Abstract: Dry, stabilized pharmaceutical spheres comprising a precisely measured amount of the pharmaceutical and a filler material that facilitates the immediate dissolution of the pharmaceutical upon contact with a solution are provided as well as methods for preparing same.

Abstract: 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).

Abstract: The invention relates to arginine and arginine-like compounds and to methods employing these compounds as ocular hypotensive agents. These compounds are effective when applied topically, may be used in low concentrations and are nontoxic. Additionally, the invention includes several new arginine derivatives with varying lipophilicities particularly suited for topical administration.

Abstract: A novel compound for the treatment and prevention of ocular and other types of inflammation is disclosed. The compound, OB-101, is effective at both the early and late phases of inflammation. The compound is useful for the treatment of inflammation in both the anterior and posterior portions of the eye, as well as in other parts of the body.

Abstract: Compositions and methods for systemic delivery of polypeptides through the eyes are disclosed. The compositions include a systemically active polypeptide at a concentration such that the composition is substantially isotonic with tear fluid. The compositions may include a permeation-enhancing agent to aid systemic absorption of higher molecular weight polypeptides, as well as peptidase inhibitors. Therapeutically effective amounts of the polypeptide compositions can be administered to the eyes where the drug passes into the nasolacrimal duct and becomes absorbed into circulation.

Abstract: Compositions and methods for systemic delivery of polypeptides through the eyes are disclosed. The compositions include a systemically active polypeptide at a concentration such that the composition is substantially isotonic with tear fluid. The compositions may include a permeation-enhancing agent to aid systemic absorption of higher molecular weight polypeptides, as well as peptidase inhibitors. Therapeutically effective amounts of the polypeptide compositions can be administered to the eyes where the drug passes into the nasolacrimal duct and becomes absorbed into circulation.

Abstract: The invention relates to a method for increasing blood flow to the retina and choroid in subjects with decreased retinal or choroidal blood flow. The method involves the topical administration of droperidol and is useful for the treatment of low pressure glaucoma and ischemic retinal degeneration.

Abstract: The invention relates to a method for increasing blood flow to the retina and choroid in subjects with decreased retinal or choroidal blood flow. The method involves the topical administration of metoclopramide and is useful for the treatment of low pressure glaucoma and ischemic retinal degeneration.

Abstract: The invention relates to a method for increasing blood flow to the retina and choroid in subjects with decreased retinal or choroidal blood flow. The method involves the topical administration of loxapine and is useful for the treatment of low pressure glaucoma and ischemic retinal degeneration.

Abstract: A novel compound for controlling (treatment and prevention) of ocular inflammation or systemic inflammatory disease is disclosed. The compound, OB-186, is effective at both the early and late phases of inflammation. The compound is useful for the treatment or prevention of inflammation in both the anterior and posterior portions of the eye and systemic inflammatory diseases, such as rheumatoid arthritis, inflammatory bowel disease, glyomerulonephritis, allergic inflammation and allergic encephalomyelitis.

Abstract: A novel compound for the treatment and prevention of ocular inflammation is disclosed. The compound, OB-104, is effective at both the early and late phases of inflammation.

Abstract: A novel compound for the treatment and prevention of ocular inflammation is disclosed. The compound, OB-101, is effective at both the early and late phases of inflammation. The compound is useful for the treatment of inflammation in both the anterior and posterior portions of the eye.

Abstract: Compositions and methods for systemic delivery of polypeptides through the eyes are disclosed. The compositions include a systemically active polypeptide at a concentration such that the composition is substantially isotonic with tear fluid. The compositions may include a permeation-enhancing agent to aid systemic absorption of higher molecular weight polypeptides, as well as peptidase inhibitors. Therapeutically effective amounts of the polypeptide compositions can be administered to the eyes where the drug passes into the nasolacrimal duct and becomes absorbed into circulation.

Abstract: The present invention contemplates a treatment for ocular inflammation.More particularly, one aspect of the present invention relates to a method of reducing, inhibiting or preventing ocular inflammation in a mammal which comprises administering to said mammal an effective amount of matrine or a derivative thereof.Another aspect of the present invention is directed to a pharmaceutical composition useful in reducing, inhibiting or preventing ocular inflammation in a mammal comprising an effective amount of matrine or a derivative thereof and a pharmaceutically acceptable carrier.Yet another aspect of the present invention contemplates a method of inducing ocular analgesia and a pharmaceutical composition useful for same.

Abstract: Methods are provided for improvement in retinal and choroidal blood flow. The compounds can be administered topically or systemically to enhance the retinal blood flow in a variety of physiologically acceptable formulations.

Abstract: Aqueous humor formation and intraocular pressure in mammals having ocular hypertension or glaucoma may be reduced by topically administering to a hypertensive eye an ophthalmologically acceptable amount of certain dopamine antagonists or acid addition salts thereof. A preferred group of dopamine antagonists is the 4-piperidino-4'-fluoro-butyrophenones, especially haloperidol, trifluperidol, and moperone. The phenothiazines are another suitable group of dopamine antagonists. An ophthalmic composition for topically treating glaucoma may comprise an aqueous solution containing 0.01% to 5% by weight of a water-soluble ophthalmologically acceptable acid addition salt of such dopamine antagonist.

Abstract: Aqueous humor formation and intraocular pressure in mammals having ocular hypertension or glaucoma may be reduced by topically administering to a hypertensive eye an ophthalmologically acceptable amount of a dopamine antagonist or acid addition salt thereof. A preferred group of dopamine antagonists is the butyrophenones, especially haloperidol, trifluperidol, and moperone. An ophthalmic composition for topically treating glaucoma may comprise an aqueous solution containing 0.01% to 5% by weight of a water-soluble ophthalmologically acceptable acid addition salt of such dopamine antagonist.

Abstract: Antiglaucoma compositions that contain enriched R-(+)-1-tert-butylamino-3-[(4-morpholino-1,2,5-thiadiazol-3-yl)oxy]-2-prop anol compared to the S-(-)-isomer and the ophthalmologically acceptable acid addition salts thereof are useful in methods for treating glaucoma and elevated intraocular pressure.

Abstract: Compositions for treating open-angle glaucoma comprising N,N-dimethylaminoethyl carbamate and method of treating ocular hypertension by topically administering such compound to the hypertensive eye.