Cybulski W, Larsson P, Tjälve H, Kowalska-Pylka H, Sylla M, Semeniuk S
Department of Toxicology and Environmental Protection, Faculty of Veterinary Medicine, Agricultural University, Lublin, Poland.
J Vet Pharmacol Ther. 1996 Oct;19(5):352-8. doi: 10.1111/j.1365-2885.1996.tb00063.x.
Hens were given single intravenous or oral doses (30 mg/kg body weight) of metronidazole and the plasma concentrations of the drug were determined by high-performance liquid chromatography (HPLC) at intervals from 10 min to 24 h after drug administration. Pharmacokinetic variables were calculated by the Lagrange algorithm technique. The elimination half-life (t1/2 beta) after the intravenous injection was 4.2 +/- 0.5 h, the volume of distribution (Vd(ss) 1.1 +/- 0.2 L/kg and the total body clearance (ClB) 131.2 +/- 20 mL/h.kg. Oral bioavailability of the metronidazole was 78 +/- 16%. The plasma maximum concentration (Cmax) 31.9 +/- 2.3 micrograms/mL was reached 2 h after the oral administration and the oral elimination half-life (t1/2 beta) was 4.7 +/- 0.2 h. The binding of metronidazole to proteins in hen plasma was very low (less than 3%). Whole body autoradiography of [3H] metronidazole in hens and quails showed an even distribution of labelled material in various tissues at short survival intervals (1-4 h) after oral or intravenous administration. A high labelling was seen in the contents of the small and large intestines. In the laying quails a labelling was also seen in the albumen and in a ring in the periphery of the yolk at long survival intervals. Our results show that a concentration twofold above the MIC is maintained in the plasma of hens for at least 12 h at an oral dose of 30 mg/kg metronidazole.
给母鸡静脉注射或口服单次剂量(30毫克/千克体重)的甲硝唑,给药后10分钟至24小时内,每隔一段时间通过高效液相色谱法(HPLC)测定血浆中药物浓度。药代动力学变量通过拉格朗日算法技术计算。静脉注射后的消除半衰期(t1/2β)为4.2±0.5小时,分布容积(Vd(ss))为1.1±0.2升/千克,全身清除率(ClB)为131.2±20毫升/小时·千克。甲硝唑的口服生物利用度为78±16%。口服给药后2小时达到血浆最大浓度(Cmax)31.9±2.3微克/毫升,口服消除半衰期(t1/2β)为4.7±0.2小时。甲硝唑与母鸡血浆中蛋白质的结合率非常低(小于3%)。[3H]甲硝唑在母鸡和鹌鹑体内的全身放射自显影显示,口服或静脉给药后短存活时间间隔(1-4小时)内,标记物质在各种组织中分布均匀。在小肠和大肠内容物中可见高标记。在产蛋鹌鹑中,在长存活时间间隔时,蛋清和蛋黄周边的一个环中也可见标记。我们的结果表明,口服30毫克/千克甲硝唑剂量时,母鸡血浆中维持的浓度比最低抑菌浓度高两倍至少12小时。