Hansen I B, Jacobsen E, Weis J
Clin Pharmacol Ther. 1975 Mar;17(3):339-47. doi: 10.1002/cpt1975173339.
In a pharmacolinetic study on a new semisynthetic penicillin, alpha-sulfobenzylpenicillin, sulbenicillin, serum level, serum half-life, apparent distribution volume, renal clearance, urinary excretion, and metabolism were determined after a 4-gm intravenous dose and compared to that of carbenicillin in 5 patients with normal renal function. In the case of sulbenicillin, the mean serum concentration at 1 hr was 157 plus or minus 25 mug/ml, the mean serum half-life was 70 plus or minus 10 min, the renal clearance was 95 plus or minus 25 ml/min, and the total urinary recovery after 24 hr was about 80% of the dose. The only metabolite detected in the urine was the penicilloic acid derivative, in an amount usually less than 5% of the dose. Serum values, serum half-live, renal clearances, and excretion pattern did not differ significantly from that of carbenicillin. In 8 patients with decreased renal function (creatinine clearance less than 50 ml/min) there was an inverse correlation between creatinine clearance and serum half-life.
在一项关于新型半合成青霉素——α-磺苄青霉素(羧磺苄青霉素)的药代动力学研究中,对5例肾功能正常的患者静脉注射4克药物后,测定了血清水平、血清半衰期、表观分布容积、肾清除率、尿排泄及代谢情况,并与羧苄青霉素进行了比较。就羧磺苄青霉素而言,1小时时的平均血清浓度为157±25微克/毫升,平均血清半衰期为70±10分钟,肾清除率为95±25毫升/分钟,24小时后的尿总回收率约为给药剂量的80%。尿液中检测到的唯一代谢物是青霉素酸衍生物,其含量通常少于给药剂量的5%。血清值、血清半衰期、肾清除率及排泄模式与羧苄青霉素相比无显著差异。在8例肾功能减退(肌酐清除率低于50毫升/分钟)的患者中,肌酐清除率与血清半衰期呈负相关。