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177Lu-EDTMP和177Lu-DOTMP的制备及其生物分布

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

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【作者】 邓新荣李洪玉叶肇云郭红源李凤林罗志福

【Author】 DENG Xin-rong,LI Hong-yu,YE Zhao-yun,GUO Hong-yuan,LI Feng-lin,LUO Zhi-fu(Department of Isotope,China Institute of Atomic Energy,Beijing 102413,China)

【机构】 中国原子能科学研究院同位素研究所

【摘要】 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-MP 25 mg、177LuCl3溶液100μL(12.8 MBq)、pH8,100℃下反应30 min;177Lu-DOTMP的最佳标记条件为:DOTMP6.3 mg、177LuCl3溶液100μL(5 MBq),pH9,100℃下反应15 min。177Lu-EDTMP和177Lu-DOT-MP均具有较好的体外稳定性,室温下存放7 d,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。

【Abstract】 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 fo-llows: EDTMP 25 mg,177LuCl3 solution 100 μL(12.8 MBq),pH 8 at 100 ℃ for 30 min and DOTMP 6.3 mg,177LuCl3 solution 100 μL(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.

【关键词】 177LuEDTMPDOTMP生物分布
【Key words】 177LuEDTMPDOTMPbiodistribution
【基金】 IAEA资助项目(CRP-14054)
  • 【分类号】R817
  • 【被引频次】5
  • 【下载频次】93
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