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2016 (v.24 no.3)

Translational and Clinical Pharmacology

Korean Society for Clinical Pharmacology and Therapeutics
ISSN: 2289-0882

  • Comparison of R(+)-α-lipoic acid exposure after R(+)-α-lipoic acid 200 mg and 300 mg and thioctic acid 600 mg in healthy Korean male subjects

    Jangsoo Yoon, Seol Ju Moon, Kwang-Ok Lee, Seo Hyun Yoon, In-Jin Jang, Kyung-Sang Yu, SeungHwan Lee

    TCP | v.24, no.3, pp.137-142, Sep, 2016


    Alpha-lipoic acid, a physiological form of thioctic acid, is a strong antioxidant that relieves diabetic
    neuropathic symptoms. R(+)-α-lipoic acid shows superior antioxidative effects to its racemate. We
    compared the pharmacokinetics (PKs) and tolerability of R(+)- and S(-)-α-lipoic acid after a single
    oral dose of R(+)-α-lipoic acid, Dexid®, and its racemate, thioctic acid in healthy male subjects. We
    used an open-label, randomized, single-dose, three-treatment, parallel study design to compare
    the PK exposure of the active form, R(+)-α-lipoic acid. Thirty subjects completed the study with
    no clinically relevant safety issues. The peak concentrations (Cmax, mean±SD) of R(+)-α-lipoic acid
    after doses of R(+)-α-lipoic acid 200 mg, 300 mg and thioctic acid 600 mg were 4186.8±1956.7,
    6985.6±3775.8 an6498.4±3575.6 μg/L, respectively, and the areas under the plasma concentrationtime 

    curve from 0 to the last measurable concentration (AUClast) were 1893.6±759.4, 3575.2±1149.2
    and 3790.0±1623.0 μg·h-1·L-1, respectively. The geometric mean ratio and 90% confidence intervals
    of R(+)-α-lipoic acid 200 mg to thioctic acid 600 mg for the Cmax and AUClast were 0.71 (0.43-1.15)
    and 0.51 (0.37-0.70), respectively. The corresponding R(+)-α-lipoic acid 300 mg to thioctic acid 600
    mg values were 1.11 (0.68-1.80) and 0.97 (0.71-1.34), respectively. In conclusion, R(+)-α-lipoic acid
    300 mg showed PK characteristics similar to those of thioctic acid 600 mg and both formulations
    were well tolerated.


    pharmacokinetics, racemate, R(+)-α-lipoic acid, thioctic acid, tolerability