Preformulation study of a proton pump inhibitor Ilaprazole

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• 作者：Seo-Kyung Kim ; Hyo-Choon Bang…
• 关键词：Crystal form ; DSC ; Ilaprazole ; Partition coefficient ; Polymorphism ; Preformulation ; PXRD ; TG
• 刊名：Journal of Thermal Analysis and Calorimetry
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：127
• 期：2
• 页码：1715-1723
• 全文大小：
• 刊物类别：Chemistry and Materials Science
• 刊物主题：Physical Chemistry; Analytical Chemistry; Polymer Sciences; Inorganic Chemistry; Measurement Science and Instrumentation;
• 出版者：Springer Netherlands
• ISSN：1588-2926
• 卷排序：127

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.