^(225)Ac-^(213)Bi发生器的制备与使用

Preparation and use of the 225Ac-213Bi generator

目的:构建简便可用的^(225)Ac-^(213)Bi发生器,为研发靶向α治疗药物提供短半衰期α核素^(213)Bi。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^(213)Bi进行纯度分析,验证使用活度计对^(225)Ac与^(213)Bi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^(225)Ac、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^(225)Ac-^(213)Bi发生器,通过注射盐酸淋洗获得^(213)Bi;获得^(213)Bi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^(R)活度计刻度号#086和#018可用于测量^(225)Ac和^(213)Bi活度,平均测量误差分别为-2.6%和+0.2%。^(225)Ac-^(213)Bi发生器使用2 mol/L盐酸作为淋洗液,320μl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^(225)Ac-^(213)Bi发生器可制备^(213)Bi用于靶向α治疗。

Objective To develop radiopharmaceuticals for targeted alpha therapy(TAT),a simple and useful^(225)Ac-^(213)Bi generator was developed to provide a short half-lifeα-emitter^(213)Bi.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.Theγspectrometer was used to determine the purity of the eluted^(213)Bi and verify the method to measure the radioactivity of^(225)Ac and^(213)Bi 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^(225)Ac,100 mg DIPEX resin and a Sep-Pak Alumina N Plus Light Cartridge column,a^(225)Ac-^(213)Bi generator with a column volume of 0.35 ml was constructed,which could be eluted^(213)Bi with a syringe drenched with hydrochloric acid.The produced^(213)Bi 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^(225)Ac and^(213)Bi with the average errors of-2.6%and+0.2%respectively.The eluent for the^(225)Ac-^(213)Bi generator was 2 mol/L hydrochloric acid,of which 320μl was required only to get 90%elution yield.The generator was recommended to be stored directly in the eluent to avoid drying.Conclusion The^(225)Ac-^(213)Bi generator can be constructed to obtain^(213)Bi for TAT.