School of Pharmacy and Health Products, University of Camerino, Camerino, Macerata, Italy.
Minerva Med. 2011 Dec;102(6):475-82.
α-Lipoic acid is an important micronutrient with several pharmacological as well as antioxidant properties. The present study was aimed to examine the human bioavailability, pharmacokinetics (PK) and tolerability of an innovative oral formulation (ALA600) containing racemic α-lipoic acid 600 mg.
After a single 600-mg oral administration in healthy volunteers, blood samples were collected up to 8 hours post dosing, and plasma α-lipoic acid concentrations were determined by Liquid Chromatography-Mass Spectrometry (LC-MS) detection.
The PK data revealed a short time to reach plasma peak oncentrations (50.8± 4.2 min) with a C(max) of 6.86±1.29 µg/mL. The C(max) implying that the new pharmaceutical form positively influences absorption and absorption time. The AUC value of 5.65±0.79 µg/mL*h is the more reliable measure of new formulation bioavailability. The half-life and MRT values further show that new formulation is absorbed consistently and rapidly and is eliminated efficiently. These PK data appear to promote further refinement of present formulation. Should the authors compare the obtained data with the recent published data, the new formulation of α-lipoic acid tends to show an improvement of C(max) value (2.5-5.4 times) and AUC (1.8 times).
ALA600 formulation is characterized by rapid absorption, high bioavailability, brief half-life and low toxicity. These PK parameters could significantly increase clinical use of lipoic acid with improvement of the therapeutic effects at the cellular level and might also prove to be the most suitable formulation for chronic administration such as peripheral neuropathies.
α-硫辛酸是一种重要的微量营养素，具有多种药理学和抗氧化特性。本研究旨在检查含有外消旋α-硫辛酸 600mg 的新型口服制剂（ALA600）的人体生物利用度、药代动力学（PK）和耐受性。
在健康志愿者单次口服 600mg 后，采集血样至给药后 8 小时，采用液相色谱-质谱（LC-MS）检测法测定血浆α-硫辛酸浓度。
PK 数据显示，血浆峰浓度（Cmax）达到时间较短（50.8±4.2min），Cmax 为 6.86±1.29μg/mL。Cmax 表明新的药物剂型能积极影响吸收和吸收时间。AUC 值为 5.65±0.79μg/mL*h，是新制剂生物利用度的更可靠指标。半衰期和 MRT 值进一步表明，新制剂的吸收一致且迅速，消除效率高。这些 PK 数据似乎促进了目前制剂的进一步改进。如果作者将获得的数据与最近发表的数据进行比较，新型α-硫辛酸制剂的 Cmax 值（2.5-5.4 倍）和 AUC 值（1.8 倍）呈上升趋势。
ALA600 制剂的特点是吸收迅速、生物利用度高、半衰期短、毒性低。这些 PK 参数可显著提高硫辛酸的临床应用，改善细胞水平的治疗效果，也可能被证明是最适合慢性给药的制剂，如周围神经病变。
