Development and validation of a sensitive UHPLC-MS/MS method for quantitation of prucalopride in rat plasma and its application to pharmacokinetics study

J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Oct 15:1033-1034:328-333. doi: 10.1016/j.jchromb.2016.09.006. Epub 2016 Sep 5.

Abstract

A rapid, sensitive, selective and accurate ultra high performance liquid chromatography with tandem mass spectrometry (UHPLC-MS/MS) method was developed and validated for the quantitation of prucalopride in rat plasma using carbamazepine as an internal standard (IS). Separation was achieved on a Waters ACQUITY UHPLC(®) HSS C18 column (2.1mm×50mm, 1.8μm) column with a gradient mobile phase consisting of acetonitrile-water (containing 0.1% formic acid) as mobile phase at a flow rate of 0.2mL/min. Prucalopride and IS were monitored using positive electrospray triple quadrupole mass spectrometer (Waters Xevo TQD) via multiple reaction monitoring (MRM) mode. The monitored transitions were set at m/z 367.99→195.89 and m/z 236.97→194.04 for prucalopride and IS, respectively. The achieved lower limit of quantitation was 0.1ng/mL. The validated method had an excellent linearity in the range of 0.1-100ng/mL (r>0.996). The intra- and inter-day precisions were both≤7.8% for prucalopride and IS, and the average intra- and inter-day accuracies ranged from -3.0% to 8.5%. Extraction recoveries at three levels QC concentrations were in the range of 90.0-110.0% for prucalopride and 99.6% for IS. Matrix effects were found to be acceptable. The validated assay was successfully applied to a pharmacokinetic study of prucalopride following oral administration of 0.25, 0.5, 1.0mg/kg to female and male rats respectively.

Keywords: Pharmacokinetics; Prucalopride; Rat plasma; UHPLC–MS/MS.

Publication types

  • Validation Study

MeSH terms

  • Administration, Oral
  • Animals
  • Benzofurans / administration & dosage
  • Benzofurans / blood*
  • Benzofurans / chemistry
  • Benzofurans / pharmacokinetics*
  • Calibration
  • Chromatography, High Pressure Liquid / methods*
  • Drug Stability
  • Female
  • Male
  • Rats, Sprague-Dawley
  • Reference Standards
  • Reproducibility of Results
  • Tandem Mass Spectrometry / methods*
  • Time Factors

Substances

  • Benzofurans
  • prucalopride