5-氨基水杨酸结肠定位微丸丸芯的制备

【目的]制备治疗炎症性肠病的5-氨基水杨酸双层包衣微丸的丸芯。【方法】采用挤出-滚圆技术制备丸芯，考察丸芯的最大载药量；考察崩解剂（CMS—Na）对药物溶出速度的影响，考察润湿剂（不同浓度乙醇）对丸芯硬度、药物溶出速度和丸芯脆碎度的影响。【结果]平衡对工艺有利；滚圆载量和滚圆时间需要控制在-定范围内；最大载药量为75％（w／w）；崩解剂在处方中的最大含量为4％（w／w），崩解剂含量越高，药物溶出速度越快；乙醇浓度越高，丸芯硬度越低，药物溶出速度越快，物料／润湿剂中水（质量比）需要在维持在1．6左右，才能使挤出工艺顺利进行；乙醇浓度越高，丸芯脆碎度越大。结论1应用本实验中确定的处方和工艺参数制备出的丸芯表面光滑、坚硬，圆整度良好，能够进行下一步的流化床包衣。

Preparation of the core with 5-Aminosalicylic acid in pellet of colon-specific delivery system

Objective] To prepare the cores in pellets for colon inflammatory disease with 5-aminosalicylic acid.Methods] The maximum drug load of the pellet cores was studied.The effect of CMS-Na on the speed of dissolution was observed,and the effects of ethanol on hardness,the speed of dissolution and the friability of the cores were also observed.Results] The maximum drug load of the pellet was 75%(w/w).The maximum of CMS-Na was 4%(w/w) and the more the CMS-Na was contained the fast the dissolution was.Increased...