摘要
目的:应用AllinOne合成模块自动化合成雌激素受体(ER)显像剂16α-氟18(^(18)F)-17β-雌二醇(^(18)F-FES),为^(18)F-FES在临床中的进一步应用提供支持。方法:采用AllinOne合成模块,以3-O-(甲氧甲基)-16,17-O-磺酰基-16-表雌二醇(MMSE)为前体,与干燥后的^(18)F-发生亲核反应,再依次经酸水解及碱中和,经过高效液相色谱(HPLC)法分离并纯化后获得^(18)F-FES产品,并进行质量控制检测。结果:在^(18)F-FES的合成中,合成时间为70 min,6次合成不校正合成平均效率为(38.87±3.52)%,产品放射化学纯度>98%,无菌检测、细菌内毒素检测、异常毒性检测及残留溶剂乙腈含量检测结果均符合《中华人民共和国药典》(2020年版)要求。结论:应用AllinOne合成模块成功地自动化合成了ER受体显像剂^(18)F-FES,制备出的^(18)F-FES产品质量符合临床要求,为推动^(18)F-FES在临床上的应用提供了支持。
Objective:To apply AllinOne synthesis module in automatic synthesizing photographic developer 16α-Fluorine18(^(18)F)-17β-estradiol(^(18)F-FES)of estrogen receptor(ER)so as to provide support for the further application of ^(18)F-FES in clinical practice.Methods:AllinOne synthesis module was adopted,and 3-O-methoxymethyl-16,17-O-sulfuryl-16-epiestriol(MMSE)was used as the precursor to react with dried ^(18)F ion as nucleophilic reaction.And they underwent successively acid hydrolysis and neutralization with NaOH.And then,the high performance liquid chromatography(HPLC)was used to separate and purify the reaction mixture,and the ^(18)F-FES was obtained finally.The corresponding test of quality controls of the product ^(18)F-FES were performed.Results:In the synthesis of ^(18)F-FES,the synthesized time was 70 min,and synthesized average efficiency of 6 syntheses without rectification was(38.87%±3.52)%,radiochemistry purity of the product was over 98%.The results of sterility test,bacterial endotoxins test,abnormal toxicity test and the content of residual solvent acetonitrile all met the requirements of Chinese Pharmacopoeia(2020 Edition).Conclusion:The ER receptor photographic developer ^(18)F-FES was successfully automatically synthesized by using AllinOne synthesis module.The product quality of produced ^(18)F-FES meets the clinical requirements,which provides support for promoting the clinical application of ^(18)F-FES.
作者
黄政海
任超
霍力
HUANG Zheng-hai;REN Chao;HUO Li(HTA Co.,Ltd.,Beijing 102413,China;不详)
出处
《中国医学装备》
2022年第2期31-35,共5页
China Medical Equipment
基金
清华大学-北京协和医院合作课题(PTQH201906006)“PET/CT介导消融手术机器人关键技术研究及样机研制”。
