星点设计-效应面法优化齐墩果酸长循环脂质体的制备工艺  

Optimization of Preparation of Oleanolic Acid Long-circulation Liposomes by Central Composite Design-Response Surface Methodology

作　　者：周惠恩 王婴[1] 王岩[1] 李子雯[1] 黄春连[1] 

机构地区：[1]广东药学院,广东广州510006

出　　处：《中药新药与临床药理》2015年第5期702-707,共6页Traditional Chinese Drug Research and Clinical Pharmacology

基　　金：广东省科技计划项目(20120318055);广东省教育厅学科建设专项资金(2013KJCX0110)

摘　　要：目的为了提高齐墩果酸的生物利用度和靶向性,以卵磷脂和胆固醇为包封材料,研究齐墩果酸脂质体的处方和制备工艺。方法采用薄膜超声分散法制备脂质体,用高效液相法(HPLC)测定齐墩果酸的含量。以包封率为指标,采用星点设计-效应面法优选处方和工艺。结果齐墩果酸脂质体的最佳处方和工艺条件为:卵磷脂与胆固醇的质量比为7;卵磷脂与齐墩果酸的质量比为5.5,超声时间为35 min。制备的脂质体平均粒径为312 nm,平均包封率为90.66%。结论该工艺方法简便、稳定可行,适用于齐墩果酸长循环脂质体的制备。Objective To improve the bioavailability and targeting property of oleanolic acid（OA）. Phospholipid and cholesterol were used as the carrier material to optimize the prescription and preparation technology of OA liposomes. Methods Liposomes were prepared by thin-film ultrasonic dispersion method, and the content of oleanolic acid was determined by HPLC. With the entrapment efficiency as the index, prescription and process were optimized by central composite design-response surface methodology. Results The optimum prescription and process conditions were as follows： the mass ratio of lecithin to cholesterol was 7, the mass ratio of lecithin to oleanolic acid was 5.5, and time for ultrasound vibration was 35 min. The average particle size of liposomes was 312 nm, and the average entrapment efficiency was 90.66 %. Conclusion The optimized process is feasible, stable and applicable for the production of long circulation liposomes of oleanolic acid.

关 键 词：齐墩果酸 长循环脂质体 制备工艺 星点设计-效应面法 

分 类 号：R284.2[医药卫生—中药学]