Pharmaceutical Compositions for the Deterrence and/or Prevention of Abuse

A pharmaceutical composition comprising an antagonist in direct contact with a seal coat, an agonist in direct contact with the seal coat and a sequestering polymer but not the antagonist, wherein the antagonist and agonist are present within a single multilayer pharmaceutical unit.

A pharmaceutical composition comprising a pharmaceutical dosing unit consisting essentially of a multilayer bead comprising an antagonist and an agonist that are not in direct contact with one another.

A pharmaceutical composition comprising a plurality of pharmaceutically active units wherein each unit comprises an antagonist, an agonist, a seal coat, and a sequestering polymer wherein the antagonist and the agonist are not in direct contact with one another.

A pharmaceutical composition comprising a pharmaceutically inert support material, an antagonist in direct contact with the support material, a seal coat in direct contact with the antagonist and an agonist, and a sequestering polymer in direct contact with the agonist.

A pharmaceutical composition comprising an antagonist indirectly and fixably bound to an agonist such that physical disruption of the intact dosage form causes the antagonist and agonist to be admixed together.

The pharmaceutical composition of claim 31 wherein the amount of charge-neutralizing additive relative to the amount of sequestering polymer on a weight-by-weight basis is approximately 1%, approximately 1.5%, approximately 2%, approximately 2.5%, approximately 3%, approximately 3.5%, approximately 4%, approximately 4.5%, approximately 5%, approximately 5.5%, approximately 1-2%, approximately 2-3%, approximately 3-4% or approximately 4-5%.

A method for correlating the amount of naltrexone released from a pharmaceutical composition comprising naltrexone by measuring plasma levels of 6-beta-naltrexol.

A method for measuring the amount of antagonist or derivative thereof in a biological sample, the antagonist or derivative having been released from a pharmaceutical composition in vivo, the method comprising the USP paddle method at 37° C., 100 rpm, but further comprising incubation in a buffer containing a surfactant.

A method for preparing a pharmaceutical composition comprising adhering an antagonist to a pharmaceutically inert support material, coating the antagonist with a seal coat, coating the seal coat with an agonist, and coating the agonist with a sequestering polymer.

A multiple layer pharmaceutical composition comprising an agonist and an antagonist within distinct layers of the composition, wherein at least 90% of the antagonist is sequestered for at least 24 hours following administration to a human being.

A multiple layer pharmaceutical composition comprising an agonist and an antagonist within distinct layers of the composition, wherein at least 95% of the antagonist is sequestered for at least 24 hours following administration to a human being.

A pharmaceutical composition comprising naltrexone within a sequestering subunit and morphine in contact with the subunit but not the naltrexone, wherein administration of the composition to a human being results in the release of substantially all of the morphine from the composition but less than 10% of the naltrexone from the composition within 24 hours of administration.

A pharmaceutical composition comprising naltrexone within a sequestering subunit and morphine in contact with the subunit but not the naltrexone, wherein administration of the composition to a human being results in the release of substantially all of the morphine from the composition but less than 5% of the naltrexone from the composition within 24 hours of administration.