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头孢菌素SM - 1652在小鼠、大鼠、兔子、狗和恒河猴体内的药代动力学。

Pharmacokinetics of the cephalosporin SM-1652 in mice, rats, rabbits, dogs, and rhesus monkeys.

作者信息

Matsui H, Yano K, Okuda T

出版信息

Antimicrob Agents Chemother. 1982 Aug;22(2):213-7. doi: 10.1128/AAC.22.2.213.

Abstract

The pharmacokinetics of SM-1652 were studied in mice, rats, rabbits, dogs, and rhesus monkeys. The plasma half-lives of SM-1652, administered intravenously at a dose of 20 mg/kg, were 11.0 min in mice, 26.0 min in rats, 65.8 min in rabbits, 72.6 min in dogs, and 150.9 min in monkeys. The 24-h urinary excretion of SM-1652 was 30 to 35% of the dose in mice and rats, 70 to 75% in rabbits and dogs, and 45% in monkeys. Biliary excretion of the antibiotic over a 24-h period was 60 and 19% in rats and rabbits, respectively; it was 19% in dogs over a 9-h period after SM-1652 administration. Approximately 95% of the intravenous dose of SM-1652 was recovered as the unchanged form in the urine and bile of rats and rabbits. The binding of SM-1652 to serum protein was 44.0% in mice, 46.0% in rats, 90.4% in rabbits, 93.2% in monkeys, 30.0% in dogs, and 96.3% in humans.

摘要

在小鼠、大鼠、兔子、狗和恒河猴中研究了SM - 1652的药代动力学。以20mg/kg的剂量静脉给药后,SM - 1652在小鼠中的血浆半衰期为11.0分钟,在大鼠中为26.0分钟,在兔子中为65.8分钟,在狗中为72.6分钟,在猴子中为150.9分钟。SM - 1652在小鼠和大鼠中的24小时尿排泄量为剂量的30%至35%,在兔子和狗中为70%至75%,在猴子中为45%。在24小时内,抗生素在大鼠和兔子中的胆汁排泄量分别为60%和19%;在给SM - 1652后9小时内,狗的胆汁排泄量为19%。静脉注射剂量的SM - 1652中约95%以原形在大鼠和兔子的尿液和胆汁中回收。SM - 1652与血清蛋白的结合率在小鼠中为44.0%,在大鼠中为46.0%,在兔子中为90.4%,在猴子中为93.2%,在狗中为30.0%,在人类中为96.3%。

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