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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)
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Submitter: 武隈 洋
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