Stereoselective analysis of carvedilol in human plasma and urine using HPLC after chiral derivatization

✍ Scribed by Rosângela G. Peccinini; Valdecir F. Ximenes; Evandro J. Cesarino; Vera L. Lanchote

• Publisher: John Wiley and Sons
• Year: 2008
• Tongue: English
• Weight: 112 KB
• Volume: 29
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/bdd.613

✦ Synopsis

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 75.64 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.