METHODS AND COMPOSITIONS FOR DETERRING ABUSE

• US 20110077238A1
• Filed: 09/29/2010
• Published: 03/31/2011
• Est. Priority Date: 09/30/2009
• Status: Active Grant

• Current Assignee: Acura Pharmaceuticals Incorporated (Abuse Deterrent Pharma LLC)
• Original Assignee: Acura Pharmaceuticals Incorporated (Abuse Deterrent Pharma LLC)
• Inventors: LEECH, Ronald L., HALL YUNG, Rachelle L., BRZECZKO, Albert W.
• Granted Patent: US 8,901,113 B2
• Time in Patent Office: Days
• US Class Current: 514/220
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/4458 only substituted in position 2, e.g. methylphenidate
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/5517 condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• 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 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• 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 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2059 Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
• CPC Class Codes: A61K 9/2072 characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms A61K9/0004, A61K9/0056, A61K9/0065 take precedence
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/30 for treating abuse or dependence
• CPC Class Codes: A61P 39/00 : General protective or antinoxious agents

Abstract

Effective methods and compositions to deter abuse of pharmaceutical products (e.g., orally administered pharmaceutical products) including but not limited to immediate release, sustained or extended release and delayed release formulations for drugs subject to abuse comprising at least 10% by weight hydroxypropylcellulose; polyethylene oxide; and a disintegrant selected from the group consisting of crospovidone, sodium starch glycolate and croscarmellose sodium; wherein the ratio of hydroxypropylcellulose to polyethylene oxide on a weight basis is between about 10:1 and 1:10.

Claims

1. A therapeutic composition comprising:

a drug susceptible to abuse;

at least 10% by weight hydroxypropylcellulose;

polyethylene oxide; and

a disintegrant selected from the group consisting of crospovidone, sodium starch glycolate and croscarmellose sodium;

wherein the ratio of hydroxypropylcellulose to polyethylene oxide on a weight basis is between about 10;

1 and 1;

10.

2. The therapeutic composition of claim 1, wherein the composition comprises an immediate release formulation.

3. The therapeutic composition of claim 1, wherein the drug susceptible to abuse comprises one or more of alfentanil, amphetamines, buprenorphine, butorphanol, carfentanil, codeine, dezocine, diacetylmorphine, dihydrocodeine, dihydromorphine, diphenoxylate, diprenorphine, etorphine, fentanyl, hydrocodone, hydromorphone, β

-hydroxy-3-methyl fentanyl, levo-α

-acetylmethadol, levorphanol, lofentanil, meperidine, methadone, methylphenidate, morphine, nalbuphine, nalmefene, o-methylnaltrexone, naloxone, naltrexone, oxycodone, oxymorphone, pentazocine, pethidine, propoxyphene, remifentanil, sufentanil, tilidine and tramodol.

4. The therapeutic composition of claim 1, wherein the hydroxypropylcellulose has a viscosity of about 1,500 mPa·

s to about 3,000 mPa·

s at 1%.

5. The therapeutic composition of claim 1, wherein the hydroxypropylcellulose has a molecular weight of about 1,150,000.

6. The therapeutic composition of claim 1, comprising ethylcellulose.

7. The therapeutic composition of claim 6, wherein the ethylcellulose includes an ethoxyl content of about 45% to about 52%.

8. The therapeutic composition of claim 1, wherein the polyethylene oxide is present in an amount of about 3 wt % to about 7 wt %.

9. The therapeutic composition of claim 1, wherein the polyethylene oxide is present in an amount of about 5.10 wt %.

10. The therapeutic composition of claim 1, wherein the crospovidone is present in an amount of about 15 wt % to about 25 wt %.

11. The therapeutic composition of claim 1, wherein the crospovidone is present in an amount of about 18 wt % to about 22 wt %.

12. The therapeutic composition of claim 1, wherein the crospovidone is present in an amount of about 20.41 wt %.

13. The therapeutic composition of claim 1, further comprising a glidant.

14. The therapeutic composition of claim 12, wherein the glidant comprises colloidal silicon dioxide.

15. The therapeutic composition of claim 1, further comprising a lubricant.

16. The therapeutic composition of claim 14, wherein the lubricant comprises magnesium stearate.

17. The therapeutic composition of claim 1, wherein the composition is a suppository, capsule, caplet, pill, gel, soft gelatin capsule, or compressed tablet form.

18. The therapeutic composition of claim 1, wherein the composition is in unit dose foam.

19. A therapeutic composition comprising:

a drug susceptible to abuse;

at least 10% by weight hydroxypropylcellulose;

ethylcellulose;

polyethylene oxide; and

a disintegrant selected from the group consisting of crospovidone, sodium starch glycolate and croscarmellose sodium;

wherein the ratio of hydroxypropylcellulose to polyethylene oxide on a weight basis is between about 10;

1 and 1;

10.

20. The therapeutic composition of claim 19, wherein the ethylcellulose has a viscosity of about 70 mPa·

s or less.

21. The therapeutic composition of claim 19, wherein the ethylcellulose has a standard ethoxyl content.

22. The therapeutic composition of claim 19, wherein the ethylcellulose has a high ethoxyl content.

23. The therapeutic composition of claim 19, wherein the ethylcellulose has a medium ethoxyl content.

24. A composition suitable for reducing the chemical conversion of precursor compounds included in the composition to a drug susceptible to abuse comprising:

a precursor compound that can be used in a chemical synthesis of a drug that is susceptible to abuse;

at least 10% by weight hydroxypropylcellulose;

ethylcellulose;

polyethylene oxide; and

a disintegrant selected from the group consisting of crospovidone, sodium starch glycolate and croscarmellose sodium;

wherein the ratio of hydroxypropylcellulose to polyethylene oxide on a weight basis is between about 10;

1 and 1;

10.

25. The composition of claim 24, wherein the precursor compound comprises pseudoephedrine.

26. The composition of claim 24, wherein the composition is an immediate release composition.

27. The therapeutic composition of claim 24, wherein the ethylcellulose has a viscosity of about 70 mPa·

s or less.

28. The therapeutic composition of claim 24, wherein the ethylcellulose has a standard ethoxyl content.

29. The therapeutic composition of claim 24, wherein the ethylcellulose has a high ethoxyl content.

30. The therapeutic composition of claim 24, wherein the ethylcellulose has a medium ethoxyl content.

31. A composition suitable for reducing the chemical conversion of precursor compounds included in the composition to a drug susceptible to abuse comprising:

a precursor compound that can be used in a chemical synthesis of a drug that is susceptible to abuse;

at least 10% by weight hydroxypropylcellulose;

ethylcellulose; and

polyethylene oxide.

32. The composition of claim 31, further comprising a disintegrant selected from the group consisting of crospovidone, sodium starch glycolate and croscarmellose sodium.

33. The composition of claim 31, wherein the ratio of hydroxypropylcellulose to polyethylene oxide on a weight basis is between about 10:

1 and 1;

10.

34. The therapeutic composition of claim 31, wherein the ethylcellulose has a viscosity of about 70 mPa·

s or less.

35. The therapeutic composition of claim 31, wherein the ethylcellulose has a standard ethoxyl content.

36. The therapeutic composition of claim 31, wherein the ethylcellulose has a high ethoxyl content.

37. The therapeutic composition of claim 31, wherein the ethylcellulose has a medium ethoxyl content.

38. The therapeutic composition of claim 31, wherein the composition comprises an immediate release formulation.

39. The therapeutic composition of claim 31, wherein the composition comprises a controlled release formulation.

40. The therapeutic composition of claim 31, wherein the composition comprises an extended release formulation.