title: Solid state of CG-400549, a novel FabI inhibitor: characterization, dissolution, transformation.
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 Na(2)Cr(2)O(7)2H(2)O/20°C) and 95% RH (saturated solution of Na(2)HPO(4)/20°C), all crystal forms were not transformed.
authors.affiliation: College of Pharmacy, Duksung Women's University, Seoul 132-714, Korea.
authors.forename: Bo-Yeon
authors.initials: BY
authors.lastname: Kim
authors.forename: Young-Taek
authors.initials: YT
authors.lastname: Sohn
mesh_terms: D000900:Anti-Bacterial Agents / Q000032:analysis / Q000737:chemistry*; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors*; D002152:Calorimetry, Differential Scanning; D004355:Drug Stability; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH) / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000032:analysis / Q000737:chemistry*; D005750:Gastric Juice / Q000737:chemistry; D006358:Hot Temperature / Q000009:adverse effects; D006863:Hydrogen-Ion Concentration; D008968:Molecular Conformation; D033362:Powder Diffraction; D011725:Pyridines / Q000032:analysis / Q000737:chemistry*; D012995:Solubility; D013227:Steam; D013535:Suspensions; D013818:Thermogravimetry; D013876:Thiophenes / Q000032:analysis / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; C523750:CG 400549; D004791:Enzyme Inhibitors; D011725:Pyridines; D013227:Steam; D013535:Suspensions; D013876:Thiophenes; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH)