国产氟多功能模块自动化合成18F-6-氟-L-DOPA及其临床初步应用

Automatic Synthesis of 18F-6-F-L-DOPA and its Application in Clinical PET Imaging

  • 摘要: 18F-6-氟-L-DOPA (18F-DOPA)在神经内分泌肿瘤诊断中具有重要价值,本研究利用国产氟多功能模块合成了18F-DOPA并进行临床初步研究。以6-硼酯-二甲氧基-L-DOPA为前体,铜盐Cu(OTf)2(py)4为催化剂直接亲核反应,再经氢碘酸水解得到18F-DOPA ,并进行质量控制,测量其体外稳定性,研究18F-DOPA在正常人和一例神经内分泌肿瘤患者的显像。18F-DOPA合成耗时60 min,不校正合成效率为(10.0±2.3)%(n=6),放化纯度大于99%,产量大于7.4 GBq;加入微量抗坏血酸或乙醇可提高其体外稳定性。人体PET结果显示:18F-DOPA在脑内浓聚于纹状体,主要经肾脏代谢,见胰岛细胞瘤显像。结果表明, 国产氟多功能模块自动化合成18F-DOPA简单快捷、重复性好,产品质量符合临床要求。

     

    Abstract: 18F-6-Fluoride-L-DOPA (18F-DOPA) has an important value in the imaging diagnosis of neuroendocrine tumors. In this study, we used homemade Fluoride-module to synthesis 18F-DOPA and evaluate its clinical imaging. 18F-DOPA was synthesized by direct nucleophilic reaction with 6-boric acid-dimethoxy-L-DOPA as precursor, Cu(OTf)2(py)4 as catalyst, and hydrolysis by hydriodic acid. Quality control and the in vitro stability were preformed. The 18F-DOPA was confirmed PET imaging of neuroendocrine neoplasms and control. It took 60 minutes from 18F ions to 18F-DOPA, no corrected efficiency was (10.0±2.3)% (n=6), radiochemistry purity was over 99%. It could got 7.4 GBq of 18F-DOPA once time. The trace of ascorbic acid or ethanol could prevent radiolysis of 18F-DOPA. The striatum was seen at 18F DOPA imaging. The radioactivity were mainly extracted through kidney and urine. A positive lesion in pancreatic in patient with neuroendocrine tumor. 18F-DOPA was synthesized by direct nucleophilic reaction with homemade Fluoride-module. It could got good repeatability and high quality for clinical used.

     

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