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.
CITATION STYLE
Deng, J. H., Lu, T. B., Sun, C. C., & Chen, J. M. (2017). Dapagliflozin-citric acid cocrystal showing better solid state properties than dapagliflozin. European Journal of Pharmaceutical Sciences, 104, 255–261. https://doi.org/10.1016/j.ejps.2017.04.008
Mendeley helps you to discover research relevant for your work.