E. S. Berezina, E. A. Nepogodina, F. V. Sobin, N. A. Pulina, N. V. Dozmorova
{"title":"开发鉴定具有抗凝血活性的 BAS 的方法","authors":"E. S. Berezina, E. A. Nepogodina, F. V. Sobin, N. A. Pulina, N. V. Dozmorova","doi":"10.33380/2305-2066-2023-12-4(1)-1634","DOIUrl":null,"url":null,"abstract":"Introduction. Vascular pathologies associated with thromboembolism are common complications and the leading cause of morbidity and mortality among patients of various nosological groups. Previously, we obtained water-soluble 2-hydroxy-4-oxo-4-R-2-butenoates of hetarylammonium, which exhibit a significant pharmacological effect on the blood coagulation system». A compound with a pronounced anticoagulant effect was found in various routes of administration. It was of interest to study various methods of confirming the authenticity of a potential anticoagulant.Aim. Development of methods for identification of a potential anticoagulant 2-hydroxy-4-oxo-(4-chlorophenyl)-2-butenoate of thiazolinammonium.Materials and methods. The studies were carried out on three series of the substance 2-hydroxy-4-oxo-(4-chlorophenyl)-2-butenoate of thiazolinammonium obtained in laboratory conditions. The melting point of BAS was measured by the capillary method according to GF XV OFS.1.2.1.0011 \"Melting point\". The solubility of the substance was determined in accordance with GF XV of the OFS.1.2.1.0005 \"Solubility\". The absorption spectra in the IR region were taken in accordance with GF XV of the OFS.1.2.1.1.0002 \"Spectrophotometry in the middle infrared region\". Absorption spectra in the UV region were taken in accordance with GF XV of the OFS.1.2.1.1.0003 \"Spectrophotometry in the ultraviolet and visible regions\". In carrying out qualitative reactions, reagents prepared in accordance with GF XV of the OFS were used.1.3.0001 \"Reagents. Indicators\".Results and discussion. A description of the substance has been carried out. The melting point and solubility of the compound were determined. Spectra in the IR and UV regions of the spectrum were taken. Methods were selected, and qualitative reactions of authenticity of a potential anticoagulant were carried out.Conclusion. The studied characteristics of the new BAS can be used in the standardization of the substance according to the indicators \"Description\", \"Solubility\", \"Identification\", \"Melting point\". These indicators characterize the physico-chemical properties of 2-hydroxy-4-oxo-(4-chlorophenyl)-2-butenoate of thiazolinammonium, and will be included in the draft regulatory documentation for the substance in the future.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"9 24","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2023-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Development of Methods for Identifying BAS Exhibiting Anticoagulant Activity\",\"authors\":\"E. S. Berezina, E. A. Nepogodina, F. V. Sobin, N. A. Pulina, N. V. Dozmorova\",\"doi\":\"10.33380/2305-2066-2023-12-4(1)-1634\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Introduction. Vascular pathologies associated with thromboembolism are common complications and the leading cause of morbidity and mortality among patients of various nosological groups. Previously, we obtained water-soluble 2-hydroxy-4-oxo-4-R-2-butenoates of hetarylammonium, which exhibit a significant pharmacological effect on the blood coagulation system». A compound with a pronounced anticoagulant effect was found in various routes of administration. It was of interest to study various methods of confirming the authenticity of a potential anticoagulant.Aim. Development of methods for identification of a potential anticoagulant 2-hydroxy-4-oxo-(4-chlorophenyl)-2-butenoate of thiazolinammonium.Materials and methods. The studies were carried out on three series of the substance 2-hydroxy-4-oxo-(4-chlorophenyl)-2-butenoate of thiazolinammonium obtained in laboratory conditions. The melting point of BAS was measured by the capillary method according to GF XV OFS.1.2.1.0011 \\\"Melting point\\\". The solubility of the substance was determined in accordance with GF XV of the OFS.1.2.1.0005 \\\"Solubility\\\". The absorption spectra in the IR region were taken in accordance with GF XV of the OFS.1.2.1.1.0002 \\\"Spectrophotometry in the middle infrared region\\\". Absorption spectra in the UV region were taken in accordance with GF XV of the OFS.1.2.1.1.0003 \\\"Spectrophotometry in the ultraviolet and visible regions\\\". In carrying out qualitative reactions, reagents prepared in accordance with GF XV of the OFS were used.1.3.0001 \\\"Reagents. Indicators\\\".Results and discussion. A description of the substance has been carried out. The melting point and solubility of the compound were determined. Spectra in the IR and UV regions of the spectrum were taken. Methods were selected, and qualitative reactions of authenticity of a potential anticoagulant were carried out.Conclusion. The studied characteristics of the new BAS can be used in the standardization of the substance according to the indicators \\\"Description\\\", \\\"Solubility\\\", \\\"Identification\\\", \\\"Melting point\\\". 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引用次数: 0
摘要
导言。与血栓栓塞有关的血管病变是常见的并发症,也是各病种患者发病和死亡的主要原因。此前,我们获得了水溶性 2-hydroxy-4-oxo-4-R-2-butenoates of hetarylammonium,它对血液凝固系统有显著的药理作用"。在各种给药途径中发现了一种具有明显抗凝作用的化合物。研究确认潜在抗凝剂真伪的各种方法很有意义。开发潜在抗凝剂 2-羟基-4-氧代-(4-氯苯基)-2-丁烯酸噻唑啉铵盐的鉴定方法。研究对象是在实验室条件下获得的三个系列的 2-羟基-4-氧代-(4-氯苯基)-2-丁烯酸噻唑啉铵盐。根据 GF XV OFS.1.2.1.0011 "熔点",用毛细管法测量了 BAS 的熔点。该物质的溶解度根据 OFS.1.2.1.0005 的 GF XV "溶解度 "测定。红外区域的吸收光谱根据 OFS.1.2.1.1.0002 的 GF XV "中红外区域分光光度法 "测定。紫外区的吸收光谱根据 OFS.1.2.1.1.0003 的 GF XV "紫外和可见光区的分光光度法 "拍摄。1.3.0001 "试剂、指标"。指标"。对物质进行了描述。确定了化合物的熔点和溶解度。拍摄了红外和紫外光谱。选择了方法,并对潜在抗凝剂的真实性进行了定性分析。根据 "描述"、"溶解度"、"鉴定 "和 "熔点 "等指标,所研究的新 BAS 特性可用于物质的标准化。这些指标描述了噻唑啉铵的 2-羟基-4-氧代-(4-氯苯基)-2-丁烯酸酯的物理化学特性,今后将纳入该物质的监管文件草案。
Development of Methods for Identifying BAS Exhibiting Anticoagulant Activity
Introduction. Vascular pathologies associated with thromboembolism are common complications and the leading cause of morbidity and mortality among patients of various nosological groups. Previously, we obtained water-soluble 2-hydroxy-4-oxo-4-R-2-butenoates of hetarylammonium, which exhibit a significant pharmacological effect on the blood coagulation system». A compound with a pronounced anticoagulant effect was found in various routes of administration. It was of interest to study various methods of confirming the authenticity of a potential anticoagulant.Aim. Development of methods for identification of a potential anticoagulant 2-hydroxy-4-oxo-(4-chlorophenyl)-2-butenoate of thiazolinammonium.Materials and methods. The studies were carried out on three series of the substance 2-hydroxy-4-oxo-(4-chlorophenyl)-2-butenoate of thiazolinammonium obtained in laboratory conditions. The melting point of BAS was measured by the capillary method according to GF XV OFS.1.2.1.0011 "Melting point". The solubility of the substance was determined in accordance with GF XV of the OFS.1.2.1.0005 "Solubility". The absorption spectra in the IR region were taken in accordance with GF XV of the OFS.1.2.1.1.0002 "Spectrophotometry in the middle infrared region". Absorption spectra in the UV region were taken in accordance with GF XV of the OFS.1.2.1.1.0003 "Spectrophotometry in the ultraviolet and visible regions". In carrying out qualitative reactions, reagents prepared in accordance with GF XV of the OFS were used.1.3.0001 "Reagents. Indicators".Results and discussion. A description of the substance has been carried out. The melting point and solubility of the compound were determined. Spectra in the IR and UV regions of the spectrum were taken. Methods were selected, and qualitative reactions of authenticity of a potential anticoagulant were carried out.Conclusion. The studied characteristics of the new BAS can be used in the standardization of the substance according to the indicators "Description", "Solubility", "Identification", "Melting point". These indicators characterize the physico-chemical properties of 2-hydroxy-4-oxo-(4-chlorophenyl)-2-butenoate of thiazolinammonium, and will be included in the draft regulatory documentation for the substance in the future.