Development and validation of an UPLC-MS/MS method for the simultaneous determination of fexofenadine and olmesartan in human serum: Application to in vivo pharmacokinetic studies

J Pharm Biomed Anal. 2024 Aug 1:245:116179. doi: 10.1016/j.jpba.2024.116179. Epub 2024 Apr 23.

Abstract

A sensitive, reproducible, robust, high-throughput ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated for the simultaneous quantification of fexofenadine and olmesartan in human serum. Samples (50 µL) undergo protein precipitation prior to UPLC-MS/MS analysis. The analytes were separated using an Acquity BEH C18 column (2.1 mm × 50 mm, 1.7 µm) at a flow rate of 0.5 mL/min using a gradient elution with a total run time of 4 min. The analytes were detected in positive ion mode and selected reaction monitoring (SRM) was used for quantitation. The standard curve concentration range was 1.0-500.0 ng/mL for both analytes and each analyte showed excellent linearity with correlation coefficients (R2 > 0.99). The intra- and inter-day accuracy and precision were ±15% for each analyte, and excellent recovery was demonstrated (93-98%) for both analytes. The method is well suited for high-throughput quantitative determination of fexofenadine and olmesartan simultaneously and was successfully applied to an in vivo pharmacokinetic and transporter phenotyping study in humans.

Keywords: Fexofenadine; LC-MS/MS; Mass spectrometry; Olmesartan; Pharmacokinetics.

Publication types

  • Validation Study

MeSH terms

  • Chromatography, High Pressure Liquid / methods
  • Humans
  • Imidazoles* / blood
  • Imidazoles* / pharmacokinetics
  • Liquid Chromatography-Mass Spectrometry
  • Reproducibility of Results
  • Tandem Mass Spectrometry / methods
  • Terfenadine* / analogs & derivatives
  • Terfenadine* / blood
  • Terfenadine* / pharmacokinetics
  • Tetrazoles* / blood
  • Tetrazoles* / pharmacokinetics

Substances

  • fexofenadine
  • Imidazoles
  • olmesartan
  • Terfenadine
  • Tetrazoles