Insite Vision Corporation

Catalent Pharma Solutions, LLC

Roy D Archibald

Santosh K Chandrasekaran

Lyle M Bowman

Joseph R Robinson

Jeffrey P Davis

David Mufson

Stephen Pham

John C Babcock

James Frederick Foreman

S Kumar Chandrasekaran

Yansheng Su

Margaret J Reents

Randal R Schettl

Christa D Nicholas

The present invention relates to formulations of concentrated azalide antibiotics and methods for making and using them. Specifically, the invention relates to a method of treating an infection comprising administering to a patient in need thereof, an effective amount of a concentrated aqueous azalide antibiotic formulation made according to the method comprising dissolving an azalide antibiotic in an aqueous solution comprising a strong acid. The invention also relates to methods for making concentrated aqueous azalide antibiotic formulations for use in pulmonary infection, a nasopharyngeal infection, an otic infection, an ocular infection, a dermal or a vaginal infection. The invention also relates to concentrated aqueous azalide antibiotic formulations made by dissolving an azalide antibiotic in an aqueous solution comprising a strong acid.

Concentrated aqueous azalide formulations

Charging fixture with valves

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.

Liquid droplet dispensing apparatus

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Fremont, CA, United States of America

Roy D Archibald