ANESTHETIC COMPOSITION AND METHOD OF EYE ANESTHETIZATION Russian patent published in 2024 - IPC A61K31/245 A61K31/38 A61P27/02 A61P23/02 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: group of inventions relates to aqueous ophthalmic anesthetic compositions and a method of their preparation. An aqueous ophthalmic anesthetic composition for topical use contains articaine in an amount from 4.0 to 12.0 w/v.% based on the volume of the composition and a buffer in an amount that provides a pH from 3.5 to 7.0 and an osmolality from 275 to 1,171 mOsmol/kg to facilitate topical use for ophthalmic anesthesia, where the specified buffer does not react with articaine and stabilizes it and inhibits the decomposition of the said articaine during the storage. The method of obtaining the specified composition includes stages in which the acid or its salt is mixed with a sugar alcohol in solution to form a complex, the pH is adjusted to a value from 3.5 to 7.0 and articaine is added to the resulting solution in an amount sufficient to obtain a composition containing from 4.0 to 12.0 w/v.% based on the volume of the composition. The aqueous ophthalmic composition contains 80 mg/g of articaine HCl, 1.373 mg/g of sodium dihydrogen phosphate monohydrate, 1.413 mg/g of anhydrous dibasic sodium phosphate, 8.1 mg/g of hydroxypropyl methylcellulose, 4 mg/g of PEG400 and the said composition has a pH of 6.0 to 7.0, viscosity from 0.743 to 0.803 Pa⋅ (743 to 803 cP) and an osmolality of 517 mOsmol/kg, and wherein the said buffer does not react with articaine and stabilizes the said articaine by inhibiting the degradation of the said articaine during storage. The aqueous ophthalmic anesthetic composition contains articaine in an amount of at least 7.0 w/v.% based on the volume of the composition and a buffer in an amount that ensures a pH from 4.0 to 5.5 and stabilization of articaine, wherein the said buffer is a complex obtained from boric acid or a salt of boric acid and a sugar alcohol, in an amount that preserves the said articaine in solution or suspension and inhibits the decomposition of the said articaine during storage.

EFFECT: above group of inventions makes it possible to ensure the stability of articaine during long-term storage of the resulting compositions.

30 cl, 2 tbl, 2 ex