Abstract: A disintegrating loadable tablet product in compressed form comprising i) at least 60% w/w of a sorbent material having a specific surface area (BET surface area) of at least 50 m2/g as measured by gas adsorption or mixtures of such sorbent materials, and ii) a disintegrant or a mixture of disintegrants wherein the tablet in compressed form has a) a porosity of 45% v/v or more, b) a hardness of at least 20 Newton, and c) a loading capacity of at least 30% of a liquid. The tablet is suitable for the preparation of a tablet containing an active substance by e.g. immersing the tablet in a liquid containing the active substance. The invention thus provides a safe and reproducible new method of preparing pharmaceutical tablets.

Abstract: A novel dosage form. The dosage form is presented in particulate form and before oral ingestion the particulate material is subjected to an aqueous medium, whereby it is converted to a semi-solid form by swelling or gelling of one or more of the components, especially of a gellan gum, of the particulate matter. The invention also relates to a vehicle for oral administration of one or more active substances, the vehicle comprising a gellan gum arranged in a configuration allowing optimal water diffusion so that upon addition of a predetermined amount of an aqueous medium, without the necessity of applying shear forces or other mixing forces, within a time period of 5 minutes or less swells and/or gels and the texture of the swelled vehicle being similar to that of a soft pudding and having a viscosity of at least about 10,000 cps as measured by a Brookfield Viscometer with a #4 LV spindle at 6 rpm and at 20-25° C.

Abstract: A controlled release pharmaceutical composition for oral use comprising carvedilol. The composition releases carvedilol after oral administration to a mammal, including a human, in such a manner that a prolonged residence of carvedilol is obtained in the circulatory system compared with the known compositions of carvedilol. Furthermore, a composition according to the present invention makes available to the body a suitable plasma concentration of one or both of the enantiomeric species, namely R(+) and/or S(?) carvedilol for obtaining the desired therapeutic effect.

Abstract: A pharmaceutical composition for controlled release of an active substance is provided. The active substance is released into an aqueous medium by erosion of at least one surface of the composition. The composition comprises i) a matrix comprising a) polymer or a mixture of polymers, b) an active substance and, optionally, c) one or more pharmaceutically acceptable excipients, and ii) a coating.

Abstract: A pharmaceutical composition for controlled release of an active substance, the composition being a matrix composition of: (a) a substantially water soluble or crystalline polymer, (b) an active substance, and optionally, (c) one or more pharmaceutically acceptable excipients having a water solubility of at least 1 mg/ml at ambient temperature. The matrix composition does not contain a water dispersible or water soluble surface active agent that has at least one domain, which is compatible with the polymer in the matrix composition, and which substantially eliminates water diffusion between the interface between the polymer crystals.

Abstract: A controlled release pharmaceutical composition for oral use comprising a solid dispersion of i) at least one therapeutically, prophylactically and/or diagnostically active substance, which at least partially is in an amorphous form, ii) a pharmaceutically acceptable polymer that has plasticizing properties, and iii) optionally a stabilizing agent, the at least one active substance having a limited water solubility, and the composition being designed to release the active substance with a substantially zero order release. The polymer is typically a poly ethylene glycol and/or polyethylene oxide having a molecular weight of at least about 20,000 in crystalline and/or amorphous form or a mixture of such polymers, and the active substance is typically carvedilol.

Abstract: A novel matrix composition for pharmaceutical use. The matrix composition has been designed so that it is especially suitable in those situation where an improved bioavailability is desired and/or in those situation where a slightly or insoluble active substance is employed. Accordingly, a controlled release pharmaceutical composition for oral use is provided in the form of a coated matrix composition, the matrix composition comprising i) a mixture of a first and a second polymer that have plasticizing properties and which have melting points or melting intervals of a temperature of at the most 200° C.

Abstract: A composition for controlled release of an opioid from a pharmaceutical composition, the method comprises controlling the release of at least one opioid into an aqueous medium by erosion of at least one surface of a pharmaceutical composition comprising I) a matrix composition comprising a) polymer or a mixture of polymers, b) an opioid and, optionally, c) one or more pharmaceutically acceptable excipients, and (i) a coating. The matrix composition has a conus-like shape so the surface area exposed to the aqueous medium increases at least during initial erosion of the matrix composition, and the dissolution of the opioid-when tested in a Dissolution Test as described herein with or without application of sinkers-results in a zero order release of at least 80% of the opioid contained in the composition. Such compositions are especially suitable for controlled release of an opioid to obtain a delayed pead concentration and a prolonged therapeutically effective plasma concentration upon oral administration.

Abstract: A controlled release pharmaceutical composition for oral use comprising a solid dispersion of: i) at least one therapeutically, prophylactically and/or diagnostically active substance, which at least partially is in an amorphous form, ii) a pharmaceutically acceptable polymer that has plasticizing properties, and iii) optionally, a stabilizing agent, the at least one active substance having a limited water solubility, and the composition being designed to release the active substance with a substantially zero order release. The polymer is typically a polyethylene glycol and/or polyethylene oxide having a molecular weight of at least about 20,000 in crystalline and/or amorphous form or a mixture of such polymers, and the active substance is typically carvedilol.

Abstract: A pharmaceutical composition for controlled release of an active substance. The active substance is released into an aqueous medium by erosion of at least one surface of the composition. The composition comprises i) a matrix comprising a) polymer or a mixture of polymers, b) an active substance and, optionally, c) one or more pharmaceutically acceptable excipients, and ii) a coating. Zero order release is desirable. The matrix typically comprises PEO and the active substance is typically an opioid such as morphine or a glucuronide thereof. The coating comprises a first cellulose derivative which is substantially insoluble in the aqueous medium and at least one of a) a second cellulose derivative which is soluble or dispersible in water, b) a plasticizer, and, d) a filler.

Abstract: A method for controlling the release of at least one therapeutically, prophylactically and/or diagnostically active substance into an aqueous medium by erosion of at least one surface of a pharmaceutical composition. The method comprises adjusting the concentration and/or the nature of the ingredients making up the matrix composition in such a manner so as to obtain an approximately zero order release of the active substance from the pharmaceutical composition when subject to an in vitro dissolution test as described herein. The composition comprises i) a matrix composition comprising a) a polymer or a mixture of polymers that may be substantially water soluble and/or crystalline, b) an active substance and, optionally, c) one or more pharmaceutically acceptable excipients, and ii) a coating. Typical polymers are PEO.

Abstract: A controlled release pharmaceutical composition for oral use comprising carvedilol. The composition releases carvedilol after oral administration to a mammal, Including a human, in such a manner that a prolonged residence of carvedilol is obtained In the circulatory system compared with the known compositions of carvedilol. Furthermore, a composition according to the present invention makes available to the body a suitable plasma concentration of one or both of the enantiomeric species, namely R(+) and/or S(−) carvedilol for obtaining the desired therapeutic effect.