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Last Updated: April 19, 2024

Claims for Patent: 9,295,641


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Summary for Patent: 9,295,641
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): Graham; Richard (Irvine, CA), Bakhit; Peter (Huntington Beach, CA), Olejnik; Orest (Coto De Caza, CA)
Assignee: ALLERGAN, INC. (Irvine, CA)
Application Number:14/484,017
Patent Claims: 1. A method of reducing elevated intraocular pressure in a patient, the method comprising administering a therapeutically effective amount of a first composition comprising from about 0.1% (w/v) to about 0.15% (w/v) brimonidine tartrate and about 0.5% (w/v) carboxymethyl cellulose, wherein the composition is administered to at least one eye of the patient three times daily.

2. The method of claim 1, wherein the method lowers intraocular pressure as effectively and results in a lower incidence of one or more side effects as compared to the administration of a second composition comprising 0.2% (w/v) brimonidine tartrate three times daily.

3. The method of claim 2, wherein the one or more side effects are selected from the group consisting of allergic conjunctivitis, oral dryness, conjunctival hyperemia, eye discharge, asthenia, and eye pruritis.

4. The method of claim 1, wherein the composition further comprises about 0.005% (w/v) stabilized oxychloro complex.

5. The method of claim 1, wherein the first composition has a pH about equal to or greater than 7.

6. The method of claim 5, wherein the first composition has a pH of 7.4 to 8.0.

7. The method of claim 1, wherein the first composition comprises 0.15% (w/v) brimonidine tartrate.

8. The method of claim 1, wherein the first composition comprises 0.1% (w/v) brimonidine tartrate.

9. The method of claim 1, wherein the method is effective at treating open-angle glaucoma.

10. The method of claim 1, wherein the method is effective at treating ocular hypertension.

11. The method of claim 1, wherein the first composition is administered approximately every eight hours.

12. The method of claim 2, wherein the first composition comprises 0.15% (w/v) brimonidine tartrate, 0.5% (w/v) carboxymethyl cellulose, and 0.005% (w/v) stabilized oxychloro complex.

13. The method of claim 2, wherein the first composition comprises 0.1% (w/v) brimonidine tartrate, 0.5% (w/v) carboxymethyl cellulose, and 0.005% (w/v) stabilized oxychloro complex.

14. A method of treating glaucoma or ocular hypertension, the method comprising administering to the eye a therapeutically effective amount of a first composition comprising up to about 0.15% (w/v) of a therapeutically active alpha-2-adrenergic agonist component selected from the group consisting of 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline and a salt thereof, in an amount effective to provide a therapeutic benefit to a patient to whom the first 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 first composition relative to the solubility of an identical alpha-2-adrenergic agonist component in a similar composition without the solubility enhancing component.

15. The method of claim 14, wherein the first composition comprises a pH of about 7.0 or greater.

16. The method of claim 15, wherein the therapeutically active alpha-2-adrenergic agonist component is 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline tartrate.

17. The method of claim 16, wherein the first composition comprises 0.1% (w/v) 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline tartrate.

18. The method of claim 16, wherein the first composition comprises 0.15% (w/v) 5-bromo-6-(2-imidozolin-2-ylamino) quinoxaline tartrate.

19. The method of claim 14, wherein the polyanionic solubility enhancing component is selected from the group consisting of carboxymethyl cellulose and polyvinyl alcohol.

20. The method of claim 14, wherein administering the first composition lowers intraocular pressure as effectively as administering a second composition comprising 0.2% (w/v) 5-bromo-6-(2-imidozolin-2-ylamino)quinoxaline tartrate.

21. The method of claim 20, wherein the first composition is administered three times daily.

22. The method of claim 20, wherein administering the first composition results in a lower incidence of one or more side effects as compared to the second composition.

23. The method of claim 22, wherein the one or more side effects are selected from the group consisting of oral dryness, asthenia, eye pruritis, allergic conjunctivitis, conjunctival hyperemia, and eye discharge.

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