Claims for Patent: 5,034,230

Summary for Patent: 5,034,230

Title:	Anti-allergic ophthalmics
Abstract:	This invention relates to low irritative ophthalmics containing the compound of the formula or salts thereof which are useful for treatment of anti-allergic eye diseases such as allergic conjunctivitis ##STR1##
Inventor(s):	Morita; Takakazu (Toyonaka, JP), Iso; Tadashi (Kawachinagano, JP), Kawashima; Youichi (Kyoto, JP), Hikida; Mitsushi (Takatsuki, JP)
Assignee:	Santen Pharmaceutical Co., Ltd. (Osaka, JP)
Application Number:	07/392,922
Patent Claims:	1. An anti-allergic ophthalmic solution comprising a potassium salt of a compound of the formula (I) ##STR4## in a concentration from 0.01 to 1% and at least one buffer selected from the group consisting of disodium hydrogen phosphate, sodium dihydrogen phosphate, boric acid and sodium borate, either alone or in admixture with one or more pharmaceutically acceptable excipients. 2. An anti-allergic ophthalmic solution comprising a potassium salt of a compound of the formula (I) ##STR5## disodium hydrogen phosphate, sodium dihydrogen phosphate and optionally one or more pharmaceutically acceptable excipients, wherein the concentrations of the potassium salt of the compound of the formula (I), the disodium hydrogen phosphate and the sodium dihydrogen phosphate are 0.01 to 1%, 0.1 to 2% and 0.002 to 1%, respectively. 3. An anti-allergic ophthalmic solution comprising a potassium salt of a compound of the formula (I) ##STR6## disodium hydrogen phosphate, potassium dihydrogen phosphate and optionally one or more pharmaceutically acceptable excipients, wherein the concentrations of the potassium salt of the compound of the formula (I), the disodium hydrogen phosphate, and the potassium dihydrogen phosphate are 0.01 to 1%, 0.1 to 1% and 0.002 to 0.7%, respectively. 4. An anti-allergic ophthalmic solution comprising a potassium salt of a compound of the formula (I) ##STR7## boric acid, sodium borate and optionally one or more pharmaceutically acceptable excipients, wherein the concentrations of the potassium salt of the compound of the formula (I), the boric acid and the sodium borate are 0.01 to 1%, 0.3 to 2% and 0.3 to 1%, respectively. 5. An anti-allergic ophthalmic solution comprising a potassium salt of a compound of the formula (I) ##STR8## boric acid, monoethanolamine and optionally one or more pharmaceutically acceptable excipients, wherein the concentrations of the potassium salt of the compound of the formula (I), the boric acid and the monoethanolamine are 0.01 to 1%, 0.3 to 2% and 0.1 to 1%, respectively. 6. The anti-allergic ophthalmic solution according to claim 1, wherein the solution is in a dosage form and the dosage form comprises sterile aqueous eyedrops. 7. An anti-allergic ophthalmic solution prepared by dissolving a potassium salt of the compound of formula (I) ##STR9## to provide said salt in a concentration from 0.01 to 1%, in sterile water containing disodium hydrogen phosphate, sodium dihydrogen phosphate and optionally one or more pharmaceutically acceptable excipients, wherein the concentrations of the disodium hydrogen phosphate and the sodium dihydrogen phosphate are 0.1 to 2% and 0.002 to 1%, respectively. 8. An anti-allergic ophthalmic solution prepared by dissolving a potassium salt of the compound of the formula (I) ##STR10## to provide said salt in a concentration from 0.01 to 1%, in sterile water containing disodium hydrogen phosphate, potassium dihydrogen phosphate and optionally one or more pharmaceutically acceptable excipients, wherein the concentrations of the disodium hydrogen phosphate and the potassium dihydrogen phosphate are 0.1 to 1% and 0.002 to 0.7%, respectively. 9. An anti-allergic ophthalmic solution prepared by dissolving a potassium salt of the compound of the formula (I), ##STR11## to provide salt in a concentration from 0.1 to 1%, in sterile water containing boric acid, sodium borate and optionally one or more pharmaceutically acceptable excipients, wherein the concentrations of the boric acid and the sodium borate are 0.3 to 2% and 0.3 to 1%, respectively. 10. An anti-allergic ophthalmic solution prepared by dissolving a potassium salt of the compound of the formula (I) ##STR12## to provide said salt in a concentration from 0.01 to 1%, in a sterile water containing boric acid, monoethanolamine and optionally one or more pharmaceutically acceptable excipients, wherein the concentrations of the boric acid and the monoethanolamine are 0.3 to 2% and 0.1 to 1%, respectively. 11. A method of treatment of allergic eye diseases which comprises administering to a patient the anti-allergic ophthalmic solution according to claim 1 in an amount effective to treat an allergic eye disease. 12. The method according to claim 11, wherein the solution is topically administered to the eye of the patient in a dosage form and the dosage form comprises sterile aqueous eye drops. 13. A method of treatment of allergic eye diseases which comprises administering to a patient the anti-allergic ophthalmic solution according to claim 2 in an amount effective to treat an allergic eye disease. 14. A method of treatment of allergic eye diseases which comprises administering to a patient the anti-allergic ophthalmic solution according to claim 3 in an amount effective to treat an allergic eye disease. 15. A method of treatment of allergic eye diseases which comprises administering to a patient the anti-allergic ophthalmic solution according to claim 4 in an amount effective to treat an allergic eye disease. 16. A method of treatment of allergic eye diseases which comprises administering to a patient the anti-allergic ophthalmic solution according to claim 5 in an amount effective to treat an allergic eye disease. 17. The anti-allergic ophthalmic solution according to claim 1, wherein the concentration of the potassium salt of the compound of the formula (I) is about 0.1 to 1%. 18. The anti-allergic ophthalmic solution according to claim 2, wherein the concentration of the potassium salt of the compound of the formula (I) is about 0.1 to 1%. 19. The anti-allergic ophthalmic solution according to claim 3, wherein the concentration of the potassium salt of the compound of the formula (I) is about 0.1 to 1%. 20. The anti-allergic ophthalmic solution according to claim 4, wherein the concentration of the potassium salt of the compound of the formula (I) is about 0.1 to 1%. 21. The anti-allergic ophthalmic solution according to claim 5, wherein the concentration of the potassium salt of the compound of the formula (I) is about 0.1 to 1%. 22. A method of treatment of an allergic eye disease which comprises topically administering to a patient the anti-allergic ophthalmic solution according to claim 17 in an amount effective to treat an allergic eye disease.