The impact of the phase state of dihydroquercetin on the pharmacological and technological properties of lozenges

Introduction. Dihydroquercetin (DHQ) has anti-inflammatory and antibacterial activities, which allows this compound to be considered as a promising candidate for designing lozenges in the treatment of the nosological entity sore throat. Objective: to develop the optimal composition of lozenges based on DHQ in terms of its phase state. Material and methods. The investigation object was lozenges based on the amorphous modifications of DHQ. The composition of the tablets was optimized by the following indicators: disintegration, crushing strength, abrasion resistance, and dissolution. Results. The empirically selected optimal weight of the lozenges was 300 mg with a ratio of the components: DHQ, sucrose, crospovidone, calcium stearate, and menthol (7:87:3:1:2) (wt%). There was a statistically significant difference in disintegration time between the lozenges with the above described composition based on crystalline and amorphous formulations (7.1 and 36.4 min, respectively). The dissolution profiles of the tablets based on two DHQ modifications were not equivalent (difference coefficient, 23.0%; similarity factor, 42.8%), while a more prolonged release mode was noted for tablets based on the amorphous formulation of DHQ. Conclusion. The optimal composition of the lozenges comprised the amorphous formulation of DHQ, sucrose, crospovidone, calcium stearate, and menthol in a ratio of 20:265:8:2:5 (mg). The crushing strength, abrasion resistance, and disintegration met the requirements of the State Pharmacy, 14th edition (RF SP-14). The designed lozenges are a promising target for further investigations.

dihydroquercetin (taxifolin), lozenges, phytopreparation, dissolution profile, biopharmacy, sore throat