Abstract

α-Lipoic acid is a fatty acid, which in its physiological effect is on a par with vitamins and minerals, is a vitamin-like substance (vitamin N). A review of clinical trials of the effectiveness of α-lipoic acid in evidence-based diseases is presented. It is proved that the main indication for the use of α-lipoic acid is diabetes mellitus and complications associated with impaired glucose metabolism, including neuropathy, comprising children and adolescents. In addition, α-lipoic acid can be used for medicinal purposes and for a number of other diseases. α-Lipoic acid is an active substance with “critical bioavailability”: when introduced into the interior, its inter- and intra-individual plasma levels can vary significantly. Therefore, the therapeutic effectiveness of lipoic acid preparations largely depends on its form. A comparative characteristic of solid dosage forms of α-lipoic acid according to pharmacokinetic and clinical indicators is given. It was shown that the pharmacokinetic indices of the solid forms of α-lipoic acid practically do not differ, and the bioavailability of all forms is in the range of 30-60%. The advantages (for manufacturers and consumers / patients) and the disadvantages of α-lipoic acid drugs in solid forms - capsules and tablets are shown. Results proving the best therapeutic effect of α-lipoic acid in micellar form are presented.

Highlights

  • Lipoic acid, thioctic acid (Thioctic acid is the internationally accepted name for the substance), 5- (2,3-dithiacyclopentyl) pentanoic acid, 6,8-dithiocanoic, 1,2-dithiolan-3pentanoic acid is a fatty acid, a natural sulfur-containing compound

  • It is proved that the main indication for the use of α-lipoic acid is diabetes mellitus and complications associated with impaired glucose metabolism, including neuropathy, comprising children and adolescents

  • It was shown that the pharmacokinetic indices of the solid forms of α-lipoic acid practically do not differ, and the bioavailability of all forms is in the range of 30-60%

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Summary

Introduction

Thioctic acid (Thioctic acid is the internationally accepted name for the substance), 5- (2,3-dithiacyclopentyl) pentanoic acid, 6,8-dithiocanoic, 1,2-dithiolan-3pentanoic acid is a fatty acid, a natural sulfur-containing compound. It was first isolated in 1951 in crystalline form from the lipid extract of the liver of cattle L. More than ten methods for its synthesis have been developed [10]. Its synthesis decreases with the age, as well as in chronic diseases, including diabetes mellitus and its complications, for example, diabetic neuropathy [27]

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