冬凌草甲素固体分散体的制备及溶解性能研究

Studies on Preparation and Dissolution of Oridonin Solid Dispersions

关键词:  冬凌草甲素  固体分散体  溶解度  溶出速率  差示热分析

Key words:  oridonin  solid dispersion  solubility  dissolution rate  differential thermal analysis

摘要:

目的 采用固体分散技术，提高冬凌草甲素的体外溶解性能。方法 分别以聚乙二醇6000(PEG6000)、聚乙烯吡咯烷酮K30(PVPK30)为载体，制备冬凌草甲素固体分散体。采用紫外分光光度法进行含量测定，差示热分析法鉴别药物在载体中的存在状态，并进行溶解度、体外溶出速率实验。结果 两种载体的固体分散体均能增加药物的溶解度和溶出速率，冬凌草甲素在载体中以高度分散状态存在。结论 以 PVPK30为载体制备的冬凌草甲素固体分散体体外溶解度和溶出速率明显提高。

Abstract:

OBJECTIVE To prepare and characterize the solid dispersions (SDs) with improved solubility and dissolution rates of oridonin. METHODS The SDs were prepared with polyethyleneglycol 6000 (PEG6000) and polyvinylpyrrolidone K30 (PVPK30) as carriers respectively. UV-spectrophotometry was used to determine the contents of oridonin. The physical and chemical properties of SDs, starting material and physical mixtures were investigated by differential thermal analysis (DTA) and dissolution rate in vitro. The solubilities were studied. RESULTS It was found that the solubility and dissolution rates of oridonin were enhanced for the formation of SDs. Oridonin exists in a highly dispersed state in the carriers. CONCLUSION The SDs prepared with PVPK30 can increase the solubility and dissolution rate of oridonin remarkablely.