Preparation and investigation of properties of resveratrol and solubilizers compositions

Abstract

Background. The search for technology or the use of excipients for the development of drugs containing poorly soluble pharmaceutical substances is an urgent task of pharmacy. According to the biopharmaceutical classification system, resveratrol belongs to group 4: the substance has low solubility and low permeability. Therefore, one of the priorities in the development of drugs with resveratrol is to increase its solubility and, as a result, increase its permeability. The article presents the results of physicochemical studies of resveratrol compositions with solubilizers (poloxamer 407, polysorbate 80, methyl-beta-cyclodextrin) after dissolution in a common solvent followed by evaporation.Aim. Obtaining compositions of resveratrol with solubilizers and auxiliary formations with an exclusive study of their properties for the development of solid dosage forms.Materials and methods. Trans-resveratrol, poloxamer 407, polysorbate 80, methyl-beta-cyclodextrin, citric and ascorbic acids, glycerin, methanol; high performance liquid chromatography, differential scanning calorimetry.Results. Physical and chemical studies of the obtained compositions of resveratrol with excipients were carried out. Excipients used: citric and ascorbic acids for all compositions, as well as glycerin for compositions with tween 80. Stability studies were carried out under conditions of «accelerated aging», as a result of which a noticeable decrease in the amount of resveratrol was found (80 % of the original). Studies of the stability of resveratrol have shown that at low pH, inherent in the stomach, its content remains practically unchanged for two days. And at pH close to neutral, the content of resveratrol is reduced to 90 % of the original amount. The obtained results indicate the feasibility of developing drugs that promote the absorption of resveratrol in the stomach and are stored at low temperatures (in the refrigerator).Conclusion. Compositions of resveratrol with solubilizers were obtained and the choice of excipients for the development of solid dosage forms was substantiated. Recommendations are given for obtaining solid dosage forms for each of the developed formulations and storage conditions are determined.