Wills R J
J Clin Pharmacol. 1984 Apr;24(4):194-201. doi: 10.1002/j.1552-4604.1984.tb01830.x.
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.
在四项独立研究中，对健康男性志愿者研究了食物对新型抗溃疡前列腺素E2衍生物曲莫前列素生物利用度的影响。在有食物和无食物的情况下，均口服0.75、1.5和3.0毫克剂量的曲莫前列素，随后在24小时内进行连续采血。通过气相色谱-负化学电离-质谱法测定血浆曲莫前列素浓度，用于药代动力学评估。食物降低了曲莫前列素的吸收速率，表现为各剂量下tmax延迟（P<0.01）以及相应的较低Cmax。然而，食物对tmax的影响随着剂量增加而减弱。尽管Cmax降低，但食物并未改变吸收程度，喂食和禁食状态下的AUC相似（P>0.05）表明了这一点。Cmax和AUC均随剂量增加而成比例增加。消除的调和平均半衰期在所有剂量下相似（P>0.05），范围为27至55分钟。
