Alcon Laboratories, Inc.

Alcon Research, Ltd.

Alcon, Inc.

Alcon Manufacturing, Ltd.

Novartis Ag

Alcon Pharmaceuticals Ltd.

Wesley Wehsin Han

Steven Howard Gerson

Ernesto J Castillo

Masood A Chowhan

Onkar N Singh

Rajni Jani

L Wayne Schneider

Huixiang Zhang

Bhagwati P Kabra

Yusuf Ali

G Michael Wall

Haresh G Bhagat

Suresh Dixit

Joseph Paul Bullock

Bahram Asgharian

Thomas R Dean

David W Stroman

Malay Ghosh

Robert E Roehrs

Ronald F Berry

John G Edwards

Glenn D Stafford, Jr

Thomas C Hohman

Suresh C Dixit

The present invention is related to pharmaceutical compositions that include a phosphonium antimicrobial agent. In a preferred embodiment, the present invention relates to an otic, nasal or ophthalmic composition (e.g., an aqueous ophthalmic solution) that includes a phosphonium salt compound as an antimicrobial agent. The compositions typically possess sufficient antimicrobial activity to satisfy USP preservative efficacy requirements and/or similar preservative standards (e.g., EP and JP).

Pharmaceutical compositions with phosphonium antimicrobial agents

The present invention is directed to the provision of an ophthalmic composition suitable for intravitreal injection. The composition includes an amount of complexing agent that reacts with one or more endogenous components (e.g., hyaluronic acid) in the eye to form a mass of enhanced viscosity. This mass can aid in creating a desirable release profile of therapeutic agent.

Injectable aqueous ophthalmic composition and method of use therefor

The present invention generally relates to suspension compositions having a carboxyvinyl polymer such as a carbomer, a galactomannan such as guar, and a borate compound. A sparingly soluble particulate compound such as nepafenac is also included in the compositions. The sparingly soluble particulate compound has a small particle size to enhance bioavailability of the compound.

Carboxyvinyl polymer-containing nanoparticle suspensions

Topical formulations of olopatadine for treatment of allergic or inflammatory disorders of the nose are disclosed. The aqueous formulations contain approximately 0.6% (w/v) of olopatadine.

Olopatadine formulations for topical nasal administration

The present invention is directed to the provision of multi-dose, self-preserved ophthalmic compositions. The compositions possess sufficient antimicrobial activity to satisfy USP preservative efficacy requirements, as well as similar preservative standards (e.g., EP and JP), without requiring the presence of conventional anti-microbial preservative agents, such as benzalkonium chloride. The compositions are effectively preserved by a balanced ionic buffer system containing zinc ions at a concentration of 0.04 to 0.9 mM, preferably 0.04 to 0.4 mM. One aspect of the balanced buffer system is limitation of the amount of buffering anions present to a concentration of 15 mM or less, preferably 5 mM or less. In a preferred embodiment, the compositions also contain borate or, most preferably, one or more borate/polyol complexes. The use of propylene glycol as the polyol in such complexes is strongly preferred. Limiting the amount of divalent metals other than zinc and the amount of ionized salts present has also been determined to be important to maximize the antimicrobial activity of the balanced buffer systems.

Self-preserved aqueous pharmaceutical compositions

The present invention is directed to the provision of multi-dose, self-preserved ophthalmic compositions. The compositions possess sufficient antimicrobial activity to satisfy USP preservative efficacy requirements, as well as similar preservative standards (e.g., EP and JP), without requiring the presence of conventional anti-microbial preservative agents, such as benzalkonium chloride. The compositions are effectively preserved by a balanced ionic buffer system containing zinc ions at a concentration of 0.04 to 0.9 mM, preferably 0.04 to 0.4 mM. One aspect of the balanced buffer system is limitation of the amount of buffering anions present to a concentration of 15 mM or less, preferably 5 mM or less. In a preferred embodiment, the compositions also contain borat or, most preferably, one or more borate/polyol complexes. The use of propylene glycol as the polyol in such complexes is strongly preferred. Limiting the amount of divalent metals other than zinc and the amount of ionized salts present has also been determined to be important to maximize the antimicrobial activity of the balanced buffer systems.

Self preserved aqueous pharmaceutical compositions

Topical formulations of olopatadine for treatment of allergic or inflammatory disorders of the eye and nose are disclosed. The aqueous formulations contain approximately 0.17-0.62% (w/v) of olopatadine and an amount of polyvinylpyrrolidone or polystyrene sulfonic acid sufficient to enhance the physical stability of the formulations.

Olopatadine formulations for topical administration

Aqueous pharmaceutical solution compositions preserved with a cationic preservative and comprising a cationic drug and a sulfonated styrene/maleic anhydride copolymer are disclosed. The compositions are particularly well suited for topical ophthalmic use, but may also be used as topically administrable otic or nasal compositions.

Ophthalmic compositions containing copolymers of sulfonated styrene and maleic anhydride

Fatty acid/amino acid soaps are used to enhance antimicrobial effectiveness in topically administrable pharmaceutical compositions containing at least one active ingredient, a cationic preservative and an anionic polyelectrolyte, such as a carboxyvinyl polymer, xanthan gum, polystyrene sulfonic acid polymer or cationic exchange resin.

Use of certain fatty acid/amino acid soaps to enhance antimicrobial effectiveness of topically administrable pharmaceutical compositions

Fatty acid/amino acid soaps are used in conjunction with an antifungal acid and a chelating agent as a new preservative system for topically administrable pharmaceutical compositions.

Preservative system for topically administrable pharmaceutical compositions containing a fatty acid/amino acid soap

Anionic surfactants are used in conjunction with an antifungal acid and a chelating agent to preserve topically administrable pharmaceutical compositions without the need for a conventional preservative such as benzalkonium chloride.

Preservative system for topically administrable pharmaceutical compositions

Anionic amino acid based surfactants are used to enhance antimicrobial effectiveness in topically administrable pharmaceutical compositions containing at least one active ingredient, a cationic preservative and an anionic polyelectrolyte, such as carboxyvinyl polymers, xanthan gum, polystyrene sulfonic acid polymers and cationic exchange resins.

Use of certain anionic amino acid based surfactants to enhance

The present invention is directed to topical ophthalmic formulations of carbonic anhydrase inhibitors and polyethoxylated derivatives of castor oil. Methods for using the formulations for treating and controlling glaucoma and ocular hypertension are also disclosed.

Growing community of inventors

Arlington, TX, United States of America

Wesley Wehsin Han