Department of Pharmacology and Toxicology, College of Veterinary Science, Guru Angad Dev Veterinary and Animal Sciences University, Ludhiana, Punjab 141004, India.
Res Vet Sci. 2010 Aug;89(1):108-12. doi: 10.1016/j.rvsc.2010.01.015. Epub 2010 Mar 3.
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).
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。
