Abbvie Deutschland Gmbh and Co Kg

Abbott Gmbh & Co Kg

Basf Aktiengesellschaft

Janssen R&d Ireland

Abbott Laboratories Corporation

Abbvie Inc.

Jörg Rosenberg

Laman L Alani

Jörg Breitenbach

Christoph Schmidt

Gunther Berndl

Bernd Liepold

Harald Krull

Thomas Kessler

Soumojeet Ghosh

Kennan C Marsh

Ulrich Reinhold

Robert Heger

Matthias Degenhardt

Ute Lander

Markus Mägerlein

Volker Laux

Ulrich Westedt

Jürgen Hofmann

Dieter Herr

Martin Knobloch

Harald Hach

Norbert Steiger

Rainer Klenz

Peter Heilmann

Helmuth Steininger

Michael Stadler

Peter Wilke

Thomas Hantke

Bettina Rehbock

Hans Bührle

Thomas Müller

Katja Fastnacht

Anamarija Curic

Benjamin-Luca Keller

A method is described for the production of dosage forms, which comprise a solid dispersion of a microcrystalline active substance, in which a thermoplastic polymer with a glass transition temperature Tg of at least 40&#xb0; C. is melted and an active substance is dissolved homogeneously in the melt; crystallization of the active substance is initiated in the mass obtained; and the mass is cooled. Crystallization of the active substance can be initiated by adding a nonsolvent, seed crystals of the active substance or a derivatization reagent. In addition, crystallization can be initiated by holding the mass for a sufficient length of time at a temperature that is below the temperature at which the active substance is completely soluble in the mass.

Production of dosage forms comprising a solid dispersion of a microcrystalline agent

Pharmaceutically acceptable solubilizing compositions comprising (i) at least one tocopheryl compound having a polyalkylene glycol moiety and (ii) at least one alkylene glycol fatty acid monoester or mixture of alkylene glycol fatty acid mono-and diester are disclosed. The solubilizing compositions are useful in the manufacture of pharmaceutical dosage forms comprising a melt-processed mixture of at least one active ingredient and at least one pharmaceutically acceptable polymer. The solubilizing compositions enhance the bioavailability of the active ingredient following oral intake.

Pharmaceutically acceptable solubilizing composition and pharmaceutical dosage form containing same

A process for producing a solid dispersion of an active ingredient which comprises feeding the active ingredient and a matrix-forming agent to an extruder and forming a uniform extrudate, wherein the extruder comprises at least two rotating shafts (), each of the shafts () carrying a plurality of processing elements disposed axially one behind the other, the processing elements defining (i) a feeding and conveying section (R; A), (ii) at least one reverse-flight section (D), and (iii) a discharging section (E), wherein the processing elements defining the reverse-flight section (R; D) comprise at least one reverse-flight element () which is based on a screw-type element having a conveying direction being opposite to the general conveying direction of the extruder.

Process for producing a solid dispersion of an active ingredient

A process for producing a solid dispersion of an active ingredient which comprises feeding the active ingredient and a matrix-forming agent to an extruder and forming a uniform extrudate, wherein the extruder comprises at least two rotating shafts (), each of the shafts () carrying a plurality of processing elements disposed axially one behind the other, the processing elements defining (i) a feeding and conveying section (A), (ii) at least one mixing section (B), and (iii) a discharging section (E), wherein the processing element(s) defining the mixing section (B) comprise(s) a mixing element () that is derived from a screw type element (FIG.).

A pharmaceutically acceptable solubilizing composition comprising (i) at least one tocopheryl compound having a polyalkylene glycol moiety and (ii) at least one alkylene glycol fatty acid monoester or mixture of alkylene glycol fatty acid mono- and diester is disclosed. The solubilizing composition is useful in the manufacture of a pharmaceutical dosage form which comprises a melt-processed mixture of at least one active ingredient, at least one pharmaceutically acceptable polymer. The active ingredient(s) may be inhibitors of HIV protease. The solubilizing composition enhances the bioavailability of the active ingredient after oral intake.

Rate-controlled particles, comprising compounds of the formula as a solid dispersion.

Rate-controlled particles

The present invention relates to a solid dosage form with at least one film, which contains an active substance at least in sections, and the concentration of the active substance in the film or in the films has a gradient in a direction normal to the thickness of film. The invention further relates to a method of producing a solid dosage form, in which at least one film is produced, containing an active substance at least in sections, with the concentration of the active substance having a gradient in the longitudinal direction of the film.

Solid dosage form with a film containing an active substance, as well as its method of production

The present invention relates to self-emulsifying formulations based on an active ingredient component and a formulation base with a lipid component and with a binder component and to the use of this formulation as dosage form in the life science sector. The invention also describes a process for producing self-emulsifying formulations by mixing the formulation components to form a plastic mixture and, where appropriate, to manufacture the formulations as dosage form advantageously by use of melt extrusion. The formulations spontaneously form emulsions in water or aqueous media.

Self-emulsifying active substance formulation and use of this formulation

A description is given of a process for the preparation of a pharmaceutical composition of a macrolide antibiotic in essentially noncrystalline form, in which the macrolide antibiotic, a water-swellable polymer and a proton donor are blended in an extruder in the presence of water and forced through a die, the ratio by weight of the sum of macrolide antibiotic, water-swellable polymer and proton donor to water being at least 1:1. The macrolide antibiotic is preferably clarithromycin and the water-swellable polymer is preferably chosen from crosslinked polyvinylpyrrolidone, crosslinked sodium carboxymethylcellulose and crosslinked polyacrylic acid.

Preparation of compositions with essentially noncrystalline embedded macrolide antibiotics

The invention concerns a method for producing solid galenic formulations which consists in: forming a processable paste comprising a) 50 to 99.4 wt. % of at least one non-thermoplastic carrier, b) 0.5 to 30 wt. % of at least an adjuvant selected among thermoplastic polymers, lipids, sugar alcohols and solubilizing agents, c) 0.1 to 49.5 wt. % of at least one active principle, at a temperature not less than the softening temperature of the adjuvant but rising to at least 70&#xb0; C.; then in cooling the resulting paste. Said solid galenic formulations quickly disintegrate in an aqueous medium.

Method for producing solid galenic formulations using a crosslinked non-thermoplastic carrier

The present invention relates to formulations based on at least one heparin, glycosaminoglycan or heparinoid and on a formulation base with a lipid component and a polymer component. The use of this formulation as drug form for oral administration of at least one heparin, glycosaminoglycan or heparinoid, and also a process for producing the formulations by mixing the formulation components to form a plastic mixture and, where appropriate, to manufacture the formulations as drug form, advantageously using melt extrusion, are described. The lipid component advantageously has active ingredient-promoting properties, while the polymer component is soluble or swellable. At least parts of the lipid component are embedded in a polymer matrix, preferably in the form of a molecular dispersion. The formulations can form emulsions in water or aqueous liquids.

Formulation based on heparin, glycosaminoglycan or heparinoid, use of the formulation and the formulation base

The present invention relates to an apparatus for producing solid active ingredient-containing forms from an active ingredient-containing formulation which comprises at least one polymeric binder. The apparatus according to the invention has at least one extruderfor continuous plastication of the formulation and at least two injection unitswhich are provided separate from one another, each of which is connected to the extruder, and through which the formulation can be injected into at least one mold. In the process according to the invention for producing solid active ingredient-containing forms from an active ingredient-containing formulation which comprises at least one binder, the active ingredient-containing formulation is continuously plasticated, the plasticated formulation is fed into an injection unit, and the formulation present in this injection unitis injected into a mold, and plasticated formulation is fed into another injection molding unit, and the formulation present in the other injection molding unitis injected into the moldor another mold.

Method of producing solid shape forms containing an active ingredient

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Ellerstadt, Germany

Jörg Rosenberg