Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: Lightly crosslinked polymers, preferably ones prepared by suspension or emulsion polymerizing at least about 90% by weight of a carboxyl-containing monoethylenically unsaturated monomer such as acrylic acid with from about 0.1% to about 5% by weight of a polyfunctional, and preferably difunctional, crosslinking agent such as divinyl glycol (3,4-dihydroxy-1,5-hexadiene), having a particle size of not more than about 50 .mu.m in equivalent spherical diameter, when formulated with an ophthalmic medicament, e.g., fluorometholone, into suspensions in aqueous medium in which the amount of polymer ranges from about 0.1% to about 6.5% by weight, based on the total weight of the aqueous suspension, the pH is from about 3.0 to about 6.

Abstract: 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).

Abstract: A disposable unit- or multi-dose liquid dispensing container device, particularly adapted for delivery of ophthalmic liquid medicament in the form of discrete droplets to the eye. The structural configuration of the device including an angularly offset leading end permits the user to employ a free hand for manipulation of the eyelid to enhance reception of the discharge opening of the dispenser into the conjunctival cul-de-sac while at the same time, enabling the user to look directly into a wall-mounted mirror for accurate placement of the medicament. A small capacity reservoir and ease of control of accurate orifice size enables the application of uniform liquid-ejection pressure by the user to deliver droplets of reproducible dosage size with the multi-dose embodiment.

Abstract: A dosage form that coadministers a drug and a percutaneous absorption enhancer to a defined area of the skin. The dosage form comprises a body that contains supplies of drug and enhancer and has a basal surface that contacts the area of skin and transmits the drug and enhancer to the area for absorption thereby. The drug is provided to the basal surface at a rate at least as great as the rate at which the skin is able to absorb the drug whereas the enhancer is via a rate controlling means at a substantially constant rate that increases the permeability of the treated area of skin to the drug to a level at which the drug is absorbed a therapeutically effective rate.

Abstract: Method and therapeutic system in the form of a bandage that administer scopolamine base transdermally in an initial pulse of 10 to 200 .mu.g/cm.sup.2 of skin that quickly brings the concentration of scopolamine in the plasma to a level at which emesis and nausea are inhibited without intolerable side effects, followed by a substantially constant dosage in the range of 0.3 to 15 .mu.g/hr that holds said level. The bandage is a four-layer laminate of, from the top: a protective backing; a gelled, mineral oil-polyisobutene-scopolamine reservoir lamina that is the source of the constant dosage; a microporous membrane that controls the constant dosage rate; and a gelled, mineral oil-polyisobutene-scopolamine adhesive layer that is the source of the pulse dose and the means by which the bandage is attached to the skin.

Abstract: A dosage form that coadministers a drug and a percutaneous absorption enhancer to a defined area of the skin. The dosage form comprises a body that contains supplies of drug and enhancer and has a basal surface that contacts the area of skin and transmits the drug and enhancer to the area for absorption thereby. The drug is provided to the basal surface at a rate at least as great as the rate at which the skin is able to absorb the drug whereas the enhancer is via a rate controlling means at a substantially constant rate that increases the permeability of the treated area of skin to the drug to a level at which the drug is absorbed at a therapeutically effective rate.

Abstract: Drug dispensers comprising a flat body composed of a drug solute phase dispersed in a continuous polymer matrix phase in which the release rate of drug from the body is substantially constant and is controlled by the rate at which the drug solute phase dissolves in the continuous polymer matrix phase. Such control and constancy are realized by establishing specific correlations between the diffusion coefficient, dissolution rate constant, and thickness of the body.

Abstract: A bandage for administering drugs to the skin that consists of an impermeable backing layer, a drug reservoir layer composed of drug and a carrier, and a contact adhesive layer by which the bandage is adhered to the skin. The contact adhesive layer controls the rate at which drug is administered and maintains that rate at an approximately constant level by virtue of there being a particular correlation between the solubility of the drug in the carrier and in the contact adhesive, the diffusion coefficient of the drug in the carrier and in the contact adhesive, the concentration of drug in the reservoir, and the thickness of the contact adhesive layer.

Abstract: Therapeutic system in the form of a skin patch that administers clonidine transdermally in an initial priming dose of 10 to 300 mcg/cm.sup.2 of skin that brings the concentration of clonidine in the blood to a level sufficient to elicit alpha-adrenergic stimulation without intolerable side effects, followed by a substantially constant continuous dosage in the range of 0.1 to 100 mcg/hr that maintains said level. The system is a four-layer laminate of, from the top: a protective backing; a gelled, mineral oil-polyisobutene-clonidine reservoir lamina that is the source of the clonidine for the continuous constant dosage; a microporous membrane that controls the constant dosage rate; and a gelled, mineral oil-polyisobutene-clonidine contact adhesive layer that is the source of the clonidine for the priming dose and the means by which the system is attached to the skin.