星点设计法优化汉防己甲素壳聚糖微球的处方

目的:星点设计法优化汉防己甲素壳聚糖微球的处方,提高该制剂的肺靶向性。方法:采用乳化交联法制备壳聚糖微球,自变量为汉防己甲素和壳聚糖的重量比、水相和油相的体积比、壳聚糖浓度,以微球收率、载药量、包封率、平均粒径和跨距为因变量对各自变量的各水平进行多元线性回归和二项式拟合,选择较佳工艺条件并对优化区间进行预测分析。结果:收率、载药量、包封率、平均粒径和跨距用二项式模型拟合较好,最佳优化制备处方的汉防己甲素和壳聚糖的重量百分比为61·97%,水相和油相的体积比为13·51%,壳聚糖浓度为2·37%。结论:星点设计可用于优化制剂处方,所制汉防己甲素壳聚糖微球粒径大小适宜,可满足肺靶向的要求。

Optimization of Preparation Formulation of Tetrandrine Chitosa Microspheres by Central Composite Design

OBJECTIVE：The preparation of microspheres was optimized by central composite design in order to improve the lung targeting of tetrandrine chitosa microspheres. METHODS： Microspheres were prepared using an emulsion - chemical crosslink technique. Effects of three independent variables i.e. weight percent of tetrandrine and christon, volume percent of water phase and organic phase and christon concentration in aqueous phase were investigated on four response variables. Response variables selected in the research were yield, drug loading, envelop efficiency, mean diameter and span of dispersity. Second- order polynomial and linear equations were fitted to the data, and the resulting equations were used to produce three dimensional response surface graphs, by which optimal experimental conditions were selected. RESULTS：Five response variables were found to be dependent on three independent variables. According to optimal experimental conditions. An optimized formulation contained weight percent of tetrandrine and christon was 61.97%, volume percent of water phase and organic phase was 13.51% and christon concentration in aqueous phase was 2.37% . CONCLUSION：The central composite design can be used to optimazation of preparation formulation,diameter of the microspheres optimized by it can meet the demands of lung-targeting.