摘要
目的研究固相柱水解和氢离子交换柱(IC-H)中和法自动化合成2-18F-β-D-脱氧葡萄糖(18F-FDG)的方法,并分析合成过程中的放射性损失。方法经可调节的风浴加热反应管,分两次共沸除体系中的水,加入前体2-三氟甲基磺酰基-β-D-甘露糖,亲核反应270s,风浴冷却,用水将18F-FDG-OAc4中间体负压转移到Sep-PakC18固相水解柱上,冲洗C18柱;NaOH慢慢加入到C18柱床上,室温下反应;将18F-FDG转移,经IC-H柱、Al2O3柱、C18柱纯化后收集于产品瓶。结果合成18F-FDG全过程只需22min,不校正合成效率(EOS)为(66.9±4.0)%(n=15),产品pH值为6.0左右,经TLC检测,放射性化学纯度>98%。废液,IC-H柱、Al2O3柱、C18纯化柱,C18水解柱,无菌滤膜等都有不同程度的放射性损失。结论固相柱水解和IC-H柱中和法自动化合成18F-FDG,方法简单高效。
Objective To develop a new base hydrolysis and neutralization with IC-H carcridge method on solid phase cartridge for automatic preparation of xs F-FDG and analyze the loss of radioactive nuclide. Method The ^18F- was processed by azeotropic drying with anhydrous acetonitrile using hot air bath for two times. Subsequently triflate precursor was added at an air bath, and heated for 270s. The residue was cooled down with air bath. The labeled intermediate was trapped on a Cxs solid phase exchange cartridge using water, and hydrolyzed by NaOH at room temperature. The XSF-FDG was collected in a product bottle after it was neutralized with IC-H cartridge and purified with AluminN, an C18 cartridge. Results The radiochemical yield was （66. 9 ±4. 0）% [ n = 15, end of synthesis（EOS） ]. After it was checked by radio-TLC, the pH of XSF-FDG was about 6. 0 and the radiochemical purity was higher than 98%. Conclusion The base hydrolysis method on solid phase cartridge for automatic preparation of ^18F- FDG is simple with high yield.
出处
《国际药学研究杂志》
CAS
2008年第1期1-3,17,共4页
Journal of International Pharmaceutical Research
