抄録
Proton pump inhibitors (PPIs) are substituted benzimidazoles, which are unstable at a low pH. We hypothesized that rapid transit of a PPI to the upper small intestine has some benefit in PPI therapy. Mosapride citrate, a 5-hydroxytryptamine 4 receptor (5-HT4) agonist, has a profound effect on facilitating gastric motility. The aim of this study was to examine the effect of mosapride citrate on the pharmacokinetics of omeprazole. Eleven healthy volunteers were enrolled. After overnight fasting, 20 mg of omeprazole was given orally and plasma samples were obtained before and after 1, 2, 3 and 4 hours of dosing. Two weeks later, 5 mg of masapride citrate was given one hour before administration of 20 mg of omeprazole and plasma samples were obtained at the same time intervals as above. The plasma concentrations of omeprazole were determined by high performance liquid chromatography. Pharmacokinetic parameters, including the peak plasma concentration (Cmax), the time to reach Cmax (Tmax) and the area under the time-concentration curve during four hours of dosing (AUC4) were used for statistical analyses. Data from 10 out of 11 subjects was available. The Tmax was shifted from 2.22±0.44 h (mean±SD) to 1.66±0.50 h by mosapride citrate (P<0.05) . The Cmax increased from 363.5±293.3 ng / ml to 527.4±233.0 ng / ml in the presence of mosapride citrate (P<0.01) . The AUC4 was 632.0±183.3 ng h/ml and 1041.3±450.8 ng h/ml in the absence and presence of mosapride citrate, respectively (P<0.05) . Conclusions. Mosapride citrate beneficially affected pharmacokinetics of omeprazole probably by accelerating gastric motility.
