title: Enantioselective and highly sensitive determination of carvedilol in human plasma and whole blood after administration of the racemate using normal-phase high-performance liquid chromatography.
abstract: A highly sensitive HPLC method for enantioselective determination of carvedilol in human whole blood and plasma was developed. Carvedilol and S-carazolol as an internal standard extracted from whole blood or plasma were separated using an enantioselective separation column (Chiralpak AD column; 2.0 diameter x 250 mm) without any chiral derivatizations. The mobile phase was hexane:isopropanol:diethylamine (78:22:1, v/v). The excitation and emission wavelengths were set at 284 and 343 nm, respectively. The limits of quantification for the S(-)- and R(+)-carvedilol enantiomers in plasma and blood were both 0.5 ng/ml. Intra- and inter-day variations were less than 5.9%. As an application of the assay, concentrations of carvedilol enantiomer in plasma and blood samples from 15 patients treated with carvedilol for congestive heart failure were determined.
authors.affiliation: Department of Biopharmaceutics, Meiji Pharmaceutical University, 2-522-1 Noshio, Kiyose, Tokyo 204-8588, Japan.
authors.forename: Masako
authors.initials: M
authors.lastname: Saito
authors.forename: Junichi
authors.initials: J
authors.lastname: Kawana
authors.forename: Tetsuro
authors.initials: T
authors.lastname: Ohno
authors.forename: Masahiro
authors.initials: M
authors.lastname: Kaneko
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Mihara
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Hanada
authors.forename: Risa
authors.initials: R
authors.lastname: Sugita
authors.forename: Natsuki
authors.initials: N
authors.lastname: Okada
authors.forename: Sachiko
authors.initials: S
authors.lastname: Oosato
authors.forename: Masatoshi
authors.initials: M
authors.lastname: Nagayama
authors.forename: Tetsuya
authors.initials: T
authors.lastname: Sumiyoshi
authors.forename: Hiroyasu
authors.initials: H
authors.lastname: Ogata
mesh_terms: D000317:Adrenergic alpha-Antagonists / Q000097:blood*; D000319:Adrenergic beta-Antagonists / Q000097:blood*; D002138:Calibration; D002227:Carbazoles / Q000097:blood*; D000077261:Carvedilol; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D006333:Heart Failure / Q000097:blood; D006801:Humans; D011412:Propanolamines / Q000097:blood*; D012680:Sensitivity and Specificity; D013237:Stereoisomerism
chemical_list: D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists; D002227:Carbazoles; D011412:Propanolamines; D000077261:Carvedilol