NATURAL POLYMERS AS EXCIPIENTS TO OPTIMIZE THE MYDRIATIC EFFECT OF PHENYLEPHRINE HYDROCHLORIDE

Abstract

A comparative in vivo study examined the main characteristics of the mydriatic effect of eye drops containing the active substance 2.5% phenylephrine hydrochloride with and without auxiliary components, as well as their effect on the ocular mucosa. The research was carried out on 40 mature male rabbits of the Soviet Chinchilla breed. The mydriatic effect of the drug when instilled into the conjunctival sac of an awake rabbit was studied. The local irritant effect of GDF eye drops on the cornea of the eye of an experimental animal was determined. A single instillation of 1 drop of a 2.5% solution of GDF phenylephrine hydrochloride containing hypromellose as an excipient exceeds the depth of the mydriatic effect of the drug without them, and in terms of the speed of achieving the maximum mydriatic effect and its duration, it is ahead of the effect of GLF containing hyaluronic acid. It is also not accompanied by the formation of a local irritant reaction to the cornea of a rabbit's eye, in contrast to a moderate reaction against the background of instillation. The results obtained suggest that the inclusion of hypromellose as an excipient in GDF eye drops with phenylephrine hydrochloride leads to optimization of the pharmacodynamics and pharmacokinetics of the active substance due to acceleration its penetration into the moisture of the anterior chamber of the eye, increasing local bioavailability and prolonging the exposure time of the substance.