喹赛多及其主要代谢物在猪体内的药代动力学研究  

Pharmacokinetics of Cyadox and its Mainly Metabolites in Swine

作　　者：郭军朋[1] 张展[1] 远立国[1] 余军军[1] 胡红丽[1] 邓辉[1] 刘雅红[1] 

机构地区：[1]华南农业大学兽医学院,广东广州510642

出　　处：《中国畜牧兽医》2011年第9期228-231,共4页China Animal Husbandry & Veterinary Medicine

基　　金：国家重点基础研究发展计划项目(973计划)(2009CB118805)

摘　　要：试验研究了灌服单剂量喹赛多(40mg/kg体重)后原药及其代谢物在健康猪体内的药代动力学特征。液相色谱-串联质谱法测定血浆中喹赛多及其代谢物的浓度,通过WinNonlin 5.2药代动力学软件分析,用非房室模型统计矩原理计算喹赛多及其代谢产物的药动学参数。主要药动学参数分别为喹赛多:t1/2(7.52±1.77)h,Cmax(0.02±0.01)μg/mL,AUC(0-36h)(0.26±0.24)(h.μg)/mL,MRT(11.37±3.21)h;N1(脱一氧喹赛多):t1/2(3.05±1.12)h,Cmax(0.35±0.18)μg/mL,AUC(0-36h)(2.13±2.31)(h.μg)/mL,MRT(11.83±3.34)h。N4(脱一氧喹赛多):t1/2(2.91±1.15)h,Cmax(0.60±0.32)μg/mL,AUC(0-36h)(3.78±4.28)(h.μg)/mL,MRT(11.00±2.86)h。脱二氧喹赛多:t1/2(3.85±1.30)h,Cmax(0.46±0.19)μg/mL,AUC(0-36h)(4.21±2.47)(h.μg)/mL,MRT(13.35±2.65)h。QCA(喹噁啉-2-羧酸):t1/2(5.08±0.57)h,Cmax(0.25±0.11)μg/mL,AUC(0-36h)(3.05±1.46)(h.μg)/mL,MRT(15.15±1.83)h。结果表明,血浆中主要存在形式为代谢物,各代谢物的血药浓度及AUC(0-∞)均高于喹赛多,喹赛多消除半衰期最长,QCA平均滞留时间最长。To study the pharmacokinetics of cyadox and its metabolites following single oral cyadox（40 mg/kg body weight） in healthy swine.A LC-MS/MS assay was used to determine plasma cyadox and its metabolites concentrations.The plasma concentration was analyzed with the pharmacokinetics software WinNonlin 5.2.Rosenblueth method of non compartment model was used to calculate the pharmacokinetic parameters of cyadox and its metabolites.The main pharmacokinetic parameters of cyadox and its metabolites were as follows.Cyadox：t1/2（7.52±1.77） h,Cmax（0.02±0.01） μg/mL,AUC（0-36 h）（0.26±0.24）（h·μg）/mL,MRT（11.37±3.21）h.N1（cyadox 1-monoxide）：t1/2（3.05±1.12） h,Cmax（0.35±0.18） μg/mL,AUC（0-36 h）（2.13±2.31）（h·μg）/mL,MRT（11.83±3.34） h.N4（cyadox 4-monoxide：t1/2（2.91±1.15） h,Cmax（0.60±0.32） μg/mL,AUC（0-36 h）（3.78±4.28）（h·μg）/mL,MRT（11.00±2.86）h.Bisdesoxycyadox：t1/2（3.85±1.30） h,Cmax（0.46±0.19） μg/mL,AUC（0-36 h）（4.21±2.47）（h·μg）/mL,MRT（13.35±2.65）h.Quinoxaline-2-carboxylic acid（QCA）：t1/2（5.08±0.57） h,Cmax（0.25±0.11） μg/mL,AUC（0-36 h）（3.05±1.46）（h·μg）/mL,MRT（15.15±1.83）h.The results showed the mainly form in plasma was metabolites,concentration and area under the curve of metabolites were higher than cyadox.Cyadox is the longest elimination half-life of each metabolites,and quinoxaline-2-carboxylic acid（QCA） mean residence time is the longest time.

关 键 词：猪 喹赛多 液相色谱-串联质谱 喹噁啉-2-羧酸 

分 类 号：S859.84[农业科学—临床兽医学]