星点设计-效应面法优化丹皮酚片剂处方

目的:通过星点设计-效应面法优化丹皮酚片剂处方.方法:以MCC102、乳糖复合物Cellactose80和黏合剂PVPS630的用量、片剂硬度为考察因素,以崩解时间和脆碎度为考察指标,并计算其“归一值(OD)”,分别用多元线性模型、二次多项式和三次多项式模型描述考察指标和3个考察因素之间的数学关系,绘制效应面和等高线图,确定较优处方并进行验证.结果:根据拟合模型,发现3个考察因素和考察指标之间存在可信的定量关系;优选的最佳处方为MCC102与Cellactose80的比例为1∶1,PVP S630含量为1％,优化处方各设定的预测值和测定值非常接近.结论:采用星点设计-效应面法,得到了基于二次多项式和三次多项式模型的丹皮酚片剂处方优化模型,实现了该片剂的处方优化.

Optimization of Paeonol Tablets Formulation by Central Composite Design-Response Surface Methodology

Objective:To optimize the formulation of paeonol tablets by the central composite design-response surface methodology.Method: In the formulation design using response surface methodology plus central composite design,independent variables included the amounts of MCC102,Cellactose 80,PVP S63 and the tablet hardness.Disintegration time and friability of tablets were taken as dependent variables,and overall desirability was calculated from the geometric mean of the two desirabilities of each formulation.Multilinear,quadratic and cubic models were used to estimate the relationship between the dependent and the independent variables,and to delineate response surface method and overlay contour plots in order to select the optimal formulations.Finally,predicted responses were verified.Result: The quantitative relationships between three factors and 3 evaluation indexes were characterized.Optimal formulation was proposed to contain 1% PVP S630,the proportion of MCC 102 and Cellactose 80 was 1 ∶ 1.Dissolution test of the selected optimal formulation indicated that there existed high approximation between the observed and estimated values.Conclusion: The muti-objective simultaneous optimization of paeonol tablets formulation could be achieved by the central composite design and response surface methodology.