实验设计在自微乳化给药系统处方优化中的应用

Application of Design of Experiment in Formulation Optimization of Self-microemulsifying Drug Delivery System

自微乳化给药系统(SMEDDS)是提高难溶性药物溶解度和生物利用度的有效方法之一。处方筛选以及优化是开发该类制剂的关键。实验设计(DoE)可以评估自变量及其相互作用对因变量的主要影响,因而被广泛应用于处方优化。文章主要概述了几种实验设计方法的原理、优缺点及其在SMEDDS处方优化中的应用,着重介绍了D-最优混合物设计,以期为SMEDDS的处方优化方法选择提供参考。

Self-microemulsifying drug delivery system(SMEDDS)is one of the effective approaches to improve the solubility and bioavailability of poorly soluble drugs.The formulation screening and optimization is the key steps in the development of SMEDDS products.Design of experiment(DoE)methods are employed to evaluate the main effects of independent variables and their interactions on response variables in formulations,therefore they are widely used in formulation optimization.This review summarizes the principles,advantages and disadvantages of several experimental design methods and their application in SMEDDS products development,focusing on the D-optimal mixtures design,in order to provide some references for the selection of SMEDDS formulation optimization methods.