Development of eutectics of pioglitazone with citric acid and its effect on crystallite properties and dissolution.

IF 1.2 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY
Mouli Das, Shibashis Panigrahy, Rasmita Dash, Rudra Narayan Sahoo, Rakesh Swain, Souvik Nandi, Sk Habibullah, Tanisha Das, Subrata Mallick
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引用次数: 0

Abstract

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.

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
以柠檬酸(CA)为共聚物,开发了吡格列酮的共晶体,并研究了其对结晶特性和溶解性的影响。通过简单的溶剂蒸发法制备了不同摩尔比(分别为 3:1、3:2、1:1 和 3:4)的吡格列酮-柠檬酸共晶体(PC1、PC2、PC3 和 PC4)。与 PC2、PC3 和 PC4 相比,PC1 的最大应变值可能是由于其具有最高的变形活性。羰基-噻唑烷或羧基-吡啶弱键的形成可能是产生 PGZ-CA 共晶而不是对接得分为 - 2.2 Kcal/M 的共晶的原因。同样,与纯 PGZ 和其他共晶相比,PC1 的粒径最小。360 分钟后,PC1 的药物溶解度(68%)比其他共晶(54%-61%)和 PGZ(44%)高。
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来源期刊
Acta Chimica Slovenica
Acta Chimica Slovenica 化学-化学综合
CiteScore
2.50
自引率
25.00%
发文量
80
审稿时长
1.0 months
期刊介绍: Is an international, peer-reviewed and Open Access journal. It provides a forum for the publication of original scientific research in all fields of chemistry and closely related areas. Reviews, feature, scientific and technical articles, and short communications are welcome.
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