Influence of food on the bioavailability of trimoprostil: an overview

The influence of food on the bioavailability of trimoprostil , a new antiulcer prostaglandin E2 derivative, was investigated in healthy male volunteers in four separate studies. Doses of 0.75, 1.5, and 3.0 mg were administered orally in both the presence and absence of food followed by serial blood sampling through 24 hours. Plasma trimoprostil concentrations were determined by a gas chromatograph-negative chemical ionization-mass spectrometric method for pharmacokinetic evaluation. Food decreased the absorption rate of trimoprostil as indicated by a later tmax (P less than 0.01) and corresponding lower Cmax at each dose. However, the food effect on tmax diminished as the dose increased. Although Cmax was reduced, food did not alter the extent of absorption, indicated by similar AUC (P greater than 0.05) between fed and fasted states. Both Cmax and AUC increased proportionately with an increase in dose. The harmonic mean half-lives of elimination were similar (P greater than 0.05) across all doses and ranged from 27 to 55 minutes.