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US 2008/0166405 A1Published application
Abuse-resistant oral dosage forms and method of use thereof
OwnerAtul M. Mehtainventor
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Abstract
An opioid-antagonist oral dosage form which does not release a therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, but whereby a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist. An embodiment of the oral dosage form includes an opioid-antagonist layer coated onto a biologically inert pellet, and a non-releasing membrane coated onto the opioid-antagonist layer. Optionally, the oral dosage form can also include an opioid agonist, such that a method of preventing the abuse of an oral dosage form of an opioid agonist is provided by forming the oral dosage form including an opioid agonist and an opioid antagonist.
Claims43
An oral dosage form comprising:
- a biologically inert pellet;
- an opioid-antagonist layer coated on the biologically inert pellet, wherein the opioid-antagonist layer comprises a therapeutically effective amount of an opioid antagonist;
- and
- a non-releasing membrane coated on the opioid-antagonist layer, wherein the non-releasing membrane comprises a water-retardant polymer which is a non-ionic poly(ethyl acrylate-co-methyl methacrylate) 2:1, wherein 2:1 indicates the molar proportions of the ethyl acrylate and methyl methacrylate monomer units, respectively;
- wherein the oral dosage form does not release the therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, and wherein a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist.
2 more elements
An oral dosage form including:
- a first pellet comprising:
- a biologically inert pellet;
- an opioid-antagonist layer coated on the biologically inert pellet, wherein the opioid-antagonist layer comprises a therapeutically effective amount of an opioid antagonist;
- and
- a non-releasing membrane coated on the opioid-antagonist layer, wherein the non-releasing membrane comprises a water-retardant polymer which is a non-ionic poly(ethyl acrylate-co-methyl methacrylate) 2:1, wherein 2:1 indicates the molar proportions of the ethyl acrylate and methyl methacrylate monomer units, respectively;
- wherein the oral dosage form does not release the therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, and wherein a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist;
- and
- a second pellet comprising an opioid agonist.
5 more elements
An oral dosage form comprising:
- an opioid-antagonist formulation, wherein the opioid-antagonist formulation comprises a therapeutically effective amount of an opioid antagonist;
- and
- a non-releasing membrane coated on the opioid-antagonist layer, wherein the non-releasing membrane comprises a water-retardant polymer which is a non-ionic poly(ethyl acrylate-co-methyl methacrylate) 2:1, wherein 2:1 indicates the molar proportions of the ethyl acrylate and methyl methacrylate monomer units, respectively;
- wherein the oral dosage form does not release the therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, and wherein a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist.
1 more element
A method of preventing the abuse of an oral dosage form of an opioid agonist, comprising:
- coating a non-releasing membrane onto an opioid-antagonist formulation, and coating an opioid-agonist layer onto the non-releasing membrane to form an oral dosage form;
- wherein the opioid-antagonist formulation comprises a therapeutically effective amount of an opioid antagonist, wherein the non-releasing membrane comprises a water-retardant polymer which is a non-ionic poly(ethyl acrylate-co-methyl methacrylate) 2:1, wherein 2:1 indicates the molar proportions of the ethyl acrylate and methyl methacrylate monomer units, respectively, and wherein the opioid-agonist layer comprises an opioid agonist;
- wherein the oral dosage form does not release the therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, and wherein a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist.
A method of preventing the abuse of an oral dosage form of an opioid agonist, comprising:
- forming an oral dosage form by combining:
- a first pellet comprising an opioid agonist;
- and
- a second pellet comprising:
- a biologically inert pellet;
- an opioid-antagonist layer coated on the biologically inert pellet, wherein the opioid-antagonist layer comprises a therapeutically effective amount of an opioid antagonist;
- and
- a non-releasing membrane coated on the opioid-antagonist layer, wherein the non-releasing membrane comprises a water-retardant polymer which is a non-ionic poly(ethyl acrylate-co-methyl methacrylate) 2:1, wherein 2:1 indicates the molar proportions of the ethyl acrylate and methyl methacrylate monomer units, respectively;
- wherein the oral dosage form does not release the therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, and wherein a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist.
6 more elements
Dependencies are inferred from the claim text.