Elan Pharma International Limited

Alkermes Pharma Ireland Limited

Nanosystems L.l.c.

Eastman-Kodak Company

Sterling Winthrop Inc.

Sterling Drug Inc.

Gary G Liversidge

Stephen B Ruddy

Scott Jenkins

Eugene Rex Cooper

W Mark Eickhoff

Pramod P Sarpotdar

Mary E Roberts

Elaine Liversidge

John G Devane

Sui-Ming Wong

Kenneth C Cundy

David A Engers

Shuqian Xu

H William Bosch

Gregory L McIntire

Niels Peter Ryde

Rajeev A Jain

Kathleen J Illig

Maurice Joseph Anthony Clancy

Jon Swanson

Janet Elizabeth Codd

Robert Hontz

J Michael Shaw

John F Bishop

David A Czekai

Gurvinder Singh Rekhi

Paul Stark

David Manser

Christian F Wertz

Christopher P Phillips

Laura Kline

Lawrence De Garavilla

Elaine M Liversidge

Kenneth Iain Cumming

Philip Conzentino, Jr

Kenneth Ian Cumming

Niall M N Fanning

Vaghefi Farid

An abuse-resistant controlled release pharmaceutical composition comprising a pharmaceutically effective amount of discrete particles of an active capable of abuse, wherein surfaces of said particles are wetted with a water insoluble coating material, and preferably wherein said composition comprises a matrix, in which said particles are distributed, and which renders the abuse-capable compound within the matrix difficult to separate from the matrix; and a method for the preparation of a controlled release pharmaceutical composition having a reduced potential for abuse, comprising applying a pressure force to a mixture comprising a water insoluble material, and particles of a pharmaceutically active compound capable of inducing in a subject a reaction that is physiologically or psychologically detrimental if administered in an immediate release dosage form, thereby resulting in surface coated particles, and incorporating said surface coated particles into a pharmaceutical composition.

Abuse-resistant pharmaceutical compositions

The present invention is directed to nanoparticulate carvedilol compositions having improved pharmacokinetic profiles, improved bioavailability, dissolution rates and efficacy. In one embodiment, the nanoparticulate carvedilol composition has an effective average particle size of less than about 2000 nm.

Nanoparticulate carverdilol formulations

The present invention is directed to nanoparticulate quinazoline derivative compositions having improved pharmacokinetic profiles and reduced fed/fasted variability. The nanoparticulate quinazoline derivative particles of the composition have an effective average particle size of less than about 2000 nm and are useful in the treatment of hyperproliferative disorders, such as cancer and other neoplastic diseases. The compositions may include quinazolinamine derivatives such as erlotinib or a salt thereof.

Nanoparticulate quinazoline derivative formulations

Described are controlled release nanoparticulate formulations comprising a nanoparticulate agent to be administered and a rate-controlling polymer which functions to prolong the release of the agent following administration. The novel compositions release the agent following administration for a time period ranging from about 2 to about 24 hours or longer.

Controlled-release nanoparticulate compositions

The present invention is directed to nanoparticulate compositions comprising glipizide. The glipizide particles of the composition preferably have an effective average particle size of less than about 2 microns.

Glipizide compositions

Nanoparticulate bisphosphonate compositions, having an effective average particle size of less than 2000 nm, are described. The compositions are useful in treating bone resorption in a mammal.

Nanoparticulate bisphosphonate compositions

The present invention provides a composition comprising a cefditoren, or a salt, derivative, prodrug, or other form thereof, for example, cefditoren pivoxil, useful in the treatment and prevention of infections and related conditions. The invention provides a composition which comprises nanoparticulate particles comprising the cefditoren, or a salt, derivative, prodrug, or other form thereof and at least one surface stabilizer. The nanoparticulate particles have an effective average particle size of less than about 2000 nm. The invention provides also a composition that delivers a cefditoren, or a salt, derivative, prodrug, or other form thereof, or nanoparticles comprising the same, in a pulsatile or continuous manner.

Nanoparticulate and controlled release compositions comprising cefditoren

Compositions comprising a nanoparticulate corticosteroid and an antihistamine are described. The compositions are useful in the prophylaxis and chronic treatment of asthma in adults and pediatric patients and for the relief of allergic conjunctivitis, symptoms of seasonal allergic rhinitis in adults and pediatric patients. Combining an antihistamine with a nanoparticulate corticosteroid in a single formulation results in improved efficacy.

Nanoparticulate corticosteroid and antihistamine formulations methods of making, and methods of administering thereof

Described are injectable formulations of nanoparticulate olanzapine that produce a prolonged duration of action upon administration, and methods of making and using such formulations. The injectable formulations comprise nanoparticulate olanzapine.

Injectable nanoparticulate olanzapine formulations

The present invention is directed to a composition comprising a nanoparticulate cyclosporine having improved bioavailability. The nanoparticulate cyclosporine particles of the composition have an effective average particle size of less than about 2000 nm in diameter and are useful in the prevention and treatment of organ transplant rejection and autoimmune diseases such as psoriasis, rheumatoid arthritis, and other related diseases. The invention also relates to a controlled release composition comprising a cyclosporine or a nanoparticulate cyclosporine that in operation delivers the drug in a pulsed or bimodal manner for the prevention and treatment of organ transplant rejection and autoimmune diseases such as psoriasis, rheumatoid arthritis, and other related diseases.

Nanoparticulate and controlled release compositions comprising cyclosporine

Disclosed are methods of intravenous administration of nanoparticulate drug formulations to a mammal to avoid adverse hemodynamic effects: by reducing the rate and concentration of the nanoparticles in the formulations; or by pre-treating the subject with histamine; or by pretreating the subject with a desensitizing amount of the nanoparticulate drug formulations.

Reduction of intravenously administered nanoparticulate-formulation-induced adverse physiological reactions

The present invention is directed to nanoparticulate compositions comprising one or more polycosanols. The polycosanol particles of the composition have an effective average particle size of less than about 2000 nm. In another aspect of this invention, novel combinations of polycosanols and other cholesterol lowering agents are described and methods of using same are taught.

Nanoparticulate polycosanol formulations and novel polycosanol combinations

Particulate crystalline therapeutic substances are formulated with stabilizers to enhance contact between the crystalline therapeutic substances and the mucosal membranes to provide extended therapeutic effect.

Methods for targeting drug delivery to the upper and/or lower gastrointestinal tract

The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increased rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HIV-2) protease inhibitors are described.

Methods of treating mammals using nanocrystalline formulations of human immunodeficiency virus (HIV) protease inhibitors

The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increased rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HV-2) protease inhibitors are described.

Growing community of inventors

West Chester, PA, United States of America

Gary G Liversidge