Development of a pharmaceutical cocrystal of a monophosphate salt with phosphoric acid

Alex M. Chen; Martha E. Ellison; Andrey Peresypkin; Robert M. Wenslow; Narayan Variankaval; Cecile G. Savarin; Theresa K. Natishan; David J. Mathre; Peter G. Dormer; Danielle H. Euler; Richard G. Ball; Zhixiong Ye; Yaling Wang; Ivan Santos

doi:10.1039/B612353H

Development of a pharmaceutical cocrystal of a monophosphate salt with phosphoric acid†

Alex M. Chen,*^a Martha E. Ellison,*^a Andrey Peresypkin,^a Robert M. Wenslow,^a Narayan Variankaval,^a Cecile G. Savarin,^a Theresa K. Natishan,^a David J. Mathre,^a Peter G. Dormer,^a Danielle H. Euler,^b Richard G. Ball,^a Zhixiong Ye,^a Yaling Wang^a and Ivan Santos^a

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^a Merck & Co. Inc., P.O. Box 2000, Rahway, New Jersey, USA
E-mail: alex_chen2@merck.com, martha_ellison@merck.com
Fax: +1 732 594 9140
Tel: +1 732 594 1599

^b Merck & Co. Inc., P.O. Box 4, West Point, PA, USA

Abstract

We report the first case of a pharmaceutical cocrystal formed between an inorganic acid and an active pharmaceutical ingredient (API), which enabled us to develop a stable crystalline and bioavailable solid dosage form for pharmaceutical development where otherwise only unstable amorphous free form or salts could have been used.

Chemical Communications

Development of a pharmaceutical cocrystal of a monophosphate salt with phosphoric acid†

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Development of a pharmaceutical cocrystal of a monophosphate salt with phosphoric acid

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