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放射性核素标记多肽在肿瘤诊断和治疗中具有巨大的潜在应用前景。用 Re 以柠檬酸和酒石酸的混合物为转换络合剂直接标记 188Lanreotide,研究了 Re-Lanreotide 的标记条件、体外稳定性及动 188物实验,建立了 Re-Lanreotide 的质量控制方法。 实验结果表明, 188在 pH 2～3 和 60 ℃反应 40 min,标记率为 88%～94%,经 Sep-PakC18 反相萃取柱纯化后放射化学纯度大于 95%。188Re-Lanreotide 血清除快,经肝胆排出体外,肠和肺的摄取量较高。
Radionuclide labeled peptides have great potential applications in tumor diagnosis and treatment. Re-Lanreotide was labeled with 188Lanreotide directly by using a mixture of citric acid and tartaric acid as the conversion complex. Re-Lanreotide labeling conditions, in vitro stability and kinetics were studied. The quality control method of Re-Lanreotide was established. The experimental results showed that 188 was labeled with 88% ~ 94% at pH 2 ~ 3 and 60 ℃ for 40 min, and the radiochemical purity of 188 was more than 95% after purification by Sep-Pak C18 reversed-phase extraction column. 188Re-Lanreotide serum in addition to fast, excreted by the liver and gallbladder, intestinal and pulmonary uptake.