多孔利福平/聚乳酸-羟基乙酸共聚物微球的制备及其性质研究  

Study on the preparation and characterization of porous rifampicin-loaded poly( lactic-co-glycolic acid) microspheres

作　　者：钦富华[1] 蔡雁 赵黛坚[1] 

机构地区：[1]浙江医药高等专科学校,浙江宁波315100 [2]宁波市第九医院,浙江宁波315020

出　　处：《广东药学院学报》2014年第6期675-678,共4页Academic Journal of Guangdong College of Pharmacy

基　　金：浙江省教育厅科研项目(Y201226177)

摘　　要：目的制备多孔利福平/聚乳酸-羟基乙酸共聚物（PLGA）微球,并考察其理化特性和体外释放行为。方法以PLGA为载体,NH4HCO3为致孔剂,改良乳化溶剂扩散法制备多孔利福平微球,扫描电镜观察微球的形态,测定微球的空气动力学直径,HPLC法测定微球的载药量和包封率,并考察微球的体外释放行为。结果多孔利福平/PLGA微球为多孔状,粒径和孔道大小随NH4HCO3的量的增加而相应增大,空气动力学直径在1~5μm范围内,载药量和包封率分别约为5%和60%,体外累积释放率24 h可达60%左右。结论多孔微球具有适宜的吸入特性,或可成为递送利福平的新载体。Objective To prepare the porous rifampicin-loaded poly（ lactic-co-glycolic acid）（ PLGA）microspheres and investigate the physicochemical characteristics and drug release in vitro of the microspheres. Methods Porous microparticles were prepared from PLGA by modified emulsion solventextraction method with ammonium bicarbonate as the porogen. The morphology of the microspheres was examined by scanning electron microscope and the mass median aerodynamic diameter were calculated.Drug loading and encapsulation efficiency were determined by high performance liquid chromatography and the in vitro release behavior of microspheres were investigated. Results Microspheres were porous,and the particle size and pore size increased as the porogen concentration increased. The aerodynamic diameter was within 1-5 μm. The drug loading and encapsulation efficiency in the porous PLGA microparticles were about 5% and 60%,respectively,and the in vitro drug release from porous microspheres was faster than that from non-porous microspheres,approximately 60% in 24 h. Conclusion Porous PLGA microspheres were suitable for inhalation,they could be a new drug carrier for rifampicin.

关 键 词：利福平 聚乳酸-羟基乙酸共聚物 多孔微球 理化特性 体外释放 

分 类 号：R943[医药卫生—药剂学]