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Small bowel tissue concentration of rebamipide: study of two dosages in healthy subjects.

Akamatsu T, Nagaya T, Ichikawa S, Sudo T, Takeda R, Takenaka K, Kodama R, Ito T, Arakura N, Tanaka E - J Clin Biochem Nutr (2010)

Bottom Line: The purpose of this study is to investigate whether the effective concentrations of rebamipide (COR) are present in the small intestine after taking an ordinary clinical dose and double dose of this drug.Mean COR in the stomach was less than 100 µM at 1 h in the 100 mg group; however it was higher than 100 µM in the 200 mg group.In conclusion, the COR level in the jejunum was sufficient to protect for NSAID-induced gastrointestinal complications.

View Article: PubMed Central - PubMed

Affiliation: Endoscopy Center, Nagano Prefectural Hospital Organization, Suzaka Hospital, 1332 Suzaka, Suzaka, Nagano 382-0091, Japan.

ABSTRACT
Non-steroidal anti-inflammatory drug (NSAID)-related small intestinal complications exist, since developed new diagnostic modalities, such as balloon and capsule endoscopies. Some experiments have shown rebamipide to protect from NSAID-induced small intestinal complications. The purpose of this study is to investigate whether the effective concentrations of rebamipide (COR) are present in the small intestine after taking an ordinary clinical dose and double dose of this drug. Twelve healthy male subjects were enrolled. After taking 100 or 200 mg of rebamipide, balloon enteroscopy was performed at 1 and 3 h, and biopsy samples were obtained from the jejunum and the stomach. Venous blood samples were taken simultaneously. Samples were analyzed by high-performance liquid chromatography. The mean COR in the jejunum was higher than 100 µM at 1 h and higher than 10 µM at 3 h in both the 100 and 200 mg groups. Mean COR in the stomach was less than 100 µM at 1 h in the 100 mg group; however it was higher than 100 µM in the 200 mg group. In conclusion, the COR level in the jejunum was sufficient to protect for NSAID-induced gastrointestinal complications.

No MeSH data available.


Related in: MedlinePlus

Gastric mucosa, small intestine and serum concentration of rebamipide at 1 h and 3 h after administration (mean ± SD, n = 6 each). Broken lines show pharmacological actions of rebamipide have been confirmed by in vitro experimental studies to require COR of more than 1 µM to 100 µM.
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Related In: Results  -  Collection


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Figure 2: Gastric mucosa, small intestine and serum concentration of rebamipide at 1 h and 3 h after administration (mean ± SD, n = 6 each). Broken lines show pharmacological actions of rebamipide have been confirmed by in vitro experimental studies to require COR of more than 1 µM to 100 µM.

Mentions: In the 100 mg group, the mean COR level was 146.3 ± 203.1 µM at 1 h after taking rebamipide, and 54.9 ± 47.8 µM at 3 h. In the 200 mg group, the mean COR level was 153.5 ± 183.1 µM at 1 h, and 36.0 ± 43.5 µM at 3 h. The mean COR level in both groups was higher than 100 µM at 1 h, and higher than 1 µM at 3 h (shown in Fig. 2).


Small bowel tissue concentration of rebamipide: study of two dosages in healthy subjects.

Akamatsu T, Nagaya T, Ichikawa S, Sudo T, Takeda R, Takenaka K, Kodama R, Ito T, Arakura N, Tanaka E - J Clin Biochem Nutr (2010)

Gastric mucosa, small intestine and serum concentration of rebamipide at 1 h and 3 h after administration (mean ± SD, n = 6 each). Broken lines show pharmacological actions of rebamipide have been confirmed by in vitro experimental studies to require COR of more than 1 µM to 100 µM.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC2966936&req=5

Figure 2: Gastric mucosa, small intestine and serum concentration of rebamipide at 1 h and 3 h after administration (mean ± SD, n = 6 each). Broken lines show pharmacological actions of rebamipide have been confirmed by in vitro experimental studies to require COR of more than 1 µM to 100 µM.
Mentions: In the 100 mg group, the mean COR level was 146.3 ± 203.1 µM at 1 h after taking rebamipide, and 54.9 ± 47.8 µM at 3 h. In the 200 mg group, the mean COR level was 153.5 ± 183.1 µM at 1 h, and 36.0 ± 43.5 µM at 3 h. The mean COR level in both groups was higher than 100 µM at 1 h, and higher than 1 µM at 3 h (shown in Fig. 2).

Bottom Line: The purpose of this study is to investigate whether the effective concentrations of rebamipide (COR) are present in the small intestine after taking an ordinary clinical dose and double dose of this drug.Mean COR in the stomach was less than 100 µM at 1 h in the 100 mg group; however it was higher than 100 µM in the 200 mg group.In conclusion, the COR level in the jejunum was sufficient to protect for NSAID-induced gastrointestinal complications.

View Article: PubMed Central - PubMed

Affiliation: Endoscopy Center, Nagano Prefectural Hospital Organization, Suzaka Hospital, 1332 Suzaka, Suzaka, Nagano 382-0091, Japan.

ABSTRACT
Non-steroidal anti-inflammatory drug (NSAID)-related small intestinal complications exist, since developed new diagnostic modalities, such as balloon and capsule endoscopies. Some experiments have shown rebamipide to protect from NSAID-induced small intestinal complications. The purpose of this study is to investigate whether the effective concentrations of rebamipide (COR) are present in the small intestine after taking an ordinary clinical dose and double dose of this drug. Twelve healthy male subjects were enrolled. After taking 100 or 200 mg of rebamipide, balloon enteroscopy was performed at 1 and 3 h, and biopsy samples were obtained from the jejunum and the stomach. Venous blood samples were taken simultaneously. Samples were analyzed by high-performance liquid chromatography. The mean COR in the jejunum was higher than 100 µM at 1 h and higher than 10 µM at 3 h in both the 100 and 200 mg groups. Mean COR in the stomach was less than 100 µM at 1 h in the 100 mg group; however it was higher than 100 µM in the 200 mg group. In conclusion, the COR level in the jejunum was sufficient to protect for NSAID-induced gastrointestinal complications.

No MeSH data available.


Related in: MedlinePlus