| 摘要 |
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 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. |
| 主权项 |
1. A method for treating a patient suffering from pain that is sensitive to an opioid comprising orally administering such opioid in a controlled release pharmaceutical composition, comprising
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, wherein the erodible matrix composition comprises a polyethylene glycol, a polyethylene oxide and/or a block copolymer of ethylene oxide and propylene oxide, and does not comprise polyethylene glycol 2000 monostearate or polyethylene glycol 400 monostearate, the matrix composition being provided with a single coating that is substantially insoluble in and impermeable to aqueous media, the coating comprising one or more polymers selected from the group consisting of ethylcellulose, cellulose acetate, polyamide, polyethylene, polyethylene terephthalate, polypropylene, polyurethane, polyvinyl acetate, polyvinyl chloride, silicone rubber, latex, polyhydroxybutyrate, polyhydroxyvalerate, teflon, polylactic acid or polyglycolic acid and copolymers thereof, ethylene vinyl acetate (EVA), styrene-butadienestyrene (SBS) and styrene-isoprene-styrene (SIS), the coating having two openings and exposing at least one surface of the matrix, thereby allowing controlled release of said opioid by erosion of said matrix surface, wherein the composition exhibits a zero order release profile and wherein about 75% w/w of the opioid is released from the composition within 4-10 hours when tested in a Dissolution Test in accordance with USP 24, NF 19, (711), Dissolution, apparatus 2, equipped with a paddle, with or without sinkers. |
