IP Library Granted Patent US 7,795,203
Granted Patent B2
US 7,795,203 · App. 10/480,724 · Granted Sep 14, 2010

Method for topical treatment of eye disease and composition and device for said treatment

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Quick Facts
Patent No.
US 7,795,203
App. No.
10/480,724
Granted
Sep 14, 2010
Kind
B2
Abstract

A method for the prevention or treatment of an eye disease, which includes topically applying to a patient in need of the treatment an aqueous ophthalmic composition which includes N-acetylcarnosine, a N-acetylcarnosine derivative or a pharmacologically acceptable salt of N-acetylcarnosine, in combination with an amount of a cellulose compound or a pharmacologically acceptable salt which is effective to increase intraocular absorption of N-acetylcarnosine or L-carnosine or a derivative of L-carnosine, such as anserine or balenine, in the aqueous humor. A hydrophilic hydrogel contact lens and an ocular polymer insert for topical application of an ophthalmic composition to the eyes of a patient is also disclosed, with the lens or insert containing N-acetylcarnosine, a N-acetylcarnosine derivative or a pharmacologically acceptable salt of N-acetylcarnosine.

Claims (93)

1. A method for the treatment of an eye disease, comprising

topically applying to a mammal in need of said treatment an aqueous ophthalmic composition comprising N-acetylcarnosine, a N-acetylcarnosine derivative or a pharmacologically acceptable salt of N-acetylcarnosine, in combination with carboxymethylcellulose or its pharmacologically acceptable salt, in an amount effective to increase intraocular absorption of L-carnosine or a L-carnosine derivative into the aqueous humor,

wherein said N-acetylcarnosine is present in an amount ranging from 0.5% to 2% by weight of the composition.

2. The method of claim 1 , wherein a pharmacologically acceptable salt of said cellulose compound is carboxymethylcellulose sodium salt.

3. The method of claim 1 , wherein said aqueous ophthalmic composition comprises at least one preservative selected from the group consisting of benzyl alcohol and para-amino-benzoic acid.

4. The method of claim 1 , wherein said aqueous ophthalmic composition comprises at least one polyoxyethylene fatty acid ester.

5. The method of claim 4 , wherein said polyoxyethylene fatty acid ester is a member selected from the group consisting of polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monostearate, polyoxyethylene sorbitan monooleate and polyoxyethylene sorbitan tristearate.

6. The method of claim 1 , wherein said aqueous ophthalmic composition comprises at least one vitamin compound selected from the group consisting of vitamin A and vitamin E.

7. The method of claim 1 , wherein said aqueous ophthalmic composition comprises glycerine in an amount effective to prevent excessive corneal hydration (oedema) or ocular irritation.

8. The method of claim 1 , wherein said cellulose compound is carboxymethylcellulose, present in an amount ranging from 0.2% to 0.4% by weight of the composition.

9. The method of claim 1 , wherein said aqueous ophthalmic composition comprises at least one buffer in an amount effective to maintain a pH of said composition in a range of from 6.0 to 6.8.

10. The method of claim 9 , wherein said pH ranges from 6.3 to 6.8.

11. The method of claim 9 , wherein said aqueous ophthalmic composition comprises sodium or potassium borate in combination with sodium or potassium bicarbonate.

12. The method of claim 1 , wherein said eye disease is a member selected from the group consisting of cataract, open-angle primary glaucoma, corneal disorders, presbyopia, computer vision syndrome, eye strain, ocular inflammation, blurred vision, dry eye syndrome, retinal diseases, vitreous opacities and lesions, and complications of diabetes mellitus and systemic disorders.

13. The method of claim 1 , wherein said mammal is selected from the group consisting of humans, canines, cats, rabbits and equines.

14. The method of claim 1 , wherein said aqueous ophthalmic composition comprises Formulation No. 1:

Deionized Water

970

grams,

Glycerine,

13

grams,

N-acetylcarnosine,

10

grams,

Carboxymethylcellulose,

3

grams,

Benzyl Alcohol,

3

grams,

Potassium Borate

7.9

grams or the amount necessary to adjust

the pH to 6.3-6.5,

Potassium Bicarbonate

3.4

grams or the amount necessary to adjust

the pH to 6.3-6.5.

15. The method of claim 1 , wherein said aqueous ophthalmic composition comprises Formulation No. 2:

Deionized Water

970

grams,

Glycerine,

13

grams,

N-acetylcarnosine,

10

grams,

Carboxymethylcellulose,

3

grams,

Phenyl-ethyl Alcohol,

3

grams,

Sodium Borate

7.9

grams or the amount necessary to adjust

the pH to 6.3-6.5,

Sodium Bicarbonate

3.4

grams or the amount necessary to adjust

the pH to 6.3-6.5.

16. The method of claim 1 , wherein said aqueous ophthalmic composition comprises Formulation No. 5:

Deionized Water

970

grams,

Glycerine,

13

grams,

N-acetylcarnosine,

10

grams,

Taurine,

40

grams,

p-aminobenzoic acid,

0.07

grams,

Carboxymethylcellulose,

3

grams,

Benzyl Alcohol,

3

grams,

Potassium Borate

7.9

grams or the amount necessary to adjust

the pH to 6.3-6.5,

Potassium Bicarbonate

3.4

grams or the amount necessary to adjust

the pH to 6.3-6.5.

Continuity (2)
Provisional Application 6041435700 · Sep 30, 2002
Related Publication 20040192647A1 · Sep 30, 2004