Bergan T, Olszewski W, Engeset A
J Antimicrob Chemother. 1986 Jan;17(1):97-103. doi: 10.1093/jac/17.1.97.
An intravenous dose of 3.0 g ticarcillin and 0.2 g clavulanic acid was given to 11 healthy human volunteers in whom peripheral lymph, serum and urine were monitored for 8 h. The concentrations were assayed microbiologically. The mean levels in lymph collected during the period 0-1 h was 39.3 mg/l of ticarcillin and 2.93 mg/l of clavulanic acid. The mean peak concentration in lymph (appearing between 1.25 and 2.25 h) was 66.3 mg/l for ticarcillin and 4.1 mg/l for clavulanic acid. Elimination was slightly slower from lymph than from serum, the half-life being only 1.04 times longer from lymph than from serum for ticarcillin, but 1.22 times longer for clavulanic acid. The total areas under the concentration curves in lymph was 58% of the serum value of ticarcillin and 81.0% of clavulanic acid. This reflects the ability of the substances to penetrate to lymph. The mean 8-h urinary recovery was 63.7% of the dose of ticarcillin and 43.8% of clavulanic acid. The total body clearances were 14.61/h for ticarcillin and 7.91/h for clavulanic acid and the corresponding d beta distribution volumes 12.21 and 19.11. The ratio of the concentrations of ticarcillin to clavulanic acid in all body fluids increased with time. Pharmacokinetically, clavulanic acid is well suited to be given together with ticarcillin.
给11名健康志愿者静脉注射3.0克替卡西林和0.2克克拉维酸,并对其外周淋巴、血清和尿液进行8小时监测。采用微生物学方法测定浓度。0 - 1小时收集的淋巴液中替卡西林的平均水平为39.3毫克/升,克拉维酸为2.93毫克/升。淋巴液中的平均峰值浓度(出现在1.25至2.25小时之间)替卡西林为66.3毫克/升,克拉维酸为4.1毫克/升。淋巴液中的消除速度略慢于血清,替卡西林在淋巴液中的半衰期仅比血清长1.04倍,但克拉维酸长1.22倍。淋巴液中浓度曲线下的总面积为替卡西林血清值的58%,克拉维酸的81.0%。这反映了这些物质渗透到淋巴液中的能力。替卡西林8小时的平均尿回收率为给药剂量的63.7%,克拉维酸为43.8%。替卡西林的全身清除率为14.6升/小时,克拉维酸为7.9升/小时,相应的分布容积分别为12.2升和19.1升。所有体液中替卡西林与克拉维酸浓度之比随时间增加。从药代动力学角度来看,克拉维酸很适合与替卡西林一起给药。