~(188)Re-AEDP 的标记条件研究及小鼠体内分布

  • 摘要: 研究了配体用量、亚锡含量、抗坏血酸用量、pH及葡萄糖用量对188Re-AEDP标记率的影响,确定了最佳标记条件。实验结果表明,188Re-AEDP标记率>90%,放化纯度>90%,标记后24h放化纯度基本不变。小鼠体内分布表明,药物有良好骨吸收,骨/肌肉、骨/血在3h达到高峰,到24h仍维持一定水平,血清除较快。188Re-AEDP作为骨痛冶疗药物具有临床研究价值。

     

    Abstract: STUDY ON THE LABELING CONDITION OF 188ReAEDP ANDTHE BIODISTRIBUTION IN RATSZhang Yadong\ Lu Jie\ Lü Gongxu(Department of Chemistry, Beijing Normal University, Beijing 100875)ABSTRACTLabeling of 1aminoethylene diphosphonate acid(AEDP) with 188Re is studied by a direct labeling method in the presence of SnCl2·2H2O as reducing agent. The effects of mass of AEDP, glucose, ascorbic acid,pH value and the concentration of SnCl2·2H2O on labeling efficiency are investigated. The optimum labeling condition is determined. The results show that the labeling yield is more than 90%, the radiochemistry purity of 188ReAEDP is more than 90% and can remain for more than 5 h.The biodistribution in rats shows that the proportion of muscles and bone to blood reach the peak value within three hours and remain high value within twentyfour hours. The clear of drug from blood is fast. So 188ReAEDP is perhaps a potential palliation therapeutic agent and the further study is worthwhile.Key words biodistribution in rats 188ReAEDP labeling condition

     

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