Penetrations of latamoxef (LMOX) and cefaclor (CCL) into the aqueous humor after intravenous or oral administration were investigated in rabbits. Concentrations of antibiotics in plasma and aqueous humor after administration were determined periodically by microbiological assay. LMOX disappeared from plasma in a monoexponential manner with a half-life of 43 min after intravenous administration at a dose of 50 mg/kg. The maximum concentration of LMOX in aqueous humor (6.4 micrograms/ml) was observed 1 h after administration. When CCL was administered orally at a dose of 50 mg/kg, the maximum concentration of CCL in aqueous humor was 1.00 microgram/ml 1.5 h after administration, whereas the maximum plasma concentration of 19.2 micrograms/ml was observed at 30 min. Pharmacokinetic analysis (simultaneous simulation) of plasma and aqueous humor concentration-time courses was made using the best fitted compartment model examined (modified two-compartment model). Prediction of the concentration of antibiotics in aqueous humor from the plasma concentration profile was also examined using the same compartment model in a separate experiment. The predicted concentration in aqueous humor was proved to coincide reasonably well with the measured concentration.