Insite Vision Corporation

Other

Santosh K Chandrasekaran

Lyle M Bowman

Jon R Polansky

Erwin C Si

John C Babcock

Sheng-Wan Tsao

Roy D Archibald

Joseph R Robinson

Takemitsu Asaoka

Katsumi Imamori

Akihiro Shibata

Masami Takahashi

Samir Roy

Jeffrey P Davis

Rajesh A Patel

Yansheng Su

Margaret J Reents

Hoa Vinh Vo

Christa D Nicholas

John G Babcock

The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid compounds. The invention also relates to quinolone carboxylic acid compositions and methods of preparing the same.

Quinolone carboxylic acid compositions and related methods of treatment

A controlled release medicament delivery system comprises a plasticized bioerodible polymer, such as a polyorthoester. Medicament desirably is entrapped in the plasticized polymer. The resulting delivery system is able to release the medicament in a controlled and sustained manner. The formulation is particularly advantageous for use as a once-a-day eyedrop. During preparation, the polymer may be heated to an elevated temperature for a sufficient time to substantially reduce its molecular weight.

Plasticized bioerodible controlled delivery system

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

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 6.5, and the osmotic pressure (osmolality or tonicity) is from about 10 mOsM to about 400 mOsM, provide new topical ophthalmic medicament delivery systems having suitably low viscosities which permit them to be easily administered to the eye in drop form, and hence be comfortably administrable in consistent, accurate dosages. These suspension will rapidly gel in the eye after coming into contact with the eye's tear fluid to a substantially greater viscosity than that of the originally-introduced suspension and thus remain in place for prolonged periods of time to provide sustained release of the ophthalmic medicament.

Ophthalmic suspensions

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).

Topical ophthalmic suspensions

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.

Growing community of inventors

Moraga, CA, United States of America

Santosh K Chandrasekaran