Composition for treating ocular effects of diabetes

摘要

The composition for treating ocular effects of diabetes is a composition that contains an aldose reductase inhibitor in an ophthalmic gel for topical application to the eye. The composition includes a carrier having, by weight, about 0.4% carbomer, 4.0% sorbitol, 0.01% centrimide, 0.01% ethylenediaminetetraacetic acid (EDTA) and effective amounts of sodium chloride and sodium hydroxide for adjusting the pH of the topical carrier to about 7 and to achieve a desired viscosity, with the balance being water. The aldose reductase inhibitor (ARI) is mixed with the topical carrier at about 0.1%-6% by weight of the composition to form an ophthalmic gel. Preferably, the ARI is 2R,4S-6-fluoro-2-methyl-spiro[chroman-4,4′-imidazolidine]-2′,5′-dione, referred to as 2-methyl sorbinil, having the structure:;
or a pharmaceutically acceptable salt thereof. In use, the ophthalmic gel is preferably applied as an eye drop at a dosage of one drop per eye administered two to three times daily.

主权项

1. A composition for treating ocular effects of diabetes, comprising:
a topical carrier having by weight about 0.4% carbomer, 4.0% sorbitol, 0.01% cetrimide, and 0.01% ethylenediaminetetraacetic acid, the balance being water; and an aldose reductase inhibitor mixed with the topical carrier to form an ophthalmic gel, wherein the topical carrier has a viscosity of about 1,928 cps prior to admixture with the aldose reductase inhibitor, and wherein the aldose reductase inhibitor has a standardized particle size of less than 10 microns.