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  1. 学術雑誌論文
  2. 各雑誌掲載論文

Simple LC-MS/MS Methods for the Quantitation of Total and Free Aprepitant and its Active N-Dealkylated Metabolites in Human Plasma

http://hdl.handle.net/10271/00003895
http://hdl.handle.net/10271/00003895
3718dc41-47e9-400d-bfa2-1919eb9e8d28
名前 / ファイル ライセンス アクション
Ther Ther Drug Monit-43-422.pdf (1.5 MB)
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Item type 学術雑誌論文 / Journal Article(1)
公開日 2021-09-22
タイトル
タイトル Simple LC-MS/MS Methods for the Quantitation of Total and Free Aprepitant and its Active N-Dealkylated Metabolites in Human Plasma
言語 en
言語
言語 eng
キーワード
主題 aprepitant
キーワード
主題 LC-MS/MS
キーワード
主題 metabolite
キーワード
主題 human plasma
キーワード
主題 free fraction
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
その他のタイトル
その他のタイトル Quantitation of plasma free aprepitant and its metabolite
著者 Naito, Takafumi

× Naito, Takafumi

Naito, Takafumi

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Suzuki, Yusuke

× Suzuki, Yusuke

Suzuki, Yusuke

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Shibata, Kaito

× Shibata, Kaito

Shibata, Kaito

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Kawakami, Junichi

× Kawakami, Junichi

Kawakami, Junichi

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書誌情報 Therapeutic Drug Monitoring

巻 43, 号 3, p. 422-428, 発行日 2021-06
出版者
出版者 Wolters Kluwer Health
権利
権利情報 Copyright 2021 Wolters Kluwer Health.
権利
権利情報 """This is a non-final version of an article published in final form in """"Therapeutic Drug Monitoring"""", 43(3): p422-428."""
抄録
内容記述タイプ Abstract
内容記述 Background: Aprepitant, an antiemetic selective neurokinin-1 receptor antagonist, is primarily metabolized to active N-dealkylated form (ND-AP) and then converted to its carbonyl form (ND-CAP) in humans. This study developed simple liquid chromatography-tandem mass spectrometry methods using electrospray ionization (ESI) for the quantitation of plasma total and free aprepitant and its N-dealkylated metabolites and applied it to patient plasma.
Methods: Free aprepitant and ND-AP in plasma were fractionated by centrifugal ultrafiltration. The analytes in plasma or its ultrafiltrated specimen treated by triethylamine/acetonitrile were isocratically separated on a 3-μm octadecylsilyl column with a total run time of 10 minutes and scanned with positive ion ESI.
Results: The calibration curves of total aprepitant, ND-AP, and ND-CAP ranged from 50?2500, 20?1000, and 5?250 ng/mL, respectively, while that of free aprepitant and ND-AP ranged from 2?150 ng/mL. Their intra- and inter-assay accuracy and imprecision values were 93.5 107.7% and 94.6?103.3%, and 2.1?7.5% and 1.0?8.9%, respectively. Aprepitant and its metabolites did not exhibit any matrix effects or instabilities in plasma specimens. In cancer patients receiving oral aprepitant, the plasma concentration ranges of total aprepitant, ND-AP, and ND-CAP, and of free aprepitant and ND-AP were 137?2170, 104?928, 22.4?97.6, 8.11?60.0, and 3.53?56.0 ng/mL, respectively. The median plasma free fraction rates of aprepitant and ND-AP were 4.14% and 4.90%, respectively.
Conclusions: The present methods with acceptable analytical performance can be used to evaluate total and free aprepitant and its N-dealkylated metabolites in patient plasma.
注記
内容記述 雑誌掲載タイトル:Simple Liquid Chromatography?Tandem Mass Spectrometry Method for Quantitation of Total and Free Aprepitant and Its Active N-Dealkylated Metabolites in Human Plasma
ISSN
収録物識別子タイプ ISSN
収録物識別子 0163-4356
EISSN
収録物識別子タイプ ISSN
収録物識別子 1536-3694
PubMed番号
関連タイプ isVersionOf
識別子タイプ PMID
関連識別子 32960546
出版社DOI
関連タイプ isVersionOf
識別子タイプ DOI
関連識別子 10.1097/FTD.0000000000000815
著者版フラグ
出版タイプ AM
出版タイプResource http://purl.org/coar/version/c_ab4af688f83e57aa
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