Claims
- 1. An ophthalmic composition comprising an aqueous medium containing an effective amount of a non-steroidal anti-inflammatory agent, wherein at least about 80 mol. % of said agent is in the form of a precipitate, and at least about 0.5 mole equivalents of a pharmacologically acceptable divalent cation per mole of said non-steroidal anti-inflammatory agent precipitate; said aqueous medium having a pH in the range of from 4.0 to 6.7.
- 2. The composition according to claim 1, wherein said non-steroidal anti-inflammatory agent is selected from the group consisting of diclofenac, suprofen, and flurbiprofen.
- 3. The composition according to claim 2, wherein said non-steroidal anti-inflammatory agent is diclofenac.
- 4. The composition according to claim 1, wherein said pharmacologically acceptable divalent cation is a Group IIA metal.
- 5. The composition according to claim 4, wherein said Group IIA divalent metal cation is calcium or magnesium.
- 6. The composition according to claim 1, wherein said precipitate is in a free-acid form.
- 7. The composition according to claim 6, wherein said divalent cation is present as a solute in said aqueous medium.
- 8. The composition according to claim 7, wherein said divalent cation is present from 1 to 5 times the stoichiometric amount equivalent to the molar amount of said non-steroidal anti-inflammatory agent precipitate.
- 9. The composition according to claim 8, wherein 85 to 95% of said non-steroidal anti-inflammatory agent is in said precipitate form.
- 10. The composition according to claim 9, wherein said NSAI agent is diclofenac and said divalent cation is Mg++.
- 11. The composition according to claim 1, further comprising a polymer.
- 12. The composition according to claim 11, wherein said polymer is water insoluble and water swellable.
- 13. The composition according to claim 12, wherein said polymer is a crosslinked carboxy-containing polymer.
- 14. The composition according to claim 13, wherein said polymer is a polycarbophil.
- 15. The composition according to claim 13, wherein said polymer is a Carbopol.
- 16. The composition according to claim 15, wherein said polymer is Carbopol 974P
- 17. The composition according to claim 13, further comprising EDTA.
- 18. The composition according to claim 1, wherein said aqueous medium has a pH of from 4.0 to 6.5.
- 19. The composition according to claim 1, wherein said non-steroidal anti-inflammatory agent is contained in an amount of from 0.01 to 5.0% by weight of the entire composition.
- 20. The composition according to claim 1, further comprising a perborate salt.
- 21. A method for treating an eye, which comprises administering to an eye in need thereof an effective amount of the composition according to claim 1.
- 22. A method for making the composition according to claim 1, which comprises:
combining a non-steroidal anti-inflammatory agent and a divalent cation source in an aqueous medium to form a precipitate-containing solution.
- 23. The method according to claim 22, wherein said non-steroidal anti-inflammatory agent is added to an aqueous solution containing a polymer dispersed therein and said divalent cation source.
- 24. The method according to claim 23, wherein said aqueous solution further comprises EDTA and said dispersed polymer is a water insoluble, water-swellable crosslinked carboxy-containing polymer.
- 25. The method according to claim 24, wherein said non-steroidal anti-inflammatory agent comprises diclofenac and said divalent cation source is CaCl2 MgCl2 or MgSO4.
- 26. An ophthalmic composition obtained by combining at least (1) sodium diclofenac, (2) a divalent metal salt, (3) a water insoluble, water-swellable polymer, and (4) water.
- 27. The composition according to claim 26, which further comprises EDTA and wherein said divalent metal salt is CaCl2, MgCl2 or MgSO4.
- 28. The composition according to claim 26, wherein said sodium diclofenac is added to an aqueous suspension comprising said divalent metal salt, said water-swellable polymer and said water.
- 29. The composition according to claim 1, further comprising benzalkonium chloride.
- 30. An ophthalmic composition comprising an aqueous suspension of a crosslinked carboxyl-containing polymer, solid diclofenac in free-acid form, dissolved diclofenac, and dissolved Mg++ or Ca++ cations in an amount of from about 1 to 5 times the stoichiometric equivalent amount per mole of said solid diclofenac; said composition having a pH of from about 4.0 to about 6.7 and the total amount of diclofenac being a pharmaceutically effective amount and said solid diclofenac comprising 85 to 95 mol % of the total amount of diclofenac.
- 31. The composition according to claim 30, further comprising 0.03 to 0.3 wt. % sodium perborate, 0.003 to 0.03 wt. % polyphosphonic acid peroxy stabilizer and 0.01 to 0.1 wt. % EDTA.
- 32. The composition according to claim 31, wherein said sodium perborate is contained in an amount of about 0.28 wt. % and said polyphosphonic acid peroxy stabilizer is diethylene triamine penta(methylene-phosphonic acid).
- 33. A preserved ophthalmic composition comprising water, about 0.01 to 0.5 wt. % of a perborate salt, about 0.001 to 0.06 wt. % of a polyphosphonic acid peroxy stabilizer, and about 0.01 to 0.1 wt. % of ethylenediaminetetraacetic acid.
- 34. The composition according to claim 33, wherein said water is sterile water, said perborate is sodium perborate contained in an amount of from 0.03 to 0.3 wt. %, and said polyphosphonic acid peroxy stabilizer is a compound of formula I or II:
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Parent Case Info
[0001] This application is a Continuation-in-Part of prior co-pending application Ser. No. 08/863,015, filed May 23, 1997, the entire contents of which are incorporated herein by reference.
Continuations (1)
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Number |
Date |
Country |
Parent |
09074419 |
May 1998 |
US |
Child |
09863294 |
May 2001 |
US |
Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
08863015 |
May 1997 |
US |
Child |
09074419 |
May 1998 |
US |