Coated pharmaceutical or nutraceutical preparation with enhanced pulsed active substance release

摘要

The present invention relates to a pharmaceutical or nutraceutical preparation comprising a) a core containing a pharmaceutically or nutraceutically active substance and a substance that acts in a modulatory manner with regard of the release of pharmaceutically or nutraceutically active substances; and b) a controlling layer surrounding the core comprising i) 55 to 92% by weight based on the total weight of (meth)acrylic copolymers present in the layer of one or a mixture of a plurality of (meth)acrylate copolymers composed of 80 to 98% by weight based on the weight of the (meth)acrylic copolymer of structural units derived from C1 to C4 alkyl esters of (meth)acrylic acid and 2 to 20% by weight based on the weight of the (meth)acrylic copolymer of structural units derived from (meth)acrylate monomers with a quaternary ammonium group in the alkyl radical; and ii) 8 to 45% by weight based on the total weight of (meth)acrylic copolymers present in the layer of one or a mixture of a plurality of (meth)acrylate copolymers composed of more than 5 to 59% by weight based on the weight of the copolymer of structural units derived from acrylic acid or methacrylic acid and to tablets or capsules comprising same.

主权项

1. A pharmaceutical or nutraceutical preparation having a sigmoidal release profile which releases more than 90% of its pharmaceutically or nutraceutically active components within 10 hours of oral administration, consisting essentially of:
a) a core comprising a pharmaceutically or nutraceutically active substance and a substance that acts in a modulatory manner, during release of the pharmaceutically or nutraceutically active substance; and b) a single controlling layer surrounding the core comprising i) 55 to 92% by weight, based on a total weight of (meth)acrylic acid ester copolymers present in the layer, of first (meth)acrylic acid ester copolymers; and ii) 8 to 45% by weight, based on the total weight of (meth)acrylic acid ester copolymers present in the layer, of second (meth)acrylic acid ester copolymers;
wherein said first (meth)acrylic acid ester copolymers comprise one or a mixture of a plurality of (meth)acrylate copolymers comprising 80 to less than 93% by weight, based on the total weight of the first (meth)acrylic acid ester copolymers, of structural units obtained from C1 to C4 alkyl esters of (meth)acrylic acid, and more than 7 to 20% by weight, based on the total weight of the first (meth)acrylic acid ester copolymers, of structural units obtained from (meth)acrylate monomers with a quaternary ammonium group in an alkyl radical; andwherein said second (meth)acrylic acid ester copolymers comprise one or a mixture of a plurality of (meth)acrylate copolymers comprising more than 5 but not more than 59% by weight, based on the total weight of the second (meth)acrylic acid ester copolymers, of structural units obtained from acrylic acid or (meth)acrylic acid.