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Design aspects of the combined medicinal product with multifunctional action based on herbal drugs 以草药为基础的具有多功能作用的组合药物的设计方面
Pub Date : 2021-10-22 DOI: 10.32352/0367-3057.5.21.06
С. А. Котов, Т. М. Гонтова, А. Г. Котов
Combined herbal medicines for the treatment and prevention of allergic diseases are perspective substitutes for the «classic» drugs of H-1 receptor blockers of the 1st and 2nd generation. Literary-logical methods are quite effectively used for scientifically justified design of these drugs, namely phytopharmacological drug design (PPD) and phytochemical drug design (PCD). The aim of the work – the search for ways of the scientifically justified design of a combined multifunctional medicine based on the bur-marigold, which normalizes the functioning of the body's defence systems, increases the body's nonspecific resistance, normalizes the immune status using literary-logical and statistical methods of analysis. The design of the preparation was carried out using literature data for PPD and experimental and literature data for PCD. Statistical processing method – Spearman's rank correlation coefficient was used. Design aspects of the combined herbal medicine, which includes a bur-marigold herb, calendula flowers, hawthorn leaves and flowers were considered using of a system-comparative analysis of information and its processing by the method of the Spearman's rank correlation coefficient determination. When PCD development of various combinations of herbal drugs, information about the content of such biologically active substances (BAS) as flavonoids, oxycinnamic acids, polyphenols, triterpenes, proteins/amino acids, polysaccharides was used. When PPD development the spectra of pharmacological activity were determined and a quantitative assessment to them in the system of marks for each of the herbal drug of the combined medicine was given. The PCD and PPD data into the matrix for calculating the Spearman rank correlation coefficient of the «action–sum of BAS» was entered. As a result, a strong, direct and statistically significant correlation relation (p from 0.924 to 0.997) between the content of oxycinnamic acids, polyphenols, triterpenes, proteins/amino acids, polysaccharides and such pharmacological actions as capillary-strengthening, anti-inflammatory, immunostimulating; choleretic, hepatoprotective, improving metabolism; diuretic, hypotensive, sedative, tonic, desensitizing, antipruritic, reparative for the studied herbal combinations was found. The obtained results of the PCD and PPD development as well as the study of the correlation «action–sum of BAS» by calculating the Spearman's rank correlation coefficient, this suggests the developed combined herbal medicinal product with multifunctional action is perspective in the complex therapy of allergic diseases accompanied by a decrease in the body's resistance and immunostatus.
用于治疗和预防过敏性疾病的联合草药是第一代和第二代H-1受体阻滞剂“经典”药物的理想替代品。文献逻辑方法被有效地用于这些药物的科学合理设计,即植物药理学药物设计(PPD)和植物化学药物设计(PCD)。这项工作的目的是寻找一种基于金盏花的联合多功能药物的科学合理设计方法,该药物使身体防御系统的功能正常化,增加身体的非特异性抵抗力,并使用文献逻辑和统计分析方法使免疫状态正常化。使用PPD的文献数据以及PCD的实验和文献数据进行制剂的设计。统计处理方法——采用Spearman秩相关系数。采用Spearman秩相关系数确定方法,采用系统信息比较分析及其处理,考虑了包括金盏花、金盏花和山楂叶和花在内的组合草药的设计方面。在开发各种草药组合的PCD时,使用了关于生物活性物质(BAS)含量的信息,如类黄酮、氧肉桂酸、多酚、三萜、蛋白质/氨基酸、多糖。当PPD发展时,确定了药理活性的光谱,并在联合药物的每种草药的标记系统中对其进行了定量评估。将PCD和PPD数据输入矩阵,用于计算“BAS的行动-总和”的Spearman秩相关系数。结果表明,羟基肉桂酸、多酚、三萜、蛋白质/氨基酸、多糖的含量与毛细血管强化、抗炎、免疫刺激等药理作用之间存在强、直接且具有统计学意义的相关性(p从0.924-0.997);利胆护肝,改善新陈代谢;发现所研究的草药组合具有利尿、降压、镇静、补药、脱敏、止痒、修复作用。所获得的PCD和PPD的开发结果,以及通过计算Spearman秩相关系数对“BAS的作用-总和”相关性的研究,表明所开发的具有多功能作用的联合草药产品在伴随身体抵抗力和免疫状态下降的过敏性疾病的复杂治疗中具有前景。
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引用次数: 1
Scientific and practical approaches to optimizing the pharmaceutical supply of pediatric palliative patients with paralytic syndromes 优化小儿麻痹综合征姑息治疗患者药物供应的科学实用方法
Pub Date : 2021-10-22 DOI: 10.32352/0367-3057.5.21.01
І. В. Кубарєва, М. С. Бекетова
Today, palliative care (PC) as a system has a complex structure with stable orderliness, interrelated elements and subsystems. The problem of providing PD with an appropriate level and quality to the children population is particularly acute; it is due to differences in the duration of provision, the necessity to provide educational services, and the socialization of palliative children. At the same time, an important aspect in achieving an appropriate quality of life for children and their families related to health is the assessment of not only medical and social, but also pharmaceutical provision. The aim of the work is to substantiate the approaches to optimization of pharmaceutical support of pediatric palliative patients with paralytic syndromes. The study objects were data from medical records, theactual consumption of medicines by pediatric patients of the Kharkiv healthcare institution where palliative care was provided, as well as data on the state registration of medicines in Ukraine. During the study, clinical and anamnestic, sociological, and marketing methods were used. Based on the results of the analysis of clinical and anamnestic data and the overall assessment of symptoms in a sample group of palliative children with paralytic syndromes, which was 115 people, pathological conditions that led to frequent or permanent distress were identified. Among them, the spastic syndrome prevailed in 100% of cases, the pain syndrome in 66% of cases, the convulsive syndrome in 59%, respectively, and digestive disorders were observed in 82.6% of patients in the sample. It was found that a large proportions of drugs for pharmacological correction of symptoms in the sample of patients were formed by antiepileptic drugs, laxatives and centrally acting muscle relaxants. The results of the marketing analysis of a definite segment of the pharmaceutical market showed a rather limited range of drugs for pediatric dosage forms and concentrations, and it on average ranged from 3.1% to 25% in the pharmacotherapeutic groups studied. Thus, the results obtained prove the need to develop mechanisms for optimizing the pharmaceutical supply of pediatric palliative patients, in particular, expanding the range of medicines approved for use in pediatric practice.
今天,姑息治疗作为一个系统具有复杂的结构,具有稳定的有序性、相互关联的元素和子系统。向儿童群体提供适当水平和质量的PD问题尤为严重;这是由于在提供教育服务的持续时间、提供教育服务和缓和儿童社会化方面的差异。与此同时,为儿童及其家庭实现与健康相关的适当生活质量的一个重要方面是,不仅要评估医疗和社会,还要评估药物供应。这项工作的目的是证实优化小儿麻痹综合征姑息治疗患者药物支持的方法。研究对象是来自医疗记录的数据、提供姑息治疗的哈尔科夫医疗机构儿科患者的实际用药情况,以及乌克兰国家药品注册数据。在研究过程中,使用了临床和记忆、社会学和营销方法。根据临床和记忆数据的分析结果,以及对115名患有麻痹综合征的姑息性儿童样本组症状的总体评估,确定了导致频繁或永久性痛苦的病理状况。其中,痉挛综合征占100%,疼痛综合征占66%,抽搐综合征占59%,消化系统疾病占82.6%。研究发现,在患者样本中,很大一部分用于药物纠正症状的药物是由抗癫痫药物、泻药和中枢作用的肌肉松弛剂形成的。对药品市场某一特定细分市场的营销分析结果显示,用于儿科剂型和浓度的药物范围相当有限,在所研究的药物治疗组中,平均范围为3.1%至25%。因此,所获得的结果证明,有必要开发优化儿科姑息治疗患者药物供应的机制,特别是扩大批准用于儿科实践的药物范围。
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引用次数: 1
Study of the effect of dermatological phytogel on the ability of microorganisms to form a biofilm 皮肤植物酚对微生物形成生物膜能力影响的研究
Pub Date : 2021-10-22 DOI: 10.32352/0367-3057.5.21.07
В. С. Миргород, Н. І. Філімонова, О. Г. Башура, С. Г. Бобро
The development of many chronic infections, including skin diseases, is caused by bacteria growing in the form of biofilms. Bacterial biofilms provide beneficial survival mechanisms that determine virulence, disease pathogenesis, or resistance of the pathogen to antibiotics. As shown by a large number of studies, biofilms play an important role in the pathogenesis of dermatological diseases, including atopic dermatitis. The close relationship between the microbial biofilm that colonizes the skin surface and the negative consequences for human health makes the skin microbiome an object of therapeutic intervention in dermatological pathogenic processes. The work aims to study the effect of dermatological phytogel on the ability of microorganisms to form biofilms. The objects of research were samples of gel containing dry walnut leaf extract with the sum of tannins in terms of gallic acid and dry matter 30 mg/100 g of gel, dry nettle extract with the sum of hydroxycinnamic acids in terms of chlorogenic acid, and dry matter 20 mg/100 g of gel, dry thyme extract with the sum of flavonoids in terms of rutin and dry matter 35 mg/100 g of gel both monocomponent and combined. The study of the ability of individual plant components of phytogel samples N 1, N 2, N 3 and samples of combined phytogel N 4, N 5, and N 6 to influence biofilm formation have shown that the most pronounced decceleration of biofilms formation was registered in the gel sample with phytocomplex N 4 and was 19.7–20.7% to S. aureus, E. coli, P. aerugenosis and C. albicans respectively. The activity of the gel sample with phytocomplex N 4 was 1.3–1.4 times higher than that of monocomponent gel samples N 1, N 2, and N 3. When determining the ability of the test samples to destroy biofilms, it has been found that the gel sample with phytocomplex N 4 showed the greatest activity, which exceeded the specified properties of samples N 5 and N 6 by an average of 1.2 and 1.8 times. The activity of single-component gel samples N 1, N 2, and N 3 was lower in S. aureus, E. coli, P. aerugenosis and C. albicans biofilm destruction. The conducted studies prove the feasibility of further study of the combined gel with the phyto complex № 4 containing dry walnut leaf extract with the sum of tannins in terms of gallic acid and dry matter 30 mg/100 g of gel, dry nettle extract with the sum of hydroxycinnamic acids in terms of chlorogenic acid, and dry matter 20 mg/100 g of gel, dry thyme extract with the sum of flavonoids in terms of rutin and dry matter 35 mg/100 g of gel.
许多慢性感染的发展,包括皮肤病,是由细菌以生物膜的形式生长引起的。细菌生物膜提供了有益的生存机制,决定了毒力、疾病发病机制或病原体对抗生素的耐药性。大量研究表明,生物膜在包括特应性皮炎在内的皮肤病的发病机制中起着重要作用。定植在皮肤表面的微生物生物膜与人类健康的负面后果之间的密切关系使皮肤微生物组成为皮肤病致病过程中治疗干预的对象。本研究旨在研究皮肤植物酚对微生物形成生物膜能力的影响。研究对象为:以没食子酸和干物质和单宁之和为30 mg/100 g凝胶的核桃叶干提取物、以绿原酸和干物质之和为20 mg/100 g凝胶的荨麻干提取物、以芦丁和干物质为35 mg/100 g凝胶的百里香干提取物。研究了植物复合物n1、n2、n3和组合植物复合物n4、n5、n6对生物膜形成的影响,结果表明,含植物复合物n4的凝胶样品对金黄色葡萄球菌、大肠杆菌、绿源性假单胞菌和白色假单胞菌的生物膜形成速度减慢最明显,分别为19.7-20.7%。含有植物复合物n4的凝胶样品的活性是单一组分n1、n2和n3凝胶样品的1.3 ~ 1.4倍。在测定样品破坏生物膜的能力时,发现含有植物复合物n4的凝胶样品的活性最大,其平均超过n5和n6样品的规定性能的1.2倍和1.8倍。单组分凝胶样品n1、n2和n3对金黄色葡萄球菌、大肠杆菌、绿脓杆菌和白色念珠菌生物膜破坏的活性较低。研究证明的可行性进行进一步研究复合凝胶的发朵复杂№4包含干核桃叶提取物与单宁的和没食子酸和干物质30毫克/ 100克的凝胶,干荨麻提取物与hydroxycinnamic酸的和绿原酸,和干物质20毫克/ 100克的凝胶,干百里香和类黄酮的提取芦丁和干物质35毫克/ 100克的凝胶。
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引用次数: 0
Phytochemical analysis of the main groups of secondary metabolites in the Dracocephalum moldavica L. herb 草中主要次生代谢产物的植物化学分析
Pub Date : 2021-10-22 DOI: 10.32352/0367-3057.5.21.09
М. І. Шанайда
The genus Dragonhead (Dracocephalum L.) includes 72 species of essential oil-bearing plants belonging to the Lamiaceae family. Many of them have long been used in a folk medicine of different countries. Moldavian dragonhead (D. moldavica L.) has been identified as the most promising species for the complex phytochemical research since it was successfully introduced in the climatic conditions of the Ukrainian forest-steppe zone and due to the presence of its various botanical forms and varieties. The aim of this study was the phytochemical analysis of the main groups of secondary metabolites in the herb of violet-flowered form of Moldavian dragonhead  (D. moldavica L.) under its cultivation in Ternopil region (Ukraine). The herb of the plant was harvested in July of 2018‒2019 years during the flowering period. The essential oil was obtained from the plant raw material by the hydrodistillation. Such physical and chemical parameters of the essential oil as a relative density, refractive index, optical rotation, acid number and solubility in ethanol were studied. The method of thin layer chromatography (TLC) was used to determine the specific sequence of bands in the chromatograms of essential oil. The method of high-performance thin-layer chromatography (HPTLC) was used for the identification of phenolic compounds in the herb. The component composition of polyphenols was determined by the high performance liquid chromatography (HPLC). The specific physical and chemical parameters as well as the «chromatographic profile» of essential oil have been established. The main compounds of the polyphenolic nature were revealed by the chromatographic methods. In particular, rosmarinic and caffeic hydroxycinnamic acids were identified in the methanol extract of herb by the HPTLC method. The HPLC analysis of phenolic compounds in the 70% ethanol extract of raw material established that rosmarinic acid was its main polyphenol. It was found the decreasing of polyphenol contents in the D. moldavica herb in such direction: rosmarinic acid (3.01%) > apigenin-7-О-glucoside (0.67%) > apigenin (0.29%) > caffeic acid (0.28%) > luteolin-7-О-glucoside (0.13%)> hyperoside (0.12%) > ferulic acid (0.09%) > chlorogenic acid (0.08%). The obtained data could be used for planning pharmacological studies of the phytosubstances developed from the Moldavian dragonhead herb.
龙脑属(Draocephalum L.)包括属于Lamiaceae科的72种必需的含油植物。它们中的许多长期以来一直被用于不同国家的民间医学。Moldavian dragonhead(D.moldavica L.)是在乌克兰森林草原区的气候条件下成功引入的,由于其各种植物形式和品种的存在,已被确定为最有希望进行复杂植物化学研究的物种。本研究的目的是对在捷尔诺波尔地区(乌克兰)种植的摩尔多瓦龙舌兰(D.moldavica L.)紫罗兰花草本植物中的主要次生代谢产物进行植物化学分析。该植物的草本植物于2018年7月至2019年开花期收获。以植物原料为原料,经加氢蒸馏得到精油。研究了精油的相对密度、折射率、旋光度、酸值和在乙醇中的溶解度等理化参数。采用薄层色谱法测定了挥发油色谱图中谱带的具体序列。采用高效薄层色谱法对该药材中的酚类化合物进行了鉴定。采用高效液相色谱法测定了多酚的组分组成。精油的具体物理和化学参数以及“色谱图谱”已经确定。用色谱法分析了主要的多酚类化合物。采用高效薄层色谱法对该药材甲醇提取物中的迷迭香酸和咖啡羟基肉桂酸进行了鉴别。通过对原料70%乙醇提取物中酚类化合物的高效液相色谱分析,确定迷迭香酸是其主要多酚。结果表明,苜蓿多酚含量下降的方向为:迷迭香酸(3.01%)>芹菜素-7-О-葡萄糖苷(0.67%)>芹菜元(0.29%)>咖啡酸(0.28%)>木犀草素-7-Г-葡萄苷(0.13%)>金丝桃苷(0.12%)>阿魏酸(0.09%)>绿原酸(0.08%)由摩尔多瓦龙舌兰草本植物发展而来。
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引用次数: 0
Some transformations and physicochemical properties of new S-substituted 5-thiophene-(3-ylmethyl)-4R-1,2,4-triazole-3-thiols 新型S-取代5-噻吩-(3-基甲基)-4R-1,2,4-三唑-3-硫醇的一些转化及其理化性质
Pub Date : 2021-10-22 DOI: 10.32352/0367-3057.5.21.05
А. В. Хільковець
Nitrogen-containing heterocyclic compounds are widely represented in modern organic chemistry. A special place among the huge number of substances presented is occupied by derivatives of 1,2,4-triazole due to their uniqueness and prospects. In recent years, these derivatives have remained the object of close attention of both synthetic chemists and researchers engaged in the search for new biologically active substances of a wide spectrum of action, the synthesis of optical materials, dyes, corrosion inhibitors, veterinary drugs, etc. It is known from the literature that the combination of the aromatic heterocycle of thiophene and 1,2,4-triazole is a promising area for research. The result of such combinations is a number of compounds obtained with fairly high yields and a wide range of activities. Thus, further chemical modification of 1,2,4-triazole derivatives by additional administration of a typical thiophene pharmacophore is an urgent task. The aim of the study is to obtain new compounds in a number of S-substituted 5-thiophene-(3-ylmethyl)-4R-1,2,4-triazole-3-thiols and study their physico-chemical properties using complex analysis methods. The study of the physical and chemical properties of the compounds obtained was carried out according to methods that meet the standards of the state pharmacopoeia of Ukraine. The synthesis of new compounds was carried out according to generally accepted methods. The previously obtained 5-thiophene-(3-ylmethyl)-4h-1,2,4-triazole-3-thiol and 5-thiophene-(3-ylmethyl)-4-phenyl-1,2,4-triazole-3-thiol were used as starting compounds. Preparation of thioethanones was performed in an alkaline medium in the presence of methanol. The acids were obtained in an alcohol-alkaline medium with the addition of monochloroacetic acid. To obtain esters, two conventional methods were used. The first method is based on the alkylation in an alkaline-alcohol medium of the starting thiols with isopropyl ester of monochloroacetic acid. The second method is the classical esterification reaction. To confirm the structure and study of the physical and chemical properties, all the resulting compounds were crystallized. As a result, some new compounds that were not previously described were obtained, namely: thioethanones, thioacetamides, thioacetic acids, thioacetates, and a number of other thiopo-derivatives of these initial compounds. The structure and individuality of the obtained molecules were confirmed by elemental analysis (CHNS), IR and 1H NMR spectra. A number of new S-derivatives of 5-thiophene-(3-ylmethyl)-4R-1,2,4-triazole-3-thiols have been obtained. The physical and chemical properties of the obtained compounds are determined and their structure is confirmed using modern analysis methods. Some compounds will be transferred for further research.
含氮杂环化合物在现代有机化学中有着广泛的代表性。1,2,4-三唑衍生物由于其独特性和前景,在众多物质中占有特殊地位。近年来,这些衍生物一直是合成化学家和研究人员密切关注的对象,他们致力于寻找具有广泛作用的新生物活性物质,合成光学材料、染料、缓蚀剂、兽药等。从文献中可以看出,噻吩与1,2,4-三唑的芳香杂环的结合是一个很有前途的研究领域。这种组合的结果是以相当高的产率和广泛的活性获得了许多化合物。因此,通过额外给药典型的噻吩药效团对1,2,4-三唑衍生物进行进一步的化学修饰是一项紧迫的任务。本研究的目的是在一些S-取代的5-噻吩-(3-基甲基)-4R-1,2,4-三唑-3-硫醇中获得新的化合物,并使用复杂的分析方法研究它们的物理化学性质。根据符合乌克兰国家药典标准的方法对获得的化合物的物理和化学性质进行了研究。新化合物的合成是根据公认的方法进行的。使用先前获得的5-噻吩-(3-基甲基)-4h-1,2,4-三唑-3-硫醇和5-噻吩-。硫代乙酮的制备是在甲醇存在下在碱性介质中进行的。酸是在添加一氯乙酸的醇碱性介质中获得的。为了获得酯,使用了两种常规方法。第一种方法基于起始硫醇与一氯乙酸异丙酯在碱性醇介质中的烷基化。第二种方法是经典的酯化反应。为了证实结构和物理化学性质的研究,所有得到的化合物都被结晶。结果,获得了一些以前没有描述的新化合物,即:硫代乙酮、硫代乙酰胺、硫代乙酸、硫代乙酸盐和这些初始化合物的许多其他硫代衍生物。通过元素分析(CHNS)、IR和1H NMR光谱证实了所获得的分子的结构和个性。得到了一些新的5-噻吩-(3-基甲基)-4R-1,2,4-三唑-3-硫醇的S-衍生物。使用现代分析方法测定了所获得的化合物的物理和化学性质,并确认了它们的结构。一些化合物将被转移用于进一步研究。
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引用次数: 1
Analysis of the vitamin’s list with pharmacoeconomic rates for the treatment of long covid conditions during the pandemic COVID-19 in Ukraine 在乌克兰新冠肺炎大流行期间,维生素列表与治疗长期新冠肺炎疾病的药物经济率分析
Pub Date : 2021-10-22 DOI: 10.32352/0367-3057.5.21.02
Я. О. Гриньків, О. Б. Блавацька, Г. Ю. Яцкова, О. М. Заліська
To ensure adequate vital activity, especially during the COVID-19 pandemic, the human body needs, in particular vitamins, minerals (macro and micronutrients). The purpose of the study is the range, qualitative and quantitative composition of vitamin complexes (VC) in the pharmaceutical market of Ukraine; to develop a method of pharmacoeconomic analysis to determine the cost of treatment of VC. Materials of research – data DRLZ, «Compendium», prices for VC (www.tabletki.ua). Research methods: webometric, comparative, content, «cost minimization» analysis; systematization, generalization. 20 VCs were analyzed, of which 15 – group A11A (75%) and 5 – A11B (25%). The highest content of vitamins in: Elevit Pronatal, Vitrum Energy, etc. All groups of vitamins contain: Vitrum Centuri, Vitrum Energy. The least vitamins in – Metovitan, Optics. Vitrum Centuri and Vitrum Energy contain most of the trace elements. Metovitan, Optics, Quadevit contain the least amount of trace elements. In addition to trace elements, the composition of VC includes: amino acids (cysteine, methionine), papain, fish oil, etc. It is established that the recommended doses of vitamins A, C, B1, B2, B5, B6, B12 in Ukraine are higher than recommended by the WHO; D, B9, H – the recommended doses in Ukraine are lower than recommended by the WHO; recommended doses of all trace elements in Ukraine are higher than the WHO. 20 VCs are registered in Ukraine, of which 15 are group A11A and 5 are A11B. 90% of VC contain vitamins A, E, C, B1, B2, B9, B12, PP. Vitamin B6 – in 85% of VC; vitamin D3 is in the composition of 62% of VC; vitamin B5 – 58%; vitamins H and K – in the composition of almost 15% of VC. It was found that 54% of VCs contain calcium; 61.5% of VC contain iron and copper; 31% of VC contain phosphorus and manganese; up to 23% of VCs contain molybdenum, boron, nickel, vanadium, tin, etc. It is established that Zinc is a part of 62% of VCs registered in Ukraine. The results of pharmacoeconomic analysis by the method of «minimization of cost» showed that the affordability of domestic multivitamin and vitamin-mineral complexes are 1.5–4.7 times more economically affordable for treatment compared to imported, with a qualitative composition are similar. Quantitative content of vitamins and minerals in domestic VC meets the national requirements of daily intake.
为确保足够的生命活动,特别是在2019冠状病毒病大流行期间,人体需要维生素、矿物质(宏量营养素和微量营养素)。该研究的目的是范围,定性和定量组成的维生素复合物(VC)在乌克兰的医药市场;开发一种药物经济学分析方法来确定VC的治疗费用。研究资料-数据DRLZ,«纲要»,价格为VC (www.tabletki.ua)。研究方法:网络测量法、比较法、内容分析法、“成本最小化”分析法;系统化、泛化。分析了20个vc,其中A11A组15个(75%),A11B组5个(25%)。维生素含量最高的有:升脂、维生素能等。所有种类的维生素都含有:半人马座维生素,能量维生素。维他命最少的-美托维坦,光学。半人马座的Vitrum和Vitrum Energy含有大部分的微量元素。美托维坦、光学、Quadevit中微量元素含量最少。VC的组成除微量元素外,还包括:氨基酸(半胱氨酸、蛋氨酸)、木瓜蛋白酶、鱼油等。现已确定,乌克兰的维生素A、C、B1、B2、B5、B6、B12的推荐剂量高于世界卫生组织的推荐剂量;D、B9、H——乌克兰的推荐剂量低于世卫组织的推荐剂量;乌克兰所有微量元素的推荐剂量都高于世界卫生组织。在乌克兰注册的vc有20家,其中A11A组15家,A11B组5家。90%的VC含有维生素A、E、C、B1、B2、B9、B12、PP, 85%的VC含有维生素B6;维生素D3占VC的62%;维生素B5 - 58%;维生素H和K -几乎占VC的15%研究发现,54%的vc含有钙;61.5%的VC含铁、铜;31%的VC含有磷和锰;高达23%的vc含有钼、硼、镍、钒、锡等。可以确定的是,Zinc是在乌克兰注册的62%的vc的一部分。采用“成本最小化”方法进行的药物经济学分析结果表明,国产复合维生素和维生素矿物质复合物的经济可承受性是进口的1.5-4.7倍,其定性成分相似。国产VC中维生素、矿物质定量含量符合国家每日摄入量要求。
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引用次数: 1
Determination of the total content of flavonoids in herbal mixtures with anti-diabetic activity 抗糖尿病中药合剂中总黄酮含量的测定
Pub Date : 2021-10-22 DOI: 10.32352/0367-3057.5.21.08
А. О. Савич, Л. С. Криськів, Л. М. Мосула
Diabetes mellitus is an important social and medical problem, as it causes the development of dangerous complications that lead to disability and mortality. This disease is characterized by a multi-vector pathogenesis that requires a comprehensive approach to treatment. Due to the use of mixtures of medicinal plants in the treatment of diabetes, it is possible to cover all aspects of the development of this disease and its complications, because the combination of different medicinal plants contain more biologically active substances that affect all parts of the pathogenetic mechanism of diabetes mellitus and its complications. Plant biocompounds have a wide range of pharmacological action and various mechanisms of influence on the development of diabetes and diabetic angiopathies (inactivation of the antioxidant defense system, activation of lipid peroxidation and the development of oxidative stress). In addition, the niche of the pharmaceutical market of Ukraine with phytomixtures is almost empty. The aim of the work was to study the total flavonoid content in some herbal mixtures, which have established hypoglycemic, hypolipidemic and antioxidant activity in previous studies in vivo The study of the total flavonoid content in herbal samples was carried out by UV-spectrophotometry with the recording of the absorption spectrum of complexation product of flavonoids with aluminum chloride (λmax 415 nm) in terms of rutin. According to the results of UV-spectrophotometric determination, it was found that the total flavonoid content in the herbal mixture No 3 was 1.47 ± 0.04%, in the herbal mixture No 4 – 1.78 ± 0.04%, in the herbal mixture No 7 – 1.29 ± 0.02%, in the herbal mixture No 13 – 1.16 ± 0.02% and in the herbal mixture No 19 – 3.62 ± 0.06% in terms of rutin. It was found that the best flavonoid content (3.62 ± 0.06%) was found in the plant mixture № 19, which contains nettle leaves, dandelion roots, blueberry leaves, rose hips and peppermint herb. Phytochemical studies may indicate a correlation between the content of flavonoids and pharmacological properties of the studied mixtures, because the functional hydroxyl groups of the latter cause strong antioxidant activity by neutralizing free radicals, chelation of heavy metal ions, increasing the activity of antioxidant protection products, which has been confirmed in previous in vivo and in vitro studies.
糖尿病是一个重要的社会和医学问题,因为它会导致危险的并发症,导致残疾和死亡。这种疾病的特点是多媒介发病机制,需要综合治疗。由于将药用植物的混合物用于治疗糖尿病,因此有可能涵盖该疾病及其并发症发展的各个方面,因为不同药用植物的组合含有更多的生物活性物质,这些物质影响糖尿病及其并发症发病机制的各个部分。植物生物化合物对糖尿病和糖尿病血管病变的发展具有广泛的药理作用和各种影响机制(抗氧化防御系统的失活、脂质过氧化的激活和氧化应激的发展)。此外,乌克兰药用植物混合物市场的利基市场几乎空无一人。本工作的目的是研究一些草药混合物中的总黄酮含量,以往体内研究中的降血脂和抗氧化活性采用紫外分光光度法研究了中草药样品中总黄酮的含量,记录了黄酮与氯化铝络合产物(λmax 415nm)以芦丁表示的吸收光谱。根据紫外分光光度法测定结果,发现3号草药混合物中总黄酮含量为1.47±0.04%,4–1.78±0.04%、7–1.29±0.02%、13–1.16±0.02%和19–3.62±0.06%,以芦丁计。结果表明,该植物混合物中黄酮类化合物含量最高(3.62±0.06%)№ 19,含有荨麻叶、蒲公英根、蓝莓叶、玫瑰果和薄荷草。植物化学研究可能表明黄酮类化合物的含量与所研究混合物的药理学性质之间存在相关性,因为后者的功能羟基通过中和自由基、螯合重金属离子、增加抗氧化保护产物的活性、,这已在先前的体内和体外研究中得到证实。
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引用次数: 0
Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles 新型3- r -6-(5-芳基呋喃-2-基-[1,2,4]三唑[3,4-b][1,3,4]噻二唑的合成及抗肿瘤性能
Pub Date : 2021-10-22 DOI: 10.32352/0367-3057.5.21.04
І. І. Мирко, Ю. И. Горак, Тарас И. Чабан, І. В. Драпак, В. С. Матійчук
One of the promising methods of creating antitumor drugs is the screening of potential antitumor agents among synthesized compounds. Nitrogen-based heterocycle analogues are an extremely important class of organic substances that are widely used in medical chemistry. [1,2,4]Triazolo[3,4-b][1,3,4] thiadiazoles are among the little-studied and hard-to-reach members of this class of compounds. The aim of our work was to synthesize some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, as well as the study of their antitumor activity. The objects of study were 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. The composition and structure of the synthesized compounds were confirmed by the data of elemental analysis and 1H NMR spectroscopy. The antitumor activity of the synthesized compounds was studied in the framework of the international scientific program of the National Cancer Institute (Bethesda, Maryland, USA) DTP NCI (Developmental Therapeutic Program). The synthesis of 11 derivatives of 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles was carried out. These substances are obtained by the interaction of 5-arylfuran-2-carboxylic acids with 5-substituted 4-amino-4H-1,2,4-triazolo-3-thiols. Primary screening revealed individual 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles, which showed pronounced selective antitumor activity. The most active among the tested compounds were 3 d, 3 e and 3 j, which were further investigated during secondary screening. The results of these studies confirm the high antitumor activity of these compounds. The proposed approaches and the developed synthesis protocols made it possible to obtain a series of new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles. The results of studies of the antitumor activity of the synthesized compounds made it possible to single out 3 highly active compounds with high antitumor activity, which gives reason to consider this condensed system as a promising molecular framework for the design of potential antitumor agents.
从合成的化合物中筛选潜在的抗肿瘤药物是开发抗肿瘤药物的一种很有前途的方法。氮基杂环类似物是一类极为重要的有机物质,在医学化学中有着广泛的应用。[1,2,4]三唑[3,4-b][1,3,4]噻二唑是这类化合物中研究较少且难以达到的成员之一。本文的目的是合成一些新的3- r -6-(5-芳基呋喃-2-基-[1,2,4]三唑[3,4-b][1,3,4]噻二唑,并研究它们的抗肿瘤活性。研究对象为3- r -6-(5-芳基呋喃-2-基-[1,2,4]三唑[3,4-b][1,3,4]噻二唑。合成的化合物的组成和结构经元素分析和核磁共振氢谱分析证实。合成化合物的抗肿瘤活性在美国国家癌症研究所(Bethesda, Maryland, USA) DTP NCI (Developmental Therapeutic program)国际科学计划框架下进行了研究。合成了11个3- r -6-(5-芳基呋喃-2-基-[1,2,4]三唑[3,4-b][1,3,4]噻二唑衍生物。这些物质是由5-芳基呋喃-2-羧酸与5-取代的4-氨基- 4h -1,2,4-三唑-3-硫醇相互作用得到的。初步筛选发现个别3- r -6-(5-芳基呋喃-2-基-[1,2,4]三唑[3,4-b][1,3,4]噻二唑具有明显的选择性抗肿瘤活性。其中活性最高的是3d、3e和3j,这些化合物在二次筛选中得到了进一步的研究。这些研究结果证实了这些化合物具有较高的抗肿瘤活性。所提出的方法和所开发的合成方案使得得到一系列新的3- r -6-(5-芳基呋喃-2-基-[1,2,4]三唑[3,4-b][1,3,4]噻二唑成为可能。通过对所合成化合物抗肿瘤活性的研究,可以筛选出3种具有高抗肿瘤活性的高活性化合物,这就有理由认为该浓缩体系是设计潜在抗肿瘤药物的一个有前途的分子框架。
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引用次数: 0
Research of the relationship between educational and professional programs of higher pharmaceutical education in Ukraine with the «Ten-star pharmacist» concept 以“十星级药剂师”概念研究乌克兰高等药学教育教育与专业课程的关系
Pub Date : 2021-10-22 DOI: 10.32352/0367-3057.5.21.03
Ю. І. Кремінь, Б. П. Громовик
Currently, the training of Masters of Pharmacy (MPh) in Ukraine is based on the competency model as a list of competencies and program learning outcomes according to academic disciplines, which is reflected in the educational and professional programs (EPP) institutions of higher pharmaceutical education (IHPhE). At the same time, MPh, as public trust workers, must have all professional roles (PR) in accordance with of the «ten-star pharmacist» concept. The aim of the study was to analyze the relationship between general (GC) and professional (PC) competencies of MPh and current PR according to the «ten-star pharmacist» concept. The materials of the study were EPP of twenty-two IHPhE that train masters in the specialty 226 «Pharmacy, industrial pharmacy». Methods of critical analysis, generalization, specification and interpretation of results are used. It was found that the lists of GC and PC differ in the analyzed EPP. It is determined that according to the presence of common GC IHPhE can be divided into three groups, while for PC there are six such groups. Significant differences in the formation of individual PR of future MPh due to acquisition them of different numbers of GC and PC are noted. It is established that in the studied EPP of twenty-two IHPhE for the preparation of masters in the specialty 226 «Pharmacy, Industrial Pharmacy» there are 15 GC and 35 PC. At the same time, the majority of GC (12 out of 15) and the minority of PC (16 out of 35) of the studied EPP are similar. Significant differences were found in the formation of the PR MPh, in particular, the analyzed GC do not sufficiently reflect PR a life-long-learner (only GC 4 in all groups and GC 15 in group Z). In PC, this picture is typical for PR a decision-maker (only PC 16 in all groups) and a teacher (PC 1 and 2 in all groups). It is shown that the lack of unified compliance of the studied EPP with PC will not contribute to the formation of MPh, adequate to pharmaceutical practice, and their acquisition of the necessary PR in accordance with the «ten-star pharmacist» concept.
目前,乌克兰的药学硕士(MPh)培训是基于能力模型作为根据学科的能力和项目学习成果列表,这反映在高等药学教育(IHPhE)的教育和专业课程(EPP)机构中。同时,MPh作为社会信托工作者,必须具备符合“十星级药剂师”理念的所有专业角色(PR)。本研究的目的是根据“十星级药剂师”的概念,分析普通(GC)和专业(PC)能力与当前PR之间的关系。本研究的材料是22名培养专业226“药学,工业药学”硕士的IHPhE的EPP。使用批判性分析,概括,规范和结果解释的方法。在分析的EPP中,GC和PC的表列不同。根据常见GC的存在,确定IHPhE可分为3类,PC可分为6类。由于获取不同数量的GC和PC,未来MPh个体PR的形成有显著差异。结果表明,在为226“药学,工业药学”专业硕士学位准备的22名IHPhE中,有15名GC和35名PC。同时,所研究的EPP中大多数GC(12 / 15)和少数PC(16 / 35)是相似的。在PR - MPh的形成上发现了显著的差异,特别是,所分析的GC并没有充分反映PR作为终身学习者(所有组中只有GC 4, Z组中只有GC 15)。在PC中,这幅图是典型的PR作为决策者(所有组中只有pc16)和教师(所有组中只有pc1和2)。结果表明,所研究的EPP与PC缺乏统一的符合性,将不利于形成符合制药实践的MPh,并根据“十星级药剂师”的概念获得必要的PR。
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引用次数: 1
Research of assortment and price condition of the regional market of antidepressants for treatment of women in prenatal and postnatal periods 妇女产前产后抗抑郁药区域市场分类及价格状况研究
Pub Date : 2021-08-26 DOI: 10.32352/0367-3057.4.21.05
М. Є. Матвійчук, Б. П. Громовик
According to studies, depression in women occurs during pregnancy or within 4 weeks after delivery and can last up to 6 months. or even up to a year after birth. The most common in treating depression in pregnant women and during breastfeeding are antidepressants of selective serotonin reuptake inhibitors (SSRIs) group. The study aimed research the range and price situation in pharmacies (on the example of Lviv) of antidepressants SSRIs group used to treat depression in women in the prenatal and postnatal periods. The objects were the data of the State Register of Medicinal Products of Ukraine and the ATC / DDD Index 2021 and also information on the prices for medicines in pharmacies in Lviv and the average salary of full-time employees in Lviv region as of February 2021. Methods used: system, statistical, comparison analysis, generalization. It is shown that in Lviv pharmacies there were more than half of the trade names (TNs) of antidepressants of the SSRIs group registered in Ukraine. Based on 1 defined daily dose (DDD), on the one hand, competitive pricing and relative economic affordability for four-fifths of the studied drugs in terms of specific TNs, on the other ‒ a small number (14.6%) of the most affordable TNs antidepressants of the SSRIs group. We researched that there were six international non-proprietary names of antidepressants of the SSRIs group in the form of 77 trade names (TN) were registered in Ukraine in February 2021. There were only 41 or 53.9% of their TN was present in Lviv pharmacies. We determined that the lowest prices of 1 DDD among the TNs antidepressants of SSRIs group are characteristic of Fluxen capsules № 30 and Fluoxetine 20 mg tablets of Ukrainian production. The highest prices of 1 DDD are inherent in the Cipramil 20 mg tablets and Cipralex 10 mg tablets of Danish production. We found that the overall value of the price liquidity ratio for the vast majority (33 or 80,5% out of 41 TNs) antidepressants of SSRIs group of TNs present in pharmacies in Lviv does not exceed 0.5, which indicates an intensely competitive environment in the regional market of these drugs and the relative availability in pharmacies of a particular TN of the studied antidepressants. On the other hand, the most affordable for a price of 1 DDD were only 6 or 14.6% of TNs antidepressants of the SSRIs group, which have low values of affordability.
根据研究,女性的抑郁症发生在怀孕期间或产后4周内,可能持续6个月。甚至在出生后一年内。治疗孕妇和哺乳期抑郁症最常见的是选择性血清素再摄取抑制剂组的抗抑郁药。该研究旨在研究药店(以利沃夫为例)用于治疗产前和产后妇女抑郁症的抗抑郁药SSRIs组的范围和价格情况。对象是乌克兰国家药品注册局和2021年ATC/DDD指数的数据,以及利沃夫药店药品价格和利沃夫地区全职员工截至2021年2月的平均工资信息。采用的方法有:系统法、统计法、比较分析法、归纳法。研究表明,在利沃夫的药店中,有一半以上的抗抑郁药在乌克兰注册。基于1个限定日剂量(DDD),一方面,五分之四的研究药物在特定TNs方面的竞争性定价和相对经济可负担性,另一方面,SSRIs组中少数(14.6%)最负担得起的TNs抗抑郁药。我们研究了2021年2月在乌克兰注册的SSRIs集团抗抑郁药的六个国际非专有名称,其形式为77个商品名(TN)。利沃夫的药店中只有41个或53.9%的TN。我们确定,在SSRIs组的TNs抗抑郁药中,1 DDD的最低价格是Fluxen胶囊的特征№ 30和乌克兰生产的氟西汀20mg片剂。1 DDD的最高价格是丹麦生产的20 mg西帕明片剂和10 mg西帕乐片剂的固有价格。我们发现,利沃夫药店中存在的绝大多数(41种TNs中的33种或80.5%)SSRIs类TNs抗抑郁药的价格流动性比率的总体值不超过0.5,这表明这些药物的区域市场竞争激烈,并且所研究的抗抑郁药在药店中的特定TN的相对可用性。另一方面,对于1 DDD的价格,最负担得起的是SSRIs组中只有6%或14.6%的TNs抗抑郁药,它们的负担能力值较低。
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Farmatsevtichnii zhurnal
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