ABUSE-RESISTANT OPIOID DOSAGE FORM

• US 20130209561A1
• Filed: 02/21/2013
• Published: 08/15/2013
• Est. Priority Date: 05/11/2001
• Status: Abandoned Application

• Current Assignee: Purdue Pharma L.P.
• Original Assignee: Endo Pharmaceuticals Incorporated (Endo International PLC)
• Inventors: Kao, Huai-Hung, Zeng, Yadi, Howard-Sparks, Michelle, Jim, Fai
• Application Number:
  US13/773,123
• Publication Number:
  US 20130209561A1
• Time in Patent Office: Days
• US Class Current: 424/471
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/1635 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer
• CPC Class Codes: A61K 9/282 Organic compounds, e.g. fats
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/36 Opioid-abuse
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

We provide a pharmaceutical dosage form including an opioid antagonist surrounded by a controlled release matrix and an opioid agonist in a surrounding matrix.

Claims

1. A pharmaceutical dosage form comprising an opioid antagonist surrounded by a controlled release matrix and an opioid agonist in a surrounding matrix.

2. pharmaceutical dosage form of claim 1, Wherein the opioid antagonist is selected from the group consisting of naloxone, naltrexone, nalorphine, diprenorphine, levallorphan, pentazocine, metazocine, cyclazocine, etazocine, N-cyclopropylmethyl -7,8-dihydro-14-hydroxynormophinone, 21-cyclopropyl-z,-(1-hydroxy-1-methylethyl)-6,14-endo-ethano-tetrahydrooripavine, 21-cyclopropyl-z,-(1-hydroxy-1-methylethyl)-6,14-endo-ethano-tetrahydrodiphenorphine and pharmaceutically acceptable addition salts thereof;

and the opioid agonist is selected from the group consisting of codeine, dihydrocodeine, hydrocodone, hydromorphone, levorphanol, meperidine, buprenorphine, fentanyl, fentanyl derivatives, dipipanone, heroin, tramadol, etorphine, dihydroetorphine, butorphanol, methadone, morphine, oxycodone, oxymorphone, propoxyphene and pharmaceutically acceptable salts thereof.

3. The pharmaceutical dosage form of claim 2, wherein the opioid antagonist surrounded by a controlled release matrix is in the form of a granule.

4. The pharmaceutical dosage form of claim 3, wherein the opioid antagonist surrounded by a controlled release matrix is located in the center of the pharmaceutical dosage form.

5. The pharmaceutical dosage form of claim 4, wherein the surrounding matrix releases the opioid agonist in a patient body and the dosage form is eliminated from the patient body prior to release of the opioid antagonist surrounded by a controlled release matrix when the pharmaceutical dosage form is administered intact to the patient body.

6. The pharmaceutical dosage form of claim 5, wherein the surrounding matrix comprises at least one selected from the group consisting of a cellulose, a quaternary ammonium acrylic polymer, a quaternary ammonium methacrylic polymer, an acrylic ester copolymer and a methacrylic ester copolymer.

7. The pharmaceutical dosage form of claim 6 which is a tablet.

8. The pharmaceutical dosage form of claim 4, wherein the surrounding matrix releases the opioid agonist in a patient body and the dosage form releases a therapeutically ineffective amount of the opioid antagonist surrounded by a controlled release matrix in the patient body when the pharmaceutical dosage form is administered intact to the patient body.

9. The pharmaceutical dosage form of claim 8, wherein the surrounding matrix comprises at least one selected from the group consisting of a cellulose, a quaternary ammonium acrylic polymer, a quaternary ammonium methacrylic polymer, an acrylic ester copolymer and a methacrylic ester copolymer.

10. The pharmaceutical dosage form of claim 9 which is a tablet.