Abuse resistant pharmaceutical compositions
The present invention relates to a composition comprising pharmaceutical active ingredients which are susceptible to, or have potential for, abuse. The invention provides an oral pharmaceutical composition comprising a first population of beads and a second population of beads. The first bead population comprises a pharmaceutically active ingredient susceptible to, or having the potential for, abuse. The second bead population comprises a gelling agent and a coating substantially surrounding the gelling agent, but containing no pharmaceutically active ingredient. The first bead population and the second bead population are physically separable, but visually indistinguishable to the naked eye. Upon ingress of water into the second population of beads, the gelling agent is caused to swell forming a viscous mass inhibiting or preventing the extraction of the active ingredient.
1. An oral pharmaceutical composition comprising:
a first population of beads comprising hydrocodone or a pharmaceutically acceptable salt thereof, wherein the first population of beads is substantially free of polyethylene oxide; and
a second population of beads comprising polyethylene oxide and a permeable or semi-permeable coating, wherein the second population of beads is substantially free of any pharmaceutically active ingredient.
2. The composition according to claim 1 , wherein the second population of beads further comprises povidone.
3. The composition according to claim 2 , wherein the polyethylene oxide is present in particulate form.
4. The composition according to claim 1 , wherein the hydrocodone is hydrocodone bitartrate.
5. The composition according to claim 4 , wherein the hydrocodone bitartrate is present in an amount of from 5 to 250 mg.
6. The composition according to claim 1 , wherein the permeable or semi-permeable coating is a cellulose acetate, cellulose alkanylate, cellulose acrylate, polyamides, polyurethane, sulfonated polystyrene, ammonio methacrylate copolymer, methacrylic acid copolymer, or a mixture thereof.
7. The composition according to claim 1 , wherein the composition produces a diffuse gel of substantially uniform viscosity when mixed in 200 ml of water.
8. The composition according to claim 1 , wherein the hydrocodone, or a pharmaceutically acceptable salt thereof, that is extractable from the composition when mixed in 200 ml of water is about 23%.
9. An oral pharmaceutical composition comprising:
a population of immediate release beads comprising hydrocodone bitartrate that is substantially free of polyethylene oxide;
a population of controlled release beads comprising hydrocodone bitartrate that is substantially free of polyethylene oxide; and
a population of beads comprising polyethylene oxide and a permeable or semi-permeable coating that is substantially free of any pharmaceutically active ingredient.
10. The composition according to claim 9 , wherein the immediate release beads comprise from 1 to 75% w/w of the total amount of hydrocodone bitartrate in the composition, and the controlled release beads comprise from 25 to 99% w/w of the total amount of hydrocodone bitartrate in the composition.
11. The composition according to claim 9 , wherein the permeable or semi-permeable coating is a cellulose acetate, cellulose alkanylate, cellulose acrylate, polyamides, polyurethane, sulfonated polystyrene, ammonio methacrylate copolymer, methacrylic acid copolymer, or a mixture thereof.
12. The composition according to claim 9 , wherein the composition produces a diffuse gel of substantially uniform viscosity when mixed in 200 ml of water.
13. The composition according to claim 9 , wherein the hydrocodone bitartrate that is extractable from the composition when mixed in 200 ml of water is about 23%.
14. A unit dosage form comprising a composition according to claim 1 in the form of a capsule or a tablet.
15. The unit dosage form according to claim 14 , in the form of a capsule, wherein the capsule comprises at least about 20 mg of polyethylene oxide.
16. The unit dosage form comprising a composition according to claim 14 , in the form of a capsule or a tablet.
17. The unit dosage form according to claim 16 , in the form of a capsule, wherein the capsule comprises at least about 20 mg of polyethylene oxide.
18. The unit dosage form according to claim 14 , wherein the unit dosage form produces a diffuse gel of substantially uniform viscosity when mixed in 200 ml of water.
19. The unit dosage form according to claim 14 , wherein the hydrocodone, or a pharmaceutically salt thereof, that is extractable from the composition when mixed in 200 ml of water is about 23%.
20. A method for the treatment of pain comprising administering to a subject in need thereof an oral pharmaceutical composition comprising a first population of beads comprising hydrocodone or a pharmaceutically acceptable salt thereof, wherein the first population of beads is substantially free of polyethylene oxide; and a second population of beads comprising polyethylene oxide and a permeable or semi-permeable coating, wherein the second population of beads is substantially free of any pharmaceutically active ingredient.
21. The method according to claim 20 , wherein the second population of beads does not interfere with the in vivo release and bioavailability of the hydrocodone as compared to an oral pharmaceutical composition without the second population of beads comprising polyethylene oxide.
22. The method according to claim 20 , wherein the permeable or semi-permeable coating is a cellulose acetate, cellulose alkanylate, cellulose acrylate, polyamides, polyurethane, sulfonated polystyrene, ammonio methacrylate copolymer, methacrylic acid copolymer, or a mixture thereof.
23. A method for the treatment of pain comprising administering to a subject in need thereof an oral pharmaceutical composition comprising a population of immediate release beads comprising hydrocodone bitartrate that is substantially free of polyethylene oxide, a population of controlled release beads comprising hydrocodone bitartrate that is substantially free of polyethylene oxide, and a population of beads comprising polyethylene oxide and a permeable or semi-permeable coating that is substantially free of any pharmaceutically active ingredient.
24. The method according to claim 23 , wherein the population of beads comprising polyethylene oxide does not interfere with the in vivo release and bioavailability of the hydrocodone as compared to the oral pharmaceutical composition without the population of beads comprising polyethylene oxide.
25. The method according to claim 23 , wherein the permeable or semi-permeable coating is a cellulose acetate, cellulose alkanylate, cellulose acrylate, polyamides, polyurethane, sulfonated polystyrene, ammonio methacrylate copolymer, methacrylic acid copolymer, or a mixture thereof.