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Influence of gastrointestinal activity on the absorption of nilotinib

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Title: Influence of gastrointestinal activity on the absorption of nilotinib
Authors: Sasaki, Maaya Browse this author
Aoyama, Tsuyoshi Browse this author
Sugawara, Mitsuru Browse this author →KAKEN DB
Takekuma, Yoh Browse this author →KAKEN DB
Keywords: Tyrosine kinase inhibitor (TKI)
Nilotinib
Peristalsis movements
Gastric empty rate (GER)
Bile
Issue Date: Feb-2020
Publisher: Japanese Society for the Study of Xenobiotics
Journal Title: Drug metabolism and pharmacokinetics
Volume: 35
Issue: 1
Start Page: 102
End Page: 110
Publisher DOI: 10.1016/j.dmpk.2019.08.006
Abstract: Nilotinib has bioavailability (BA) of only about 25% or less. The purpose of this study was to evaluate the influence of gastrointestinal activity on the absorption of nilotinib. In order to change gastrointestinal activity, mosapride was used for enhancement and butylscopolamine was used for suppression. Experiments on oral administration of nilotinib using rats whose gastrointestinal activity was altered by mosapride or butylscopolamine were carried out. The results of oral administration of acetaminophen to rats with peristalsis movement changed showed that the effects of peristalsis and gastric emptying rate (GER) on drug absorption could be evaluated in this experimental system. Similarly, even with nilotinib, no change in T-max was observed, but C-max increased and decreased significantly. Due to the change in gastrointestinal activity, C-max of nilotinib changed greatly. This showed that gastrointestinal activity affected the emulsifying action of bile and that the absorbability changed. As a result of examining the contribution to the emulsifying action, it was found that when the bile does not exist in the gastrointestinal tract, absorption of nilotinib did not change even when gastrointestinal motility was enhanced. Therefore, the results suggested that gastrointestinal activity influenced the emulsifying action of bile and the absorption of nilotinib was changed. (C) 2019 The Japanese Society for the Study of Xenobiotics. Published by Elsevier Ltd. All rights reserved.
Rights: © 2019. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/
http://creativecommons.org/licenses/by-nc-nd/4.0/
Type: article (author version)
URI: http://hdl.handle.net/2115/80327
Appears in Collections:北海道大学病院 (Hokkaido University Hospital) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 武隈 洋

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