177Lu-EDTMP的药盒法制备、大鼠体内生物分布及显像

doi:10.7538/tws.2010.23.02.0065

同位素 ›› 2010, Vol. 23 ›› Issue (2): 65-70.DOI: 10.7538/tws.2010.23.02.0065

• 放射性药物和标记化合物 • 下一篇

¹⁷⁷Lu-EDTMP的药盒法制备、大鼠体内生物分布及显像

李洪玉¹;梁积新¹;向学琴¹;邓新荣¹;郑德强¹;罗洪义¹;陈阳²;刘海春²;鲁佳¹;罗志福¹

1.中国原子能科学研究院同位素研究所，北京102413；2.中国核工业北京401医院，北京102413

收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:2010-05-20 发布日期:2010-05-20

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

LI Hong-yu¹; LIANG Ji-xin¹; XIANG Xue-qin¹; DENG Xin-rong¹; ZHENG De-qiang¹; LUO Hong-yi¹; CHEN Yang²; LIU Hai-chun²; LU Jia¹; LUO Zhi-fu¹

1. Department of Isotope, China Institute of Atomic Energy, Beijing 102413, China; 2. China Nuclear Industry Beijing 401 Hospital, Beijing 102413, China

Received:1900-01-01 Revised:1900-01-01 Online:2010-05-20 Published:2010-05-20

摘要/Abstract

摘要： 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%•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。

关键词: ¹⁷⁷Lu, EDTMP药盒, 生物分布, 显像

Abstract: ¹⁷⁷Lu was produced by thermal neutron bombardment on natural Lu₂O₃target 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.

Key words: ¹⁷⁷Lu, EDTMP kit, biodistribution, imaging

李洪玉 ;梁积新 ;向学琴 ;邓新荣 ;郑德强 ;罗洪义 ;陈阳 ;刘海春 ;鲁佳 ;罗志福 . ¹⁷⁷Lu-EDTMP的药盒法制备、大鼠体内生物分布及显像[J]. 同位素, 2010, 23(2): 65-70.

LI Hong-yu; LIANG Ji-xin; XIANG Xue-qin; DENG Xin-rong; ZHENG De-qiang; LUO Hong-yi; CHEN Yang; LIU Hai-chun; LU Jia; LUO Zhi-fu. Biodistribution and Imaging Study on ¹⁷⁷Lu-EDTMP Prepared by Kit Method[J]. Journal of Isotopes, 2010, 23(2): 65-70.

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¹⁷⁷Lu-EDTMP的药盒法制备、大鼠体内生物分布及显像

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

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