JOURNAL OF ISOTOPES

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Modified Auto-synthesis and Clinical Trial of the 11C-PIB as a Potential β-amyloid Imaging Agent

ZHANG Zheng-wei1,2;ZHU Jian-hua2;YAO Zhi-wen3;GUAN Yi-hui1;HUA Feng-chun1   

  1. 1.PET Center, Huashan Hospital, Fudan University, Shanghai 200235, China;2.Department of Radiopharmacy, School of Pharmacy, Fudan University, Shanghai 200032, China;3.Department of Neurology, Yangpu Hospital, Tongji University, Shanghai, 200090, China
  • Online:2017-02-20 Published:2017-03-06

淀粉样蛋白显像剂11C-PIB的自动化制备优化及临床初步应用

张政伟1,2;朱建华2;姚志文3;管一晖1;华逢春1   

  1. 1.复旦大学附属华山医院 PET中心,上海200235;2.复旦大学药学院 放射药学教研室,上海200032;3.上海同济大学附属杨浦医院 神经内科,上海200090

Abstract:

The auto-synthesis method was developed for the on-line preparation of amyloid-beta (Aβ) plaques image agent 11C-PIB. A intermediate, 11CH3OTf, made from 11CH3 which was produced from 11CO2 with LAH/THF, was bubbled into 1.0 mg precursor 6-OH-BTA-0 butanone solution in salt-ice condition. The final crude product was then purified though prep-HPLC to get purified product. The human images were obtained in four cases of AD and 1 normal volunteer. The total synthesis process took about 35 minutes. The synthesis yield (EOS) was (25±5)% (not correct), the radiochemical purity over 98%, and the specific activity about 5.55 GBq/μmol. The modified automated preparation of 11C-PIB was verified in producing 11C-PIB of high radiochemical purity and synthesis yield in a short time. The results showed that this promising product could be used in clinical imaging.

Key words: positron emission tomography, Alzheimer’s disease, 11C-PIB

摘要:

采用国产自动化碘代甲烷仪,通过氢化锂铝/四氢呋喃(LAH/THF)还原法制得的11C-碘代甲烷(11CH3I),在线转换成活性更高的11C-三氟磺酸甲酯(11CH3OTf),通入锥形反应瓶内,和1.0 mg PIB前体6-OH-BTA-0丁酮溶液在盐冰浴条件下反应,利用改进的HPLC方法纯化产品,并对最终产品进行质量控制。用昆明小鼠进行急性毒性试验,并行4例临床AD患者及1例正常人PET/CT显像。结果表明,改进后的自动化制备工艺,最终得到可供注射的11C-PIB 10%乙醇溶液,改进后使用前体原料更少,产率稳定。改进后的11C-PIB制备路线稳定可靠,初步临床研究表明,制备的11C-PIB显像剂可以用于阿尔茨海默病诊断。

关键词: 正电子发射断层扫描显像, 阿尔茨海默病, [N-甲基-11C]2-[4&prime, -(甲氨基)苯基]-6-羟基苯并噻唑