Buniva G, Del Favero A, Bernareggi A, Patoia L, Palumbo R
Institute of First Internal Medicine, University of Perugia, Italy.
J Antimicrob Chemother. 1988 Jan;21 Suppl A:23-8. doi: 10.1093/jac/21.suppl_a.23.
Five healthy male volunteers received over 60 sec a single intravenous injection of 400 mg of teicoplanin labelled with 41 microCi of 14C. Plasma and urine total radioactivity was measured up to 10 and 16 days, respectively. Teicoplanin was assayed in plasma and urine also by a microbiological method, with similar results. Pharmacokinetic parameters were estimated by model-independent analysis and the following mean values were obtained: elimination half-life 77 h; total body clearance 9.8 ml/h/kg; renal clearance 7.81 ml/h/kg; volume of distribution at steady-state 0.759 l/kg. Similar estimates were obtained by a compartmental analysis. A total of 80% of the administered dose was recovered in urine in 16 days; 2.7% of the dose was recovered in faeces collected for eight days after administration. The mean total recovery of the drug was 83 +/- 0.6%. The plasma and urine concentrations of teicoplanin observed after a single 400 mg iv dose exceeded the MIC for most pathogens for at least one day, and this suggests that a daily dosage regimen would be satisfactory for patients with normal renal function.
5名健康男性志愿者在60多秒内接受了单次静脉注射400毫克标记有41微居里¹⁴C的替考拉宁。分别在长达10天和16天内测定血浆和尿液中的总放射性。还通过微生物学方法测定血浆和尿液中的替考拉宁，结果相似。通过非模型分析估算药代动力学参数，得出以下平均值：消除半衰期77小时；全身清除率9.8毫升/小时/千克；肾清除率7.81毫升/小时/千克；稳态分布容积0.759升/千克。通过房室分析也得到了类似的估算值。16天内尿液中回收了80%的给药剂量；给药后8天收集的粪便中回收了2.7%的剂量。药物的平均总回收率为83±0.6%。单次静脉注射400毫克剂量后观察到的替考拉宁血浆和尿液浓度超过了大多数病原体的最低抑菌浓度至少一天，这表明对于肾功能正常的患者，每日给药方案是令人满意的。
