Claims for Patent: 9,662,398

Summary for Patent: 9,662,398

Title:	Carboxylvinyl polymer-containing nanoparticle suspensions
Abstract:	The present invention generally relates to suspension compositions having a carboxyvinyl polymer such as a carbomer, a galactomannan such as guar, and a borate compound. A sparingly soluble particulate compound such as nepafenac is also included in the compositions. The sparingly soluble particulate compound has a small particle size to enhance bioavailability of the compound.
Inventor(s):	Chowhan; Masood A. (Arlington, TX), Ghosh; Malay (Fort Worth, TX), Asgharian; Bahram (Arlington, TX), Han; Wesley Weshin (Arlington, TX)
Assignee:	Alcon Research, Ltd. (Fort Worth, TX)
Application Number:	14/539,996
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,662,398
Patent Claims:	1. A topically administrable aqueous ophthalmic suspension composition comprising: a carboxyvinyl polymer at a concentration of 0.1 to 0.5 w/v %, and wherein said carboxyvinyl polymer is a carbomer; a galactomannan at a concentration of 0.1 to 0.4 w/v %, said galactomannan selected from the group consisting of guar, native guar, and hydroxypropyl guar; borate at a concentration of 0.4 to 2.0 w/v %; and a sparingly soluble particulate compound, said compound having a solubility in water at 25.degree. C. of 0.001 to 0.1 w/v % and wherein said sparingly soluble particulate compound is nepafenac at a concentration of 0.1 to 1.0 w/v %. 2. A composition according to claim 1, further comprising a pH-adjusting agent in an amount sufficient to cause the composition to have a pH of 5.0 to 7.2. 3. A composition according to claim 1, further comprising a tonicity-adjusting agent in an amount sufficient to cause the composition to have an osmolality of 250 to 350 mOsm/kg. 4. A composition according to claim 1 wherein said carboxyvinyl polymer is carbomer at a concentration of 0.4 w/v %. 5. A composition according to claim 1 further comprising a milling agent at a concentration of 0.005 to 0.1 w/v %. 6. A composition according to claim 5 wherein said milling agent is a surfactant or polymer. 7. A composition according to claim 6 wherein said milling agent is sodium carboxylmethylcellulose. 8. A composition according to claim 1 further comprising a metal chloride salt tonicity-adjusting agent. 9. A composition according to claim 8 wherein said metal chloride salt is sodium chloride at a concentration of 0.4 w/v %. 10. A composition according to claim 1 further comprising a non-ionic hydroxyl compound as a tonicity-adjusting agent. 11. A composition according to claim 1 further comprising both a preservative and a chelating agent. 12. A composition according to claim 11 wherein the preservative is benzalkonium chloride at a concentration of 0.005 w/v % and the chelating agent is edetate disodium at a concentration of 0.01 w/v %. 13. A composition according to claim 1 wherein said carboxyvinyl polymer is carbomer, said galactomannan is native guar, said borate is boric acid, and said sparingly soluble particulate compound is nepafenac at a concentration of 0.1 to 1.0 w/v %. 14. A composition according to claim 13 comprising 0.4 w/v % carbomer, 0.2 w/v % native guar, 0.5 w/v % boric acid, and 0.3 w/v % nepafenac. 15. A composition according to claim 14 wherein said nepafenac has an average particle size of 400 nm. 16. The composition according to claim 2, further comprising a pH adjusting agent in an amount sufficient to cause the composition to have a pH of 7.0. 17. The composition according to claim 7 wherein said milling agent is 0.06 w/v % sodium carboxymethylcellulose. 18. The composition according to claim 10, wherein said non-ionic hydroxyl compound is propylene glycol at a concentration of 0.5 w/v %. 19. The composition according to claim 1 wherein said carboxylvinyl polymer is Carbopol.RTM. 974p. 20. The composition according to claim 19 wherein said carboxylvinyl polymer is present at a concentration of 0.4 w/v %. 21. The composition according to claim 1 wherein said galactomannan is guar or native guar. 22. The composition according to claim 21 wherein said galactomannan is present at a concentration of 0.2 w/v %. 23. The composition according to claim 1 wherein said borate is boric acid. 24. The composition according to claim 23 wherein said borate is present at a concentration of 0.4 to 0.6 w/v %. 25. The composition according to claim 24 wherein said borate is present at a concentration of 0.5 w/v %. 26. The composition according to claim 1 wherein said sparingly soluble particulate compound is present at a concentration of 0.25 to 0.35 w/v %. 27. The composition according to claim 1 wherein said sparingly soluble particulate compound is present at a concentration of 0.3 w/v %. 28. The composition according to claim 1 further comprising a chelating agent. 29. The composition according to claim 28 wherein said chelating agent is edetate disodium. 30. The composition according to claim 29 wherein said chelating agent is present at a concentration of 0.001 to 0.1 w/v %. 31. The composition according to claim 30 wherein said chelating agent is present at a concentration of 0.01 w/v %. 32. A topically administrable ophthalmic suspension composition consisting essentially of a) 0.3 w/v % nepafenac; b) 0.4 w/v % carbomer; c) 0.2 w/v % native guar; d) 0.5 w/v % boric acid; e) 0.06 w/v % sodium carboxymethylcellulose; f) 0.4 w/v % sodium chloride; g) 0.5 w/v % propylene glycol; i) 0.005% (w/v) benzalkonium chloride; j) 0.01% edetate disodium; and k) purified water.