~(99)Tc~m-CQDO和~(99)Tc~m-CQDO-MeB的小鼠体内分布和药代动力学比较

  • 摘要: 以氯化亚锡为还原剂制备了99Tcm-CQDO及其甲基硼酸加成物99Tcm-CQDO-MeB,经萃取纯化,其放化纯度均>90%。小鼠体内分布表明,两者均能被小鼠心肌迅速摄取;99Tcm-CQDO的心肌清除快,10min时已清除至(5.88±1.66)%ID/g;而99Tcm-CQDO-MeB在心肌内却有较长的滞留时间,60min时心肌摄取仍有(7.42±0.17)%ID/g。两者在血中清除均符合双指数二室模型,T1/2α分别为1.38min和1.51min。pH为7.40时,99Tcm-CQDO和99Tcm-CQDO-MeB的分配系数分别为25和12

     

    Abstract: COMPARISON OF BIODISTRIBUTION IN MICE AND PHARMACOKINETICS OF 99Tcm CQDO WITH 99Tcm CQDO MeBZhu Junqing\ Luo Shineng\ Wu Chunying\ Ji ShurenCao Guoxian\ Zhou Xiang\ Chen Zhengping\ Mo Yiqing (State Key Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063) Abstract\ 99Tcm CQDO and its adduct of methaneboronic acid 99Tcm CQDO MeB are prepared by the reduction of SnCl 2·2H 2O with Na 99 Tc mO 4. The radiochemical purity of 99Tcm CQDO and 99Tcm CQDO MeB are higher than 90%\ after being purified by extration. The biodistribution of 99Tcm CQDO and 99Tcm CQDO MeB in mice demonstrate that both of them can be easily absorbed by myocardium. 99Tcm CQDO shows rapid clearence in myocardial issue and its uptake is only (5.88±1.66)% ID/g in 10 min postinjection. However, 99Tcm CQDO MeB has longer retention in heart muscle and its uptake is (7.42±0.17)% ID/g in 60 min postinjection. The elimination of each from blood accords with a biexponential pattern. The first T 1/2 is 1.38 min and 1.51 min, respectively. The partition coefficient of 99Tcm CQDO and 99Tcm CQDO MeB are 25 and 12 respectively at pH7.40.Key words 99Tcm CQDO\ 99Tcm CQDO MeB\ pharmacokinetics\ biodistribution in mice

     

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