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在水牛犊牛(Bubalus bubalis)静脉注射后,丹氟沙星的药代动力学、尿排泄和血浆蛋白结合。

Pharmacokinetics, urinary excretion and plasma protein binding of danofloxacin following intravenous administration in buffalo calves (Bubalus bubalis).

机构信息

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

出版信息

Vet Res Commun. 2009 Oct;33(7):659-67. doi: 10.1007/s11259-009-9215-6. Epub 2009 Mar 19.

Abstract

Pharmacokinetics, urinary excretion and plasma protein binding of danofloxacin was investigated in buffalo calves following intravenous administration at the dose rate of 1.25 mg/kg to select the optimal dosage regimen of danofloxacin. Drug concentrations in plasma and urine were measured by microbiological assaying. In vitro plasma protein binding was determined employing the equilibrium dialysis technique. The distribution and elimination of danofloxacin were rapid, as indicated by values (mean +/-SD) of distribution half-life (t(1/2)alpha = 0.16 +/- 0.07 h) and elimination half-life (t(1/2)beta = 4.24 +/- 1.78 h), respectively. Volume of distribution at steady state (Vss) = 3.98 +/- 1.69 L/kg indicated large distribution of drug. The area under plasma drug concentration versus time curve (AUC) was 1.79 +/- 0.28 micrg/ml x h and MRT was 8.64 +/- 0.61 h. Urinary excretion of danofloxacin was 23% within 48 h of its administration. Mean plasma protein binding was 36% at concentrations ranging from 0.0125 microg/ml to 1 microg/ml. On the basis of pharmacokinetic parameters obtained, it is concluded that the revision of danofloxacin dosage regimen in buffalo calves is needed because the current dosage schedule (1.25 mg/kg) is likely to promote resistance.

摘要

在水牛犊牛中,以 1.25mg/kg 的剂量静脉注射研究了丹氟沙星的药代动力学、尿排泄和血浆蛋白结合情况,以选择丹氟沙星的最佳剂量方案。采用微生物测定法测定血浆和尿液中的药物浓度。采用平衡透析技术测定体外血浆蛋白结合率。丹氟沙星的分布和消除迅速,分布半衰期(t(1/2)alpha = 0.16 +/- 0.07 h)和消除半衰期(t(1/2)beta = 4.24 +/- 1.78 h)的平均值(SD)分别表示。稳态分布容积(Vss)= 3.98 +/- 1.69 L/kg 表明药物分布广泛。血浆药物浓度-时间曲线下面积(AUC)为 1.79 +/- 0.28 mcg/ml x h,MRT 为 8.64 +/- 0.61 h。给药后 48 小时内,丹氟沙星的尿液排泄率为 23%。在 0.0125 mcg/ml 至 1 mcg/ml 的浓度范围内,平均血浆蛋白结合率为 36%。根据获得的药代动力学参数,得出结论,需要修订水牛犊牛的丹氟沙星剂量方案,因为目前的剂量方案(1.25mg/kg)可能会促进耐药性的产生。

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