Flunixin meglumine is a highly efficacious nonsteroidal anti-inflammatory drug commonly used in equine medicine and especially in performance horses. Recently, a new transdermal flunixin meglumine product has been approved for use in cattle. Although not currently approved for use in the horse, the convenience of this product may prove appealing for use in horses, warranting study. Six horses were administered a single transdermal dose of 500 mg and blood and urine samples collected for up to 96 h post-administration. Serum for determination of thromboxane concentrations and whole blood samples was collected at various time and challenged with lipopolysaccharide, calcium ionophore, or methanol to induce ex vivo synthesis of eicosanoids. Concentrations of flunixin, 5-OH flunixin, and eicosanoids were measured using LC-MS/MS and non-compartmental pharmacokinetic analysis performed on concentration data. Serum concentrations of flunixin and 5-OH flunixin were above the limit of quantitation at 96 h post-administration in both serum and urine. The mean (range) for C_max, T_max and the terminal half-life were 515.6 (369.7–714.0) ng/ml, 8.67 (8.0 12.0) h, and 22.4 (18.3–42.5) h, respectively. Following transdermal administration, based on effects on eicosanoid synthesis, flunixin meglumine inhibited cyclooxygenase 1 and 2 and 15-lipooxygenase activity, with anti-inflammatory effects lasting for 24–72 h.

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透皮氟尼辛葡甲胺的药代动力学及其对马炎症生物标志物的影响

氟尼辛葡甲胺是一种非常有效的非甾体抗炎药，常用于马医学，尤其是用于性能马。最近，一种新的透皮氟尼辛葡甲胺产品已被批准用于牛。虽然目前尚未批准用于马，但该产品的便利性可能证明对马具有吸引力，值得研究。对六匹马进行单次透皮给药 500 毫克，并在给药后 96 小时内收集血液和尿液样本。在不同时间收集用于测定血栓烷浓度和全血样品的血清，并用脂多糖、钙离子载体或甲醇激发体外诱导类花生酸的合成。使用 LC-MS/MS 和对浓度数据进行的非隔室药代动力学分析测量氟尼辛、5-OH 氟尼辛和类花生酸的浓度。在给药后 96 小时，血清和尿液中氟尼辛和 5-OH 氟尼辛的血清浓度均高于定量限。C _max、T _max和终末半衰期的平均值（范围）分别为515.6 (369.7–714.0) ng/ml、8.67 (8.0 ± 12.0) h 和 22.4 (18.3–42.5) h。透皮给药后，基于对类花生酸合成的影响，氟尼辛葡甲胺抑制环氧合酶 1 和 2 以及 15-脂氧合酶活性，抗炎作用持续 24-72 小时。