Abstract: The invention relates to a multilayer dosage form comprised of: a) a neutral core; b) an inner coating consisting of a methacrylate copolymer; c) an outer coating consisting of a copolymer of which 40 to 95% by weight is composed of radically polymerized C1 to C4 alkyl esters of acrylic acid or of methacrylic acid and of which 5 to 60% by weight is composed of (meth)acrylate monomers having an anionic group in the alkyl radical. The invention is characterized in that the inner coating is essentially comprised of a methacrylate copolymer, of which at least up to 90% by weight consists of (meth)acrylate monomers with neutral radicals, which, in accordance with DIN 53 787, has a minimum film formation temperature of no higher than 30° C., and which contains the pharmaceutical active substance in bound form.

Abstract: This application relates to a homogeneous biorelevant composition for preparing fasted state biorelevant media having a surface tension between 25 mN/m and 50 mN/m for simulating fasted state gastric and fasted state upper small intestinal fluids of mammalian species, especially humans, dogs, etc. comprising at least one bile salt, eg. sodium taurocholate or sodium taurodeoxycholate; at least one phospholipid, especially 60-99 wt % phosphatidylcholine (PC), enzyme digested diacylphospholipids containing 50-90 wt % of monoacyl-PC; or mixtures thereof; and at least one fatty acid or monovalent salt of the fatty acid, such as sodium oleate. The application also relates to an aqueous biorelevant media composed of surfactants occurring in the gastrointestinal tract of mammals, in particular when prepared from above homogeneous biorelevant composition.

Abstract: The invention relates to a pharmaceutical composition comprising a mixture of at least one cationic, water-soluble (meth)acrylate copolymer, at least one water-insoluble polymer and at least one active ingredient having a solubility in demineralized water of 3.3 g/l or less, characterized in that the water-insoluble polymer and the active ingredient are present in a ratio of at most 3.5 to 1 parts by weight, and the pharmaceutical composition has the property of releasing the active ingredient present in a medium buffered to pH 1.2 in dissolved form in a concentration which, after 2 hours at pH 1.2, corresponds to at least sixteen times the solubility value of the active ingredient alone at pH 1.2.

Abstract: The invention relates to a multiparticulate drug form suitable for uniform release of an active pharmaceutical ingredient in the small intestine and in the large intestine, comprising at least two forms of pellets A and B which comprise an active pharmaceutical ingredient in the core and have different polymer coatings which determine the release of the active ingredient at different pH values, characterized in that pellet form A is provided with an inner polymer coating which enables continuous release of active ingredient, and has an outer enteric coating which rapidly dissolves above about pH 5.5, and pellet form B is provided with a polymer coating which, in the USP release test, releases less than 20% of the active ingredient at pH 6.8 in 6 hours and releases more than 50% of the active ingredient at pH 7.2 in 6 hours. The invention additionally relates to a process for producing the multiparticulate drug form and to the use of pellet forms A and B for producing the drug form.

Abstract: The invention relates to a dosage form, containing the active ingredient cholylsarcosine, in the form of pellets, which are provided with a polymer coating that is resistant to gastric juices. The invention is characterised in that it discloses pellets comprising an active ingredient, which contain between 50 and 80 wt. % of the active ingredient cholylsarcosine and between 50 and 20 wt. % of one or more conventional pharmaceutical adjuvants as binding agents, whereby at least 90 wt. % of said adjuvants are water-soluble and the size of at least 80 % of the pellets comprising an active ingredient is between 800 and 2,500 $g(m)m. The granulates containing an active ingredient are coated with an anonic, film-forming polymer coating agent, which dissolves in a 0.07M sodium phosphate buffer with a pH value of 5.5 at a dissolution rate of at least 10 mg/min*g and whose dissolution rate in a 0.07M sodium phosphate buffer with a pH value of 6.0 is at least 200 mg/min*g.

Abstract: Disclosed herein are pharmaceutical compositions comprising carboxyalkylcellulose esters for delivery of pharmaceutically active substances having low solubility in a medium such as water, an acidic aqueous buffer, a neutral aqueous buffer, or a basic aqueous buffer. Also disclosed are methods for making pharmaceutical compositions and methods of administering the compositions.

Abstract: The invention relates to a multilayer dosage form comprised of: a) a neutral core; b) an inner coating consisting of a methacrylate copolymer; c) an outer coating consisting of a copolymer of which 40 to 95% by weight is composed of radically polymerized C1 to C4 alkyl esters of acrylic acid or of methacrylic acid and of which 5 to 60% by weight is composed of (meth)acrylate monomers having an anionic group in the alkyl radical. The invention is characterized in that the inner coating is essentially comprised of a methacrylate copolymer, of which at least up to 90% by weight consists of (meth)acrylate monomers with neutral radicals, which, in accordance with DIN 53 787, has a minimum film formation temperature of no higher than 30° C., and which contains the pharmaceutical active substance in bound form.

Abstract: The invention relates to a pharmaceutical composition containing a ?-lactam antibiotic and/or a pharmaceutically tolerable salt thereof in the form of coated pellets that may optionally contain a ?-lactamase inhibitor and/or a pharmaceutically tolerable salt thereof, some or all pellets comprising coatings that dissolve at different pH values depending on the composition of said coatings. This pharmaceutical composition allows the blood plasma level of the ?-lactam antibiotic and/or a pharmaceutically tolerable salt thereof to remain above 2 ?g/ml for at least 12 hours within a period of 24 hours if administered twice a day.

Abstract: The invention relates to a multiparticulate drug form suitable for uniform release of an active pharmaceutical ingredient in the small intestine and in the large intestine, comprising at least two forms of pellets A and B which comprise an active pharmaceutical ingredient in the core and have different polymer coatings which determine the release of the active ingredient at different pH values, characterized in that pellet form A is provided with an inner polymer coating which enables continuous release of active ingredient, and has an outer enteric coating which rapidly dissolves above about pH 5.5, and pellet form B is provided with a polymer coating which, in the USP release test, releases less than 20% of the active ingredient at pH 6.8 in 6 hours and releases more than 50% of the active ingredient at pH 7.2 in 6 hours. The invention additionally relates to a process for producing the multiparticulate drug form and to the use of pellet forms A and B for producing the drug form.

Abstract: The invention relates to a pharmaceutical formulation containing essentially a) an inner layer which can optionally be applied to a core, with the active substance budesonide, bound with a binding agent; b) a middle layer with a polymer covering agent which is soluble in intestinal juice or retardant; and c) an outer envelope or outer layer which is resistant to stomach juice, said layers being able to contain in a manner known per se other pharmaceutically usual adjutants. The inventive formulation is characterised in that the binding agent is a polymer or a copolymer with acid groups and the formulation of the inner layer without the middle and outer layer releases the bound active ingredient in a release test according to USP XXIII monography <711> dissolution with apparatus 2 (addle) at a rotational speed of 100/min in a phosphate buffer pH 7.5 after 30 min to a value of more than 80%.

Abstract: The invention relates to a multiparticulate drug form suitable for uniform release of an active pharmaceutical ingredient in the small intestine and in the large intestine, comprising at least two forms of pellets A and B which comprise an active pharmaceutical ingredient in the core and have different polymer coatings which determine the release of the active ingredient at different pH values, characterized in that pellet form A is provided with an inner polymer coating which enables continuous release of active ingredient, and has an outer enteric coating which rapidly dissolves above about pH 5.5, and pellet form B is provided with a polymer coating which, in the USP release test, releases less than 20% of the active ingredient at pH 6.8 in 6 hours and releases more than 50% of the active ingredient at pH 7.2 in 6 hours. The invention additionally relates to a process for producing the multiparticulate drug form and to the use of pellet forms A and B for producing the drug form.

Abstract: The invention relates to a multiparticulate drug form suitable for uniform release of an active pharmaceutical ingredient in the small intestine and in the large intestine, comprising at least two forms of pellets A and B which comprise an active pharmaceutical ingredient in the core and have different polymer coatings which determine the release of the active ingredient at different pH values, characterized in that pellet form A is provided with an inner polymer coating which enables continuous release of active ingredient, and has an outer enteric coating which rapidly dissolves above about pH 5.5, and pellet form B is provided with a polymer coating which, in the USP release test, releases less than 20% of the active ingredient at pH 6.8 in 6 hours and releases more than 50% of the active ingredient at pH 7.2 in 6 hours. The invention additionally relates to a process for producing the multiparticulate drug form and to the use of pellet forms A and B for producing the drug form.