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KMID : 0043320110340050775
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Archives of Pharmacal Research
2011 Volume.34 No. 5 p.775 ~ p.779
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Solid state of CG-400549, a novel FabI inhibitor: Characterization, dissolution, transformation
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Kim Bo-Yeon
Sohn Young-Taek
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Abstract
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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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KEYWORD
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CG-400549, Dissolution, Polymorphism, Pseudopolymorphism, Transformation
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