Crystal forms of an angiotensin II receptor antagonist BR-A657

2011

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.

Section: Introductionmentioning

confidence: 99%

Solid state of CG-400549, a novel FabI inhibitor: Characterization, dissolution, transformation

Kim

2011

“…Various techniques are currently utilized to characterize polymorphs including differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), hot-stage microscopy (HSM), Fourier transform infrared (FT-IR) spectroscopy, solidstate nuclear magnetic resonance (SSNMR) spectroscopy, fluorescence and thermogravimetric analysis (TG) (Giron, 1995;Ceolin et al, 1997;Patel et al, 2000;Brittain, 2004;Atassi and Byrn, 2006;Sohn, 2007;An and Sohn, 2009). SK-3530, (Mirodenafil 2HCl, Fig.…”

Section: Introductionmentioning

confidence: 99%

Crystal forms of SK-3530

Song

2010

The objective of this work was to investigate the existence of polymorphs of SK-3530 and the transformation of crystal forms. Two crystal forms of SK-3530 have been isolated by recrystallization and characterized by differential scanning calorimetry, powder X-ray diffractometry and thermogravimetric analysis. The differential scanning calorimetry and powder X-ray diffractometry patterns of two crystal forms were different respectively. 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), Form 2 was not transformed to Form 1 and two forms were shown to have a good physical stability at room temperature for 1 month. In the dissolution studies in pH 6.8 buffer at 37 ± 0.5°C, the dissolution rate of Form 2 was significantly higher than that of Form 1 under 30 min.

“…Various techniques are currently utilized to characterize polymorphs including powder X-ray diffraction (PXRD), hot-stage microscopy (HSM), differential scanning calorimetry (DSC), Fourier transform infrared (FT-IR) spectroscopy, solid-state nuclear magnetic resonance (SSNMR) spectroscopy, and thermogravimetric analysis (TG) (Shell, 1963;Kuhnert-Brandstätter and Winkler, 1976;Burger et al, 1980;Bauer-Brandl and Sohn, 1994;Aso et al, 2001;Sohn and Lee, 2005;Sohn, 2007;Lee and Sohn, 2008).…”

Section: Introductionmentioning

confidence: 99%

Crystal forms of atorvastatin

2009

The objective of this work was to investigate the existence of new polymorphs and pseudopolymorphs of atorvastatin and the transformation of crystal forms. Three crystal forms of atorvastatin have been isolated by recrystallization and characterized by powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC), and thermogravimetric analysis (TG). The PXRD and DSC patterns of the three crystal forms were different respectively and it was confirmed that Form 3 is a new crystal form. After storage of 2 years at room temperature, this new crystal form was not transformed and it was shown to have a good physical stability.