含天然乳化剂的盐酸小檗碱自微乳的制备与体内外性能评价  

Preparation and evaluation of berbenine hydrochloride self-microemulsion containing natural emulsifier in vitro and in vivo

作　　者：黄嗣航[1] 龙晓英[1] 袁飞[1] 陈莉[1] 张妙虹[1] 蔡宝玲[1] 刘昌顺[1] 

机构地区：[1]广东药学院中药学院,广州510006

出　　处：《中国新药杂志》2012年第23期2794-2799,共6页Chinese Journal of New Drugs

基　　金：国家自然科学基金(30973953C1909)

摘　　要：目的:制备含阿拉伯胶的盐酸小檗碱自微乳,考察其体内外性能。方法:以天然乳化剂阿拉伯胶部分代替合成非离子型乳化剂聚山梨酯80制备盐酸小檗碱自微乳;评价两种自微乳的自乳化速率、微乳形态、粒径分布和释放度;采用大鼠在体单向肠灌流模型对两种自微乳的吸收动力学进行体内评价。结果:与合成乳化剂自微乳相比,天然乳化剂自微乳的自乳化速率基本相同,微乳乳滴粒径及粒径分布范围有所变大,体外释放速度略有降低,对盐酸小檗碱在大鼠在体肠吸收的促进效果更好。结论:用天然乳化剂阿拉伯胶部分代替合成乳化剂所制备的盐酸小檗碱自微乳可保持自微乳原有的体内外行为。Objective： To prepare berbenine hydrochloride self-microemulsion with acacia, and evaluate its performance in vitro and in vivo. Methods： Berbenine hydrochloride self-microemulsion was prepared by using aca- cia to replace 50% nonionic surfactants （Tween-80）. The efficiency, shape, distribution of particle size, and in vitro releasing rate were evaluated. Meanw hydrochloride was compared. Results： Th hile, e effi the intestinal absorption of two self-microemulsions upon berbenine ciency of natural emulsifier self-microemulsion （NE-SMEDDS） was almost the same as nonionic surfactants self-microemulsion （NS-SMEDDS）. NE-SMEDDS had wider particle size distribution than NS-SMEDDS, and its release rate became little slow. The absorption efficiency of NE-SMEDDS was better than NS-SMEDDS. Conclusions： Using natural emulsifier （acacia） to replace 50% nonionic surfactants can reduce the concentration of synthetic emulsifier and the toxicity effectively. Meanwhile, it can maintain the ac- tivities in vitro and in vivo.

关 键 词：盐酸小檗碱 自微乳 在体单向肠灌流法 吸收 

分 类 号：R943[医药卫生—药剂学]