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Local Gastric and Serum Concentrations of Rebamipide Following Oral Ingestion in Healthy Volunteers

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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 μg/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 μg/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.

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Authors and Affiliations

  1. Department of Endoscopy, Internal Medicine, and Laboratory Medicine, Shinshu University School of Medicine, 3-1-1 Asahi, Matsumoto, 390-8621, Japan

    Taiji Akamatsu, Naoshi Nakamura, Naoyuki Furuya, Toshiki Shimizu, Akira Gotou, Kendo Kiyosawa & Tsutomu Katsuyama

  2. Tokushima Research Institute, Otsuka Pharmaceutical Co., Ltd., 463-10 Kagasuno Kawauchi-cho, Tokushima, 771-0192, Japan

    Takahiko Osumi, Yukihiro Hirao & Gohatiro Miyamoto

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  1. Taiji Akamatsu
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  2. Naoshi Nakamura
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  3. Naoyuki Furuya
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  4. Toshiki Shimizu
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  5. Akira Gotou
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  6. Kendo Kiyosawa
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  7. Tsutomu Katsuyama
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  8. Takahiko Osumi
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  9. Yukihiro Hirao
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  10. Gohatiro Miyamoto
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Akamatsu, T., Nakamura, N., Furuya, N. et al. Local Gastric and Serum Concentrations of Rebamipide Following Oral Ingestion in Healthy Volunteers. Dig Dis Sci 47, 1399–1404 (2002). https://doi.org/10.1023/A:1015347219999

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