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Last Updated: March 28, 2024

Details for Patent: 6,627,210


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Title: Compositions containing .alpha.-2-adrenergic agonist components
Abstract:Compositions useful for improving effectiveness of alpha-2-adrenergic agonist components include carrier components, alpha-2-adrenergic agonist components, solubility enhancing components which aid in solubilizing the alpha-2-adrenergic agonist components. In one embodiment, the alpha-2-adrenergic agonist components include alpha-2-adrenergic agonists. In another embodiment, the solubility enhancing components include carboxymethylcellulose.
Inventor(s): Olejnik; Orest (Coto de Coza, CA), Kerslake; Edward D. S. (Charlestown, MA)
Assignee: Allergan, Inc. (Irvine, CA)
Filing Date:Jul 10, 2001
Application Number:09/904,018
Claims:1. A therapeutically effective aqueous composition comprising: a therapeutically active alpha-2-adrenergic agonist component selected from the group consisting of 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline, a salt thereof, and an ester thereof in an amount effective to provide a therapeutic benefit to a patient to whom the composition is administered; and a polyanionic solubility enhancing component in an amount effective to increase the solubility of the alpha-2-adrenergic agonist component in the composition relative to the solubility of an identical alpha-2-adrenergic agonist component in a similar composition without the solubility enhancing component.

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

3. The composition of claim 1 wherein the therapeutically active component is substantially unionized.

4. The composition of claim 1 wherein the therapeutically active component is substantially unionized in a biological environment to which the composition is administered.

5. 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 the solubility enhancing component.

6. 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.

7. The composition of claim 1 wherein said polyanionic component 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.

8. The composition of claim 1 wherein the solubility enhancing component is selected from the group consisting of anionic cellulose derivatives and mixtures thereof.

9. The composition of claim 1 wherein the solubility enhancing component is selected from the group consisting of carboxymethylcelluloses and derivatives thereof.

10. 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).

11. 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).

12. 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).

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

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

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

16. A therapeutically effective aqueous composition comprising: a therapeutically active component selected from the group consisting of 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline, a salt thereof, and an ester thereof in an amount effective to provide a therapeutic benefit to a patient to whom the composition is administered; and an anionic cellulose derivative in an amount effective to increase the solubility of the therapeutically active component.

17. The composition of claim 16 wherein the alpha-2-adrenergic agonist component comprises a tartrate of 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline.

18. The composition of claim 16 wherein the anionic cellulose derivative comprises carboxymethylcellulose.

19. The composition of claim 16 wherein the anionic cellulose derivative is present in an amount in a range of about 0.2% (w/v) to about 0.6% (w/v).

20. A therapeutically effective aqueous 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; and an anionic solubility enhancing component in an amount effective to increase the solubility of the tartrate of 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline.

21. The composition of claim 20 wherein the solubility enhancing component comprises a carboxymethylcellulose.

22. The composition of claim 20 which is ophthalmically acceptable.

23. The composition of claim 1 which further comprises a preservative selected from the group consisting of an oxy-chloro component and a quaternary ammonium compound in an amount effective to at least assist in preserving the composition.

24. The composition of claim 23 in which the preservative comprises benzalkonium chloride.

25. The composition of claim 23 in which the preservative comprises an oxy-chloro component.

26. The composition of claim 23 in which the preservative comprises a chlorite component.

27. The composition of claim 16 which further comprises a preservative selected from the group consisting of an oxy-chloro component and a quaternary ammonium compound in an amount effective to at least assist in preserving the composition.

28. The composition of claim 27 which the preservative comprises benzalkonium chloride.

29. The composition of claim 27 in which the preservative comprises an oxy-chloro component.

30. The composition of claim 27 in which the preservative comprises a chlorite component.

31. The composition of claim 20 which further comprises a preservative selected from the group consisting of an oxy-chloro component and a quaternary ammonium compound in an amount effective to at least assist in preserving the composition.

32. The composition of claim 31 in which the preservative comprises benzalkonium chloride.

33. The composition of claim 31 in which the preservative comprises an oxy-chloro component.

34. The composition of claim 31 in which the preservative comprises a chlorite component.

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