Hepatobiliary excretion and brain distribution of caffeine in rats using microdialysis

Ming Hwang Shyr, Lie Chwen Lin, Chun Hao Chang, Yu Tse Wu, Yen Ju Hsieh, Tung Hu Tsai*

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

4 Scopus citations

Abstract

To investigate the pharmacokinetic mechanism of hepatobiliary excretion and brain distribution of caffeine, this study uses a method based on microdialysis technique and liquid chromatography that allows continuous and concurrent in vivo monitoring of extracellular caffeine in the blood, brain and bile of anesthetized rats following the administration of caffeine (3 or 10 mg/kg, i.v.) through the femoral vein. Dialysates of the blood, brain and bile were directly injected onto the liquid chromatographic system and no further clean-up procedures were required. The study design consisted of two groups of six rats in parallel: the rats of the control group received caffeine (3 or 10 mg/kg, i.v.) alone and those of the cyclosporine treated-group were injected cyclosporine (10 mg/kg, i.v.) 10 min prior to caffeine administration (3 or 10 mg/kg, i.v.). The decline of caffeine in the blood, brain striatum and bile suggested that caffeine had rapid exchange and equilibration between the peripheral compartment and the central nervous system. In addition, the results indicated that caffeine underwent hepatobiliary excretion and was distributed into brain. When cyclosporine was co-administered, the pharmacokinetic parameters were not significantly altered. The results of this study reveal that the pharmacokinetic mechanism of hepatobiliary excretion and brain distribution of caffeine might not relate to P-glycoprotein.

Original languageEnglish
Pages (from-to)265-270
Number of pages6
JournalAnalytica Chimica Acta
Volume566
Issue number2
DOIs
StatePublished - 04 05 2006
Externally publishedYes

Keywords

  • Caffeine
  • Hepatobiliary excretion
  • Microdialysis
  • P-glycoprotein
  • Pharmacokinetics

Fingerprint

Dive into the research topics of 'Hepatobiliary excretion and brain distribution of caffeine in rats using microdialysis'. Together they form a unique fingerprint.

Cite this