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头孢拉定:一种新型头孢菌素抗生素在动物体内的吸收、排泄及组织分布

Cephradine: absorption, excretion, and tissue distribution in animals of a new cephalosporin antibiotic.

作者信息

Weliky I, Gadebusch H H, Kripalani K, Arnow P, Schreiber E C

出版信息

Antimicrob Agents Chemother. 1974 Jan;5(1):49-54. doi: 10.1128/AAC.5.1.49.

Abstract

Metabolic studies were conducted with cephradine administred by the oral, subcutaneous, intravenous, or rectal routes to mice, rats, and dogs. Peak blood levels were usually attained in 30 to 150 min after dosing, depending on the animal species studied. Based on urinary excretion, cephradine appeared to be well absorbed after oral or subcutaneous administration; after rectal doses, cephradine was absorbed poorly. In rats and dogs given oral or intravenous doses of cephradine, about 70 to 100% of the administered dose was recovered during a 24-h collection period. Cephradine was excreted unchanged. After the oral or intravenous administration of [(3)H]cephradine to rats and dogs, respectively, its plasma half-life was about 1 h. After oral administration to rats, cephradine was distributed widely throughout the body tissues, with the greatest concentrations in the kidneys and liver; at 45 min to 6 h postdose, cephradine concentrations in the kidneys and liver were about 8 and 3 times higher, respectively, than those in plasma.

摘要

采用口服、皮下注射、静脉注射或直肠给药的方式,对小鼠、大鼠和犬进行了头孢拉定的代谢研究。给药后,血药浓度峰值通常在30至150分钟内达到,这取决于所研究的动物种类。基于尿排泄情况,口服或皮下给药后,头孢拉定似乎吸收良好;直肠给药后,头孢拉定吸收较差。给大鼠和犬口服或静脉注射头孢拉定后,在24小时的收集期内,约70%至100%的给药剂量被回收。头孢拉定以原形排泄。分别给大鼠和犬口服或静脉注射[(3)H]头孢拉定后,其血浆半衰期约为1小时。给大鼠口服后,头孢拉定广泛分布于全身组织,在肾脏和肝脏中的浓度最高;给药后45分钟至6小时,肾脏和肝脏中的头孢拉定浓度分别比血浆中的浓度高约8倍和3倍。

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