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225Ac- 213Bi发生器的制备与使用

Preparation and use of the 225Ac- 213Bi generator

摘要目的:构建简便可用的 225Ac- 213Bi发生器,为研发靶向α治疗药物提供短半衰期α核素 213Bi。 方法:以DIPEX树脂作为发生器固定相,采用Sep-Pak Alumina N Plus Light Cartridge小柱作为柱体构建发生器,以盐酸作为淋洗液。使用γ能谱对淋洗所得的 213Bi进行纯度分析,验证使用活度计对 225Ac与 213Bi活度进行测量的方法。研究不同浓度盐酸溶液及不同保存状态下发生器的洗脱曲线,确定最佳使用方案。 结果:使用商品化 225Ac、100 mg DIPEX树脂和Sep-Pak Alumina N Plus Light Cartridge小柱构建柱体积为0.35 ml的 225Ac- 213Bi发生器,通过注射盐酸淋洗获得 213Bi;获得 213Bi的γ能谱纯净,测定半衰期为(45.75±0.12) min,与理论值(45.6 min)一致。CRC ?活度计刻度号#086和#018可用于测量 225Ac和 213Bi活度,平均测量误差分别为-2.6%和+0.2%。 225Ac- 213Bi发生器使用2 mol/L盐酸作为淋洗液,320 μl淋洗体积可获得90%洗脱率;发生器应在淋洗溶液中保存,避免干燥。 结论:构建的 225Ac- 213Bi发生器可制备 213Bi用于靶向α治疗。

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abstractsObjective:To develop radiopharmaceuticals for targeted alpha therapy (TAT), a simple and useful 225Ac- 213Bi generator was developed to provide a short half-life α-emitter 213Bi. Methods:DIPEX resin was used as the stationary phase of the generator, a Sep-Pak Alumina N Plus Light Cartridge column was utilized as the column to construct the generator, and hydrochloric acid was used as the eluent. The γ spectrometer was used to determine the purity of the eluted 213Bi and verify the method to measure the radioactivity of 225Ac and 213Bi by using radioisotope calibrators. The elution curves of the generator at various settings were analyzed to find the best elute and storage conditions. Results:Using commercial 225Ac, 100 mg DIPEX resin and a Sep-Pak Alumina N Plus Light Cartridge column, a 225Ac- 213Bi generator with a column volume of 0.35 ml was constructed, which could be eluted 213Bi with a syringe drenched with hydrochloric acid. The produced 213Bi was pure, and the measured half-life was (45.75±0.12) min, which was consistent with the theoretical value (45.6 min). CRC ? calibrators with setting numbers of #086 and #018 could measure the activity of 225Ac and 213Bi with the average errors of -2.6% and + 0.2% respectively. The eluent for the 225Ac- 213Bi generator was 2 mol/L hydrochloric acid, of which 320 μl was required only to get 90% elution yield. The generator was recommended to be stored directly in the eluent to avoid drying. Conclusion:The 225Ac- 213Bi generator can be constructed to obtain 213Bi for TAT.

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