CAJ | 학술논문

目的：探讨新型分子探针99 m Tc－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 m Tc－RRL，在健康小鼠体内进行99 m Tc－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 kBq? 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） mL? 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 m Tc－RRL 48 h内，小鼠无不良反应与死亡发生。结论99 m Tc－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。
목적：탐토신형분자탐침99 m Tc－RRL적약대동역학급급성독성작용。방법용일보법제비분자탐침99 m Tc－RRL，재건강소서체내진행99 m Tc－RRL적생물분포특성연구급소서체내급성독성실험，이급재건강백토체내진행99 mTc－RRL적약대동역학。결과99 mTc－RRL표기솔위（76．9±4．5）％，방사성화학순도체96％이상，비활도체1480 kBq? mg－1이상。시종제체내분포부합권중위1／c2적삼실모형，쾌분포상반쇠기、만분포상반쇠기급소제상반쇠기분별위（2．04±1．53）、（19．50±7．07）、（361．30±187．90） min，청제솔위（2．03±0．41） mL? min－1。시종제재혈액중청제신속，주요통과신배설，기여조직기관방사성균수시간축점강저，주사99 m Tc－RRL 48 h내，소서무불량반응여사망발생。결론99 m Tc－RRL구유이상적조직분포특점，무급성독성작용，시일충용우인체비교이상적종류분자현상제。
Objective To evaluate the pharmacokinetics and acute toxicity of RRL(Arg-Arg-Leu) molecular probe labeled with technetium-99 m (99 mTc-RRL).Methods 99 m Tc -RRL was prepared by one -step method.Biodistribution, and the acute toxicity test of 99 m Tc -RRL in mice and pharmacokinetics in health rabbits were performed. Results Labeling efficiencies of 99 m Tc-RRL reached (76.9 ±4.5)%. The radiochemical purity was above 96%, and the specific activity was up to 1480 kBq? mg -1 .Its dynamics in rabbits conformed to the three-compartment model with the weight of 1/c2 , and the main parameters were as follows: fast distribution phase half-life, slow distribution and elimination half -life phase half -life were ( 2.04 ± 1.53 ) , (19.50 ±7.07) and ( 361.30 ±187.90 ) min respectively, clearance was (2.03 ±0.41) mL? min-1.The pharmacokinetics and distribution results showed that the peptide could be quickly cleared from blood in healthy animals and distributed more in the kidney, and the other organs and tissue were decreased gradually.Conclusion The results demon-strated that 99 m Tc-RRL had a ideal tissue distribution and no acute toxicity, suggesting its development as a potential tumor imaging agent.