Ophthalmic composition
View Patent ↗The present invention relates to ophthalmic compositions for treatment of conditions in the eye. More specifically, the present invention relates to ophthalmic compositions comprising a polyquaternium compound and an anionic polymer. Methods for reducing and/or preventing the incompatibility of polyquaternium compounds with anionic polymers are also disclosed.
1. An eye care composition comprising:
a. from about 10 ppm to about 1000 ppm of a polyquaternium compound having a weight average molecular weight of from about 150 to about 15,000 Daltons;
b. from about 0.001% to about 0.5% of an anionic polymer having a weight average molecular weight of from about 250 to about 4,000,000 Daltons; and
c. an effective amount of an organic acid, salts thereof or mixtures thereof, to achieve complete association of the organic acid with the polyquaternium compound such that the organic acid binds with the polyquaternium compound at at least a 1:1 molar ratio;
wherein the composition is substantially free of cationic oligomer compounds and precipitation inhibiting compounds and wherein the composition is in the form of an eye-drop solution, an eye wash solution, or a solution, spray or mist for lubricating or rewetting a contact lens.
2. The composition of claim 1 wherein the polyquaternium compound has weight average molecular weight of from about 200 to about 13,500 Daltons.
3. The composition of claim 2 wherein the polyquaternium compound is selected from the group consisting of polyquatemium-1, polyquaternium-10, polyquaternium-42 or mixtures thereof.
4. The composition of claim 3 wherein the polyquaternium compound is polyquaternium-42.
5. The compositions of claim 1 wherein the anionic polymer has a weight average molecular weight of from about from about 100,000 to about 3,000,000 Daltons.
6. The composition of claim 5 wherein the anionic polymer is selected from the group consisting of alginates; carageenans; carbomers, high molecular weight, non-linear polyacrylic acid cross-linked with polyalkenyl polyethers; sodium carboxymethylcellulose; internally cross-linked sodium carboxymethylcelluloses; gellan gum; hyaluronic acid; pectin; xanthan gum; alkylvinyl ether/maleic anhydride copolymer; and mixtures of thereof.
7. The composition of claim 6 wherein the anionic polymer is selected from the group consisting of hyaluronic acid, gellan gum, alkylvinyl ether/maleic anhydride copolymer and mixtures thereof.
8. The composition of claim 7 wherein the anionic polymer is hyaluronic acid.
9. The composition of claim 7 wherein the anionic polymer is gellan gum.
10. The composition of claim 7 wherein the anionic polymer is an alkyl vinyl ether/maleic anhydride copolymer.
11. The composition of claim 10 wherein the anionic polymer is a free acid of alkyl vinyl ether/maleic anhydride copolymer.
12. The composition of claim 1 wherein the organic acid is selected from the group consisting of carboxylic acids, dicarboxylic acids, tricarboxylic acids and mixtures thereof.
13. The composition of claim 12 wherein the organic acid is a carboxylic acid.
14. The composition of claim 13 wherein the carboxylic acid is selected from the group consisting of formic acid, acetic acid, propionic acid, salts thereof, and mixtures thereof.
15. The composition of claim 12 wherein the organic acid is a dicarboxylic acid.
16. The composition of claim 15 wherein the dicarboxylic acid is selected from the group consisting of glutaric acid, maleic acid, tartaric acid, salts thereof, and mixtures thereof.
17. The composition of claim 16 wherein the dicarboxylic acid is tartaric acid.
18. The composition of claim 12 wherein the organic acid is a tricarboxylic acid.
19. The composition of claim 18 wherein the tricarboxylic acid is selected from the group consisting of citric acid, isocitric acid, aconitic acid, trimesic acid, propane-1,2,3-tricarboxylic acid and mixtures thereof.
20. The composition of claim 19 wherein the tricarboxylic acid is citric acid.
21. A method of reducing the precipitation of a polyquaternium compound and an anionic polymer in an eye composition comprising such compounds, comprising the steps of:
i) providing from about 0.001% to about 0.5% of an anionic polymer having a weight average molecular weight of from about 250 to about 4,000,000 Daltons;
ii) adding an effective amount of an organic acid, salts thereof or mixtures thereof, to achieve complete association of the organic acid with the polyquaternium compound such that the organic acid binds with the polyquaternium compound at at least a 1:1 molar ratio; and
iii) adding from about 10 ppm to about 1000 ppm of a polyquaternium compound having a weight average molecular weight of from about 150 to about 15,000 Daltons;
wherein the composition is substantially free of cationic oligomer compounds and precipitation inhibiting compounds and wherein the composition is in the form of an eye-drop solution, an eye wash solution, or a solution, spray or mist for lubricating or rewetting a contact lens.