染料木素固体分散体的制备及体外评价

Preparation and in vitro Assessment of Genistein Solid Dispersions

以聚乙烯吡咯烷酮(PVP K30)为载体,利用喷雾干燥法制备染料木素(1)的固体分散体。采用X射线粉末衍射(XRPD)、差示扫描量热分析(DSC)和激光粒度分析(LD-PSD)对制品进行表征。结果表明,1在固体分散体中均以无定形或分子状态存在。所制备的1-PVP K30(1∶5,w/w)固体分散体平均粒径为(8.9±1.1)?m,在pH 6.8缓冲液中不但可显著提高1的溶解度至8.37 mg/ml,而且可使1在2 h内完全溶出;此外,在25℃/相对湿度60%条件下放置2个月,物理和化学稳定性较好。

The solid dispersions （SD） of genistein （1） were prepared by spray drying method with polyvinylpyrrolidone （PVP） K30 as carriers and characterized by X-ray powder diffraction （XRPD）, differential scanning calorimetry （DSC） and laser diffraction particle size distribution （LD-PSD）. The results showed that 1 existed in the form of amorphous or molecule in the polymeric carriers. The average particle size of the SDs in the drug carrier ratio of 1 ： 5 was （8.9±1.1）μm. The solubility of 1 in this product was significantly increased and reached 8.37 mg/ml in pH 6.8 buffer, meanwhile the dissolution of 1 was complete within 2 h. In addition, the product was rather stable after storage for 2 months at 25℃and relative humidity of 60 %.