~(177)Lu-EDTMP的药盒法制备、大鼠体内生物分布及显像

通过反应堆辐照Lu2O3,再经化学处理制得177LuCl3溶液;制备了不同配比的含钙EDTMP药盒,并对其进行了177Lu标记;完成了177Lu-EDTMP在大鼠体内的生物分布及显像实验。标记实验结果表明,制得的177Lu标记自制EDTMP药盒可获得95%以上的标记率,且标记溶液的稳定性较好,在室温下放置一周后,放化纯度95%。生物分布及显像实验结果显示,药盒法制备的177Lu-EDTMP骨摄取高且滞留时间长,在注药1 h后骨的放射性摄取率3%ID.g-1,而在注药11 d后仍保持在2%ID.g-1以上,注药后13 d,显像图片中全身骨骼仍可清晰显示;主要经肾清除,血液清除快,注药3 h后,在血液及肌肉中的摄取率已接近本底水平;显像结果显示,除膀胱外其它主要器官及软组织中均未见明显的放射性浓集,体现出其作为骨痛治疗药物的良好体内分布特性。

Biodistribution and Imaging Study on 177Lu-EDTMP Prepared by Kit Method

177Lu was produced by thermal neutron bombardment on natural Lu2O3 target in the research reactor and obtained as 177LuCl3 solution after corresponding chemical process.EDTMP kits containing Ca with different formulations were prepared,and 177Lu labelling of these kits was evaluated under different conditions such as pH,reaction time,reaction volume and the molar ratio of Lu to EDTMP.The biodistribution and imaging experiments were performed in normal male SD rats.The results of labelling indicated that the labelling yields could be obtained over 95%,and the stability of the reaction solution was also satisfactory.The results of biodistribution and imaging demonstrated that 177Lu-EDTMP showed significant uptake and strong retention in bones and it was excreted mainly via urinary system and cleared very rapidly from blood and soft tissues.The images showed no noticeable accumulation of 177Lu-EDTMP in main organs and soft tissues except in bladder.177Lu-EDTMP prepared by kit method exhibited desired in vivo distribution properties as a potential therapeutic radiopharmaceutical for bone pain palliation.