OPHTHALMIC PHARMACEUTICAL COMPOSITIONS Russian patent published in 2024 - IPC A61K31/53 A61K47/02 A61K47/10 A61K47/14 A61K47/18 A61K9/08 A61P27/02 

FIELD: pharmaceutics.

SUBSTANCE: group of inventions relates to an ophthalmic pharmaceutical composition and aqueous ophthalmic compositions. An ophthalmic pharmaceutical composition for treating a dry eye disorder contains (a) a compound of Formula I:

or a pharmaceutically acceptable acid addition salt thereof in concentration of 0.005–0.5% weight/volume, in terms of the compound of Formula I, in said composition, (b) water, (c) 1–15% weight/volume of a solubiliser, (d) 0.5–10% weight/volume of a cosolvent, and (e) 0.01–0.6% weight/volume of an antioxidant system. An aqueous ophthalmic composition for treating a dry eye disorder contains: (a) a compound of Formula I in concentration of 0.005–0.5% weight/volume, in terms of the compound of Formula I, in said composition:

(b) water, (c) 1–15% weight/volume of a solubiliser, (d) 0.5–10% weight/volume of a cosolvent, and (e) 0.01–0.6% weight/volume of the antioxidant system, in which the amount of the compound of Formula II:

present in said composition does not increase by more than 200% wt.% or area % when determined by HPLC, when storing said composition in a closed container for at least 6 months, at least 12 months, at least 18 months, at least 24 months, or before the expiration of the commercially acceptable shelf life of the composition. An aqueous ophthalmic composition for treating a dry eye disorder contains: (a) a compound of Formula I in concentration of 0.005-0.5% weight/volume, in terms of the compound of Formula I, in said composition:

(b) water, (c) 1–15% weight/volume of a solubiliser , (d) 0.5–10% weight/volume of cosolvent, and (e) 0.01–0.6% weight/volume of the antioxidant system, wherein said antioxidant system maintains the amount of the compound of Formula II:

present in said composition at or below 0.5%, preferably at level or below 0.2% by HPLC  % or area % relative to the amount of the compound of Formula I, when storing said composition in a closed container for at least 6 months, at least 12 months, at least 18 months, at least 24 months, or before the expiration of the commercially acceptable shelf life of the composition.

EFFECT: group of inventions described above makes it possible to slow down and/or eliminate formation of a compound of Formula II when using an antioxidant system in pharmaceutical compositions.

78 cl, 4 ex