Abstract: The present invention relates to nanoparticles based on optionally alkoxylated poly(alkyl cyanoacrylates) having a defined molecular mass and dispersity, a method for preparing such nanoparticles, compositions comprising such nanoparticles and medical uses thereof. The invention further relates to the use of optionally alkoxylated poly(alkyl cyanoacrylates) having a defined molecular mass and dispersity for preparing nanoparticles as well as to a method for preparing such polymers.

Abstract: 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° 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.

Abstract: The present invention relates to nanoparticles based on optionally alkoxylated poly(alkyl cyanoacrylates) having a defined molecular mass and dispersity, a method for preparing such nanoparticles, compositions comprising such nanoparticles and medical uses thereof. The invention further relates to the use of optionally alkoxylated poly(alkyl cyanoacrylates) having a defined molecular mass and dispersity for preparing nanoparticles as well as to a method for preparing such polymers.

Abstract: A solid dosage form having a matrix with at least one active compound dispersed homogeneously in the matrix, which is obtainable by melting a powder mixture, wherein the powder mixture comprises at least one thermoplastic binder and a combination of highly disperse silica and at least one inorganic pigment, is described. The co-use of the highly disperse silica and the inorganic pigments leads to better flow properties of the powder mixture, has the effect of a faster release of the active compound from the dosage forms obtained, and imparts a visually pleasing appearance to the dosage forms. A process for the preparation of the dosage form is also described.

Abstract: 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.

Abstract: 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 (2), each of the shafts (2) 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 (14) which is based on a screw-type element having a conveying direction being opposite to the general conveying direction of the extruder.

Abstract: 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 (2), each of the shafts (2) 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 (11, 12, 13) that is derived from a screw type element (FIG. 2).

Abstract: 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.

Abstract: 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.

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

Abstract: 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 (2), each of the shafts (2) 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 (11, 12, 13) that is derived from a screw type element (FIG. 2).

Abstract: 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 (2), each of the shafts (2) 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 (14) which is based on a screw-type element having a conveying direction being opposite to the general conveying direction of the extruder.

Abstract: 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.

Abstract: 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.

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

Abstract: 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.

Abstract: 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.

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

Abstract: 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.

Abstract: 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.