用于 PET 肿瘤成像的放射性药物[N-甲基-11C]胆碱的自动合成

IF 0.9 Q4 CHEMISTRY, INORGANIC & NUCLEAR

Radiochemistry Pub Date : 2024-10-06 DOI:10.1134/S106636222404012X

D. D. Vaulina, O. F. Kuznetsova, V. V. Orlovskaya, O. S. Fedorova, R. N. Krasikova

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引用次数: 0

摘要

我们开发了一种自动合成[N-甲基-11C]胆碱的方法，这是一种利用正电子发射断层扫描（PET）诊断癌症的放射性药物（RP）。合成是在一个自制模块上进行的，采用了在线 11C 甲基化过程和固相萃取方法的组合技术。[N-甲基-11C]胆碱的放射化学收率为 80%（基于甲基化剂[11C]CH3I 的活性，衰变已校正），这确保了一次批量生产多个临床剂量的放射性药物。获得的[N-甲基-11C]胆碱的放射化学纯度超过 99%，2-二甲氨基乙醇（主要化学杂质）的含量为 0.06 mg/mL，符合俄罗斯和欧洲药典的要求。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Automated Synthesis of [N-Methyl-11C]choline, Radiopharmaceutical for Tumor Imaging by PET

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Automated Synthesis of [N-Methyl-11C]choline, Radiopharmaceutical for Tumor Imaging by PET

An automated method has been developed for the synthesis of [N-methyl-¹¹C]choline, a radiopharmaceutical (RP) for the diagnosis of cancer using positron emission tomography (PET). The synthesis was carried out on a home-made module, using combined technology of on-line ¹¹C-methylation processes and solid-phase extraction methods. The radiochemical yield of [N-methyl-¹¹C]choline was 80% (based on the activity of the methylating agent, [¹¹C]CH₃I, decay corrected), which ensures the production of several clinical doses of radiopharmaceutical in one batch. [N-Methyl-¹¹C]choline was obtained with a radiochemical purity of more than 99% and an amount of 2-dimethylaminoethanol (the main chemical impurity) of 0.06 mg/mL, which meets the requirements of the Russian and European Pharmacopoeia.

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来源期刊

Radiochemistry CHEMISTRY, INORGANIC & NUCLEAR-

CiteScore

1.30

自引率

33.30%

发文量

期刊介绍： Radiochemistry is a journal that covers the theoretical and applied aspects of radiochemistry, including basic nuclear physical properties of radionuclides; chemistry of radioactive elements and their compounds; the occurrence and behavior of natural and artificial radionuclides in the environment; nuclear fuel cycle; radiochemical analysis methods and devices; production and isolation of radionuclides, synthesis of labeled compounds, new applications of radioactive tracers; radiochemical aspects of nuclear medicine; radiation chemistry and after-effects of nuclear transformations.