ICNAS Producao Unipessoal, Lda., Ed. ICNAS, Polo das Ciencias da Saude, University of Coimbra, Coimbra, Portugal.
CIBIT/ICNAS - Institute for Nuclear Sciences Applied to Health, University of Coimbra, Coimbra, Portugal.
Curr Radiopharm. 2021;14(4):420-428. doi: 10.2174/1874471013666201112141844.
Expanding the range of metal-based PET radiopharmaceuticals that can be produced by the widely available network of biomedical cyclotrons is a major priority. Copper- 61 is a positron emitter with very favourable physical (61.5% β+, 1.22 MeV max.) and chemical properties, which emerged as a promising PET imaging agent.
This work aimed to develop and optimise a GMP-automated purification method for copper-61 produced in a cyclotron using a natural zinc liquid target.
The automated purification process was performed using a commercially available Synthera ® Extension module (IBA, Louvain-la-Neuve, Belgium) using a three-column method: two extraction chromatographic resins and a strong anion exchange resin. The final product was evaluated using HPGe and ICP-MS analysis, to assess the radionuclidic and chemical purity of the final copper- 61 solution.
The automated purification process was completed within 1 h of processing time, with an average yield of 63.0 ± 15.0%, in a maximum volume of 5 mL. The radionuclidic purity of copper- 61 in the final solution was over 95% for 7 h after EOB. ICP-MS analysis revealed 4.8 ± 2.4 μg of natural zinc in the final purified sample, and the copper-61 molar activity was 230.5 ± 139.3 GBq/μmol.
The described purification process allows for the production of a highly radionuclidically and chemically pure, GMP compliant copper-61 solution, ready to be used for the development of copper-61 based radiopharmaceuticals for routine clinical use.
扩大可通过广泛应用的生物医学回旋加速器网络生产的基于金属的正电子发射断层扫描（PET）放射性药物的范围是一个主要重点。铜-61 是一种正电子发射体，具有非常有利的物理（61.5%β+，最大 1.22 MeV）和化学性质，已成为一种很有前途的 PET 成像剂。
本工作旨在开发和优化一种使用天然锌液体靶在回旋加速器中生产的铜-61 的 GMP 自动化纯化方法。
使用市售的 Synthera ® Extension 模块（IBA，Louvain-la-Neuve，比利时）通过三柱法进行自动化纯化过程：两种萃取色谱树脂和一种强阴离子交换树脂。使用 HPGe 和 ICP-MS 分析评估最终产品，以评估最终铜-61 溶液的放射性核纯度和化学纯度。
在处理时间为 1 h 内完成了自动化纯化过程，在最大体积为 5 mL 时，平均产率为 63.0±15.0%。在 EOB 后 7 h 内，最终溶液中铜-61 的放射性核纯度超过 95%。ICP-MS 分析显示，最终纯化样品中含有 4.8±2.4μg的天然锌，铜-61 的摩尔活度为 230.5±139.3GBq/μmol。
所描述的纯化过程可生产出高放射性核纯度和化学纯度的 GMP 合规铜-61 溶液，可用于开发常规临床应用的基于铜-61 的放射性药物。
