A preliminary pharmacokinetic study of the enantiomers of the terfenadine acid metabolite in humans.
A stereoselective and sensitive achiral/chiral method for the determination of terfenadine acid metabolite in human plasma was developed. The metabolite was separated and quantitated using an achiral chromatographic procedure with a cyano column. The mobile phase was 1 mM sodium acetate buffer (pH 4.0) and acetonitrile (25:75% v/v) at a flow rate of 2 ml/min, at ambient temperature. The stereospecific resolution was accomplished using a chiral-AGP column and a mobile phase consisting of sodium acetate (0.01 M): methanol (98.7:1.3% v/v), and 20 mM di-n-butylamine at a flow rate of 1.2 ml/min. The column temperature was maintained at 32 degrees C. The eluent was monitored at 230 nm (excitation) and 300 nm (emission) with a cut-off filter at 270 nm. This assay was used for a pharmacokinetic study in five subjects after administration of a single dose of 60 mg of terfenadine. The t1/2 values of the two enantiomers were similar, but the AUC values of the (+)-enantiomer were 2.05-2.35 times higher than those of (-)-enantiomer.
Surapaneni
S
S
Department of Pharmaceutical Sciences, North Dakota State University, Fargo 58105.
Khalil
S K
SK
D000284:Administration, Oral; D000328:Adult; D002845:Chromatography / Q000379:methods*; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D008297:Male; D010880:Piperidines / Q000097:blood; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D016593:Terfenadine / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*
D010880:Piperidines; C100095:azacyclonol; D016593:Terfenadine