Simultaneous quantification of vortioxetine, carvedilol and its active metabolite 4-hydroxyphenyl carvedilol in rat plasma by UPLC-MS/MS: Application to their pharmacokinetic interaction study

J Pharm Biomed Anal. 2016 Sep 5:128:184-190. doi: 10.1016/j.jpba.2016.05.029. Epub 2016 May 19.

Abstract

To establish a rapid and sensitive ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method for the determination of vortioxetine, carvedilol and its metabolite 4-hydroxyphenyl carvedilol in rat plasma. The analytes and the internal standard (diazepam) were separated on an Acquity UPLC BEH C18 chromatography column (2.1mm×50mm, 1.7μm) using gradient elution with a mobile phase of acetonitrile and 0.1% formic acid in water at a flow rate of 0.4mL/min. The detection was performed on a triple quadrupole tandem mass spectrometer by multiple reaction monitoring (MRM) mode to monitor the precursor-to-product ion transitions of m/z 299.2→150.1 for vortioxetine, m/z 407.2→100.3 for carvedilol, m/z 423.2→100.1 for 4-hydroxyphenyl carvedilol and m/z 285.2→193.1 for diazepam (IS) using a positive electrospray ionization interface. The method was validated over a concentration range of 0.5-100ng/mL for vortioxetine, 0.5-1000ng/mL for carvedilol and 0.1-50ng/mL for 4-hydroxyphenyl carvedilol. Total time for each chromatograph was 3.0min. The intra- and inter-day precision and accuracy of the quality control samples at low, medium, and high concentration levels exhibited relative standard deviations (RSD)<11.6% and the accuracy values ranged from -12.2% to 11.3%. The analytical method was successfully applied to a pharmacokinetic interaction study of vortioxetine and carvedilol after oral administration vortioxetine and carvedilol in rats. Results suggested that the co-administration of vortioxetine and carvedilol results in a significant drug interaction in rats.

Keywords: 4-hydroxyphenyl carvedilol; Carvedilol; Pharmacokinetics; UPLC–MS/MS; Vortioxetine.

MeSH terms

  • Adrenergic beta-Antagonists / blood*
  • Adrenergic beta-Antagonists / pharmacokinetics*
  • Animals
  • Antidepressive Agents / blood*
  • Antidepressive Agents / pharmacokinetics*
  • Calibration
  • Carbazoles / blood*
  • Carbazoles / pharmacokinetics*
  • Carvedilol
  • Chromatography, High Pressure Liquid
  • Diazepam / chemistry
  • Drug Interactions
  • Male
  • Piperazines / blood*
  • Piperazines / pharmacokinetics*
  • Propanolamines / blood*
  • Propanolamines / pharmacokinetics*
  • Quality Control
  • Rats
  • Rats, Sprague-Dawley
  • Reference Standards
  • Reproducibility of Results
  • Spectrometry, Mass, Electrospray Ionization
  • Sulfides / blood*
  • Sulfides / pharmacokinetics*
  • Tandem Mass Spectrometry
  • Vortioxetine

Substances

  • 4-hydroxyphenyl carvedilol
  • Adrenergic beta-Antagonists
  • Antidepressive Agents
  • Carbazoles
  • Piperazines
  • Propanolamines
  • Sulfides
  • Carvedilol
  • Vortioxetine
  • Diazepam