A highly sensitive LC-MS/MS method for simultaneous determination of glycyrrhizin and its active metabolite glycyrrhetinic acid: Application to a human pharmacokinetic study after oral administration
| Autor: | Hideo Inoue, Tsuneharu Suzuki, Michiko Tsukahara, Yuko Akasaka |
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| Rok vydání: | 2016 |
| Předmět: |
Adult
Male Electrospray ionization Clinical Biochemistry Cmax Administration Oral Tandem mass spectrometry 030226 pharmacology & pharmacy 01 natural sciences Biochemistry Sensitivity and Specificity Analytical Chemistry 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Pharmacokinetics Liquid chromatography–mass spectrometry Tandem Mass Spectrometry Drug Discovery Humans Selected ion monitoring Glycyrrhizin Molecular Biology Active metabolite Pharmacology Chromatography 010401 analytical chemistry Reproducibility of Results General Medicine Glycyrrhizic Acid 0104 chemical sciences chemistry Linear Models Glycyrrhetinic Acid Chromatography Liquid |
| Zdroj: | Biomedical chromatography : BMC. 31(12) |
| ISSN: | 1099-0801 |
| Popis: | A highly sensitive liquid chromatography tandem mass spectrometry (LC-MS/MS) method for simultaneous determination of glycyrrhizin (GL) and its active metabolite, glycyrrhetinic acid (GA) from human plasma was validated and applied to a human pharmacokinetic study. The analytes were extracted from human plasma using an Oasis MAX cartridge and chromatographic separation was performed on an Inertsil ODS-3 column. The detection was performed using an API 4000 mass spectrometer operating in the positive electrospray ionization mode. Selected ion monitoring transitions of m/z 823→453 for GL and m/z 471→149 for GA were obtained. The response was a linear function of concentration over the ranges of 0.5–200 ng/mL for GL and 2–800 ng/mL for GA (both R2 > 0.998). Using this method, pharmacokinetics of GL after single oral administration of a clinical dose (75 mg) to six healthy male Japanese volunteers were evaluated. GL was detected in the plasma of all subjects and the average Cmax was 24.8 ± 12.0 ng/mL. In contrast, Cmax of GA was 200.3 ± 60.3 ng/mL, i.e., ~8-fold higher than that of GL. This is the first report clarifying pharmacokinetic profiles of GL and GA simultaneously at a therapeutic oral dose of a GL preparation. |
| Databáze: | OpenAIRE |
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