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Minerva Medica 2011 December;102(6):475-82


language: English

Single dose bioavailability and pharmacokinetic study of a innovative formulation of α-lipoic acid (ALA600) in healthy volunteers

Mignini F. 1, Capacchietti M. 1, Napolioni V. 2, Reggiardo G. 1, Fasani R. 1, Ferrari P. 3

1 School of Pharmacy and Health Products, University of Camerino, Camerino, Macerata, Italy; 2 School of Bioscience and Biotechonologies, University of Camerino, Camerino, Macerata, Italy; 3 Scientific Service, Alfa Wassermann, Bologna, Italy


AIM: 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.
METHODS: 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.
RESULTS: The PK data revealed a short time to reach plasma peak oncentrations (50.8± 4.2 min) with a Cmax of 6.86±1.29 µg/mL. The Cmax 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 Cmax value (2.5-5.4 times) and AUC (1.8 times).
CONCLUSIION: 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.

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