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Last Updated: March 28, 2024

Claims for Patent: 6,569,443


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Summary for Patent: 6,569,443
Title: Topical treatment or 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, Inc. (Alameda, CA)
Application Number:09/767,943
Patent Claims: 1. A process for treating an eye, comprising: topically applying an azalide antibiotic to an eye in an amount effective to treat infection in a tissue of the eye, wherein said topically applying comprises supplying a depot of a composition containing said azalide antibiotic on the eye.

2. The process according to claim 1, wherein said eye is suffering from at least one condition selected from the group consisting of conjunctivitis, ophthalmia neonatorum, trachoma, corneal ulcers, keratitis, keratoconjunctivitis, endophthalmitis, infectious uveitis and combinations thereof, and said amount of said azalide antibiotic is therapeutically effective to treat said condition.

3. The process according to claim 1, wherein said azalide antibiotic is a compound of formula (I): ##STR2##

wherein R.sup.1 and R.sup.2 each independently represent a hydrogen atom or methyl group.

4. The process according to claim 3, wherein said azalide antibiotic is azithromycin.

5. The process according to claim 3, wherein said applying provides a therapeutically effective concentration of azalide antibiotic within a tissue of the eye for at least 8 hours.

6. The process according to claim 5, wherein said applying provides a therapeutically effective concentration of azalide antibiotic within a tissue of the eye for at least 12 hours.

7. The process according to claim 6, wherein said applying provides a therapeutically effective concentration of azalide antibiotic within a tissue of the eye for at least 18 hours.

8. The process according to claim 1, wherein said depot is an aqueous polymeric suspension of said azalide antibiotic.

9. The process according to claim 8, wherein said aqueous polymeric suspension further comprises an additional medicament.

10. The process according to claim 9, 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.

11. The process according to claim 1, wherein said depot is a composition selected from the group consisting of an aqueous suspensions, ointments, and inserts.

12. The process according to claim 11, wherein said composition further comprises an additional medicament.

13. The process according to claim 12, wherein said additional medicament is selected from the group consisting of antibiotics, antivirals, antifungals, anesthetics, anti-inflammatory agents, and anti-allergic agents.

14. The process according to claim 1, wherein said depot remains for at least 30 minutes after administration.

15. The process according to claim 14, wherein said depot remains for at least 4 hours after administration.

16. A topical ophthalmic composition comprising an aqueous polymeric suspension comprising water, 0.01% to 1.0% of an azalide antibiotic and 0.1 to 10% of a polymeric suspending agent, wherein said topical ophthalmic composition has an osmotic pressure of from 10 to 400 mOsM and wherein said composition does not contain constituents that are physiologically or ophthalmically harmful to the eye.

17. The composition according to claim 16, wherein said suspension further comprises an additional medicament selected from the group consisting of antibiotics, antivirals, antifungals, anesthetics, anti-inflammatory agents, and anti-allergic agents.

18. The composition according to claim 17, wherein said additional medicament is contained in the amount of from 0.01 to 5.0%.

19. The composition according to claim 17, 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, bacitran, vancomycin, tetracyclines, rifampins, cycloserine, beta-lactams, cephalosporins, amphotericins, fluconazole, flucytosine, matamycin, miconazole, ketoconazole, corticosteroids, diclofenac, flurbiprofen, ketorolac, suprofen, comolyn, lodoxamide, levocabastin, naphazoling, antazoline, and pheniramimane.

20. A topical ophthalmic composition comprising about 0.01 to about 5% of an azalide antibiotic, an ophthalmically acceptable carrier, and an additional medicament selected from the group consisting of antibiotics, antivirals, antifungals, anesthetics, anti-inflammatory agents, and anti-allergic agents, wherein said topical ophthalmic composition has an osmotic pressure of from 10 to 400 mOsM and wherein said composition does not contain constituents that are physiologically or ophthalmically harmful to the eye.

21. The composition according to claim 20, wherein said composition is fluid; said azalide antibiotic is contained in an amount of from about 0.01 to 2.0%; and said additional medicament is contained in an amount of from about 0.01 to 5.0%.

22. The composition according to claim 21, wherein said ophthalmically acceptable carrier is water or an aqueous solution and 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.

23. A process for treating an eye, comprising: topically applying an azalide antibiotic to an eye of a non-human animal in an amount effective to treat infection in a tissue of the eye, wherein said topically applying comprises supplying a depot of a composition containing said azalide antibiotic on the eye.

24. The process according to claim 23, wherein said non-human animal is a mammal.

25. The process according to claim 23, wherein said mammal is selected from the group consisting of cows, sheep, horses, pigs, goats, rabbits, dogs, and cats.

26. The process according to claim 23, wherein said depot is an aqueous polymeric suspension of said azalide antibiotic.

27. The process according to claim 26, wherein said aqueous polymeric suspension further comprises an additional medicament.

28. The process according to claim 27, 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.

29. The process according to claim 23, wherein said depot is a composition selected from the group consisting of an aqueous suspensions, ointments, and inserts.

30. The process according to claim 29, wherein said depot remains for at least 30 minutes after administration.

31. The process according to claim 30, therein said depot remains for at least 4 hours after administration.

32. The process according to claim 23, wherein said composition further comprises an additional medicament.

33. The process according to claim 32, wherein said additional medicament is selected from the group consisting of antibiotics, antivirals, antifungals, anesthetics, anti-inflammatory agents, and anti-allergic agents.

34. The process according to claim 23, 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 azalide antibiotic is therapeutically effective to treat said condition.

35. The process according to claim 23, wherein said azalide antibiotic is a compound of formula (I): ##STR3##

wherein R.sup.1 and R.sup.2 each independently represent a hydrogen atom or methyl group.

36. The process according to claim 35, wherein said azalide antibiotic is azithromycin.

37. The process according to claim 23, wherein said applying provides a therapeutically effective concentration of azalide antibiotic within a tissue of the eye for at least 8 hours.

38. The process according to claim 37, wherein said applying provides a therapeutically effective concentration of azalide antibiotic within a tissue of the eye for at least 12 hours.

39. The process according to claim 38, wherein said applying provides a therapeutically effective concentration of azalide antibiotic within a tissue of the eye for at least 18 hours.

40. The process according to claim 1, wherein the amount of said azalide antibiotic is at least about 5.0%.

41. The process according to claim 1, wherein the amount of said azalide antibiotic is from about 0.1 to about 5.0%.

42. The composition according to claim 20, wherein said composition is fluid; said azalide antibiotic is contained in an amount from at least about 5.0%, and said additional medicament is contained in an amount of from about 0.01 to 5.0%.

43. The composition according to claim 20, wherein said composition is fluid; said azalide antibiotic is contained in an amount from about 0.1 to about 5.0%, and said additional medicament is contained in an amount of from about 0.001 to 5.0%.

44. A topical ophthalmic composition comprising an aqueous polymeric suspension comprising water, from about 0.1 to about 5.0% of an azalide antibiotic, and 0.1 to 10% of a polymeric suspending agent, wherein said topical ophthalmic composition has an osmotic pressure of from 10 to 400 mOsM and wherein said composition does not contain constituents that are physiologically or ophthalmically harmful to the eye and said topical ophthalmic composition is in the form of a depot which is capable of sustained release of said azalide antibiotic.

45. The composition according to claim 20, wherein said azalide antibiotic is azithromycin.

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