Polymeric artificial tear system
View Patent ↗The present invention relates to artificial tear 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 cis-diol such as sorbitol that interferes with the cross-linking of galactomannan and borate. Optionally, the formulations are substantially free of divalent cations.
1. An ophthalmic formulation comprising a galactomannan, borate, and a cis-diol, wherein said formulation is substantially free of divalent cations and wherein said galactomannan is present at a concentration of 0.16 w/v % to 0.19 w/v% and said borate is present at a concentration of 0.7 w/v %, and wherein said cis-diol is sorbitol at a concentration of 0.5 to 5.0 w/v %, and wherein said galactomannan is selected from the group consisting of guar, hydroxylpropyl guar, and combinations thereof.
2. A formulation according to claim 1 wherein said cis-diol is present at a concentration of 1.4 w/v %.
3. A formulation according to claim 1 wherein said borate is boric acid.
4. A formulation according to claim 1 further comprising a demulcent selected from the group consisting of:
glycerin, polyvinyl pyrrolidone, polyethylene oxide, polyethylene glycol, propylene glycol, polyacrylic acid, and combinations thereof.
5. A formulation according to claim 4 wherein said demulcent is polypropylene glycol or polyethylene glycol.
6. In an ophthalmic formulation comprising a galactomann and borate, the improvement comprising adding a cis-diol to prevent galactomann and borate cross-linking, thereby reducing the viscosity of the formulation, and wherein said cis-diol is sorbitol at a concentration of 0.5 to 5.0 w/v %.
7. A formulation according to claim 6 , said formulation further being substantially free of divalent cations, thereby reducing the viscosity of the formulation.
8. A method for lubricating the eye comprising administering to the eye a formulation of claim 1 .
9. 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.
10. An improved ophthalmic formulation comprising galactomannan and borate, said formulation comprising a cis-diol that is eliminated from tear film more rapidly than said galactomannan when the formulation is instilled in an eye and wherein said galactomannan is present at a concentration of 0.16 w/v % to 0.19 w/v % and said borate is present at a concentration of 0.7 w/v %, and wherein said cis-diol is sorbitol at a concentration of 0.5 to 5.0 w/v %, and wherein said galactomannan is selected from the group consisting of guar, hydroxylpropyl guar, and combinations thereof.
11. An improved ophthalmic formulation according to claim 10 , said formulation further being substantially free of divalent cations, thereby reducing the viscosity of the formulation.
12. An improved ophthalmic formulation according to claim 10 , said formulation further comprising a demulcent selected from the group consisting of:
glycerin, polyvinyl pyrrolidone, polyethylene oxide, polyethylene glycol, propylene glycol, polyacrylic acid, and combinations thereof.
13. An ophthalmic formulation according to claim 1 , said formulation having an osmolality of 220-320 mOsm/kg.