星点设计-效应面优化单凝聚法制备氟苯尼考微球

Optimization of the Preparation Technology of Florfenicol Microsphere by Simple Coacervation Based on Central Composite Design and Response Surface Methodology

关键词:  星点设计-效应面优化法  单凝聚法  微球  氟苯尼考

Key words:  central composite design and response surface methodology  simple coacervation  microspheres  florfenicol

摘要:

目的 优化单凝聚法制备氟苯尼考缓释微球工艺。方法 以单凝聚法制备微球，以粒径、包封率的总评“归一值”为评价指标，采用星点设计考察芯材比、成囊pH、搅拌速度3因素对微球制备的影响，对结果进行二项式拟合，效应面法选取最佳工艺条件，优化工艺后制得的微球在人工体液中进行体外释放。结果 最佳工艺条件为药/囊材0.375、成囊pH 4.8、搅拌速度615 r·min^-1；制得的微球圆整均一，粒径40~50 μm，包封率57.45%，载药量17.52%，制得的微球在Hank’s 人工模拟体液中有良好的缓释特征。结论 优化制备工艺条件下制得的微球外形良好，载药量较大，缓释效果好。

Abstract:

OBJECTIVE To optimize the preparation technology of florfenicol sustained release microspheres by simple coacervation method. METHODS Microspheres were prepared by simple coacervation method. The effects of influences factors such as the ratio of core to material, encysted pH and stirring speed, on overall desirability (OD) of diameter and entrapment efficiency were investigated by central composite design and response surface method. The data were imitated using second-order polynomial. Microspheres prepared by optimal condition were releasing in vitro in artificial body fluid. RESULTS The optimal conditions were as follow: the ratio of core to material as 0.375, encysted pH as 4.8, and stirring speed as 615 r·min^-1. The microspheres prepared by optimal condition were round and uniform with particle size of 40~50 μm. The entrapment efficiency was 57.45% and the drug loading reached 17.52%. The microspheres had good slow-release characteristics in Hank’s artificial body fluid. CONCLUSION Microspheres prepared by optimal method load more drug with good shape, and the slow-release characteristics are good.