ScienceRise: Pharmaceutical Science最新文献

{"title":"Determination of standardization parameters of Oxycoccus macrocarpus (Ait.) Pursh and Oxycoccus palustris Pers. Leaves","authors":"I. Vlasova, T. Gontova, L. Grytsyk, G. Zhumashova, Galiya Sayakova, A. Boshkayeva, M. Shanaida, O. Koshovyi","doi":"10.15587/2519-4852.2022.260352","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.260352","url":null,"abstract":" The aim. Extracts of cranberry large leaves have prospects when used to correct insulin-resistant conditions. There­fore, to create new drugs based on cranberry leaves, you need to develop instructions for cultivating the plant, harvesting raw materials and methods of quality control. Therefore, the aim of the research was to determine the pa­rameters of standardization of large cranberry leaves (Oxycoccus macrocarpus (Ait.) Pursh) and swamp cranberries (Oxycoccus palustris Pers.).\u0000Materials and methods. Macro- and microscopic studies of raw materials were performed according to the method of SPhU 2.8.23 “Microscopic examination of medicinal plant raw materials”. Macroscopic examinations were per­formed using a magnifying glass and MBS-9 binocular microscope. Identification of basic substances was performed by TLC, testing and quantification of flavonoids according to SPhU methods.\u0000Results. The morphological and anatomical features of the leaves of common cranberry and large cranberry were determined. The general features of the structure of stems and leaves species and different differences for each species are were revealed. TLC identification of the main BAS of raw materials was developed and standardization parameters were determined.\u0000Conclusions. The parameters of cranberry leaf standardization are determined by the following indicators: mac­ro-and microscopic features, TLC identification of the main BAS raw materials (hyperoside, rutin and caffeic acid), impurities (not more than 2 %), brown stems not more than 5 %, weight loss during drying (not more than 10 %), total ash (not more than 7 %) and not less than 1 % of flavonoids, in terms of hyperoside","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75387534","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}

{"title":"Research on the use of motivational tools in the practical activity of pharmaceutical specialists","authors":"I. Horodetska, O. Levytska, Iryna Chukhray, Oleksandra Korniyenko, H. Bilushchak","doi":"10.15587/2519-4852.2022.259784","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.259784","url":null,"abstract":"The aim. Research on the peculiarities of the use of modern motivational tools by domestic employers in the pharmaceutical industry (including training and involvement of pharmaceutical specialists in social projects). \u0000Materials and methods. An anonymous online survey in the Google Form was conducted from April 3, 2021 to November 1, 2021 on the social network \"Facebook\" (including in four pharmaceutical groups of this network). Methods: analysis, synthesis, and generalization. \u0000Results of the research. The main motivating factors of respondents and the main motivational tools used by employers in the pharmaceutical industry have been identified. The state of training and education during professional activities and the evaluation of their effectiveness by respondents have been studied. Professional and motivational-psychological trainings are in the lead in the ranking of educational projects (75.2 % of respondents). The methods of evaluation of pharmaceutical specialists used by employers in the pharmaceutical industry have been generalized. The attitude of respondents to the participation of employers in the pharmaceutical industry in social and charitable projects has been studied. Most respondents (67.5 %) positively perceives the participation of employers in social and charitable projects, for some of them this is a motivational advantage when choosing a place of work. \u0000Conclusions. An online survey of 508 pharmaceutical professionals, conducted in a Google Form has allowed us to establish the features of current motivational approaches used today in pharmaceutical organizations and the attitude of respondents to them. It has been found that such motivational tools as trainings (innovative form of education) (55.1 %), as well as material forms of incentives (73.2 %) are widely used. At the same time, the main topics of the trainings are regarding the professional aspects of activity. An important factor in the life of a pharmaceutical organization is its social and charitable work, which forms a positive attitude towards it on the part of pharmaceutical professionals, and sometimes serves as a motivational advantage in choosing a place of work","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"2016 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86599427","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}

{"title":"Experimental research on the development of the composition of the transdermal therapeutic system of anti-inflammatory action based on composition of natural substances","authors":"L. Vyshnevska, Anastasia Olefir, D. Lytkin, L. Bodnar","doi":"10.15587/2519-4852.2022.259877","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.259877","url":null,"abstract":"The aim of the work is to develop the composition of the transdermal therapeutic system of anti-inflammatory action based on active pharmaceutical ingredients of natural origin.\u0000Materials and methods. Selection of adhesive materials, plasticizers and solvents, the effect of introduction to the base of active pharmaceutical ingredients, determination of optimal temperature and drying time, pharmacological screening was performed by physicochemical, biopharmaceutical and biological research methods.\u0000Results. The composition of the hydrophilic adhesive composition, which includes polyvinylpyrrolidone, eudragit (adhesives), PEO-400 (plasticizer), isopropyl alcohol (solvent) 50: 8: 12: 30, respectively. This composition has excellent organoleptic properties, is easily applied to the polymer base, holds its shape well (does not flow beyond the base), is applied in a thin layer and evenly distributed on the base. The optimal mode of drying of the adhesive composition based on PVP is 75 °C for 30 min, based on PVA – 75 °C for 35 min, the composition containing eudragit - 50 °C for 10 min. It is established that the addition of active substances to the adhesive composition does not adversely affect its properties.\u0000The study of antiexudative activity using different combinations of substances of natural origin as API and found that the best anti-inflammatory properties (25 %) have a sample No. 4, which includes dry extracts of white willow bark and sage leaves and quercetin 3:1:3 in accordance.\u0000Conclusions. Based on physicochemical, biopharmaceutical and pharmacological studies, the composition of the transdermal therapeutic system of anti-inflammatory action with active pharmaceutical ingredients of natural origin has been developed","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"24 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81579466","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}

{"title":"Comparative analysis of drug consumption for the treatment of epilepsy in Ukraine, Kazakhstan and Belarus","authors":"I. Korzh, Natalia Olieinikova, Marharyta Beketova, I. Kubarieva, Yevheniia Korobova, O. Sevriukov, O. Afanasenko","doi":"10.15587/2519-4852.2022.255840","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.255840","url":null,"abstract":"The aim to conduct a comparative analysis of the population's consumption of antiepileptic drugs in the retail pharmaceutical markets of developing countries, including Ukraine, Kazakhstan and Belarus in the period 2016-2020. \u0000Materials and methods. The objects of the research were the data of marketing agencies that monitor the domestic pharmaceutical market in the countries under study. In particular, the range of AED in Ukraine was determined using the market research system «Pharmstandard» of the company «Morion». Analytical-comparative, systematic, graphical, logical, mathematical-statistical research methods were used. \u0000Results. The results of the study show that the market of antiepileptic drugs in Ukraine, Kazakhstan and Belarus mainly depends on foreign manufacturers, in particular by 60 %, 92 % and 46 % respectively in 2020, and does not meet the needs of the population in accordance with WHO recommendations. It is established that in the market of Ukraine, Kazakhstan during 2016-2019 there is a general trend of increasing retail sales of antiepileptic drugs, which are not included in the WHO Basic List of Essential Medicines, both in natural and in monetary terms. The results of the analysis of retail sales of drugs in the Belarusian market in quantitative and monetary terms indicate an increase in sales of drugs for the treatment of epilepsy, which are included in the WHO Basic List of Essential Medicines. \u0000Conclusions. The presence in Ukraine of a difficult situation with the consumption of antiepileptic drugs in comparison with other countries of the reference group indicates the need to implement comprehensive programs to combat the spread of epilepsy and the introduction of models for the rational use of limited health resources","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"81 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79041470","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}

{"title":"Status and analysis of trends in the metformin -based drug development: formation of the logistic system of scientific research","authors":"E. Litvinova, O. Posilkina, S.Ju. Kovalenko, R. Yeromenko, Yu. A. Bratishko, Anastasiya Lisna","doi":"10.15587/2519-4852.2022.255536","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.255536","url":null,"abstract":"The aim of the work is analysis of the current state and trends in the metformin-based drug development with the subsequent formation of the logistics system of scientific research. \u0000Materials and methods. Studies were conducted using databases on the Internet (2015-2022): PubMed; U.S. Food and Drug Administration, European Medicines Agency, the State Expert Center of the Ministry of Health of Ukraine, scientific and metric databases - Scopus, Cochrane Database, US Patent Office. It has used retrospective, logical, graphic research methods, content analysis, modelling. \u0000Results. The model of the logistic system of metformin scientific research has developed. It represents the set of elements that are interconnected through information communication, its composition and features, which are associated with the pharmacological action of metformin, are determined. \u0000Logistic system of metformin scientific research allows: to demonstrate the uniqueness of the drug, to reveal its potential and new opportunities for medical use, prospects for the development of new types of dosage forms and new combined drugs; to identify the threat of patent infringement, to identify opportunities for establishing partnerships; to present scientific products in the form of a drug on the pharmaceutical market, optimizing the research time, reducing the development stages due to the available information and documentation, ensuring the synchronization of innovative information flows; to optimize the total costs of scientific research and receive at the expense of the specified profit. \u0000Logistic system of metformin scientific research is recommended for implementation in scientific organizations and pharmaceutical companies that perform R&D to achieve concentration of information search in solving logistics problems in the field of creating medicines based on metformin. \u0000Conclusions. Thus, the management of scientific research in pharmacy using the logistic approach ensures the time reduction of the medicine to entry into the market, reduces the cost of its creation, prevents duplication of research, and promotes optimization of solutions. The analysis revealed that the creation of medicines based on metformin should be aimed at the search and development of combined sugar-reducing drugs with mutually complementary mechanisms of action","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"203 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82900056","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}

{"title":"An overview on 1,2,4-triazole and 1,3,4-thiadiazole derivatives as potential anesthesic and anti-inflammatory agents","authors":"Andriy Koval, A. Lozynskyi, S. Shtrygol’, R. Lesyk","doi":"10.15587/2519-4852.2022.255276","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.255276","url":null,"abstract":"The aim. The purpose of this review is to summarize data on the synthesis and structural modification of heterocyclic systems with triazole and thiadiazole fragments in molecules as promising objects in bioorganic and medicinal chemistry. \u0000Materials and methods. The research based on bibliosemantic and analytical methods using bibliographic and abstract databases, as well as databases of chemical compounds. \u0000Results. Modern medicinal chemistry faces many challenges, one of which is the determination of the activity and specificity of therapeutic agents. Recent scientific data showed that triazoles and/or thiadiazoles have broad spectrum of biological activities, in particular antimicrobial, antifungal, antiviral, anticancer and anticonvulsant. Synthetic research allows to propose a whole number of new molecular design directions of biological active triazole and/or thiadiazole derivatives, as well as to obtain directed library that include hundreds of new compounds. This review is an effort to summarize data of its analgesic and anti-inflammatory activity over the last decade. We summarized and analyzed the series of triazole and/or thiadiazole derivatives and provided data of their structure-activity relationship. For optimization and rational design of highly active molecules with optimal «drug-like» characteristics and discovering of possible mechanism of action SAR, QSAR analysis and molecular docking were summarized. \u0000Conclusions. It has been shown that heterocyclic systems containing fragments of triazole and / or thiadiazole are a significant source of promising analgesic and/or anti-inflammatory agents. It has been established that the mentioned heterocyclic derivatives have a high selectivity of action, low toxicity and an effect commensurate with standard drugs","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83165906","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}

{"title":"Development of a unified approach to the method of identification, quantitative determination of active substances and accompanying impurities in a combined drug by HPLC method","authors":"O. Rudakova, S. Gubar, N. Smielova, M. Yaremenko, N. Bevz, V. Georgiyants","doi":"10.15587/2519-4852.2022.255851","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.255851","url":null,"abstract":"The aim of the work is to develop a method of identification, quantification of acetylsalicylic and ascorbic acids in the combined presence and concomitant impurities in the combined drug in the form of effervescent powder for preparation of oral solution by liquid chromatography and study of validation characteristics.\u0000Materials and methods. ProStar liquid chromatograph with “Varian” spectrophotometric detector. Chromatographic column with a size of 150×4.6 mm, filled with aminopropylsilyl silica gel for chromatography (Supelcosil LC-NH2, “Supelco”) with a precolumn (particle size 3 μm), mobile phase - buffer solution pH 3.2 - acetonitrile P (80:20), elution mode – isocratic; mobile phase velocity – 1.2 ml/min; the detection wavelength is 240 nm.\u0000Results. To determine acetylsalicylic and ascorbic acids by high-performance liquid chromatography with UV detection, the optimal chromatographic conditions were selected considering the influence of other active and excipients in the drug. To prove the possibility of applying the proposed technique in the subsequent analysis of the effervescent powder, its validation was performed. The obtained validation characteristics indicate that the method of quantitative determination of acetylsalicylic acid in the studied dosage form corresponds to the parameters: accuracy, precision, linearity ( =0.92≤max =1.60, d=0.19≤maxd=0.51, a=0.17 max a=2.60, r=0.9994 min r=0.9981). In the quantitative determination of ascorbic acid in the combined effervescent powder it is established that the correctness, precision, linearity are performed ( =0.86≤max =1.60, d=0.02≤max d=0.51, a=1.99 max a=2.60, r=0.9997 min r=0.9981).\u0000Conclusions. A new method for the identification, quantification of acetylsalicylic and ascorbic acids in the combined presence and concomitant impurities in the effervescent powder using high performance liquid chromatography has been developed. The validation of the proposed method is carried out and its acceptability for use in pharmaceutical analysis is proved","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"154 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72991842","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}

{"title":"Spectrophotometric methods for quantitative determination of sotalol in tablets","authors":"Olena Maletska, S. Vasyuk","doi":"10.15587/2519-4852.2022.255534","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.255534","url":null,"abstract":"The aim of the work. To develop a method for spectrophotometric determination of sotalol with diazonium salts. Establish optimal conditions for the quantitative determination of sotalol in drugs. Validate the developed methodology.\u0000Materials and methods. Reagents and solvents used in the study were: diazole red 2J (obtained from NVF “Sinbias”), tablets “Sotalol Sandoz” 40 mg (Salyutas Pharma GmbH, series JZ1188), “Sotalol Sandoz” 80 mg (Salyutas Pharma GmbH, series KA0464) and “Sotalol Sandoz” 160 mg (Salyutas Pharma GmbH, series JY3504), methanol (LAB-SCAN, Ireland, batch № 5120/13), sodium carbonate (Sinbias) and purified water were also used.\u0000Analytical equipment: spectrophotometer “SPECORD-200” (Analytic Jena AG, Germany), scales laboratory electronic RADWAG XA 210.4Y, bath ultrasonic Sonorex Digitec DT100H, laboratory glassware of class A.\u0000All studies were conducted in the experimental pharmaceutical research department of the scientific medical laboratory center (SMLC) of the Zaporizhzhia State Medical University.\u0000Results and discussion. The technique of spectrophotometric determination of the quantitative content of sotalol based on its reaction with red diazole in water-methanol medium has been developed. The stoichiometric ratios of the reactive components as 1:1 were obtained by the methods of continuous changes and the saturation method. Validation of the developed on such indicators as linearity, precision, correctness and robustness is carried out. Based on these data, the developed method is correct and could be used in the quality control departments of chemical and pharmaceutical companies.\u0000Conclusions. A method of quantitative spectrophotometric determination of sotalol in the tablet dosage form “Sotalol Sandoz” 40 mg, “Sotalol Sandoz” 80 mg and “Sotalol Sandoz” 160 mg of industrial production was developed, validation characteristics were investigated: linearity, precision, correctness, range of application and robustness","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"71 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74985026","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}

{"title":"Results of analysis of epidemological indicators of viral hepatitis c in regions of the world as part of activities to improve pharmaceutical provision for patients","authors":"A. Nozdrina, A. Volkova, Alina Cherkashyna, O. Ovakimian","doi":"10.15587/2519-4852.2022.255858","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.255858","url":null,"abstract":"Viral hepatitis affects hundreds of millions of people worldwide, the most dangerous of which are hepatitis B and C.\u0000The aim of our study was to study the prevalence and incidence of HC in the world and in Ukraine, as well as approaches in pharmacotherapy of HC to further identify effective measures to eliminate HC and improve pharmaceutical supply to patients in HC in Ukraine. The materials of the study were WHO statistical reports, national country reports, national recommendations for pharmacotherapy, the analysis of which was carried out by methods of generalization of information, analytical, comparative method.\u0000Results of the research. According to the WHO segmentation, the most frequent cases of HC are found in the populations of the Nordic-Mediterranean region (15 million cases) and the European region (12 million cases). Four countries in the world account for more than 40 % of all people infected with HC, two of which are in the Nordic-Mediterranean region (Pakistan – 7.2 and Egypt – 5.6 million people, respectively). The incidence of HC in Western Europe is up to 0.5 %, while in Northern Europe it is up to 3.3 %. Currently, the highest number of first-time HC infections in 2019 was registered among the populations of Ireland, the United Kingdom and Finland. The lowest incidence rates were found in Romania, Italy and Greece. It has been established that males aged 20–45 years prevail among those infected with HC.\u0000It was found that the prevalence of HC in Ukraine in 2015 was 3 %, according to 2020 – 5 %, with the annual number of newly recorded cases of HC increases by at least 7 %. According to the gender distribution, the ratio is on average 1.3 patients among men to 1 patient among women.\u0000An analysis of international guidelines for the pharmacotherapy of HC has shown that their latest revisions contain new direct-acting antiviral drugs, namely combinations of drugs such as glecaprevir / pibrentasvir and sofosbuvir / velpatasvir. The standard of HC treatment in Ukraine, approved in January 2021, is more in line with the recommendations of the WHO (2018), AASLD (2019) and EASL (2020) than the 2016 treatment protocol.\u0000Conclusions. The annual rate of HC infection in the world remains very high and is estimated at 1.5 million people. Regular revision and updating of standards of HC treatment with the latest direct-acting antiviral drugs, annual increase in the number of people in the world and in Ukraine who receive timely diagnosis of HCV and its full treatment are effective steps to achieve the goal of eliminating viral hepatitis","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80479681","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}

{"title":"The influence of non-steroidal anti-inflammatory drugs with different mechanisms of action on the course of stress reaction, the functional state of kidneys, liver, and heart on the model of acute general cooling","authors":"S. Shtrygol’, O. Koiro, O. Kudina, O. Tovchiga, T. Yudkevych, D. Oklei","doi":"10.15587/2519-4852.2022.255797","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.255797","url":null,"abstract":"Inhibitors of the arachidonic acid cascade have significant potential as the agents for the prevention of severe cold injuries. The results of the previous studies have demonstrated the pronounced frigoprotective properties of certain non-steroidal anti-inflammatory drugs, primarily diclofenac sodium, etoricoxib, darbufelone mesylate, under the conditions of acute general cooling. \u0000The aim of the study: to investigate the effect of non-steroidal anti-inflammatory drugs with various mechanisms of action on the course of the stress reaction, the functional state of the kidneys, liver, and heart using the model of acute general cooling. \u0000Materials and Methods: The experiment was carried out using 35 outbreed male rats weighing 256±5 g. The studied drugs were administered intragastrically 30 minutes before cold injury modelling: diclofenac sodium at a dose of 7 mg/kg, etoricoxib at a dose of 5 mg/kg, darbufelone mesylate at a dose of 20 mg/kg. Acute general cooling was induced by exposure at –18 °C for 2 hours. The efficacy of the studied drugs was evaluated by the values as follows: the body temperature (measured rectally), the course of a stress reaction according to the criteria of “the stress triad”, the functional state of the kidney and liver according to the changes in the blood serum biochemical parameters, the functional state of the heart according to the electrocardiogram. \u0000Results: It was found that etoricoxib and darbufelone mesylate, and especially diclofenac sodium, demonstrate frigoprotective properties, reducing the severity of hypothermia, have stress-protective activity and a beneficial effect on the functional state of the kidneys. All investigated non-steroidal anti-inflammatory drugs prevent a decrease in myocardial contractility (by the effect on the systolic index) and lengthening of the QT interval caused by acute cold injury. Diclofenac sodium, unlike etoricoxib and darbufelone mesylate, does not enhance the effect of acute general cooling on intraventricular conduction. Under acute exposure to cold, no significant changes in the functional state of the liver were observed, including the groups receiving the nonsteroidal anti-inflammatory medicines. \u0000Conclusions: The prophylactic administration of the arachidonic acid cascade inhibitors, especially the non-selective COX-2 inhibitor diclofenac sodium, reduces the severity of the stress response, contributes to the maintenance of the renal and cardiac function. There are no significant changes in the functional state of the liver under conditions of the experiment","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"12 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90378632","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}