A new oral formulation of tiapride (drops): pharmacokinetic profile and therapeutic applications

Tiapride is a substituted benzamide widely used in the management of agitation and aggressiveness in the elderly. The development of an oral solution is of particular interest in geriatric medicine and in patients with difficulties swallowing solid formulations. The bioequivalence between a sweetened, flavoured oral drop and tablet forms of tiapride was investigated in a crossover design in 18 healthy male volunteers after a 100mg single-dose administration of each formulation. Plasma concentration profiles were determined. No significant differences in the extent and rate of absorption (t(max), C(max), AUC(0-t) or AUC(0-infinity), C(max )/AUC(0-infinity)) were observed, where t(max) is the time to reach the maximum plasma concentration (C(max)), AUC(0-t) is the area under the concentration-time curve from zero to the last sample at which plasma concentration could be quantified, and AUC(0-infinity) is the area under the curve extrapolated to infinity. The plasma elimination half-lives were similar (4.37 hours and 4.61 hours) and the relative bioavailability of the drop formulation was 99.7%. These results demonstrated the bioequivalence of the two formulations. The drop formulation in this bioequivalence study was the one used for clinical evaluation in the target population of elderly patients experiencing restlessness and aggressive behaviour that was assessed in a prospective double-blind, randomised, previously published trial in 176 patients. In that study, tiapride as a drop formulation compared with melperone was safe and effective with regard to restlessness and aggressive behaviour in elderly patients.