复方去甲斑蝥素片胃内滞留漂浮型缓释系统研究  

Research on stomach remaining-floating sustained-release preparation of compound demethylcantharidin

作　　者：王艳萍[1] 刘福强[1] 汤真[1] 赵楠[1] 刘莹[2] 崔海珍[2] 

机构地区：[1]中国人民解放军第208医院,吉林长春130062 [2]延边大学药学院,吉林延吉133000

出　　处：《中成药》2009年第8期1190-1194,共5页Chinese Traditional Patent Medicine

摘　　要：目的:将复方去甲斑蝥素片(含黄芪和白及)制成胃内滞留漂浮型缓释制剂。方法:将黄芪和白及制成超细粉末,选择亲水性凝胶制成胃内滞留漂浮片。结果:复方中药胃内滞留漂浮型缓释片在人工胃液中3min起漂,持续漂浮8h以上。通过同位素示踪法考察胃内漂浮,普通片饱腹和空腹1h内全部崩解,漂浮片空腹滞留2～3h,饱腹可滞留4～5h。采用药典法测释放度,5h释放50%,8h释放70%。药动学试验t1/2为5.1h(普通片为2.4h),MRT为8.3h(普通片为3.3h),相对生物利用度提高了230.71%。结论:对复方去甲斑蝥素片的药材作预处理,优选辅料和改进工艺,可制备胃漂浮片。AIM： To make compound demethycantharidin （including Radix astragali and Rhizoma bletillae） in- to stomach remaining-floating sustained-release preparation. METHODS： Radix astragal and Rhizoma betillae pulverized to superfine powders were combined with hydrophilic gel to manufacture stomach remaining-floating sustained-release tablet（floating tablet）. RESULTS： The tablet started to drift in 3 min in the artificial gastric juice and float lasted for more than 8 h. By isotopic tracering, the floating tablets given on an empty stomach were retarded for 2-3 h and on large meal for 4-5 h in combination with ordinary tablet only retarded for 1 h. A pharmacopoeia dissolution method was set up to determine the release. 50% of tablets were disintegration in 5 h, 70% in 8 h. The t1/2 was 5.1 h（2-4 h for ordinary tablets）, and the MRT was 8.3 h（3.3 h for ordinary tablets）, and the remaining-floating sustained-release tablets showed a relative bioavailability of 230.71%. CONCLUSION： Pretreatment of raw herbs from compound demethylcantharidin and selection of the excipients will help to produce the herb-containing floating tablet.

关 键 词：去甲斑蝥素片 胃内漂浮片 亲水凝胶 中药材预处理 辅料 

分 类 号：R944[医药卫生—药剂学]