Insite Vision Corporation

John C Babcock

Lyle M Bowman

Jon R Polansky

Erwin C Si

Santosh K Chandrasekaran

Sheng-Wan Tsao

Joseph R Robinson

Roy D Archibald

Santosh K Chandrasekran

Margaret J Reents

The invention provides methods for stabilizing amino-substituted steroid therapeutic agents in topical ophthalmic and other pharmaceutical formulations using effective stabilizing amounts of lightly cross-linked carboxy-containing polymers; and methods for stabilizing and solubilizing amino-substituted steroid therapeutic agents in such pharmaceutical formulations using effective stabilizing amounts of lightly cross-linked carboxy-containing polymers and amounts of selected cyclodextrin derivatives sufficient to at least partially solubilize the therapeutic agents. The cyclodextrin derivatives are selected from the group consisting of the hydroxypropyl, hydroxyethyl, glucosyl, maltosyl and maltotriosyl derivatives of .beta.- and .gamma.-cyclodextrin. Stabilized and stabilized/solubilized pharmaceutical compositions adapted for various routes of administration are also described.

Stabilization of aminosteroids for topical ophthalmic and other

The invention provides methods for stabilizing amino-substituted steroid therapeutic agents in topical ophthalmic and other pharmaceutical formulations using effective stabilizing amounts of lightly cross-linked carboxy-containing polymers; Stabilized and stabilized/solubilized pharmaceutical compositions adapted for various routes of administration are also described.

Methods and compositions for preventing or treating ophthalmic diseases or disorders wherein an ophthalmically effective amount of the C.sub.20 through C.sub.26 aminosteroids of formula XI and their pharmaceutical, acceptable salts, hydrates or solvates is administered in an inert vehicle to arrest oxidation processes damaging to the eye.

Aminosteroids for ophthalmic use

A topical, aqueous ophthalmic gel suspension for dry eye is administrable to the eye in drop form, remains as a gel in the eye for a prolonged time, and releases water and one or more ophthalmic demulcents or vasoconstrictors. It comprises water and from 0.1% to 6.5% by weight of lightly cross-linked carboxyl-containing polymer having a particle size of not more than about 50 .mu.m in equivalent spherical diameter. The suspension is at a pH of from 6.6 to 8.0, has an osmolality of from 50 to 400 mOsM, and a viscosity of from about 500 to about 4,000 centipoise (0.5 to 4 Pa.s).

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Olga, WA, United States of America

John C Babcock