Solid state of CG-400549, a novel FabI inhibitor: Characterization,dissolution, transformation |
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| Authors: | Bo-Yeon Kim Young-Taek Sohn |
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| Affiliation: | (1) Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Weaver-Densford Hall, 308 Harvard Street, S.E., Minneapolis, Minnesota, 55455-0343;(2) Department of Chemistry, University of Minnesota, Smith Hall, 207 Pleasant Street S.E., Minneapolis, MN, 55455-0343;(3) Present address: Department of Pharmaceutical Chemistry, University of Kansas, 2095 Constant Avenue, Lawrence, Kansas, 66047-3729;(4) The NutraSweet Company, 601 E. Kensington Road, Mount Prospect, Illinois, 60056 |
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| Abstract: | The polymorphic and pseudopolymorphic forms of CG-400549, a novel FabI inhibitor with potent in vivo activity were prepared and characterized by differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD) and thermogravimetric analysis (TG). Seven crystal forms of CG-400549, one anhydrate and six solvates, have been isolated by recrystallization and the DSC and PXRD patterns of the seven crystal forms of CG-400549 were different respectively. The dissolution patterns of these seven crystal forms of CG-400549 were studied and they showed significant differences in the dissolution rate. After storage of 1 month at 0% RH (silica gel, 20°C), 52% RH (saturated solution of Na2Cr2O72H2O/20°C) and 95% RH (saturated solution of Na2HPO4/20°C), all crystal forms were not transformed. |
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