COMPOSITIONS AND METHODS FOR CONTROLLING ABUSE OF MEDICATIONS

• US 20070020339A1
• Filed: 07/20/2006
• Published: 01/25/2007
• Est. Priority Date: 07/20/2005
• Status: Abandoned Application

• Current Assignee: Pharmorx, Inc.
• Original Assignee: Pharmorx, Inc.
• Inventors: Bear, David
• Application Number:
  US11/458,890
• Publication Number:
  US 20070020339A1
• Time in Patent Office: Days
• US Class Current: 424/490
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/2081 with microcapsules or coated microparticles according to A61K9/50
• CPC Class Codes: A61K 9/5078 with drug-free core
• CPC Class Codes: A61K 9/5084 Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs tablets containing such a mixture A61K9/2077

Abstract

Pharmaceutical dosage forms are provided for use in deterring abuse of opioids or other medications, which help avoid harm to a patient dependent on the medication. In one case, a pharmaceutical oral dosage form is provided that includes a plurality of microcapsules, each microcapsule of the plurality containing an opioid agonist medication in a controlled release form, and a partial opioid agonist sequestered in the pharmaceutical dosage form, such that upon oral administration of the pharmaceutical oral dosage form the partial opioid agonist will pass through the gastrointestinal tract without uptake by the body.

Claims

1. A pharmaceutical dosage form comprising:

a first plurality of microcapsules, each microcapsule of the first plurality containing an opioid agonist medication in a controlled release form; and

a second plurality of microcapsules, each microcapsule of the second plurality containing a partial opioid agonist,

wherein the partial opioid agonist is provided in a sequestered form in the pharmaceutical dosage form, such that the partial opioid agonist is released in an effective amount in vivo if the pharmaceutical dosage form is administered to a person in an altered form but is not released in an effective amount in vivo if the pharmaceutical dosage form is administered to a person in a substantially unaltered form.

2. The pharmaceutical dosage form of claim 1, wherein the opioid agonist medication comprises oxycodone, hydromorphone, hydrocodone, or a combination thereof.

3. The pharmaceutical dosage form of claim 1, wherein the partial opioid agonist comprises buprenorphine.

4. The pharmaceutical dosage form of claim 1, wherein the microcapsules of the first plurality and of the second plurality have the same specific density.

5. The pharmaceutical dosage form of claim 1, wherein the microcapsules of the first plurality and of the second plurality have the same flocculation characteristics.

6. The pharmaceutical dosage form of claim 1, wherein the microcapsules of the first plurality and of the second plurality have the same color, size, and textural appearance.

7. The pharmaceutical dosage form of claim 1, wherein the microcapsules of the first plurality further comprise one or more matrix materials.

8. The pharmaceutical dosage form of claim 7, wherein matrix material comprises a hydrophobic and/or amphiphilic compound.

9. The pharmaceutical dosage form of claim 7, wherein matrix material comprises a bioerodible or biodegradable polymer.

10. The pharmaceutical dosage form of claim 1, which comprises a tablet or capsule suitable for oral administration.

11. The pharmaceutical dosage form of claim 1, wherein the microcapsules of the second plurality comprise a non-degradable layer covering the partial opioid agonist.

12. The pharmaceutical dosage form of claim 1, wherein the microcapsules of the first plurality and of the second plurality are mixed together within a unit dose form.

13. A pharmaceutical oral dosage form comprising:

a plurality of microcapsules, each microcapsule of the plurality containing an opioid agonist medication in a controlled release form; and

a partial opioid agonist sequestered in the pharmaceutical dosage form, such that upon oral administration of the pharmaceutical oral dosage form the partial opioid agonist will pass through the gastrointestinal tract without uptake by the body.

14. The pharmaceutical oral dosage form of claim 13, wherein the first opioid agonist medication comprises oxycodone, hydromorphone, hydrocodone, or a combination thereof.

15. The pharmaceutical dosage form of claim 14, wherein the partial opioid agonist comprises buprenorphine.

16. The pharmaceutical dosage form of claim 13, wherein the partial opioid agonist is covered by a non-degradable layer.

17. A pharmaceutical oral dosage form comprising:

opioid agonist medication particles coated by or dispersed in a degradable matrix material which provides controlled release in vivo; and

partial opioid agonist coated by or dispersed in a non-degradable material.