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Claims for Patent: 6,562,873

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Claims for Patent: 6,562,873

Title: Compositions containing therapeutically active components having enhanced solubility
Abstract:Compositions which include therapeutically active components, solubility enhancing components other than cyclodextrins, and oxy-chloro components, wherein the oxy-chloro components are substantially effective as preservatives. In one embodiment, the oxy-chloro components are useful for preserving the therapeutically active components. In one embodiment, the oxy-chloro components include chlorite components. In a useful embodiment, the solubility enhancing components include carboxymethylcellulose.
Inventor(s): Olejnik; Orest (Coto de Coza, CA), Kerslake; Edward D. S. (Charleston, MA)
Assignee: Allergan, Inc. (Irvine, CA)
Application Number:09/903,962
Patent Claims: 1. A composition comprising: a therapeutically active component selected from the group consisting of alpha-2-adrenergic agonists and mixtures thereof, and being present in an amount effective to provide a desired therapeutic benefit to a patient to whom the composition is administered; a solubility enhancing component, other than a cyclodextrin, in an amount effective to increase the solubility of the therapeutically active component in the composition relative to the solubility of an identical therapeutically active component in a similar composition without the solubility enhancing component; an oxy-chloro component in an effective amount to at least aid in preserving the composition; and a liquid carrier component.

2. The composition of claim 1 wherein the therapeutically active component is selected from the group consisting of imino-imidazolines, imidazolines, imidazoles, azepines, thiazines, oxazolines, guanidines, catecholamines, and mixtures thereof.

3. The composition of claim 1 wherein the therapeutically active component includes a quinoxaline component.

4. The composition of claim 3 wherein the quinoxaline component is selected from the group consisting of quinoxalines, quinoxaline derivatives, and mixtures thereof.

5. The composition of claim 3 wherein the quinoxaline component is selected from the group consisting of quinoxaline, (2-imidozolin-2-ylamino) quinoxaline, 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline, and tartrate of 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline, and mixtures thereof.

6. The composition of claim 1 wherein the therapeutically active component comprises a tartrate of 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline.

7. The composition of claim 1 wherein the therapeutically active component has increased diffusion through a lipid membrane relative to an identical therapeutically active component in a similar composition without the solubility enhancing component.

8. The composition of claim 1 wherein the solubility enhancing component is effective to increase the solubility in a biological environment of the therapeutically active component relative to the solubility in a biological environment of an identical therapeutically active component in a similar composition without the solubility enhancing component.

9. The composition of claim 1 wherein the solubility enhancing component comprises a polyanionic component.

10. The composition of claim 9 wherein said polyanionic components is selected from the group consisting of anionic cellulose derivatives, anionic polymers derived from acrylic acid, anionic polymers derived from methacrylic acid, anionic polymers derived from alginic acid, anionic polymers derived from amino acids and mixtures thereof.

11. The composition of claim 1 wherein the solubility enhancing component comprises an anionic cellulose derivative.

12. The composition of claim 1 wherein the solubility enhancing component comprises a carboxymethylcellulose.

13. The composition of claim 1 wherein the solubility enhancing component is present in an amount in a range of about 0.1% (w/v) to about 30% (w/v).

14. The composition of claim 1 wherein the solubility enhancing component is present in an amount in a range of about 0.2% (w/v) to about 10 (w/v).

15. The composition of claim 1 wherein the solubility enhancing component is present in an amount in a range of about 0.2% (w/v) to about 0.6% (w/v).

16. The composition of claim 1 wherein the oxy-chloro component is selected from the group consisting of hypochlorite components, perchlorate components, chlorite components and mixtures thereof.

17. The composition of claim 1 wherein the oxy-chloro component comprises a chlorite component.

18. The composition of claim 1 wherein the oxy-chloro component comprises stabilized chlorine dioxide.

19. The composition of claim 1, wherein the oxy-chloro component is present in an amount of about 500 ppm (w/v) or less.

20. The composition of claim 1 wherein the oxy-chloro component is present in an amount in a range of about 10 ppm (w/v) to about 200 ppm (w/v).

21. The composition of claim 1 which further comprises an additional preservative component other than the oxy-chloro component in an amount effective to at least aid in preserving the composition.

22. The composition of claim 21, wherein the additional preservative component is selected from the group consisting of sorbic acid, benzalkonium chloride, chlorbutol and alkyl esters of p-hydroxybenzoic acid and mixtures thereof.

23. The composition of claim 1 wherein the liquid carrier is an aqueous liquid carrier component.

24. The composition of claim 1 which is a solution.

25. The composition of claim 1 which has a pH of about 7 or greater.

26. The composition of claim 1 which has a pH in a range of about 7 to about 9.

27. The composition of claim 1 which is ophthalmically acceptable.

28. A composition comprising: a therapeutically active component selected from the group consisting of alpha-2-adrenergic agonists and mixtures thereof in an amount effective to provide a therapeutic benefit to a patient to whom the composition is administered; an anionic cellulose derivative in an amount effective to increase the solubility of the therapeutically active component; a chlorite component in an effective amount to at least aid in preserving the composition; and an aqueous liquid carrier component.

29. The composition of claim 28 wherein the therapeutically active component comprises a tartrate of 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline.

30. The composition of claim 28 wherein the anionic cellulose derivative comprises carboxymethylcellulose.

31. The composition of claim 28 wherein the anionic cellulose derivative is present in an amount in a range of about 0.2% to about 0.6% (w/v).

32. A composition comprising: a tartrate of 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline in an amount effective to provide a therapeutic benefit to a patient to whom the composition is administered; a solubility enhancing component in an amount effective to increase the solubility of the tartrate of 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline; a chlorite component in an effective amount to at least aid in preserving the composition; and an aqueous liquid carrier component.

33. The composition of claim 32 wherein the solubility enhancing component comprises a carboxymethylcellulose.

34. The composition of claim 32 which is ophthalmically acceptable.

35. A composition comprising: a therapeutically active component in an amount effective to provide a desired therapeutic benefit to a patient to whom the composition is administered; an oxy-chloro component in an effective amount to at least aid in preserving the composition; and a liquid carrier component, wherein the composition is substantially free of cyclodextrins.

36. The composition of claim 35 wherein the therapeutically active component is selected from the group consisting of antibacterials, antihistamines, decongestants, antiinflammatories, antiparasitics, miotics, anticholinergics, adrenergics, antivirals, local anesthetics, antifungals, amoebicidals, trichomonocidals, analgesics, mydriatics, antiglaucoma drugs, carbonic anhydrase inhibitors, ophthalmic diagnostic agents, ophthalmic agents used as adjuvants in surgery, chelating agents, antineoplascics, antihypertensives, muscle relaxants, diagnostics, and mixtures thereof.

37. The composition of claim 35 wherein the therapeutically active component is selected from the group consisting of adrenergic agonists and mixtures thereof.

38. The composition of claim 35 wherein the therapeutically active component is selected from the group consisting of alpha-2-adrenergic agonists and mixtures thereof.

39. The composition of claim 35 wherein the therapeutically active component is selected from the group consisting of imino-imidazolines, imidazolines, imidazoleS, azepines, thiazines, oxazolines, guanidines, catecholamines, and mixtures thereof.

40. The composition of claim 35 wherein the therapeutically active component includes a quinoxaline component.

41. The composition of claim 40 wherein the quinoxaline component is selected from the group consisting of quinoxalines, quinoxaline derivatives, and mixtures thereof.

42. The composition of claim 40 wherein the quinoxaline component is selected from the group consisting of quinoxaline, (2-imidozolin-2-ylamino) quinoxaline, 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline, and tartrate of 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline, and mixtures thereof.

43. The composition of claim 35 wherein the therapeutically active component comprises a tartrate of 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline.

44. The composition of claim 35, which further includes a solubility enhancing component, other than a cyclodextrin, in an amount effective to increase the solubility of the therapeutically active component in the composition relative to the solubility of an identical therapeutically active component in a similar composition without the solubility enhancing component.

45. The composition of claim 44 wherein the solubility enhancing component comprises a polyanionic component.

46. The composition of claim 35 wherein the oxy-chloro component is selected from the group consisting of hypochlorite components, perchlorate components, chlorite components and mixtures thereof.

47. The composition of claim 35 wherein the oxy-chloro component comprises a chlorite component.

48. The composition of claim 35 wherein the oxy-chloro component comprises stabilized chlorine dioxide.

49. The composition of claim 35 which is ophthalmically acceptable.
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