中心复合设计法优化盐酸普罗帕酮缓释微丸包衣液处方

Optimization of coated film formulation of propafenone hydrochloride sustained-release pellets by central composite design

目的采用Eudragit NE30D对盐酸普罗帕酮微丸包衣,制备了日服2次的盐酸普罗帕酮缓释微丸。方法通过单因素实验考察药物释放的影响因素,确立处方组成;采用中心复合设计试验对处方进行优化。结果包衣增质量和抗黏剂滑石粉用量是影响药物释放的主要因素,以综合评分值为考察指标拟合所得多元二次方程为Y=100.066 1-19.368 4X1-0.808 0X2+1.183 6X21+0.048 21X1X2+0.003 214X22,复相关系数r=0.974 7。结论中心复合设计优化处方预测性良好,制得盐酸普罗帕酮缓释微丸符合实验设计要求。

Objective To design and prepare a sustained-release pellets of propafenone hydrochloride by using Eudragit＊ NE30D. Methods The formulation was developed based on single-factor tests, which were carried out to screen the critical factors influencing the drug release. The optimal formulation was obtained by central composite design. Results The coating levels and the talc levels were the main factors, and the grading values of synthesizing were selected as the response variable. Second-order polynomial and linear equation was Y = 100.066 1 - 19. 368 4X1 - 0.8080X2 ＋ 1.1836X1^2 ＋ 0.04821X1X2 ＋ 0.003214X2^2, the regression coefficient was 0. 974 7. Conclusions Central composite design is successfully used to optimize the preparation of sustained-release pellets of propafenone hydrochloride. The pellets comply with the requirements of the experiment design.