为提高生物利用率而配制和评估金丝桃素固体分散体

Devraj Pandey, Kajal Sharma, Parulben D Mehta
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引用次数: 0

摘要

本研究的目的是制备菊黄素的固体分散体,以提高其水溶解度和口服生物利用度。采用 I-opitmal 设计方法制备金丝桃素的固体分散体。采用四种不同的药物与载体比例,共制备了八种配方。甘露醇和 PVP-K30 被用作两种不同的载体,以乙醇作为药物和载体的共同溶剂,通过溶剂蒸发法配制 SD 来提高金丝桃素的溶解度。在蒸馏水中对金丝桃素进行了溶解度研究,发现其溶解度为 3.7 µg/mL。颗粒呈不规则球形,平均粒径为 34.90-38.09 微米。F5 的 SD 产率最高(93.2%),F8 最低(91.14%)。然而,所有配方的收率都高于 90%,这表明二元混合物的形成是正确的。药物含量在配方 SD4 中最高(94.23 ± 0.351 %),在配方 SD5 中最低(91.18 ± 0.251 %)。关键词:固体分散体、菊脂、甘露醇、PVP K30、溶剂蒸发
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FORMULATION AND EVALUATION OF SOLID DISPERSION OF CHRYSIN FOR IMPROVED BIOAVAILABILITY
The objective of the present study was to prepared solid dispersion of chrysin for improving its aqueous solubility and in turn its oral bioavailability. I-opitmal design approach was used for preparing the solid dispersion of chrysin. A total of eight formulations were prepared using four different ratios of drug to carrier. Mannitol and PVP-K30 were used as the two different carriers to improve the solubility of chrysin by formulating SD using solvent evaporation method employing ethanol as the common solvent for the drug and the carrier. The solubility study of chrysin was performed in distilled water and was found to be 3.7 µg/mL. The particles were irregular to spherical in shape and the average particle size ranged from 34.90-38.09 µm for the particles. The yield of the SD was highest for F5 (93.2%) and least for F8 (91.14%). For all the formulations the yield was nevertheless higher than 90% suggesting a proper binary mixture formation. The drug content was found to be highest in the formulation SD4 (94.23 ± 0.351 %) and the lowest in formulation SD5 (91.18 ± 0.251 %). KEYWORDS: Solid dispersion, chrysin, mannitol, PVP K30, solvent evaporation
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