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99mTc(Ⅳ)标记双膦酸配合物的制备及其在动物体内骨显像性能

程文,林建国,邱玲*,叶万忠,罗世能   

  1. (江苏省原子医学研究所，卫生部核医学重点实验室，江苏省分子核医学重点实验室 无锡 214063)
  • 收稿日期:2012-07-06 修回日期:2012-10-30 出版日期:2013-05-10 发布日期:2013-05-10
  • 通讯作者: 邱玲，副研究员; Tel:0510-85514482; Fax:0510-85513113; E-mail:qiulingwx@gmail.com; 研究方向：肿瘤诊治药物的设计与合成
  • 基金资助:
    国家自然科学基金（20801024）江苏省自然科学基金（BK2009077）和江苏省医学重点人才基金（RC2011097）资助项目

Preparation and in vivo Bone Imaging Properties of 99mTc(Ⅳ)-Labeled Diphosphonic Acid Complex

CHENG Wen, LIN Jianguo, QIU Ling*, YE Wanzhong, LUO Shineng   

  1. (Key Laboratory of Nuclear Medicine,Ministry of Health,Jiangsu Key Laboratory of
    Molecular Nuclear Medicine,Jiangsu Institute of Nuclear Medicine,Wuxi 214063,China)
  • Received:2012-07-06 Revised:2012-10-30 Published:2013-05-10 Online:2013-05-10
  • Contact: Ling Qiu

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摘要： 以2-乙基咪唑、5-溴戊酸乙酯和PCl3为原料，合成了一种唑来膦酸衍生物：1-羟基-5-（2-乙基-1H-咪唑-1-基）戊烷-1,1-双膦酸（EIPeDP），将其与放射性元素99mTc(Ⅳ)进行标记形成配合物，研究了EIPeDP用量和反应体系pH值对标记率的影响。 结果表明，当pH值为5~6、EIPeDP为5 mg、SnCl2·2H2O为100 μg和Na99mTcO4为92.5 MBq时,可获得满意的标记率和放化纯（均大于97％）。 标记物99mTc-EIPeDP具有良好的体外稳定性。 动物体内实验表明，兔经注射99mTc-EIPeDP 1 h后获得的骨显像图质量明显优于99mTc-ZL和99mTc-MDP。 表明99mTc-EIPeDP是一种制备简便、稳定性好和骨显像性能优异的新型放射显像剂。

关键词: 唑来膦酸衍生物, 99mTc标记, 质控, 稳定性, 骨显像

Abstract: A zoledronic acid derivative, 1-hydroxy-5-(2-ethyl-1H-imidazol-1-yl)pentane-1,1-diphosphonic acid(EIPeDP), was synthesized using 2-ethylimidazole， 5-bromo valeric acid ethyl ester and PCl3 as the starting material and further labeled with 99mTc. The influence of the amount of EIPeDP and the pH value of the reaction system on the labeling yield of 99mTc-EIPeDP has been studied. Satisfactory radiolabelling yield(RLY) and the radiochemical purity(RCP)(over 97％) were obtained when the pH was 5~6 and the amount of EIPeDP, SnCl2·2H2O and Na99mTcO4 were 5 mg, 100 μg and 92.5 MBq, respectively. The radiolabeled complex was very stable in vitro. In vivo SPECT bone imaging of rabbit showed that a clearer image can be obtained from 99mTc-EIPeDP at 1 h post injection, which is superior to 99mTc-ZL and 99mTc-MDP. These results showed that 99mTc-EIPeDP is a potential bone imaging agent with advantages of simple preparation, good stability and superior bone imaging characteristics.

Key words: zoledronic acid derivative, 99mTc radiolabeling, quality control, stability, bone imaging

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