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  1. 原著論文

Biological Distribution after Oral Administration of Radioiodine-Labeled Acetaminophen to Estimate Gastrointestinal Absorption Function via OATPs, OATs, and/or MRPs

https://repo.qst.go.jp/records/2000119
https://repo.qst.go.jp/records/2000119
b4592bf6-dcd0-45e9-9ecf-cc6f331965f6
名前 / ファイル ライセンス アクション
7bebeb188d9e6a4698914ed713843191.pdf Biological Distribution after Oral Administration of Radioiodine-Labeled Acetaminophen to Estimate Gastrointestinal Absorption Function via OATPs, OATs, and/or MRPs (641.1 KB)
アイテムタイプ 学術雑誌論文 / Journal Article(1)
公開日 2024-05-02
タイトル
タイトル Biological Distribution after Oral Administration of Radioiodine-Labeled Acetaminophen to Estimate Gastrointestinal Absorption Function via OATPs, OATs, and/or MRPs
言語 en
言語
言語 eng
資源タイプ
資源タイプ識別子 http://purl.org/coar/resource_type/c_6501
資源タイプ journal article
著者 Sato Kakeru

× Sato Kakeru

Sato Kakeru

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Mizutani Asuka

× Mizutani Asuka

Mizutani Asuka

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Yao Jianwei

× Yao Jianwei

Yao Jianwei

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Kobayashi Masato

× Kobayashi Masato

Kobayashi Masato

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Yamazaki Kana

× Yamazaki Kana

Yamazaki Kana

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Nishii Ryuichi

× Nishii Ryuichi

Nishii Ryuichi

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Nishi Kodai

× Nishi Kodai

Nishi Kodai

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Nakanishi Takeo

× Nakanishi Takeo

Nakanishi Takeo

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Tamai Ikumi

× Tamai Ikumi

Tamai Ikumi

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Kawai Keiichi

× Kawai Keiichi

Kawai Keiichi

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抄録
内容記述タイプ Abstract
内容記述 We evaluated the whole-body distribution of orally-administered radioiodine-125 labeled acetaminophen (125I-AP) to estimate gastrointestinal absorption of anionic drugs. 125I-AP was added to human embryonic kidney (HEK)293 and Flp293 cells expressing human organic anion transporting polypeptide (OATP)1B1/3, OATP2B1, organic anion transporter (OAT)1/2/3, or carnitine/organic cation transporter (OCTN)2, with and without bromosulfalein (OATP and multidrug resistance-associated protein (MRP) inhibitor) and probenecid (OAT and MRP inhibitor). The biological distribution in mice was determined by oral administration of 125I-AP with and without bromosulfalein and by intravenous administration of 125I-AP. The uptake of 125I-AP was significantly higher in HEK293/OATP1B1, OATP1B3, OATP2B1, OAT1, and OAT2 cells than that in mock cells. Bromosulfalein and probenecid inhibited OATP- and OAT-mediated uptake, respectively. Moreover, 125I-AP was easily excreted in the urine when administered intravenously. The accumulation of 125I-AP was significantly lower in the blood and urinary bladder of mice receiving oral administration of both 125I-AP and bromosulfalein than those receiving only 125I-AP, but significantly higher in the small intestine due to inhibition of OATPs and/or MRPs. This study indicates that whole-body distribution after oral 125I-AP administration can be used to estimate gastrointestinal absorption in the small intestine via OATPs, OATs, and/or MRPs by measuring radioactivity in the urinary bladder.
言語 en
書誌情報 Pharmaceutics

巻 15, 号 2, p. 497, 発行日 2023-02
出版者
出版者 MDPI
ISSN
収録物識別子タイプ ISSN
収録物識別子 1999-4923
DOI
識別子タイプ DOI
関連識別子 10.3390/pharmaceutics15020497
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