A rapid LC-ESI-MS/MS method for the quantitation of choline, an active metabolite of citicoline: Application to in vivo pharmacokinetic and bioequivalence study in Indian healthy male volunteers

J Pharm Biomed Anal. 2012 Dec;71:144-7. doi: 10.1016/j.jpba.2012.07.003. Epub 2012 Jul 31.


A rapid, simple, and sensitive high performance liquid chromatography-tandem mass spectrometry method (LC-ESI-MS/MS) was developed and validated for the determination and pharmacokinetic investigation of choline (CL), active metabolite of citicoline in human plasma using metformin (MF) as IS. The chromatographic separation was performed on a reversed-phase Phenomenx Gemini C18 column with a mobile phase of methanol:water (containing 10mM ammonium formate) (9:1, v/v). The calibration curves were linear over the range of 0.05-5μg/ml. The validated LC-ESI-MS/MS method was successfully applied for the evaluation of pharmacokinetic parameters and bioequivalence study of test and reference control release (CR) tablet preparation of citicoline 1000mg after a single oral administration to all 12 healthy male volunteers.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Adult
  • Choline / blood*
  • Choline / chemistry
  • Choline / pharmacokinetics
  • Chromatography, High Pressure Liquid / methods*
  • Cross-Over Studies
  • Cytidine Diphosphate Choline / blood*
  • Cytidine Diphosphate Choline / chemistry
  • Cytidine Diphosphate Choline / pharmacokinetics
  • Delayed-Action Preparations / chemistry
  • Humans
  • Male
  • Reproducibility of Results
  • Spectrometry, Mass, Electrospray Ionization / methods
  • Tablets / chemistry
  • Tandem Mass Spectrometry / methods*
  • Therapeutic Equivalency


  • Delayed-Action Preparations
  • Tablets
  • Cytidine Diphosphate Choline
  • Choline