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|Title:||Nonirritating aqueous ophthalmic compositions comfort formulation for ocular therapeutic agents|
|Abstract:||Xanthine derivatives are described which decrease the stinging associated with the application of ophthalmic acidic anti-inflammatory agents.|
|Inventor(s):||Han; Wesley W. (Mansfield, TX), Roehrs; Robert E. (Fort Worth, TX)|
|Assignee:||Alcon Laboratories, Inc. (Fort Worth, TX)|
1. An aqueous, nonirritating, nonsteroidal, ophthalmic composition for topical application to the eye comprising:
a therapeutically effective amount of suprofen for topical treatment of inflammation of the eye, and pharmaceutically acceptable salts thereof;
a xanthine derivative being present in an amount between the amount of derivative soluble in the water of said composition and 0.05% by weight/volume of said composition which is effective to reduce the discomfort associated with suprofen upon topical application of said composition, said xanthine derivative being selected from the group consisting of theophylline, caffeine, theobromine and mixtures thereof;
an ophthalmic preservative; and
a buffer, to provide an isotonic, aqueous, nonirritating nonsteroidal ophthalmic composition.
2. An aqueous, nonirritating, nonsteroidal, ophthalmic composition as recited in claim 1 wherein said xanthine derivative is caffeine.
3. An aqueous, nonirritating, nonsteroidal ophthalmic composition as recited in claim 2 wherein said suprofen comprises between about 0.5 to about 3.0 percent by weight/volume of said ophthalmic composition.
4. A method for reducing the stinging and discomfort associated with the topical application to the eye of an aqueous solution of a therapeutically effective amount of anti-inflammatory agent for topical treatment of inflammation of the eye, said agent selected from the group consisting of mefenamic acid, flufenamic acid, clonixin, flufenisal, 4-(t-butyl)benzeneacetic acid, ibufenac, ibuprofen, alclofenac, feneprofen, naproxen, indomethacin, tolmetin, flurbiprofen, ketoprofen, namoxyrate, suprofen, pharmaceutically acceptable salts of the foregoing acids and mixtures thereof, said method comprising adding to said aqueous solution an xanthine derivative in an amount between the amount of derivative soluble in the water of said composition and 0.05% by weight/volume of said composition which is effective to reduce the discomfort associated with said anti-inflammatory agent upon said topical application, said xanthine derivative having the formula ##STR2## where each of R.sub.1, R.sub.2 and R.sub.3 is selected from hydrogen, methyl and ethyl, and at least two of R.sub.1, R.sub.2 and R.sub.3 are selected from methyl and ethyl, and mixtures thereof forming a nonirritating ophthalmic composition.
5. A method as recited in claim 4 wherein said xanthine derivative is selected from the group consisting of theophylline, caffeine, theobromine and mixtures thereof.
6. A method as recited in claim 5 wherein said anti-inflammatory agent is suprofen and said xanthine derivative is caffeine.
7. A method as recited in claim 6 wherein said suprofen comprises between about 0.5 to about 3.0 percent by weight/volume of said ophthalmic composition.
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