肺靶向顺铂白蛋白微球在小鼠体内分布及肺器官中药代动力学研究

The Distribution and Pharmacokinetics in Lung of Bovine Serum Albumin Microspheres for Pulmonary Targeting in Mice

用放射示踪法研究了顺铂白蛋白微球在小鼠体内分布及其在肺中的药代动力学规律。微球（７～２５μｍ）静脉注射后绝大部分被肺滤取而浓集在肺部，最高时可达注入量的９７．５２％左右，血和其它器官中的量极少。肺组织切片观察发现微球沉着在肺部毛细管及泡内肺动脉中。微球在肺内随时间延长而降解，其代谢动力学规律可用一级摄取和一级消除的一室模型进行描述。

?25I-labeled bovine serum albumin mi-crospheres loaded cisplatinum(CDDp￣-125 I-BSA-MS )with the size range of 7-25μm were prepared and in-jected into the tail vein of mice. The results showed that the microspheres were accumulated almost entire-ly in the lung after i.v. injection(about 97. 52%in-jected dose at the highest concentration ).While inblood and other organs almost no accurmulation wasfound.Photomicrographs showed that microspheresreached the lung and lodged in precapiIlary arteriolsand capillaries of lung. The microspheres、in lung wereeliminated gradually.The pharmacokinetics of micro-spheres in lung of mice was also studied with“pract-cal pharmacokinetic program-version 87”,and was fit-ted by two-compartment model with i.v,injection orone-compartment model with lst order absorption,but the meaning of some parameters changed. Basedon the analysis of the models and parameters , it wasconcluded that the pharmacokinetics of microspheresin lungs can be described by the model of“one-com-partment of first-order intake and first-order elimina-tion”。