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磺胺二甲氧嘧啶在虹鳟鱼(鲑鱼)体内的药代动力学和代谢研究综述。

A review of the pharmacokinetics and metabolism of sulfadimethoxine in the rainbow trout (Salmo gairdneri).

作者信息

Kleinow K M, Lech J J

机构信息

Department of Pharmacology, School of Veterinary Medicine, Louisiana State University, Baton Rouge 70803.

出版信息

Vet Hum Toxicol. 1988;30 Suppl 1:26-30.

PMID:3212939
Abstract

The pharmacokinetics and metabolism of sulfadimethoxine (SDM) was examined in the rainbow trout. Results from pharmacokinetic studies indicate a lengthening of the SDM half-life when administration was shifted from single to a multiple dose regime. In contrast to mammals and similar to the catfish a low magnitude nonspecific plasma protein binding was evident with SDM. Volume of distribution data indicates that SDM is distributed in plasma, extracellular and to a limited degree, intracellular fluid spaces. This distribution was greater than that demonstrated for mammals; however, lower than for the lobster or catfish. Absorption of SDM from the trout gastrointestinal tract varied with chemical form and dosage. Lower relative bioavailability values were evident with crystalline SDM and with high doses of the sodium salt. SDM accumulated to the highest levels in the bile followed by the intestine, liver, blood, skin, kidney, spleen, gill, muscle and fat respectively. Biliary SDM was composed of parent, N-acetylated SDM, an unknown polar metabolite, and what appears to be a sulfate conjugate.

摘要

对虹鳟鱼体内磺胺二甲氧嘧啶(SDM)的药代动力学和代谢情况进行了研究。药代动力学研究结果表明,给药方式从单剂量变为多剂量时,SDM的半衰期会延长。与哺乳动物不同,与鲶鱼类似,SDM表现出低水平的非特异性血浆蛋白结合。分布容积数据表明,SDM分布于血浆、细胞外液,且在一定程度上分布于细胞内液。这种分布比哺乳动物的情况更广泛;然而,低于龙虾或鲶鱼。SDM从鳟鱼胃肠道的吸收因化学形式和剂量而异。结晶SDM和高剂量钠盐的相对生物利用度值较低。SDM在胆汁中积累的水平最高,其次分别是肠道、肝脏、血液、皮肤、肾脏、脾脏、鳃、肌肉和脂肪。胆汁中的SDM由母体、N - 乙酰化SDM、一种未知的极性代谢物以及一种似乎是硫酸盐共轭物组成。

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