加速器生产医用同位素^(211)At及单抗标记  

Accelerator Production of the Medical Isotope ^(211)At and Monoclonal Antibody Labeling

作　　者：陈德胜 刘葳豪 黄清钢 曹石巍 田伟[1,2] 殷小杰 谈存敏[1,2] 王洁茹 初剑[1,4] 贾子萌 程念炜[5] 高瑞勤 吴晓蕾 秦芝 范芳丽 白静 李飞泽[3] 廖家莉 杨远友[3] 刘宁 Desheng Chen;Weihao Liu;Qinggang Huang;Shiwei Cao;Wei Tian;Xiaojie Yin;Cunmin Tan;Jieru Wang;Jian Chu;Zimeng Jia;Nianwei Cheng;Ruiqin Gao;Xiaolei Wu;Zhi Qin;Fangli Fan;Jing Bai;Feize Li;Jiali Liao;Yuanyou Yang;Ning Liu(Institute of Modern Physics,Chinese Academy of Sciences,Lanzhou 730000,China;Advanced Energy Science and Technology Guangdong Laboratory,Huizhou 516000,China;Key Laboratory of Radiation Physics and Technology,Ministry of Education,Institute of Nuclear Science and Technology,Sichuan University,Chengdu 610064,China;School of Nuclear Science and Technology,University of Chinese Academy of Sciences,Beijing 100049,China;School of Nuclear Science and Technology,Lanzhou University,Lanzhou 730000,China)

机构地区：[1]中国科学院近代物理研究所,兰州730000 [2]先进能源科学与技术广东省实验室,惠州516000 [3]四川大学,原子核科学技术研究所,辐射物理及技术教育部重点实验室,成都610064 [4]中国科学院大学核科学与技术学院,北京100049 [5]兰州大学核科学与技术学院,兰州730000

出　　处：《化学学报》2021年第11期1376-1384,共9页Acta Chimica Sinica

基　　金：甘肃省引导科技创新发展专项资金资助项目.

摘　　要：^(211)At,半衰期7.2 h,发射的α粒子具有很高的线性传能密度,是一种理想的靶向α治疗核素.利用中国科学院近代物理研究所强流超导直线加速器提供的α束流辐照Bi靶生产^(211)At,系统考察了加速器生产^(211)At的整个流程,包括加速器辐照、干蒸馏分离、质量分析以及单抗标记.研究结果表明,干蒸馏分离^(211)At的总收率最高达78.53%,获得的固体^(211)At产品具有极高的比活度、核纯度以及化学纯度,其中杂质元素Bi、Cu、Zn、Al含量均低于100 ng/GBq,且入射粒子能量低于28.2 MeV时,N(210At)/N(^(211)At)值低于10-5,研究也实现了^(211)At在尼妥珠单抗上的标记,标记率高达94.86%.基于以上研究我们确立了一套简单、高效的分离方法,为后续我国^(211)At的生产和应用奠定了良好基础.^(211)At,with a half-life of 7.2 h,is an excellent radionuclide being investigated for use in targeted alpha therapy as the result of very high linear energy transfer.However,the production of ^(211)At is limited by 210At,because 210At decays to produce long half-life(138.4 d)extremely toxic daughter 210Po.The production of ^(211)At via 209Bi(α,2n)nuclear reaction and 210At via 209Bi(α,3n)nuclear reaction,as the energy of incidentα-particle increases,the ratio of N(210At)/N(^(211)At)increases.In this research,theα-particle is provided by the Chinese Accelerator Driven Sub-critical System(ADS)Front-end Demo Linac at Institute of Modern Physics,Chinese Academy of Sciences.The technical process of ^(211)At produced was studied systemat-ically,including accelerator irradiation,separation by dry distillation method,quality analysis,and monoclonal antibody la-beling.The bismuth targets were irradiated withα-particle by 28.18,28.34,28.4828.92 MeV,and the target chamber adopts an inclined target with water cooling to improve the cooling effect.The dry distillation separation was carried out at a high temperature of 850℃,oxygen as the carrier gas,chloroform and ethanol as eluent,and the chloroform solution containing ^(211)At was blow dry with nitrogen.The results showed that the total recovery of dry distillation separation of ^(211)At reached 78.53%.After separation,the quality analysis of ^(211)At was performed using a high-purity Ge-detector,alpha energy spec-trometer,and mass spectrometer.The obtained solid ^(211)At had high specific activity,radionuclide purity and chemical purity,where the content of impurity elements Bi,Cu,Zn,and Al was less than 100 ng/GBq,and the ratio of N(210At)/N(^(211)At)was less than 10-5 when the incident particle energy is below 28.2 MeV.Finally,the labeling of ^(211)At-nimotuzumab was realized through N-succinimidyl-3-(trimethylstannyl)benzoate,and the labeling rate was 94.86%.Based on this research,a set of sim-ple and efficient separation methods was established,which laid a goo

关 键 词：加速器 医用同位素 干蒸馏法 ^(211)At 标记 

分 类 号：TL921.1[核科学技术—核燃料循环与材料]