^(188)Re-AEDP 的标记条件研究及小鼠体内分布

STUDY ON THE LABELING CONDITION OF 188 Re AEDP AND THE BIODISTRIBUTION IN RATS

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。

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.