Abstract

This study was conducted to evaluate the pharma¬cokinetics, safety and gender difference of cefuroxime axetil after single dose administration under fasting and fed conditions in healthy Chinese male and female subjects. In an open-label, two-period study, 26 subjects received a single 250 mg oral dose with or without food. Blood samples were collected at scheduled time points till 24 h after drug administration and cefuroxime axetil concentration in blood was analysed using liquid chromatography with tandem mass spectrometry. Twenty-three subjects completed the study. Under fed state, the median time to peak plasma concentration of cefuroxime axetil was de¬layed by approximately 0.5 h compared with fasting state (2.23 h vs 3.01 h) and there was a 43.9 % increase in the total systemic exposure (AUC0-∞) and 8.3, 38.7, 34.1 % reduction in elimina¬tion half-life, apparent volume of distribution and apparent clearance, respectively. No significant difference presented in maximum concentra¬tion achieved (p>0.05). There was no gender difference in pharmacokinetics and no serious adverse events reported, as well. This study indicated that the extent of absorption of cefuroxime axetil is significantly increased under fed state and it is recommended to be administrated after a meal.