PHARMACEUTICAL COMPOSITION WHICH REDUCES OR ELIMINATES DRUG ABUSE POTENTIAL

• US 20090060848A1
• Filed: 11/03/2008
• Published: 03/05/2009
• Est. Priority Date: 04/30/2001
• Status: Abandoned Application

• Current Assignee: Russell Somma, Yatindra Joshi
• Original Assignee: Russell Somma, Yatindra Joshi
• Inventors: Somma, Russell, Joshi, Yatindra
• Application Number:
  US12/263,790
• Publication Number:
  US 20090060848A1
• Time in Patent Office: Days
• US Class Current: 424/10.100
• 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 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• 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 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• 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 9/205 Polysaccharides, e.g. alginate, gums; Cyclodextrin
• CPC Class Codes: A61K 9/2063 Proteins, e.g. gelatin
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds
• CPC Class Codes: A61P 25/30 for treating abuse or dependence

Abstract

A pharmaceutical composition which reduces or eliminates the drug abuse potential of central nervous system stimulant comprising: (a) a drug selected from the group consisting of methylphenidate, amphetamine, methamphetamine, and combinations thereof; and (b) a gel forming polymer wherein the gel forming polymer is a polymer that forms a gel when contacted with moisture or placed in an aqueous solution. The present invention is based on the discovery that a central nervous system stimulant such as methylphenidate in combination with a gel forming polymer reduces or eliminates drug abuse potential by swelling in the presence of moisture, and thus, preventing nasal absorption and injectability of the drug.

Claims

1. A pharmaceutical composition which reduces or eliminates the drug abuse potential of central nervous system stimulant comprising:

(a) a drug selected from the group consisting of methylphenidate, amphetamine, methamphetamine, and combinations thereof; and

(b) a gel forming polymer wherein the gel forming polymer is a polymer that forms a gel when contacted with moisture or placed in an aqueous solution.

2. The composition according to claim 1 wherein the gel forming polymer is selected from the group consisting of a polysaccharide, gelatin, polyglucosamine, hydrophilic colloid, crosslinkable hydrophilic polymer, an acrylate ester polymerized with a monomer selected from the group consisting of a vinyl-substituted heterocyclic compound containing at least one of a nitrogen or a sulfur atom, (meth)acrylamide, a mono- or di-C₁-C₄ alkylamino C₁-C₄ alkyl (meth)acrylate, and a mono or di-C₁-C₄ alkylamino C₁-C₄ alkyl acrylamide, and combinations thereof.

3. The composition according to claim 2 wherein the polysaccharide is selected from the group consisting of an agar, carrageenan, modified cellulose, and starch.

4. The composition according to claim 3 wherein the polysaccharide is selected from the group consisting of hydroxyethylcellulose, hydroxypropylmethylcellulose, sodium carboxymethyl cellulose, hydroxypropyl methyl cellulose phthalate or acetate succinate, cellulose acetate phthalate, methyl cellulose phthalate, microcrystalline cellulose, a cold water swelling starch, sodium carboxymethyl starch, and starch acetate phthalate.

5. The composition according to claim 2 wherein the hydrophilic colloid is a derivative of alginic acid.

6. The composition according to claim 5 wherein the derivative of alginic acid is selected from the group consisting of calcium alginate, sodium alginate, potassium alginate, and propylene glycol alginate.

7. The composition according to claim 2 wherein the crosslinkable hydrophilic polymer is selected from the group consisting of polyvinyl pyrrolidone, carboxymethylamide, potassium methacrylatedivinylbenzene, polyvinylalcohol, polyoxyethyleneglycol, polyethylene glycol, carboxypolymethylene, polyacrylic acid, polymethacrylic acid, polyvinyl pyrrolidone/acrylic acid, polymethyl vinyl ether/maleic anhydride, polyethylene/maleic anhydride, polymethyl methacrylate, polyethyl methacrylate, polybutyl methacylate, polyisobutyl methacrylate, polyhexyl methacrylate, polyisodecyl methacrylate, polylauryl methacrylate, polyphenyl methacrylate, polymethyl acrylate, polyisopropyl acrylate, polyisobutyl acrylate, polyoctadecyl acrylate, copolymer of acrylic and methacrylic acid ester with a lower ammonium group content, copolymer of acrylic and methacrylic acid ester and trimethyl ammonium methacrylate, polyvinyl acetate, polyvinyl acetate phthalate, maleic acid anhydride-vinyl methyl ether, styrene-maleic acid, 2-ethyl-hexyl-acrylate maleic acid anhydride, crotonic acid-vinyl acetate, glutaminic acid/glutamic acid ester, polyarginine, polyethylene, polypropylene, polyethylene oxide, polyethylene terephthalate, polyvinyl isobutyl ether, polyvinyl chloride, polyurethane, and vinyl pyrrolidone/dimethylamino ethyl methacrylate.

8. The composition according to claim 2 wherein the acrylate ester is polymerized with a monomer selected from the group consisting of N,N-dimethylamino ethyl methacrylate, N,N-diethylamino ethyl acrylate, N,N-diethylamino ethyl methacrylate, N-t-butylamino ethyl acrylate, N-t-butylamino ethyl methacrylate, N,N-dimethylamino propyl acrylamide, N,N-dimethylamino propyl methacrylamide, N,N-diethylamino propyl acrylamide, and N,N-diethylamino propyl methacrylamide.

9. The composition according to claim 2 wherein the gel forming polymer is selected from the group consisting of polyethylene oxide, sodium alginate, a homopolymer of acrylic acid crosslinked with allyl sucrose or allylpentaerythritol, and a copolymer of acrylic acid and an alkyl acrylate and crosslinked with allylpentaerythritol, wherein the alkyl group has from 10 to 30 carbon atoms.

10. The composition according to claim 1 wherein the gel forming polymer has a molecular weight of from about 70,000 to about 2,000,000.

11. The composition according to claim 10 wherein the gel forming polymer has a molecular weight of from about 100,000 to about 1,000,000.

12. The composition according to claim 1 wherein the gel forming polymer is not crosslinked.

13. The composition according to claim 1 wherein the gel forming polymer is crosslinked.

14. The composition according to claim 1 which additionally comprises a pH modifier.

15. The composition according to claim 14 wherein the pH modifier is selected from the group consisting of sodium hydroxide, calcium hydroxide, calcium carbonate, diethyl carbonate, diphenyl carbonate, and combinations thereof.

16. The composition according to claim 1 wherein the gel forming polymer is present in an amount of from about 2 to about 40 weight percent, based on the total weight of the composition.

17. The composition according to claim 16 wherein the gel forming polymer is present in an amount of from about 10 to about 20 weight percent, based on the total weight of the composition.

18. The composition according to claim 1 wherein the central nervous system stimulant is present in an amount of from about 0.1 to about 90 weight percent, based on the total weight of the composition.

19. The composition according to claim 18 wherein the central nervous system stimulant is present in an amount of from about 1 to about 50 weight percent, based on the total weight of the composition.

20. The composition according to claim 19 wherein the central nervous system stimulant is present in an amount of from about 2 to about 10 weight percent, based on the total weight of the composition.

21. The composition according to claim 1 which is in a form selected from the group consisting of powder, granules, solution, suspension, emulsion, and combinations thereof.

22. The composition according to claim 1 which is in a form of a solid.

23. The composition according to claim 22 wherein the composition is administered in a form selected from the group consisting of a capsule, cachet, and tablet.