The effect of food on the pharmacokinetics of cefuroxime axetil was studied. Twelve healthy male subjects were included in this study. They were given single oral 500 mg doses of cefuroxime axetil alone or with food based on a balanced two-way crossover design. Plasma cefuroxime concentrations were assayed by the high performance liquid chromatographic method. When the drug was given alone, the area under the curve (AUC) was 15.77 +/- 4.12 mg*h/L, Cmax was 4.20 +/- 1.05 mg/L, Tmax was 2.36 +/- 0.84 h, T1/2 was 1.56 +/- 0.26 h, and Clp/F was 34.13 +/- 10.39 L/h; 45.12 +/- 9.59% of the dose was recovered in the urine within 24 hours, and the renal clearance was 12.58 +/- 4.41 L/h. When the drug was given with food, the corresponding AUC was 23.46 +/- 4.57 mg*h/L, Cmax was 7.10 +/- 1.41 mg/L, Tmax was 2.04 +/- 1.32 h, T1/2 was 1.40 +/- 0.23 h, and Clp/F was 21.93 +/- 5.18 L/h; the 24-hour urinary recovery was 69.33 +/- 6.13% and the renal clearance was 12.58 +/- 2.99 L/h. The above pharmacokinetic parameters obtained from the two regimens were compared by two-way ANOVA corrected for the change-over effect. No significant difference was found for Tmax, T1/2 or renal clearance (p > 0.05). Higher AUC, Cmax, urinary recovery and lower Clp/F values were observed for the regimen with food (p < 0.05). The plasma drug concentrations resulting from the regimen with food were higher throughout the 12-hour sampling period when compared to the regimen without food.(ABSTRACT TRUNCATED AT 250 WORDS)