水飞蓟宾过饱和自乳化给药系统的制备及性质研究  

Preparation and evaluation of silymarin supersaturation self-emulsifying drug delivery system

作　　者：彭璇[1] 陈苹苹[1] 包强[1] 魏颖慧[1] 李范珠[1] 

机构地区：[1]浙江中医药大学药学院,浙江杭州310053

出　　处：《中草药》2010年第1期40-44,共5页Chinese Traditional and Herbal Drugs

基　　金：浙江省新苗人才计划(2007R40G2120032)

摘　　要：目的制备水飞蓟宾过饱和自乳化给药系统(S-SEDDS),并对其基本性质进行研究。方法通过溶解度试验、处方配伍试验和伪三元相图的绘制,以乳化时间、色泽和粒径为指标,筛选过饱和自微乳的处方组成。采用HPLC法测定水飞蓟宾S-SEDDS中药物;并以水飞蓟宾自乳化给药系统(SEDDS)为对照,考察药物溶出特征。结果水飞蓟宾S-SEDDS的最佳处方组成为:油相中链甘油三酯(MCT)40%、乳化剂聚氧乙烯氢化蓖麻油(Cremophor RH40)48%、助乳化剂辛酸癸酸聚乙二醇甘油酯(Labrasol)12%,羟丙甲纤维素(HPMC)的加入量为50 mg/g;水飞蓟宾S-SEDDS的平均粒径为49.6 nm,自乳化时间<3 min,载药量为39.3 mg/g;体外溶出试验表明处方中加入少量的沉淀抑制剂,可有效维持药物在S-SEDDS中的过饱和溶解状态。结论所制备的水飞蓟宾过饱和自微乳处方达到了设计要求,为新制剂开发奠定了基础。Objective To prepare the supersaturation self-emulsifying drug delivery system （S-SEDDS） containing silymarin and to evaluate its basic properties. Methods With the time of self-emulsifying, the consequence of color visual examination and particle size as parameters, the optimum formulations of silymarin S SEDDS were screened by solubility test, compatibility tests and pseudo ternary phase diagrams. The silymarin concentration was determined by HPLC. The in vitro dissolution characteristics of silymarin S-SEDDS were investigated with silymarin SEDDS as control. Results The optimum silymarin S-SEDDS was composed of medium chain triglycerides （MCT） 40%, Cremophor RH40 （ethoxylated hydrogenatedcastor oil） 48%, Labrasol 12%. The time of self-emulsifying was less than 3 min, the average particle diameter was 49.6 nm, the adding amount of hydroxypropyl methylcellulose （HPMC） was 50 mg/g, and the average content of silymarin was 39.3 mg/g. The in vitro dissolution test of silymarin S-SEDDS showed that the presence of a small amount of cellulosic polymer effectively sustained a metastable supersaturated state by retarding precipitation kinetics. Conclusion The designed formulation of silymarin S-SEDDS is reasonable and provides a strong foundation for further development of new preparations.

关 键 词：水飞蓟宾 过饱和自乳化给药系统(S—SEDDS) 微乳 羟丙甲纤维素(HPMC) 

分 类 号：R284.2[医药卫生—中药学] R286.02[医药卫生—中医学]