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磺胺苯吡唑在绵羊体内的药代动力学

Pharmacokinetics of sulfaphenazole in sheep.

作者信息

Odegaard S A

出版信息

Acta Vet Scand. 1986;27(2):243-9. doi: 10.1186/BF03548168.

Abstract

Proprietary formulations of sulfaphenazole were administered intravenously and orally to sheep. After intravenous injection the disposition of sulfaphenazole was described by an open two compartment model, and the elimination half-time was on average 5.58 h. The apparent volume of distribution was 0.273 1/kg and total body clearance 34.1 ml/kg/h. Judged from the area under the curves, the oral dose was completely absorbed, Drug plasma concentrations versus time fitted an open one compartment model, the half-time of absorption and elimination being 2.66 and 7.12 h, respectively. The binding to plasma proteins was high i.e. 93–96 % at therapeutic concentrations, and concentration dependent. The results demonstrate that the doses indicated by the manufacturer appear to be low and more appropriate for drugs with a longer elimination half-time. Consequently, considerable adjustments in the dosage regimen are recommended.

摘要

将磺胺苯吡唑的专利配方通过静脉注射和口服的方式给予绵羊。静脉注射后,磺胺苯吡唑的处置过程可用开放二室模型描述,消除半衰期平均为5.58小时。表观分布容积为0.273升/千克,全身清除率为34.1毫升/千克/小时。从曲线下面积判断,口服剂量被完全吸收,药物血浆浓度与时间的关系符合开放一室模型,吸收半衰期和消除半衰期分别为2.66小时和7.12小时。在治疗浓度下,其与血浆蛋白的结合率很高,即93%-96%,且呈浓度依赖性。结果表明,制造商所指示的剂量似乎偏低,对于消除半衰期较长的药物而言更为合适。因此,建议对给药方案进行大幅调整。

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