天然膨胀性基质作为渗透泵片推动剂的适用性研究  

Applicability of a natural swelling matrix as the propellant of osmotic pump tablets

作　　者：伍丽[1,2] 李海燕[2] 殷宪振[2] 李颖[1,2] 陈建秀[1,2] 胡容峰[1] 张继稳[1,2] 

机构地区：[1]安徽中医学院,安徽合肥230038 [2]中国科学院上海药物研究所,上海201203

出　　处：《药学学报》2013年第8期1319-1324,共6页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81273453;81173556);国家科技重大专项资助项目(2012ZX09301001-001)

摘　　要：本文以聚氧乙烯(WSR-N10和WSR-303)为对比,测定源自胖大海的天然膨胀性基质(SMS)的糖组成、静态膨胀性、吸水特征与黏度。以SMS为渗透活性物质,采用水溶性药物利巴韦林和难溶性药物格列吡嗪为模型药物,分别制备单层与双层渗透泵片并进行药物释放度测定,判断SMS作为渗透泵片推动剂的可行性。结果表明:SMS主要由鼠李糖、阿拉伯糖、木糖和半乳糖组成;SMS的膨胀性强,吸水600 s时基质压制片的崩解物覆盖面积为初始值的20.1倍;具有较低的黏度,25℃时0.5%SMS水溶液的黏度为(3.66±0.03)mPa.s。以其为渗透活性物质制备的利巴韦林和格列吡嗪渗透泵片具有典型的渗透泵释药特征。研究结果表明,作为渗透泵片推动剂,天然膨胀性基质SMS具有一定的应用价值。The purpose of this study is to investigate the applicability of a natural swelling matrix derived from boat-fruited sterculia seed （SMS） as the propellant of osmotic pump tablets. The sugar components, static swelling, water uptake and viscosity of SMS were determined and compared with that of polythylene oxide （WSR-N10 and WSR-303）. Both ribavirin and glipizide were used as water-soluble and water-insoluble model drugs. Then, the monolayer osmotic pump tablets of ribavirin and the bilayer osmotic pump tablets of glipizide were prepared using SMS as the osmotically active substance and propellant. SMS was mainly composed of rhamnose, arabinose, xylose and galactose and exhibited relatively high swelling ability. The area of the disintegrated matrix tablet was 20.1 times as that at initial after swelling for 600 s. SMS swelled rapidly and was fully swelled （0.5%） in aqueous solution with relative low viscosity （3.66 ± 0.03） mPa＇s at 25 ℃. The monolayer osmotic pump tablets of ribavirin and the bilayer osmotic pump tablets of glipizide using SMS as propellant exhibited typical drug release features of osmotic pumps. In conclusion, the swelling matrix derived from boat-fruited sterculia seed, with low viscosity and high swelling, is a potential propellant in the application of osmotic pump tablets.

关 键 词：渗透泵片 胖大海 推动剂 吸水特征 膨胀性 黏度 

分 类 号：R943[医药卫生—药剂学]