Topical treatment of ocular hypertension, glaucoma, ischemic retinopathy and age-related macular degeneration with ophthalmic formulation of dopamine antagonists
OwnerGeorge C.Y. Chiouinventor
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OwnerGeorge C.Y. Chiouinventor
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This invention provides ocular formulations comprising an ocular drug and a carboxylic acid in an amount sufficient to maintain the pH of the formulation from about 4.5 to about 7.5. The ocular drug may be a dopamine antagonist and the acid may be lactic acid, citric acid or tartaric acid. In some aspects, the pH of the formulation is about 5.5 The ocular formulations of this invention provide enhanced bioavailability which results in increased drug concentrations across the cornea and in the eye ball, i.e., aqueous humor and intraocular organs and chambers. Moreover, the present formulations are non-irritating when applied topically and have a shelf-life of at least fourteen days at 25° C. Methods are also provided to increase ocular blood flow by using present ocular formulations comprising dopamine antagonists or other drugs for the prevention and treatment of ocular hypertension, glaucoma, ischemic retinopathy and age-related macular degeneration (AMD).
A formulation for ocular delivery comprising an ocular drug and a carboxylic acid in an amount sufficient to maintain the pH of the formulation from about 4.5 to about 7.5.
16 The formulation of claim 15, wherein the hydroxydicarboxylic acid is selected from the group consisting of tartronic acid, malic acid, tartaric acid, arabiraric acid, ribaric acid, xylaric acid, lyxaric acid, saccharic acid, mucic acid, mannaric acid, gularic acid, allaric acid, altraric acid, idaric acid and talaric acid.
A formulation for ocular delivery comprising a dopamine antagonist, a carboxylic acid in an amount sufficient to maintain the pH of the formulation from about 4.5 to about 7.5, wherein the dopamine antagonist is metoclopromide, loxapine, or droperidol, and the acid is tartaric acid, lactic acid or citric acid and the pH of the formulation is about 5.5.
A method to increase blood flow to the retina or choroid, to reduce intraocular pressure, or to treat or prevent visual deterioration associated with decreased retinal or choroidal blood flow or increased intraocular pressure, which method comprises ocularly administering a formulation comprising a therapeutically effective amount of a dopamine antagonist and a carboxylic acid in an amount sufficient to maintain the pH of the formulation from about 4.5 to about 7.5 to a subject having decreased retinal or choroidal blood flow or increased intraocular pressure.
Dependencies are inferred from the claim text.