Abo-El-Sooud K, Goudah A
Pharmacology Department, Cairo University, Giza, Egypt.
Vet J. 2009 Feb;179(2):282-6. doi: 10.1016/j.tvjl.2008.05.011. Epub 2008 Jul 7.
Single-dose disposition kinetics of difloxacin (5mg/kg bodyweight) were determined in clinically normal male dromedary camels (n=6) following intravenous (IV) and intramuscular (IM) administration. Difloxacin concentrations were determined by high performance liquid chromatography with fluorescence detection. The concentration-time data were analysed by compartmental and non-compartmental kinetic methods. Following a single IV injection, the plasma difloxacin concentration-time curve was best described by a two-compartment open model, with a distribution half-life (t(1/2alpha)) of 0.22+/-0.02h and an elimination half-life (t(1/2beta)) of 2.97+/-0.31h. Steady-state volume of distribution (V(dss)) and total body clearance (Cl(tot)) were 1.02+/-0.21L/kg and 0.24+/-0.07L/kg/h, respectively. Following IM administration, the absorption half-life (t(1)(/)(2ab)) and the mean absorption time (MAT) were 0.44+/-0.03h and 1.53+/-0.22h, respectively. The peak plasma concentration (C(max)) of 2.84+/-0.34microg/mL was achieved at 1.42+/-0.21h. The elimination half-life (t(1/2el)) and the mean residence time (MRT) was 3.46+/-0.42h and 5.61+/-0.23h, respectively. The in vitro plasma protein binding of difloxacin ranged from 28-43% and the absolute bioavailability following IM administration was 93.51+/-11.63%. Difloxacin could be useful for the treatment of bacterial infections in camels that are sensitive to this drug.
在临床正常的雄性单峰骆驼(n = 6)中,静脉注射(IV)和肌肉注射(IM)5mg/kg体重的双氟沙星后,测定了其单剂量处置动力学。双氟沙星浓度通过带荧光检测的高效液相色谱法测定。浓度-时间数据采用房室和非房室动力学方法进行分析。单次静脉注射后,血浆双氟沙星浓度-时间曲线最适合用二房室开放模型描述,分布半衰期(t(1/2α))为0.22±0.02小时,消除半衰期(t(1/2β))为2.97±0.31小时。稳态分布容积(V(dss))和总体清除率(Cl(tot))分别为1.02±0.21L/kg和0.24±0.07L/kg/h。肌肉注射后,吸收半衰期(t(1)(/)(2ab))和平均吸收时间(MAT)分别为0.44±0.03小时和1.53±0.22小时。在1.42±0.21小时达到的血浆峰浓度(C(max))为2.84±0.34μg/mL。消除半衰期(t(1/2el))和平均驻留时间(MRT)分别为3.46±0.42小时和5.61±0.23小时。双氟沙星的体外血浆蛋白结合率在28%-43%之间,肌肉注射后的绝对生物利用度为93.51±11.63%。双氟沙星可用于治疗对该药物敏感的骆驼细菌感染。