A preliminary pharmacokinetic study of the enantiomers of the terfenadine acid metabolite in humans

✍ Scribed by Sekhar Surapaneni; Dr. Shoukry K. W. Khalil

• Publisher: John Wiley and Sons
• Year: 1994
• Tongue: English
• Weight: 415 KB
• Volume: 6
• Category: Article
• ISSN: 0899-0042
• DOI: 10.1002/chir.530060606

✦ Synopsis

A stereoselective and sensitive achirdchiral 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 d m i n , 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 d m i n . The column temperature was maintained at 32°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.