1. Co-Crystal Screening of Diclofenac.
- Author
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Christer B. Aakeröy, Angela B. Grommet, and John Desper
- Subjects
DICLOFENAC ,CRYSTALLINE polymers ,PHARMACEUTICAL industry ,PYRAZOLES ,PYRIDINE ,PYRIMIDINES ,CRYSTALLIZATION - Abstract
In the pharmaceutical industry, co-crystals are becoming increasingly valuable as crystalline solids that can offer altered/improved physical properties of an active pharmaceutical ingredient (API) without changing its chemical identity or biological activity. In order to identify new solid forms of diclofenac--an analgesic with extremely poor aqueous solubility for which few co-crystal structures have been determined--a range of pyrazoles, pyridines, and pyrimidines were screened for co-crystal formation using solvent assisted grinding and infrared spectroscopy with an overall success rate of 50%. The crystal structures of three new diclofenac co-crystals are reported herein: (diclofenac)·(2-aminopyrimidine), (diclofenac)·(2-amino-4,6-dimethylpyrimidine), and (diclofenac)·(2-amino-4-chloro-6-methylpyrimidine). [ABSTRACT FROM AUTHOR]
- Published
- 2011
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