Enantioselective pharmacokinetics of lercanidipine in healthy volunteers.
OBJECTIVE
The enantioselective 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.


METHODS
Serial plasma samples were obtained from 0 to 24 h after drug administration. Lercanidipine enantiomers were analysed using a chiral LC-MS-MS method.


RESULTS
The following differences (p < 0.05, Wilcoxon test) between (S) and (R) enantiomers were found (median): C(max) 2.071 ng mL(-1) versus 1.681 ng mL(-1); AUC(0-24)12.352 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 AUC(0-infinity) values for (S)-LER were 1.21-fold higher than those for (R)-LER.


CONCLUSIONS
The pharmacokinetics of LER was enantioselective in healthy volunteers following a single dose of 20 mg of the unlabeled racemic drug.
Jabor
Valquiria Aparecida Polisel
VA
Departamento de Análises Clínicas, Toxicológicas e Bromatológicas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brazil.
Coelho
Eduardo Barbosa
EB
Lanchote
Vera Lucia
VL
D019540:Area Under Curve; D002121:Calcium Channel Blockers / Q000493:pharmacokinetics*; D004095:Dihydropyridines / Q000493:pharmacokinetics*; D006801:Humans
D002121:Calcium Channel Blockers; D004095:Dihydropyridines; C060343:lercanidipine