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

Jun Hui Deng, Tong Bu Lu, Changquan Calvin Sun, Jia Mei Chen

Research output: Contribution to journalArticlepeer-review

28 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)255-261
Number of pages7
JournalEuropean Journal of Pharmaceutical Sciences
Volume104
DOIs
StatePublished - Jun 15 2017

Keywords

  • Acetonitrile (PubChem CID: 6342)
  • Citric acid (PubChem CID: 311)
  • Dapagliflozin (PubChem CID: 9887712)
  • Dapagliflozin propanediol (PubChem CID: 24906252)
  • Isopropyl acetate (PubChem CID: 7915)

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