REPEATED DOSE PHARMACOKINETICS OF PANCOPRIDE IN HUMAN VOLUNTEERS

The aim of this study was to assess the pharmacokinetic profile of pan copride after repeated oral dose administration of 20 mg pancopride in tablet form once a day for 5 d in 12 healthy male volunteers. Plasma levels were measured by HPLC using a solid phase extraction method and automated injection. The minimum quantification limit of pancopride i n plasma was 2 ng mL(-1). The maximum plasma concentration (mean+/-SD) after the first dose was 92.5+/-41.5 ng mL(-1) and t(max) was 1.7+/-0 .9 h. The elimination half-life (t(1/2)) was 14.3+/-6.9 h. The area un der the concentration-time curve from zero to infinity (AUC) was 997+/ -396 ng h mL(-1). The maximum plasma concentration (mean+/-SD) at stea dy state (day 5) was 101.8+/-36.9 ng mL(-1) and t(max) was 2.2+/-1.2 h . The elimination half-life (t(1/2)) was 16.3+/-2.7 h and the minimum plasma concentration (C-min(ss) was 16.6+/-6.9 ng mL(-1). The area und er the concentration-time curve during the dosing interval (AUC(r)(ss) ) was 995+/-389 ng h mL(-1). The average plasma concentration at stead y state (C-av(ss)) was 43.3+/-16.1 ng mL(-1) and the experimental accu mulation ratio (R(AUC)) was 1.34+/-0.19, whereas the mean theoretical value (R) was 1.40+/-0.29. The results obtained showed a good correlat ion between the experimental plasma levels and the expected values cal culated using a repeated dose two-compartment model assessed by means of the Akaike value. It is concluded that the pharmacokinetics of panc opride are not modified after repeated dose administration. The safety parameters showed no clinically relevant alterations.