申请人:Egalet A/S
公开号:EP2301526A2
公开(公告)日:2011-03-30
A pharmaceutical composition for controlled release of at least one opioid into an aqueous medium by erosion of at least one surface of the composition, the composition comprising
i) a matrix composition comprising a) a polymer or a mixture of polymers, wherein the polymer comprises a polyethylene glycol, a polyethylene oxide and/or a block copolymer of ethylene oxide and propylene oxide, b) an opioid as an active substance and, optionally, c) one or more pharmaceutically acceptable excipients, and
ii) a coating having at least one opening exposing at the one surface of said matrix, the coating comprising a polymer selected from polyamide, polyethylene, polyethylene terephthalate, polypropylenem polyurethane, polyvinyl acetate, polyvinyl chloride, silicone rubber, latex, polyhydroxybutyrate, polyhydroxyvalerate, teflon, polylactic acid or polyglycolic acid and copolymers thereof, copolymers such as ethylene vinyl acetate (EVA), styrene-butadienestyrene (SBS) and styrene-isoprene-styrene (SIS),
wherein the matrix composition has a conus-like shape so that 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 in accordance with the USP 24, NF 19, (711), Dissolution, apparatus 2 equipped with a paddle; with or without application of sinkers - results in a zero order release of at least 80% of the opioid contained in the composition, and about 75% w/w of the opioid is released from the composition within 4-10 hours.
一种药物组合物,用于通过侵蚀组合物的至少一个表面将至少一种阿片类药物控 制释放到
水介质中,该组合物包括
i) 基质组合物,包括 a) 聚合物或聚合物混合物,其中聚合物包括聚
乙二醇、聚
环氧乙烷和/或
环氧乙烷与环氧
丙烷的嵌段共聚物;b) 作为活性物质的阿片类药物;以及 c) 一种或多种药学上可接受的赋形剂,以及
硅橡胶、乳胶、聚羟基
丁酸酯、聚羟基
戊酸酯、聚
四氟乙烯、聚
乳酸或聚
乙醇酸及其共聚物,以及
乙烯-
醋酸乙烯(
EVA)、
苯乙烯-
丁二烯-
苯乙烯(SBS)和
苯乙烯-
异戊二烯-
苯乙烯(SIS)等共聚物、
其中,基质组合物具有圆锥状形状,这样至少在基质组合物的初始侵蚀期间,暴露于
水介质的表面积会增加,并且
阿片类药物的溶解--当按照美国药典 24,NF 19,(711),溶解,配备桨的仪器 2 进行溶解测试时;无论是否使用沉降片--导致组合物中所含阿片类药物至少 80% 的零阶释放,约 75% w/w 的阿片类药物在 4-10 小时内从组合物中释放。