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1. 上海科兴药业公司
2. 中国科学院上海原子核研究所,上海,201800
3. 中国科学院上海原子核研究所上海,201800
纸质出版日期:2002-11-01
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[1]闵小锋,须剑鹰,崔海燕,张炯,周伟,陈敏峰,尹端沚.~(188)Re-HEDP注射液药物代谢动力学研究[J].核技术,2002(11):957-960.
MIN Xiaofeng 1 XU Jianying 1 CUI Haiyan 1, 2 ZHANG Jiong 1, 2 ZHOU Wei 1, et al. Study on pharmacodynamics of188Re-HEDP injection[J]. Nuclear techniques, 2002, (11): 957-960.
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.
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