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 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: This invention relates to novel crystalline lopinavir/surfactant adducts, methods for their preparation, therapeutic uses of those crystalline lopinavir/surfactant adducts, and pharmaceutical compositions containing them or made from them.

Abstract: A solid dispersion product comprising itraconazole and hydroxypropyl methylcellulose, which satisfies the Formula 0.35>?Htr (1) (wherein ?Htr represents the endotherm (J/g) accompanying a transition at about 240° C.). The solid dispersion product shows an improved bioavailability.

Abstract: A solid dispersion product comprising an effective amount of one or more active ingredients and an effective amount of one or more hydroxypropyl methylcellulose(s), which satisfies the Formula 0.35>?Htr (1) (wherein AHtr represents the endotherm (J/g) accompanying a transition at about 240° C.). The solid dispersion product is used for the manufacture of a dosage form having improved bioavailability of said one or more active ingredients by oral administration to a patient in need thereof.

Abstract: A viable strategy to enhance the bioavailability of poorly soluble drugs is to use amorphous solids in place of the more commonly used crystalline solids in pharmaceutical formulations. However, amorphous solids are physically meta-stable and tend to revert back to their crystalline counterpart. An effective approach to stabilizing an amorphous drug against crystallization is to disperse it in a polymer matrix. The drug's solubility in the chosen polymer defines the upper limit of drug loading without any risk of crystallization. Measuring the solubility of a drug in a polymer has been a scientific and technological challenge because the high viscosity of polymers makes achieving solubility equilibrium difficult and because pharmaceutically important drug/polymer dispersions are glasses, which undergo structural relaxation over time. The invention provides a method based on Differential Scanning calorimetry (DSC) for measuring the solubility of crystalline drugs in polymeric matrices.

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 solid dispersion product comprising itraconazole and hydroxypropyl methylcellulose, which satisfies the Formula 0.35>?Htr (1) (wherein ?Ht, represents the endotherm (J/g) accompanying a transition at about 240° C.). The solid dispersion product shows an improved bioavailability.

Abstract: A method for evaluating the solubility of a crystalline substance in a polymer comprises a) providing at least one sample of an intimate crystalline substance/polymer mixture at a predetermined crystalline substance concentration; b) annealing the sample at a constant temperature Ta for a period of time; c) heating the annealed sample while recording the heat flux over time by DSC; d) identifying a DSC dissolution endotherm in the recorded heat flux, if any; e) considering the crystalline substance concentration as a concentration above the crystalline substance solubility in the polymer at temperature Ta when there is a DSC dissolution endotherm identified, and considering the crystalline substance concentration as a concentration less than or equal to the crystalline substance solubility in the polymer at temperature Ta when there is no DSC dissolution endotherm identified.

Abstract: A solid dispersion product comprising itraconazole and hydroxypropyl methylcellulose, which satisfies the Formula 0.35>?Htr (1) (wherein ?Htr represents the endotherm (J/g) accompanying a transition at about 240° C). The solid dispersion product shows an improved bioavailability.

Abstract: A solid dispersion product comprising an effective amount of one or more active ingredients and an effective amount of one or more hydroxypropyl methylcellulose(s), which satisfies the Formula 0.35>?Htr (1) (wherein AHtr represents the endotherm (J/g) accompanying a transition at about 240° C.). The solid dispersion product is used for the manufacture of a dosage form having improved bioavailability of said one or more active ingredients by oral administration to a patient in need thereof.

Abstract: A viable strategy to enhance the bioavailability of poorly soluble drugs is to use amorphous solids in place of the more commonly used crystalline solids in pharmaceutical formulations. However, amorphous solids are physically meta-stable and tend to revert back to their crystalline counterpart. An effective approach to stabilizing an amorphous drug against crystallization is to disperse it in a polymer matrix. The drug's solubility in the chosen polymer defines the upper limit of drug loading without any risk of crystallization. Measuring the solubility of a drug in a polymer has been a scientific and technological challenge because the high viscosity of polymers makes achieving solubility equilibrium difficult and because pharmaceutically important drug/polymer dispersions are glasses, which undergo structural relaxation over time. The invention provides a method based on Differential Scanning calorimetry (DSC) for measuring the solubility of crystalline drugs in polymeric matrices.

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 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 composition which comprises a solid or semi-solid matrix having at least one active ingredient uniformly dispersed therein, the matrix comprising at least one pharmaceutically acceptable matrix-forming agent and a 1,3-bis(lactamyl)-butane compound, in particular 1,3-bis(pyrrolidon-1-yl)-butane. The active ingredient is preferably dispersed in the matrix in a state of a solid solution. The matrix-forming agent is preferably a pharmaceutically acceptable polymer. The composition is useful for the manufacture of pharmaceutical dosage forms.

Abstract: A solid dispersion product comprising itraconazole and hydroxypropyl methylcellulose, which satisfies the Formula 0.35>?Htr (1) (wherein ?Htr represents the endotherm (J/g) accompanying a transition at about 240° C). The solid dispersion product shows an improved bioavailability.

Abstract: A solid dispersion product comprising an effective amount of one or more active ingredients and an effective amount of one or more hydroxypropyl methylcellulose(s), which satisfies the Formula 0.35>?Htr (1) (wherein ?Htr represents the endotherm (J/g) accompanying a transition at about 240° C.). The solid dispersion product is used for the manufacture of a dosage form having improved bioavailability of said one or more active ingredients by oral administration to a patient in need thereof.

Abstract: A dosage form and method for the delivery of drugs, particularly drugs of abuse, characterized by resistance to solvent extraction, tampering, crushing, or grinding, and providing an initial burst of release of drug followed by a prolonged period of controllable drug release.

Abstract: Stable pharmaceutical preparations, comprising torasemide in noncrystalline form.

Abstract: The present invention relates to a solid pharmaceutical composition, comprising