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Pharmacology: Pharmacodynamics: Rebamipide increases prostaglandin E2 in gastric mucosa, decreases gastric mucosa injury, increases gastric mucous, increases blood flow of gastric mucosa, increases secretion of gastric alkaline, stimulates growth of gastric mucosa cells.
Pharmacokinetics: The drug is rapidly absorbed. The absorption tended to be slow when the drug was administered orally after a meal. However, food did not affect bioavailability.
Peak plasma concentration: 210 ng/mL.
Time to peak concentration: 2 hours.
Elimination half-life: 1.5 hours.
Protein binding: 98.4%-98.6%.
Approximately 10% of the administered dose was excreted in the urine as the unchanged compound. A metabolite with a hydroxyl group at the 8th position was identified in the urine. The excretion of this metabolite was only 0.03% of the administered dose. The enzyme involved in the formation of the metabolite was CYP3A4.
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