STABILIZED OPHTHALMIC GALACTOMANNAN FORMULATIONS
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 a diol alcohol.
2 . A formulation according to claim 1 wherein said galactomannan is present at 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 %.
3 . 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 %.
4 . A formulation according to claim 1 wherein said galactomannan is selected from the group consisting of:
guar, hydroxylpropyl guar, and combinations thereof.
5 . A formulation according to claim 1 wherein said diol alcohol is selected from the group consisting of sorbitol, mannitol, polyethylene glycols, polypropylene glycols, glycerol and combinations thereof.
6 . A formulation according to claim 1 wherein said diol alcohol is sorbitol or mannitol.
7 . A formulation according to claim 6 wherein said diol alcohol is present at a concentration of about 0.5 w/v % to about 5.0 w/v %.
8 . A formulation according to claim 7 wherein said diol alcohol is present at a concentration of about 0.5 w/v % to about 2.0 w/v %.
9 . A formulation according to claim 1 further comprising a pharmaceutically acceptable salt of magnesium, calcium, zinc, or combinations thereof.
10 . A formulation according to claim 9 wherein said salt is magnesium chloride at a concentration of about 0.05 w/v % to about 0.25 w/v %.
11 . In an ophthalmic formulation comprising a galactomann and borate, the improvement comprising adding a diol alcohol to stabilize the viscosity of the formulation.
12 . A formulation according to claim 11 , said formulation further comprising a pharmaceutically acceptable salt of magnesium, calcium, zinc, or combinations thereof.
13 . A formulation according to claim 12 wherein the salt is magnesium chloride at a concentration of about 0.05 w/v % to about 0.25 w/v %.
14 . A method for lubricating the eye comprising administering to the eye a formulation of claim 1 .
15 . 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.
16 . A method for manufacturing a sterile ophthalmic formulation comprising:
preparing an ophthalmic formulation comprising galactomannan and borate;
adding a diol alcohol in a quantity sufficient to stabilize the viscosity of the formulation to form a stabilized ophthalmic formulation; and
sterilizing the stabilized ophthalmic formulation.
17 . A method according to claim 16 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 %.
18 . A method according to claim 16 wherein said galactomannan is selected from the group consisting of:
guar, hydroxylpropyl guar, and combinations thereof.
19 . A method according to claim 16 wherein said diol alcohol is selected from the group consisting of sorbitol, mannitol, glycerol, polyethylene glycols, polypropylene glycols, and combinations thereof.
20 . A method according to claim 19 wherein said diol alcohol is sorbitol or mannitol.
21 . A method according to claim 16 , said formulation further comprising a pharmaceutically acceptable salt of magnesium, calcium, zinc, or combinations thereof.
22 . A method according to claim 21 wherein said salt is magnesium chloride at a concentration of about 0.05 w/v % to about 0.25 w/v %.