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氟尼辛在小母牛口服和静脉注射后的药代动力学及其对前列腺素F2α代谢物浓度的影响。

Pharmacokinetics of flunixin and its effect on prostaglandin F2 alpha metabolite concentrations after oral and intravenous administration in heifers.

作者信息

Odensvik K

机构信息

Department of Obstetrics and Gynaecology, Faculty of Veterinary Medicine, Swedish University of Agricultural Sciences, Uppsala.

出版信息

J Vet Pharmacol Ther. 1995 Aug;18(4):254-9. doi: 10.1111/j.1365-2885.1995.tb00589.x.

Abstract

Flunixin meglumine (FM) was administered either orally as granules or intravenously to six heifers in a two period crossover study. Single doses of 2.2 mg/kg body weight were used. Pharmacokinetic variables were calculated using statistical moment methods. The effect exerted by flunixin was measured as changes in the basal plasma concentration of the main metabolite of prostaglandin (PG) F2 alpha. After oral FM the arithmetic means of pharmacokinetic variables were: MRT = 12.7 h; MAT = 6.3 h; Cmax = 0.9 microgram/mL; tmax = 3.5 h. The bioavailability was 60% and the mean half-life (harmonic mean) was 6.2 h. Oral administration of FM inhibited as effectively as intravenous administration the prostaglandin biosynthesis. The concentration of the PG metabolite decreased almost as rapidly as after intravenous administration. The duration of the effect was prolonged and the PG metabolite concentration was significantly lower between 10 and 30 h after oral than after intravenous administration. The results indicate that oral dosing of flunixin, in the form of granules, can be an alternative to intravenous administration for therapeutic use in cattle.

摘要

在一项两阶段交叉研究中,给6头小母牛口服氟尼辛葡甲胺颗粒剂或静脉注射氟尼辛葡甲胺(FM)。使用的单剂量为2.2毫克/千克体重。采用统计矩方法计算药代动力学变量。以前列腺素(PG)F2α主要代谢物的基础血浆浓度变化来衡量氟尼辛产生的效应。口服FM后,药代动力学变量的算术平均值为:平均滞留时间(MRT)=12.7小时;达峰时间(MAT)=6.3小时;最大血药浓度(Cmax)=0.9微克/毫升;达峰时间(tmax)=3.5小时。生物利用度为60%,平均半衰期(调和均值)为6.2小时。口服FM抑制前列腺素生物合成的效果与静脉注射一样有效。PG代谢物的浓度下降速度几乎与静脉注射后一样快。效应持续时间延长,口服后10至30小时的PG代谢物浓度显著低于静脉注射后。结果表明,颗粒剂形式的氟尼辛口服给药可作为牛治疗用途静脉注射的替代方法。

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