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磺胺类药物在食用动物体内的处置IV:静脉注射剂量及三种口服剂型给药后磺胺二甲嘧啶在牛体内的药代动力学

Disposition of sulfonamides in food-producing animals IV: Pharmacokinetics of sulfamethazine in cattle following administration of an intravenous dose and three oral dosage forms.

作者信息

Bevill R F, Dittert L W, Bourne D W

出版信息

J Pharm Sci. 1977 May;66(5):619-23. doi: 10.1002/jps.2600660503.

Abstract

The plasma and urine data obtained following intravenous administration of sulfamethazine to cattle were fit to a one-compartment pharmacokinetic model with a half-life of elimination of 9 hr and a volume of distribution of 0.35 liter/kg. Sulfamethazine was eliminated by excretion of unchanged sulfamethazine (18%) into urine and by formation of three metabolites subsequently excreted into urine. Sulfamethazine also was administered as a solution, a rapid-release bolus, and a sustained-release bolus. The change in the urinary metabolic pattern with different routes of administration suggested that first-pass metabolism was occurring during the absorption process. The absorption half-life was 6 hr. The absorption process for the two solid boluses kinetically appeared to include a dissolution step.

摘要

给牛静脉注射磺胺二甲嘧啶后获得的血浆和尿液数据符合一室药代动力学模型,消除半衰期为9小时,分布容积为0.35升/千克。磺胺二甲嘧啶通过将未变化的磺胺二甲嘧啶(18%)排泄到尿液中以及形成三种随后排泄到尿液中的代谢物来消除。磺胺二甲嘧啶还以溶液、速释丸剂和缓释丸剂的形式给药。不同给药途径下尿液代谢模式的变化表明在吸收过程中发生了首过代谢。吸收半衰期为6小时。两种固体丸剂的吸收过程在动力学上似乎包括一个溶解步骤。

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