Comparative crossover, randomized, open-label bioequivalence study on the bioequivalence of two formulations of thioctic acid in healthy volunteers.
An open-label, randomized, crossover single-dose study, using two periods and two sequences with a washout period of seven days was conducted to assess the comparative bioavailability of thioctic (alpha-lipoic) acid (ALA) 600 mg formulation and that of a reference formulation. Blood samples were collected up to +6 h post dosing, the plasma was separated, and thioctic acid concentrations were determined by high-performance liquid chromatographic method with single mass spectrometry detection (HPLC-MS) and a lower limit of quantification of 190.1 ng/ml. Mean values of the individual C(max) were 1338.6 +/- 751.8 ng/ml and 1215.8 +/- 560.5 ng/ml for the test and reference preparations, respectively. Mean +/- standard deviation (SD) total area under the curve up to the last measurable concentration (AUC(t)) was 3510.9 +/- 1088.6 ng x h/ml for the test formulation and 3563.5 +/- 1374.1 ng x h/ml for the reference formulation. Mean +/- SD total area under the curve (AUC(inf)) was 6925.6 +/- 4045.8 ng x h/ml for the test formulation and 7797.1 +/- 5963.1 ng x h/ml for the reference preparation. Terminal elimination half-life was 5.68 +/- 5.05 h for the test and 6.11 +/- 6.15 h for the reference formulations. Time of maximum concentration (t(max)) was 1.24 +/- 1.23 h for the test and 2.05 +/- 1.21 h for the reference formulations. Ninety percent confidence intervals were comprised within the bioequivalence acceptance criteria (80-125%) for all of the parameters analyzed except t(max). The comparison between males and females showed no significant difference for the two drug treatment.
Mignini
Fiorenzo
F
Centro di Ricerche Cliniche, Dipartimento di Medicina Sperimentale e Sanità Pubblica, Università di Camerino, Camerino, Italy.
Streccioni
Valentino
V
Tomassoni
Daniele
D
Traini
Enea
E
Amenta
Francesco
F
D000293:Adolescent; D000328:Adult; D019540:Area Under Curve; D001682:Biological Availability; D018592:Cross-Over Studies; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D013810:Therapeutic Equivalency; D008063:Thioctic Acid / Q000097:blood / Q000493:pharmacokinetics*
D008063:Thioctic Acid