Pharmacokinetics of an oral controlled release formulation of remoxipride : a double-blind, crossover comparison with conventional formulation in chronic schizophrenics

Twenty-four stable, chronic schizophrenic inpatients were entered in a double-blind, crossover study designed to compare single-dose and steady-state pharmacokinetics of remoxipride immediate release (IR) 200 mg twice daily and controlled release (CR) 400 mg once daily. The CR formulation showed a significantly delayed absorption of remoxipride from the gastrointestinal tract. At steady state there was significantly less fluctuation in plasma concentrations. The other pharmacokinetic variables studied showed no difference. The mean relative bioavailability with regard to the amount of remoxipride absorbed after administration in CR form as compared with the IR form was 97%. Both formulations were well tolerated and there was no difference in either the incidence or the severity of adverse events. It was concluded that, from a pharmacokinetic point of view, the CR formulation of remoxipride was suitable for a once daily dosage schedule.