Compositions and Methods for Eye Whitening

• US 20140038973A1
• Filed: 10/03/2013
• Published: 02/06/2014
• Est. Priority Date: 12/17/2009
• Status: Active Grant

• Current Assignee: Eye Therapies, LLC
• Original Assignee: Eye Therapies, LLC
• Inventors: Horn, Gerald
• Granted Patent: US 9,259,425 B2
• Time in Patent Office: Days
• US Class Current: 514/249
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/198 Alpha-amino acids, e.g. alanine or edetic acid [EDTA] betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00
• CPC Class Codes: A61K 31/4168 having a nitrogen attached in position 2, e.g. clonidine
• CPC Class Codes: A61K 31/4174 Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
• CPC Class Codes: A61K 31/4178 not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
• CPC Class Codes: A61K 31/498 Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
• CPC Class Codes: A61K 33/14 Alkali metal chlorides; Alkaline earth metal chlorides
• CPC Class Codes: A61K 33/20 Elemental chlorine; Inorganic compounds releasing chlorine
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system

Abstract

The invention provides compositions and methods for whitening of eyes. The provided compositions and methods utilize low concentrations of selective α-2 adrenergic receptor agonists. The compositions preferably include brimonidine.

Claims

1. A method of increasing whiteness of an eye comprising administering to a subject in need thereof a composition comprising a selective α

-2 adrenergic receptor agonist having a binding affinity of 300 fold or greater for α

-2 over α

-1 adrenergic receptors, or a pharmaceutically acceptable salt thereof.

2. The method of claim 1, wherein said selective α

-2 adrenergic receptor agonist has a binding affinity of 500 fold or greater for α

-2 over α

-1 adrenergic receptor.

3. The method of claim 1, wherein said α

-2 adrenergic receptor agonist is present at a concentration from between about 0.001% to about 0.05% weight by volume.

4. The method of claim 1, wherein said α

-2 adrenergic receptor agonist is brimonidine at a concentration from between about 0.01% to about 0.025% weight by volume.

5. A method of reducing redness of an eye comprising administering to a subject in need thereof a composition comprising a selective α

-2 adrenergic receptor agonist having a binding affinity of 300 fold or greater for α

-2 over α

-1 adrenergic receptors, or a pharmaceutically acceptable salt thereof.

6. The method of claim 5, wherein said selective α

-2 adrenergic receptor agonist has a binding affinity of 500 fold or greater for α

-2 over α

-1 adrenergic receptor.

7. The method of claim 5, wherein said α

-2 adrenergic receptor agonist is present at a concentration from between about 0.001% to about 0.05% weight by volume.

8. The method of claim 5, wherein said α

-2 adrenergic receptor agonist is brimonidine at a concentration from between about 0.01% to about 0.025% weight by volume.

9. A method of reducing redness of an eye while simultaneously increasing whiteness of the eye comprising administering to a subject in need thereof a composition comprising a selective α

-2 adrenergic receptor agonist having a binding affinity of 300 fold or greater for α

-2 over α

-1 adrenergic receptors, or a pharmaceutically acceptable salt thereof.

10. The method of claim 9, wherein said selective α

-2 adrenergic receptor agonist has a binding affinity of 500 fold or greater for α

-2 over α

-1 adrenergic receptor.

11. The method of claim 9, wherein said α

-2 adrenergic receptor agonist is present at a concentration from between about 0.001% to about 0.05% weight by volume.

12. The method of claim 9, wherein said α

-2 adrenergic receptor agonist is brimonidine at a concentration from between about 0.01% to about 0.025% weight by volume.