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

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: 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 solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.

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 formulation comprising i) fenofibric acid, a physiologically acceptable salt or derivative thereof and optionally other active substances, ii) a binder component comprising at least one enteric binder, and optionally iii) other physiologically acceptable excipients is described. Fenofibric acid, the physiologically acceptable salt or derivative thereof is preferably in the form of a molecular dispersion in these formulations. An advantageous process for their preparation, in particular by melt extrusion, and the use of this formulation for oral administration of fenofibric acid, a physiologically acceptable salt or derivative thereof are likewise described.

Abstract: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.

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: 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 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.

Abstract: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.

Abstract: A pharmaceutical dosage form, comprising a) a liquid or flowable core, b) a shell of a polysaccharide or proteinaceous material completely enclosing said core, the core comprising an active ingredient dissolved in a pharmaceutically acceptable compound of the formula (I) wherein n is an integer from 3 to 5, and wherein the (i) the at least one active ingredient and the compound of the formula (I) account for at least 50% by weight of the composition; and (ii) the water activity aw of the composition is less than 0.4.

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: 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: The present invention relates to a solid dosage form with at least one film (1), which contains an active substance at least in sections. The dosage form is characterized in that the concentration of active substance in film (1) or in the films has a gradient in a direction normal to the thickness of film (1). The invention further relates to a method of production of a solid dosage form with an active substance, in which at least one film (1) is produced, which contains an active substance at least in sections, with the concentration of active substance in film (1) or in the films having a gradient in the longitudinal direction of the film. This film is then formed to produce the dosage form.

Abstract: 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.

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: A process for at least partially enveloping a pharmaceutical dosage form, in which the dosage form is surrounded by a shrinkable film, and the film is subsequently shrunk is described.