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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >A novel solid dispersion system for natural product-loaded medicine: silymarin-loaded solid dispersion with enhanced oral bioavailability and hepatoprotective activity
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A novel solid dispersion system for natural product-loaded medicine: silymarin-loaded solid dispersion with enhanced oral bioavailability and hepatoprotective activity

机译：用于天然药物的新型固体分散系统：水飞蓟素的固体分散体具有增强的口服生物利用度和保肝活性

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摘要

A surface-attached silymarin-loaded solid dispersion with improved dissolution profile and enhanced oral bioavailability was formulated using silymarin, polyvinylpyrrolidone (PVP) and Tween 80 in water. In this solid dispersion, hydrophilic PVP was adhered onto the surface of crystalline drug rendering silymarin hydrophilic without changing its crystallinity. The drug solubility from the optimised solid dispersion prepared with silymarin/PVP/Tween 80 at the weight ratio of 5/2.5/2.5 increased by almost 650-fold compared to drug powder. The drug was physically and chemically stable in the solid dispersion for at least 6 months. Moreover, the solid dispersion enhanced the oral bioavailability of the drug in rats by almost 3-fold compared to the commercial product. The silymarin-loaded solid dispersion also exhibited advanced hepatoprotective bioactivity against CCl4-induced liver damage compared to silymarin or the commercial product. Thus, this silymarin-loaded solid dispersion would be useful for the enhancement of oral bioavailability and hepatoprotective activity of poorly water-soluble silymarin.
机译：使用水飞蓟素，聚乙烯吡咯烷酮（PVP）和吐温80在水中配制了表面附着水飞蓟素的固体分散体，具有改善的溶出度和增强的口服生物利用度。在该固体分散体中，亲水性PVP附着在结晶药物的表面上，使水飞蓟素具有亲水性而不改变其结晶度。与水粉相比，以5 / 2.5 / 2.5的重量比用水飞蓟素/ PVP /吐温80制备的优化的固体分散体的药物溶解度增加了近650倍。该药物在固体分散体中在物理和化学上稳定至少6个月。而且，与市售产品相比，该固体分散体将药物在大鼠中的口服生物利用度提高了几乎3倍。与水飞蓟素或市售产品相比，水飞蓟素负载的固体分散体还具有针对CCl4诱导的肝损伤的先进的肝保护生物活性。因此，这种水飞蓟素负载的固体分散体可用于提高水溶性差的水飞蓟素的口服生物利用度和肝保护活性。

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