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NaOH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pH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,pH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 6.3 to 7.3 min were collected. The components were heated with NaOH solution at 100℃for 10 min to hydrolyze, then neutralized with HCl solution. The product was obtained after the solution passed through the 0.22 m sterile filter. The clarity was tested visually, the pH value was tested with precise pH paper, and its radiochemical purity and stability were also measured. The microPET 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.
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