Pharmacokinetics of gastrodin and its metabolite p-hydroxybenzyl alcohol in rat blood, brain and bile by microdialysis coupled to LC-MS/MS

J Pharm Biomed Anal. 2008 Nov 4;48(3):909-17. doi: 10.1016/j.jpba.2008.07.013. Epub 2008 Jul 29.


Gastrodin is a pharmacologically active substance isolated from Gastrodia elata Blume with sedation, anti-convulsion and anti-epilepsy activities. A rapid and sensitive liquid chromatography technique coupled to tandem mass spectrometry (LC-MS/MS) system was developed to determine gastrodin and its metabolite p-hydroxybenzyl alcohol (HBA) in rat blood, brain and bile collected using microdialysis technique. The analytes were separated using a reversed phase column (4.6 mm x 150 mm, 5 microm). The mobile phase for column separation was 30% methanol with a flow rate of 0.6 mL/min. As a post-column addition, 1% ammonium hydroxide solution (in methanol) was additionally pumped via a T-connection using a chromatographic pump (BAS PM-80, USA) at a flow rate of 0.2 mL/min after the column separation. A LC-MS/MS system equipped with a negative electrospray ionization (ESI) source in multiple reaction monitoring (MRM) mode was used to monitor m/z 285.0-->122.9 and m/z 123.0-->105.0 transitions for gastrodin and HBA, respectively. The lower limit of quantification (LLoQ) for gastrodin and HBA were 0.5 and 2 ng/mL, respectively. The calibration curves were linear over the range of 0.5-5,000 ng/mL and 2-1,000 ng/mL for gastrodin and HBA with a coefficient of determination >0.995, respectively. This selective and sensitive method is useful for the determination of gastrodin and HBA and in the pharmacokinetic studies of these compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzyl Alcohols / blood*
  • Benzyl Alcohols / chemistry
  • Benzyl Alcohols / isolation & purification
  • Benzyl Alcohols / metabolism
  • Benzyl Alcohols / pharmacokinetics*
  • Bile / metabolism*
  • Brain / metabolism*
  • Calibration
  • Chromatography, Liquid / methods*
  • Glucosides / chemistry
  • Glucosides / isolation & purification
  • Glucosides / metabolism
  • Glucosides / pharmacokinetics*
  • Male
  • Microdialysis*
  • Molecular Structure
  • Plant Roots / chemistry
  • Rats
  • Rats, Sprague-Dawley
  • Sensitivity and Specificity
  • Spectrometry, Mass, Electrospray Ionization / methods
  • Tandem Mass Spectrometry / methods*
  • Time Factors


  • Benzyl Alcohols
  • Glucosides
  • 4-hydroxybenzyl alcohol
  • gastrodin