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Stereospecific assay of nicoumalone: application to pharmacokinetic studies in man.
Author(s) -
Gill TS,
Hopkins KJ,
Rowland M
Publication year - 1988
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1988.tb03350.x
Subject(s) - enantiomer , bioavailability , pharmacokinetics , stereospecificity , volume of distribution , chemistry , pharmacology , chromatography , stereochemistry , medicine , biochemistry , catalysis
1. A stereospecific h.p.l.c. assay of nicoumalone in plasma has been developed. 2. The assay was applied to a study in which 20 mg racemic nicoumalone was given orally to three volunteers and blood samples taken for 168 h. 3. The mean pharmacokinetic parameters of the individual enantiomers were: clearance/bioavailability 1.28 1 h‐1, R‐ enantiomer; 17.5 1 h‐1, S‐enantiomer: volume of distribution/bioavailability 12.5 1, R‐enantiomer; 22.6 1, S‐ enantiomer: terminal half‐life 6.8 h, R‐enantiomer; 0.91 h, S‐ enantiomer. 4. The data are consistent with a substantial first‐pass hepatic loss of S‐nicoumalone.