. The Minimum Inhibitory Concentration was determined at 10 mg/mL for the aqueous extract and 20 mg/mL for the ethanol extract. The zones of inhibition in-creased with concentration. Conclusion: The extracts of A. indica displayed antibacterial activity against E. coli in a dose-dependent manner. Compara-tively, the aqueous extract produced better antibacterial properties against E. coli than the ethanolic extract.
背景:传统医学已经使用印楝来治疗各种疾病。然而,关于在赞比亚使用这种植物的信息很少。目的:评价印楝叶提取物的化学成分及对大肠杆菌的抑菌活性。材料与方法:本实验采用乙醇和水浸渍法提取。然后对叶提取物进行植物化学分析。采用圆盘扩散法,对不同浓度的籼稻水提液和乙醇提液进行抑菌活性测定。被试微生物对水提液和乙醇提液的敏感性通过培养后的抑制区来显示。结果:对籼稻叶片进行植物化学筛选,发现乙醇和水提物中均含有酚类物质和单宁。皂苷、黄酮类化合物和生物碱仅存在于水提物中。而类固醇只存在于乙醇提取物中。通过抑菌区测定了籼稻叶提取物的抑菌活性,结果表明,水提物和乙醇提物对大肠杆菌均有抑菌活性。最低抑菌浓度为:水提物10 mg/mL,乙醇提物20 mg/mL。抑制区随浓度增加而增加。结论:籼稻提取物对大肠杆菌的抑菌活性呈剂量依赖性。相比之下,水提物对大肠杆菌的抑菌性能优于乙醇提物。
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引用次数: 8
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Pharmacology & Pharmacy
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