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Controlled release pharmaceutical compositions for prolonged effect

机译:控释药物组合物可延长效果

摘要

Layered pharmaceutical composition suitable for oral use in the treatment of diseases where absorption takes place over a large part of the gastrointestinal tract. The composition comprising A) a solid inner layer comprisingi) an active substance, andii) one or more disintegrants/exploding agents, one of more effervescent agents or a mixture thereof.;The solid inner layer being sandwiched between two outer layers B1) and B2), each outer layer comprisingiii) a substantially water soluble and/or crystalline polymer or a mixture of substantially water soluble and/or crystalline polymers, the polymer being a polyglycol in the form of one of a) a homopolymer having a MW of at least about 100,000 daltons, and b) a copolymer having a MW of at least about 2,000 daltons, or a mixture thereof, andiv) an active substance, which is the same as in said solid inner layer A), and layer A being different from layer B,the layered composition being coated with a coating C) that has at least one opening exposing at least one surface of said outer layer, the coating being substantially insoluble in and impermeable to fluids and comprising a polymer, and the composition having a cylindrical form optionally with one or more tapered ends, wherein the ratio between the surface area of one end surface of the cylinder and the length of the cylinder is in a range of from 0.02 to 45 mm.
机译:适合于口服使用的层状药物组合物,用于治疗其中吸收在胃肠道的大部分区域发生的疾病。包含A)的固体内层的组合物包括 i)活性物质,并且 ii)一种或多种崩解剂/爆炸剂,一种或多种泡腾剂或它们的混合物。 ;固体内层夹在两个外层B1)和B2)之间,每个外层包括 iii)基本为水溶性和/或结晶的聚合物或基本为水溶性和/或结晶的混合物聚合物为以下形式之一的聚乙二醇:a)MW至少约为100,000道尔顿的均聚物,和b)MW至少约为2,000道尔顿的共聚物,或其混合物,和 iv)一种活性物质,与所述固体内层A)中的相同,并且层A与层B不同,所述层状组合物用涂层C)涂覆,所述涂层C)具有至少一个暴露所述外层的至少一个表面的开口,所述涂层基本上不溶于流体并且不可渗透流体并且包含聚合物,并且所述组合物具有圆柱形形式,任选地具有一个或多个锥形端,其中,圆柱体的一个端面的表面积与圆柱体的长度之比在0.02至45mm的范围内。

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