摘要
目的制备头孢氨苄胃漂浮微丸,使药物在胃中缓慢释放,降低毒性及不良反应,延长药物在胃中的滞留时间,提高其生物利用度。方法采用挤出滚圆法制备头孢氨苄载药丸心,用Eudragit?NE-30D水分散体为控释层包衣材料,NaHCO3和HPMC E5为产气层,Eudragit?RL-30D水分散体为气体阻滞层,以流化床包衣的方法进行包衣操作制备头孢氨苄胃漂浮微丸,并考察各包衣层处方组成、包衣增重对微丸体外漂浮性质,释药特性的影响,筛选出最优处方。结果控释层材料的包衣增重对药物的释放有显著的影响,产气层的增质量以及组成和气体阻滞层增重对微丸的起漂时间和持续漂浮时间都有影响。结论所制备的头孢氨苄胃漂浮微丸,具有良好的胃漂浮特性和零级释药特征。
Objective To prepare cephalexin gastric floating pellets with the intention to release the drug slowly, reduce the toxic and side effect, prolong the gastric rensidentce time and thereby increase the bioavailability. Method The drug-loaded pellets was prepared by extrusion and spheronization method and then coated with three successive layers in a fluid bed. In particular, Eudragit? NE-30D aqueous solids was used as controlled release film, sodium bicarbonate with HPMC E5 as gas formation layer and Eudragit?RL-30D aqueous solids as gas entrapped membrane. The effects of the composition of coating layers and coating weight gain on the gastric floating characteristic and drug release profile were investigated to optimize the formulation. Results The coating weight gain of controlled release film had a significant effect on the drug release, and both the gas formation layer and the controlled release membrane had influence on the floating lag time(FLT) and floating duration. Conclusion The cephalexin gastric floating pellets were successfully prepared with a nice gastric floating characteristic and zero-oreder release profile.
出处
《中国药剂学杂志（网络版）》
2014年第4期5-16,共12页
Chinese Journal of Pharmaceutics：Online Edition
