Insite Vision Corporation

Advanced Polymer Systems, Inc.

Therasys, Inc.

Rajesh A Patel

Lyle M Bowman

Thomas B Ottoboni

Peng Shen

Raymond Chen

Margarita Vildaver

Santosh K Chandrasekaran

Martin A Katz

Sergio Nacht

Chung-Heng Cheng

Robert P Eury

John H Williford

Hoa Vinh Vo

Brian J Picard

Victor Manneth

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

Compositions for topical ophthalmic application comprising an aqueous mixture of a non-steroidal anti-inflammatory agent. The compositions are formulated with a pH and concentration of agent chosen to maintain at least some of the therapeutic agent of the formulation in suspension.

Non-steroidal anti-inflammatory ophthalmic suspensions

Compositions and methods for the modulation of melanin production are provided in which the active component is an adenosine receptor antagonist or agonist.

Methods for modulating melanin production

Ophthalmic methods and compositions are disclosed where particles of the dispersed phase of emulsions are themselves dispersed and stably maintained in physical separation by lightly crosslinked, water swellable polymers present in an aqueous polymeric system formulated for administration to the eye in drop or ribbon form. Medicament is dissolved in that dispersed phase is delivered over a sustained release period.

Sustained release emulsions

Topical ophthalmic compositions for treatment of the eye are provided which comprise aqueous mixtures of a non-steroidal agent having a pKa, a pH, and a concentration of agent chosen so as to maintain at least a therapeutic amount of the agent in suspension and a therapeutic amount of the agent in solution. A method for treating diseases of the eye, including inflammation, is also provided by topically applying such aqueous mixtures to eyes in need of treatment, whereby the therapeutic amount of the drug in solution has an immediate therapeutic effect at full concentration, and the therapeutic amount of drug in suspension has a delayed therapeutic effect by release from the suspension over a period of time by reason of dissolution kinetics.

Non-steroidal ophthalmic mixtures

Topical ophthalmic medicament delivery system combining an aqueous ophthalmic gel suspension at a pH equal to or greater than 7.5 and an osmotic pressure of from 10 to about 400 mOsM containing a pharmaceutically effective mount of one or more ophthalmic medicaments of from about 0.05% to about 10% by weight, based on the total weight of the suspension, of a carboxyl-containing polymer prepared by polymerizing one or more carboxyl-containing monoethylenically unsaturated monomers and less then about 5% by weight of a cross-linking agent. The systems have a viscosity of from about 1,000 to about 30,000 centiposes prior to administration to the eye and remain a gel in the eye for a prolonged period of time allowing for the sustained release of one or medicaments such as amine containing antibiotics alone or in combination with cortiscosteroids.

Alkaline ophthalmic suspensions

Flavored food and pharmaceutical compositions include one or more flavor additives incorporated within polymeric particles, usually within an internal pore network defined by individual polymeric particles. The polymeric particles are, in turn, dispersed within and/or over a surface of an orally-deliverable matrix material, which is usually a solid or semi-solid substrate. In the case of chewable compositions, the flavor additives will be released into the orally-deliverable matrix material as the composition is chewed and held in the mouth, thus prolonging the flavor of the composition. In the case of dried powders and mixes, the flavor will typically be made available as the product is consumed or be released into the matrix material as the composition is further processed. When two flavors are combined with the polymeric particles, the relative amounts of the additives can be selected to provide simultaneous release and exhaustion of the additives.

Methods and compositions for flavoring orally-delivered products

Topical ophthalmic medicament delivery system combining an aqueous ophthalmic gel suspension at a pH equal to or greater than 7.5 and an osmotic pressure of from 10 to about 400 mOsM containing a pharmaceutically effective amount of one or more ophthalmic medicaments of from about 0.05% to about 10% by weight, based on the total weight of the suspension, of a carboxyl-containing polymer prepared by polymerizing one or more carboxyl-containing monoethylenically unsaturated monomers and less then about 5% by weight of a cross-linking agent. The systems have a viscosity of from about 1,000 to about 30,000 centiposes prior to administration to the eye and remain a gel in the eye for a prolonged period of time allowing for the sustained release of one or medicaments such as amine containing antibiotics alone or in combination with cortiscosteroids.

A composition for the controlled release of an active substance comprises a polymeric particle matrix, where each particle defines a network of internal pores. The active substance is entrapped within the pore network together with a blocking agent having physical and chemical characteristics selected to modify the release rate of the active substance from the internal pore network. In an exemplary embodiment, drugs may be selectively delivered to the intestines using an enteric material as the blocking agent. The enteric material remains intact in the stomach but will degrade under the pH conditions of the intestines. In another exemplary embodiment, the sustained release formulation employs a blocking agent which remains stable under the expected conditions of the environment to which the active substance is to be released.

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San Mateo, CA, United States of America

Rajesh A Patel