水飞蓟素自微乳的研制  

Silymarin self-microemulsifying drug delivery systems (SMEDDS)

作　　者：刘琳婕[1] 逄秀娟[1] 张伟[1] 高雪峰[1] 段江瑛[1] 王思玲[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2007年第9期532-536,共5页Journal of Shenyang Pharmaceutical University

摘　　要：目的筛选水飞蓟素自微乳的处方并对其体外溶出及稳定性进行考察。方法通过溶解度实验、正交设计及伪三元相图的建立,筛选水飞蓟素自微乳的组成。采用HPLC法测定处方中的药物含量,并对照市售制剂考察其溶出度及稳定性。结果水飞蓟素自微乳化系统的组成为水飞蓟素、油酸乙酯、聚氧乙烯氢化蓖麻油(Cremophor EL)和乙二醇单乙基醚(transcutol)的质量比为0.07∶0.45∶0.45∶0.1;自微乳的平均粒径为72.1 nm;于4种溶出介质中均完全溶出,且溶出曲线明显高于市售制剂;强光照射(4 500 lx)、高温(60℃)及高低温循环实验(40℃和4℃)结果表明,该自微乳性状、含量均无明显变化。结论水飞蓟素自微乳粒径小,溶出度及稳定性良好。Objective To design the formulation for silymarin self-emulsifying microemulsion and evaluate its dissolution and stability. Methods The formulation was established through solubility experiments, orthogonal design and pseudo- ternary phase diagrams. The dissolution and stability were evaluated by HPLC assay. Results The optimal formulation was composed of silymarin, ethyl oleate, Cremophor EL and transcutol, with the ratio of 0.07：0.45：0.45：0.1. The average particle size was 72.1 nm.Silymarin from SMEDDS was completely and rapidly dissolved in four different buffer media and obtained a higher dissolution profile compared with commerdal preparations. The appearance and average silybin content of SM-SMEDDS were of no significant changes after 10 days of iUumination（4500 lx）, high temperature （60℃） and temperature cycling tests（40℃, 4℃）. Conclusions The acquired microemulsion is stable, with small particle size and good dissolution.

关 键 词：水飞蓟素 自微乳 假三元相图 溶出度 稳定性 

分 类 号：R94[医药卫生—药剂学]