Absolute bioavailability of carbamazepine after oral administration of a 2% syrup

Two healthy male volunteers received 10 mg carbamazepine (CBZ) as a 2-h constant-rate intravenous (i.v.) infusion and 100 mg 15N-labeled CBZ as a 2% oral suspension, concomitantly. The two compounds have identical pharmacokinetics. Their respective concentrations in plasma were determined by gas chromatography-mass spectrometry (GC-MS) for 168 h. The comparison of the areas under the plasma curves (AUC) obtained by the two routes of administration, showed the systemic availability of CBZ given as an oral suspension to be equal to its availability when given intravenously. A two-compartment model was estimated: The apparent volume of distribution of CBZ at the steady-state (Vss) was approximately 1 L/kg.