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Details for Patent: 6,486,138

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Details for Patent: 6,486,138

Title: Ophthalmic compositions containing galactomannan polymers and borate
Abstract:The present invention is directed to ophthalmic compositions containing a gelling amount of a combination of galactomannan polysaccharides and borates. The compositions gel or partially gel upon administration to the eye. The present invention also discloses methods of topical ophthalmic administration of the compositions to the eye.
Inventor(s): Asgharian; Bahram (Arlington, TX), Cagle; Gerald (Fort Worth, TX), Shah; Mandar V. (Forth Worth, TX), Markwardt; Kerry L. (Mansfield, TX)
Assignee: Alcon Manufacturing, Ltd. (Fort Worth, TX)
Filing Date:Nov 23, 1999
Application Number:09/447,146
Claims:1. A liquid anesthetic composition for topical application to the eye, comprising an effective amount of an ophthalmically acceptable anesthetic drug, 0.1 to 5% (w/v) of a galactomannan selected from the group consisting of guar or a derivative thereof, 0.05 to 5.0% (w/v) of a borate compound and water, said liquid composition having a pH such that the composition thickens to form a gel or partial gel when one or more drops of the liquid composition are topically administered to the eye.

2. A liquid anesthetic composition according to claim 1, wherein the composition has a slightly acidic to neutral pH.

3. A liquid anesthetic composition according to claim 1, wherein the borate compound is selected from the group consisting of boric acid, sodium borate, potassium borate and combinations thereof.

4. A liquid anesthetic composition according to claim 3, wherein the composition contains hydroxypropyl guar.

5. A liquid anesthetic composition according to claim 4, wherein the hydroxypropyl guar has a molar substitution of less than 0.6.

6. A liquid anesthetic composition according to claim 4, wherein the borate compound comprises boric acid.

7. A liquid anesthetic composition according to claim 6, wherein the composition comprises hydroxypropyl guar in a concentration of 0.2 to 2.0% (w/v) and boric acid in a concentration of 0.1 to 2.0% (w/v).

8. A liquid anesthetic composition according to any one of claims 1-7, wherein the composition has a pH of 6.0 to 7.0.

9. A liquid anesthetic composition according to any one of claims 1-7, wherein the ophthalmically acceptable anesthetic drug is selected from the group consisting of proparacaine, lidocaine, cocaine, oxybuprocaine, benoxinate, butacaine, mepivacaine, etidocaine, dibucaine, bupivacaine, levobupivacaine, tetracaine and procaine.

10. A liquid anesthetic composition according to claim 9, wherein the ophthalmically acceptable anesthetic drug is selected from the group consisting of levobupivacaine, proparacaine and tetracaine.

11. A liquid anesthetic composition according to claim 9, wherein the composition has a pH of 6 to 7.

12. A method of administering an ophthalmically acceptable anesthetic drug to the eye, which comprises topically applying to the eye a therapeutically effective amount of a liquid anesthetic composition comprising an effective amount of an ophthalmically acceptable anesthetic drug, 0.1 to 5% (w/v) of a galactomannan selected from the group consisting of guar or a derivative thereof, 0.05 to 5.0% (w/v) of a borate compound and water, said liquid composition having a pH such that the composition thickens to form a gel or partial gel when one or more drops of the liquid composition are topically applied to the eye.

13. A method according to claim 12, wherein the composition has a slightly acidic to neutral pH.

14. A method according to claim 13, wherein the borate compound is selected from the group consisting of boric acid, sodium borate, potassium borate and combinations thereof.

15. A method according to claim 14, wherein the composition contains hydroxypropyl guar.

16. A method according to claim 15, wherein the hydroxypropyl guar has a molar substitution of less than 0.6.

17. A method according to claim 16, wherein the borate compound comprises boric acid.

18. A method according to claim 17, wherein the composition comprises hydroxypropyl guar in a concentration of 0.2 to 2.0% (w/v) and boric acid in a concentration of 0.1 to 2.0% (w/v).

19. A method according to any one of claims 12-18, wherein the composition has a pH of 6.0 to 7.0.

20. A method according to any one of claims 12-18, wherein the ophthalmically acceptable anesthetic drug is selected from the group consisting of proparacaine, lidocaine, cocaine, oxybuprocaine, benoxinate, butacaine, mepivacaine, etidocaine, dibucaine, bupivacaine, levobupivacaine, tetracaine and procaine.

21. A method according to claim 20, wherein the ophthalmically acceptable anesthetic drug is selected from the group consisting of levobupivacaine, proparacaine and tetracaine.

22. A method according to claim 20, wherein the composition has a pH of 6 to 7.
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