目的 应用星点设计-效应面法优化广金钱草总黄酮(TFDS)固体分散体微孔渗透泵控释片处方。方法 以促渗剂用量、致孔剂用量、包衣增重为考察因素,2、6、12 h TFDS的累积释放度及线性相关系数为综合评价指标,采用Design-expert软件对实验数据进行多元线性模型和二次多项式模型拟合,得出最佳数学模型,绘制效应图,通过数值优化法得到最优处方并进行验证。结果 二次多项式模型优于多无线性模型,为最终拟合模型;最佳处方的各时间点累积释放度的实际值和预测值接近,相对偏差绝对值小于5%。结论 通过星点设计-效应面法建立的模型预测性良好,可用于对TFDS固体分散体微孔渗透泵控释片处方的优化。

Objective To optimize the formulations of microporosity osmotic pump controlled release tablet of solid dispersion for total flavonoids from Desmodium styracifolium (TFDS) by central composite design-response surface methodology. Methods The independent variables comprised of the amount of lactose, pore-forming agent, and coating weight gain, and the dependent variables involved the cumulative release after 2, 6, and 12 h, and the linear correlation coefficient of cumulative release curve. Design-expert software was used to fit multivariate linear models and quadratic multinomial models for experimental data. Response surface was delineated according to best-fit mathematic models and the optimum formulation was selected by Numerical Optimization. Results The correlation coefficients of quadratic multinomial models were better than those of multivariate linear models. There was close agreement between the observed and predicted values for the cumulative release, and bias were all less than 5%. Conclusion The model established by Design-expert Software is better to predict and could be used to optimize the formulations of microporosity osmotic pump controlled release tablets of solid dispersion for TFDS.