title: Local gastric and serum concentrations of rebamipide following oral ingestion in healthy volunteers.
abstract: The purpose of this study was to investigate whether sufficient concentrations of rebamipide (COR) are actually present in the stomach after its oral ingestion at an ordinary clinical dose. Twenty healthy volunteers (total 42 man-days) participated in the study. After ingestion of 100, 200, or 300 mg of rebamipide, endoscopy was performed at 1, 2, 4, and 6 hr, and gastric mucosa or gastric mucus was taken from the antrum. Venous blood samples were taken simultaneously. Samples were analyzed by high-performance liquid chromatography. The COR in the gastric mucosa and gastric mucus did not depend on the original amount ingested. After ingestion of rebamipide, each COR was higher than 10(-4) M (37 microg/g tissue) at 1 or 2 hr. On the other hand, the COR in serum did depend on the amount ingested and was lower than 10(-6) M (0.37 microg/ml) at every time tested. These results suggest that the COR in the stomach exceeds the levels that are needed for various antiulcer actions and that the rebamipide levels present in the gastric mucosa and gastric mucus result from local penetration.
authors.affiliation: Department of Endoscopy, Shinshu University School of Medicine, Matsumoto, Nagano, Japan.
authors.forename: Taiji
authors.initials: T
authors.lastname: Akamatsu
authors.forename: Naoshi
authors.initials: N
authors.lastname: Nakamura
authors.forename: Naoyuki
authors.initials: N
authors.lastname: Furuya
authors.forename: Toshiki
authors.initials: T
authors.lastname: Shimizu
authors.forename: Akira
authors.initials: A
authors.lastname: Gotou
authors.forename: Kendo
authors.initials: K
authors.lastname: Kiyosawa
authors.forename: Tsutomu
authors.initials: T
authors.lastname: Katsuyama
authors.forename: Takahiko
authors.initials: T
authors.lastname: Osumi
authors.forename: Yukihiro
authors.initials: Y
authors.lastname: Hirao
authors.forename: Gohatiro
authors.initials: G
authors.lastname: Miyamoto
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000409:Alanine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics*; D000897:Anti-Ulcer Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D005753:Gastric Mucosa / Q000378:metabolism*; D006801:Humans; D008297:Male; D009093:Mucus / Q000737:chemistry*; D015363:Quinolones / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
chemical_list: D000897:Anti-Ulcer Agents; D015363:Quinolones; C052785:rebamipide; D000409:Alanine