多孔利福平 PLGA 微球的制备工艺研究

目的：以利福平为模型药物，研究多孔聚乳酸—羟基乙酸共聚物（poly（lactic-co-glycolic acid），PLGA）微球的最佳制备工艺。方法乳化溶剂扩散法制备多孔微球，采用扫描电镜观察微球形态，HPLC 法测定微球包封率。通过单因素考察实验，筛选影响微球形态和包封率的主要因素并优选条件。结果制备过程中 PLGA 种类、PLGA 浓度、致孔剂浓度、均质速度、外水相 PVA 浓度等影响微球的粒径、多孔结构和包封率。按优化工艺制备的微球平均粒径为8．6μm，密度为0．1 g·cm －3，易于吸入并提高肺部的沉积率。结论低密度多孔微球具有适宜的吸入特性和肺部沉积率，或可成为递送抗结核药物的新载体。

Preparation of porous rifampicin-loaded PLGA microspheres

Objective To study and optimize the preparation process of porous rifampicin-loaded PLGA microspheres.Methods Por-ous microparticles were prepared by double emulsion solvent-extraction method.The morphology of the microspheres was examined by scanning electron microscope and the encapsulation efficiency was determined by high performance liquid chromatography.Through sin-gle factor selecting experiment,the major factors affecting the morphology and encapsulation efficiency of microspheres were investigated and optimized.Results The particle size,porous structure and encapsulation efficiency of the microspheres were influenced by the PL-GA type,PLGA concentration,porogenic agent concentration,homogeneous velocity and PVA concentration.Microspheres prepared by optimized process had an average particle diameter of 8.6 μm,and density of 0.1g·cm -3 ,which could be easily inhaled.Conclusion Low density porous microspheres with good inhalation characteristics and higher pulmonary deposition could be a new drug delivery carrier for anti-tuberculosis drugs.