SINGLE ORAL DOSE PHARMACOKINETICS OF CENTBUTINDOLE, A NEW NEUROLEPTIC AGENT, IN HEALTHY-HUMAN VOLUNTEERS

Centbutindole, a butyrophenone derivative, is a new neuroleptic agent developed at the Central Drug Research Institute, Lucknow, India. The pharmacokinetics of this compound were investigated after oral administration of single 3mg tablets in 5 healthy male volunteers. Serum levels of the unchanged drug were measured by high pressure liquid chromatography (HPLC) with fluorescence detection. Mean peak serum levels (3.48 +/- 1.58 mg/L) were reached at 4 hours, and the mean biological half-life was calculated as 12.45 +/- 3.59 hours. The data were best fitted to a 1-compartment open model with first-order absorption and elimination kinetics. Considerable intersubject variability was noted in the absorption characteristics of centbutindole. and further study is planned to better define the pharmacokinetics of this drug.