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头孢噻吩和头孢曲松在兔实验性间质组织液中的分布。

Distribution of cephalothin and ceftriaxone into experimental interstitial tissue fluid in rabbits.

作者信息

Gonzalez Molinello A, Alonso Gonzalez A C, Mariño E L, Dominguez-Gil A

出版信息

Arzneimittelforschung. 1986 Jul;36(7):1082-5.

PMID:3768077
Abstract

A study was carried out on the access and residence of cephalothin and ceftriaxone in interstitial tissue fluid (ITF) produced experimentally by subcutaneous implantation of spiral steel cages after administration of 30 mg/kg of the two antibiotics to rabbits. The levels reached by the drug in serum and ITF were determined by a microbiological plate diffusion method. The elimination half-lives of cephalothin and ceftriaxone showed mean values of 0.23 and 1.77 h, respectively. Both these values were lower than those found for the disappearance half-lives from ITF. Cephalothin reached a maximum concentration in ITF of 4.37 micrograms/ml at 0.52 h, while ceftriaxone showed a maximum concentration of 24.94 micrograms/ml at 2.09 h. The area under the curve of tissue concentrations of ceftriaxone was approximately 20-fold greater than that of cephalothin at the same dose and using same administration route. The index of the penetration capacity expressed as the quotient of the respective AUC's in ITF and in the systemic circulation gave a value for ceftriaxone which was approximately double that obtained for cephalothin.

摘要

对家兔皮下植入螺旋钢笼以实验性地产生间质组织液(ITF)后,给予30mg/kg的头孢噻吩和头孢曲松这两种抗生素,对其在ITF中的进入和存留情况进行了一项研究。通过微生物平板扩散法测定药物在血清和ITF中达到的水平。头孢噻吩和头孢曲松的消除半衰期分别显示出平均值为0.23小时和1.77小时。这两个值均低于从ITF中消失半衰期的值。头孢噻吩在0.52小时时在ITF中达到最大浓度4.37微克/毫升,而头孢曲松在2.09小时时显示最大浓度24.94微克/毫升。在相同剂量和相同给药途径下,头孢曲松的组织浓度曲线下面积比头孢噻吩大约大20倍。以ITF和体循环中各自的AUC之商表示的渗透能力指数,头孢曲松的值约为头孢噻吩所得值的两倍。

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