吲哚美辛酶解型结肠靶向压制包衣片的研制  

Study on indomethacin compression-coated tablet for colon specific drug delivery

作　　者：曹健[1] 陆锦芳[1] 

机构地区：[1]复旦大学药学院药剂教研室,上海200032

出　　处：《中国药学杂志》2005年第5期367-370,共4页Chinese Pharmaceutical Journal

摘　　要：目的　研制用于结肠靶向的吲哚美辛瓜尔胶压制包衣片。方法　正交设计得吲哚美辛片芯的最佳处方 ,湿法制粒得到瓜尔胶压制包衣用颗粒 ,将两者压片得到压制包衣片 ,并测其体外释放度。结果　体外释药试验表明 ,压制包衣 ,使药物在0 1mol·L-1HCl和pH 7 4磷酸盐缓冲液中不释放 ,在有半乳甘露糖苷酶的pH 6 8磷酸盐缓冲液中能全部释放。结论　瓜尔胶作为压制包衣材料 ,能使药物达到结肠靶向给药效果。OBJECTIVE: To prepare indomethacin compression tablets coated with guar gum for colon-specific drug delivery. METHODS: According to disintegration test results, indomethacin core tablets were designed by orthogonal methods and a guar gmn/microcrystalline celulose mixture as the coat layer was used with wet granulation technique. The release properties of indomethacin from compression coated tablets were investigated in the physiological environment of stomach and small intestine. RESULTS: Drug release was influenced while varying the grade of guar gum and the ratio of guar gum and microcrystalline cellulose. No drug release was observed in 0.1 mol &middot L-1 HCI and pH 7.4 phosphate buffer solution(PBS). The coat would erode/degrade with the presence of enzyme (galactomannanase), and drug delivered completely to the colon (pH 6.8 PBS). CONCLUSION: The study clearly established that guar gum, in the form of compression coat, is a potential carrier for drug targeting to colon.

关 键 词：吲哚美辛 瓜尔胶 多糖 压制包衣 结肠靶向 

分 类 号：R94[医药卫生—药剂学]