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目的:探索国产n 177Lu-前列腺特异膜抗原(PSMA)-617的最佳标记条件，研究其生物分布、稳定性及安全性。n 方法:手动合成国产n 177Lu-PSMA-617，确定最佳标记条件，检测其放化纯、体内外稳定性、脂水分配系数及血浆蛋白结合率；评价前列腺癌细胞22RV1对其的摄取率；设置进口n 177Lu-PSMA-617对照组，研究2种标记物在正常小鼠体内的生物分布及其SPECT/CT显像特点；通过测定小鼠血常规等，评估药物安全性。n 结果:国产n 177Lu-PSMA-617在pH值4.5、100 ℃恒温条件下反应30 min即可得到最佳标记结果，产物放化纯≥99%，72 h内放化纯仍>95%，体内外稳定性好。在体外的血浆蛋白结合率为(35.3±5.3)%,脂水分配系数为-2.27±0.06, 22RV1细胞对国产n 177Lu-PSMA-617的特异性摄取率在1 h达最高[(7.58±0.84)%]，略低于进口n 177Lu-PSMA-617，但差异无统计学意义[(7.86±0.96)%; n t＝-0.439, n P>0.05]。正常小鼠体内分布及显像表明，国产和进口n 177Lu-PSMA-617在血液清除速率相当，主要经肾排泄。两者毒性实验均未见明显不良反应，血常规、肝肾功能未见明显异常。n 结论:国产n 177Lu-PSMA-617质控合格，产物具有良好的生物学性能及安全性，在前列腺肿瘤的诊断中有潜在的应用价值。n “,”Objective:To synthesize n 177Lu-prostate-specific membrane antigen (PSMA)-617 with domestic n 177Lu (made in China), and explore its optimal labeling condition, biodistribution, stability, and safety.n Methods:177Lu-PSMA-617 was prepared with domestic n 177Lu by a manual method. The optimal labeling condition, radiochemical purity, stability (n in vivo and n in vitro), lipid-water partition coefficient, and plasma protein binding rate were determined. The uptake rate of n 177Lu-PSMA-617 was evaluated by using 22RV1 cells. Biodistribution and SPECT/CT imaging were performed on normal mice with imported n 177Lu-PSMA-617 as control group. The blood routine test was performed to evaluate the safety.n Results:The best labeling result of domestic n 177Lu-PSMA-617 can be obtained under the following conditions: pH=4.5, 100 ℃ for 30 min. And the radiochemical purity was ≥99%. The product was stable n in vivo and n in vitro, with the radiochemical purity >95% in 72 h. The plasma protein binding rate was (35.3±5.3)%, the lipid-water partition coefficient was -2.27±0.06, and the specific uptake rate of domestic n 177Lu-PSMA-617 by 22RV1 cells reached the highest in 1 h ((7.58±0.84)%), which was slightly lower than the imported n 177Lu-PSMA-617 ((7.86±0.96)%), but there was no significant difference between them (n t=-0.439, n P>0.05). The distribution and SPECT/CT imaging of normal mice showed that domestic and importedn 177Lu-PSMA-617 in blood were cleared quite fast, and both of them were excreted mainly through the kidneys. No obvious adverse reactions were found in the toxicity test of domestic and imported n 177Lu-PSMA-617. There was no obvious abnormality in blood routine and liver and kidney metabolism.n Conclusion:The domestic n 177Lu-PSMA-617 has many advantages, such as qualified quality control, good biological properties and safety, which support its potential application value in diagnosis of prostatic neoplasms.n