Claims for Patent: 10,639,297

Summary for Patent: 10,639,297

Title:	Ophthalmic pharmaceutical compositions and uses relating thereto
Abstract:	The disclosure relates to ophthalmic pharmaceutical compositions comprising pilocarpine or a pharmaceutically acceptable salt. Aspects of the disclosure further relate to uses and preparations of ophthalmic pharmaceutical compositions comprising pilocarpine or a pharmaceutically acceptable salt, for correcting presbyopia and other ocular conditions in a subject.
Inventor(s):	Claes Feinbaum, Franc SALAMUN, Sudhir PATEL
Assignee:	Orasis Pharmaceuticals Ltd
Application Number:	US16/032,044
Patent Claims:	1. An ophthalmic pharmaceutical composition consisting of pilocarpine or a pharmaceutically acceptable salt thereof at a concentration of about 0.01% (w/w or w/v) to about 0.45% (w/w or w/v), a lubricant, and one or more pharmaceutically acceptable carriers; wherein the lubricant is selected from the group consisting of hyaluronic acid or pharmaceutically acceptable salt thereof, cellulose, carboxymethyl cellulose sodium, hydroxyethyl cellulose, methylcellulose, dextran, gelatin, a polyol, glycerin, polyethylene glycol 300, polyethylene glycol 400, polysorbate, propylene glycol, polyvinyl alcohol, hydroxypropyl methylcellulose, or povidone, or mixtures thereof. 2. The ophthalmic pharmaceutical composition of claim 1, wherein the pilocarpine salt is pilocarpine hydrochloride or pilocarpine nitrate. 3. The ophthalmic pharmaceutical composition of claim 1, wherein the lubricant is sodium hyaluronate at a concentration of 0.01% (w/w or w/v) to 0.9% (w/w or w/v) and/or hydroxypropyl methylcellulose at a concentration of 0.1% (w/w or w/v) to 2.0% (w/w or w/v). 4. The ophthalmic pharmaceutical composition of claim 1, wherein the lubricant is sodium hyaluronate. 5. The ophthalmic pharmaceutical composition of claim 1, wherein the concentration of the lubricant is about 0.01% (w/w or w/v) to about 3.0% (w/w or w/v). 6. The ophthalmic pharmaceutical composition of claim 1, wherein the pilocarpine or a pharmaceutically acceptable salt thereof is at a concentration of about 0.2% (w/w or w/v) to about 0.45% (w/w or w/v), and the lubricant is sodium hyaluronate at a concentration of 0.01% (w/w or w/v) to 0.9% (w/w or w/v) and/or hydroxypropyl methylcellulose at a concentration of 0.1% (w/w or w/v) to 2.0% (w/w or w/v). 7. The ophthalmic pharmaceutical composition of claim 1, wherein the ophthalmic pharmaceutical composition is effective for correction of presbyopia for up to 24 hours. 8. A method of correcting presbyopia in a subject comprising administering to the subject a therapeutically effective amount of an ophthalmic pharmaceutical composition consisting of pilocarpine or a pharmaceutically acceptable salt thereof at a concentration of about 0.01% (w/w or w/v) to about 0.45% (w/w or w/v), a lubricant, and one or more pharmaceutically acceptable carriers; wherein the lubricant is selected from the group consisting of hyaluronic acid or pharmaceutically acceptable salt thereof, cellulose, carboxymethyl cellulose sodium, hydroxyethyl cellulose, methylcellulose, dextran, gelatin, a polyol, glycerin, polyethylene glycol 300, polyethylene glycol 400, polysorbate, propylene glycol, polyvinyl alcohol, hydroxypropyl methylcellulose, or povidone, or mixtures thereof. 9. The method of claim 8, wherein the pilocarpine salt is pilocarpine hydrochloride or pilocarpine nitrate. 10. The method of claim 8, wherein the lubricant is sodium hyaluronate at a concentration of 0.01% (w/w or w/v) to 0.9% (w/w or w/v) and/or hydroxypropyl methylcellulose at a concentration of 0.1% (w/w or w/v) to 2.0% (w/w or w/v). 11. The method of claim 8, wherein the pilocarpine or a pharmaceutically acceptable salt thereof is at a concentration of about 0.2% (w/w or w/v) to about 0.45% (w/w or w/v), and the lubricant is sodium hyaluronate at a concentration of 0.01% (w/w or w/v) to 0.9% (w/w or w/v) and/or hydroxypropyl methylcellulose at a concentration of 0.1% (w/w or w/v) to 2.0% (w/w or w/v). 12. The method of claim 8, wherein the concentration of lubricant is about 0.01% (w/w or w/v) to about 3.0% (w/w or w/v). 13. The method of claim 8, wherein the lubricant is sodium hyaluronate. 14. The method of claim 9, wherein the ophthalmic pharmaceutical composition is: a) effective for up to 24 hours; and/or b) effective without adversely affecting night vision. 15. The method of claim 9, wherein the administration is topical or by surgical intervention. 16. The method of claim 9, wherein the subject: a) is a spectacle wearer who cannot or will not use progressive or bifocal lenses; b) underwent cataract surgery; c) developed presbyopia after a corneal procedure; d) has mono-focal or multifocal intraocular lenses; e) uses contact lenses and does not tolerate mono-vision contact lenses; f) uses contact lenses and does not tolerate multifocal contact lenses; g) suffers from a higher order aberration after corneal surgery; h) suffers from hyperopia or tropias; i) does not tolerate a change in spectacle prescription; j) experiences a rapid change in spectacle prescription; k) is at risk of falls when using progressive or bifocal lenses; and/or l) suffers from a higher order aberration at night or under light conditions. 17. A method of increasing the depth of field in a subject's eye comprising administering to the subject a therapeutically effective amount of an ophthalmic pharmaceutical composition consisting of pilocarpine or a pharmaceutically acceptable salt thereof at a concentration of about 0.01% (w/w or w/v) to about 0.45% (w/w or w/v), a lubricant, and one or more pharmaceutically acceptable carriers; wherein the lubricant is selected from the group consisting of hyaluronic acid or pharmaceutically acceptable salt thereof, cellulose, carboxymethyl cellulose sodium, hydroxyethyl cellulose, methylcellulose, dextran, gelatin, a polyol, glycerin, polyethylene glycol 300, polyethylene glycol 400, polysorbate, propylene glycol, polyvinyl alcohol, hydroxypropyl methylcellulose, or povidone, or mixtures thereof. 18. The method of claim 17, wherein the pilocarpine salt is pilocarpine hydrochloride or pilocarpine nitrate. 19. The method of claim 17, wherein the lubricant is sodium hyaluronate at a concentration of 0.01% (w/w or w/v) to 0.9% (w/w or w/v) and/or hydroxypropyl methylcellulose at a concentration of 0.1% (w/w or w/v) to 2.0% (w/w or w/v). 20. The method of claim 17, wherein the lubricant is sodium hyaluronate. 21. The method of claim 17, wherein the concentration of lubricant is about 0.01% (w/w or w/v) to about 3.0% (w/w or w/v). 22. The method of claim 18, wherein the pilocarpine or a pharmaceutically acceptable salt thereof is at a concentration of about 0.2% (w/w or w/v) to about 0.45% (w/w or w/v), and the lubricant is sodium hyaluronate at a concentration of 0.01% (w/w or w/v) to 0.9% (w/w or w/v) and/or hydroxypropyl methylcellulose at a concentration of 0.1% (w/w or w/v) to 2.0% (w/w or w/v). 23. A method of reducing the size of a pupil in a subject comprising administering to the subject a therapeutically effective amount of an ophthalmic pharmaceutical composition consisting of pilocarpine or a pharmaceutically acceptable salt thereof at a concentration of about 0.01% (w/w or w/v) to about 0.45% (w/w or w/v), a lubricant, and one or more pharmaceutically acceptable carriers; wherein the lubricant is selected from the group consisting of hyaluronic acid or pharmaceutically acceptable salt thereof, cellulose, carboxymethyl cellulose sodium, hydroxyethyl cellulose, methylcellulose, dextran, gelatin, a polyol, glycerin, polyethylene glycol 300, polyethylene glycol 400, polysorbate, propylene glycol, polyvinyl alcohol, hydroxypropyl methylcellulose, or povidone, or mixtures thereof. 24. The method of claim 23, wherein the pilocarpine salt is pilocarpine hydrochloride or pilocarpine nitrate. 25. The method of claim 24, wherein the lubricant is sodium hyaluronate at a concentration of 0.01% (w/w or w/v) to 0.9% (w/w or w/v) and/or hydroxypropyl methylcellulose at a concentration of 0.1% (w/w or w/v) to 2.0% (w/w or w/v). 26. The method of claim 23, wherein the lubricant is sodium hyaluronate. 27. The method of claim 23, wherein the concentration of lubricant is about 0.01% (w/w or w/v) to about 3.0% (w/w or w/v). 28. The method of claim 23, wherein the pilocarpine or a pharmaceutically acceptable salt thereof is at a concentration of about 0.2% (w/w or w/v) to about 0.45% (w/w or w/v), and the lubricant is sodium hyaluronate at a concentration of 0.01% (w/w or w/v) to 0.9% (w/w or w/v) and/or hydroxypropyl methylcellulose at a concentration of 0.1% (w/w or w/v) to 2.0% (w/w or w/v). 29. The method of claim 23, wherein the ophthalmic pharmaceutical composition is effective for correction of presbyopia for up to 24 hours. 30. An ophthalmic pharmaceutical composition consisting of pilocarpine or a pharmaceutically acceptable salt thereof at a concentration of about 0.01% (w/w or w/v) to about 0.45% (w/w or w/v), a lubricant, and one or more pharmaceutically acceptable carriers; wherein the lubricant is selected from the group consisting of hyaluronic acid or pharmaceutically acceptable salt thereof, cellulose, carboxymethyl cellulose sodium, hydroxyethyl cellulose, methylcellulose, dextran, gelatin, a polyol, glycerin, polyethylene glycol 300, polyethylene glycol 400, polysorbate, propylene glycol, polyvinyl alcohol, hydroxypropyl methylcellulose, or povidone, or mixtures thereof; and wherein the one or more pharmaceutically acceptable carriers are selected from the group consisting of one or more solvents, one or more solubilizers, one or more pH agents, one or more dispersing agents, one or more diluents, one or more suspension aids, one or more surface active agents, one or more isotonic agents, one or more stabilizers, one or more thickening or emulsifying agents, one or more preservatives, one or more buffers, one or more core-shell nanoparticles, one or more polymers, one or more peptides, one or more proteins, or mixtures thereof. 31. The ophthalmic pharmaceutical composition of claim 30, wherein the one or more dispersing agents are selected from the group consisting of polyethoxylated castor oil, alcohol having 12 to 20 carbon atoms, polyethylene-glycol, or mixtures thereof. 32. The ophthalmic pharmaceutical composition of claim 30, wherein the one or more isotonic agents are selected from the group consisting of glycerin, mannitol, sorbitol, sodium chloride, or mixtures thereof. 33. The ophthalmic pharmaceutical composition of claim 30, wherein the one or more stabilizers are selected from the group consisting of sodium hydrogen sulphite and/or ethylenediaminetetraacetic acids, or mixtures thereof. 34. The ophthalmic pharmaceutical composition of claim 30, wherein the one or more thickening or emulsifying agents are selected from the group consisting of non-ionic water-soluble polymers, fatty alcohols, fatty acids, anionic polymers, and their alkali salts, or mixtures thereof. 35. The ophthalmic pharmaceutical composition of claim 30, wherein the one or more preservatives are selected from the group consisting of phenol, cresol, p-aminobenzoic acid, BDSA, sorbitrate, chlorhexidine, benzalkonium chloride, sorbic acid, polyhexamethylene biguanide, sodium perborate, or mixtures thereof. 36. The ophthalmic pharmaceutical composition of claim 30, wherein the one or more buffers are selected from the group consisting of an acetate buffer, borate buffer, carbonate buffer, citrate buffer, phosphate buffer, or mixtures thereof. 37. The ophthalmic pharmaceutical composition of claim 30, wherein the one or more solubilizers are selected from the group consisting of polysorbate, polyethylene glycol, propylene glycol, and macrogol 4000. 38. The ophthalmic pharmaceutical composition of claim 30, wherein the lubricant is sodium hyaluronate.