Stabilized ophthalmic galactomannan formulations
View Patent ↗The present invention relates to viscosity stabilized ophthalmic formulations and ophthalmic formulations suitable for drug delivery. The formulations comprise galactomannans such as guar or hydroxypropyl guar and a borate source such as boric acid. The formulations further comprise a diol alcohol such as sorbitol and, optionally, a pharmaceutically acceptable divalent cation salt such as magnesium chloride.
1. A viscosity-stabilized ophthalmic formulation comprising a galactomannan, borate and sorbitol, and wherein said galactomannan is guar or hydroxypropylguar, and wherein the said galactomannan is present in a concentration of about 0.1 w/v % to about 2.0 w/v % and said borate is present at a concentration of about 0.2 w/v % to about 2.0 w/v % and said sorbitol is present at a concentration of about 0.5% w/v % to about 5.0 w/v %.
2. A formulation according to claim 1 wherein said galactomannan is present at a concentration of about 0.05 w/v % to about 0.5 w/v % and said borate is present at a concentration of about 0.1 w/v % to about 1.5 w/v %.
3. A formulation according to claim 1 wherein said sorbitol is present at a concentration of about 0.5 w/v % to about 2.0 w/v %.
4. A formulation according to claim 1 further comprising a pharmaceutically acceptable salt of magnesium, calcium, zinc, or combinations thereof.
5. A formulation according to claim 4 wherein said salt is magnesium chloride at a concentration of about 0.05 w/v % to about 0.25 w/v %.
6. In an ophthalmic formulation comprising a galactomannan and borate, the improvement comprising adding sorbitol to stabilize the viscosity of the formulation, and wherein the said galactomannan is present in a concentration of about 0.1 w/v % to about 2.0 w/v % and said borate is present at a concentration of about 0.2 w/v % to about 2.0 w/v % and said sorbitol is present at a concentration of about 0.5% w/v % to about 5.0 w/v %.
7. A formulation according to claim 6 , said formulation further comprising a pharmaceutically acceptable salt of magnesium, calcium, zinc, or combinations thereof.
8. A formulation according to claim 7 wherein the salt is magnesium chloride at a concentration of about 0.05 w/v % to about 0.25 w/v %.
9. A method for lubricating the eye comprising administering to the eye a formulation of claim 1 .
10. A method for delivering a pharmaceutically active agent to the eye comprising:
administering to the eye a formulation of claim 1 further comprising a pharmaceutically active agent.
11. A method for manufacturing a sterile ophthalmic formulation comprising:
preparing an ophthalmic formulation comprising galactomannan and borate, wherein the said galactomannan is present in a concentration of about 0.1 w/v % to about 2.0 w/v % and said borate is present at a concentration of about 0.2 w/v % to about 2.0 w/v %;
adding sorbitol at a concentration of about 0.5% w/v % to about 5.0 w/v % to stabilize the viscosity of the formulation to form a stabilized ophthalmic formulation; and sterilizing the stabilized ophthalmic formulation.
12. A method according to claim 11 wherein said galactomannan is present at a concentration of about 0.05 w/v % to about 0.5 w/v % and said borate is present at a concentration of about 0.7 w/v %.
13. A method according to claim 11 wherein said galactomannan is selected from the group consisting of:
guar, hydroxylpropyl guar, and combinations thereof.
14. A method according to claim 11 , said formulation further comprising a pharmaceutically acceptable salt of magnesium, calcium, zinc, or combinations thereof.
15. A method according to claim 14 wherein said salt is magnesium chloride at a concentration of about 0.05 w/v % to about 0.25 w/v %.