芹菜素固体分散体的制备及其体外溶出研究
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刘雅莉1，袁文蛟2，刘晓红1，孙 进1，孙英华1，何仲贵1
(1.沈阳药科大学 药学院，辽宁 沈阳 110016；2.华东理工大学 化学与制药学院，上海 200237 )
摘要：目的 制备芹菜素固体分散体，并检测其体外溶出度。 方法 选择聚乙烯吡咯烷酮(PVP)、聚乙二醇(PEG)等3种载体，分别采用溶剂法和熔融法制备芹菜素固体分散体，并进行了体外溶出研究。X-射线粉末衍射分析鉴别药物在载体中的存在状态。结果 所制得的固体分散体均可改善芹菜素的溶出，特别是质量比为1:9的芹菜素-PVP固体分散体。芹菜素在该固体分散体中以无定型 状态存在。结论 PVP是提高芹菜素溶出的理想载体。芹菜素溶出度的增大与其无定形的存在状态有关。
关键词：药剂学；体外溶出度；固体分散体；芹菜素；聚乙烯吡咯烷酮；聚乙二醇
中图分类号：R969.1 文献标识码：A
Preparation and evaluation of apigenin solid dispersions in vitro
LIU Ya-li1, YUAN Wen-jiao2,LIU Xiao-hong1, Sun jin1, Sun Ying-hua1, HE Zhong-gui1
(1. School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China;2. School of Chemistry and Pharmacy, East China of a University of Science and Technology, Shanghai 200237, China)
Abstract: Objective To prepare apigenin (AP) solid dispersion and measure its dissolution in vitro. Methods Apigenin solid dispersions were obtain with PVP, PEG4000 and PEG6000 as carriers by coevaporation and melting methods respectively, The dissolution characteristics in vitro were studied in simulated intestinal juice and powder X-ray diffraction were used to determine the status of drug in carriers. Results The dissolution of apigenin was improved significantly by solid dispersions prepared, especially the AP-PVP (m: m＝1:9) solid dispersion. The drug was an amorphous state in AP-PVP solid dispersion. Conclusions PVP is a very useful carrier in improving the dissolution of apigenin. It is clear that the enhancement of the dissolution rate of AP from PVP solid dispersion is relative to its amorphous state in PVP.
Key words: pharmaceutics; dissolution in vitro; solid dispersion; apigenin; PVP; PEG
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