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Hydrophilic Interaction Liquid Chromatography Tandem Mass Spectrometry: An Attractive and Prospective Method for Quantitative Bioanalysis in Drug Metabolism

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Background: During the development, dosage optimization and safety evaluation of a drug, rapid and precise monitoring of an administered drug and/or its metabolites in biological samples. As drug biotransformation produces more hydrophilic metabolites for the enhancement of drug elimination, it often presents a challenge for traditional reversed-phase liquid chromatography (RPLC) separation. Because hydrophilic interaction liquid chromatography (HILIC) is capable of retaining polar compounds and is readily compatible with mass spectrometry (MS), HILIC has been used as a complementary separation technique to RPLC for the analysis of polar metabolites, especially polar drugs and their metabolites.

Methods: We undertook a comprehensive search of databases for HILIC-related research literature. The characteristics including method, result and innovation of screened papers were described, and an inductive and analytical method was applied to analyze those studies using a reasonable framework.

Results: This paper covers core aspects of the HILIC-MS/MS method and the overall profile of its application in drug and/or its metabolites analysis by reviewing 102 papers. The emphasis of this paper has been placed on the applications of the HILIC-MS/MS method in quantitative bioanalysis of drugs alone or along with their metabolites in drug metabolism studies in recent years. As a fundamental and critical step of the bioanalytical method, conventional sample preparation techniques of biological matrices for the HILIC-MS/MS analysis of drugs and/or their metabolites are also briefly featured.

Conclusion: The findings of this review confirm the powder of HILIC-MS/MS methods in the separation and quantification of drugs and/or their metabolites.
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Keywords: HILIC-MS/MS; drug metabolism; metabolites; pharmacokinetic study; quantitative bioanalysis; sample preparation

Document Type: Research Article

Publication date: May 1, 2016

More about this publication?
  • Current Drug Metabolism aims to cover all the latest and outstanding developments in drug metabolism and disposition. The journal serves as an international forum for the publication of timely reviews in drug metabolism. Current Drug Metabolism is an essential journal for academic, clinical, government and pharmaceutical scientists who wish to be kept informed and up-to-date with the latest and most important developments. The journal covers the following areas:

    In vitro systems including CYP-450; enzyme induction and inhibition; drug-drug interactions and enzyme kinetics; pharmacokinetics, toxicokinetics, species scaling and extrapolations; P-glycoprotein and transport carriers; target organ toxicity and interindividual variability; drug metabolism and disposition studies; extrahepatic metabolism; phase I and phase II metabolism; recent developments for the identification of drug metabolites and adducts.
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