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目的探讨新型分子探针99 mTc-RRL的药代动力学及急性毒性作用。方法用一步法制备分子探针99 mTc-RRL,在健康小鼠体内进行99 mTc-RRL的生物分布特性研究及小鼠体内急性毒性实验,以及在健康白兔体内进行99 mTc-RRL的药代动力学。结果99 mTc-RRL标记率为(76.9±4.5)%,放射性化学纯度达96%以上,比活度达1480 k Bq·mg-1以上。示踪剂体内分布符合权重为1/c2的三室模型,快分布相半衰期、慢分布相半衰期及消除相半衰期分别为(2.04±1.53)、(19.50±7.07)、(361.30±187.90)min,清除率为(2.03±0.41)m L·min-1。示踪剂在血液中清除迅速,主要通过肾排泄,其余组织器官放射性均随时间逐渐降低,注射99 mTc-RRL 48 h内,小鼠无不良反应与死亡发生。结论99 mTc-RRL具有理想的组织分布特点,无急性毒性作用,是一种用于人体比较理想的肿瘤分子显像剂。
Objective To investigate the pharmacokinetics and acute toxicity of 99mTc-RRL. Methods The 99mTc-RRL molecular probe 99mTc-RRL was prepared by one-step method. The biodistribution of 99mTc-RRL was studied in healthy mice and the acute toxicity test in mice, and the pharmacokinetics of 99mTc-RRL in healthy rabbits dynamics. Results The 99mTc-RRL labeling rate was (76.9 ± 4.5)%, the radiochemical purity was over 96% and the specific activity was over 1480 kBq · mg-1. The distribution of tracer in vivo was in accordance with the three-compartment model with a weight of 1 / c2. The fast half-life, slow half-life and half-life of elimination phase were 2.04 ± 1.53, 19.50 ± 7.07 and 361.30 ± 187.90 min, respectively The rate was (2.03 ± 0.41) m L · min-1. Tracer cleared rapidly in the bloodstream and mainly excreted through the kidneys. The radioactivity of the remaining tissues and organs decreased gradually over time. No adverse reactions and death occurred in the mice within 48 h after injection of 99mTc-RRL. Conclusion 99 mTc-RRL has the ideal tissue distribution characteristics, no acute toxicity and is an ideal tumor molecular imaging agent for the human body.