苦参碱结肠靶向微丸的制备及体外释放性能评价  

Preparation and in vitro release evaluation of matrine colon targeted pellets

作　　者：张永强 李晰 李龙飞 张松 刘新友 杨鹏 ZHANG Yong-qiang;LI Xi;LI Long-fei;ZHANG Song;LIU Xin-you;YANG Peng(Department of Pharmacy, Tangdu Hospital, Fourth Military Medical University, Shaanxi Xi'an 710038, China)

机构地区：[1]空军军医大学唐都医院药剂科,陕西西安710038

出　　处：《中国医院药学杂志》2018年第23期2416-2420,共5页Chinese Journal of Hospital Pharmacy

基　　金：国家自然科学基金(编号:81403170)

摘　　要：目的:优选苦参碱结肠靶向微丸的制备工艺。方法:采用挤出-滚圆法制备苦参碱载药丸芯,利用流化床包衣技术对苦参碱载药丸芯进行包衣,并进行体外释放度的考察。结果:苦参碱载药丸芯的优化处方工艺为:苦参碱10g,微晶纤维素40g,羧甲基纤维素钠0.5g,纯化水46mL。其包衣微丸外层衣尤特奇L30D-55增重20%,内层衣尤特奇EPO增重30%。体外释放度实验表明,苦参碱包衣微丸在模拟的胃液中基本不释放,在pH 5.0磷酸缓冲液中较快释放,在pH 6.8磷酸缓冲液中则释放缓慢。结论:苦参碱载药丸芯处方工艺简单稳定。苦参碱包衣微丸结肠靶向性较好,同时模拟实验提示在结肠pH发生明显下降时苦参碱结肠靶向微丸仍具有结肠靶向性。OBJECTIVE To optimize the prescription of colon targeted pellets of matrine.METHODS The pellet core was prepared by using extrusion-spheronization method, the prescription was optimized by fluidized bed coating techniques and the drug release was evaluated in vitro. RESULTS The pellet core was prepared by matrine 10 g, cellulose microcrystalline 40 g, CMC-Na 0.5 g and purified water 46 mL. The coat solution was prepared by Eudragit L30D-55 and Eudragit EPO. The outer layer accounted for 20% weight and inner layer for 30% weight. The results of in vitro release showed the coating pellets had no release in artificial gastric juice and delayed release in pH 5.0 phosphate buffer and slow release in pH 6.8 phosphate buffer.CONCLUSION The matrine colon targeted pellet prescription is simple and stable. The matrine colon targeted pellets have the obvious colon specific features. And the same time, the matrine colon targeted pellets have the obvious colon specific features when the colon pH is reduced.

关 键 词：苦参碱 挤出滚圆 流化床包衣 体外释放度 结肠靶向 

分 类 号：R944[医药卫生—药剂学]