| 陈俊艺,李银龙,王峰,张天爵,刘志博.化学通报,2021,84(11):1210-1218. |
| 基于100 MeV质子回旋加速器与固相萃取方法制备与纯化靶向放射治疗核素锕-225 |
| Production and isolation of actinium-225 with a 100 MeV proton cyclotron and solid-phase extraction for targeted radiotherapy |
| 投稿时间：2021-04-22 修订日期：2021-05-24 |
| DOI： |
| 中文关键词: 锕-225 固相萃取 靶向阿尔法粒子治疗 回旋加速器 |
| 英文关键词:Actinium-225, Solid-phase extraction, Targeted alpha therapy, Cyclotron |
| 基金项目:国家自然科学基金项目(U1867209,21778003)和国家重点研发计划项目(2017YFA0506300)资助 |
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| 中文摘要: |
| 锕-225可发射4个α粒子和2个β粒子,具有较高的传能线密度和局部肿瘤损伤,因此是靶向放射性核素治疗中受到最多关注的放射性核素之一。经典的锕-225是由铀-233衰变产生,或通过natTh(p,x)225Ac反应生产。但目前我国无论是233U来源或natTh来源的225Ac均无法供应。本研究中,我们基于国产CYCIAE-100高能强流回旋加速器实现了我国首次225Ac的加速器生产,获得了超过600 μCi的225Ac,足够2-3个病人的靶向核素治疗。同时我们设计并优化了全固相萃取的225Ac纯化流程,分离出的225Ac的放射性纯度在99.5%以上,该流程操作简便、高效、且可自动化,可随时用于225Ac的大规模生产。综上所述,我们成功地进行了225Ac的生产和分离的初步研究,为我国进一步发展225Ac供应链奠定基础,为我国学者和医生进行靶向α核素治疗提供了225Ac的额外选择。 |
| 英文摘要: |
| Actinium-225 emits four alpha particles and two beta particles and provides high linear energy transfer and localized tumor cell damage; therefore, it is one of the most attractive radionuclides for targeted radionuclide therapy. In general, actinium-225 is generated from uranium-233 decay or the natTh(p,x)225Ac reaction. However, this material is not available in China. Recently, we successfully overcame this bottleneck and performed the first cyclotron production of 225Ac in China. Over 600 μCi of 225Ac was produced, which is sufficient for 2-3 patient treatments. An optimized 225Ac purification protocol was developed; the radioactive purity of the isolated 225Ac is over 99.5%, and the operation is user-friendly and convenient for automation and could be readily used for the large-scale production of 225Ac. In summary, we successfully performed a pilot study on the production and isolation of 225Ac, demonstrating an alternative source of 225Ac for Chinese scholars and doctors for targeted alpha therapy. |
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