葛根素固体分散体制备方法的比较

A Comparison on Preparation Methods for Solid Dispersion of Puerarin

考察了不同方法制备的固体分散体对葛根素(1)溶出性能的改善效果。分别采用超临界抗溶剂技术(SAS)、喷雾干燥法和溶剂法制备1-聚乙烯吡咯烷酮(PVP K30)固体分散体,通过扫描电镜和粉末X射线衍射(PXRD)分析进行表征,并对比了3种固体分散体的溶出行为。结果表明,3种方法均可制得固体分散体,药物以无定形或分子形式存在。与1原料药相比,不同固体分散体中1的溶出均得到明显改善。其中,SAS法制备的1固体分散体粒径更小、溶出速度和程度更高。

The solid dispersions （SDs） of puerarin （I） with polyvinylpyrrolidone （PVP K30） as carriers were prepared to improve the dissolution, and the effect of preparation method on the morphology, diameter and dissolution behavior were investigated. Firstly, the SDs were prepared by supercritical anti-solvent （SAS） method, spray drying process and solvent method, respectively. Then, scanning electron microscopy （SEM） and powder X-ray （PXRD） diffraction were used to characterize these samples. The results showed that the drug existed in a non-crystalline solid form in all three SDs. Compared with the bulk drug, three SDs could significantly improve the dissolution of 1. Among the three SDs, the product prepared by SAS had a smaller particle size, a higher dissolution degree and a faster dissolution rate.