STEREOSELECTIVE DISTRIBUTION OF ACENOCOUMAROL ENANTIOMERS IN HUMAN PLASMA - CHIRAL CHROMATOGRAPHIC ANALYSIS OF THE ULTRAFILTRATES

Stereoselectivities for the binding of rac-acenocoumarol to human serum albumin (HSA), alpha1-acid glycoprotein (AGP), and human plasma were determined by chiral HPLC analysis of the ultrafiltrates on a Chiral-AGP column. The results confirmed the previously detected inverse stereoselectivities; for HSA the ratio of the enantiomeric constants was K(R)/K(S) approximately 2, while for AGP it was K(R)/K(S) approximately 0.3. In plasma the contribution of HSA dominates, although in pathological states, elevated AGP levels may compensate for stereoselective distribution. (C) 1993 Wiley-Liss, Inc.