Ceska a Slovenska Farmacie最新文献_第6页

Synthesis, characterization, molecular docking studies of new alkyl derivatives of 5-(2-bromo-4-fluorophenyl)-4-ethyl-4H- -1,2,4-triazole-3-thiol. 5-（2-溴-4-氟苯基）-4-乙基-4H--1,2,4-三唑-3-硫醇新烷基衍生物的合成、表征和分子对接研究。

Ceska a Slovenska Farmacie Pub Date : 2023-01-01

Roman Shcherbyna, Valerü Kalchenko, Sergii Kulish, Volodymyr Salionov, Liubov Morozova, Natalia Nedorezaniuk, Olha Mazur

{"title":"Synthesis, characterization, molecular docking studies of new alkyl derivatives of 5-(2-bromo-4-fluorophenyl)-4-ethyl-4H- -1,2,4-triazole-3-thiol.","authors":"Roman Shcherbyna, Valerü Kalchenko, Sergii Kulish, Volodymyr Salionov, Liubov Morozova, Natalia Nedorezaniuk, Olha Mazur","doi":"","DOIUrl":"","url":null,"abstract":"The main goal of this article is to present the results of the synthesis of new alkyl derivatives of 5-(2-bromo4-fluorophenyl)-4-ethyl-4H-1,2,4-triazole-3-thiol and molecular docking studies against COX-1 and COX-2. Previous studies have established a wide range of biological activity of 1,2,4-triazole derivatives. Therefore, it was essential to determine how a new series of 1,2,4-triazole derivatives would provide potential anti-inflammatory activity. To reach the goal, raw alkyl derivatives of 5-(2-bromo-4-fluorophenyl)-4-ethyl-4H-1,2,4-triazole-3-thiols (2a-2i) from 5-(2-bromo-4-fluorophenyl)-4-ethyl-4H-1,2,4-triazole3-thiol (1e) were obtained. The structure of the synthesized compounds was confirmed by 1H-NMR elemental analyses. The individuality and purity of compounds were confirmed by the method of liquid chromatography-mass spectrometry. These compounds have a relatively simple synthesis scheme, which gives them an advantage in creating a potential drug, and the appearance of alkyl radicals in the molecule should positively affect pharmacokinetic indicators, stability, selectivity, and bioavailability. An in silico study was conducted for the synthesized compounds, namely molecular docking, in relation to the interaction with COX-1 and COX-2. Based on the selectivity indexes of binding modes observed for the selected compounds (2e, 2g) with active COX-1 centers, it was found that compounds can reliably exhibit their anti-inflammatory effect through the prostaglandin biosynthesis pathway, inhibiting COX-1 instead of COX-2. The effect of hydrophobic interactions of alkyl groups of 1,2,4-triazole derivatives on changes in affinity and selectivity to COX-1 or COX-2 has also been proven. Therefore, derivatives of 1,2,4 are promising candidates for improvement, further study, and future development of new, more powerful antiinflammatory drugs for therapeutic use.","PeriodicalId":38771,"journal":{"name":"Ceska a Slovenska Farmacie","volume":"72 4","pages":"190-200"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41162693","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

Entry and competition of retail pharmacies: A case study of OTC drugs sales and ownership deregulation1. 零售药店的进入与竞争:以非处方药销售与所有权放松管制为例

Ceska a Slovenska Farmacie Pub Date : 2023-01-01 DOI: 10.5817/csf2023-1-11

Matúš Bilka, A. P. Duarte, M. Lábaj

{"title":"Entry and competition of retail pharmacies: A case study of OTC drugs sales and ownership deregulation1.","authors":"Matúš Bilka, A. P. Duarte, M. Lábaj","doi":"10.5817/csf2023-1-11","DOIUrl":"https://doi.org/10.5817/csf2023-1-11","url":null,"abstract":"This study provides new empirical evidence on the changes in competition and entry decisions of pharmacies after regulatory changes. It investigates the development of the retail pharmacy market in Portugal, which underwent major regulatory changes in 2004 and 2007. Sale of OTC drugs and ownership of pharmacies were liberalized while entry restrictions related to market size and the location of new pharmacies prevailed. Our empirical strategy was based on entry models and provided indirect information on the toughness of competition and entry decisions of firms in the market. We estimated and compared the entry thresholds and their ratios before and after liberalization. Such a comparison allows to see if competition got tenser with OTC drugs deregulated. There were three main findings from the study. First, the entry thresholds decreased regardless of the number of pharmacies in the market, suggesting that room for the realization of profits is broader than it was in the past. Second, although the entry thresholds were lower in value, their increase was steeper with each incumbent in 2020, suggesting harsher price competition with new entrants. Third, the current rule of 3,500 patients per pharmacy is likely overly restrictive, pharmacies could break-even even in smaller markets.","PeriodicalId":38771,"journal":{"name":"Ceska a Slovenska Farmacie","volume":"72 1 1","pages":"11-20"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"71344677","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

Prospects of сomplex pharmaceutical composition application for pharmacological correction of metabolic syndrome. 应用复方药物成分对代谢综合征进行药物矫正的前景。

Ceska a Slovenska Farmacie Pub Date : 2023-01-01

Kateryna Kalko, Nadia Dukhnich, Oksana Mishchenko, Viktor Khomenko, Olena Toziuk

{"title":"Prospects of сomplex pharmaceutical composition application for pharmacological correction of metabolic syndrome.","authors":"Kateryna Kalko, Nadia Dukhnich, Oksana Mishchenko, Viktor Khomenko, Olena Toziuk","doi":"","DOIUrl":"","url":null,"abstract":"Metabolic syndrome (MetS) is a symptomatic complex characterized by insulin resistance, impaired prooxidant-antioxidantbalance of the body with the development of subchronic inflammation, and dyslipidemia. The aim of the study is to investigate the effect of a complex pharmaceutical composition (CPC) (antioxidants and metabolitotropic agents), which is widely used in medical practice in Ukraine as a multivitamin complex, on experimental metabolic syndrome in rats. The effectof CPC on the correction of experimental MetS in rats, induced by a high content of carbohydrates and fats in the diet, was assessed. MetS in rats was characterized by a decrease in the sensitivity of cells to insulin, increased glucose content, and aviolation of its utilization, prooxidant-antioxidant disbalance. The results of the conducted studies indicate the positive effect of CPC, which contains ethyl esters of omega-3 acids, vitamin E, coenzyme Q10, zinc, vitamin A, biotin, and selenium, on the sensitivity of cells to insulin, glucose utilization, duration of hyperglycemia and indicators of free radical oxidation processes and antioxidant defense systems in rats with experimental MetS. These results prove the feasibility of using CPC to correct metabolic syndrome.","PeriodicalId":38771,"journal":{"name":"Ceska a Slovenska Farmacie","volume":"72 6","pages":"287-295"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139724406","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

Entry and competition of retail pharmacies: A case study of OTC drugs sales and ownership deregulation1. 零售药店的进入与竞争:以非处方药销售与所有权放松管制为例

Ceska a Slovenska Farmacie Pub Date : 2023-01-01

Matúš Bilka, António Portugal Duarte, Martin Lábaj

{"title":"Entry and competition of retail pharmacies: A case study of OTC drugs sales and ownership deregulation1.","authors":"Matúš Bilka, António Portugal Duarte, Martin Lábaj","doi":"","DOIUrl":"","url":null,"abstract":"This study provides new empirical evidence on the changes in competition and entry decisions of pharmacies after regulatory changes. It investigates the development of the retail pharmacy market in Portugal, which underwent major regulatory changes in 2004 and 2007. Sale of OTC drugs and ownership of pharmacies were liberalized while entry restrictions related to market size and the location of new pharmacies prevailed. Our empirical strategy was based on entry models and provided indirect information on the toughness of competition and entry decisions of firms in the market. We estimated and compared the entry thresholds and their ratios before and after liberalization. Such a comparison allows to see if competition got tenser with OTC drugs deregulated. There were three main findings from the study. First, the entry thresholds decreased regardless of the number of pharmacies in the market, suggesting that room for the realization of profits is broader than it was in the past. Second, although the entry thresholds were lower in value, their increase was steeper with each incumbent in 2020, suggesting harsher price competition with new entrants. Third, the current rule of 3,500 patients per pharmacy is likely overly restrictive, pharmacies could break-even even in smaller markets.","PeriodicalId":38771,"journal":{"name":"Ceska a Slovenska Farmacie","volume":"72 1","pages":"11-20"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10823793","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

A study of hypoglycemic activity of acids and salts containing 1,2,4-triazole. 含有1,2,4-三唑的酸和盐的降糖活性研究。

Ceska a Slovenska Farmacie Pub Date : 2023-01-01

Dmytro Dovbnia, Yuliia Frolova, Andrii Kaplaushenko

{"title":"A study of hypoglycemic activity of acids and salts containing 1,2,4-triazole.","authors":"Dmytro Dovbnia, Yuliia Frolova, Andrii Kaplaushenko","doi":"","DOIUrl":"","url":null,"abstract":"This article presents the study results of the hypoglycemic properties among 1,2,4-triazole derivatives synthesized at the Department of Physical and Colloidal Chemistry of the Zaporizhzhia State Medical University. Today, many people have a sedentary way of life, also most of their diet contains products that they frequently use, which increase the level of glucose in the blood, which can provoke the development of serious diseases. Therefore, to date, the creation of drugs that exhibit hypoglycemic activity and have a low level of toxicity remains an urgent task for medicine and pharmacy. In the first stage of our research, acute toxicity prediction was performed. The hypoglycemic activity of the synthesized compounds was assessed by performing an intraperitoneal glucose tolerance test (IPGTT) with a change in the blood glucose concentration of the animal after its single intraperitoneal administration in the form of a 40% solution at a dose of 2 g/kg of rat body weight. Thirty-eight compounds of the different classes were studied for hypoglycemic activity. Zinc (II) 2-{5-[(3,4-methoxyphenyl)-3H-1,2,4-triazole-3-yl]thio} acetate (3.18) showed the highest efficiency in terms of the ability to lower blood glucose levels, namely, by 27.3% (approximately 1.3 times).","PeriodicalId":38771,"journal":{"name":"Ceska a Slovenska Farmacie","volume":"72 3","pages":"113-124"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10127439","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

Diazotization titrations in pharmacopoeial quality control of medicines and proposals for their revision in the European Pharmacopoeia. 药典药品质量控制中的重氮滴定法及其在《欧洲药典》中的修订建议。

Ceska a Slovenska Farmacie Pub Date : 2023-01-01

Jan Šubert, Jozef Kolář, Jozef Čižmárik

引用次数: 0

Study of the anti-inflammatory properties of a thick extract of Tribulus terrestris L. 雷公藤粗提物抗炎作用的研究。

Ceska a Slovenska Farmacie Pub Date : 2023-01-01

Saida Yunusova, Yaroslav Rozhkovskyi, Bohdan Prystupa, Svitlana Bohatu

{"title":"Study of the anti-inflammatory properties of a thick extract of Tribulus terrestris L.","authors":"Saida Yunusova, Yaroslav Rozhkovskyi, Bohdan Prystupa, Svitlana Bohatu","doi":"","DOIUrl":"","url":null,"abstract":"The most promising direction in the treatment of chronic prostatitis is the use of medicinal plants and preparations based on them, which contain natural compounds with a broad spectrum of pharmacological activity: anti-inflammatory, antimicrobial, reparative, immunomodulatory, hormone-regulating, antisclerotic, etc., and which can provide a complex therapeutic effect on the course of chronic prostatitis. A promising raw material in this direction is Tribulus terrestris L., a herbal preparation traditionally used to treat erectile dysfunction and atherosclerosis. This experimental work aims to study the anti-inflammatory activity of a thick extract of the Tribulus terrestris grass (freed from fruits) on the models of carrageenan and zymosan inflammation in rats. In the models of carrageenan and zymosan edema in rats, a thick extract of Tribulus terrestris L. in doses from 50 mg/kg to 200 mg/kg shows anti-inflammatory activity, the efficacy of which in the dose range of 150-200 mg/g in the initial stages of carrageenan inflammation is not inferior to sodium diclofenac at a dose of 8.0 mg/kg, and in the initial stages of zymosan inflammation, respectively, before the reference drug corvitin at a dose of 10 mg/kg. It indicates the anticyclogenase and antilipoxygenase properties of this thick extract.","PeriodicalId":38771,"journal":{"name":"Ceska a Slovenska Farmacie","volume":"72 4","pages":"184-189"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41162456","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

Ethical aspects of conducting clinical trials of human medicinal products. 进行人类医药产品临床试验的伦理问题。

Ceska a Slovenska Farmacie Pub Date : 2023-01-01

Anetta Jedličková

引用次数: 0

Marketing research of combined drugs for treatment of cardiovascular diseases. 治疗心血管疾病联合用药的市场研究。

Ceska a Slovenska Farmacie Pub Date : 2023-01-01

Nataliia S Behei, Oksana V Tryhubchak

引用次数: 0

Childhood obesity: causes, consequences, and prevention. 儿童肥胖:原因、后果和预防。

Ceska a Slovenska Farmacie Pub Date : 2023-01-01

Aus Tariq Ali, Faisal Al-Ani, Osamah Al-Ani

{"title":"Childhood obesity: causes, consequences, and prevention.","authors":"Aus Tariq Ali, Faisal Al-Ani, Osamah Al-Ani","doi":"","DOIUrl":"","url":null,"abstract":"As a result of the dramatic increase in the prevalence of overweight and obesity among children, childhood obesity is one of the most critical global public health challenges of the 21st century. Weight gain occurs when energy intake exceeds energy expenditure. Both genetic and environmental factors (such as a sedentary lifestyle) are implicated in its pathogenesis. Childhood obesity is associated with physical, psychological, and social consequences. Obese children are at higher risk of elevated fasting blood glucose, insulin resistance, impaired glucose tolerance, type 2 diabetes, hypertension, polycystic ovarian syndrome (PCOS), atherosclerosis and cardiovascular disease (CVD), sleep apnea, and asthma. Psychological and social consequences include low self-esteem, social discomfort and isolation, and depression. Since COVID-19 was declared a global pandemic, millions of children and adolescents worldwide have been affected drastically. While COVID-19 has increased the prevalence of weight gain and childhood obesity, obese children, on the other hand, have suffered excessively from COVID-19. Here, we provide details on the endocrine, metabolic, and epidemiological aspects of childhood obesity with a concise discussion of the relationship between COVID-19 and childhood obesity. The endocrine chapter is focused on childhood obesity pathophysiology and the role of adipocytes and insulin in the mechanism of obesity. The metabolic chapter covered metabolic diseases related to childhood obesity. In contrast, the epidemiological chapter covered the risk factors of childhood obesity and current approaches to the prevention of childhood obesity.","PeriodicalId":38771,"journal":{"name":"Ceska a Slovenska Farmacie","volume":"72 1","pages":"21-36"},"PeriodicalIF":0.0,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9384834","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