11C/18F-乙酸盐在CFN-MPS200上的自动合成

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

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(V∶V)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。

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%(V∶V)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.