Absorption

Grepafloxacin is rapidly and extensively absorbed following oral administration of RAXAR Tablets Bioavailability of the tablet is equivalent to the bioavailability of an oral solution of grepafloxacin. The absolute bioavailability of RAXAR Tablets was estimated by comparing the areas under the plasma grepafloxacin concentration versus time curve (AUC) after intravenous and oral administration of grepafloxacin in separate studies. The absolute bioavailability is approximately 70%.

Single-dose and steady-state pharmacokinetic parameters following administration of 400 mg and 600 mg doses to healthy adult males are displayed in Table 1.

*AUC=AUC_¥ for single-dose; AUC_0-24 for steady-state.

On average, the peak plasma drug concentration (C_max) is achieved 2 to 3 hours after dosing. Steady-state concentrations of grepafloxacin are achieved within 7 days of once a day dosing.

Grepafloxacin pharmacokinetic parameters were determined following administration of 600 mg grepafloxacin immediately following a high fat meal (1000 kcal, 67 grams fat, 38 grams protein, 63 grams carbohydrates) and administration in the fasted state (n=29). There was no difference in grepafloxacin pharmacokinetic parameters between the fasted and fed treatments. Milk had no effect on the C_max, T_max, or AUC of grepafloxacin after oral administration. Neutralization of gastric acidity by intravenous administration of the histamine type-2 receptor antagonist famotidine did not affect the absorption or other pharmacokinetic properties of RAXAR Tablets

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