盐酸小檗碱自组装小珠载药系统的制备与体外评价  

Preparation and in vitro evaluation of self-assembled beads drug delivery system of berberine hydrochloride

作　　者：刘川[1] 许岩[1] 欧阳辉[1] 易涛[2] 

机构地区：[1]西南大学药学院,重庆400715 [2]澳门科技大学中药质量研究国家重点实验室,澳门药物及健康应用研究院,中国澳门000853

出　　处：《中国中药杂志》2013年第12期1924-1928,共5页China Journal of Chinese Materia Medica

基　　金：澳门科学技术发展基金项目(051/2012/A)

摘　　要：该文主要研究一种使用α-环糊精和大豆油在室温下连续振荡即可制得的自组装小珠给药系统,在制备过程中不需要使用任何表面活性剂或有机溶剂。以盐酸小檗碱为模型药物,对制备的小珠进行形态、结构、载药量、体外释药行为考察。药物的负载方法为制备之前溶解于大豆油中,小珠粒径为(2.25±0.23)mm,载药量为(67.02±0.64)μg.g-1。荧光标记后激光共聚焦显微镜观察显示,小珠为核壳结构,水难溶性药物主要分布在大豆油内核中。小珠在模拟肠液中的释药速率和累积释药量均显著高于原料药。这表明小珠是一种适用于水难溶性中药的有发展潜力的脂质新剂型。The purpose of the present work was to investigate the innovative self-assembling system, ＂ beads＂, prepared by continuously shaking α-eyclodextrin and soybean oil without the use of organic solvents and surfactants at room temperature. Berberine hydrochloride previously dissolved in soybean oil was chosen as a model drug to explore the shape, structure, drug loading and in vitro release of beads. The particle size and drug loading of berberine hydrochloride-loaded beads were （ 2. 25 ± 0. 23 ） mm and （ 67. 02 ± 0. 64） μg . g-1, respectively. Confocal microscopy showed that the core-shell structure of beads could contain poorly water soluble drugs or lipophilic drugs in the lipid core. The drug release rate and cumulative releases of beads were both higher than those of raw medicine of berberine hydrochloride in simulated intestinal fluid. These results suggested that beads were the novel and potential lipid- based drug delivery system for lipophilie or poorly water soluble traditional Chinese medicine.

关 键 词：小珠 Α-环糊精 大豆油 盐酸小檗碱 自组装给药系统 脂质制剂 

分 类 号：R283[医药卫生—中药学]