18F-阿法肽的自动化制备及其前列腺癌PET/CT显像

Automatic preparation of 18F-AlfatideⅡand its PET/CT imaging in prostate cancer

目的:探讨基于CFN-100氟多功能模块自动化制备18F-阿法肽(AlfatideⅡ)的方法并进行前列腺癌显像。方法:通过氟离子分装器分出200~500μl氟离子至反应管中,与标记前体1,4,7-三氮杂环壬烷-1,4,7-三乙酸-E[(聚乙二醇)4-环(精氨酸-甘氨酸-天冬氨酸-D-苯丙氨酸-酪氨酸)]2{NOTA-E[PEG 4-c(RGDfk)]2}(冻干药盒)反应,在水相中与18F经铝介导螯合标记,再经C18柱分离纯化,自动化制备得到18F-阿法肽,测定其放化产率。对18F-阿法肽注射液进行质量分析,并对2例前列腺癌患者(72岁和66岁)行18F-阿法肽PET/CT显像。结果:采用结合双管路氟离子分装器的CFN-100氟多功能模块成功自动化制备18F-阿法肽,合成时间约30 min,放化产率为(28±3)%(非衰变校正,n=6),放化纯>98%,比活度为2.8×10^7 MBq/mmol,核素纯度大于99%。2例患者PET/CT显像示18F-阿法肽高度浓聚于前列腺癌病灶,最大标准摄取值(SUV max)分别为35.6和5.0。结论:利用改进的CFN-100氟多功能模块成功自动化制备18F-阿法肽,产物合成方法稳定,合成时间短,放化产率高,可高度浓聚于前列腺癌病灶。

Objective To prepare 18F-AlfatideⅡautomatically based on the improved CFN-100 fluorine multifunctional module and assess its PET/CT imaging in prostate cancer patients.Methods A certain volume(200-500μl)of fluoride ion was separated into the reaction tube by a fluoride ion separator and reacted with the labeled precursor l,4,7-triazacylononane-1,4,7-triacetic acid-E[(polyethylene glycol)4-cyclo(Arg-Gly-Asp-D-Phe-Tyr)]2(NOTA-E[PEG4-c(RGDfk)]2)(lyophilized kit).In the aqueous phase,18F was chelated with aluminum.After being separated and purified by C18 column,18F-AlfatideⅡwas prepared automatically.The radiochemical yield and its quality were analyzed.Quality control was carried out and 18F-AlfatideⅡPET/CT imaging was performed in 2 patients(72 and 66 years old)with prostate cancer.Results 18F-AlfatideⅡwas prepared automatically by the improved CFN-100 fluorine multifunctional module combined with a double channel-fluorine ion separation device.18F-AlfatideⅡwas synthetized in about 30 min,with radiochemical yield of(28±3)%(non-decay corrected,n=6).The radiochemical purity of the product was more than 98%,the specific activity was 2.8×10^7 MBq/mmol and the nuclear purity was>99%.PET/CT imaging of 2 patients showed that 18F-AlfatideⅡwere highly concentrated in prostate cancer lesions with the maximum standardized uptake value(SUVmax)of 35.6 and 5.0,respectively.Conclusion 18F-AlfatideⅡcan be prepared successfully by improved CFN-100 fluorine multifunctional module with stable synthesis method,short synthesis time and high radiochemical yield,which can be highly concentrated in prostate cancer.