优化18F-FHBG自动化合成方法及其质量评估

目的 优化¹⁸F-FHBG的合成方法，并评估合成¹⁸F-FHBG的质量稳定性。方法 自行设计¹⁸F-FHBG自动化合成流程，待前体N₂-（对甲氧苯基二苯基甲基）-9-（4-甲苯磺酰基）-3-对甲氧苯基二苯基甲氧基-甲基丁基]鸟嘌呤与¹⁸F^-发生亲核取代反应后，经洗脱、纯化获得¹⁸F-FHBG。记录合成时间，评估合成效率，测定产品放射化学纯度及其体外稳定性，观察其生物分布及PET/CT显像特征。结果 ¹⁸F-FHBG的合成时间为19~25 min，未校正合成效率为（19.00±5.00）%（n>10）；室温放置5、30、60、90、120 min及6 h后，放射化学纯度均>97%。生物分布实验结果显示，¹⁸F-FHBG主要分布于正常昆明小鼠的肝脏、胃肠道及肾脏，脑组织内摄取较少。PET/CT显像结果显示，对新西兰大白兔注射¹⁸F-FHBG后，放射性分布遍及全身较快，注射60 min时显像效果较好。结论 优化的全自动合成方法能快速、高效合成纯度高、稳定性好的¹⁸F-FHBG，适用于PET/CT全身显像。

Optimization of 18F-FHBG automated synthesis method and quality assessment

Objective To optimize the synthesis method of ¹⁸F-FHBG, and to investigate the quality stability of the synthesized ¹⁸F-FHBG. Methods The automated synthesis process of ¹⁸F-FHBG was self-designed, and the N₂-(p-methoxyphenyldiphenylmethyl)-9-(-3-p-methoxyphenyl diphenylmethoxy) was directly labeled with ¹⁸F^- by the nucleophilic reaction, then ¹⁸F-FHBG product was obtained by elution and purification. The synthesized time was recorded. The synthesis efficiency, radiochemical purity and the stability of the products were evaluated. The biodistribution of ¹⁸F-FHBG and the specificity of imaging characteristics were also observed, respectively. Results The synthesis time of ¹⁸F-FHBG was 19-25 min, the uncorrected synthesis efficiency was (19.00±5.00)% (n>10), and the radiochemical purity was all >97% after 5, 30, 60, 90, 120 min and 6 h at room temperature. The results of biodistribution experiments showed that ¹⁸F-FHBG was mainly distributed in normal Kunming mice in the liver, gastrointestinal tract and kidney, and the brain tissue was less ingested. PET/CT imaging showed that after injection of ¹⁸F-FHBG into New Zealand white rabbits, the radioactivity distribution was faster throughout the body, and the imaging effect was good at 60 min. Conclusion The optimized automatic synthesis method can quickly and efficiently synthesize ¹⁸F-FHBG with high purity and stability, which is suitable for PET/CT whole body imaging.