中国医疗前沿
中國醫療前沿
중국의료전연
CHINA HEALTHCARE INNOVATION
2013年
7期
8-11
,共4页
S-11C-甲基-L-半胱氨酸%正电子发射计算机断层显像%肿瘤显像
S-11C-甲基-L-半胱氨痠%正電子髮射計算機斷層顯像%腫瘤顯像
S-11C-갑기-L-반광안산%정전자발사계산궤단층현상%종류현상
S-11C-methyl-L-cysteine%Positron Emission Tomography%Tumor imaging
目的 S-11C-甲基-L-半胱氨酸是一种肿瘤显像剂,是11C-MET类似物,我们自行研制合成了11C-MCYS,并对其质量控制.方法由医用回旋加速器生产11CO2,11CO2通过11CH3I全自动合成系统转化为11C-碘代甲烷(11CH3I).11CH3I与前体L-半胱氨酸的碱性溶液在Sep-Pak Plus C18小柱上发生烷基化反应,经Sep-Pak Plus C18小柱分离,得到11C-MCYS.并对新制剂进行质量控制.结果回旋加速器生产的11CO2传输到11CH3I全自动合成模块,11CO2经氢化锂铝还原转化为11CH3OH,再经氢碘酸(HI)碘代法生产出11CH3I,11CO2转化为11CH3I的时间约为8-10min,未校正放化产率约60%-70%.11C-MCYS放化合成时间约为2min,放化纯度大于98%,总合成时间约12min.主要质量控制指标达到正电子放射性药物质量要求.结论11C-MCYS的合成操作简便,产品化学纯度、放化纯度、pH值都符合注射剂的要求,符合进一步的动物探索性研究要求.
目的 S-11C-甲基-L-半胱氨痠是一種腫瘤顯像劑,是11C-MET類似物,我們自行研製閤成瞭11C-MCYS,併對其質量控製.方法由醫用迴鏇加速器生產11CO2,11CO2通過11CH3I全自動閤成繫統轉化為11C-碘代甲烷(11CH3I).11CH3I與前體L-半胱氨痠的堿性溶液在Sep-Pak Plus C18小柱上髮生烷基化反應,經Sep-Pak Plus C18小柱分離,得到11C-MCYS.併對新製劑進行質量控製.結果迴鏇加速器生產的11CO2傳輸到11CH3I全自動閤成模塊,11CO2經氫化鋰鋁還原轉化為11CH3OH,再經氫碘痠(HI)碘代法生產齣11CH3I,11CO2轉化為11CH3I的時間約為8-10min,未校正放化產率約60%-70%.11C-MCYS放化閤成時間約為2min,放化純度大于98%,總閤成時間約12min.主要質量控製指標達到正電子放射性藥物質量要求.結論11C-MCYS的閤成操作簡便,產品化學純度、放化純度、pH值都符閤註射劑的要求,符閤進一步的動物探索性研究要求.
목적 S-11C-갑기-L-반광안산시일충종류현상제,시11C-MET유사물,아문자행연제합성료11C-MCYS,병대기질량공제.방법유의용회선가속기생산11CO2,11CO2통과11CH3I전자동합성계통전화위11C-전대갑완(11CH3I).11CH3I여전체L-반광안산적감성용액재Sep-Pak Plus C18소주상발생완기화반응,경Sep-Pak Plus C18소주분리,득도11C-MCYS.병대신제제진행질량공제.결과회선가속기생산적11CO2전수도11CH3I전자동합성모괴,11CO2경경화리려환원전화위11CH3OH,재경경전산(HI)전대법생산출11CH3I,11CO2전화위11CH3I적시간약위8-10min,미교정방화산솔약60%-70%.11C-MCYS방화합성시간약위2min,방화순도대우98%,총합성시간약12min.주요질량공제지표체도정전자방사성약물질량요구.결론11C-MCYS적합성조작간편,산품화학순도、방화순도、pH치도부합주사제적요구,부합진일보적동물탐색성연구요구.
Objective 11C-MCYS is a tumor imaging agent, as an analogue of 11C-MET. We expore the method and quality control of 11C-MCYS. Methods 11CO2 was produced by 14N(p,α)11C nuclear reactions, which was delivered to the radiochemical laboratory. 11CO2 was trapped and released into the synthesis module. Production of 11CH3I consisted of the reduction of 11CO2 with LiAlH4, hydrolysis of the intermediately formed organometallic complex and subsequent iodination of 11C-methanol with hydrogen iodide. 11CH3I was delivered to a Sep-Pak plus C18 cartridge previously loaded with a solution of L-cysteine(2-3mg) dissolved in NaOH 0.5mol/L in ethanol/water 50/50(v/v, 0.210ml). 11C-MCYS was eluted with NaH2PO4 0.05mol/L buffer(5ml, pH 3-4) and collected in a vented sterile vial. Contents and analytical methods of quality control for 11C-MCYS were investigated. Results 11CH3I was prepared routinely in our laboratories by utilizing a simple remotely controlled chemical module. The uncorrected radiochemical yield of 11CH3I was 60-70% from 11CO2 and the synthesis time was 8-10min after release of 11CO2. 11C-MCYS was prepared by adopting on-column methylation described above. The uncorrected radiochemical yield of 11C-MCYS was 60%-70%with the synthesis time of 2 min. The radiochemical purity of 11C-MCYS was above 98%, and the total synthesis time about 12 min. Conlusion It is easy to perform the automated synthesis of 11C-MCYS. All quality criteria of 11C-MCYS met the requirements of the positron radio-pharmaceuticals.
