文献类型：期刊文献

中文题名：盐酸小檗碱微囊的制备及其体外释放研究

英文题名：Preparation of Berberine Hydrochloride Microcapsules and Its in vitro Release Behavior

作者：余琰[1];范凌云[1];高建德[1];魏舒畅[1];马立新[2]

第一作者：余琰

机构：[1]甘肃中医学院;[2]兰州佛慈制药股份有限公司

第一机构：甘肃中医药大学

年份：2015

卷号：26

期号：1

起止页码：109

中文期刊名：中国药房

外文期刊名：China Pharmacy

收录：CSTPCD;;北大核心:【北大核心2014】；

语种：中文

中文关键词：盐酸小檗碱;微囊;释药率;正交设计试验;制备

外文关键词：Berberine hydrochloride; Microcapsules; Release rate; Orthogonal test; Preparation

摘要：目的：为改善口感、减小对胃黏膜的刺激,制备盐酸小檗碱微囊,并考察其体外释药特性。方法：以阿拉伯胶、明胶为囊材,采用复凝聚法制备盐酸小檗碱微囊,以包封率、载药量、外形为指标,采用正交设计试验对囊心（盐酸小檗碱）-囊材质量比、囊材质量分数、搅拌速度进行优化,并进行验证。考察所制制剂的粒径分布及在人工肠液中5 h内的体外释药率。结果：最优处方为囊心-囊材质量比为1∶3,阿拉伯胶和明胶的质量分数均为2.50%,搅拌速度为200 r/min,成囊温度为53℃。所制盐酸小檗碱微囊的包封率为38%,载药量为41.71%;微囊圆整光滑,无粘连,粒径均匀,外形评分50.6;80%以上分布在3-9μm;3 h的累积释药率即达90%。结论：成功制得盐酸小檗碱微囊。
OBJECTIVE： To prepare Berberine hydrochloride microcapsules, and to investigate in vitro release behavior of it in order to improve taste and decrease gastric mucosa irritation. METHODS： Berberine hydrochloride microcapsules were prepared by complex agglutination method using gum acacia and gelatin as capsule wall material. Using encapsulation efficiency, drug-loading amount and appearance as index, mass ratio of capsule core （berberine hydrochloride）-capsule wall material, the mass fraction of capsule wall material and mixing speed were optimized by orthogonal test, and it was validated. The particle size and in vitro re- lease rate in 5 h of the preparation in simulated intestinal fluid were investigated. RESULTS： The optimal formulation was as fol- lows： mass ratio of capsule core-capsule wall material was 1：3; the mass fraction of gelatin and arabic gum were both 2.50% ; the stirring speed was 200 r/min; the temperature of forming microcapsules was at 53 ℃. The encapsulation efficiency, drug-loading amount and appearance scores of Berberine hydrochloride microcapsules were 38%, 41.71% , 50.6. The microcapsules were smooth round in shape without adhesions; particle size were distributed regularly, and more than 80% of them were space within the range of 3-9 μm; 3 h accumulative release rate reached 90%. CONCLUSIONS： Berberine hydrochloride microcapsules is prepared successfully.