脱二氧喹赛多在大鼠血浆及组织的药代动力学研究  

Plasma and tissue Pharmacokinetics of 1,4-bisdesoxycyadox in rats

作　　者：杨雪[1] 赵东豪[1] 于洋[1] 周宇峰[1] 时伟[1] 方炳虎[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：《中国兽医杂志》2015年第6期97-99,共3页Chinese Journal of Veterinary Medicine

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

摘　　要：本试验研究单剂量口服喹赛多(200 mg/kg体重)后,其主要代谢物脱二氧喹赛多(1.4-bisdesoxycyadox)在健康大鼠血浆及各组织内的药代动力学特征。灌服后在设定的时间点用剖杀的方法采集血浆及组织,经处理后,利用液相色谱-串联质谱法测定血浆及各组织中的药物浓度。通过Win Nonlin 6.1软件,用非房室模型统计矩原理计算脱二氧喹赛多在血浆及各组织中的药动学参数。主要药动学参数分别为血浆:T1/2β(4.63)h,Cmax(1534.00)μg/L,AUC0→∞(9937.08)h*μg/L,MRT(8.49)h;肝脏:T1/2β(32.45)h,Cmax(1982.50)μg/L,AUC0→∞(15489.71)h*μg/L,MRT(10.04)h;肾脏:T1/2β(18.96)h,Cmax(1286.67)μg/L,AUC0→∞(7671.06)h*μg/L,MRT(9.08)h;肌肉:T1/2β(10.19)h,Cmax(2293.33)μg/L,AUC0→∞(16154.84)h*μg/L,MRT(9.00)h;脂肪:T1/2β(8.47)h,Cmax(711.50)μg/L,AUC0→∞(5107.22)h*μg/L,MRT(8.79)h。脱二氧喹赛多在大鼠血浆及各组织中的消除速率缓慢,达峰浓度高,分布较广泛。The pharmacokinetics of 1,4-bisdesoxycyadox in rats were determined by oral administration of a single dose of200 mg/kg body weight. Blood and tissue samples were collected at the set time. The samples were determined by high-perfor-mance liquid chromatography-tandem mass spectrometry after sample preparation.The pharmacokinetic parameters of 1,4-bisdes-oxycyadox were calculated using WINNONLIN software based on a non-compartmental method for distinctive animals. The mainpharmacokinetic parameters were as follows:plasma:T1/2β(4.63)h,Cmax(1534.00)μg/L,AUC0→∞(9937.08)h*μg/L,MRT(8.49)h;liver:T1/2β(32.45)h,Cmax(1982.50)μg/L,AUC0→∞(15489.71)h*μg/L,MRT(10.04)h;kidney:T1/2β(18.96)h,Cmax(1286.67)μg/L,AUC0→∞(7671.06)h*μg/L,MRT(9.08)h;muscle:T1/2β(10.19)h,Cmax(2293.33)μg /L,AUC0→∞(16154.84)h*μg/L,MRT(9.00)h;fat:T1/2β(8.47)h,Cmax(711.50)μg/L,AUC0→∞(5107.22)h*μg/L,MRT(8.79)h.Elimination rate of 1,4-bisdesoxycyadoxwas slow in plasma and tissues in rat.The concentrations of 1,4-bisdesoxycyadox in all tissues were relatively high and 1,4-bis-desoxycyadox was distributed extensively in rats.

关 键 词：脱二氧喹赛多 药物代谢动力学 药时曲线下面积 半衰期 大鼠 

分 类 号：S859.79[农业科学—临床兽医学]