首页|2-18F-氟丁酸的自动化合成及荷前列腺癌裸鼠PET/CT显像评价

2-18F-氟丁酸的自动化合成及荷前列腺癌裸鼠PET/CT显像评价

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目的 研究2-18F-氟丁酸(2-18F-FBA)自动化合成工艺小柱纯化方法,使其能满足GMP生产要求缩短合成时间提高产率,并对其进行荷前列腺癌裸鼠PET/CT显像评价。方法 以GE TRACERlab FX-FN模块为基础,用"一锅法"和"柱水解法"合成2-18F-FBA。两种方案均使用2-溴丁酸甲酯为前体,经氟化、纯化和水解得终产品2-18F-FBA。荷前列腺癌裸鼠尾静脉注射2-18F-FBA后于不同时间点行micro-PET/CT显像,PMOD软件勾画感兴趣区并计算最大标准化摄取值。结果 "一锅法"和"柱水解法"合成2-18F-FBA的时间分别为35 min和27 min,未校正放化产率为(34±5。2)%和(41±3。7)%。Micro-PET/CT显示,注射2-18F-FBA 30 min肿瘤处放射性摄取明显,60 min后,肿瘤/肌肉比相对较高。两种方案均能合成2-18F-FBA,"柱水解法"合成时间相对更短、产率更高。结论 2-18F-FBA荷前列腺癌裸鼠肿瘤处显像清晰,60 min时有较高的靶本比。
Automated production of 2-18F-fluorobutyric acid and as a PET imaging agent for prostate cancer
Objective To investigate the automatic synthesis process of 2-18F-fluorobutyric acid(2-18F-FBA)and its C18 column purification method,so as to meet the production requirements of Good Manufacturing Practice of Medical Products(GMP),shorten the synthesis time and improve the yield.To evaluate the PET imaging of 2-18F-FBA in nude mice with prostate tumor.Methods Based on the GE TRACERlab FX-FN module,2-18F-FBA was automatically synthesized by'one-pot method'and'column hydrolysis method',respectively.Both schemes used methyl 2-bromobutyrate as a precursor,which was fluorinated,purified and hydrolyzed to obtain 2-18F-FBA.Micro-PET/CT was performed at different time points after tail vein injection of 2-18F-FBA in nude mice bearing prostate tumor,and the PMOD software was used to outline the region of interest and calculate the maximum standardized uptake value.Results The synthesis time of 2-18F-FBA by'one-pot method'and'column hydrolysis method'was 35 min and 27 min,respectively,and the uncorrected radiochemical yield was(34±5.2)%and(41±3.7)%.Micro-PET/CT showed significant radio-concentration at the tumor at 30 min after injection of 2-18F-FBA,and the tumor/muscle ratio was relatively high at 60 min.Both schemes were able to synthesize 2-18F-FBA,with the'column hydrolysis'method having a relatively shorter synthesis time and higher yield.Conclusion The 2-18F-FBA is clearly visualized in tumor of prostate tumor bearing nude mice with a high target/non-target ratio at 60 min.

2-18F-FBAmicro-PET/CTprostate cancerradiosynthesis

董伟璇、秦开心、胡文豪、沈聪、牛晨、段小艺

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西安交通大学第一附属医院PET/CT室,陕西 西安 710061

山西医科大学第一医院核医学科,山西 太原 030001

2-18F-FBA micro-PET/CT 前列腺癌 放化合成

国家自然科学基金陕西省留学人员科技活动择优资助项目

821020142022-006

2024

分子影像学杂志
南方医科大学

分子影像学杂志

CSTPCD
ISSN:1674-4500
年,卷(期):2024.47(7)
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