2-^(18)F-氟代丙酸的自动化合成及其Micro PET肺癌小鼠显像  

The automated synthesis of 2-^(18)F-fluoropropoinic acid and micro PET imaging in mice of lung cancer

作　　者：党永红[1] 蔡炯[1] 王玲[1] 李欣[1] 吕京桥[1] 李方[1] 

机构地区：[1]中国医学科学院北京协和医院核医学科,北京100730

出　　处：《中国医学装备》2015年第6期46-50,共5页China Medical Equipment

基　　金：国家自然科学基金(30670741)"AAV介导的淀粉样肽单链抗体基因治疗AD的研究";国家自然科学基金(30500573)"阿尔茨海默病Beta淀粉样肽单链抗体和全人抗体的研究"

摘　　要：目的:利用国产PET-MF-2V-IT-I型氟多功能合成模块建立2-18F-氟代丙酸(2-18F-FPA)稳定合成方法,并评价其在肿瘤显像中的价值。方法:前体2-溴代丙酸乙酯与18F-发生氟代反应,中间体2-18F-FPA乙酯采用高压液相色谱法(HPLC)分离,收集保留时间在6.3~7.3 min的组分,将组分与Na OH溶液于100℃加热水解10 min,加入HCl调至中性,经过0.22μm除菌滤膜后得终产品。目测澄清度,测定p H值、放射化学纯度和稳定性后行C57BL/Micro PETJ荷瘤小鼠显像。结果:自动合成过程约40 min,放化收率(35±2)%(未经时间校正),产品放化纯度>98%。产品澄清无颗粒,p H值为6.0,在室温放置6 h稳定,小鼠肿瘤显像清晰。结论:利用国产PET-MF-2V-IT-I型氟多功能合成模块合成肿瘤显像剂2-18F-FPA,操作简便,合成时间短,收率及放射化学纯度高,稳定性好,在肿瘤显像中值得进一步的研究。Objective： To establish a stable automated synthetic technology of 2-18F-fluoropropoinic acid （2-18F-FPA） using PET-MF-2V-IT-I multifunction synthesizer. To evaluate its value in tumor imaging. Methods： The precursor, ethyl 2-bromopropoinitatewas fluorinated with 18F .The intermediate, ethyl 2-[18F] fluoropropoinitate was separated by HPLC. The components which retention time was from 6.5 to 7.5 min were collected. The components were heated with NaOH solution at 100 C for 10 min to hYdrolyze, then neutralized with HCI solution. The product was obtained after the solution passed, through the 0.22 m sterile filter. The clarity was t ested visually, the. pH value was tested with precise pH paper, and its radiochemical purity and stability were also measured. The micro-PET imagings were performed on C57BL/J mice with lung cancer. Results： The whole synthesis procedure was about 40 min. The radiochemical yield was about 35% _＋2%（decay uncorrected）. The radiochemical purity of 2-18F-FPA was 〉98%.The product solution was clear and no particles. The pH value was 6.0.The product solution was stable in room temperature 6 h later.The imaging of tumor was clearly. Conclusion： Tumor imaging agent 2-18F-FPA can be synthesized on PET-MF-2V-IT-I multifunction synthesizer simply and rapidly. The synthetic yield, radiochemical purity and stability at room temperature can meet the clinical requirements and worth further studies.

关 键 词：2-18F-氟代丙酸 肿瘤显像剂 自动化合成 

分 类 号：R817.4[医药卫生—影像医学与核医学]