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氟尼辛葡甲胺在马体内的处置与排泄

Disposition and excretion of flunixin meglumine in horses.

作者信息

Soma L R, Behrend E, Rudy J, Sweeney R W

机构信息

School of Veterinary Medicine, New Bolton Center, University of Pennsylvania, Kennett Square 19348-1692.

出版信息

Am J Vet Res. 1988 Nov;49(11):1894-8.

PMID:3247913
Abstract

The disposition of flunixin meglumine administered IV at a dosage of 1.1 mg/kg was described by a 2-compartment model; the alpha and beta half-lives (t1/2) were 0.61 and 1.5 hours, respectively. When administered IV at a rate of 2.2 mg/kg, the disposition was best described by a 3-compartment model, and the alpha, beta, and lambda t1/2 were 0.16, 1.52, and 6.00 hours, respectively. The zero-time plasma concentrations after flunixin meglumine was administered at 1.1 and 2.2 mg/kg were 9.3 +/- 0.76 and 21.5 +/- 7.4 mg/L, respectively. The bioavailability after oral administration of 1.1 mg/kg was 85.8%. The absorption t1/2 was 0.57 hours, with a peak concentration of 2.50 +/- 1.25 mg/L. The cumulative urinary recoveries for IV and oral administrations were 61.0% and 63.3%, respectively, of the dose for the 12-hour collection period. The final asymptotic points of urine excretion after IV and oral administrations were 406.4 +/- 65.5 and 357.7 +/- 53.5 mg, respectively, which represented 75.5 and 77.5% of the drug accounted for between 30 and 35 hours after administration. Flunixin meglumine was rapidly excreted in urine over a 2- to 4-hour period after drug administration and was highly bound to protein in plasma.

摘要

以1.1mg/kg的剂量静脉注射氟尼辛葡甲胺后的处置情况可用二室模型描述;α和β半衰期(t1/2)分别为0.61小时和1.5小时。以2.2mg/kg的速率静脉注射时,其处置情况用三室模型描述最佳,α、β和λ t1/2分别为0.16小时、1.52小时和6.00小时。以1.1mg/kg和2.2mg/kg的剂量静脉注射氟尼辛葡甲胺后的零时血浆浓度分别为9.3±0.76mg/L和21.5±7.4mg/L。口服1.1mg/kg后的生物利用度为85.8%。吸收t1/2为0.57小时,峰值浓度为2.50±1.25mg/L。在12小时收集期内,静脉注射和口服给药的累积尿回收率分别为给药剂量的61.0%和63.3%。静脉注射和口服给药后尿排泄的最终渐近点分别为406.4±65.5mg和357.7±53.5mg,分别占给药后30至35小时药物总量的75.5%和77.5%。氟尼辛葡甲胺在给药后2至4小时内迅速经尿液排泄,且在血浆中与蛋白质高度结合。

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