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LC-MS/MS quantitation of antimalarial drug piperaquine and metabolites in human plasma

Journal article
Authors Mohd Yusmaidie Aziz
Kurt-Jürgen Hoffmann
Michael Ashton
Published in Journal of chromatography. B
Volume 1063
Pages 253-258
ISSN 1570-0232
Publication year 2017
Published at Institute of Neuroscience and Physiology, Department of Pharmacology
Pages 253-258
Language en
Keywords Piperaquine, Malaria, LC-MS/MS, Pharmacokinetics, Drug metabolism, plasmodium-falciparum malaria, dihydroartemisinin-piperaquine, artemether-lumefantrine, uncomplicated malaria, pharmacokinetics, children, Biochemistry & Molecular Biology, Chemistry
Subject categories Pharmacology, Chemical Sciences, Biochemistry and Molecular Biology


Purpose: This study aimed to develop a sensitive, quantitative assay for the antimalarial piperaquine (PQ) and its metabolites M1 and M2 in human plasma. Results: Analytes were gradiently separated on a C18 column and detected with a Sciex API 4000 MS/MS with an ESI source operated in the positive ion mode with deuterated PQ as internal standard. The response was linear in the range 3.9-2508 nM with a runtime of 7.0 min per sample. The method was applied to clinical samples from healthy volunteers. Conclusion: This LC-MS/MS method for the simultaneous quantitation of PQ and two of its metabolites in plasma may prove helpful for assessment of metabolite safety issues in vivo.

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