^18F-氟代乙酸盐自动化合成及其动物实验研究  

Rapid Automated Radiosynthesis and Animal Experiments of [^(18)F]Fluoroacetate

作　　者：邓怀福[1,2] 文富华[1] 唐刚华[1] 王红亮[1] 易畅[1] 吴克宁[1] 史新冲[1] 孟悛非[3] 

机构地区：[1]中山大学附属第一医院放射科,广东广州510080 [2]中山大学附属第一医院,核医学科PET-CT,广东广州510080 [3]中山大学附属第一医院核医学科PET-CT,广东广州510080

出　　处：《中山大学学报（医学科学版）》2011年第1期99-103,115,共6页Journal of Sun Yat-Sen University:Medical Sciences

基　　金：国际原子能机构(IAEA)资助课题(15245);中山大学“百人计划”引进人才科研启动基金(80000-3126132);国家高技术研究发展计划(863计划)专题课题(2008AA02Z430)

摘　　要：【目的】研究肿瘤显像剂18F-氟代乙酸盐(18F-FAC)的自动化合成工艺及其临床前肿瘤显像评价。【方法】以溴代乙酸苄酯为前体,一种方法是应用商用PET-MF-2V-IT-I型氟-18多功能自动化合成仪,采用在柱水解法,经亲核氟化、在柱水解及Sep-Pak小柱分离纯化制备18F-FAC注射液;另一种方法,采用"一锅法"在同一反应瓶中经亲核氟化、NaOH水解两步反应及Sep-Pak分离纯化制备18F-FAC注射液。对荷肝细胞癌小鼠进行18F-FAC和18F-FDG PET显像。【结果】两种方法制备的18F-FAC注射液放化纯度均大于95%。采用在柱水解法自动化合成18F-FAC,未校正放化产率为50%～60%,总合成时间约28 min。采用"一锅法"自动化合成18F-FAC,未校正放化产率为15%～25%(n=5),总合成时间约26 min。荷肝细胞癌小鼠PET显像结果表明,18F-FAC静脉注射1 h后肿瘤对18F-FAC的摄取明显高于周围的正常组织,肿瘤对18F-FAC的摄取明显高于18F-FDG。【结论】采用在柱水解法自动化合成18F-FAC注射液,操作简便,能满足科研和临床正电子发射断层显像的需要。生产的18F-FAC有助于对肝细胞癌的诊断。【Objective】 The aim of the study was to investigate and validate the feasibility of fully automated synthesis of fluoroacetate（18F-FAC） as an oncologic PET tracer.【Methods】 Two fully automated synthetic procedures of 18F-FAC have been developed using benzyl-2-bromoacetate as a precursor.One was an on-column hydrolysis procedure using a IBA 18F-FDG synthesizer,consisting of nucleophilic fluorination,hydrolysis and purification on the Sep-Pak cartridges.The other one was a two-step one-pot procedure using a modified commercial PET-MF-2V-IT-I synthesizer,consisting of nucleophilic fluorination and hydrolysis in the same reaction vessel,and purification with the Sep-Pak cartridges.Also,18F-FAC and 18F-FDG PET images were performed on the mice models bearing hepatocellular carcinoma.【Results】 The radiochemical purity of 18F-FAC was 95% by the two procedures.The on-column hydrolysis procedure was a simple,rapid,and fully automated synthesis of 18F-FAC in a high and reproducible radiochemical yield exceeding 50-60%（decay uncorrected） within the total synthesis time of 28 min.Whereas,18F-FAC was produced by the one-pot procedure in an uncorrected radiochemical yield of 15-25% within the total synthesis time of 26 min.18F-FAC PET imaging showed higher uptake of 18F-FAC than 18F-FDG in the tumors.【Conclusion】 The new,simple,and rapid on-column hydrolysis procedure should be adaptable to the fully automated synthesis of 18F-FAC on a commercial fluorodeoxyglucose synthesizer.18F-FAC PET imaging is helpful to the diagnosis of hepatocellular carcinoma.

关 键 词：18F-氟代乙酸盐 在柱水解法 一锅法 自动化合成 PET显像 肝细胞癌 

分 类 号：R817.4[医药卫生—影像医学与核医学]