Beermann B, Dalén E, Lindström B, Rosén A
Eur J Clin Pharmacol. 1975 Oct 10;9(1):51-61. doi: 10.1007/BF00613429.
35S-furosemide was administered orally (n=7) or i.v. (n=2) to healthy subjects. The average gastrointestinal uptake estimated by comparison of the urinary recovery of label and the areas under the plasma curves after the two routes of administration was 65%. The half life of radioactivity in the plasma after oral 35S-furosemide was 90 +/- 17 min (estimated on the slope between 2 and 6 h); the corresponding figure after 35S-furosemide i.v. was 47-53 min (slope 0.5-4 h). There was probably a slower phase after 4-6 h. Fractionation of labelled material in urine from two subjects demonstrated that approximately two thirds of the label recovered at 24 h had the same chromatographic properties as furosemide. A major part of the metabolite(s) was probably furosemide glucuronide. There was no evidence that 4-chloro-5-sulfamoylanthranilic acid was formed in man. The total urinary recovery of label (5-7 d) after oral and intravenous administration was 55.1 +/- 3.2 (mean +/- SD) and 82-84%, respectively. After 35S-furosemide i.v., 6-9% of the label was recovered in faeces, and it could not be accounted for solely by biliary excretion of furosemide.
将35S - 速尿口服(n = 7)或静脉注射(n = 2)给予健康受试者。通过比较两种给药途径后尿液中标记物的回收率和血浆曲线下面积估算的胃肠道平均摄取率为65%。口服35S - 速尿后血浆中放射性的半衰期为90±17分钟(根据2至6小时之间的斜率估算);静脉注射35S - 速尿后的相应数值为47 - 53分钟(斜率0.5 - 4小时)。4 - 6小时后可能存在一个较慢的阶段。对两名受试者尿液中标记物质的分级分离表明,在24小时回收的标记物中约三分之二具有与速尿相同的色谱性质。代谢物的主要部分可能是速尿葡糖醛酸苷。没有证据表明人体中会形成4 - 氯 - 5 - 氨磺酰基邻氨基苯甲酸。口服和静脉注射后标记物的总尿回收率(5 - 7天)分别为55.1±3.2(平均值±标准差)和82 - 84%。静脉注射35S - 速尿后,6 - 9%的标记物在粪便中回收,且不能仅通过速尿的胆汁排泄来解释。