摘要
目的:通过星点设计-效应面法优化香青兰黄酮缓释片处方并探讨释药机制。方法:以HPMC的用量和乳糖/淀粉(1∶1)的用量为考察因素,以2,6,12 h的累积释放度为考察指标,分别用线性和二项式模型描述因素与考察指标之间的数学关系,根据模型绘制等高线图,通过重叠等高线图确定优化处方并进行验证实验,探讨药物释放机制。结果:优化后的处方为HPMC 50 mg,乳糖68 mg,淀粉68 mg,主药150 mg,释放模型符合Higuchi方程。结论:星点设计-效应面法优化香青兰黄酮缓释片的处方具有良好的预测性。
OBJECTVE To optimize the formulation of sustained-release preparation by the central composite design-response surface methodology. METHODS The amounts of HPMC and lactose： strarch （1 ： 1 ） as independent variables were optimized with RSM plus CCD by selecting percentages of in vitro cumulative releases at 2,6 and 12 h as dependent variables. Multi-linear and quadratic models were used to estimate the relationship between the dependent and the independent variables, and to delineate RSM and overlay contour plots in order to select the optimal formulations with the application of hypothesized in vitro cumulative release（%） at 2,6 and 12 h. RESULTS Regression coefficients of second-order models were higher than first-order model. Optimized formulation was proposed to consist of HPMC 50 mg, lactose 68 mg, starch 68 mg, remedium cardinale 150 mg. In vitro release indicated that there existed high approximation between the observed and estimated values. The release was conformed to Higuehi equation. CONCLUSION Central composite design-response surface methodology can be applied to optimize the coating formulation for Dracocephalum moldevica flavones sustained release tablets and the models are proved to be predictable.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2011年第15期1238-1241,共4页
Chinese Journal of Hospital Pharmacy
基金
国家科技重大专项课题新药创制(编号:2009ZX09103-448)
关键词
香青兰黄酮
星点设计-效应面法
HPMC缓释片
释药机制
Dracocephalum moldevica flavones
central composite design-response surface
HPMC sustained-release tab- lets
release mechanism.
