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Influence of Food on the Bioavailability of Trimoprostil: An Overview
Author(s) -
WILLS ROBERT J.
Publication year - 1984
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1984.tb01830.x
Subject(s) - bioavailability , pharmacokinetics , chemistry , absorption (acoustics) , plasma concentration , pharmacology , zoology , medicine , biology , physics , acoustics
The influence of food on the bioavailability of trimoprostil, a new antiulcer prostaglandin E 2 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 chromatographnegative chemical ionization‐mass spectrometric method for pharmacokinetic evaluation. Food decreased the absorption rate of trimoprostil as indicated by a later t max ( P < 0.01) and corresponding lower C max at each dose. However, the food effect on t max diminished as the dose increased. Although C max was reduced, food did not alter the extent of absorption, indicated by similar AUC ( P > 0.05) between fed and fasted states. Both C max and AUC increased proportionately with an increase in dose. The harmonic mean half‐lives of elimination were similar ( P > 0.05) across all doses and ranged from 27 to 55 minutes.