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犬静脉注射和口服两种剂量水平的单一对映体S-(+)-酮洛芬后的药代动力学。

Pharmacokinetics of the individual enantiomer S-(+)-ketoprofen after intravenous and oral administration in dogs at two dose levels.

作者信息

Serrano-Rodríguez J M, Serrano J M, Rodríguez J Morgaz, Machuca M M Granados, Gómez-Villamandos R J, Navarrete-Calvo R

机构信息

Department of Pharmacology, Toxicology and Legal and Forensic Medicine, Faculty of Veterinary Medicine, University of Cordoba, Spain.

Department of Pharmacology, Toxicology and Legal and Forensic Medicine, Faculty of Veterinary Medicine, University of Cordoba, Spain.

出版信息

Res Vet Sci. 2014 Jun;96(3):523-5. doi: 10.1016/j.rvsc.2014.03.021. Epub 2014 Apr 2.

Abstract

The pharmacokinetic of the individual S-(+)-enantiomer of ketoprofen, S-(+)-ketoprofen, after intravenous (IV) and oral (PO) administration was determined in six dogs at 1 and 3 mg/kg. Plasma concentrations were determined by high performance liquid chromatography with ultraviolet detection. The concentration-time curves were analyzed by non-compartmental methods. Steady-state volume of distribution (Vss) and clearance (Cl) of S-(+)-ketoprofen after IV administration were 0.22 ± 0.07 and 0.19 ± 0.03 L/kg, and 0.10 ± 0.02 and 0.09 ± 0.01 L/h/kg, at 1 and 3 mg/kg, respectively. Following PO administration, S-(+)-ketoprofen achieved maximum plasma concentrations of 4.91 ± 0.76 and 12.47 ± 0.62 μg/ml, at two dose levels, respectively. The absolute bioavailability after PO route was 88.66 ± 12.95% and 85.36 ± 13.90%, respectively.

摘要

在6只犬中,以1和3mg/kg的剂量静脉注射(IV)和口服(PO)给予酮洛芬的单个S-(+)-对映体,即S-(+)-酮洛芬,测定其药代动力学。通过高效液相色谱-紫外检测法测定血浆浓度。采用非房室模型方法分析浓度-时间曲线。静脉注射后,S-(+)-酮洛芬在1和3mg/kg剂量下的稳态分布容积(Vss)和清除率(Cl)分别为0.22±0.07和0.19±0.03L/kg,以及0.10±0.02和0.09±0.01L/h/kg。口服给药后,S-(+)-酮洛芬在两个剂量水平下分别达到最大血浆浓度4.91±0.76和12.47±0.62μg/ml。口服给药后的绝对生物利用度分别为88.66±12.95%和85.36±13.90%。

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