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Cocrystal of Dapagliflozin with Citric Acid: Enhanced Hygros...

Cocrystal of Dapagliflozin with Citric Acid: Enhanced Hygroscopic and Thermal Stability

作     者:Jun-Hui Deng Jia-Mei Chen Tong-Bu Lu 

作者单位:School of Pharmaceutical SciencesSun Yat-Sen University MOE Key Laboratory of Bioinorganic and Synthetic ChemistrySchool of Chemistry and Chemical EngineeringSun Yat-Sen University 

会议名称:《中国晶体学会第六届学术年会暨会员代表大会——第六届全国晶型药物研发技术学术研讨会》

会议日期:2016年

学科分类:100702[医学-药剂学] 1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学] 

摘      要:Dapagliflozin(DAP) is a potent and selective sodium-glucose contransporter-2(SGLT-2) inhibitor, and performed as an efficacious treatment for type 2 diabetes. Sever hygroscopicity of DAP hinder the usage of its free form during process of pharmaceutical production. A solvate form(dapagliflozin propanediol, DAP-PDO-HO) is used in the market, which, however, also faces problem of thermal instability as higher vapor pressure of solvent molecules in crystal lattice. The present study obtained a new cocrystal of DAP with citric acid(DAP-CA). DAP-CA cocrystal was identified and characterized by H nuclear magnetic resonance(H-NMR), Fourier transform infra-red spectroscopy(FTIR), powder X-ray diffraction(PXRD) and thermal analysis, It was also evaluated by dynamic vapor sorption(DVS) and accelerated stability test under 40 ℃/75% RH, as well as powder dissolution test. DAP-CA cocrystal showed enhanced stability against both humidity and high temperature compared to the market form without compromising the dissolution solubility.

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