Capillary electrophoretic separation of drug enantiomers in human serum

Enantiomers of various solutes including several basic drugs and alpha-amino acids were analyzed by capillary electrophoresis in diluted human serum, and chloroquine and tryptophan were found to be well enantioseparated. In order to specify the protein responsible for enantioseparation, these drug enantiomers were analyzed in the presence of various serum protein fractions. The results indicated that albumin fraction caused enantioseparation but the alpha and beta -globulin mixed fraction, the gamma-globulin fraction and the alpha(1)-acid glycoprotein fraction did not exhibit any enantioseparation. The association constants between these drugs and albumin were roughly estimated based on our method. Approximate values were 1.50 x 10(3) and 1.85 x 10(3) M(-1) for chloroquine enantiomers, and 1.51 x 10(4) and 2.45 x 10(4) M(-1) for tryptophan enantiomers. The difference of the association constant values between the enantiomers was found to be 19% for chloroquine and 38% for tryptophan, when calculated based on the slower moving enantiomers.