开发共结晶技术以提高抗糖尿病药物的溶解度

Ninad S. Burkhande, V. P. Wankhade, S. Atram, N. Bobade, S. D. Pande
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引用次数: 0

摘要

共晶体化是一种有用的晶体工程方法,可用于改变药物晶体的理化和结构特征。药物共晶体是一种非离子超分子复合物,可用于药物开发,在不改变原料药化学组成的情况下改变药物的理化性质,包括溶解性、稳定性和生物利用度。 半水合卡格列净(Canagliflozin Hemihydrate)是一种抗糖尿病药物。在 BCS 分类中,Canagliflozin 属于第四类药物,即低溶解度和低渗透性。该类药物的主要问题是在生物液体中溶解缓慢,导致口服后生物利用度较低。本研究的目的是利用共晶体技术制备卡格列净的药用共晶体,以提高其溶解度和溶出率。本研究中使用的共晶体是硫脲。通过傅立叶变换红外光谱(FTIR)、XRPD、扫描电子显微镜(SEM)对优化后的共晶体进行了表征,并对其溶解度和熔点等其他药物特性进行了评估。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development of Co-Crystallization Technique to Improve Solubility of Anti-Diabetic Drug
Co-crystallization is a useful crystal engineering approach for changing the physiochemical and structural characteristics of drug crystals. Pharmaceutical co-crystals are nonionic supramolecular complexes that can be utilized in pharmaceutical development to change physiochemical qualities including solubility, stability, and bioavailability without changing the chemical makeup of API.  Canagliflozin Hemihydrate is a anti-diabetic drug. Canagliflozin belongs to class IV drug in BCS classification. i.e. low solubility and low permeability. The major problem of this class drug is it slow solubility in biological fluids,which results into poor bioavailability after oral administration. The purpose of this study was to prepare pharmaceutical co-crystals ofCanagliflozin to enhance solubility and dissolution rate by using co-crystallization technique. The co-former used inthis study is Thiourea. The Optimized co-crystal was characterized by FTIR, XRPD, SEM and other pharmaceutical properties like solubility and melting point were alsoevaluated.
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