Abbvie Deutschland Gmbh and Co Kg

Basf Aktiengesellschaft

Abb Vie Deutschland Gmbh & Co. Kg

Abbott Laboratories Corporation

Novartis Ag

Abbott Gmbh & Co Kg

Janssen R&d Ireland

Abbvie Inc.

Bit Pharma Gmbh

The Abbott

Jörg Breitenbach

Jörg Rosenberg

Bernd Liepold

Gunther Berndl

Christoph Schmidt

Thomas Kessler

Robert Heger

Harald Krull

Kennan C Marsh

Matthias Degenhardt

Markus Mägerlein

Ute Lander

Axel Sanner

Laman L Alani

Helmut Auweter

Dirk Simon

Soumojeet Ghosh

Ulrich Reinhold

Heinrich Sack

Heribert Bohn

Folker Ruchatz

Volker Laux

Ulrich Westedt

Jürgen Hofmann

Didier Lefebvre

Dieter Herr

Vikram Kalthod

Martin Knobloch

Norbert Steiger

Harald Hach

Frithjof Sczesny

Rainer Klenz

Peter Heilmann

Jöerg Rosenberg

Peter Wilke

Hans Bührle

Michael Stadler

Cynthia Burnell

Helmuth Steininger

Frauke-Regina Rueffer

Katrin Schneider

Jürgen Weis

Claudia Henzel

Steffen Bossmann

Benedikt Steitz

Thomas Hantke

Bettina Rehbock

Ralf Altenburger

Nicoletta Loggia

Jörg Ogorka

Gunther Derndl

Shreeram Sathya

Peter HÖLIG

William Riordan

Mark Hess

John Dete

Martin Babcock

Frauke-Regina RÜFFER

Claudia Packhäuser

Thomas K Kessler

Ai Mey Chuah

Gaurav C Patel

Houston Sanders

Shannon Hertzler

Daniel Crandall

Katja Fastnacht

Christopher Rupp

George Shlieout

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 liquid mixture, comprising a) at least one compound selected from polyols, polyol ethers wherein at least one hydroxyl group is unetherified, or polyalkylene ethers wherein at least one terminal hydroxyl group is unetherified, b) 1,3-bis(caprolactam-1-yl) butane, and c) diacetoxybutane mimics the solubility properties of a graft copolymer comprising a poly(alkylene glycol) backbone and a vinyl acetate/N-vinylcaprolactam copolymer grafted onto the backbone. In a method for evaluating the compatibility of a biologically active substance with the graft copolymer i) the biologically active sub-stance is brought into contact with the liquid mixture, and ii) the phase behavior of the test system and/or the solubility of the biologically active substance in the mixture is determined.

Test solvent for evaluating the compatibility of biologically active substances and graft copolymers

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 pharmaceutical dosage form comprises a solid dispersion product of at least one active ingredient dispersed in a polymeric binder composition, the polymeric carrier composition comprising a) a vinylpyrrolidone homopolymer, wherein at least 95% by weight of the vinylpyrrolidone homopolymer has a molecular weight distribution within the range of from 1000 to 13 000; and b) a vinylpyrrolidone copolymer having a weight-average molecular weight of from 5000 to 1 500 000. The dosage form is preferably prepared by a melt extrusion process. The polymeric carrier composition exhibits a high drug dissolution power and allows a reduction of the viscosity of the melt without deteriorating the mechanical properties and storage stability of the dosage form.

Pharmaceutical dosage form comprising polymeric carrier composition

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 invention provides a dosage form, comprising a melt-processed mixture of (a) a pharmaceutically effective amount of imatinib or a salt thereof, (b) at least one polymeric binder, and (c) at least one pharmaceutically acceptable non-ionic surfactant. The invention provides imatinib dosage forms with high drug loading which can be prepared in a simple and efficient manner, imatinib dosage forms from which the active principle is released in an essentially pH-independent fashion, and extended release imatinib dosage forms.

Melt-processed imatinib dosage form

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

The present invention provides a pharmaceutical dosage formulation, and more particularly, to a pharmaceutical dosage formulation comprising an HIV protease inhibitor.

Solid pharmaceutical dosage formulation

The invention relates to excipients in powder form for use in solid pharmaceutical presentations, comprising a pharmaceutically acceptable polymer and a liquid or semisolid solubilizing surface-active substance.

Solubilizing aids in powder form for solid pharmaceutical presentation forms

Nanoparticulate preparations of pharmaceutical and cosmetic active substances with a core-shell structure, whereby the active substance is present in an X-ray amorphous form, together with a polymer matrix and the shell consists of a stabilizing sheathing matrix.

Nanoparticulate core shell systems and the use thereof in pharmaceutical and cosmetic preparation

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

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Mannheim, Germany

Jörg Breitenbach