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本文引用的文献

1
Single dose bioavailability and pharmacokinetic study of a innovative formulation of α-lipoic acid (ALA600) in healthy volunteers.一种新型 α-硫辛酸(ALA600)制剂在健康志愿者中的单剂量生物利用度和药代动力学研究。
Minerva Med. 2011 Dec;102(6):475-82.
2
Efficacy and safety of antioxidant treatment with α-lipoic acid over 4 years in diabetic polyneuropathy: the NATHAN 1 trial.α-硫辛酸抗氧化治疗糖尿病多发性神经病 4 年的疗效和安全性:NATHAN 1 试验。
Diabetes Care. 2011 Sep;34(9):2054-60. doi: 10.2337/dc11-0503. Epub 2011 Jul 20.
3
(R)-α-Lipoic acid treatment restores ceramide balance in aging rat cardiac mitochondria.(R)-α-硫辛酸处理可恢复衰老大鼠心肌线粒体中的神经酰胺平衡。
Pharmacol Res. 2011 Jan;63(1):23-9. doi: 10.1016/j.phrs.2010.09.007. Epub 2010 Oct 8.
4
Safety of long-term feeding of dl-alpha-lipoic acid and its effect on reduced glutathione:oxidized glutathione ratios in beagles.比格犬长期喂食dl-α-硫辛酸的安全性及其对谷胱甘肽还原型:氧化型谷胱甘肽比例的影响。
Vet Ther. 2002 Summer;3(2):167-76.
5
Pharmacokinetics and drug metabolism in the elderly.老年人的药代动力学与药物代谢
Drug Metab Rev. 2009;41(2):67-76. doi: 10.1080/03602530902722679.
6
Assessment of endoplasmic reticulum glutathione redox status is confounded by extensive ex vivo oxidation.内质网谷胱甘肽氧化还原状态的评估因广泛的体外氧化而混淆。
Antioxid Redox Signal. 2008 May;10(5):963-72. doi: 10.1089/ars.2007.1869.
7
Comparative crossover, randomized, open-label bioequivalence study on the bioequivalence of two formulations of thioctic acid in healthy volunteers.健康志愿者中硫辛酸两种制剂生物等效性的比较交叉、随机、开放标签生物等效性研究。
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8
Protective effects of L-carnitine and alpha-lipoic acid in rats with adjuvant arthritis.左旋肉碱和α-硫辛酸对佐剂性关节炎大鼠的保护作用。
Pharmacol Res. 2007 Oct;56(4):303-10. doi: 10.1016/j.phrs.2007.07.008. Epub 2007 Aug 3.
9
The effects and mechanisms of mitochondrial nutrient alpha-lipoic acid on improving age-associated mitochondrial and cognitive dysfunction: an overview.线粒体营养素α-硫辛酸改善年龄相关线粒体和认知功能障碍的作用及机制:综述
Neurochem Res. 2008 Jan;33(1):194-203. doi: 10.1007/s11064-007-9403-0. Epub 2007 Jun 29.
10
Cilostazol reduces inflammatory burden and oxidative stress in hypertensive type 2 diabetes mellitus patients.西洛他唑可减轻高血压合并2型糖尿病患者的炎症负担和氧化应激。
Pharmacol Res. 2007 Aug;56(2):118-23. doi: 10.1016/j.phrs.2007.04.007. Epub 2007 May 3.

年龄和性别依赖性 R-和 R,S-α-硫辛酸生物利用度:一项初步研究。

Age and gender dependent bioavailability of R- and R,S-α-lipoic acid: a pilot study.

机构信息

Linus Pauling Institute, Oregon State University, Corvallis, OR 97331, USA.

出版信息

Pharmacol Res. 2012 Sep;66(3):199-206. doi: 10.1016/j.phrs.2012.05.002. Epub 2012 May 16.

DOI:10.1016/j.phrs.2012.05.002
PMID:22609537
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4084596/
Abstract

Lipoic acid (LA) shows promise as a beneficial micronutrient toward improving elder health. Studies using old rats show that (R)-α-LA (R-LA) significantly increases low molecular weight antioxidants that otherwise decline with age. Despite this rationale for benefiting human health, little is known about age-associated alterations in absorption characteristics of LA, or whether the commercially available racemic mixture of LA (R,S-LA) is equally as bioavailable as the naturally occurring R-enantiomer. To address these discrepancies, a pilot study was performed to establish which form of LA is most effectively absorbed in older subjects relative to young volunteers. Young adults (average age=32 years) and older adults (average age=79 years) each received 500 mg of either R- or R,S-LA. Blood samples were collected for 3h after supplementation. After a washout period they were given the other chiral form of LA not originally ingested. Results showed that 2 out of 6 elder males exhibited greater maximal plasma LA and area under the curve for the R-form of LA versus the racemic mixture. The elder subjects also demonstrated a reduced time to reach maximal plasma LA concentration following R-LA supplementation than for the racemic mixture. In contrast, young males had a tendency for increased bioavailability of R,S-LA. Overall, bioavailability for either LA isoform was much more variable between older subjects compared to young adults. Plasma glutathione levels were not altered during the sampling period. Thus subject age, and potential for varied response, should be considered when determining an LA supplementation regimen.

摘要

硫辛酸(LA)作为一种有益的微量营养素,有望改善老年人的健康。使用老年大鼠的研究表明,(R)-α-硫辛酸(R-LA)显著增加了随着年龄增长而降低的低分子量抗氧化剂。尽管这一理论是为了有益于人类健康,但对于 LA 的吸收特征随年龄的变化,或者商业上可获得的 LA 外消旋混合物(R,S-LA)是否与天然存在的 R-对映体同样具有生物利用度,知之甚少。为了解决这些差异,进行了一项初步研究,以确定相对于年轻志愿者,哪种形式的 LA 在老年人中吸收效果最好。年轻成年人(平均年龄=32 岁)和老年人(平均年龄=79 岁)每人分别服用 500 毫克 R-或 R,S-LA。补充后 3 小时采集血样。经过洗脱期后,他们服用了最初未摄入的另一种手性 LA。结果表明,6 名老年男性中有 2 名表现出更高的最大血浆 LA 和 R 形式的 LA 曲线下面积相对于外消旋混合物。与外消旋混合物相比,老年受试者在补充 R-LA 后达到最大血浆 LA 浓度的时间也缩短了。相比之下,年轻男性的 R,S-LA 生物利用度有增加的趋势。总体而言,与年轻成年人相比,LA 异构体在老年受试者中的生物利用度差异更大。在采样期间,血浆谷胱甘肽水平没有改变。因此,在确定 LA 补充方案时,应考虑受试者年龄和潜在的不同反应。