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: 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 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.

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 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.

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: A delivery system for sustained release of a calcium-channel blocking agent is adapted for introduction in the cerebrospinal fluid of a subject. The delivery system comprises a solid dispersion product of a calcium-channel blocking agent in a mixture of a (i) first poly(lactide-co-glycolide) having a molecular weight distribution centered around a first number average molecular weight Mn1 and a (ii) second poly(lactide-co-glycolide) having a molecular weight distribution centered around a second number average molecular weight Mn2, wherein Mn1 is in the range of from 2000 to 3000 g/mol and the ratio of Mn1/Mn2 is from 1.8 to 3.5. The delivery system is deposited in the vicinity of or adjacent to a blood vessel showing vasospasm or suspected of developing vasospasm.

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

Abstract: 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.

Abstract: 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.

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: A curcuminoid formulation, comprising a melt-processed solid dispersion product comprising one or more curcuminoids, a nutritionally acceptable thermoplastic polymer, and a phosphatide; providing an improved oral bioavailability compared to non-formulated crystalline curcuminoid. A method for producing said formulation. A nutritional product fortified with said formulation. Said formulation for use in the treatment or prophylaxis of cancer, conditions involving an inflammatory reaction, neurological disorders, cardiovascular disease, pulmonary disease, the formation of cholesterol gallstones, and parasitic infestation.

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 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.

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