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Pharmacokinetics and intramuscular bioavailability of difloxacin in dromedary camels (Camelus dromedarius)

机译:地氟沙星在骆驼中的药代动力学和肌内生物利用度

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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+/-0.34mug/mLwas 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.
机译:在静脉内(IV)和肌肉内(IM)给药后,在临床上正常的雄性单峰骆驼(n = 6)中确定了地氟沙星(5mg / kg体重)的单剂量处置动力学。通过高效液相色谱-荧光检测法测定地氟沙星的浓度。通过隔室和非隔室动力学方法分析浓度-时间数据。一次静脉注射后,血浆二氟沙星浓度-时间曲线最好由两室开放模型描述,分布半衰期(t(1 / 2alpha))为0.22 +/- 0.02h,消除半衰期为寿命(t(1 / 2beta))为2.97 +/- 0.31h。稳态分布体积(V(dss))和全身清除率(Cl(tot))分别为1.02 +/- 0.21L / kg和0.24 +/- 0.07L / kg / h。 IM给药后,吸收半衰期(t(1)(/)(2ab))和平均吸收时间(MAT)分别为0.44 +/- 0.03h和1.53 +/- 0.22h。在1.42 +/- 0.21h达到2.84 +/- 0.34mug / mL的峰值血浆浓度(C(max))。消除半衰期(t(1 / 2el))和平均停留时间(MRT)分别为3.46 +/- 0.42h和5.61 +/- 0.23h。地氟沙星的体外血浆蛋白结合率为28-43%,IM给药后的绝对生物利用度为93.51 +/- 11.63%。地氟沙星可用于治疗对这种药物敏感的骆驼中的细菌感染。

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