Abstract: A sustained-release tramadol formulation oral administration is provided which, upon initial administration of one dose, provides an analgesic effect within 2 hours, which analgesic effect continues for at least 24 hours after administration.

Abstract: The instant invention provides a two-step polymerization process for preparing amphiphilic poly(N-vinyl-2-pyrrolidone), (PVP)-block-polyester copolymers and other diblock and triblock copolymers consisting of PVP as one block. The block copolymers of the invention can be used as vehicles for drug delivery.

Abstract: The invention relates to a once a day formulation of trazodone or a trazodone derivative. The formulation contains trazodone or a trazodone derivative and a controlled release excipient so that, once administered orally, the trazodone or the trazodone derivative is maintained at a therapeutic plasma concentration from at least 1 hour to at least 24 hours after initial administration. After administration, the initial therapeutic action takes effect within the first hour and lasts at least about 24 hours. This therapeutic effect remains relatively and substantially stable for the remaining period of 24 hours. The formulations can be used for treating depression and/or sleeping disorders.

Abstract: The invention provides compositions and methods for the targeted, in particular, pH targeted, delivery of pharmaceutically active agents in mammals. The compositions comprise pH sensitive diblock copolymers, which permit the release of the pharmaceutically active agent when exposed to an environment having a particular pH. The compositions are particularly useful for the oral delivery of water insoluble pharmaceutically active agents.

Abstract: Disclosed is a misuse preventative, controlled release formulation comprising a core comprising a superabsorbent material (for example, polycarbophil), a controlled release coat surrounding the core, and a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed within the core, the coat, or both the core and the coat. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material present in the core swells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the formulation. Also disclosed is a method of using the misuse preventative, controlled release formulation to deliver a pharmaceutically active agent to a mammal, for example, a human, in need thereof.

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 instant invention provides a two-step polymerization process for preparing amphiphilic poly(N-vinyl-2-pyrrolidone), (PVP)-block-polyester copolymers and other diblock and triblock copolymers consisting of PVP as one block. The block copolymers of the invention can be used as vehicles for drug delivery.

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: 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 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 a solid slow release oral pharmaceutical dosage unit resistant to amylase which comprises a solid dosage unit made up of an admixture of a therapeutic dosage of an orally effective pharmaceutical agent, an optional polysaccharide or polyol, and high amylose starch, wherein the cross-linking of the high amylose starch has been carried out with a cross-linking agent with from about 0.1 g to about 40 g of cross-linking agent per 100 g of high amylose starch. In a preferred embodiment of the invention, the high amylose starch is modified with a functional group-attaching reagent that covalently bonds functional groups thereto.

Abstract: Novel polymeric micelles which are used to deliver therapeutic agents, including anti tumor drugs.

Abstract: Disclosed is a pharmaceutical controlled release tablet containing an active ingredient in combination with a carrier made of cross-linked amylose in which hydroxymethylpropylcellulose (HPMC) with a viscosity higher than or equal to 4000 cps is added as an adjuvant. The addition of HPMC to the tablet permits to control the effect of enzymes, and more particular alpha-amylase present in the intestinal medium, on the cross-linked amylose used as a carrier, and thus to reduce the dependence of the kinetics of release upon the concentration of enzymes present in the medium.

Abstract: The present invention is concerned with the manufacture of solid dosage units (pharmaceutical and others). More specifically, the invention is related to powders of cross-linked amylose, having a specific cross-linking degree for use as tablet binders and disintegrants.

Abstract: The present application is concerned with a solid slow release pharmaceutical dosage unit. More specifically, the invention is directed to a tablet form prepared by direct compression of cross-linked amylose (CLA) having a definite cross-linking degree, .alpha.-amylase and a pharmaceutical agent. The presence of the cross-linked amylose allows a sustained release of the drug, while the .alpha.-amylase permits the modulation of the release time. In other words, the release time of the drug is function of the amount of .alpha.-amylase in the tablet. The amount of .alpha.-amylase is defined in terms of Enzyme Units.

Abstract: The present invention is concerned with a solid slow release oral pharmaceutical dosage unit which comprises a solid dosage unit made up of an admixture of a therapeutic dosage of an orally effective pharmaceutical product and a cross-linked polymer of amylose with a cross-linking agent selected from 2,3 dibromopropanol and epichlorohydrin, wherein the cross-linking of the polymer has been carried out with from about 0.1 to about 10 g of cross-linking agent per 100 g of amylose.