难水溶性药物橙皮苷固体分散体的制备及评价

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引用次数: 1

摘要

橙皮苷是一种植物衍生的类黄酮,大量存在于不同的柑橘类植物中,包括柠檬、橙子、酸橙和葡萄柚。它具有多种治疗意义的生物学潜力,包括抗炎、抗脂肪、抗氧化、胰岛素增敏、抗菌、神经保护和抗癌活性。本研究的目的是通过热熔挤压法制备天然聚合物作为固体分散体,提高橙皮苷的溶解度和释放速度,从而提高模型药物的溶出特性。通过傅里叶变换红外光谱(FT-IR)和差示扫描量热法(DSC)进行相容性分析。通过零级、一级、Higuchi、Korsmeyer-Peppas和Hixson-Crowell模型表征了药物释放机制的动力学研究。溶出度分析表明,固体分散体释药率达99%以上。优化后的处方符合Higuchi模型,R2值为0.919。通过热熔挤压法制备的含有天然聚合物的固体分散体与纯药物橙皮苷相比,在释放曲线上表现出显著的增强。
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 Evaluation of Solid Dispersions of Poorly Water-Soluble Drug- Hesperidin
Hesperidin is a plant-derived flavonoid, abundantly present in the different citrus species, including lemon, orange, lime, and grapefruit. It possesses the diverse biological potential of therapeutic significance, including anti-inflammatory, anti-adipogenic, antioxidant, insulin-sensitizing, antimicrobial, neuroprotective, and anti-carcinogenic activities. The objective of the present study was to enhance the dissolution characteristics of the model drug by increasing the solubility and release rate of hesperidin through solid dispersions using natural polymers by the hot-melt extrusion method. The compatibility analysis was carried out through Fourier Transform-Infrared Spectroscopy (FT-IR) and Differential scanning calorimetry (DSC). The kinetic studies for drug release mechanisms were characterized through zero-order, first-order, Higuchi, Korsmeyer-Peppas, and Hixson-Crowell models. The dissolution analysis of solid dispersions showed exhibited more than 99% drug released. The optimized formulation was found to follow the Higuchi model of drug release kinetics with an R2 value of 0.919. Solid dispersions containing natural polymers prepared through the hot-melt extrusion method exhibited significant enhancement in the release profile compared to a pure drug, hesperidin.
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CiteScore
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