Egalet Ltd.

Egalet A/s

Lifecycle Pharma A/s

Daniel Bar-Shalom

Gina Fischer

Pernille Hoyrup Hemmingsen

Lillian Slot

Per Holm

Gina Engslev Fischer

Daniel K Bar-Shalom

Christine Andersen

Anne-Marie Lademann

Pernille Høyrup Hemmingsen

Daneil Bar-Shalom

A oral pharmaceutical composition for controlled release of an opioid from a pharmaceutical composition is described that comprises (i) an erodible matrix composition comprising a mixture of (a) a polymer or a mixture of polymers (b) an opioid, and optionally, (c) one or more pharmaceutically acceptable excipients; and (ii) a single, substantially insoluble in and impermeable coating having two openings exposing at least one surface of the matrix, and comprising one or more polymers. The composition exhibits controlled release of the opioid by erosion of the matrix and exhibits a zero order release profile wherein about 75% w/w of the opioid is released from the composition within 4-10 hours when tested in a dissolution test as described herein.

Morphine controlled release system

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.

Opioid polymer release system

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.

Polymer release system

Described are controlled release oral pharmaceutical composition comprising an erodible matrix composition comprising a polyethylene oxide, a therapeutically effective amount of an opioid or a pharmaceutically acceptable salt, complex, solvate or anhydrate thereof, or a mixture thereof and, optionally, one or more pharmaceutically acceptable excipients, and a coating on the matrix composition, wherein the coating has at least one opening exposing a surface of an end portion of the matrix composition, thereby allowing controlled release of the opioid by erosion of the matrix surface, wherein the composition exhibits zero order release of at least 80% of the opioid contained in the composition. The matrix may have a cylindrical shape having a long axis and a conus-shaped end portion having a largest diameter and a smallest diameter, such that the surface area exposed increases during erosion of the conus-shaped end portion.

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&#x2014;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 peak concentration and a prolonged therapeutically effective plasma concentration upon oral administration. Once or twice daily administration is possible. The matrix typically comprises PEO and the active substance is typically an opioid such as morphine or a glucuronide thereof.

Morphine polymer release system

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(&#x2212;) carvedilol for obtaining the desired therapeutic effect.

Controlled release carvedilol compositions

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&#xb0; C. In one embodiment of the invention, the particulate matter can be molded into a desired shape or pressed onto a dispensing unit such as a spoon.

Swellable dosage form comprising gellan gum

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&#xb0; C., the first polymer being selected from the group consisting of polyethylene glycols and polyethylene oxides, and the second polymer being selected form block copolymer of ethylene oxide and propylene oxide including poly(ethylene-glycol-b-(DL-lactic acid-co-glycolic acid)-b-ethylene glycol (PEG-PLGA PEG), poly((DL-lactic acid-co-glycolic acid)-g-ethylene glycol) (PLGA-g-PEG), poloxamers and polyethylene oxide-polypropylene oxide (PEO-PPO), ii) a therapeutically, prophylactically and/or diagnostically active substance, the matrix composition being provided with a coating having at least one opening exposing at one surface of said matrix, wherein the active substance is released with a substantially zero order release.

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Virum, Denmark

Lillian Slot