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头孢乙腈、头孢唑林和头孢孟多在大鼠体内的组织分布比较

Comparative tissue distribution of ceforanide, cefazolin, and cefamandole in rats.

作者信息

Lee F H, Smyth R D, Van Harken D R

出版信息

Antimicrob Agents Chemother. 1981 Apr;19(4):625-7. doi: 10.1128/AAC.19.4.625.

Abstract

The comparative tissue distribution of ceforanide, cefazolin, and cefamandole was determined in rats after subcutaneous doses of 100 mg/kg. Ceforanide had the longest plasma half-life, 0.9 h, versus 0.5 h for cefazolin and 0.4 h for cefamandole, and the highest area under the plasma concentration time curve, 324 micrograms x h per ml, versus 184 micrograms x h per ml for cefazolin and 42 micrograms x h per ml for cefamandole. The peak plasma concentrations of ceforanide and cefazolin were 173 and 140 micrograms/ml, respectively, and were threefold higher than that of cefamandole (49 micrograms/ml). Measureable concentrations of the three compounds were found in the liver, kidneys, lungs, submaxillary glands, cervical lymph nodes, bones, heart, abdominal muscles, eyes, and testes, with cefamandole levels being generally lower and more variable. The peak tissue levels of ceforanide and cefazolin were comparable, within the limit of data variation, and were considerably higher than that of cefamandole. The tissue half-lives of these cephalosporins were similar to the respective plasma half-lives.

摘要

皮下注射剂量为100mg/kg后,在大鼠体内测定了头孢乙腈、头孢唑林和头孢孟多的组织分布情况。头孢乙腈的血浆半衰期最长,为0.9小时,而头孢唑林为0.5小时,头孢孟多为0.4小时;头孢乙腈的血浆浓度-时间曲线下面积最高,为324μg·h/ml,而头孢唑林为184μg·h/ml,头孢孟多为42μg·h/ml。头孢乙腈和头孢唑林的血浆峰值浓度分别为173μg/ml和140μg/ml,比头孢孟多(49μg/ml)高3倍。在肝脏、肾脏、肺、下颌下腺、颈部淋巴结、骨骼、心脏、腹部肌肉、眼睛和睾丸中均发现了这三种化合物的可测量浓度,其中头孢孟多的浓度通常较低且变化较大。在数据变化范围内,头孢乙腈和头孢唑林的组织峰值水平相当,且远高于头孢孟多。这些头孢菌素的组织半衰期与各自的血浆半衰期相似。

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