【摘要】 目的:采用星点设计-效应面法优化盐酸美金刚微丸的缓释包衣处方。方法:以苏丽丝缓释包衣液中致孔剂的比例（A）和包衣增重（B）为考察因素,以药物在2、4、8、16 h的累积释放度为考察指标,进行多元线性回归和二次、三次多项式回归,建立指标与因素之间的函数关系,并绘制效应面和等高线图,等高线图重合区即为最佳处方区域,在此区域内选取一点验证,并计算自制药和原研药的f₂相似因子。结果:星点设计-效应面法确定自变量的最优区域为致孔剂比例14.0%¹8.0%,包衣增重4.5%⁷.7%。结论:星点设计-效应面法优化盐酸美金刚缓释微丸包衣处方具有良好的预测性。自研制剂与原研药体外释放行为相似（f2>50）。更多还原

【Abstract】 Objective: The experiment aims is to optimize the coating formulation of memantine hydrochloride sustained-release pellets by central composite design-response surface methodology(CCD-RSM).Methods: The ratio of pore former(A) and coating level(B) were selected as independent variables, and the in vitro accumulated releases from the pellets at 2, 4, 8 and 16 h were regarded as dependable variables. Multilinear, two and three order quadratic models were applied to estimate the relationship between the independent and dependent variables and the two order quadratic model fitted best. The optimal formulations were selected from the overlaps of contour plots. Finally the optimal formulation was verified and f2 value was calculated to investigate the similarity of self-made product and Namenda XR 誖. Results: According to the CCD-RSM, the optimum values at the pore former level and coating level ranged from14.0% to 18.0% and 4.5% to 7.7%, respectively. In p H 1.2 hydrochloric acid buffer, the f2 factor of selfmade product and Namenda XRwas higher than 50 which showed the self-made product had similar dissolution behavior as the brand-name drug. Conclusion: The model developed by CCD-RSM can be used for formulation optimization of memantine hydrochloride sustained-release pellets with good predictive accuracy. According to the in vitro release behaviors, the self-made product is similar to the brand-name drug.更多还原