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磺胺二甲氧嘧啶在斑点叉尾鮰(Ictalurus punctatus)中的药代动力学与代谢

Sulfadimethoxine pharmacokinetics and metabolism in the channel catfish (Ictalurus punctatus).

作者信息

Squibb K S, Michel C M, Zelikoff J T, O'Connor J M

机构信息

Institute of Environmental Medicine, New York University Medical Center, Tuxedo 10987.

出版信息

Vet Hum Toxicol. 1988;30 Suppl 1:31-5.

PMID:3212940
Abstract

The pharmacokinetics of sulfadimethoxine (SDM) blood clearance, gastrointestinal absorption and tissue distribution and elimination were determined in channel catfish (Ictalurus punctatus) after intravenous and oral dosing using radiolabelled SDM. Blood clearance of SDM in catfish was rapid compared to mammals when the drug was given iv. Results from in vitro equilibrium dialysis studies suggest that this is due to a lower binding of SDM to plasma proteins in fish (18.4%) compared to mammalian species (60-88%). Results from oral dose studies indicated that SDM is readily absorbed from the gastrointestinal tract in channel catfish and distributes rapidly to body tissues, primarily the muscle. With time, concentrations of SDM in muscle decrease and the drug accumulates in the bile, primarily as the N-acetyl-metabolite.

摘要

使用放射性标记的磺胺二甲氧嘧啶(SDM)对沟鲶(斑点叉尾鮰)进行静脉注射和口服给药后,测定了SDM的药代动力学,包括血液清除率、胃肠道吸收、组织分布和消除情况。与哺乳动物相比,当静脉注射给药时,沟鲶体内SDM的血液清除速度很快。体外平衡透析研究结果表明,这是由于与哺乳动物(60%-88%)相比,SDM与鱼类血浆蛋白的结合率较低(18.4%)。口服剂量研究结果表明,SDM在沟鲶的胃肠道中易于吸收,并迅速分布到身体组织,主要是肌肉。随着时间的推移,肌肉中SDM的浓度降低,药物主要以N-乙酰代谢物的形式在胆汁中蓄积。

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