超顺磁性异烟肼聚乙二醇-聚乳酸共聚物微球制备工艺及体外药物释放研究  

Study on the preparation and in vitro release characteristics of super paramagnetic isoniazid sulfate-loaded PELA microsphere

作　　者：周恒[1] 黄华[1] 罗聪[2] 康权[2] 

机构地区：[1]重庆医科大学药学院药剂教研室,重庆400016 [2]重庆医科大学附属儿童医院骨科实验室,重庆400014

出　　处：《重庆医科大学学报》2010年第7期1032-1037,共6页Journal of Chongqing Medical University

基　　金：国家自然科学基金(编号:30973062);中国博士后科学基金(编号:20080430754);重庆市卫生局重点课题(编号:渝卫科教[2007]1号)

摘　　要：目的:制备超顺磁性异烟肼聚乙二醇-聚乳酸共聚物(Poly(ethylene glycol)-co-poly(d,l-lactide),PELA)微球(SPI-PELA-MS),优化其制备工艺,考察其在振荡磁场影响下的体外释放。方法:用化学共沉淀法合成超顺磁性Fe3O4纳米粒,用复乳溶剂蒸发法制备SPI-PELA-MS。考察均质机转速、内水相与油相体积比、PELA浓度等不同因素对微球的影响,通过正交实验优化制备工艺,并对其粒径分布、形态、和体外释放性质进行了研究。结果:SPI-PELA-MS最优工艺处方为:均质机转速13000r/min、内水相与油相比1∶20、内水相中药物水溶液体积与磁流体体积比1∶2、PELA浓度40mg/ml、超声功率600W、PVA浓度1.5%。在体外释放中,通过外加振荡磁场的影响,能显著提高SPI-PELA-MS中药物的释放。结论:采用复乳溶剂蒸发法可成功制备SPI-PELA-MS,体外释放表明药物具有缓释功能,振荡磁场可以增加体系中药物的释放。Objective：To prepare super paramagnetic SPI-loaded PELA microsphere,study its release characteristics in vitro with the effect of oscillating magnetic fields.Methods：The nanospheres of super paramagnetic were prepared by chemical coprecipitation and then the super paramagnetic SPI-loaded PELA microspheres were prepared by double-emulsion/solvent evaporation method.Some factors affecting preparation technic,such as concentration of PVA,PELA concentration,speed of viscolizer and so on were studied.In addition, the drug release of super paramagnetic SPI-loaded PELA microsphere with the effect of oscillating magnetic fields was studied.Results： Factors for the optimal preparation technic included：speed of viscolizer of 13 000 r/min,inter water phase/oil phase of 1/20,volume ratio of water and magnetic fluid in inter water phase of 1/2,PELA concentration of 40 mg/ml,ultrasonic efficiency of 600 W,concentration of PVA of 1.5%.Oscillating magnetic field could improve the speed of drug release.Conclusion：Super paramagnetic SPI-loaded PELA microsphere were successfully prepared according to double-emulsion/solvent evaporation method.SPI-PELA-MS had the characteristics of sustained-release.The oscillating magnetic fields could promote drug release of SPI-PELA-MS.

关 键 词：异烟肼 PELA 超顺磁性微球 振荡磁场 

分 类 号：R943[医药卫生—药剂学]