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[头孢克肟在志愿者体内的药代动力学及与新型酯前药头孢菌素的文献比较]

[Pharmacokinetics of cefixime in volunteers and a literature comparison with the new ester prodrug cephalosporins].

作者信息

Kees F, Naber K G

机构信息

Lehrstuhl für Pharmakologie der Universität, Regensburg, Germany.

出版信息

Infection. 1990;18 Suppl 3:S150-4. doi: 10.1007/BF01644636.

Abstract

The pharmacokinetic parameters of cefixime were determined in healthy volunteers following oral administration of 200 mg cefixime as tablet, syrup and dry suspension, respectively. All three galenic formulations showed reliable absorption. Mean peak plasma concentrations amounted to 2.4-3.4 mg/l and were reached after 3.3-3.5 h. Mean terminal half-lives were 2.9-3.1 h. The mean areas under the plasma concentration-time curves ranged between 18 and 26 mg/l.h; 18-24% of the dose administered were recovered unchanged in the urine. The best bioavailability was obtained with the dry suspension followed by the tablet and the syrup. With respect to the ester pro-drug cephalosporins, cefuroxime axetil, cefetamet pivoxyl and cefotiam hexetil, cefixime exhibits higher plasma half-life and area under the curve as well as, comparable absolute bioavailability but consistently lower urinary recovery which indicates higher non-renal clearance.

摘要

分别以片剂、糖浆剂和干混悬剂的形式给健康志愿者口服200毫克头孢克肟后,测定了头孢克肟的药代动力学参数。所有三种剂型均显示出可靠的吸收。平均血浆峰浓度为2.4 - 3.4毫克/升,在3.3 - 3.5小时后达到。平均末端半衰期为2.9 - 3.1小时。血浆浓度-时间曲线下的平均面积在18至26毫克/升·小时之间;给药剂量的18 - 24%以原形从尿液中回收。干混悬剂的生物利用度最佳,其次是片剂和糖浆剂。与酯前体药物头孢菌素(头孢呋辛酯、头孢他美酯和头孢替安酯)相比,头孢克肟具有更长的血浆半衰期和曲线下面积,以及相当的绝对生物利用度,但尿回收率始终较低,这表明其非肾清除率较高。

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