Pharmacokinetics of caffeic acid phenethyl ester and its catechol-ring fluorinated derivative following intravenous administration to rats

Xinyu Wang, Jihai Pang, Jacqueline A. Maffucci, Devandra S. Patel, Robert A. Newman, Sean M. Kerwin, Phillip D. Bowman, Salomon Stavchansky

Research output: Contribution to journalArticlepeer-review

Abstract

The pharmacokinetic profiles of caffeic acid phenethyl ester (CAPE) and its catechol-ring fluorinated derivative (FCAPE) were determined in rats after intravenous administration of 5, 10 or 20 mg/kg for CAPE and 20 mg/kg for FCAPE, respectively. The plasma concentrations of CAPE and FCAPE were measured using a validated liquid chromatography tandem mass spectrometric method. The pharmacokinetic parameters were estimated using non compartmental analysis (NCA) and biexponential fit. The results showed that the area under the plasma concentration-time curve for CAPE treatment increased in a proportion greater than the increase in dose from 5 to 20 mg/kg of CAPE. Total body clearance values for CAPE ranged from 42.1 to 172 ml/min/kg (NCA) and decreased with the increasing dose of CAPE. Similarly, the volume of distribution values for CAPE ranged from 1555 to 5209 ml/kg, decreasing with increasing dose. The elimination half-life for CAPE ranged from 21.2 to 26.7 min and was independent of dose. That FCAPE was distributed extensively into rat tissues and eliminated rapidly was indicated by a high value of volume of distribution and similar short elimination half-life as that of CAPE.

Original languageAmerican English
JournalBiopharmaceutics & drug disposition
Volume30
StatePublished - Jan 1 2009

Keywords

  • Animals
  • Area Under Curve
  • Caffeic Acids/administration & dosage/pharmacokinetics
  • Chromatography
  • Dose-Response Relationship
  • Drug
  • Half-Life
  • High Pressure Liquid
  • Injections
  • Intravenous
  • Male
  • Nonlinear Dynamics
  • Phenylethyl Alcohol/administration & dosage/analogs & derivatives/pharmacokinetics
  • Rats
  • Sprague-Dawley

Disciplines

  • Pharmacy and Pharmaceutical Sciences

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