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新型广谱头孢菌素SCE - 963在小鼠、大鼠、兔子和狗体内的吸收、分布及排泄情况。

Absorption, distribution and excretion of SCE-963, a new broad-spectrum cephalosporin, in mice, rats, rabbits and dogs.

作者信息

Tsuchiya K, Kondo M, Kita Y, Noji Y, Takeuchi M, Fugono T

出版信息

J Antibiot (Tokyo). 1978 Dec;31(12):1272-82. doi: 10.7164/antibiotics.31.1272.

Abstract

A single dose of 20 mg/kg of SCE-963 [7beta-]2-(aminothiazol-4-yl)acetamido]-3-[[[1-(2-dimethylaminoethyl)-1H-tetrazol-5-yl]thio]methyl]ceph-3-em-4-carboxylic acid] was administered subcutaneously to mice, intramuscularly to rats, rabbits and dogs. Plasma and tissue levels of SCE-963 reached a peak in 15 approximately 30 minutes after administration. In mice, rats and dogs, SCE-963 was distributed at high concentration in the descending order in the kidney, liver, plasma, lung and spleen, and in rabbits, in the kidney, plasma, lung, liver and spleen. The SCE-963 levels in the liver of mice, rats and dogs were higher than those of cefazolin, cephaloridine and cephalothin. The plasma and tissue levels of SCE-963 in mice and rats diminished rapidly, but those in rabbits and dogs declined gradually. SCE-963 was mainly excreted in the urine. The rate of excretion of SCE-963 in the bile was two to three times higher than that of cefazolin.

摘要

以20毫克/千克的剂量给小鼠皮下注射SCE - 963[7β - [2 -(氨基噻唑 - 4 - 基)乙酰胺基]-3 - [[[1 -(2 - 二甲基氨基乙基)-1H - 四氮唑 - 5 - 基]硫代]甲基]头孢 - 3 - 烯 - 4 - 羧酸],给大鼠、兔子和狗肌肉注射。给药后约15至30分钟,SCE - 963的血浆和组织水平达到峰值。在小鼠、大鼠和狗中,SCE - 963在肾脏、肝脏、血浆、肺和脾脏中的分布浓度由高到低,在兔子中,分布顺序为肾脏、血浆、肺、肝脏和脾脏。小鼠、大鼠和狗肝脏中的SCE - 963水平高于头孢唑林、头孢噻啶和头孢噻吩。小鼠和大鼠体内SCE - 963的血浆和组织水平迅速下降,但兔子和狗体内的水平则逐渐下降。SCE - 963主要经尿液排泄。SCE - 963在胆汁中的排泄率比头孢唑林高两到三倍。

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