盐酸小檗碱胃漂浮片的研制

Preparation of gastroretentive floating tablets of berberine hydrochloride

为筛选盐酸小檗碱胃漂浮片的处方并评价其漂浮和体外释放特性,根据辅料性质及制剂质量要求,通过单因素实验及正交试验确定影响盐酸小檗碱胃漂浮片性能的主要参数,确定了最优处方。采用干粉直接压片制得盐酸小檗碱胃漂浮片,在人工胃液中考察其漂浮性能及溶出度,并用紫外可见分光光度法检测其释药量。优选的处方为每片含HPMC(K15M)35 mg,碳酸氢钠20 mg,羧甲基淀粉钠47 mg,聚乙二醇6000(PEG6000)为15 mg。该处方研制的盐酸小檗碱胃漂浮片起漂时间小于1 min,持漂时间大于12 h,12 h的累积释药量大于80%。结果表明,研制的盐酸小檗碱胃漂浮片具有良好的漂浮特性和释药性能,且制作工艺简单。

Our aim is to optimize the formula of gastroretentive floating tablets of berberine hydrochloride and to evaluate its buoyant and drug release characteristics in vitro.In accordance to the nature of adjuvant and the quality of preparation and by using the single factor experiments to determine the main parameters which impact the properties of the gastroretentive floating tablets of berberine hydrochloride,the optimum prescription and experimental conditions were determined.Tablets were prepared by direct compression with dry powder.The floating properties in the artificial gastric juice was studied and the UV-visible spectrophotometry was used to detect the release volume of the gastroretentive floating tablets of berberine hydrochloride.Results show that the optimum prescription includs HPMC（K15M） 35 mg,NaHCO3 20 mg,CMS-Na 47 mg and PEG6000 15 mg.The tablet begins to float in 1 min,and the floating time is over 12 h.The total drug release in vitro in 12 h is more than 80 percent.The prepared tablets have good behavior of floating and release characteristics,and the preparation is simple.