Acta Chimica Sinica ›› 2021, Vol. 79 ›› Issue (11): 1376-1384.DOI: 10.6023/A21060266 Previous Articles     Next Articles



陈德胜a,b,d, 刘葳豪c, 黄清钢a,b, 曹石巍a,b, 田伟a,b, 殷小杰a,b, 谈存敏a,b, 王洁茹a,b,d,e, 初剑a,d, 贾子萌a,d, 程念炜e, 高瑞勤a,b, 吴晓蕾a,b, 秦芝a,b,*(), 范芳丽a,b, 白静a,b, 李飞泽c, 廖家莉c, 杨远友c, 刘宁c   

  1. a 中国科学院近代物理研究所 兰州 730000
    b 先进能源科学与技术广东省实验室 惠州 516000
    c 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
    d 中国科学院大学 核科学与技术学院 北京 100049
    e 兰州大学 核科学与技术学院 兰州 730000
  • 投稿日期:2021-06-11 发布日期:2021-08-17
  • 通讯作者: 秦芝
  • 基金资助:

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

Desheng Chena,b,d, Weihao Liuc, Qinggang Huanga,b, Shiwei Caoa,b, Wei Tiana,b, Xiaojie Yina,b, Cunmin Tana,b, Jieru Wanga,b,d,e, Jian Chua,d, Zimeng Jiaa,d, Nianwei Chenge, Ruiqin Gaoa,b, Xiaolei Wua,b, Zhi Qina,b(), Fangli Fana,b, Jing Baia,b, Feize Lic, Jiali Liaoc, Yuanyou Yangc, Ning Liuc   

  1. a Institute of Modern Physics, Chinese Academy of Sciences, Lanzhou 730000, China
    b Advanced Energy Science and Technology Guangdong Laboratory, Huizhou 516000, China
    c Key Laboratory of Radiation Physics and Technology, Ministry of Education, Institute of Nuclear Science and Technology, Sichuan University, Chengdu 610064, China
    d School of Nuclear Science and Technology, University of Chinese Academy of Sciences, Beijing 100049, China
    e School of Nuclear Science and Technology, Lanzhou University, Lanzhou 730000, China
  • Received:2021-06-11 Published:2021-08-17
  • Contact: Zhi Qin
  • Supported by:
    Special Fund for Scientific and Technological Innovation and Development of Gansu Province of China

211At, 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 211At is limited by 210At, because 210At decays to produce long half-life (138.4 d) extremely toxic daughter 210Po. The production of 211At via 209Bi(α,2n) nuclear reaction and 210At via 209Bi(α,3n) nuclear reaction, as the energy of incident α-particle increases, the ratio of N(210At)/N(211At) increases. In this research, the α-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 211At produced was studied systematically, including accelerator irradiation, separation by dry distillation method, quality analysis, and monoclonal antibody labeling. The bismuth targets were irradiated with α-particle by 28.18, 28.34, 28.48 28.92 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 211At was blow dry with nitrogen. The results showed that the total recovery of dry distillation separation of 211At reached 78.53%. After separation, the quality analysis of 211At was performed using a high-purity Ge-detector, alpha energy spectrometer, and mass spectrometer. The obtained solid 211At 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(211At) was less than 10–5 when the incident particle energy is below 28.2 MeV. Finally, the labeling of 211At-nimotuzumab was realized through N-succinimidyl-3-(trimethylstannyl)benzoate, and the labeling rate was 94.86%. Based on this research, a set of simple and efficient separation methods was established, which laid a good foundation for the subsequent production and application of 211At in China.

Key words: accelerator, medical isotope, dry distillation method, 211At, labeling