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

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 acacia to replace 50% nonionic surfactants (Tween-80).The efficiency, shape, distribution of particle size, and in vitro releasing rate were evaluated.Meanwhile, the intestinal absorption of two self-microemulsions upon berbenine hydrochloride was compared.Results: The efficiency 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 activities in vitro and in vivo.