Drugs In Solid Forms Research Articles

Comparative Characteristics of Dosage Forms of α-Lipoic Acid

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.

X-ray diffraction as a tool in the path from the design of an active pharmaceutical ingredient to the tablet on the shelf

Accurate knowledge of molecular structure is a prerequisite for rational drug design. X-ray diffraction has a paramount importance in providing the required structural information: the structural determination by X-ray diffraction of new drug candidates and intermediates can provide valuable information of new syntheses and parameters for quantitative structure–activity relationships. Macromolecular X-ray crystallography is an important and powerful technique used in the discovery of new medicines. The detailed analysis of crystal structures of protein–ligand complexes allows the study of the specific interactions of a particular drug with its protein target at the atomic level. Most marketed pharmaceuticals consist of molecular crystals. The arrangement of the molecules in a crystal determines its physical properties and greatly influences the processing and formulation of solid pharmaceuticals, as well as key drug properties such as dissolution rate and stability. X-ray diffraction is the main tool to characterize the drugs in solid forms. An example of the use of X-ray diffraction in the development of rifamycins is discussed.