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盐酸伊伐布雷定漂浮型口服凝胶的制备、优化与验证。

Formulation, optimization and validation of floating oral gel of Ivabradine hydrochloride.

机构信息

Department of Pharmaceutics, KLE College of Pharmacy, Belagavi, KLE Academy of Higher Education & Research, Belagavi, Karnataka, 590010, India.

出版信息

Ther Deliv. 2022 May;13(5):283-294. doi: 10.4155/tde-2022-0008. Epub 2022 May 26.

DOI:10.4155/tde-2022-0008
PMID:35615867
Abstract

Ivabradine hydrochloride is a hyperpolarized activated channel blocker used for symptomatic treatment of chronic angina pectoris. However, due to its short half-life it is rapidly eliminated from systemic circulation. Floating gel was formulated using sodium alginate and HPMC K 100 M by pH induced ion gelation technique employing 3 factorial design for optimization and evaluated. The formulation remained buoyant in gastric environment for 12 h. Optimized formulation sustained and prolonged drug release in comparison with marketed product. Kinetic analysis of drug release indicated non fickian mechanism. Short term stability studies showed no significant changes indicating good formulation stability. Formulated solution shows potential effective sustained release over a prolonged period of time.

摘要

氢氯噻嗪盐酸盐是一种超极化激活通道阻滞剂,用于治疗慢性心绞痛的症状。然而,由于其半衰期短,它会从体循环中迅速消除。采用 pH 诱导的离子凝胶化技术,以 3 因素设计进行优化,用海藻酸钠和 HPMC K 100 M 制备漂浮凝胶并进行评价。制剂在胃环境中能保持 12 小时的漂浮。与市售产品相比,优化的制剂能持续和延长药物的释放。药物释放的动力学分析表明非菲克扩散机制。短期稳定性研究表明没有显著变化,表明良好的制剂稳定性。配制的溶液具有在较长时间内有效持续释放的潜力。

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