Gas--liquid chromatographic resolution and assay of tocainide enantiomers using a chiral capillary column and study of their selective disposition in man

Journal of Chromatography
K M McErlane, G K Pillai

Abstract

Tocainide is a new antiarrhythmic agent that is used clinically as the racemic mixture. In order to study the disposition of the individual enantiomers in man, a gas--liquid chromatographic assay was developed based on the resolution of the R-(-)- and S-(+)-enantiomers as their heptafluorobutyryl derivatives on a capillary column coated with a chiral stationary phase. Two healthy male volunteers ingested an oral solution dose of racemic tocainide hydrochloride at a dose of 3 mg/kg and plasma and urine were collected at intervals for up to 54 h. Analysis of the plasma samples revealed a stereoselective disappearance of the R-(-)-enantiomer, such that the apparent half-life for the S-(+)- and R-(-)-enantiomers were 25.6 and 20.5 h, respectively in one subject and 11.1 and 9.0 h in the second subject. Similar relationships were observed in urine, where the ratio of the S-(+)- to R-(-)-enantiomers varied from 0.98 in 1 h to 3.03 in the 54-h samples in one subject over the same time period.

Citations

Jan 1, 1990·European Journal of Clinical Pharmacology·K M McErlaneG Pillai
May 10, 1985·Journal of Chromatography·M AhnoffJ Vessman
Jan 1, 1984·Journal of Pharmaceutical and Biomedical Analysis·A Hulshoff, H Lingeman
Mar 1, 1986·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·B Testa
May 1, 1986·British Journal of Clinical Pharmacology·O Grech-BelangerM Gilbert
May 3, 1991·Journal of Chromatography·R A CarrF M Pasutto

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