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Chitin biomass-nifedipine amorphous solid dispersion for enhancement of hydrophobic drug dissolution in aqueous media
Sustainable Chemistry and Pharmacy ( IF 6 ) Pub Date : 2020-06-22 , DOI: 10.1016/j.scp.2020.100284
Siriporn Taokaew , Mitsumasa Ofuchi , Takaomi Kobayashi

Solid dispersions of poorly-water soluble nifedipine using microparticles fabricated from chitin biomass were prepared to improve the drug dissolution in an aqueous medium. After the drug loading and solvent evaporation, the drug loading capacity of 1, 6, and 19 %w/w was obtained. In the microstructure, the drug was dispersed on the porous chitin carrier with minor agglomeration leading to reduced crystallization and improved dissolution, nearly 100%, as compared to the pure nifedipine powder and the physical mixture with chitin. There was an interaction between functional groups of the drug and polymer, consequently the release prolonged for the entire 6 h with the maximum drug solubility of about 300 μg/ml. An in vitro release study showed that nifedipine effectively released from chitin into a simulated gastric releasing medium (pH 1.2). In this case, the release mechanism was best fitted with a Zero-order model based on the Fick's Law in the first 2 h. This research indicated that employing microparticle obtained from chitin biomass in the solid dispersion system lowered the drug recrystallization, facilitated drug release, and provided the sustainability in pharmaceutical science.



中文翻译:

几丁质生物质-硝苯地平无定形固体分散体,用于增强疏水性药物在水性介质中的溶解

使用由几丁质生物质制得的微粒制备水溶性差的硝苯地平的固体分散体,以改善药物在水性介质中的溶解。载药量和溶剂蒸发后,载药量分别为1、6和19%w / w。在微结构中,与纯硝苯地平粉末和与几丁质的物理混合物相比,药物以较小的团聚分散在多孔几丁质载体上,导致结晶减少和溶出度提高了近100%。药物和聚合物的官能团之间存在相互作用,因此释放时间延长了整个6小时,最大药物溶解度约为300μg/ ml。一种在体外释放研究表明硝苯地平从几丁质有效地释放到模拟的胃释放介质(pH 1.2)中。在这种情况下,释放机制最适合在头2小时内基于菲克定律的零级模型。这项研究表明,在固体分散体系中使用从几丁质生物质获得的微粒可以降低药物的重结晶,促进药物的释放,并为药学提供可持续性。

更新日期:2020-06-23
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