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新型广谱头孢菌素头孢尼西的药代动力学

Pharmacokinetics of cefonicid, a new broad-spectrum cephalosporin.

作者信息

Barriere S L, Hatheway G J, Gambertoglio J G, Lin E T, Conte J E

出版信息

Antimicrob Agents Chemother. 1982 Jun;21(6):935-8. doi: 10.1128/AAC.21.6.935.

Abstract

This study determined the pharmacokinetic disposition of cefonicid. A single dose of 7.5 mg/kg of body weight was administered to five healthy volunteers as a 5-min intravenous infusion. Multiple plasma and urine samples were collected for 48 h. Peak plasma concentrations ranged from 95 to 156 micrograms/ml and fell slowly (mean plasma half-life, 4.4 +/- 0.8 h), so that levels after 12 h were in the range of 6 to 12 micrograms/ml. Urinary concentrations were high but variable and ranged from 100 to 1,000 micrograms/ml for the first 12 h after the dose and averaged 84 micrograms/ml between 12 and 24 h. Plasma and renal clearances were 0.32 +/- 0.06 and 0.29 +/- 0.05 ml/min per kg, respectively. An average of 88 +/- 6% of the dose was excreted unchanged in the urine over 48 h. The mean steady-state volume of distribution was found to be 0.11 +/- 0.01 liters/kg.

摘要

本研究确定了头孢尼西的药代动力学特征。给5名健康志愿者静脉输注7.5mg/kg体重的单剂量药物,输注时间为5分钟。在48小时内采集了多个血浆和尿液样本。血浆峰值浓度在95至156微克/毫升之间,且下降缓慢(平均血浆半衰期为4.4±0.8小时),因此12小时后的浓度在6至12微克/毫升范围内。尿液浓度较高但变化较大,给药后前12小时尿液浓度在100至1000微克/毫升之间,12至24小时平均为84微克/毫升。血浆清除率和肾脏清除率分别为0.32±0.06和0.29±0.05毫升/分钟/千克。在48小时内,平均88±6%的剂量以原形经尿液排泄。平均稳态分布容积为0.11±0.01升/千克。

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