Jabor Valquiria Aparecida Polisel, Coelho Eduardo Barbosa, Lanchote Vera Lucia
Departamento de Análises Clínicas, Toxicológicas e Bromatológicas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brazil.
J Chromatogr B Analyt Technol Biomed Life Sci. 2004 Dec 25;813(1-2):343-6. doi: 10.1016/j.jchromb.2004.09.038.
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.
Serial plasma samples were obtained from 0 to 24 h after drug administration. Lercanidipine enantiomers were analysed using a chiral LC-MS-MS method.
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.
The pharmacokinetics of LER was enantioselective in healthy volunteers following a single dose of 20 mg of the unlabeled racemic drug.
在6名健康男性志愿者单次口服20 mg消旋乐卡地平后，研究第三代二氢吡啶类钙拮抗剂乐卡地平的对映体选择性动力学处置。
给药后0至24小时采集系列血浆样本。采用手性液相色谱-质谱联用方法分析乐卡地平对映体。
（S）和（R）对映体之间存在以下差异（p < 0.05，Wilcoxon检验）（中位数）：C(max) 2.071 ng mL(-1) 对1.681 ng mL(-1)；AUC(0-24) 12.352 ng h mL(-1) 对10.063 ng h mL(-1)，以及Cl/f 732.16 L h(-1) 对1891.84 L h(-1)。（S）-乐卡地平的AUC(0-∞)值比（R）-乐卡地平高1.21倍。
单次给予20 mg未标记消旋药物后，乐卡地平在健康志愿者中的药代动力学具有对映体选择性。
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