利用新型亲水性聚合物载体改善水溶性差的抗寄生虫药物伊维菌素的体外溶解状况

Tanvir Rahman, Md Abdurrahim, Koma Afrin Rintu, Md Raihan Sarkar, Md Alamgir Kabir, Dipa Islam, Md Hasanuzzaman
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引用次数: 0

摘要

伊维菌素(IVM)是一种水溶性较弱的 BCS II 类药物,其口服吸收和溶解度极低。本研究旨在通过使用四种亲水性聚合物的固体分散方法来提高伊维菌素的溶解度:Kollicoat IR、Kollidon 90F、poloxamer 407 和羟丙基甲基纤维素(HPMC)。固体分散制剂(SDF)是通过物理混合、溶剂蒸发和熔融溶剂/熔融法制成的。使用 IVM 和亲水性载体的三种比例(1:1、1:2 和 1:3),通过物理混合、溶剂蒸发和熔融形成的制剂中 IVM 的累积释放率远远大于纯 IVM(10%)。Poloxamer 407、Kollicoat IR 和 HPMC 聚合物制剂的 IVM 释放率分别为 76%(融合技术)、69%(物理混合)和 47%(溶剂蒸发法)。研究表明,熔融法比物理混合法和溶剂蒸发法更能优化药物溶解度。研究发现,弱水溶性 IVM 与 Kollicoat IR/Poloxamer 407 的 SD 能更好地改善其体外溶解状况。孟加拉 J. Sci.58(4), 209-220, 2023
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Improvement of in vitro dissolution profile of poorly aqueous soluble anti-parasitic agent ivermectin using novel hydrophilic polymeric carriers
Ivermectin (IVM), a BCS Class II drug with weak water solubility, has minimal oral absorption and dissolution. This study aims to enhance the dissolution profile of IVM by performing solid dispersion methods using four hydrophilic polymers: Kollicoat IR, Kollidon 90F, poloxamer 407, and hydroxypropyl methylcellulose (HPMC). The solid dispersion formulations (SDF) were made through physical mixing, solvent evaporation, and melt solvent/fusion. Using three ratios of IVM and hydrophilic carriers (1:1, 1:2, and 1:3), the cumulative release rate of IVM from formulations formed by physical mixing, solvent evaporation, and fusing was much larger than pure IVM (10%). IVM release rates from formulations including Poloxamer 407, Kollicoat IR, and HPMC polymers were 76% (fusion technique), 69% (physical mixing), and 47% (solvent evaporation method). The research demonstrated that fusion optimized drug solubility better than physical mixing and solvent evaporation. The research found that SD of weakly water-soluble IVM with Kollicoat IR/Poloxamer 407 improves its in vitro dissolving profile much better. Bangladesh J. Sci. Ind. Res. 58(4), 209-220, 2023
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