AD显像剂11C-PIB合成效率的影响因素

Optimization of the Radiosynthesis of the 2-(4-N-11Cmethylaminophenyl)-6-hydroxybenzothiazole for AD

  • 摘要: 11C-PIB是诊断阿尔茨海默病(AD)的特征靶Aβ斑块的正电子放射性药物,本工作系统研究了以11CH3-Triflate为甲基化试剂合成11C-PIB合成的影响因素。在国产碳多功能合成仪上, 研究前体量、溶剂、反应温度及体系的pH等对11C-PIB效率的影响,并对合成条件进行优化。结果显示:前体量、溶剂、反应温度及体系的pH均明显影响合成效率。优化后的合成条件为:丙酮为溶剂,前体浓度为5 g/L,反应温度为常温,pH为中性。在此条件下,11C-PIB的合成效率为65.2%±4.7%(n=8,校正效率),产品的放化纯度大于99%,比活度为70.6 GBq/g(18.0 TBq/mmoL)。从11CO211C-PIB的合成时间为30 min, 单次合成的产量为3.7 GBq。以上结果表明,通过优化合成条件,可以稳定、高质量地合成11C-PIB,以满足临床需要。

     

    Abstract: 11C-PIB was the standard PET radiopharmaceuticals for Alzheimer’s disease(AD) imaging targeting beta-amyloid plaques. The optimization for high synthesis yield and specific activity was designed with 11CH3-Triflate as methylation agent for 11C-PIB. Synthesis for 11C-PIB were studied with home made carbon-11 synthesis module. The results showed that the amount of precursor, the temperature and pH could effect the labeling yield. The optimum reaction conditions were as fllows: with 5 g/L of precursor, pH=7.0, at room temperature, a yield of 65.2%±4.7%(n=8) and a specific activity of 70.6 GBq/g (18.0 TBq/mmol) were achieved, and radiochemical purity was over 99%. It took 30 min from 11CO2 to 11C-PIB. Single synthesis yielding was 3.7 GBq of 11C-PIB. The quantity and quality of 11C-PIB were suitable for clinical use after optimization.

     

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