Pharmacology Department, Faculty of Veterinary Medicine, Cairo University, Giza, Egypt.
Chemotherapy. 2010;56(1):26-31. doi: 10.1159/000290172. Epub 2010 Mar 3.
Moxifloxacin is a new fourth-generation 8-methoxy fluoroquinolone developed primarily for the treatment of community-acquired pneumonia and upper respiratory tract infections. The aim of the study was to investigate the plasma pharmacokinetics characteristic of moxifloxacin in calves, after intravenous, intramuscular and subcutaneous administration of a single dose. Meanwhile, plasma protein binding and bioavailability of moxifloxacin were also estimated.
Plasma concentrations of moxifloxacin were measured using a modified HPLC method, and the extent of plasma protein binding was determined in vitro using ultrafiltration.
Following intravenous administration, the half life of elimination, the volume of distribution at steady state and the area under the curve were 3.29 h, 0.94 l/kg and 24.72 microg x h/ml, respectively. After intramuscular and subcutaneous administration of moxifloxacin at the same dose, the peak plasma concentrations were 2.41 and 2.20 microg/ml and were obtained at 1.54 and 1.59 h, respectively. The systemic bioavailabilities were 87.19 and 75.94%, respectively. The in vitro plasma protein binding of moxifloxacin in plasma of calves was 27%.
A high peak plasma concentration, area under the curve, rapid absorption and bioavailability following intramuscular and subcutaneous administration characterize the pharmacokinetics of moxifloxacin in calves.
莫西沙星是一种新的第四代 8-甲氧基氟喹诺酮类药物，主要用于治疗社区获得性肺炎和上呼吸道感染。本研究旨在考察单剂量静脉、肌肉和皮下给予犊牛后，莫西沙星的血浆药代动力学特征。同时，还估算了莫西沙星的血浆蛋白结合率和生物利用度。
采用改良的 HPLC 法测定莫西沙星的血浆浓度，并用超滤法测定其体外血浆蛋白结合率。
静脉给药后，莫西沙星的消除半衰期、稳态分布容积和曲线下面积分别为 3.29 h、0.94 l/kg 和 24.72 μg·h/ml。以相同剂量肌肉和皮下给予莫西沙星后，达峰血浆浓度分别为 2.41 和 2.20 μg/ml，达峰时间分别为 1.54 和 1.59 h。系统生物利用度分别为 87.19%和 75.94%。莫西沙星在犊牛血浆中的体外血浆蛋白结合率为 27%。
肌肉和皮下给予莫西沙星后，具有较高的血药峰浓度、曲线下面积、快速吸收和生物利用度，这是莫西沙星在犊牛体内的药代动力学特征。
