Journal of Isotopes ›› 2009, Vol. 22 ›› Issue (3): 149-155.DOI: 10.7538/tws.2009.22.03.0149

• 研究报告 • Previous Articles     Next Articles

Preparation of 99Tcm-Gd-DTPA-Dimeglumine and Its Biologic Characteristics

DING Zhi-ling; CHEN Yue ; SUN Yuan-yuan; ZHANG Wei; HUANG Zhan-wen; ZHANG Li   

  1. Department of Nuclear Medicine, Affiliated Hospital, Luzhou Medical College
  • Received:2009-04-14 Revised:2009-06-30 Online:2009-08-20 Published:2009-08-20
  • Contact: DING Zhi-ling


丁志凌; 陈  跃; 孙媛媛;张  伟;黄占文;张  莉   

  1. 泸州医学院附属医院核医学科
  • 通讯作者: 丁志凌

Abstract: The purpose of this study was to evaluate the feasibility of Gd-DTPA-Dimeglumine, as a contrast enhancer in magnetic resonance imaging(MRI). Gd-DTPA-Dimeglumine was labeled with 99Tcm, and its biologic characteristics were observed. The radiochemical purity and the stability of 99Tcm-Gd-DTPA-Dimeglumine were measured by TLC The labelling yield of 99Tcm-Gd-DTPA-Dimeglumine was>95% and stable for at least 6 h at room temperature with the radiochemical purity more than 90%. The plasma protein binding rate of 99Tcm-Gd-DTPA-Dimeglumine was 2.25%±0.21%. The biodistribution in mice showed that 99Tcm-Gd-DTPA-Dimeglumine was excreted through kidney. The time of the highest uptake in all of the major organs was at 1 min after injection, and the decrease of deposition morn than 50% at 5 min after injection, and the brain and muscles have the lowest uptake rate less than 1%. The major organs have little uptake at 30-60 min after injection. Renal dynamic scintigraphy in rabbits were administrated via intravenous injection. The results indicated that 99Tcm-Gd-DTPA-Dimeglumine was quickly excreted by kidney, and the time to peak is about 5 min, the half time of clearance is about 7 min. It is a sample method with high labeling efficiency and radiochemical purity that Gd-DTPA-Dimeglumine labeled with 99Tcm, and its bio-distribution was not changed on the whole after labeled. The study indicated that DTPA as a bifunctional chelator may be linked with 99Tcm and Gd. So a type of new multimodality imaging agents with higher targeting characteristics, it could be applied both in SPECT and MRI scan.

Key words: DTPA, Gadolinium DTPA dimeglumine, bio-distribution, 99Tcm labeling

摘要: 以氯化亚锡为还原剂,99Tcm 一步法标记了顺磁对比剂Gd-DTPA-Dimeglumine (钆喷酸二甲葡胺),得到99Tcm-Gd-DTPA-Dimeglumine。薄层色谱法(TLC)分析标记物的标记率>95%,可在室温下稳定存放6 h,放化纯度>90%;三氯乙酸沉淀法测定99Tcm-Gd-DTPA-Dimeglumine的体外血浆蛋白结合率为2.25%±0.21%。小鼠体内生物分布结果显示,99Tcm-Gd-DTPA-Dimeglumine 主要经肾脏排泄,脑和肌肉组织摄取最少,所有脏器在注射后1 min摄取达高峰,注射后5 min滞留率下降大于50%,注射后30~60 min标记药物在主要脏器内滞留很少。家兔肾动态显像结果显示,99Tcm-Gd-DTPA-Dimeglumine 主要经肾脏排泄,达高峰时间约5 min,半排时间约7 min。99Tcm标记Gd-DTPA-Dimeglumine 方法简单,标记效率高,Gd-DTPA-Dimeglumine 经99Tcm标记后其生物学性质基本未改变。本实验表明可以通过双功能螯合剂DTPA同时链接放射性核素99Tcm 和顺磁性金属元素Gd,并有望此基础上合成一种具有较好靶向性又可同时进行核医学SPECT和MRI增强扫描的显像剂。

关键词: DTPA, Gd-DTPA-二甲葡胺, 生物学分布, 99Tcm标记

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