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.
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.
Saito
Masako
M
Department of Biopharmaceutics, Meiji Pharmaceutical University, 2-522-1 Noshio, Kiyose, Tokyo 204-8588, Japan.
Kawana
Junichi
J
Ohno
Tetsuro
T
Kaneko
Masahiro
M
Mihara
Kiyoshi
K
Hanada
Kazuhiko
K
Sugita
Risa
R
Okada
Natsuki
N
Oosato
Sachiko
S
Nagayama
Masatoshi
M
Sumiyoshi
Tetsuya
T
Ogata
Hiroyasu
H
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
D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists; D002227:Carbazoles; D011412:Propanolamines; D000077261:Carvedilol