中国临床药理学杂志Issue(16)：1610-1612,3.DOI:10.13699/j.cnki.1001-6821.2015.16.016
99mTc－RRL的药代动力学与急性毒性研究
Study on pharmacokinetics and acute toxicity of new molecular probe 99 m Tc-RRL
摘要
Abstract
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.关键词
多肽/肿瘤新生血管/体内生物分布/药代动力学/急性毒性Key words
peptide/tumor angiogenesis/biodistribution/pharmacokinetics/acute toxicity分类
医药卫生引用本文复制引用
姚宁,王荣福,闫平,张春丽,陈雪祺,郝攀,马超..99mTc－RRL的药代动力学与急性毒性研究[J].中国临床药理学杂志,2015,(16):1610-1612,3.基金项目
国家“十二五”支撑项目基金资助项目（2014BAA03B03）；国家自然科学基金资助项目（81071183）；国家重大科学仪器设备开发专项基金资助项目 （）
