^177Lu-EDTMP和^177Lu-DOTMP的制备及其生物分布

研究了乙二胺四甲撑膦酸（EDTMP）和四膦酸亚甲基-四氮杂环十二烷（DOTMP）的^177Lu标记，优化了标记条件，并对标记物在正常小鼠体内的生物分布进行了研究。^177Lu-EDTMP的最佳标记条件为：EDT—MP25mg、^177LuCl3溶液100μL（12．8MBq）、pH8，100℃下反应30min；^177Lu—DOTMP的最佳标记条件为：DOTMP6．3mg、^177LuCl3溶液100μL（5MBq），pH9，100℃下反应15min。^177Lu-EDTMP和^177Lu-DOTMP均具有较好的体外稳定性，室温下存放7d，放化纯度仍〉98％。生物分布结果显示，^177Lu-EDTMP和^177Lu-DOTMP主要浓聚于骨组织，经肾脏排泄，^177Lu-DOTMP较^177Lu-EDTMP的血液清除快。该结果表明两者都具有良好的骨靶向性。

Radiolabeling and Biodistribution of 177Lu-EDTMP and 177Lu-DOTMP

The labeling methods for ^177Lu-EDTMP and ^177Lu-DOTMP were established,and the biodistribution of ^177Lu-EDTMP and ^177Lu-DOTMP in normal mice was carried out as well. The optimal experimental condition of ^177Lu-EDTMP and ^177Lu-DOTMP was as follows： EDTMP 25 mg,^177LuCl3 solution 100μL（12.8 MBq）, pH 8 at 100 ℃ for 30 min and DOTMP 6.3 mg,^177LuCl3 solution 100μL（5 MBq） ,pH 9 at 100℃ for 15 min respectively. Both of the two radiolabeled complex were observed to be good stability for 7 days at room temperature, the radiochemical purity was more than 98%. The results showed that ^177Lu- EDTMP and ^177Lu-DOTMP were selective skeletal uptake and mainly excreted by kidney. 177Lu-DOTMP was more quickly cleared from blood than ^177Lu-EDTMP. It indicated that the two labeling compounds have good bone targeting.