Bend Research, Inc.

Pfizer Products Inc.

Walter Christian Babcock

Dwayne Thomas Friesen

Ravi Mysore Shanker

Daniel Tod Smithey

James A S Nightingale

Warren Kenyon Miller

William John Curatolo

Douglas Alan Lorenz

David Keith Lyon

David J Edlund

Bruce M Johnson

James William West

Scott B McCray

Marshall David Crew

Julian B Lo

Rodney James Ketner

William Brett Caldwell

James Blair West

Michael E Perlman

Mark E Tuttle

Ralph Tadday

Mark D Rabenstein

Roderick Jack Ray

Leah Elizabeth Appel

Kelly L Smith

Edward Dennis LaChapelle

James W Brooke

Harold K Lonsdale

Carl C Wamser

George W Rayfeld

Geoffrey D Hyde

David Kenneth Lyon

Dan Tod Smithey

Dwayne T Friensen

Sheri L Shamblin

Kris A Krichko

Michael Ellis Pfizer Global Research & Development Perlman

Marc David Rabenstein

Michael Ellis Perlman

Mark David Rabenstein

James Alan Schriver Nightingale

Ravi Mysore c/o Pfizer Global R&D Shanker

A pharmaceutical composition comprises a solid amorphous dispersion comprising a low-solubility drug and a concentration-enhancing polymer and a lipophilic microphase-forming material. Alternatively, a solid amorphous dispersion comprising a low-solubility drug and a concentration-enhancing polymer is co-administered with a lipophilic microphase-forming material to an in vivo use environment.

Pharmaceutical compositions of amorphous dispersions of drugs and lipophilic microphase-forming materials

A pharmaceutical composition comprises a solid adsorbate comprising a drug adsorbed onto a substrate and a lipophilic microphase-forming material. The solid adsorbate may also be co-administered with a lipophilic microphase-forming material to an in vivo use environment. The compositions of the present invention enhance the concentration of drug in a use environment.

Pharmaceutical compositions of adsorbates of amorphous drugs and lipophilic microphase-forming materials

A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.

Pharmaceutical compositions providing enhanced drug concentrations

A dosage form comprises a low-solubility drug, and a precipitation-inhibiting polymer. The drug is in a solubility-improved form and in the form of particles at least partially coated with the precipitation-inhibiting polymer.

Pharmaceutical dosage forms comprising a low-solubility drug and a polymer

Pharmaceutical compositions of a low-solubility drug and lower alkanoate-, phthalate- and trimellitate esters of hydroxypropyl methyl cellulose and lower alkanoate- and succinate esters of cellulose and methyl cellulose are disclosed that provide enhanced concentrations of the drug in a use environment.

Pharmaceutical compositions with enhanced performance

Solid compositions of low-solubility drugs and poloxamers that provide concentration enhancement when administered to an aqueous environment of use are disclosed.

Solid compositions of low-solubility drugs and poloxamers

Disclosed are polymers of hydroxypropyl methyl cellulose acetate succinate (HPMCAS) and hydroxypropyl methyl cellulose acetate (HPMCA) with unique degrees of substitution of hydroxypropoxy, methoxy, acetyl, and succinoyl groups. When used in making compositions comprising a low-solubility drug and such polymers, the polymers provide enhanced aqueous concentrations and/or improved physical stability.

A composition comprises a solid dispersion comprising a low-solubility drug and at least one polymer. At least a major portion of the drug in the dispersion is amorphous. The polymer has a glass transition temperature of at least 100&#xb0; C. measured at a relative humidity of fifty percent. Another aspect of the invention comprises the same composition except that the dispersion has a glass transition temperature of at least 50&#xb0; C. at a relative humidity of fifty percent. In another aspect of the invention, a composition comprises a solid dispersion comprising a low-solubility drug and a stabilizing polymer. At least a major portion of the drug in the dispersion is amorphous. The composition also includes a concentration-enhancing polymer that increases the concentration of the drug in a use environment. The stabilizing polymer has a glass transition temperature that is greater than the glass transition temperature of the concentration-enhancing polymer at a relative humidity of 50%.

Pharmaceutical solid dispersions

A composition comprises a solid dispersion comprising a low-solubility drug and at least one polymer. In another aspect of the invention, a composition comprises a solid dispersion comprising a low-solubility drug and a stabilizing polymer. At least a major portion of the drug in the dispersion is amorphous. The composition also includes a concentration-enhancing polymer that increases the concentration of the drug in a use environment. The stabilizing polymer has a glass transition temperature that is greater than the glass transition temperature of the concentration-enhancing polymer at a relative humidity of 50%.

Pharmaceutical compositions comprise a low-solubility drug adsorbed onto a high surface area substrate to form an adsorbate. The compositions in some embodiments include a concentration-enhancing polymer.

Pharmaceutical compositions of adsorbates of amorphous drug

A pharmaceutical composition comprises a dispersion comprising a low-solubility drug and a matrix combined with a concentration-enhancing polymer. At least a major portion of the drug is amorphous in the dispersion. The compositions improve the stability of the drug in the dispersion, and/or the concentration of drug in a use environment.

Pharmaceutical compositions of dispersions of amorphous drugs mixed with polymers

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Bend, OR, United States of America

Walter Christian Babcock