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Stereoselective analysis of carvedilol in human plasma and urine using HPLC after chiral derivatization
Author(s) -
Peccinini Rosângela G.,
Ximenes Valdecir F.,
Cesarino Evandro J.,
Lanchote Vera L.
Publication year - 2008
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.613
Subject(s) - derivatization , carvedilol , stereoselectivity , human plasma , chromatography , high performance liquid chromatography , urine , chemistry , pharmacokinetics , pharmacology , medicine , organic chemistry , biochemistry , heart failure , catalysis
Abstract An enantioselective high‐performance liquid chromatographic method for the analysis of carvedilol in plasma and urine was developed and validated using (‐)‐menthyl chloroformate (MCF) as a derivatizing reagent. Chloroform was used for extraction, and analysis was performed by HPLC on a C18 column with a fluorescence detector. The quantitation limit was 0.25 ng/ml for S(−)‐carvedilol in plasma and 0.5 ng/ml for R(+)‐carvedilol in plasma and for both enantiomers in urine. The method was applied to the study of enantioselectivity in the pharmacokinetics of carvedilol administered in a multiple dose regimen (25 mg/12 h) to a hypertensive elderly female patient. The data obtained demonstrated highest plasma levels for the R(+)‐carvedilol ( AUC SS 0–1275.64 vs 37.29 ng/ml). The enantiomeric ratio R(+)/S(−) was 2.03 for plasma and 1.49 for urine ( Ae 0–12 17.4 vs 11.7 µg). Copyright © 2008 John Wiley & Sons, Ltd.