Leroy A, Humbert G, Fillastre J P
Scand J Infect Dis Suppl. 1981;29:49-54.
The pharmacokinetics of azlocillin were investigated in six healthy subjects with normal renal function. 40.4 to 69.6% of the injected dose was recovered, estimated as unchanged form, in urine during 24 h. After intravenous bolus injection of 15 and 30 mg/kg doses, pharmacokinetic data were calculated, using a two-compartment open body model. The mean distribution serum half-life (T1/2 alpha) was 0.11-0.12 h and the mean elimination serum half-life (T1/2 beta) was 0.79-0.89 h. The volume of the central compartment (Vc) was 7.36-8.01 1/1.73 m2 and the apparent volume of distribution (Vdss) was 14.12-14.32 1/1.73 m2. The mean T1/2 beta after a 30 min i.v. infusion of 80 mg/kg to the same healthy subjects was 1.10 h. Serum clearances (Cs) for 15, 30 and 80 mg/kg were 251.1, 214.0 and 152.9 ml/min/1.73 m2 and renal clearance (Cr) were 99.7, 145.2 and 94.1 ml/min/1.73 m2, respectively. Azlocillin pharmacokinetics were found to be dose dependent. Administration of probenecid increased the terminal serum half-life and the total area under the serum azlocillin concentration-time curve and decreased renal clearance, indicating that azlocillin is eliminated by both glomerular filtration and tubular secretion.
在6名肾功能正常的健康受试者中研究了阿洛西林的药代动力学。在24小时内，尿液中回收了注射剂量的40.4%至69.6%，估计为未变化的形式。静脉推注15和30mg/kg剂量后，使用二室开放身体模型计算药代动力学数据。平均分布血清半衰期（T1/2α）为0.11 - 0.12小时，平均消除血清半衰期（T1/2β）为0.79 - 0.89小时。中央室容积（Vc）为7.36 - 8.01 1/1.73 m²，表观分布容积（Vdss）为14.12 - 14.32 1/1.73 m²。对相同健康受试者静脉输注80mg/kg 30分钟后的平均T1/2β为1.10小时。15、30和80mg/kg的血清清除率（Cs）分别为251.1、214.0和152.9ml/min/1.73 m²，肾清除率（Cr）分别为99.7、145.2和94.1ml/min/1.73 m²。发现阿洛西林的药代动力学具有剂量依赖性。给予丙磺舒可延长终末血清半衰期和血清阿洛西林浓度 - 时间曲线下的总面积，并降低肾清除率，表明阿洛西林通过肾小球滤过和肾小管分泌两种方式消除。
