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氟尼辛葡甲胺在绵羊体内的药代动力学

The pharmacokinetics of flunixin meglumine in the sheep.

作者信息

Welsh E M, McKellar Q A, Nolan A M

机构信息

Department of Veterinary Pharmacology, University of Glasgow Veterinary School, UK.

出版信息

J Vet Pharmacol Ther. 1993 Jun;16(2):181-8. doi: 10.1111/j.1365-2885.1993.tb00162.x.

Abstract

Flunixin meglumine was administered intravenously and intramuscularly in sheep and the pharmacokinetics of the drug studied. Plasma concentrations of flunixin were measured by high performance liquid chromatography. The decline in plasma flunixin concentration with time was best fitted by a triexponential equation. The pharmacokinetics following intravenous administration of 1.0 mg/kg indicate that flunixin has a rapid distribution half-life (t1/2 pi = 2.3 min), a slow body clearance rate (Clb = 0.6 ml/kg/min) and an elimination half-life of 229 min. Similarly, at 2.0 mg/kg, flunixin is rapidly distributed from the plasma, t1/2 pi = 2.7 min, has a slow body clearance rate (Clb = 0.7 ml/kg/min) and an elimination half-life of 205 min. Following intramuscular injection flunixin is rapidly and well absorbed from the injection site. It had a mean maximum concentration (Cmax) of > or = 5.9 micrograms/ml when administered at a dose rate of 1.1 mg/kg, and a relative bioavailability of 70%. Plasma concentrations increase proportionally to dose over the range 1.1 mg/kg-2.2 mg/kg when administered by the intramuscular route.

摘要

在绵羊身上静脉内和肌肉内注射氟尼辛葡甲胺,并研究该药物的药代动力学。通过高效液相色谱法测量血浆中氟尼辛的浓度。血浆中氟尼辛浓度随时间的下降情况最适合用三指数方程来拟合。静脉注射1.0毫克/千克后的药代动力学表明,氟尼辛具有快速分布半衰期(t1/2 pi = 2.3分钟)、缓慢的机体清除率(Clb = 0.6毫升/千克/分钟)和229分钟的消除半衰期。同样,在2.0毫克/千克时,氟尼辛从血浆中快速分布,t1/2 pi = 2.7分钟,具有缓慢的机体清除率(Clb = 0.7毫升/千克/分钟)和205分钟的消除半衰期。肌肉注射后,氟尼辛从注射部位快速且良好地吸收。以1.1毫克/千克的剂量率给药时,其平均最大浓度(Cmax)≥5.9微克/毫升,相对生物利用度为70%。通过肌肉途径给药时,在1.1毫克/千克 - 2.2毫克/千克的范围内,血浆浓度与剂量成比例增加。

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