中心复合设计法优化盐酸伪麻黄碱缓释微丸包衣液处方

目的:采用Eudragit RS30D对盐酸伪麻黄碱微丸进行缓释包衣,优化包衣液处方。方法:通过单因素考察,确定影响药物释放的主要因素,以综合评分值(Y)为评价指标,采用中心复合设计试验对包衣液处方进行优化,确立处方组成,并在优化区域内选择一点安排一次验证试验,以检验优化工艺条件的有效性。结果:理论包衣增重(X1)和抗黏剂滑石粉用量(X2)是影响药物释放的主要因素,其中理论包衣增重(X1)对评价指标有非常显著影响(P<0.01),拟合所得多元二次方程为Y=576.2-17.88X1-4.244X2 0.1449X12 0.06391X1X2 0.01080X22,r=0.9775。验证试验表明,本优化方程有良好的预测性。结论:中心复合设计法优化的制备条件良好,制得的盐酸伪麻黄碱缓释微丸的体外累积释放度符合要求。

Optimization of coating solution formulation of pseudoephedrine hydrochloride sustained-release pellets by a central composite design

Objective:To optimize coating solution formulation using Eudragit RS30D and prepare pseudoephedrine hydrochloride sustained-release pellets.Methods:The formulation was developed based on a single-factor test,which was carried out to screen the critical influencing factors for the release rate.The optimal formulations were obtained by a central composite design.Results:The theoretical increment in coating weight(X1) and the anti-adhesive agent talc(X2) were the main factors which influenced the release rate.Among the two materials,the theoretical increment in coating weight(X1) affected the release rate more dramatically(P<0.01).The correlation equation was Y=576.2-17.88X1-4.244X2 0.144 9X21 0.063 91X1X2 0.010 80X22 and the correlation coefficient was 0.977 5.Validation results showed that this equation was capable of prediction for optimization of the formulation.Conclusion:The central composite design was able to optimize the coating solution formulation of pseudoephedrine hydrochloride sustained-release pellets.