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):	Feinbaum Claes, Salamun Franc, Patel Sudhir
Assignee:	Orasis Pharmaceuticals Ltd.
Application Number:	US16032044
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) claim 1 , 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) claim 1 , a lubricant claim 1 , 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) claim 8 , 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/orb) 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/orl) 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) claim 9 , a lubricant claim 9 , 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) claim 18 , 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) claim 18 , a lubricant claim 18 , 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) claim 23 , 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) claim 23 , a lubricant claim 23 , 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; andwherein 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 claim 30 , alcohol having 12 to 20 carbon atoms claim 30 , polyethylene-glycol claim 30 , 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 claim 30 , mannitol claim 30 , sorbitol claim 30 , sodium chloride claim 30 , 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 claim 30 , 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 claim 30 , fatty alcohols claim 30 , fatty acids claim 30 , anionic polymers claim 30 , and their alkali salts claim 30 , 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 claim 30 , cresol claim 30 , p-aminobenzoic acid claim 30 , BDSA claim 30 , sorbitrate claim 30 , chlorhexidine claim 30 , benzalkonium chloride claim 30 , sorbic acid claim 30 , polyhexamethylene biguanide claim 30 , sodium perborate claim 30 , 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 claim 30 , borate buffer claim 30 , carbonate buffer claim 30 , citrate buffer claim 30 , phosphate buffer claim 30 , 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 claim 30 , polyethylene glycol claim 30 , propylene glycol claim 30 , and macrogol 4000.38. The ophthalmic pharmaceutical composition of claim 30 , wherein the lubricant is sodium hyaluronate.