The Liposome Company, Inc.

Basf Corporation

Other

Elan Pharmaceuticalstechnologies, Inc.

Shaukat Ali

Andrew S Janoff

Eric G Mayhew

J Craig Franklin

Paul R Meers

Charles Pak

Imran Ahmad

Donna J Cabral-Lilly

Gil Koehane

Soumendu Bhattacharya

Anisul Quadir

Ravi K Erukulla

Tong Shangguan

Carlos Santos

Patrick L Ahl

Walter R Perkins

Ravi Erukulla

Xingong Li

Donald Hirsh

A gastroretentive composition comprises a mixture comprising an active ingredient component and an excipient component. The excipient component comprises a first water-soluble reaction product produced from a precursor comprising a vinyl group, and a copolymer of a polyalkylene glycol and a second water-soluble reaction product produced from a precursor comprising a vinyl group. A method of forming the gastroretentive composition comprises the steps of providing the active ingredient component and the excipient component, and mixing the active ingredient component and the excipient component to form a mixture. The mixture is aggregated to form an aggregation that is dry granulated to form a plurality of granules. The plurality of granules is processed to form the gastroretentive composition.

Gastroretentive composition on the basis of a water-soluble reaction product from a vinyl group-containing precursor

A medicament carrier composition includes a medicament and a polymer component including a polyvinylpyrrolidone having a weight average molecular weight of at least 700,000 g/mol. The medicament carrier composition has a viscosity of from 500 to 5,000 cps at 250 C, is substantially free of cellulose, and includes an auxiliary polymer. The medicament carrier composition is used to form a film that is also substantially free of cellulose. The film has a consistent thickness and size, and an increased flexibility and increased moisture resistance due to the polyvinylpyrrolidone. The medicament carrier composition is also used in a method of forming the film. The method includes the steps of providing the medicament and the polymer component. The method also includes the step of combining the polymer component and the medicament to form the medicament carrier composition. The method further includes the step of drying the medicament carrier composition to form the film.

Medicament carrier composition and method of forming a film therefrom

This invention provides vehicles capable of delivering high concentrations of poorly hydrophilic/poorly lipophilic compounds to animals, by combining compounds having biocompatible hydrophobic domains with conjugates having both hydrophobic and hydrophilic regions. Such formulations are suitable for a number of uses in animals, particularly the administration thereto of high concentrations of therapeutically useful compound, without an undue level of side effects.

Particulate formulations

Provided herein is a taxane having a hydrocarbon attached at the 2&prime; and/or 7 positions, the hydrocarbon's alpha position being occupied by a &ldquo;hydrolysis-promoting group&rdquo; (&ldquo;HPG&rdquo;). In one embodiment, the hydrolysis promoting group is stereospecifically attached to the &agr;-carbon of the hydrophobic taxane. The Substitution of an HPG for the methylene unit ordinarily occupying the alpha position allows for enhanced in vivo hydrolysis of the hydrocarbon-taxane bond, and hence, for enhanced taxane therapeutic activity. Also provided herein are taxane-containing compositions, and methods of administering taxanes to animals, including those afflicted with cancers or inflammatory diseases.

Hydrolysis-promoting hydrophobic taxane derivatives

Provided herein is a taxane having a hydrocarbon attached at the 2&prime; and/or 7 positions, the hydrocarbon's alpha position being occupied by a &ldquo;hydrolysis-promoting group&rdquo; (&ldquo;HPG&rdquo;). In one embodiment, the hydrolysis promoting group is stereospecifically attached to the a-carbon of the hydrophobic taxane. The Substitution of an HPG for the methylene unit ordinarily occupying the alpha position allows for enhanced in vivo hydrolysis of the hydrocarbon-taxane bond, and hence, for enhanced taxane therapeutic activity. Also provided herein are taxane-containing compositions, and methods of administering taxanes to animals, including those afflicted with cancers or inflammatory diseases.

Peptide-lipid conjugates are incorporated into liposomes so as to selectively destabilize the liposomes in the vicinity of target peptidase-secreting cells, and hence, to deliver the liposomes to the vicinity of the target cells, or directly into the cells. The liposomes can thus be used to treat mammals for diseases, disorders or conditions, e.g., tumors, microbial infection and inflammations, characterized by the occurrence of peptidase-secreting cells.

Peptide-lipid conjugates, liposomes and lipsomal drug delivery

This invention provides liposomes containing one or more N-acylated phosphatidylethanolamines, such liposomes being useful for localizing the delivery of bioactive agents to cells.

N-acyl phosphatidylethanolamine-mediated liposomal drug delivery

Liposomal peptide-lipid conjugates and delivery using same

Provided herein is a taxane having a hydrocarbon attached at the 2' and/or 7 positions, the hydrocarbon's alpha position being occupied by a 'hydrolysis-promoting group' ('HPG'). In one embodiment, the hydrolysis promoting group is stereospecifically attached to the .alpha.-carbon of the hydrophobic taxane. The Substitution of an HPG for the methylene unit ordinarily occupying the alpha position allows for enhanced in vivo hydrolysis of the hydrocarbon-taxane bond, and hence, for enhanced taxane therapeutic activity. Also provided herein are taxane-containing compositions, and methods of administering taxanes to animals, including those afflicted with cancers or inflammatory diseases.

Peptide-lipid conjugates

Provided herein is a taxane having a hydrocarbon attached at the 2' and/or 7 positions, the hydrocarbon's alpha position being occupied by a 'hydrolysis-promoting group' ('HPG'). Substitution of an HPG for the methylene unit ordinarily occupying the alpha position allows for enhanced in vivo hydrolysis of the hydrocarbon-taxane bond, and hence, for enhanced taxane therapeutic activity. Also provided herein are taxane-containing compositions, and methods of administering taxanes to animals, including those afflicted with cancers.

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Monmouth Junction, NJ, United States of America

Shaukat Ali