Highlights
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- Single crystal X-ray analysis of cevimeline is reported for the first time.
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- Single crystal X-ray analysis of trans-cevimeline is reported for the first time.
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- PXRD, thermal analysis and solubility studies of both compounds is provided.
Abstract
Cevimeline is muscarinic receptor agonist which increases secretion of exocrine glands. Cevimeline base is a liquid (m.p. 20–25 °C) at ambient conditions, therefore its pharmaceutical formulation as a solid hydrochloride hemihydrate has been developed. The synthesis of cevimeline yields its cis- and trans-isomers and only the cis-isomer is recognized as the API and used in the finished formulation. In this study structural and physicochemical investigations of hydrochloride hemihydrates of cis- and trans-cevimelines have been performed. Single crystal X-ray analyses of both cis- and trans-isomers of cevimeline are reported here for the first time. It was found that the cis-isomer, the API, has less dense crystal packing, lower melting point and higher solubility in comparison to the trans-isomer.
Graphical abstract
Keywords
- Cevimeline;
- trans-Cevimeline;
- Impurity standard;
- Single crystal X-ray analysis;
- Thermal analysis;
- Solubility
- Soure:Sciencedirect
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