Improvement in physicochemical properties of ezetimibe using a crystal engineering technique

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• 作者：Snehal P. Mulye  ; [Author Vitae] ; Samina A. Jamadar  ; [Author Vitae] ; Poonam S. Karekar  ; [Author Vitae] ; Yogesh V. Pore ; ^{dryogeshpore@rediffmail.com}  ; [Author Vitae] ; Shashikant C. Dhawale  ; [Author Vitae]
• 关键词：Ezetimibe ; Benzoic acid ; Salicylic acid ; Crystal engineering ; Dissolution ; Physicochemical properties
• 刊名：Powder Technology
• 出版年：2012
• 期刊代码：144_00325910
• 类别：et
• 出版时间：May, 2012
• 卷：222
• 期：Complete
• 页码：131-138
• 文件大小：881 K

摘要

In an attempt to improve the physicochemical properties of poorly aqueous soluble ezetimibe, its pharmaceutical co-crystals were successfully engineered with different crystal forming agents; benzoic acid and salicylic acid in equimolar ratios by solution crystallization technique. The physicochemical properties of pure ezetimibe and corresponding co-crystals were accessed in terms of phase solubility studies, melting point, flowability, drug content uniformity, saturation solubility and dissolution studies. Fourier transformation infrared spectroscopy (FTIR), X-ray powder diffractometry (XRPD) and scanning electron microscopy (SEM) techniques were employed to investigate the hydrogen bonding interaction, crystallinity and surface morphological characteristics of prepared co-crystals respectively. The results indicated a marked improvement in flow properties and saturation solubility of co-crystals (p < 0.001). Further, in case of dissolution experiments, both the co-crystals showed a significant enhancement (DE₅ and DE₂₀, p < 0.001) in the dissolution profiles as compared to pure ezetimibe. It could be concluded that substantial manipulation of physicochemical properties of ezetimibe could be possible with benzoic acid and salicylic acid using crystal engineering technique.