^(125)I-RGD-4CY体内生物学分布与药物代谢动力学研究  

Studies on distribution and pharmacokinetics of ^(125)I-RGD-4CY in vivo

作　　者：郑秀海[1] 董家鸿[1] 李前伟[1] 张广运[1] 王曙光[1] 

机构地区：[1]第三军医大学西南医院全军肝胆外科研究所

出　　处：《消化外科》2004年第6期443-445,共3页Journal of Digestive Surgery

摘　　要：目的　研究12 5I标记的整合素αVβ3 拮抗多肽 (12 5I RGD 4CY)在小鼠体内的生物学分布及药物代谢动力学。方法　应用Iodogen法行12 5I标记RGD 4CY多肽 ,经小鼠尾静脉注射给药 ,分别在10、30、6 0、12 0和 2 4 0min不同时相点测量血液及各主要组织器官的放射性浓度 ,计算获得其体内生物学分布与药物代谢动力学数据。结果　RGD 4CY能够被12 5I有效标记 ;给药后在血液、肾脏、肝脏有较高的放射性分布 ,小肠、肺脏、肌肉呈低水平放射性分布 ;其分布相半衰期为 9.17min ,消除相半衰期为831min。结论　静脉注射12 5I RGD 4CY后 ,组织本底能够在较短的时间内达到低水平 ,血药浓度一时间曲线符合二房室模型特征 ,在体内的分布与消除为一级线性动力学过程。Objective To investigate the distribution and pharm acokinetics of 125I-RGD-4CY in mice. Methods RGD-4CY was labelled with 125I by Iodogen me thod. The drug was given via vein of mice tail, its radioactive concentration in blood and main organs were determined after 10, 30, 60, 120 and 240 min. The di stribution data and pharmacokinetics parameters in vivo were calculated. Results RGD-4CY could be labelled with 125I effectiv ely. After intravenous injection, higher radioactivity was found in blood, kidne y and liver, lower radioactivity in small intestine, lung and muscle. T 1/2α =9.17 min, t 1/2β=831 min. Conclusions After intravenous injection of 125I-RGD -4CY, the radioactivity in normal tissues can attain a lower background in shor ter time. The pharmacokinetics of the drug is in accordance with the feature of two atrioventricular model, and the distribution and clearance is a grade 1 line ar kinetic process.

关 键 词：RGD肽 ^125I标记 药物代谢动力学 

分 类 号：R96[医药卫生—药理学]