Enantiomeric analysis of terfenadine in rat plasma by HPLC.
Enantiomeric pairs of the antihistaminic drug terfenadine and its carboxylic acid derivative were directly separated by HPLC using an ovomucoid protein column. Absolute configurations of terfenadine enantiomers were assigned by comparing their circular dichroism spectra with those of 1-phenyl-1-butanol enantiomers of known absolute stereochemistry. Terfenadine and its major carboxylic acid metabolite extracted from blood plasma following an oral administration of a racemic terfenadine to rats were found to be enriched in the (S)- and (R)-enantiomers, respectively. The results indicated that the (R)-enantiomer of an orally administered racemic terfenadine was preferentially oxidized in rats to form a carboxylic acid metabolite enriched in the (R)-enantiomer.
Zamani
K
K
Division of Clinical Pharmacology, Uniformed Service, University of the Health Sciences, Bethesda, Maryland 20814-4799.
Conner
D P
DP
Weems
H B
HB
Yang
S K
SK
Cantilena
L R
LR
D000818:Animals; D002851:Chromatography, High Pressure Liquid; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013237:Stereoisomerism; D016593:Terfenadine / Q000097:blood*
D016593:Terfenadine