Mariño E L, Pajares M, Dominguez-Gil A A, Cepeda M, Dominguez-Gil A
Arzneimittelforschung. 1981;31(9):1459-61.
The pharmacokinetics of (6R,7R)-7-[(R)-2-amino-2-(p-hydroxyphenyl)-acetamido]-3-methyl-8-oxo-5-thia-1- azabicyclo-[4,2,0]-oct-2-ene-carbonic acid (cefadroxil) were studied in rabbits with normal renal function and with varying degrees of renal impairment induced experimentally by i.v. administration of uranyl nitrate at a dose of 4 mg/kg. All animals received a single oral dose of 50 mg/kg of cefadroxil. The serum, urinary and bile concentrations of the antibiotic were determined by a microbiological method. The antibiotic follows a single-compartment kinetic model. In rabbits with renal impairment a significant decrease in Ka and Ke occurred together with an increase in the values of tmax and (AUC)0 infinity, which are related to the serum creatinine concentrations, used as an index of the degree of renal function.
研究了(6R,7R)-7-[(R)-2-氨基-2-(对羟基苯基)-乙酰胺基]-3-甲基-8-氧代-5-硫杂-1-氮杂双环-[4,2,0]-辛-2-烯-碳酸(头孢羟氨苄)在肾功能正常及通过静脉注射4mg/kg硝酸铀酰实验性诱导出不同程度肾功能损害的家兔体内的药代动力学。所有动物均接受50mg/kg头孢羟氨苄的单次口服剂量。通过微生物学方法测定抗生素的血清、尿液和胆汁浓度。该抗生素符合单室动力学模型。在肾功能损害的家兔中,Ka和Ke显著降低,同时tmax和(AUC)0至无穷大的值增加,这些值与用作肾功能程度指标的血清肌酐浓度相关。