文摘
Ilaprazole (2[4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl)1H-benzimidazole, Noltec™) is a new proton pump inhibitor (PPI), which has effects on gastric acid secretion to protect gastrointestinal cells by irreversibly inhibiting H+/K+ ATPase. The objective of this study was to investigate the physicochemical properties of Ilaprazole that could affect drug performance and lead to the development of an efficacious dosage form. The n-octanol to water partition coefficients of Ilaprazole were 0.9951 at pH 6 and 0.8898 at pH 10. The particle size distribution of Ilaprazole powder was in the size range of 0.138–13.183 μm with a mean particle size of 3.311 μm. KR Patent No. 10-2009-0086121 and KR Patent No. 10-2009-0086615 disclose Forms C, D, G, K, A, B, E, F, and I. Four new crystal forms were obtained by recrystallization from different solvents. These crystal forms were characterized by differential scanning calorimetry, thermogravimetric analysis, and powder X-ray diffraction. Form 4 was a single methanol solvate, and Form 5 was a monohydrate. Forms 4 and 5 exhibit polymorphism.