淫羊藿苷元磷脂复合物的制备及其固体分散体研究  

Preparation of icaritin phytosomes and their solid dispersions

作　　者：贾东升[1,2] 赵江丽[3] 施峰[1] 贾晓斌[1,2] 

机构地区：[1]江苏省中医药研究院中药新型给药系统重点实验室,国家中医药管理局中药口服制剂释药系统重点研究室,江苏南京210028 [2]江苏大学药学院,江苏镇江212013 [3]江苏大学食品与生物工程学院,江苏镇江212013

出　　处：《中草药》2010年第9期1449-1453,共5页Chinese Traditional and Herbal Drugs

基　　金：江苏省医药高技术计划项目(BG2007614);江苏省中医药领军人才项目(2006)

摘　　要：目的制备淫羊藿苷元磷脂复合物,研究其固体分散体,提高淫羊藿苷元磷脂复合物的体外溶出度。方法以复合率为指标,通过单因素及正交设计优化制备工艺,采用溶剂回流法制备淫羊藿苷元磷脂复合物与聚乙烯吡咯烷酮(PVP)的共沉淀物;以体外溶出度法考察不同配比PVP共聚物胶囊的药物累积溶出度。结果淫羊藿苷元磷脂复合物的最佳制备条件:无水乙醇为溶剂,淫羊藿苷元质量浓度5 mg/mL,药物与大豆磷脂质量比1∶3,50℃反应1h。所得磷脂复合物使淫羊藿苷元在水及正辛醇中的平衡溶解度提高5.9、1.6倍;淫羊藿苷元磷脂复合物与PVP(质量比为1∶1)共沉淀物胶囊体外溶出度明显高于淫羊藿苷元磷脂复合物。结论淫羊藿苷元磷脂复合物可改善淫羊藿苷元的溶解性能,淫羊藿苷元磷脂复合物-PVP共沉淀物可提高淫羊藿苷元磷脂复合物的体外溶出度。Objective To optimize preparation techniques for icaritin phytosomes and explore their solid dispersions to increase the dissolution of icaritin in vitro.Methods The preparation conditions for icaritin phytosomes were optimized by means of orthogonal test,and the icaritin phytosome-PVP coprecipitates were prepared by means of solvent evaporation.The accumulative dissolution rate of icaritin in coprecipitates with different ratios of icaritin-phytosomes to PVP was investigated according to dissolution release in vitro. Results The optimized preparation conditions for icaritin phytosomes were obtained as follows： Solvent was ethanol,the concentration of icaritin was 5 mg/mL,the ratio of icaritin to phospholipid was 1 to 3,temperature was 50 ℃,reaction time was 1 h.The solubility of icaritin was enhanced by 1.6 and 5.9 times in n-octyl alcohol and water.The accumulative dissolution rate of icaritin phytosome-PVP coprecipitates（ratio of mass was 1 to 1） was significantly higher than that of icaritin phytosomes.Conclusion Phospholipid could effectively enhance the solubility of icaritin and the coprecipitate of icaritin hytosomes and PVP could improve its dissolution in vitro.

关 键 词：淫羊藿苷元 磷脂复合物 固体分散体 

分 类 号：R286.02[医药卫生—中药学]