USE OF POLYMER COMPOSITIONAL MATERIALS TO INCREASE THE BIOAVAILABILITY OF HESPERIDINE

Abstract

Purpose. Investigation of the influence of the composition of polymeric solubilizers on the phase solubilization in water of the model active pharmaceutical ingredient of flavonoid nature hesperidin.
Methods. Hesperidin was chosen as a model substance of characteristic chemical structure. Pharmaceutically acceptable high molecular weight polymers based on polyvinylpyrrolidone (PVP) with a molecular weight of from 2500 to 58000 D were used for research; cetylpyridinium chloride; β-cyclodextrin. Phase solubilization of hesperidin was investigated by the method of Higuchi and Connors. The concentration of hesperidin was determined spectrophotometrically by absorption at 284 nm. The phase solubility diagram was constructed as the dependence of the concentration of hesperidin in solution on the concentration of the polymer. The obtained phase solubility profiles of hesperidin were compared with standard curves. For different compositions at the experiment temperature of 37 ± 0.5 °C, the stability constant and the dissociation constant of intermolecular complexes were calculated.
Scientific novelty. The influence of the composition of polymer solubilizers on the phase solubilization in water of the model API of flavonoid nature of hesperidin was established. Practical significance. The optimal composition of the polymer composite material with hesperidin in the form of a solid dispersed system to maximize the solubility of flavonoids in water is substantiated. Results. The influence of the composition of polymer solubilizers on the phase solubilization in water of the model API of flavonoid nature of hesperidin was investigated. Based on the results of graphical analysis of the obtained data, it was concluded that the solubility of hesperidin increases with increasing number of polymers with different molecular weights and surfactants. The increase in solubility depends on the composition. When adding several polymers or a combination of a polymer with a surfactant, the solubility increases significantly more than when adding one compound. It is shown that the maximum value of solubility increase is observed in the system with polymer C and K surfactant - 42.7 times. It was found that the stability constants of polymeric composite materials of hesperidin based on polyvinylpyrrolidones are in the range from 161.87 to 219.88 M-1, which indicates favorable conditions for the formation of complexes.