D-最优混料设计优化阿莫罗芬自乳化基质乳膏及乳膏流变学研究

目的通过D-最优混料设计优化阿莫罗芬自乳化基质乳膏的处方,并对其流变性、过敏性和稳定性进行研究。方法以Tefose 63、液体石蜡、Labrafil M 1944CS、Carbomer 980用量为因素,以黏度、性状、平均粒径为指标,选用数学模型描述指标和因素之间的数学关系,以设定适宜的黏度,良好的外观和最小的平均粒径为目标值,预测最优处方;并对最优处方进行流变性、过敏性和稳定性研究。结果由最佳回归模型可知5个因素和3个指标之间存在较好的定量关系,4个验证处方的实验值与预测值无显著差异。阿莫罗芬自乳化基质乳膏无过敏性,属于假塑性流体,具有剪切变稀和温度变稀的特点。结论 D-最优混料设计可用于阿莫罗芬乳膏处方的优化,建立的数学模型具有准确的预测性,采用自乳化基质制备的乳膏非常稳定。

Optimization of amorolfine self-emulsifying base cream by D-optimal mixture design and its rheology

Objective To optimize the formulation of amorolfine self-emulsifying-base cream using D-optimal mixture design,and to study the rheology,hypersensitivity and stability of the cream.Methods Independent variables were amounts of Tefose 63,liquid paraffin,Labrafil M 1944CS,Carbomer 980and water,while viscosity,appearance and mean particle size were dependent variables.Optimal mathematical models were chosen to estimate the relationship be-tween the dependent and the independent variables.With appointed viscosity,appearance and average particle size as target values,overlay plot was used to predict the optimal formulation.Validation of optimal formulation was verified at last.The rheology,hypersensitivity and stability test of the cream were studied.Results In optimal regression models,there was reliable quantitative relationship between 5factors and 3evaluation indexes.The test of 4optimal check point formulations indicated that high approximation existed between their predicted and experimental values.The cream was very stable,had no hypersensitive effect on the skin of guinea pigs,and was pseudo-plastic fluid with shear thinning and temperature thinning behaviors.Conclusion D-optimal mixture experimental design facilitates the optimization of amorolfine self-emulsifying-base cream formulation.Optimal models prove high prognostic and feasible.The cream is very stable with self-emulsifying-base.