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Abstract
Arotinolol and its main metabolite, AC 623, both antihypertensive agents with β blocking properties could be separated simultaneously into their two enantiomers and determined in plasma and urine using a solid phase extraction in presence of an internal standard and HPLC using a chiral counterion (Z-glycyl-L-proline) followed by fluorimetric detection.
Extraction yields are satisfactory and reproducible. Calibration curves in plasma showed good linearity at levels from 75 to 3 75 ng/ml Arotinolol (97 % R (−) and 3 % S (+) and from 5 to 25 ng/ml AC 623 (80 % R (−) and 20% = S(+)).
Absolute amounts of each enantiomer could be calculated from the plasma standard curves, whereas percentages of each enantiomer were estimated from spiked plasma and urine. Both enantiomers of Arotinolol or AC 623 gave similar analytical response. They could be related to total amounts of drugs dosed using non-chiral HPLC (10).
Accuracy was estimated from plasma calibration curves (R. E. < 10 % for Arotinolol enantiomers; < 20%, for AC 623 enantiomers), and spikes (mean R. E. < 7% for Arotinolol enantiomers; < 24% for AC 623 enantiomers).
Precision defined by the coefficient of variation (C. V.%) over several analysis in plasma and urine showed a C. V. inferior to 10% for Arotinolol enantiomers, but reaching sometimes 40% for AC 623 enantiomers.
The poorer accuracy and precision on AC 623 analysis was essentially due to the chromatography of the drug and to the lower levels analysed in comparison with Arotinolol.
The detection limit of the method used for plasma and urine analysis was 2 ng/ml of each enantiomer (R (−) and S (+)) of Arotinolol and AC 623.
This method could succesfully be applied for quantification of Arotinolol and AC 623 enantiomers in plasma and urine.