中国兽医科学2017，Vol.47Issue(9)：1173-1179,7.DOI:10.16656/j.issn.1673-4696.2017.09.018
泰拉霉素在猪体内的药动学特征及其血浆蛋白结合率的研究
Studies on pharmacokinetics and plasma protein binding rate of tulathromycin in swine
摘要
Abstract
The study aims to investigate pharmacokinetics of tulathromycin injection and draxxin injection,and to determine the plasma protein binding rates in swine.Eighteen pigs were randomly divided into three groups and received 2.5 mg/kg of tulathromycin injection by either intravenous(i.v.) or intramuscular(i.m.)route,and six pigs were injected the same dosage of draxxin injection following i.m.administration.The plasma concentrations of tulathromycin was determined by ultra-high pressure liquid chromatography tandem mass spectrometry method (UPLC-MS/MS).The pharmacokinetic parameters were calculated by Winnonlin 5.2.1 software.Ultrafiltration was applied to determine the plasma protein binding rate of tulathromycin in swine.In result,following intravenous administration,the mainpharmacokinetic parameters were as follows:t1/2β=72.20 h±20.35 h,AUClast=11.31 μ g.h/mL±4.20 μ g·h/mL,and MRT=72.01 h±14.81 h.The main pharmacokinetic parameters for tulathromycin injection and draxxin injection administrated intramuscularly were as follows∶tmax=0.50 h±0.22 h and 0.22 h±0.07 h;Cmax=1.18 μg/mL±0.55 μg/mL and 1.81 μg/mL±0.68 μg/mL,AUCllast=10.85 μg.h/mL±4.76 μg.h/mLand 12.06 μg·h/mL±3.08 μg.h/mL,and t1/2β=68.59 h± 14.29 h and 68.01 h± 15.10 h.Compared with draxxin injection,the relative bioavailability was 92.95％±16.89％,and the absolute bioavailability was 93.90％±19.11％.In conclusion,tulathromycin was absorbed quickly,distributed widely,eliminated slowly and highly bioavailable after i.m.administration.The pharmacokinetics and bioavailability of two injections of tulathromycin are similar.The plasma protein binding rate of tulathromycin was above 95.17％,and it had the high binding ability and nonconcentration-dependent characteristic.关键词
泰拉霉素/药代动力学/血浆蛋白结合率Key words
tulathromycin/pharmacokinetics/plasma protein binding rate分类
农业科技引用本文复制引用
周巧仪,张桂君,马涛,李仲林,林晓环,李晗,方炳虎..泰拉霉素在猪体内的药动学特征及其血浆蛋白结合率的研究[J].中国兽医科学,2017,47(9):1173-1179,7.基金项目
国家自然科学基金项目(31372479) （31372479）
广东省科技计划项目(2015B090901059) （2015B090901059）
