^(188)Re-HEDP注射液药物代谢动力学研究  

Study on pharmacodynamics of^(188)Re-HEDP injection

作　　者：闵小锋 须剑鹰 崔海燕[1] 张炯 周伟 陈敏峰 尹端沚[2] 

机构地区：[1]上海科兴药业公司,上海201800 [2]中国科学院上海原子核研究所,上海201800

出　　处：《核技术》2002年第11期957-960,共4页Nuclear Techniques

摘　　要：将药物静脉注射到动物体内 ,以观察188Re -HEDP注射液在动物体内代谢动力学的特征。结果表明 ,滞留在荷瘤大鼠患骨中的放射性比在正常骨中的多 (P <0 .0 5 ) ;小鼠 72h内排泄放射性累积百分率约为 82 %(其中尿液排泄为 80 %) ;体外血浆蛋白结合率为 86 .4 %± 0 .30 %。说明该药物是亲骨药物 ,血清除快符合药物代谢动力学二室模型 ,大部分的药物以原形从肾排出。188Re-HEDP was concentrated in bone after intravenous injection into the tumor- bearing rats. Biodistribution study showed that 188Re retained in bony lesions was much higher than normal bone (P<0.05). The blood clearance curve showed its pharmacodynamics of two phase models. After injection of 188Re-HEDP, most of the radioactivity was excreted by the urinary system. Within 72h the accumulative excretion rate was 82% (80% of the injected dose was found in the urine). Radiopharmaceutical study in urine excretion was mainly in the form of 188Re-HEDP. In vitro, the binding to proteins in plasma was found to be 86.4%±0.30% for 188Re-HEDP.

关 键 词：注射液 ^188RE-HEDP 药物代谢动力学 放射性治疗药物 铼188 标记 

分 类 号：R817.5[医药卫生—影像医学与核医学] R969.1[医药卫生—放射医学]