Mezlocillinに関する薬理学的研究

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タイトル別名
  • PHARMACOLOGICAL STUDIES ON MEZLOCILLIN
  • Mezlocillin ニ カンスル ヤクリガクテキ サヨウ 2 セイタイナイ
  • SECOND REPORT: DISTRIBUTION, FATE AND EXCRETION
  • 第2報, 生体内動態

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Fates of Mezlocillin, an ureido penicillin and 14C-Mezlocillin (half life, distribution, urinary and biliary excretion, metabolism, transfer to the fetus, binding to protein and partition coefficient) were investigated in rats and rabbits.<BR>Biological half lives of 50 mg/kg of Mezlocillin injected intravenously or intramuscularly in rats were 5.73 and 11.59 min, respectively.<BR>Biological half lives of 50 mg/kg of Mezlocillin administered by infusion and one shot injection in rabbits were 59.23 min and 19.91 min, respectively. The half life prolonged with the increase in the doses applied.<BR>The biological half life of Mezlocillin in the injected site of muscle was 10.16 min. The organ levels peaked 15 min after administration, and the duodenum and kidney levels were higher than the serum level. After intravenous or intramuscular injection of Mezlocillin in rats, 28.79% or 19.71% were excreted in 24hr-urine, respectively. In rabbits, 22.90% and 27.88% excreted within 6 hr in urine, respectively. Most of it was excreted within 1 hr after administration. The total amounts excreted in 6 hr-bile of the rabbit administered Mezlocillin by infusion and one shot injection were 20.74% and 18.74%, respectively. The biliary level peaked within the first 30 min after administration. Findings show that Mezlocillin is rapidly transfered to the organs from blood, and excreted in the urine and bile. The main route of excretion of Mezlocillin is through the urine and bile, and reabsorption from the intestine is negligible. Only Mezlocillin existed in the urine, and BAY i 6296 (the cleaved substance of lactam ring of Mezlocillin) existed in the feces. The cord blood level of Mezlocillin was approximately 10% of the maternal serum level in the pregnant rat. Approximately 60% of Mezlocillin was bound to proteins. These findings were confirmed by the experiments using 14C-Mezlocillin.

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