Abstract: The invention relates to a pH-sensitive polymer which is a (meth)acrylate copolymer composed of 20 to 65% by weight acrylic and/or methacrylic acid units and 80 to 35% by weight units of C1- to C18-alkyl esters of (meth)acrylic acid, characterized in that it has a molecular weight in the range from 1 000 to 50 000 g/mol, and brings about at least 60% haemolysis at pH 5.5, and less than 5% haemolysis at pH 7.4, in a concentration of 150 ?g/ml in a cytotoxicity test with human red blood cells. The invention further relates to the use of the pH-sensitive polymer as carrier for pharmaceutically effective biomolecules or active pharmaceutical ingredients and as ingredient of corresponding dosage forms.

Abstract: The present invention is directed toward water-soluble supramolecular self-assemblies and a process for their preparation via micellization of polyelectrolytes through the use of hydrophobic monomeric units. In this invention the polyelectrolyte segment ultimately forms the core of the supramolecular assembly whereas the shell consists of uncharged hydrophilic polymers or oligomers. It has been determined that the inclusion of the hydrophobic co-monomers to the polyelectrolyte segment forming the micelle core leads to a structure of enhanced stability.

Abstract: A pharmaceutical composition comprising a polymeric binder including a high molecular weight synthetic polymer having a backbone constituted of non hydrolysable covalent bonds, said polymer being able to form electrostatic bonds at a pH lower than the isoelectric point of gluten and peptides derived from the degradation of gluten, and being able to bind to gluten or peptides derived from the degradation of gluten in the gastrointestinal tract, and a pharmaceutically acceptable carrier. Methods of using the polymeric binder for binding gluten or a peptide derived from the degradation of gluten, for decreasing the degradation of gluten into toxic peptides or for decreasing interaction of gluten or peptides derived from the degradation of gluten with the gastrointestinal mucosa.

Abstract: The present invention relates to pharmaceutical compositions for the oral administration of pharmaceutical agents having low water solubility. Those agents are solubilized with a polymer suitable for the formation of nanoparticles, especially from the EUDRAGIT L and S series which release the active agent in specific target regions of the gastrointestinal tract.

Abstract: The present invention is directed toward water-soluble supramolecular self-assemblies and a process for their preparation via micellization of polyelectrolytes through the use of hydrophobic monomeric units. In this invention the polyelectrolyte segment ultimately forms the core of the supramolecular assembly whereas the shell consists of uncharged hydrophilic polymers or oligomers. It has been determined that the inclusion of the hydrophobic co-monomers to the polyelectrolyte segment forming the micelle core leads to a structure of enhanced stability.

Abstract: A pH-sensitive polymer which has cytotoxic or membranolytic properties at pH values below pH 6.5. Carriers for natural or synthetic biomolecules or active pharmaceutical ingredients using such a pH-sensitive polymer.

Abstract: The present invention relates to a pharmaceutical composition of a biologically active agent and a block copolymer composed of a poly(ethylene oxide) forming hydrophilic segment and a poly(butyl (alkyl)acrylate-co-(alkyl)acrylic acid) that is capable of forming supramolecular assemblies or micelles under favourable conditions. The supramolecular assemblies or micelles formed from said polymers associate or dissociate reversibly upon changes in the environmental pH. The pharmaceutical compositions of the present invention contain hydrophobic drugs, cations or polycationic compounds, which can be delivered to the body by oral route or other routes of administration.

Abstract: The invention relates to a heat-sensitive composition in liquid form, containing: an organic hydrophobic liquid; an organogelling substance, the molecules of which can be bound to one another by low energy linkages; and a bioactive substance, which switches to organogel form upon coming into contact with a physiological fluid during the administration thereof into an animal body, in particular, a human.

Abstract: This invention relates to novel amphiphilic diblock, triblock copolymers and star-shaped block copolymers comprising a biodegradable polymer covalently attached at the polymer ends, to a hydrophilic vinyl polymer, via divalent sulfur atom; to a process for producing the block polymers; to a polymerization process which comprises subjecting the monomers capable of radical polymerization to radical polymerization in the presence of a macromolecular biodegradable chain-transfer agent; and to pharmaceutical compositions comprising the block copolymers loaded with therapeutic agents.

Abstract: The present invention is directed toward water-soluble supramolecular self-assemblies and a process for their preparation via micellization of polyelectrolytes through the use of hydrophobic monomeric units. In this invention the polyelectrolyte segment ultimately forms the core of the supramolecular assembly whereas the shell consists of uncharged hydrophilic polymers or oligomers. It has been determined that the inclusion of the hydrophobic co-monomers to the polyelectrolyte segment forming the micelle core leads to a structure of enhanced stability.

Abstract: The present invention is directed toward water-soluble supramolecular self-assemblies and a process for their preparation via micellization of polyelectrolytes through the use of hydrophobic monomeric units. In this invention the polyelectrolyte segment ultimately forms the core of the supramolecular assembly whereas the shell consists of uncharged hydrophilic polymers or oligomers. It has been determined that the inclusion of the hydrophobic co-monomers to the polyelectrolyte segment forming the micelle core leads to a structure of enhanced stability.

Abstract: The invention relates to a pH-sensitive polymer which is a (meth)acrylate copolymer composed of 20 to 65% by weight acrylic and/or methacrylic acid units and 80 to 35% by weight units of C1- to C18-alkyl esters of (meth)acrylic acid, characterized in that it has a molecular weight in the range from 1 000 to 50 000 g/mol, and brings about at least 60% haemolysis at pH 5.5, and less than 5% haemolysis at pH 7.4, in a concentration of 150 ?g/ml in a cytotoxicity test with human red blood cells. The invention further relates to the use of the pH-sensitive polymer as carrier for pharmaceutically effective biomolecules or active pharmaceutical ingredients and as ingredient of corresponding dosage forms.

Abstract: The present invention relates to a heat-sensitive composition in liquid form, containing a hydrophobic organic liquid, an organogelling substance, the molecules of which have the capacity to bind together via bonds of low energy, and a bioactive substance, which changes to the organogel form when it comes into contact with a physiological fluid, during its administration to an animal body, in particular man.

Abstract: The present invention describes the preparation of unimolecular polymeric micelles (UPM) that bear a hydrophilic shell and a potentially ionizable and relatively hydrophobic core at a determined pH value. The core becomes electrostatically charged as the pH is changed. Such micelles can be made from either biodegradable or non-biodegradable polymers. Loaded drugs can be physically retained in the micelles when the pH of the surrounding medium favors interactions with the core. Upon a change in pH, modification in the ionization state of the core will decrease the interactions between the drug and the inner core and facilitate the release of the micellar contents.

Abstract: The instant invention is directed toward a process for the production of a sterile, stabilized nanodispersion or loaded micelle comprising a polymer and a biologically active composition; particularly to nanodispersions produced by rehydration of a freeze-dried cake produced via the direct lyophilization of a stabilized solution comprising a polymer, such as an amphiphilic block copolymer or a small molecular weight surfactant, a biologically active agent, an optional additive, and a suitable solvent.

Abstract: The present invention relates to stealth lipid nanocapsules consisting of an essentially lipid core which is liquid or semi-liquid at ambient temperature, and an outer lipid envelope comprising at least one hydrophilic surfactant which is lipidic in nature, at least one lipophilic surfactant which is lipidic in nature and at least one amphiphilic derivative of poly(ethylene glycol), the molar mass of the poly(ethylene glycol) component of which is greater than or equal to 1 000 g/mol, preferably greater than or equal to 2 000 g/mol, to the methods for the preparation thereof and to the use thereof as a carrier for active principle(s).

Abstract: The present invention relates to a pharmaceutical composition of a biologically active agent and a block copolymer composed of a poly(ethylene oxide) forming hydrophilic segment and a poly(butyl (alkyl)acrylate-co-(alkyl)acrylic acid) that is capable of forming supramolecular assemblies or micelles under favourable conditions. The supramolecular assemblies or micelles formed from said polymers associate or dissociate reversibly upon changes in the environmental pH. The pharmaceutical compositions of the present invention contain hydrophobic drugs, cations or polycationic compounds, which can be delivered to the body by oral route or other routes of administration.

Abstract: The present invention relates to pharmaceutical compositions for the oral administration of pharmaceutical agents having low water solubility. Those agents are solubilized with a polymer suitable for the formation of nanoparticles, especially from the EUDRAGIT L and S series which release the active agent in specific target regions of the gastrointestinal tract.

Abstract: This invention relates to novel amphiphilic diblock, triblock copolymers and star-shaped block copolymers comprising a biodegradable polymer covalently attached at the polymer ends, to a hydrophilic vinyl polymer, via divalent sulfur atom; to a process for producing the block polymers; to a polymerization process which comprises subjecting the monomers capable of radical polymerization to radical polymerization in the presence of a macromolecular biodegradable chain-transfer agent; and to pharmaceutical compositions comprising the block copolymers loaded with therapeutic agents.

Abstract: The instant invention is directed toward a process for the production of a sterile, stabilized nanodispersion or loaded micelle comprising a polymer and a biologically active composition; particularly to nanodispersions produced by rehydration of a freeze-dried cake produced via the direct lyophilization of a stabilized solution comprising a polymer, such as an amphiphilic block copolymer or a small molecular weight surfactant, a biologically active agent, an optional additive, and a suitable solvent.