Enantioselective pharmacokinetics of lercanidipine in healthy volunteers

Objective: antioselective kinetic disposition of lercanidipine, a dihydropyridine type of third-generation calcium antagonist, was investigated in six healthy male volunteers following a single 20 mg racemic oral dose. s: plasma samples were obtained from 0 to 24 h after drug administration. Lercanidipine enantiomers were analysed using a chiral LC–MS–MS method. s: llowing differences (p < 0.05, Wilcoxon test) between (S) and (R) enantiomers were found (median): Cmax 2.071 ng mL−1 versus 1.681 ng mL−1; AUC0–2412.352 ng h mL−1 versus 10.063 ng h mL−1 and Cl/f 732.16 L h−1 versus 1891.84 L h−1. The AUC0–∞ values for (S)-LER were 1.21-fold higher than those for (R)-LER. sion: armacokinetics of LER was enantioselective in healthy volunteers following a single dose of 20 mg of the unlabeled racemic drug.