【作者】 孙慧萍； 周卫华； 张锦明； 张晓军； 陈英茂； 田嘉禾；

【Author】 SUN Hui-ping~1,ZHOU Wei-hua~1,ZHANG Jin-min~2, ZHANG Xiao-jun~2,CHEN Yin-mao~2,TIAN Jia-he~2 (1.Dept of Pharm,General Hospital of Chinese Peoples Armed Police Forces,Beijing 100039,China 2.Dept Nucl Med,The PLA General hospital,Beijing,100853.China)

【机构】 中国人民武装警察总医院药剂科； 中国人民解放军总医院核医学科；

【摘要】 ¹¹C-PIB是诊断阿尔茨海默病的特征靶Aβ斑块的正电子放射性药物,本研究系统研究了以¹¹CH₃-Triflate为甲基化试剂合成¹¹C-PIB的影响因素。结果表明,前体量、溶剂、反应温度及体系的pH均明显影响合成效率。优化合成条件为:在丙酮溶液中,前体浓度为5 mg/mL,常温、中性条件下的合成效率为65.2%（n=8）,产品的放化纯大于99%,比活度为18.0 TBq/mmoL.从¹¹CO₂到¹¹C-PIB的合成时间为40 min,单次合成的剂量为3.7 GBq。更多还原

【Abstract】 ¹¹C-PIB was the standard PET radiopharmaceuticals for Alzheimer imaging targeting beta-amyloid plaques. We aimed to optimization for high synthesis yield and specific activity with ¹¹CH₃-Triflate as methylation agent for ¹¹C-PIB. The result showed that the amount of precursor,the temperature and pH can effect the labeling yield.The optimum reaction condition were with 5mg/mL of precursor,pH = 7.0 at room temperature,got yielding at 65.2%（n=8）, specific activity at 18.OTBq/mmol and radiochemical purity was over 99%.It took 30min from ¹¹CO₂ to ¹¹C-PIB,and yields of 3.7 GBq with a single synthesis.The quantity and quality of ¹¹C-PIB was suitable for clinical used after optimization.更多还原