摘要
按正交设计筛选了用乳化一化学交联法制备肺靶向顺铂白蛋白微球的最佳制备工艺,并对微球的质量、稳定性、体内分布、动力学特性和安全性进行了系统研究。结果:微球表面圆整,平均粒径为13.13±3.55μm,药物包裹率为21.62%,释药特性符合双相动力学方程;微球在三种条件下贮放了3个月质量稳定;静脉注入小鼠体内,15min分布达高峰,97.52%浓集于肺部,2~3d内基本清除,在肺器官中的动力学特性可用二室开放性模型描述;肺器官病理切片观察,微球对肺组织无病理性损伤。
An
optimum procedure was established by orthogonal test preparing
cisplatinum albumin microspheres(CDDP-BSA-MS)with emulsion-chemical
cross-linking.The quality,stability ,distribution in vivo,kinetic
characteristics and safety of the albumin microspheres were
studied.The results showed that the surface was regular,the mean size
was l3.13士3.55 μm,embedding ratio was 21.62%and the release
characteristics in vitro were in accord with“biphase kinetics
equatio The stability of the albumin microspheres was good after
three months storage,The microspheres accumulated almost entirely in
the lung l5 minutes after intravenous injection to mice。The total
amount in the lung was about 97%of the injected dose at the peak
concentration,Two-compartmental model can be used to describe the
regulation of the pharmacokinetics of albumin microspheres in
lung.Observation of the lung slice of mice;showed no pathological
damage。
出处
《药学学报》
CAS
CSCD
北大核心
1994年第5期380-386,共7页
Acta Pharmaceutica Sinica
基金
国家教委博士点基金
关键词
顺铂
微球
药代动力学
清蛋白
Preparation for lung targeting
Cisplatinum
Albumin
microspheres
Pharmacokine-tics