布洛芬--环糊精包合纳米凝胶的体外扩散研究

F. Darusman, Debby Prihasti Ayustine, Saadiya Noerman, Sani Ega Priani, Widad Aghnia Shalannandia
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引用次数: 1

摘要

包合物是提高活性物质溶解度,影响药物溶出和渗透的一种方法。包合物是利用b-环糊精作为活性化合物的宿主形成的。布洛芬(2-(4-异丁基苯基)丙酸酯)是丙酸衍生物,具有低溶出性和高渗透性,在生物制药分类系统中属于II类。本研究旨在制备含布洛芬-β-环糊精包合物的纳米凝胶,其比例分别为1:1、1:2和2:1;并将其与纯布洛芬凝胶的体外扩散谱进行比较。以三摩尔比为1:1、1:2、2:1的共沉淀法制备布洛芬-β-环糊精包合物。采用凝胶凝胶法进行体外研究,比较了布洛芬β-环糊精和纯布洛芬凝胶的三种配方。实验中所测凝胶的布洛芬浓度为1%。对布洛芬-β-环糊精包合凝胶的粒径进行表征,得到粒径为510 nm的纳米级凝胶。这一特性表明,与粒径较小(156 nm)的纯布洛芬凝胶相比,包合物凝胶可以提高布洛芬的累积释放量。布洛芬纯粉粒度为763 nm,包合物粒径为957 nm。布洛芬-b-环糊精包合凝胶的摩尔比为2:1时,布洛芬的体外扩散谱增加,累积释放量为740.3µg。Cm -2。纯布洛芬凝胶的累积释放量为294.74µg。Cm -2。含有布洛芬-β-环糊精包合物的凝胶与纯布洛芬凝胶相比,能提高布洛芬的累积释放量。布洛芬-β-环糊精包合物凝胶以2:1的比例增加了布洛芬在体外的扩散。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In-vitro diffusion study of ibuprofen--cyclodextrin inclusion complex nanogel
The inclusion complex is one way to enhance active substance solubility, affecting medicine dissolution and penetration. The inclusion complex is formed by utilizing b-cyclodextrin as the host of the active compounds. The Ibuprofen (2-(4-isobutyl-phenyl)propionate) is a propionate acid derivative and classified in class II of the Biopharmaceutic Classification System, which has low dissolutions and high permeability. This study aims to develop a nanogel containing ibuprofen-β-cyclodextrin inclusion complex with the ratio of 1:1, 1:2 and 2:1; and to compare the in-vitro diffusion profile with pure ibuprofen gel. The inclusion complex of ibuprofen-β-cyclodextrin was prepared using the coprecipitation method with the three molar comparison ratio of 1:1, 1:2, and 2:1. The in-vitro study was performed using the gel-based viscolam, comparing the three formulas of ibuprofen-β-cyclodextrin with pure ibuprofen gel. The ibuprofen concentration of each gel tested in the experiment was 1%. The particle size characterization of ibuprofen-β-cyclodextrin inclusion complex gel resulted in having nanoparticle size (510 nm). This characteristic indicates that the inclusion complex gel could enhance the cumulative release amount of ibuprofen compared with pure ibuprofen gel with a relatively smaller particle size (156 nm). Pure ibuprofen and inclusion complex powder size measured to be 763 nm and 957 nm, respectively. The ibuprofen-b-cyclodextrin inclusion complex gel with a molar ratio of 2:1 demonstrated an increase in in-vitro diffusion profile of ibuprofen with a cumulative release amount of 740.3 µg.cm -2 . Meanwhile, pure ibuprofen gel had the cumulative release amount of 294.74 µg.cm -2 . The gel containing ibuprofen-β-cyclodextrin inclusion complex could enhance the cumulative release amount of ibuprofen compared to pure ibuprofen gel. The ibuprofen-β-cyclodextrin inclusion complex gel at a ratio of 2:1 exhibited an increase in the diffusion of ibuprofen in-vitro .
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