摘要
本文目的是建立125I标记重组人血小板生成素(125I-rhTPO)的分析方法并研究大鼠单剂量静脉注射125I-rhTPO后的药动学特性。以Iodogen法制备I-rhTPO,HPLC法及SDS-PAGE法鉴定并测定放化纯度。125大鼠按2μg·kg-1剂量经尾静脉给药,于不同时相取血测放射性计数,并计算相应的血药浓度及药动学参数。制备的I-rhTPO符合药动学研究要求,标记前后化合物所在电泳位置一致,放化纯度>98%,4℃100h后125放化纯度仍大于95%。尾静脉注射2μg·kg-1,在大鼠体内可以二室模型拟合血药浓度的动态变化,T1/2(α)为(1.32±0.35)h,T1/2(为(24.55±1.07)h,AUC0β)→t为(134.26±22.99)ng·h·mL-1。Iodogen法制备125I-rhTPO,经SDS-PAGE检验,标记后的I-rhTPO与rhTPO的纯度、分子量相当,且I-rhTPO在体外稳定性较好。尾125125静脉注射2μg·kg-1,在大鼠体内可以二室模型拟合,半衰期约为25h。
Purpose of this work is to establish the analytic method and investigate the pharmacokinetics of 125I-rhTPO in rats receiving single injection of vein. 125I-rhTPO was prepared with Iodogen method. The radiochemical purity of 125I-rhTPO was determined both by HPLC and SDS- PAGE. In the test, 125I-rhTPO was injected via caudal vein at the dose of 2 μg·kg-1 in rats. Blood samples were collected at different time after i.v., then the drug concentration was determined according to the radioactivity and the pharmacokinetic parameters were calculated. It is shown that radiochemical purity of 125I-rhTPO was above 98%, and the pharmacokinetics of 125I-rhTPO following i.v. with 2 μg·kg-1 in rats was fit to two-compartment model. The T1/2( was (1.32±0.35) h, T1/2 α) ( ) β was (24.55±1.07) h and AUC0 →t was (134.26±22.99) ng·h·mL-1. 125I-rhTPO prepared with Iodogen method was accordant with original rhTPO at purity and molecular weight by SDS PAGE test. The stability of 125I-rhTPO was good in vitro. Half -lives were about 25 h.
出处
《核技术》
CAS
CSCD
北大核心
2005年第1期54-56,共3页
Nuclear Techniques
