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Simplified and reproducible radiochemical separations for the production of high specific activity ~(61)Cu, ~(64)Cu, ~(86)Y and ~(55)Co

机译:用于生产高比活性〜(61)Cu,〜(64)Cu,〜(86)Y和〜(55)Co的简化和可再现的放射化学分离

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摘要

Four positron-emitting radiometals ~(61)Cu, ~(64)Cu, ~(86)Y and ~(55)Co are increasingly being employed as labels for positron emission tomography (PET) imaging due to their favorable half-lives that match the pharmacokinetics of targeting moeities such as peptides, antibodies and antibody fragments and due to their use in internal dosimetry and treatment planning of targeted radionuclide therapy when they are substituted by their therapeutic analogues ~(67)Cu, ~(90)Y and ~(58m)Co. The main disadvantage of the production methods reported in the literature for these radionuclides is that the final separated radioactive product is diluted in a large volume (> 5 mL), which obligates a lengthy evaporation step in a large vessel that is difficult to automate in-line after the chromatographic steps and that results in a highly variable amount of radioactivity lost in the vessel's surface. In this work we present simplified radiochemical separation methods for the production of ~(61)Cu, ~(64)Cu, ~(86)Y and ~(55)Co that result in: 1) a final eluate volume ≤ 600 μL; 2) reproducible separation yields of 84± 4%, 82±6%, 94±5% and 93±6%, respectively; and 3) effective specific activities of 64.0±45.0 GBq/μmol NOTA, 114.9±40.1 GBq/μmol NOTA, 1.4±0.5 GBq/μmol DTPA and 10.1±5.7 GBq/μmol NOTA, respectively; without compromising the recycling efficiencies of the respective isotopically-enriched target materials ~(60)Ni, ~(64)Ni, ~(86)SrCO_3 and ~(58)Ni, which accounted for 98±1%, 96±3%, 90±3% and 94±1%, respectively.
机译:四个正电子发光辐射摩〜(61)Cu,〜(64)Cu,〜(86)Y和〜(55)CO越来越多地被用作正电子发射断层摄影(PET)成像的标签,这是由于它们有利的半衰期匹配靶向萌发的药代动力学,例如肽,抗体和抗体片段,并且由于它们在内部剂量测定和靶向放射性核素治疗的治疗计划中使用时,当它们被其治疗性类似物取代时,〜(67)Cu,〜(90)Y和〜 (58米)有限公司。在这些放射性核素的文献中报道的生产方法的主要缺点是最终分离的放射性产物在大体积(> 5mL)中稀释,这诱导难以自动化的大容器中的冗长蒸发步骤 - 在色谱步骤之后的线,这导致容器表面中的高度可变放射性量。在这项工作中,我们提出了用于制备〜(61)Cu,〜(64)Cu,〜(86)Y和〜(55)Co的简化放射化学分离方法,其导致:1)最终洗脱体积≤600μL; 2)分别可再现分离产率为84±4%,82±6%,94±5%和93±6%; 3)有效的特定活动64.0±45.0GBQ /μmolNota,114.9±40.1GBQ /μmolNota,分别为1.4±0.5GBq /μmolDTPA和10.1±5.7GBQ /μmolNota;在不影响各种同位素富集的靶材料的再循环效率〜(60)Ni,〜(64)Ni,〜(86)Srco_3和〜(58)Ni,其占98±1%,96±3%,分别为90±3%和94±1%。

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