Abd El-Aty A M, Goudah A
Department of Pharmacology, Faculty of Veterinary Medicine, Cairo University, Giza, Egypt.
Vet Res Commun. 2002 Oct;26(7):553-61. doi: 10.1023/a:1020243615928.
The aim of this study was to elucidate some of the pharmacokinetic parameters of pefloxacin in lactating goats (n = 5) following intravenous (i.v.) or intramuscular (i.m.) injections of 10 mg/kg bw. Serially obtained serum, milk and urine samples were collected at precise time intervals, and the drug concentrations were assayed using a microbiological assay. A two-compartment open model best described the decrease of pefloxacin concentration in the serum after intravenous administration. The maximum serum concentration (C0(p)) was 8.4 +/- 0.48 microg/ml; elimination half-life (t 1/2 beta) was 1.6 +/- 0.3 h; total body clearance (Cl(tot) was 3.6 +/- 0.3 L/kg/h; steady-state volume of distribution (V(dss)) was 5.14 +/- 0.21 L/kg; and the area under the curve (AUC) was 2.78 +/- 0.22 microg.ml/h. Pefloxacin was absorbed rapidly after i.m. injection with an absorption half-life (t 1/2 ab) of 0.32 +/- 0.02 h. The peak serum concentration (Cmax) of 0.86 +/- 0.08 microg/ml was attained at 0.75 h (Tmax). The absolute bioavailability after i.m. administration was 70.63 +/- 1.13% and the serum protein-bound fraction ranged from 7.2% to 14.3%, with an average value of 9.8 +/- 1.6%. Penetration of pefloxacin from the blood into the milk was rapid and extensive, and the pefloxacin concentration in milk exceeded that in serum from 1 h after administration. The drug was detected in milk and urine for 10 and 72 h, respectively; no samples were taken after 72 h.
本研究的目的是阐明在泌乳山羊（n = 5）静脉注射（i.v.）或肌肉注射（i.m.）10 mg/kg体重的培氟沙星后，其一些药代动力学参数。在精确的时间间隔内连续采集血清、乳汁和尿液样本，并使用微生物测定法测定药物浓度。二室开放模型最能描述静脉给药后血清中培氟沙星浓度的下降情况。血清最大浓度（C0(p)）为8.4±0.48μg/ml；消除半衰期（t 1/2 beta）为1.6±0.3小时；总体清除率（Cl(tot)）为3.6±0.3 L/kg/h；稳态分布容积（V(dss)）为5.14±0.21 L/kg；曲线下面积（AUC）为2.78±0.22μg.ml/h。肌肉注射后培氟沙星吸收迅速，吸收半衰期（t 1/2 ab）为0.32±0.02小时。在0.75小时（Tmax）达到血清峰值浓度（Cmax）为0.86±0.08μg/ml。肌肉注射后的绝对生物利用度为70.63±1.13%，血清蛋白结合率在7.2%至14.3%之间，平均值为9.8±1.6%。培氟沙星从血液进入乳汁的渗透迅速且广泛，给药后1小时乳汁中的培氟沙星浓度超过血清中的浓度。药物在乳汁和尿液中分别检测到10小时和72小时；72小时后未采集样本。
