穿心莲内酯衍生物ATC-Ⅱ脂质体的制备  

Preparation of andrographolide derivatives ATC-Ⅱ-loaded liposomes

作　　者：高兴荣[1] 韩光[1] 张瑜[1] 焦文温[1] 张生杰[1] 华素[1] 

机构地区：[1]河南大学药物研究所,河南开封475004

出　　处：《中成药》2012年第4期633-637,共5页Chinese Traditional Patent Medicine

基　　金：河南省科技创新人才项目(094100510020)

摘　　要：目的采用星点设计-效应面法优化穿心莲内酯衍生物ATC-Ⅱ脂质体的处方工艺。方法采用薄膜分散法制备ATC-Ⅱ脂质体,以平均粒径、包封率,载药量为评价指标,以投药量、胆固醇用量、水化体积为处方工艺的考察因素,采用Design-expert软件进行星点设计,建立各指标与因素之间的数学关系,通过效应面法优化处方工艺条件,并通过验证性实验进行预测分析,对ATC-Ⅱ脂质体进行体外释放研究。结果各指标均采用二次多项式方程拟合最优,根据优化处方工艺制得ATC-Ⅱ脂质体的平均粒径为(146.3±2.47)nm,包封率为(88.54±1.12)%,载药量为(3.16±0.06)%;ATC-Ⅱ脂质体具有缓释特性,体外释放过程符合Riger-Peppas方程。结论星点设计效应面法可用于ATC-Ⅱ脂质体的处方工艺优化,预测性良好。AIM To optimize the formulation and preparation of andrographolide derivatives ATC- Ⅱ -loaded liposomes by composite design-response surface method. METHODS ATC- Ⅱ -loaded liposomes were prepared by film dispersion method, average particle size, encapsulation efficiency and drug loadings were used as the evaluation parameters. Dosage of drug, dosage of cholesterol, and hydration volume were used as the influence factors. Design-expert was used to establish the mathematical relationship of parameters and factors, and response surface method was used to optimize fol;mulation and process. The experimental results of the liposomes prepared under the optimum condition were compared with the predicted value to study the in vitro release of the ATC- Ⅱ -loaded liposomes. RESULTS The experiment showed that all parameters, including encapsulation efficiency, drug loadings and particle size, matched with second-order polynomial equation. According to the optimization conditions, the av erage particle size, encapsulation efficiency and drug loading were （ 146.3±2.47） nm, （88.54 ±1.12）% , （3.16± 0. 06）% , respectively. The release of ATC-Ⅱ-loaded liposomes was characteristics by Riger-Peppas equation. CONCLUSION Central composite design-response surface method is suitable to optimize ATC-Ⅱ-load liposomes formulation and process optimization, and has the advantage of the good predicted values.

关 键 词：ATC-Ⅱ 脂质体 薄膜分散法 星点设计-效应面法:体外释放 

分 类 号：R944[医药卫生—药剂学]