替莫唑胺壳聚糖缓释微球的制备及体外释药特性  

Study on preparation and drug release in vitro of temozolomide-chitosan microspheres

作　　者：陈健[1] 黄书岚[1] 何文[1] 代文兵[1] 马金阳[1] 

机构地区：[1]武汉大学人民医院,湖北武汉430060

出　　处：《中国医院药学杂志》2005年第12期1115-1118,共4页Chinese Journal of Hospital Pharmacy

基　　金：湖北省科技攻关项目(批号:2001AA307B);湖北省卫生厅科研基金项目(批号:WJ01563)

摘　　要：目的:制备替莫唑胺壳聚糖缓释微球,并对其体外释药模式进行研究.方法:以替莫唑胺为模型药物,采用乳化交联法制备壳聚糖微球,两步优化法优化处方和制备工艺.通过测定微球的粒径及其分布、载药量、包封率和体外释放速度对微球进行质量评价.结果:优化工艺制得的微球平均粒径为(3.9±1.6)μm,载药量为(7.1±0.5)%(n=3),包封率为(25.0±0.8)%(n=3),体外释药特性研究具有良好的缓释特性,在0～8 h符合Higuchi方程,Q=11.717+26.951t1/2(r=0.980),8～24 h符合一级释放曲线,lnQ=4.37+0.007 5t(r=0.983).结论:通过优化处方和制备工艺,采用乳化交联法可制备出以壳聚糖为载体、替莫唑胺为模型药物的缓释微球,其体外释药具有明显的缓释作用.OBJECTIVE To prepare temozolomide-chItosan microspheres and to study the drug release behavior in vitro. METHODS Using temozolomide as the model drug, Temozolomide-chitosan micropheres were prepared by emulsion-chemical crosslinking technique and two-stage optimization. Chitosan mierospheres were subjected to measurement of morphology, mean size（MS） and distribution, entrapment efficiency （EE%）, pay loading （PL%） and drug release rate in vitro. RESULTS The optimized microspheres had a spherical shape. The MS was （3. 9 ± 1.6） μm. The PL was （7. 1 ± 0. 5） % （n = 3）. The EE was （25.0 ± 0. 8） % （n = 3）. The drug release in vitro profile could be described by Higuehi equation Q= 11. 717 ± 26. 951t^1/2 （r= 0. 980）（0-8 h） and first order kinetics equation lnQ= 4. 37 ± 0. 007 5t（r= 0. 983）（8-24 h）. CONCLUSION Temozolomide-ehitosan mieropheres with sustained release property could be achieved by emulsion-chemical erosslinking technique and two-stage optimization.

关 键 词：替莫唑胺 壳聚糖 微球 体外释药 

分 类 号：R944.9[医药卫生—药剂学]