Objective:To optimize the prescription of colon specific pellets of glycyrrhetinic acid to evaluate drug release.Methods:The pellet was prepared by extrusion-spheronization method.The prescription was optimized by fluidized bed coating techniques and the drug release was evaluated with paddle method.Results:Microcrystalline cellulose,glycyrrhetinic acid and sodium carboxymethyl cellulose are fully stirred and mixed,and then 30 ％ ethanol added as a wetting agent,glycyrrhetinic acid hormone pills prepared by extrusion spheronization.The coat solution was prepared with Eudragit S 100 as a control membrane material,adding an appropriate amount of tfiethyl citrate and talc.When the coating weight gain of 20％,the results of the release experiments show the pellets are not release at the 0.1M potassium chloride and only 20％ was released at pH6.8 phosphate buffer in the six hour.However,the released amount of glycyrrhetinic acid reached 80％ at pH7.4 phosphate buffer in the two hour.Conclusions:The methods used in the preparing glycyrrhetinic acid hormone pill are simple.The colon specific pellets of glycyrrhetinic acid does not release in simulated gastric fluid,slowly release in simulated small intestine fluid,well release in simulated colon fluid.The study shows the colon specific pellets of glycyrrhetinic acid using the method has good colon targeting.%目的:确定甘草次酸结肠靶向微丸的制剂处方,评价其释药特性.方法:采用挤出-滚圆法制备甘草次酸素丸,利用流化床包衣技术对甘草次酸素丸进行包衣,用浆法评价微丸的体外释药性能.结果:采用微晶纤维素和甘草次酸,同时加入黏合剂羧甲基纤维素钠,经过充分搅拌混合,以30％的乙醇作为润湿剂,通过挤出-滚圆制得甘草次酸素丸.以尤特奇S100为膜控材料,加入适量柠檬酸三乙酯与滑石粉配制包衣液,对甘草次酸素丸进行包衣,制得甘草次酸包衣微丸.释放度实验表明甘草次酸素丸在其增重20％时,在0.1 moL/L的盐酸溶液中不释放,在pH6.8的磷酸缓冲液条件下6h内其释放率不到20％.而在pH7.4的磷酸缓冲液条件下2h内释放率达到80％以上.结论:所制的甘草次酸素丸处方合理,制剂工艺简便,通过流化床包衣技术所制的甘草次酸包衣微丸在模拟的胃液中不释放,在小肠液中释放缓慢,在结肠液中释药良好,具有良好的结肠靶向作用.
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