Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2486944 | Journal of Pharmaceutical Sciences | 2009 | 8 Pages |
Abstract
Three anhydrous polymorphs, a monohydrate and a dihydrate of an active pharmaceutical ingredient, N-{[(5S)-3-(4-{6-[(1R,5S)-6-cyano-3-oxabicyclo[3.1.0]hex-6-yl]pyridin-3-yl}phenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl}acetamide (Compound 1), have been crystallized and characterized. Slurry experiments and thermal data have been used to determine their relative thermodynamic stability. The hydrates of Compound 1 were found to be less stable than the most stable anhydrous Form I and converted into Form I in water within 15 min. The rate of conversion in a dry state was found to depend on the relative humidity (RH) and was highest at the two RH extremes examined, 5% and 97.5% RH. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:4111-4118, 2009
Keywords
Related Topics
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Pharmacology, Toxicology and Pharmaceutical Science
Drug Discovery
Authors
Rositza I. Petrova, Andrey Peresypkin, Christopher J. Mortko, Arlene E. McKeown, Jaemoon Lee, J. Michael Williams,