6-巯基嘌呤结肠黏附缓释微丸的处方筛选及体外释放的研究

Preparation and in vitro release of colon adhesive sustained release pellets of 6-mercaptopurine

目的:制备6-巯基嘌呤结肠黏附缓释微丸,并对释药特性进行研究。方法:以羟丙甲基纤维素K4M和卡波姆为黏附性骨架材料,乳糖为赋形剂。采用湿法制粒包衣锅滚圆法制备载药微丸,并进行Eud-ragit S100包衣。采用正交试验设计进行处方筛选,确定生物黏附材料HPMC、卡波姆的用量及配比与制剂体外释放度的关系。结果:所得微丸的制备工艺简单,微丸大小均匀,能达到缓释12 h的试验设计要求。结论:HPMC、卡波姆的用量及配比对释药速率均有较大影响。优选处方微丸的释药特性符合设计要求。

Objective ：To prepare colon adhesive sustained release pellets of 6-mercaptopurine（6-MP） and investigate in vitro release characters of the pellets. Methods： HPMC K4M and Carbomer were used as the skeleton materials and lactose as excipients. The pellets were prepared by wet granulation and coated pot spheronization,and coated with isolating layer. Orthogonal design was employed to establish the relation between the ratio of HPMC to carbomer and the dissolution rate in vitro. Results：Prepared pellets remained the slow release for 12 h. The preparation was simple. The diameters of pellets were uniformity. Conclusion： The match-ratio of HPMC to carbomer has great effect on the dissolution rate in vitro. The optimized pellets comply with the design requirements.