Optimization of the composition of solid dispersion of quercetin

Abstract

Increasing the solubility of drugs is one of the most important problems in pharmacy, because most manufactured pharmaceutical substances are sparingly soluble. Typically, such compounds represent Classes II and IV in the biopharmaceutical classification system, which is based on the classification of pharmaceutical substances by solubility and permeability. For poorly soluble substances, the limiting step of the absorption process is usually the degree and dissolution rate, so in the pharmaceutical development, much attention is paid to their improvement. To solve this problem, the technology of solid dispersions creation is used. The aim of the work was to optimize the composition of quercetin solid dispersion, whose therapeutic use is limited due to its degree of solubility in an aqueous medium. Objects of the study were samples of solid dispersions of quercetin with different carriers: polyethyleneoxide-6000, β-cyclodextrin and polyvinylpyrrolidone obtained in a ratio of 1:1 and 1:2 by liquid phase method, with and without the addition of a solvent. As a solvent, ethanol was used. To determine the optimal composition of solid dispersions, a mathematical planning method using the MathCad package and Excel software was used. In the work, a dispersion analysis was performed upon the results of the experimental studies. The ranked series of advantages of the carrier and solvent influence on solubility of solid dispersions samples are shown. To determine the amount of carrier in the solid dispersion, the theory of multi-vector optimization was applied. According to the results of the conducted studies, the optimal value of quercetin and PEO-6000 ratio is 1:2. The obtained results can be used in the development of the composition and technology of solid dispersions of active pharmaceutical ingredients insoluble in the aqueous medium.