Ophthalmic pharmaceutical compositions and methods of making and using same

摘要

A stable ophthalmic pharmaceutical composition for relief, treatment, control, alleviation, or prevention of a pathological ocular condition of the eye comprises: (a) a first polymer, a viscosity of which changes with a change in a concentration of an electrolyte, such as a salt, when added to said first polymer; (b) a second polymer that is different from the first polymer and can modify the viscosity of the first polymer; and (c) an oil. In some embodiments, the composition further comprises a non-ionic surfactant. The composition can form a stable oil-in-water emulsion on storage, but separate into an oil phase and a water phase when applied in the eye. The emulsion can comprises an ophthalmic active pharmaceutical ingredient dissolved in the oil or water phase. The emulsion can provide enhanced stability to said active pharmaceutical ingredient.

主权项

1. An ophthalmic pharmaceutical composition comprising an oil-in-water emulsion that comprises: (a) a first polymer comprising a polymer or copolymer of carboxyvinyl monomers; the first polymer being present at a concentration in the range from about 0.01 to about 1 percent by weight of the composition; (b) a second polymer comprising a polyanionic polysaccharide selected from the group consisting of alginic acid, hyaluronic acid, salts of alginic acid or hyaluronic acid, and glucuronoxylomannan extracted from Tremella fuciformis mushroom; the second polymer being present at a concentration in the range from about 0.01 to about 1 percent by weight of the composition; (c) a caprylic acid/capric acid medium-chain triglyceride present at a concentration in the range from about 0.01 to about 1 percent by weight of the composition; (d) a non-ionic surfactant present at a concentration in the range from about 0.01 to about 1 percent by weight of the composition; and (e) water; wherein the emulsion is stable on storage but breaks up into separate aqueous and oil phases when diluted with simulated tear or subjected to shear stress; and wherein the composition has a viscosity in the range from about 2 to about 1000 cP.