酪丝缬肽在Beagle犬体内药动学初步研究  

Pharmacokinetics of Tyroservatide in Beagle Dogs after Single iv Injection

作　　者：孙迎基[1] 张峰国[1] 廖建民[1] 沈子龙[1] 

机构地区：[1]中国药科大学生物技术中心,江苏南京210009

出　　处：《药物生物技术》2007年第1期60-63,共4页Pharmaceutical Biotechnology

摘　　要：初步研究酪丝缬肽单次静注给药后在Beagle犬的体内过程。建立了酪丝缬肽在Beagle犬全血中浓度测定的RP-HPLC-UV方法。绘制酪丝缬肽单次给药后在Beagle犬体内全血药物浓度-时间曲线,并求得药动学参数。本检测方法灵敏度不高,最低定量限为0.20μg/ml。酪丝缬肽静注给药后在Beagle犬体内药动学符合单房室模型,低、中、高3个剂量(60,600,6000μg/kg)的T1/2分别为(8.88±1.45),(9.00±1.70),(11.12±2.83)s,无显著性差异,C10s和AUC与剂量成良好的线性关系。本实验初步表明:酪丝缬肽静注给药在Beagle犬体内的动力学行为是线性的。酪丝缬肽在Beagle犬体内快速消除,半衰期小于20s。To study the pharmacokinetics of Tyroservatide in Beagle dogs after single iv injection a RP- HPLC-UV method for determining Tyroservatide in blood was established. The concentration-time profile was described after single iv injection of Tyroservatide in Beagle dogs, and the pharmacokinetics parameters were calculated. The RP-HPLC-UV method doesn＇t have a good LOQ, which is 0. 20μg/ml. The profile of Tyroservatide in Beagle dogs fits to one compartment model. The biological half-life of Tyroservatide at three dose levels,60,600 and 6 000 μg/kg, is （8. 88±1.45）s, （9.00±1.70） s, （11.12±2.83）s, which don＇t have significant difference between the three levels. The C10s and AUC are proportional to dose, which suggests that Tyroservatide has the pharmacokinetics linearity over the dose range from 60 μg/kg to 6 000μg/kg. The preliminary result suggests that tyroservatide has a linearity pharmacokinetics behavior in Beagle dogs after iv administration. Tyroservatide is rapidly eliminated in vivo, and the biological half-life is less than 20 seconds.

关 键 词：酪丝缬肽 药动学 高效液相色谱 

分 类 号：R969.1[医药卫生—药理学]