ScienceRise: Pharmaceutical Science最新文献

{"title":"Advanced research for physico-chemical properties and parameters of toxicity piperazinium 2-((5-(furan-2-YL)-4-phenyl-4H-1,2,4-triazol-3-YL)THIO)acetate","authors":"Y. Karpenko, Yu. R. Hunchak, B. Gutyj, Alla Hunchak, M. Parchenko, V. Parchenko","doi":"10.15587/2519-4852.2022.255848","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.255848","url":null,"abstract":"The achievements of modern domestic pharmacy clearly prove the prospects of searching for biologically active molecules among 1,2,4-triazole derivatives. \u0000The aim of our work was to predict the safest compound, select it and unambiguously prove the structure of a new promising molecule, to investigate some parameters of its toxicity. \u0000Materials and methods. X-ray diffraction analysis was performed in the laboratory of the Institute of Single Crystals of the National Academy of Sciences of Ukraine (Kharkiv). Computer methods were used to build “structure – toxicity” models and predict LD50 using already created models GUSAR, TEST. The degree of toxicity (DL50) and the approximate doses for the subacute experiment were determined by studying the acute toxicity of the test chemical and the injectable solution based on it. Determination of acute toxicity parameters by intragastric administration was performed on white rats, aged 3-4 months, body weight 200-220 g. \u0000Results. Due to the study of the toxicity of 1,2,4-triazole derivatives by non-experimental methods using GUSAR and TEST models, it was found that the test compounds could be classified as low-toxic substances. \u0000The compound is an organic salt that exists in the crystal as a solvate with one molecule of methanol and two molecules of water. When studying the structure of the crystal, it was found that the crystal is in the pinacoidal triclinic syngony. \u0000According to the results of the studies, it was found that after a single intragastric administration of the compound in doses of 1000, 3000 and 5000 mg / kg, all animals remained alive for 14 days. The basis of the biological action of chemical compounds is the violation of several biochemical processes. We found that the studied blood constants, on the background of the use of newly synthesized substance, underwent some changes. \u0000Conclusions. According to the assessment of the toxicity of the drug “VPK-434” when administered intragastrically to laboratory rats, it was found that in accordance with SOU 85.2-37-736: 2011 the test substance belongs to the IV class of toxicity (low toxicity). It was found that the average lethal dose of DL50 of the test substance by intramuscular administration to rats is 1666.66 mg / kg body weight. It was studied that some abnormalities in the hematopoietic system (increase in the number of leukocytes, including eosinophils), liver and kidney function (increased activity of transaminases, decreased serum concentrations of total protein, urea and creatinine) and changes in mineral metabolism of experimental animals groups, on the background of receiving 10 multiple doses of the study drug, was short-term, and the restoration of the functional state of the body of rats could be said as early as 4-5 days after discontinuation of the drug into their body","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":"87194488","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":"Substituted acyl thioureas and acyl thiosemicarbazides: synthesis and biological activity (minireview)","authors":"O. Kholodniak, S. Kovalenko","doi":"10.15587/2519-4852.2022.255738","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.255738","url":null,"abstract":"Acyl isothiocyanates and their functional derivatives (acyl thioureas and acyl thiosemicarbazides) are an important group of organic compounds that are widely used in the synthesis of heterocycles and in chemistry as catalysts, ligands, colorimetric hemosensors, etc. In recent years, there has been an increased interest towards this class of compounds as promising biologically active compounds, especially since the latest advances in medicinal chemistry for them are not sufficiently studied. \u0000The aim. To summarize and systematize information for the last 10 years on methods of synthesis and biological activity of substituted acyl thioureas and acyl thiosemicarbazides. \u0000Materials and methods. Web-tools for finding scientific information (Reaxys, Scopus, Google Scholar, ScienceResearch, SciFinder, Web of Science, etc.). \u0000Results and discussion. Literature sources related to the methods of synthesis of substituted acyl thioureas and acyl thiosemicarbazides were systematized and analyzed. The main approaches for the formation of these compounds are revealed: stepwise formation from carboxylic acids, through acyl chlorides and acyl isothiocyanates followed by nucleophilic addition of amines or hydrazides of carboxylic acids (\"one-pot synthesis\"), nucleophilic addition of amines or hydrazides of carboxylic acids directly to acyl isothiocyanates and parallel microwave synthesis using acyl isothiocyanates and amines as reagents. The possibility of their use as ligands for the formation of complex compounds with transition metal ions was discussed. In the review biological activity of these structures, namely antimicrobial, fungicidal, antitumor, antiviral, antifungal and other activities was detailazed. \u0000Conclusions. The basic approaches to the synthesis of substituted acylthuoureas and acyl thiosemicarbazides which include the application of carboxylic acids, their derivatives (acyl halides and isothiocyanates) and N-nucleophiles as initial compounds were discussed. It was shown that aforementioned class of the compounds reveals the versatile biological activity and are promising for further structural modification aimed to the search of novel drugs","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"2002 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88386594","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 results of a comparative analysis of the population of the population of Ukraine and countries of the European region for HIV as a rationale for improving the pharmaceutical provision of patients with socially dangerous pathologies","authors":"V. Yefremova, H. Panfilova, A. Lebedyn, G. Iurchenko, Okseniuk Oksana, Chernukha Vitaly, Tereshchenko Lyubov, Chebernina Inna","doi":"10.15587/2519-4852.2022.253507","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.253507","url":null,"abstract":"The aim: to conduct a comparative analysis of HIV morbidity in Ukraine and in some countries of the European region over the years and to determine the characteristics of the epidemiological situation on this pathology. \u0000Materials and methods. The object of the study was HIV incidence data presented on the website of the WHO European Health Portal (1990–2018) and in the Annual Report of the European Center for Disease Prevention and Control and the WHO Regional Office for Europe on HIV/AIDS Surveillance in Europe (2010–2019). Historical, analytical-comparative, systemic, graphic, logical, hypothetical-deductive, mathematical-statistical, epidemiological and other research methods were used. \u0000Results. It is established that during 1990-2018 in the group of reference countries only for Ukraine and Belarus there was a significant fluctuation in the incidence rates presented in absolute data. In all countries except Romania, the number of HIV-infected in 2019 was higher than in 1990 (Ukraine, Belarus, Poland) and in 1993 (Germany). Analysis of the dynamics of the absolute number of HIV-infected persons by indicative years (1993, 1999, 2004, 2010, 2016, 2019) allows us to assert the different nature of changes in epidemiological data by group of reference countries. Only in Poland we saw a gradual increase in data for 1993-2019. In all other countries, there was a complex nature of changes in morbidity. According to the analysis of HIV incidence, presented in relative terms, it was found that they ranged in the largest range in Belarus, namely from 11.3 (2010) to 26.1 (2017). Belarus typically had the highest mean chain growth/decline rates of HIV incidence (1.09). In turn, the lowest value of these coefficients was observed in the EU as a whole (0.97). Comparison of average values of HIV incidence per 100 thousand population suggests that in Ukraine this figure was 1.85 times higher than in Belarus, 11.36 times higher than in Poland, 8.65 times higher than in Romania, 10.27 times higher than in Germany and 5.88 times more than in the EU group. \u0000Conclusions. The presence of a complex and tense epidemiological situation with HIV infection in Ukraine in comparison with other countries of the reference group of countries suggests the need to implement comprehensive programs to counter the spread of this socially dangerous infection and introduce models for the rational use of limited health care resources and international funds","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"29 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77002456","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":"Setting the equation of regression to determine the technological factors influence on the content of flavonoids in the extract","authors":"O. Kutova, R. Sahaidak-Nikitiuk, I. Kovalevska, N. Demchenko","doi":"10.15587/2519-4852.2022.253547","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.253547","url":null,"abstract":"The aim of the article is to establish a regression equation that determines the influence of technological factors on the content of flavonoids in the extract for further use in optimizing the technology for obtaining an extract based on horse chestnut. The task of the research was to identify a mathematical model to describe the effect of technological parameters of extraction on the target quality indicators of a given dosage form, in particular, on the quantitative content of flavonoids. \u0000Materials and methods. The proposed approach is based on mathematical processing of experimental results obtained according to plan 23 using the computer program Mathcad 14 and MS Excel. To establish a mathematical description, an analysis of the separate influence of technological factors on the target indicator was carried out and the possibility of forming a geometric mean function was determined using the corresponding linear regression equations. \u0000Results. The general problem of identification was solved, when it was necessary to reveal both the mechanism of influence of technological factors on the value of the target indicator, and to give a quantitative assessment of the unknown parameters of the regression equation. Based on the results of experimental observations, an adequate mathematical model was established in the form of a linear multiple regression equation with the interaction of factors. \u0000Conclusions. The obtained mathematical description makes it possible to analyze the influence of technological factors on the quantitative content of the complex of flavonoids in the herbal extract in the range of the investigated factor space, and also to optimize the technological parameters of extraction","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"41 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82017816","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 analgesic and anti-inflammatory effect of lawsone isolated from Lawsonia inermis","authors":"A. Al-Snafi, T. Talab, Narjes Alfuraiji","doi":"10.15587/2519-4852.2022.253555","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.253555","url":null,"abstract":" This study aimed to assess the analgesic and anti-inflammatory effects of lawsone isolated from henna leaves (Lawsonia inermis).  \u0000Methods: A total of 120 healthy adult mice (weighing about 25±5 g) were included in this study. Sixty mice out of the total were used to determine LD50, 30 mice to determine the anti-inflammatory test, and the remaining (30 mice) were used for an analgesic test. The hot plate was used to determine the analgesic effect, while the anti-inflammatory effect was determined by the ability of the compound to minimize the inflammation and edema caused by the injection of carrageenan.  \u0000Results: Lawsone was isolated from Lawsonia inermis. A Stuart SMP10 digital melting point apparatus was used for measuring all melting points. Infrared spectrometer FT-IR 400D was used for measuring/recording IR spectra (KBr) which the frequency of absorption was represented as cm−1. For 1H-NMR spectrum recording, a Bruk-spectrophotometer of 400 MHz was used with internal TMS standard, with deuterated Ś 2.51 ppm for acetone-d6, remained solvent signals as well as 13C.NMR was used. TLC was utilized as adsorbent, UV light, or iodine-completed visualization to verify compounds' purities. \u0000The LD50 of the oral lawsone was 96 mg/kg, and the highest dosage that did not kill any of the experimental animals was 80 mg/kg, which was used to investigate lawsone's analgesic and anti-inflammatory effects. \u0000Lawsone and aspirin possessed an analgesic effect compared to the control group (p<0.0001 and p<0.001, respectively); however, lawsone induced a potent analgesic effect compared to aspirin (p<0.1). In contrast, Lawsone and aspirin exerted an anti-inflammatory effect (p<0.05) compared to the control group and were equipotent in carrageenan-induced hind paw edema. \u0000Conclusion: It is concluded that lawsone possesses analgesic and anti-inflammatory effects, which endorse the practical medical importance of Lawsonia inermis. The latter is widely used traditionally for these purposes own to its cost-effectiveness and safety; however, further studies are required to determine the systemic safety of lawsone","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"68 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78642909","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":"Antioxidant and anti-cytolytic activity of parsnip (Pastinaca sativa L.) herb thick extract in conditions of catecholamine myocardiodystrophy in rats","authors":"N. Symonenko, O. Shpychak, O. Mishchenko, V. Kyslychenko, Tamara Shpychak, S. Grashchenkova","doi":"10.15587/2519-4852.2022.253546","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.253546","url":null,"abstract":"The aim: to study the antioxidant and anticytolytic activity of the parsnip herb thick extract (PHTE) in conditions of catecholamine myocardial dystrophy in rats. \u0000Materials and methods. Catecholamine myocardial dystrophy was reproduced in rats by a single subcutaneous injection of 0.18 % adrenaline hydrochloride solution at a dose of 0.5 mg/kg (0.28 ml/kg) of body weight. The experiment used 36 white male rats with an initial weight of 220–250 g, 4–4.5 months of age. The tested drugs were PHTE at doses of 100 and 200 mg/kg and the reference drug (RD) “Tricardin” were administered intragastrically in a therapeutic and prophylactic regimen for 7 days, the last time on the day of the experiment 1 hour before the administration of cardiotoxin. The activity of the studied agents was assessed by the survival rate of the animals, the functional state of the myocardium (ECG studies), by the effect on the heart mass ratio (HMR), the activity of aspartate aminotransferase (ASAT), the level of active products interacting with thiobarbituric acid (TBA-AP) and the content of reduced glutathione (RG) in the heart homogenate. \u0000Results. The study of the effect of PHTE on the lipid peroxidation / antioxidant protection (LPO / AOP) system showed that a pronounced antioxidant effect of the tool was found at a dose of 200 mg/kg: there was an increase in VG at the trend level (0.05<p<0.10) and a significant decrease (p<0.05) the content of TBK-AP in 1.85 times compared with the group of positive control (PC). A similar effect was found in the comparison drug “Tricardin”. PHTE at a dose of 100 mg/kg was less influential. The use of PHTE in both doses and the comparison drug “Tricardin” reduced the severity of cytolytic processes: the activity of the enzyme AST – a marker of cardiocytolysis, was lower than in the PC group. PHTE at doses of 100 and 200 mg/kg contributed to a certain normalization of some ECG parameters compared to PC: a slight insignificant decrease in heart rate and a significant decrease (p<0.05), QT interval, systolic index (SI) and decreased ischemia marker – ST segment displacement. The comparison drug \"Tricardin\" showed a similar effect to PHTE on the functional state of the myocardium in adrenaline intoxication. \u0000Conclusions. Parsnip herb thick extract exhibits antioxidant and anticytolytic activity, improves the functional state of the myocardium, prevents a decrease in the severity of alterative processes in the organ under conditions of adrenaline myocardial dystrophy","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"15 Suppl 4 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84845597","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 effect of a modified fragment of neuropeptide y on spatial memory and learning in the Morris water maze","authors":"Ihnat Havrylov, Sergey Shtrygol’, D. Kavraiskyi","doi":"10.15587/2519-4852.2022.253372","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.253372","url":null,"abstract":"Neuropeptide Y (NPY) is a biologically active neuropeptide that is responsible for a large list of physiological processes. We propose a short modified fragment of NPY that should at least partially have a spectrum of biological activity of the original peptide. The compound was named nonapeptide NP9. \u0000The aim of our study was to investigate the ability of the modified fragment of NPY to influence spatial memory and learning. \u0000Materials and methods: the study was performed on 24 one-year-old random-bred female rats weight 220–250 g. The animals were divided into 3 groups of 8 rats each: treated with a solvent (0.9 % NaCl), a solution of peptide NP9 0.02 mg/kg and the drug “Semax” 0.1 mg/kg. All drugs were administered intranasally. The study of the effect of the peptide NP9 on spatial memory and learning ability was performed in the psychopharmacological test the Morris water maze. Navigation parameters were analyzed using Noldus EthoVision XT 14 video tracking software. The escape latency, the distance moved, the average velocity and the meander were recorded. An inter-quadrant analysis of rat behavior was also performed, for which the frequency of appearance and time spent in certain quadrants were recorded. \u0000Results: nonapeptide NP9 in the Morris water maze test demonstrated the ability to accelerate the time to find a hidden platform, reduce the distance traveled, meander, and optimize the search strategy. \u0000Conclusions: NP9 peptide has demonstrated the ability to positively influence learning and spatial memory. The improvement in cognitive performance of animals administered with the peptide NP9 was no less than that of the reference nootropic drug Semax. These results substantiate the feasibility of further research with the aim of pharmaceutical development of a new nootropic drug","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90200264","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":"Comprehensive study for the development of rectal suppositories with diosmin and hesperidin","authors":"Yelyzaveta Borko, Kovalevska Inna, V. Grudko, N. Kononenko, M. Velya","doi":"10.15587/2519-4852.2022.253518","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.253518","url":null,"abstract":"The aim. To conduct a comprehensive study of biphasic-type suppositories that contain diosmin and hesperidin. \u0000Materials and methods. Samples of biphasic-type suppositories with a mass of 4.0 were objects of the study. Pharmacological, technological and analytical research methods were used to directly or indirectly analyze the strength and completeness of the drug activity. Thus, in this work we combined the study of the specificity of the pharmacological action of the drug, experimental verification of the quantitative content of API, analysis of the structural properties of suppositories and study of the profile of the release of active pharmaceutical ingredients. \u0000Results. Therefore, based on the obtained data, the most effective dose was 75 mg / kg (in terms of a human dose of 300 mg per suppository). The drug in the selected dose showed a significant therapeutic effect, which significantly exceeded that of the test sample at a lower dose and the reference agent. According to the results of technological studies, it was determined that all samples of suppositories had satisfactory structural and mechanical properties. Studies of the histological structure of the mucous membrane of rats proved that there is a positive effect of treatment with suppositories with diosmin and hesperidin due to the improvement of the normal condition of the mucous membrane, the absence of edema and ulcerative defect. Research of the release profile of active pharmaceutical ingredients showed that the best percentage of release is characteristic of sample 2 (99.8 %) \u0000Conclusions. Therefore, suppositories with diosmin and hesperidin in therapeutically dose of 75 mg/kg of animal weight can be used for further research and will be of interest in the treatment of hemorrhoids of both acute and chronic forms","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"29 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83846494","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":"Carboxylic acids in the flowers of Veronica spicata L. and Veronica incana L.","authors":"А. Kovaleva, R. Ain, Ilina Tetiana, A. Osmachko, O. Goryacha, Ludmila Omelyanchik, O. Koshovyi","doi":"10.15587/2519-4852.2022.253541","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.253541","url":null,"abstract":"In the Ukrainian flora, species of Veronica L. genus (Plantaginaceae Juss.) are classified into 8 sections. Among the representatives of Pseudolysimachion W. D. J. Koch section in the Kharkiv region, Veronica spicata L. (spike speedwell) and Veronica incana L. (Veronica spicata L. subsp. incana (L.) Walters, silver speedwell) are common. Plants are used for the treatment of upper respiratory tract diseases, malignant neoplasms, gastrointestinal tract and genitourinary system disorders, diabetes mellitus. \u0000The aim of the research was to study the carboxylic acids of flowers of Veronica spicata L. and Veronica incana L. \u0000Materials and methods. The objects of the research were flowers of Veronica spicata L. and Veronica incana L., collected in the flowering stage in the Botanical Garden of Karazin University (Kharkiv, Ukraine) in summer 2018. The study of carboxylic acid composition was performed by chromatography-mass spectrometry on a 6890N MSD/DS Agilent Technologies chromatograph with a 5973N mass spectrometric detector. Identification of methyl esters of acids was performed using data from the mass spectrum libraries NIST 05 and Willey 2007 in a combination with programs for the identification of AMDIS and NIST; also, their retention time and the retention times of standard compounds were compared. \u0000Results. In Veronica incana L. flowers, 37 carboxylic acids were identified and quantified, constituting 1.05 %. In Veronica spicata L. flowers, 32 carboxylic acids were identified and quantified, the total content of which was 2.75 %. \u0000Conclusions. A higher carboxylic acid content was established in the flowers of Veronica spicata L. The fatty acid composition of Veronica incana L. flowers is characterized by a comparable content of saturated and unsaturated acids, while in Veronica spicata L. flowers, unsaturated fatty acids prevail over saturated fatty acids. The content of aromatic acids in the flowers of studied species was comparable. The characteristic carboxylic acids in the flowers of Veronica incana L. are oxalic, 3-hydroxy-2-methylglutaric, pentadecanoic, heneicosanoic, tricosanic,4-hydroxybenzoic, 4-methoxybenzoic and 3,4-dimethoxybenzoic acids; in the flowers of Veronica spicata L. – 2-hydroxy-3-methylglutaric, α-furanic and homovanillic acids","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"71 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75321157","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":"Pharmacological and biopharmaceutical studies of paracetamol and N-acetyl-D-glucosamine combination as an analgetic drug","authors":"O. Ruban, I. Zupanets, T. Kolisnyk, S. Shebeko, O. Vashchenko, S. Zimin, O. Dolzhykova","doi":"10.15587/2519-4852.2022.253474","DOIUrl":"https://doi.org/10.15587/2519-4852.2022.253474","url":null,"abstract":"The aim. Experimental selection of paracetamol and N-acetyl-D-glucosamine (NAG) ratio and combined dose and bioavailability study of the pharmaceutical composition and active pharmaceutical ingredient (API) in the model of cell biomembranes. \u0000Materials and methods. The following substances were used: paracetamol, Actimask Acetaminophen (gelatin-coated paracetamol), and NAG. For pharmacological studies were used laboratory rats, which received test objects intragastrically. The study was performed on the model of inflammatory hyperalgesia according to the Randall-Selitto method. The values of pain threshold before and after pathology induction were established. For biopharmaceutical studies, dry L-α-dimyristoylphosphatidylcholine purchased from Avanti Polar Lipids (purity 99.9 %) was used, hydrated with an appropriate amount of double-distilled water to obtain 70 % wt./wt. water dispersion. Differential scanning calorimetry (DSC) studies were performed employing DSC 1 microcalorimeter (Mettler Toledo). Pharmaceuticals investigated were placed on the bottom of a crucible, then a proper amount of the lipid membrane was added and this moment was taken as the time reference point (t=0). Then a crucible was sealed with a lid and a sample was undergone consecutive temperature scans, heating from 0 to 35 ºC at a scanning rate of 2 ºC/min. The procedure was repeated until no more changes in DSC profiles were observed, i.e. system equilibrium was reached. \u0000Results. It has been experimentally proven that the combination of paracetamol and NAG in the ratio of 4:1 showed better analgesic efficacy. The dose of active ingredients was determined to be 50 mg/kg by the sum of API. The active interaction of paracetamol with the bilayer of biomembranes was established and it was determined that Actimask has a worse rate of penetration into the membrane due to the coating of paracetamol with a gelatin shell. NAG didn't significantly affect the rate of penetration of Actimask through the bilayer of membranes, but the auxiliary components of the tablet mixture significantly improved the rate and completeness of penetration of paracetamol through the bilayer of biomembranes. \u0000Conclusions. The study found the most effective ratio between paracetamol and NAG in the composition, which is 4:1. The next step was to determine the dose of API, which is 50 mg/kg of the sum of active substances. It has been determined that paracetamol has good permeability through the bilayer of biomembranes, and the tablet mass significantly improves the permeability of paracetamol","PeriodicalId":21674,"journal":{"name":"ScienceRise: Pharmaceutical Science","volume":"117 1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91024972","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}