中心组合设计优化法筛选独一味分散片制备工艺

Optimization of the preparation of Lamiophlomis rotata dispersible tablets using central composite design

目的 中心组合设计法优化独一味分散片制备处方。方法 采用粉末直接压片,以分散片崩解时间、木犀草苷溶出的t80及分散片混悬后的混悬系数为考察指标,应用中心多点等距设计法及效应面优化法对独一味分散片处方进行筛选,通过对自变量各水平的多元线性回归及二项式拟合,选取较佳工艺,并进行预测分析。结果 考察指标与各因素间具有较好的相关性,优化后独一味分散片处方为12％PVPP为崩解剂、14％预胶化淀粉为溶胀剂、3％微粉硅胶为润滑剂和助流剂、45％MCC为填充剂。优化条件下制备的分散片崩解时间为20.6 s,木犀草苷溶出的t80为1.68 min,分散片混悬后的混悬系数为0.068 9。结论 中心组合设计法具有应用简便、预测性好等优点,筛选的处方可以在最适宜的范围内制备一定硬度且具有可被接受口味的速释分散片。

OBJECTIVE: To optimize the preparation of dispersible tablets using central composite design. METHODS: Dispersible tablets were prepared by direct compression method. The effects of dissolution time(t80 of luteoloside), disintegration time, suspending coefficient and overall desirability value on the PVPP, pregelatinized starch and colloidal silicium dioxide were investigated. The optimal formulation was established by the central composite design and response surface method. A second-order polynomial equation was fitted to the data and resultant model was used to predict the response in the optimal region. RESULT: All the investigated response variables were found to be highly dependent on the formulation variables. Lamiophlomis rotata dispersible tablets were prepared by selecting 12% PVPP as disintegation agent, 14% Pregelatinized Starch as sweller, 3% colloidal silicium dioxide as lubricant and clidant, and 45% MCC as filler. Under the optimized condition, the values of dissolution time (t80 of luteoloside), disintegration time and suspending coefficient were 1.68 min, 20.6 s and 0.068 9. CONCLUSION: Fast dispersible tablets with acceptable hardness and desirable taste could be prepared using central composite design.