Technology for Preventing Abuse of Solid Dosage Forms

• US 20120321674A1
• Filed: 02/18/2012
• Published: 12/20/2012
• Est. Priority Date: 02/17/2011
• Status: Abandoned Application

• Current Assignee: Edward M. Rudnic, Michael Vachon
• Original Assignee: Edward M. Rudnic, Michael Vachon
• Inventors: Vachon, Michael, RUDNIC, Edward M.
• Application Number:
  US13/400,065
• Publication Number:
  US 20120321674A1
• Time in Patent Office: Days
• US Class Current: 424/400
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2081 with microcapsules or coated microparticles according to A61K9/50
• CPC Class Codes: A61K 9/284 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
• CPC Class Codes: A61K 9/2886 having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer of the type active core-drug layer-inactive layer A61K9/209
• CPC Class Codes: A61K 9/5073 having two or more different coatings optionally including drug-containing subcoatings

Abstract

Abuse resistant pharmaceutical formulations are provided that contain one or more abusable drugs and one or more abuse deterrent components. The abuse deterrent component(s) prevent the abusable drug(s) from being removed/extracted to an appreciable extent and/or rate. The abuse deterrent component(s) may be in the form of pellets, beads, beadlets, granules, powders, or the like, and may comprise a core that contains a material that is both hydrophilic and hydrophobic, and optionally a pH-dependent coating.

Claims

1. An abuse resistant pharmaceutical formulation comprising:

(a) one or more abusable drugs, and

(b) one or more abuse deterrent components, wherein each abuse deterrent component comprises;

(i) a core comprising one or more materials that are both hydrophilic and hydrophobic; and

(ii) optionally a coating;

wherein the one or more abuse deterrent components slows, reduces, or slows and reduces, extraction by aqueous or alcoholic liquids of the one or more abusable drugs from the formulation.

2. The abuse resistant pharmaceutical formulation of claim 1, wherein the one or more abusable drugs comprises one or more water soluble abusable drugs.

3. The abuse resistant pharmaceutical formulation of claim 1, wherein the one or more abusable drugs comprises one or more opioids.

4. The abuse resistant pharmaceutical formulation of claim 3, wherein the one or more opioids comprises morphine and oxycodone.

5. The abuse resistant formulation of claim 1, wherein the one or more abuse deterrent components is in a form selected from the group consisting of pellets, beads, beadlets, granules, powder, or a combination thereof.

6. The abuse resistant formulation of claim 1, wherein the one or more abuse deterrent components is in a ratio to the rest of the formulation of between about 1:

1 w/w and about 1;

5 w/w.

7. The abuse resistant formulation of claim 1, wherein the one or more abuse deterrent components is in a ratio to the one or more abusable drugs of between about 1:

1 w/w and about 1;

10 w/w.

8. The abuse resistant pharmaceutical formulation of claim 1, wherein the material that is both hydrophilic and hydrophobic is selected from the group consisting of polyacrylic acid, acrylic acid cross-linked with allyl ethers of polyalcohols, hydroxypropyl cellulose, hydroxypropyl methylcellulose:

hydroxypropyl cellulose mixture, polyvinylpyrrolidone, polyethylene oxide, methylcellulose, xanthan gum, guar gum, polyethylene glycol, methacrylic acid copolymer, colloidal silicon dioxide, cellulose gum, starch, sodium starch glycolate, sodium alginate, and combinations thereof.

9. The abuse resistant pharmaceutical formulation of claim 8, wherein the material that is both hydrophilic and hydrophobic is acrylic acid cross-linked with allyl ethers of polyalcohols.

10. The abuse resistant pharmaceutical formulation of claim 9, wherein the acrylic acid cross-linked with allyl ethers of polyalcohols is a carbomer.

11. The abuse resistant pharmaceutical formulation of claim 1, wherein the pH-sensitive coating comprises methacrylic acid copolymer dispersion, hypromellose acetate succinate, and cellulose acetate phthalate.

12. The abuse resistant pharmaceutical formulation of claim 1, further comprising an alkalizing agent.

13. The abuse resistant pharmaceutical formulation of claim 12, wherein the alkalizing agent is selected from the group consisting of polyplasdone XL, talc, meglumine, NaHCO₃, and polyvinylpyrrolidone.

14. The abuse resistant pharmaceutical formulation of claim 13, wherein the alkalizing agent is meglumine.

15. The abuse resistant pharmaceutical formulation of claim 12, wherein the alkalizing agents is in a form selected from the group consisting of pellets, beads, beadlets, granules, powder, or a combination thereof.

16. The abuse resistant pharmaceutical formulation of claim 11, wherein the one or more alkalizing agents is in a ratio to the one or more abuse deterrent components of about 40:

60 w/w to about 80;

20 w/w.

17. The abuse resistant pharmaceutical formulation of claim 1 further comprising a plasticizer.

18. The abuse resistant pharmaceutical formulation of claim 1, wherein the formulation is immediate release, controlled release, or a combination thereof.

19. A method of reducing the amount of abusable drug that can be extracted by aqueous or alcoholic liquids from a pharmaceutical formulation that comprises said abusable drug, wherein the method comprises admixing the abusable drug with one or more abuse deterrent components, each abuse deterrent component comprising (a) a core comprising one or more materials that are both hydrophilic and hydrophobic;

and (b) optionally a coating.

20. A method of reducing the rate at which an abusable drug can be extracted by aqueous or alcoholic liquids from a pharmaceutical formulation that comprises said abusable drug, wherein the method comprises admixing the abusable drug with one or more abuse deterrent components, each abuse deterrent component comprising:

(a) a core comprising one or more materials that are both hydrophilic and hydrophobic; and

(b) optionally a coating.