5-氨基水杨酸结肠定位微丸丸芯的制备

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

[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一定范围内;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]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。

[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 ethanol was helpful in improving the hardness and friability of cores and in decreasing the time of dissolution. The weight ratio of solid powder to water should be kept around 1.6 to guarantee the process of extrusion. [Conclusion] With the prescription and parameters of this study, the produced cores are smooth, hard and round enough to be coated in the following step.