富马酸喹硫平骨架缓释片的研发  

Development and Research of Quetiapine Fumarate Matrix Sustained- Release Tablets

作　　者：何广卫[1] 苏峰[1] 许国琴[2] 许慧雷 

机构地区：[1]合肥医工医药有限公司,安徽合肥230088 [2]安徽中医药大学,安徽合肥230031

出　　处：《广州化工》2014年第13期47-51,共5页GuangZhou Chemical Industry

基　　金：十二五国家"重大新药创制"科技重大专项项目;合肥医工医药创新药物孵化基地建设(No:2012ZX09401006)

摘　　要：以HPMC为骨架缓释材料,乳糖为填充剂,枸橼酸钠为pH调节剂,硬脂酸镁为润滑剂,采用单因素试验和正交实验设计方法,通过f2相似因子和累积释放度综合评分进行评价,最终确定富马酸喹硫平缓释片的处方组成为:富马酸喹硫平230 g,HPMC K100Lv 180 g,HPMC K4M 60 g,乳糖50 g,柠檬酸钠75 g,硬脂酸镁6 g。自研缓释片释放行为与原研制剂一致(f2≥50),且符合Higuchi模型和Ritger-Peppas方程,表明药物释放机制是扩散与溶蚀并存的双重机制。Using f2 similarity factor and comprehensive score of the cumulate release rate as response value , single factor test and orthogonal experimental design were used to determine the viscosity and dosage of HPMC as matrix materials and dosage of lactose as diluents and sodium citrate as pH regulators and magnesium stearate as lubricants .The optimal formulation （1 000 units） was quetiapine fumarate 230 g, HPMC K100Lv 180 g, HPMC K4M 60 g, lactose 50 g, sodium citrate 75 g and magnesium stearate 6 g.The dissolution profile in difference pH media was consistent with reference listed drug （ f2≥50 ） , and the sustained -release tablets in vitro release fitted to the Higuchi model and Ritger -Peppas equation , the release mechanism in vitro was diffusion combined with corrosion.

关 键 词：富马酸喹硫平 骨架缓释片 羟丙甲纤维素 F2 相似因子 累积释放度 

分 类 号：R944.9[医药卫生—药剂学]