CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS FOR PROLONGED EFFECT
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Accused Products
Abstract
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 comprising
i) an active substance, and
ii) 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 comprising
iii) 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, and
iv) 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.
9 Citations
55 Claims
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1-28. -28. (canceled)
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29. A layered pharmaceutical composition for controlled release of an active substance, comprising:
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a solid inner layer (A) comprising the active substance and a disintegrant, the solid inner layer (A) being positioned between two outer layers (B1) and (B2), each outer layer (B1) and (B2) comprising a polymer selected from the group consisting of (i) substantially water soluble or crystalline polyglycol homopolymers having a molecular weight (MW) of about 100,000 daltons or greater and (ii) substantially water soluble or crystalline polyglycol copolymers having a MW of about 2,000 daltons or greater, and mixtures thereof, wherein each outer layer is free of the disintegrant and optionally further comprises a second active substance, and a coating (C) forming a shell covering the solid inner layer (A) and partially covering outer layers (B1) and (B2) with two openings exposing a surface of each outer layer (B1) and (B2), wherein the coating (C) comprises a polymer and is substantially insoluble in and impermeable to gastrointestinal fluids; wherein the solid inner layer (A), without the outer layers (B1) and (B2) and the coating (C), disintegrates within 60 minutes when subjected to disintegrating test according to the Eur. Ph. - View Dependent Claims (30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55)
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Specification