使用原生淀粉和改性淀粉配制布洛芬固体分散体并确定其特性

A. O. Olagunju, B. O. A. B. A-C, L. G. B. A-C
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引用次数: 0

摘要

背景:布洛芬是一种抗炎镇痛药,具有弱水溶性,生物利用度较低:布洛芬是一种抗炎镇痛药,水溶性弱,生物利用度低:本研究旨在使用天然聚合物(原生木薯和转基因木薯(GMS)、木薯纳米晶和玉米淀粉)作为可能的亲水性载体,以不同的重量比例通过溶剂蒸发法配制布洛芬固体分散体,以优化布洛芬的溶解度和溶出度:采用溶剂蒸发法配制不同药物聚合物比例的布洛芬固体分散体。使用扫描电子显微镜(SEM)、傅立叶变换红外光谱(FTIR)、差示扫描量热仪(DSC)、X 射线衍射仪(XRD)、粒度和体外药物释放对纯药物和固体分散体进行表征:用淀粉纳米晶体配制的固体分散体的溶解度最高。所有药物与聚合物比例为 1:2 的固体分散体一般都显示出最高的溶解度。根据傅立叶变换红外光谱,布洛芬的化学结构在无定形固体分散体中保持不变,但根据 XRD 和 DSC 也证实了这一点。扫描电子显微镜显示,固体分散体比纯药物更多孔。纳米晶体固体分散体的溶解速率更高,T50(释放 50%药物所需的时间)在 1.8 到 4.1 分钟之间:这项研究表明,使用这些天然聚合物提高了布洛芬的溶解度和溶解速率。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and characterization of ibuprofen solid dispersions using native and modified starches
Background: Ibuprofen is an anti-inflammatory analgesic drug that is weakly water-soluble with a poor bioavailability.Objectives: The aim of this study is to formulate ibuprofen solid dispersions by solvent evaporation method using natural polymers (native cassava and genetically modified cassava (GMS), Cassava nanocrystal and corn starches) as possible hydrophilic carriers at varying weight proportions to optimize ibuprofen solubility and dissolution.Material and Methods: Solvent evaporation method was used to formulate the ibuprofen solid dispersions at different drug polymer ratios. The pure drug and solid dispersions were characterized using Scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray diffractometer (XRD), particle size, and in vitro drug release.Results: Solid dispersions formulated with starch nanocrystals showed the highest solubility. All solid dispersions prepared with drug:polymer ratio 1:2 generally showed highest solubility. According to the FTIR, the chemical structure of ibuprofen remained intact in the amorphous solid dispersion, but the structure changed from crystalline to amorphous, according to the XRD and the DSC also confirmed this. The scanning electron microscopy showed the solid dispersions were more porous than the pure drug. Higher dissolution rate was observed with nanocrystal solid dispersions with T50 (time required for 50% of the medication to be released) between 1.8 and 4.1 minutes.Conclusion: This study has shown that using these natural polymers increased the solubility and dissolution rate of ibuprofen.
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