Institute for Health Care Science, Suntory Wellness Ltd., 1-1-1 Wakayamadai, Shimamoto-cho, Mishima-gun, Osaka, 618-8503, Japan.
Biopharm Drug Dispos. 2013 Nov;34(8):462-73. doi: 10.1002/bdd.1862. Epub 2013 Oct 17.
A single-blind, placebo-controlled, parallel-group and multiple oral dose study was conducted in 48 healthy subjects to investigate the pharmacokinetics and safety of multiple oral doses of sesame lignans (sesamin and episesamin). Subjects were randomly divided into two groups. Each subject was administered 50 mg of sesame lignans (sesamin/episesamin=1/1) or placebo once daily for 28 days. The pharmacokinetics of the sesame lignans were investigated using 10 of the 24 subjects in the sesame lignans group. No serious adverse events were observed in this study. Sesamin was absorbed with a peak plasma concentration at 5.0 h. The plasma concentration of the main metabolite, SC-1, reached a peak at 5.0 h and decreased rapidly with a terminal half-life of 2.4 h. Episesamin was also absorbed with a peak plasma concentration at 5.0 h and decreased with a terminal half-life of 7.1 h. The plasma concentration of the main metabolite, EC-1, reached a peak at 5.0 h and decreased rapidly with a terminal half-life of 3.4 h. The plasma concentrations of sesamin and episesamin reached a steady state by day 7. Sesame lignans were confirmed to be safe and tolerable in healthy subjects. The results of the pharmacokinetic study demonstrate that no accumulation was observed following multiple 50 mg doses of sesame lignans.
一项在 48 名健康受试者中进行的单次、双盲、安慰剂对照、平行分组和多次口服剂量研究，旨在研究多次口服芝麻木脂素（芝麻素和表芝麻素）的药代动力学和安全性。受试者随机分为两组。每组受试者每日口服 50mg 芝麻木脂素（芝麻素/表芝麻素=1/1）或安慰剂，连续 28 天。采用芝麻木脂素组的 24 名受试者中的 10 名，对芝麻木脂素的药代动力学进行了研究。在这项研究中，没有观察到严重的不良事件。芝麻素在 5.0 小时时达到血浆峰浓度，被吸收。主要代谢物 SC-1 的血浆浓度在 5.0 小时达到峰值，然后迅速下降，半衰期为 2.4 小时。表芝麻素也在 5.0 小时时被吸收，半衰期为 7.1 小时。主要代谢物 EC-1 的血浆浓度在 5.0 小时达到峰值，半衰期为 3.4 小时，然后迅速下降。芝麻素和表芝麻素的血浆浓度在第 7 天达到稳态。芝麻木脂素在健康受试者中被证实是安全和耐受的。药代动力学研究结果表明，多次给予 50mg 芝麻木脂素后没有观察到蓄积。
