{"title":"吡格列酮与柠檬酸共晶的开发及其对结晶特性和溶解的影响","authors":"Mouli Das, Shibashis Panigrahy, Rasmita Dash, Rudra Narayan Sahoo, Rakesh Swain, Souvik Nandi, Sk Habibullah, Tanisha Das, Subrata Mallick","doi":"10.17344/acsi.2024.8793","DOIUrl":null,"url":null,"abstract":"<p><p>Eutectics of pioglitazone were developed using citric acid (CA) as the co-former, and the effect on crystallite properties and dissolution has correspondingly been studied. Pioglitazone-citric acid eutectics (PC1, PC2, PC3, and PC4) in different molar ratios (3:1, 3:2, 1:1, and 3:4 respectively) were prepared by simple solvent evaporation method. Difference in dislocation density and strain value of the eutectics were observed, and the maximum strain value of PC1 might be due to the highest deformation activity compared to PC2, PC3, and PC4. Carbonyl-thiazolidine or carboxyl-pyridine weak bond formation might be the reason of producing eutectics of PGZ-CA rather than cocrystal with a docking score of - 2.2 Kcal/M. Likewise, lowest particle size was found with PC1 rather than that of pure PGZ and other eutectics. PC1 demonstrated highest dissolution of drug (68 %) rather than other eutectics (54 to 61 %) and PGZ (44 %) after 360 min.</p>","PeriodicalId":7122,"journal":{"name":"Acta Chimica Slovenica","volume":"71 3","pages":"482-491"},"PeriodicalIF":1.2000,"publicationDate":"2024-08-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Development of eutectics of pioglitazone with citric acid and its effect on crystallite properties and dissolution.\",\"authors\":\"Mouli Das, Shibashis Panigrahy, Rasmita Dash, Rudra Narayan Sahoo, Rakesh Swain, Souvik Nandi, Sk Habibullah, Tanisha Das, Subrata Mallick\",\"doi\":\"10.17344/acsi.2024.8793\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Eutectics of pioglitazone were developed using citric acid (CA) as the co-former, and the effect on crystallite properties and dissolution has correspondingly been studied. Pioglitazone-citric acid eutectics (PC1, PC2, PC3, and PC4) in different molar ratios (3:1, 3:2, 1:1, and 3:4 respectively) were prepared by simple solvent evaporation method. Difference in dislocation density and strain value of the eutectics were observed, and the maximum strain value of PC1 might be due to the highest deformation activity compared to PC2, PC3, and PC4. Carbonyl-thiazolidine or carboxyl-pyridine weak bond formation might be the reason of producing eutectics of PGZ-CA rather than cocrystal with a docking score of - 2.2 Kcal/M. Likewise, lowest particle size was found with PC1 rather than that of pure PGZ and other eutectics. PC1 demonstrated highest dissolution of drug (68 %) rather than other eutectics (54 to 61 %) and PGZ (44 %) after 360 min.</p>\",\"PeriodicalId\":7122,\"journal\":{\"name\":\"Acta Chimica Slovenica\",\"volume\":\"71 3\",\"pages\":\"482-491\"},\"PeriodicalIF\":1.2000,\"publicationDate\":\"2024-08-27\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Acta Chimica Slovenica\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.17344/acsi.2024.8793\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Acta Chimica Slovenica","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.17344/acsi.2024.8793","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Development of eutectics of pioglitazone with citric acid and its effect on crystallite properties and dissolution.
Eutectics of pioglitazone were developed using citric acid (CA) as the co-former, and the effect on crystallite properties and dissolution has correspondingly been studied. Pioglitazone-citric acid eutectics (PC1, PC2, PC3, and PC4) in different molar ratios (3:1, 3:2, 1:1, and 3:4 respectively) were prepared by simple solvent evaporation method. Difference in dislocation density and strain value of the eutectics were observed, and the maximum strain value of PC1 might be due to the highest deformation activity compared to PC2, PC3, and PC4. Carbonyl-thiazolidine or carboxyl-pyridine weak bond formation might be the reason of producing eutectics of PGZ-CA rather than cocrystal with a docking score of - 2.2 Kcal/M. Likewise, lowest particle size was found with PC1 rather than that of pure PGZ and other eutectics. PC1 demonstrated highest dissolution of drug (68 %) rather than other eutectics (54 to 61 %) and PGZ (44 %) after 360 min.
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