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KMID : 1146920210510060759
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Journal of Pharmaceutical Investigation
2021 Volume.51 No. 6 p.759 ~ p.766
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Effect of gastric residence time on the oral absorption of rebamipide sustained-release tablets in beagle dogs
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Seok Su-Hyun
Ha Jung-Myung
Kim Tae-Hwan
Kim Gyoung-Won
Kim Byung-Hoo
Lee Dong-Woo
Choi Min-Seok
Lee Sung-Hoon
Kim Ju-Young
Park Eun-Seok
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Abstract
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Purpose: Rebamipide (RBM) is known to have a specific absorption window in the upper GI tract. However, there have been no in vivo studies reporting the regional absorption of RBM, which may lead to misjudgment in formulation development considering the many other physiological factors involved in oral absorption. Therefore, this study aimed to assess the regional absorption of RBM.
Methods: Barium sulfate was incorporated into RBM-sustained release (SR) tablets as a radiopaque marker and the location of RBM-SR tablets was monitored using X-ray imaging after oral administration of RBM-SR tablets in Beagle dogs.
Results: Based on the gastric residence time (GRT) of RBM-SR tablets, dogs were divided into two groups: GRTlow for 0.25 and 1.5 h and GRThigh for 3 and 5 h. GRThigh had significantly delayed time to reach peak plasma concentration (Tmax), longer mean residence time (MRT), and higher area under the plasma concentration?time curve from time zero to the last observation time point (AUClast) than GRTlow, which indicates the presence of an absorption window in the upper GI tract.
Conclusion: This study, for the first time, reports on the regional absorption of RBM. The findings of this study may be useful for developing RBM-SR formulations.
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KEYWORD
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Rebamipide, Sustained-release tablets, Gastric residence time, Pharmacokinetics, Regional absorption
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