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Last Updated: October 23, 2020

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Claims for Patent: 9,662,398

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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.

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