Crystal forms of SK-3530

Abstract

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.

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

“…Because of their structural differences, polymorphs may have different physicochemical properties. For example, polymorphs can have different density, habit, melting properties, vapor pressure, solubility, dissolution rate, tableting and mechanical properties (Haleblian and McCrone, 1969;Haleblian, 1975;Hüttenrauch, 1988;Song and Sohn, 2010).…”