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新型头孢菌素头孢匹罗的药代动力学及组织穿透性

Pharmacokinetics and tissue penetration of cefpirome, a new cephalosporin.

作者信息

Kavi J, Andrews J M, Ashby J P, Hillman G, Wise R

机构信息

Department of Medical Microbiology, Dudley Road Hospital, Birmingham, UK.

出版信息

J Antimicrob Chemother. 1988 Dec;22(6):911-6. doi: 10.1093/jac/22.6.911.

Abstract

The pharmacokinetics and tissue penetration (as measured by a blister fluid model) of cefpirome were studied in six male volunteers following a 1 g intravenous dose. A mean peak serum concentration (at 5 min) of 97.4 mg/l was followed by rapid distribution into an apparent volume of 21.3 1. The serum elimination half-life was 2.3 h. Cefpirome penetrated rapidly into inflammatory fluid with a mean peak concentration of 39.2 mg/l at 1.9 h. The mean inflammatory fluid elimination half-life was 2.5 h. The availability of the drug in inflammatory fluid was high with a mean per cent penetration of 123%. The plasma and renal clearances were 109.5 and 82.1 ml/min respectively. Twenty-four hour urinary recovery was 75.5% of the administered dose. This study suggests that a twice daily dosage may be sufficient to treat tissue infections with susceptible pathogens.

摘要

在6名男性志愿者静脉注射1g剂量头孢匹罗后,对其药代动力学及组织穿透性(通过水疱液模型测定)进行了研究。静脉注射后5分钟血清平均峰浓度为97.4mg/L,随后迅速分布至表观分布容积21.3L。血清消除半衰期为2.3小时。头孢匹罗迅速穿透至炎症液中,1.9小时时平均峰浓度为39.2mg/L。炎症液平均消除半衰期为2.5小时。药物在炎症液中的可利用度较高,平均穿透率为123%。血浆清除率和肾脏清除率分别为109.5ml/min和82.1ml/min。24小时尿回收率为给药剂量的75.5%。本研究提示,每日两次给药剂量可能足以治疗由敏感病原体引起的组织感染。

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