Dapagliflozin-citric acid cocrystal showing better solid state properties than dapagliflozin

Publication date: Available online 13 April 2017
Source:European Journal of Pharmaceutical Sciences
Author(s): Jun-Hui Deng, Tong-Bu Lu, Changquan Calvin Sun, Jia-Mei Chen
Dapagliflozin (DAP) is a potent and selective sodium-glucose contransporter-2 inhibitor, for treating type 2 diabetes. DAP propanediol monohydrate (DAP-PDO-H2O, 1:1:1) is the solid form used in the current tablet product to address the severe hygroscopicity problem of DAP free form. DAP-PDO-H2O, however, suffers the problem of instability when exposed to high temperature, which renders it amorphous. In this work, we report on the preparation and evaluation of a new 1:1 cocrystal between DAP and citric acid (DAP-CA). The DAP-CA cocrystal exhibits superior stability against high temperature and high relative humidity without compromising dissolution and tableting performance. Thus, DAP-CA is a promising solid form for developing the next generation DAP tablet products with improved performance.

Graphical abstract

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