同位素 ›› 2020, Vol. 33 ›› Issue (2): 110-116.DOI: 10.7538/tws.2018.youxian.088

• 放射性药物与标记化合物 • 上一篇    下一篇

11C/18F-乙酸盐在CFN-MPS200上的自动合成

程亮;陈尚东;崔夫新;刘丹;何爽;朴永男   

  1. 沈阳化工大学 应用化学学院,沈阳110142;北京安迪科电子有限责任公司,北京100021;延边大学附属医院 核医学科, 延吉133000
  • 出版日期:2020-04-20 发布日期:2020-04-24

Automatic Synthesis of 11C-Acetate and 18F-Acedate on CFN-MPS200 Synthesizer

CHENG Liang;CHEN Shangdong;CUI Fuxin;LIU Dan;HE Shuang;PIAO Yongnan   

  1. Applied Chemistry Department, Shenyang University of Chemical Technology, Shenyang 110142, China;Beijing Advance Medical Systems Limited, Beijing 100021,China;The Affiliated Hospital of Yanbian University PET-CT Center, Yanji 133000, China
  • Online:2020-04-20 Published:2020-04-24

摘要:

采用CFN-MPS200多功能合成模块分别进行11C-乙酸盐(11C-Acetate)和18F-乙酸盐(18F-Acatate)合成,并用TLC法和HPLC法进行质量分析。将11CO2释放到1.0 mol/L甲基溴化镁的四氢呋喃溶液中,2 min后用1 mol/L盐酸水解,反应液经ON Guard-Ag、ON Guard-H柱纯化后,再经PS-OH柱吸附,用生理盐水淋洗,最后由CM柱纯化并经无菌滤膜过滤得到11C-乙酸盐;合成时间约为10 min,不校正放化合成产率(53.5±5)%(n=6)。18F与溴代乙酸苄酯发生取代反应,经C-18柱吸附去除杂质后洗脱,碱水解后经IC-H、PS-2、氧化铝柱纯化后通过无菌滤膜得到产品18F-乙酸盐;合成时间为40 min,不校正放化合成产率(20.2±5)%(n=5)。分别对两类化合物进行TLC和HPLC分析,以95%乙腈水溶液(VV)为TLC的展开剂,比移值Rf分别为0.31 min与0.60 min,放化纯度大于99%;HPLC进样质控,紫外检测器和放射性检测器的出峰时间均在2.3~2.4 min之间,化学纯度和放化纯度大于99%。11C-乙酸盐和18F-乙酸盐的合成均由CFN-MPS200多功能合成模块自动合成,过程简单,合成产率稳定,放化纯度和化学纯度高,可以满足临床使用。

关键词: 11C-乙酸盐, 18F-乙酸盐, CFN-MPS200合成模块, 自动化合成

Abstract:

The synthesis of 11C-acetate and 18F-acetate was carried out by CFN-MPS200 multi-functional synthesizer, and the quality control comparison analysis was obtianed by TLC method and HPLC method. 11CO2 was released into 1.0 mol/L methylmagnesium bromide in THF solution. After 2 min, it was hydrolyzed with 1 mol/L hydrochloric acid. The reaction solution was purified by ON Grad-Ag and ON Grad-H column, and then adsorbed by PS-OH column. The saline was rinsed, and finally purified by a CM column and filtered through a sterile filter to obtain 11C-acetate. The synthesis time was about 10 min, and the EOS%=(53.5±5)%(n=6). Substitution reaction of 18F- with benzyl bromide, the impurities were removed by adsorption on a C-18 column, eluted by alkali hydrolysis, purified by IC-H, PS-2, alumina column and subjected to sterile filtration to obtain product 18F- Acetate. The synthesis time was 40 min, and the EOS%=(20.2±5)%(n=5). The TLC and HPLC quality control analysis of the two types of acetate compounds were carried out. The 95% (VV) acetonitrile aqueous solution was used as the developing agent of TLC, the Rf values were 0.31 min and 0.60 min, respectively, and the radiochemical purity was more than 99%. With HPLC injection quality control, the peak time of the UV detector and the radioactivity detector is between 2.3-2.4 min, and the chemical purity and radiochemical purity are greater than 99%.The synthesis of 11C-Acetate and 18F-Acetate is automatically synthesized by CFN-MPS200 synthesizer, without human intervention, the synthesis process is simple, the synthesis yield is stable. Radiochemical purity and chemical purity are high, which can meet the clinical requirements.

Key words: 11C-acetate, 18F-acetate, CFN-MPS200 synthesizer, automated synthesis