Egalet Ltd.

Egalet A/s

Christine Andersen

Gina Engslev Fischer

Lillian Slot

Daniel K Bar-Shalom

Anne-Marie Lademann

Karsten Lindhardt

Martin Rex Olsen

Jan Martin Oevergaard

Anne-Mette Haahr

Louise Inoka Lyhne-Iversen

Pernille Kristine Hoeyrup Hemmingsen

Daneil Bar-Shalom

Gina Fischer

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.

Controlled release formulations and methods for preparing controlled release formulations for delivery of active drug substances are described herein. The formulations described herein may be employed to produce pharmaceutical compositions, such as controlled release dosage forms, adjusted to a specific administration scheme.

Formulations and methods for the controlled release of active drug substances

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.

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Vedbaek, Denmark

Christine Andersen