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Last Updated: March 29, 2024

Details for Patent: 7,749,970


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Title:Topical treatment of prevention of ocular infections
Abstract: The topical application of an azalide antibiotic such as azithromycin to the eye is useful in treating or preventing ocular infections. In one embodiment, the azalide antibiotic is supplied to the eye in a depot for sustained release. A more convenient dosing regimen can also be provided by the use of an appropriate depot. Furthermore, a composition containing a combination of medicaments is also provided.
Inventor(s): Dawson; Chandler R. (Mill Valley, CA), Bowman; Lyle M. (Pleasanton, CA)
Assignee: Insite Vision Incorporated (Alameda, CA)
Filing Date:Apr 07, 2003
Application Number:10/407,425
Claims:1. An aqueous topical ophthalmic composition comprising azithromycin, a polymeric suspending agent and a steroidal anti-inflammatory agent, wherein said topical ophthalmic composition has a pH of 6 to 7.

2. The topical ophthalmic composition according to claim 1, wherein said steroidal anti-inflammatory agent is selected from the group consisting of Prednisolone acetate, Fluorometholone and Dexamethasone.

3. The topical ophthalmic composition according to claim 2, wherein said steroidal anti-inflammatory agent is Dexamethasone.

4. The topical ophthalmic composition according to claim 1, wherein said topical ophthalmic composition comprises an additional medicament.

5. The topical ophthalmic composition according to claim 4, wherein said additional medicament is selected from the group consisting of antibiotics, antivirals, antifungals, anesthetics, anti-inflammatory agents, and anti-allergic agents.

6. The topical ophthalmic composition according to claim 4, wherein said additional medicament is selected from the group consisting of amikacin, gentamycin, tobramycin, streptomycin, netilmycin, kanamycin, ciprofloxacin, norfloxacin, ofloxacin, trovafloxacin, lomefloxacin, levofloxacin, enoxacin, sulfonamides, polymyxin, chloramphenicol, neomycin, paramomomycin, colistimethate, bacitracin, vancomycin, tetracyclines, rifampins, cycloserine, beta-lactams, cephalosporins, amphotericins, fluconazole, flucytosine, natamycin, miconazole, ketoconazole, corticosteroids, diclofenac, flurbiprofen, ketorolac, suprofen, comolyn, lodoxamide, levocabastin, naphazoling, antazoline, and pheniramimane.

7. The topical ophthalmic composition according to claim 1, wherein said azithromycin is azithromycin dihydrate.

8. The topical ophthalmic composition according to claim 1, wherein the amount of said azithromycin is at least about 5.0%.

9. The topical ophthalmic composition according to claim 1, wherein the amount of said azithromycin is from about 0.1 to about 5.0%.

10. The topical ophthalmic composition according to claim 1, wherein said topical ophthalmic composition is in the form of an aqueous solution, or aqueous suspension.

11. The topical ophthalmic composition according to claim 1, wherein said topical ophthalmic composition has an osmotic pressure of from 10 to 400 mOsM.

12. The topical ophthalmic composition according to claim 1, wherein said topical ophthalmic composition does not contain constituents that are physiologically or ophthalmically harmful to the eye.

13. The topical ophthalmic composition according to claim 1, wherein said steroidal anti-inflammatory agent is contained in an amount of from about 0.01 to 5.0%.

14. The topical ophthalmic composition according to claim 1, wherein said polymeric suspending agent is a water-swellable water-insoluble crosslinked carboxy-vinyl polymer.

15. The topical ophthalmic composition according to claim 14, wherein said water-swellable water-insoluble crosslinked carboxy-vinyl polymer comprises at least 90% acrylic acid monomers and 0.1% to 5% crosslinking agent.

16. The topical ophthalmic composition according to claim 15, wherein the crosslinking agent comprises a difunctional crosslinking agent.

17. The topical ophthalmic composition according to claim 16, wherein said crosslinking agent is selected from the group consisting of divinyl glycol, 2,3-dihydroxyhexa-1,5-diene, 2,5-dimethyl-1,5-hexadiene, divinylbenzene, N,N-diallylacrylamide, N,N-diallymethacrylamide, and mixtures thereof.

18. The topical ophthalmic composition according to claim 14, wherein said water-swellable water-insoluble crosslinked carboxy-vinyl polymer comprises a polycarbophil.

19. The topical ophthalmic composition according to claim 14, wherein said water-swellable water-insoluble crosslinked carboxy-vinyl polymer is contained in an amount of from about 0.5 to 1.2%.

20. The topical ophthalmic composition according to claim 14, wherein said polymer has a monodisperse particle size distribution.

21. The topical ophthalmic composition according to claim 1, comprising 0.01% to 1.0% of said azithromycin.

22. The topical ophthalmic composition according to claim 1, comprising 0.1 to 10% of said polymeric suspending agent.

23. The topical ophthalmic composition according to claim 1, wherein an eye is suffering from at least one condition selected from the group consisting of conjunctivitis, ophthalmic neonatorum, trachoma, corneal ulcers, keratitis, keratoconjunctivitis, endophthalmitis, infectious uveitis and combinations thereof, and said amount of said azithromycin is therapeutically effective to treat said condition.

24. The topical ophthalmic composition according to claim 1, wherein said topical ophthalmic composition is in the form of a depot.

25. A process for treating infection in a tissue of the eye, which comprises: topically applying an aqueous ophthalmic composition to an eye, wherein said ophthalmic composition comprises azithromycin in an amount effective to treat infection in a tissue of the eye, a polymeric suspending agent and a steroidal anti-inflammatory agent, wherein said topical ophthalmic composition has a pH of 6 to 7.

26. The process for treating an eye of claim 25, wherein said steroidal anti-inflammatory agent is selected from the group consisting of Prednisolone acetate, Fluorometholone and Dexamethasone.

27. The process for treating an eye of claim 25, wherein said steroidal anti-inflammatory agent is Dexamethasone.

28. The process for treating an eye of claim 25, wherein said topical ophthalmic composition comprises an additional medicament.

29. The process for treating an eye of claim 28, wherein said additional medicament is selected from the group consisting of antibiotics, antivirals, antifungals, anesthetics, anti-inflammatory agents, and anti-allergic agents.

30. The process for treating an eye of claim 25, wherein said azithromycin is azithromycin dihydrate.

31. The process for treating an eye of claim 25, wherein the amount of said azithromycin is azithromycin dehydrate is about 1.0%.

32. The process for treating an eye of claim 25, wherein the amount of said azithromycin is from about 0.1 to about 5.0%.

33. The process for treating an eye of claim 25, wherein said topical ophthalmic composition is in the form of an aqueous solution, or aqueous suspension.

34. The process for treating an eye of claim 25, wherein said steroidal anti-inflammatory agent is contained in an amount of from about 0.01 to 5.0%.

35. The process for treating an eye of claim 25, wherein said polymeric suspending agent is a water-swellable water-insoluble crosslinked carboxy-vinyl polymer.

36. The process for treating an eye of claim 35, wherein said water-swellable water-insoluble crosslinked carboxy-vinyl polymer comprises a polycarbophil.

37. The process for treating an eye of claim 25, comprising 0.01% to 1.0% of said azithromycin.

38. The process for treating an eye of claim 25, comprising 0.1 to 10% of said polymeric suspending agent.

39. A process for treating an eye, which comprises: topically applying an aqueous ophthalmic composition to an eye, wherein said ophthalmic composition comprises azithromycin, a polymeric suspending agent and a steroidal anti-inflammatory agent and wherein said ophthalmic composition has a pH of 6 to 7, wherein said eye is suffering from at least one condition selected from the group consisting of conjunctivitis, ophthalmic neonatorum, trachoma, corneal ulcers, keratitis, keratoconjunctivitis, endophthalmitis, infectious uveitis and combinations thereof, and said amount of said azithromycin is therapeutically effective to treat said condition.

40. The process for treating an eye of claim 25, wherein said applying provides a therapeutically effective concentration of azithromycin within a tissue of the eye for at least 8 hours.

41. The process for treating an eye of claim 25, wherein said applying provides a therapeutically effective concentration of azithromycin within a tissue of the eye for at least 12 hours.

42. The process for treating an eye of claim 25, wherein said applying provides a therapeutically effective concentration of azithromycin within a tissue of the eye for at least 18 hours.

43. The process for treating an eye of claim 25, wherein said topical ophthalmic composition is in the form of a depot.

44. The process for treating an eye of claim 43, wherein said depot remains for at least 30 minutes after administration.

45. The process for treating an eye of claim 43, wherein said depot remains for at least 4 hours after administration.

46. The topical ophthalmic composition according to claim 3, comprising 0.1 to 2% of said Dexamethasone and 0.1 to 2% of said azithromycin.

47. The topical ophthalmic composition according to claim 3, further comprising: Hydroxypropyl methyl Cellulose or Noveon AA-1; and Sodium Chloride; Mannitol; Edetate Disodium; Poloxamer; Benzalkonium Chloride; Boric Acid; Sodium Hydroxide; and Water.

48. The process for treating an eye of claim 27, comprising 0.1 to 2% of said Dexamethasone and 0.1 to 2% of said azithromycin.

49. The process for treating an eye of claim 27, further comprising: Hydroxypropyl methyl Cellulose or Noveon AA-1; and Sodium Chloride; Mannitol; Edetate Disodium; Poloxamer; Benzalkonium Chloride; Boric Acid; Sodium Hydroxide; and Water.

50. The topical ophthalmic composition according to claim 1, wherein the polymeric suspending agent comprises a polyacrylic acid polymer and said topical ophthalmic composition has a pH of less than about 6.7.

51. The process for treating an eye of claim 25, wherein the polymeric suspending agent comprises a polyacrylic acid polymer and said topical ophthalmic composition has a pH of less than about 6.7.

52. The process for treating an eye of claim 39, wherein the polymeric suspending agent comprises a polyacrylic acid polymer and said topical ophthalmic composition has a pH of less than about 6.7.

53. The topical ophthalmic composition according to claim 1, wherein said topical ophthalmic composition retains substantially the same viscosity in the eye as it had prior to administration to the eye or has increased viscosity after application to the eye.

54. The process for treating an eye of claim 25, wherein said topical ophthalmic composition retains substantially the same viscosity in the eye as it had prior to administration to the eye or has increased viscosity after application to the eye.

55. The process for treating an eye of claim 39, wherein said topical ophthalmic composition retains substantially the same viscosity in the eye as it had prior to administration to the eye or has increased viscosity after application to the eye.

56. The topical ophthalmic composition according to claim 1, wherein the polymeric suspending agent is a polyacrylic acid-type polymer.

57. The process according to claim 25, wherein the polymeric suspending agent is a polyacrylic acid-type polymer.

58. The process according to claim 39, wherein the polymeric suspending agent is a polyacrylic acid-type polymer.

59. An aqueous topical ophthalmic drop composition comprising azithromycin, a polymeric suspending agent and a steroidal anti-inflammatory agent, wherein said aqueous topical ophthalmic drop solution has a pH of 6 to 7, and wherein said composition is in drop form.

60. The aqueous topical ophthalmic drop solution according to claim 59, wherein said steroidal anti-inflammatory agent is Prednisolone acetate.

61. The aqueous topical ophthalmic drop solution according to claim 59, wherein said steroidal anti-inflammatory agent is Fluorometholone.

62. The aqueous topical ophthalmic drop solution according to claim 59, wherein said steroidal anti-inflammatory agent is Dexamethasone.

63. The aqueous topical ophthalmic drop solution according to claim 59, wherein said topical ophthalmic composition comprises an additional medicament.

64. A process for treating infection in a tissue of the eye, which comprises: topically applying an aqueous ophthalmic composition to an eye, wherein said ophthalmic composition comprises azithromycin in an amount effective to treat infection in a tissue of the eye, a polymeric suspending agent and a steroidal anti-inflammatory agent, wherein said topical ophthalmic composition has a pH of 6 to 7, and wherein said composition is in drop form.

65. The process for treating an eye of claim 64, wherein said steroidal anti-inflammatory agent is Prednisolone acetate.

66. The process for treating an eye of claim 64 wherein said steroidal anti-inflammatory agent is Fluorometholone.

67. The process for treating an eye of claim 64, wherein said steroidal anti-inflammatory agent is Dexamethasone.

68. The aqueous topical ophthalmic drop solution according to claim 64, wherein said topical ophthalmic composition comprises an additional medicament.

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