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乳酸山羊静脉内、皮下和肌肉注射地氟沙星后的药代动力学及乳汁渗透情况

Pharmacokinetics and milk penetration of difloxacin after intravenous, subcutaneous and intramuscular administration to lactating goats.

作者信息

Marín P, Escudero E, Fernández-Varón E, Cárceles C M

机构信息

Department of Pharmacology, Faculty of Veterinary Medicine, University of Murcia, Campus de Espinardo, Murcia, Spain.

出版信息

J Vet Pharmacol Ther. 2007 Feb;30(1):74-9. doi: 10.1111/j.1365-2885.2007.00818.x.

Abstract

The single-dose disposition kinetics of difloxacin were determined in clinically normal lactating goats (n = 6) after intravenous (i.v.), subcutaneous (s.c.) and intramuscular (i.m.) administration of 5 mg/kg. Difloxacin concentrations were determined by high performance liquid chromatography with fluorescence detection. The concentration-time data were analysed by compartmental and noncompartmental kinetic methods. Steady-state volume of distribution (V(ss)) and total body clearance (Cl) of difloxacin after i.v. administration were estimated to be 1.16 +/- 0.26 L/kg and 0.32 +/- 0.05 L/h x kg respectively. Following s.c. and i.m. administration difloxacin achieved maximum plasma concentrations of 1.33 +/- 0.25 and 1.97 +/- 0.40 mg/L at 3.37 +/- 0.36 and 1.79 +/- 1.14 h respectively. The absolute bioavailabilities after s.c. and i.m. routes were 90.16 +/- 11.99% and 106.79 +/- 13.95% respectively. Difloxacin penetration from the blood into the milk was extensive and rapid, and the drug was detected for 36 h after i.v. and s.c. dosing, and for 72 h after i.m. administration.

摘要

在临床健康的泌乳山羊(n = 6)中,静脉注射(i.v.)、皮下注射(s.c.)和肌肉注射(i.m.)5 mg/kg剂量的二氟沙星后,测定了其二氟沙星的单剂量处置动力学。通过高效液相色谱荧光检测法测定二氟沙星浓度。采用房室和非房室动力学方法分析浓度-时间数据。静脉注射后,二氟沙星的稳态分布容积(V(ss))和全身清除率(Cl)估计分别为1.16±0.26 L/kg和0.32±0.05 L/h×kg。皮下注射和肌肉注射后,二氟沙星分别在3.37±0.36小时和1.79±1.14小时达到最大血浆浓度1.33±0.25和1.97±0.40 mg/L。皮下注射和肌肉注射途径后的绝对生物利用度分别为90.16±11.99%和106.79±13.95%。二氟沙星从血液向乳汁的渗透广泛且迅速,静脉注射和皮下注射给药后36小时可检测到该药物,肌肉注射给药后72小时可检测到该药物。

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