关键词: 硫辛酸, 药代动力学, LC-MS/MS, 药物蓄积

Abstract:

This study aimedto evaluate the pharmacokinetics for lipoic acid (LA) after oral administration of 12 healthy Chinese volunteers with single and multiple-dose of lipoic acid dispersal tablets using a liquid chromatography-temdend mass spectrometry (LC-MS/MS) methods. In single-dose study, healthy Chinese male and female volunteers received three dose levels at 0.2, 0.3, and 0.4 g of LA dispersal tablets with a 3×3 Latina square design. In multiple-dose study, 12 healthy Chinese volunteers received orally a 0.1 g of LA dispersible tablet three times daily for 6 consecutive days and 0.3 g once on day 7. The results showed that pharmacokinetics of LA fitted a two-compartment open model. The values of area under the curve (AUC) increased proportionally within the range of 0.2–0.4 g, while the Vd/F, CL/F, MRT, t_1/2 and t_max of LA were similar at three dose levels. The steady-state pharmacokinetic parameters of LA were similar to those following a single dose and no accumulation was found following multiple-dose of LA dispersal tablets.

Key words: Lipoic acid, Pharmacokinetics, LC-MS/MS, Drug accumulation