A NEW ORAL FORMULATION OF TIAPRIDE (DROPS) - PHARMACOKINETIC PROFILE AND THERAPEUTIC APPLICATIONS

Tiapride is a substituted benzamide widely used in the management of a gitation and aggressiveness in the elderly. The development of an oral solution is of particular interest in geriatric medicine and in patie nts with difficulties swallowing solid formulations. The bioequivalenc e between a sweetened, flavoured oral drop and tablet forms of tiaprid e 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-infi nity), 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 wh ich plasma concentration could be quantified, and AUC(0-infinity),is t he area under the curve extrapolated to infinity. The plasma eliminati on half-lives were similar (4.37 hours and 4.61 hours) and the relativ e bioavailability of the drop formulation was 99.7%. These results dem onstrated the bioequivalence of the two formulations. The drop formula tion in this bioequivalence study was the one used for clinical evalua tion in the target population of elderly patients experiencing restles sness and aggressive behaviour that was assessed in a prospective doub le-blind, randomised, previously published trial in 176 patients. In t hat study, tiapride as a drop formulation compared with melperone was safe and effective with regard to restlessness and aggressive behaviou r in elderly patients.