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Pharmacokinetics of caffeic acid phenethyl ester and its catechol‐ring fluorinated derivative following intravenous administration to rats
Author(s) -
Wang Xinyu,
Pang Jihai,
Maffucci Jacqueline A.,
Pade Devendra S.,
Newman Robert A.,
Kerwin Sean M.,
Bowman Phillip D.,
Stavchansky Salomon
Publication year - 2009
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.657
Subject(s) - caffeic acid phenethyl ester , pharmacokinetics , volume of distribution , chemistry , cape , caffeic acid , distribution (mathematics) , pharmacology , catechol , derivative (finance) , distribution volume , chromatography , antioxidant , biochemistry , medicine , mathematical analysis , mathematics , archaeology , financial economics , economics , history
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. Copyright © 2009 John Wiley & Sons, Ltd.