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莫西沙星在水牛犊牛体内的药代动力学和生物利用度。

Pharmacokinetics and bioavailability of moxifloxacin in buffalo calves.

机构信息

Department of Pharmacology and Toxicology, College of Veterinary Science, Guru Angad Dev Veterinary and Animal Sciences University, Ludhiana, Punjab 141004, India.

出版信息

Res Vet Sci. 2010 Aug;89(1):108-12. doi: 10.1016/j.rvsc.2010.01.015. Epub 2010 Mar 3.

Abstract

The pharmacokinetics of moxifloxacin were investigated in buffalo calves following a single intravenous and intramuscular administration of moxifloxacin (5 mg kg(-1) body wt.). Moxifloxacin concentrations in plasma and urine were determined by microbiological assay. Pharmacokinetic analysis of disposition data indicated that intravenous administration data were best described by a two compartment open model, whereas intramuscular administration data were best described by a one compartment open model. Following intravenous administration, the elimination half life (t(1/2beta)), volume of distribution (Vd(area)) and total body clearance were 2.69+/-0.14 h, 1.43+/-0.08 L kg(-1) and 371.2+/-11.2 ml kg(-1)h(-1), respectively. Following intramuscular administration, the absorption half life (t(1/2ka)) was 0.83+/-0.20 h. The systemic bioavailability (F) of moxifloxacin in buffalo calves was 80.0+/-4.08%. Urinary excretion of moxifloxacin was less than 14% after 24h of administration of drug. In vitro binding of moxifloxacin to plasma proteins of buffalo calves was 28.4+/-3.77%. From the data of surrogate markers (AUC/MIC, C(max)/MIC), it was determined in the buffalo calves that when administered by intravenous or intramuscular route at 5 mg kg(-1), moxifloxacin is likely to be effective against bacterial isolates with MIC< or =0.1 microg ml(-1).

摘要

本研究考察了水牛犊单次静脉和肌肉注射莫西沙星(5mg/kg 体重)后的药代动力学。采用微生物检测法测定血浆和尿液中的莫西沙星浓度。药物处置数据的药代动力学分析表明,静脉给药数据符合二室开放模型,而肌肉注射数据符合一室开放模型。静脉给药后,消除半衰期(t(1/2β))、分布容积(Vd(area))和全身清除率分别为 2.69+/-0.14 h、1.43+/-0.08 L/kg 和 371.2+/-11.2 ml/kg/h。肌肉注射后,吸收半衰期(t(1/2ka))为 0.83+/-0.20 h。水牛犊的莫西沙星系统生物利用度(F)为 80.0+/-4.08%。给药 24h 后,莫西沙星的尿液排泄率低于 14%。水牛犊血浆蛋白与莫西沙星的体外结合率为 28.4+/-3.77%。根据替代标志物(AUC/MIC、C(max)/MIC)的数据,当以 5mg/kg 体重经静脉或肌肉途径给药时,莫西沙星可能对 MIC<或=0.1μg/ml 的细菌分离株有效。

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