Preparation of Piretanide Polymorphs and Their Physicochemical Properties and Dissolution Behaviors

概要

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Piretanide polymorphs were prepared by recrystallization using 27 organic solvents. We identified a new polymorphism, forms A and B, and 6 solvates. They were characterized by X-ray powder diffractometry, differential scanning calorimetry (DSC), thermogravimetry (TG), Fourier-transform infrared (FTIR) spectroscopy, elemental analysis and scanning electron microscopy. After heating, some solvates transformed to the stable form A , and others to form B. X-ray powder diffraction patterns and FTIR spectra of forms A and B were significantly different. However, the X-ray powder diffraction patterns and FTIR spectra of form A and the bulk sample were similar. The DSC curve of form A showed only an endothermic peak at 227℃ corresponding to the melting point. The DSC curve of form B showed endothermic and exothermic peaks at 213 and 216℃, respectively, as well as a subsequent endothermic peak at 227℃. The metastable form B transformed to form A. The dissolution profiles of the bulk sample and form B in JP XII, 1st fluid (pH 1.2) at 37℃ were measured by means of the dispersed amount. The solubilities of the bulk sample and form B were estimated to be 8.3 and 13.3mg/100ml, respectively.
社団法人日本薬学会の論文
1994-05-15