ABUSE-DETERRENT CONTROLLED RELEASE FORMULATIONS

• US 20150283087A1
• Filed: 04/06/2015
• Published: 10/08/2015
• Est. Priority Date: 04/07/2014
• Status: Active Grant

• Current Assignee: Patheon Softgels, Inc. (Thermo Fisher Scientific Incorporated)
• Original Assignee: Banner Life Sciences, LLC (Thermo Fisher Scientific Incorporated)
• Inventors: Vamvakas, George, Fatmi, Aqeel A.
• Granted Patent: US 10,182,992 B2
• Time in Patent Office: Days
• US Class Current: 1/1
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/485 Inorganic compounds
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds
• CPC Class Codes: A61K 9/4875 Compounds of unknown constitution, e.g. material from plants or animals oils, fats, waxes, shellac A61K9/4858

Abstract

Described herein are abuse deterrent controlled release oral pharmaceutical compositions comprising and methods for making the same. In particular, an abuse deterrent controlled release oral pharmaceutical composition comprising a soft capsule and an abuse deterrent controlled release matrix comprising an active pharmaceutical ingredient are described.

Claims

1. An abuse deterrent oral pharmaceutical composition comprising a tamper resistant controlled release matrix comprising:

(a) at least one lipid or lipophilic vehicle;

(b) at least one hydrophilic polymer;

(c) at least one hygroscopic polymer; and

(d) at least one active pharmaceutical ingredient;

wherein the matrix is resistant to tampering and is encapsulated in a soft capsule shell.

2. The composition of claim 1, further comprising

(e) at least one suspension agent.

3. The composition of claim 1 wherein the lipid or lipophilic vehicle comprises about 25% to about 90% of the total matrix mass.

4. The composition of claim 1, wherein the at least one hygroscopic polymer comprises from about 1% to about 10% of the total matrix mass.

5. The composition of claim 1, wherein the at least one hydrophilic polymer comprises about 5% to about 17% of the total matrix mass.

6. The composition of claim 1, wherein the at least one active pharmaceutical ingredient comprises about 1% to about 50% of the total matrix mass.

7. The composition of claim 1, wherein the ratio of the active pharmaceutical ingredient percent mass to the matrix percent mass is about 1:

100 to about 1;

1.

8. The composition of claim 1, wherein the lipid or lipophilic vehicle comprises at least one liquid lipid or lipophilic vehicle and at least one semisolid lipid or lipophilic vehicle.

9. The composition of claim 1, wherein the liquid lipid or lipophilic vehicle comprises:

olive oil, sunflower oil, canola oil, palmitoleic acid, oleic acid, myristoleic acid, linoleic acid, arachidonic acid, paraffin oil, or mineral oil.

10. The composition of claim 1, wherein the lipid or lipophilic vehicle comprises olive oil or soybean oil.

11. The composition of claim 1, wherein the semisolid lipid or lipophilic vehicle comprises one or more of:

polyethylene glycol glyceride ester, paraffin wax, or bee'"'"'s wax.

12. The composition of claim 1, wherein the lipid or lipophilic vehicle comprises soybean oil, a polyethylene glycol glyceride ester, and bee'"'"'s wax.

13. The composition of claim 1, wherein the polyethylene glycol glyceride esters comprises glycerol esters of saturated fatty acids of about 8 to about 18 carbon molecules in length.

14. The composition of claim 1, wherein the lipid or lipophilic vehicle comprises about 48% to about 52% of the total matrix mass.

15. The composition of claim 14, wherein the hygroscopic polymer comprises one or more of:

polyvinylpyrrolidone, copovidone, hydroxypropylmethylcellulose, hydroxypropylcellulose, ethyl cellulose, methylcellulose, or polyethylene oxide.

16. The composition of claim 1, wherein the hygroscopic polymer comprises polyvinylpyrrolidone having a K value from about 70 to about 90.

17. The composition of claim 1, wherein the hydrophilic polymer comprises:

polyhydroxylalkylenediamine, dimethylaminoethyl methacrylate copolymer, sodium carboxy methylcellulose, ethylenediamine, sodium alginate, carbomers, poly galacturonic acid, or acrylic methacrylate copolymers.

18. The composition of claim 1, wherein the active pharmaceutical ingredient comprises at least one of:

oxycodone, morphine, morphine analogues, or morphine antagonists, tapentadol, codeine, morphine, methadone, fentanyl and analogs, opioid pain relievers;

oxycodone hydrochloride, hydrocodone bitartrate, hydromorphone, oxymorphone, meperidine, propoxyphene, flunitrazepam, barbiturates, amytal, nembutal, seconal, phenobarbital;

benzodiazepines, zolpidem, zaleplon, eszopiclone, amphetamines, methylphenidate, or a combination of any of the foregoing.

19. The composition of claim 1, wherein the active pharmaceutical ingredient comprises tapentadol.

20. The composition of claim 2, wherein the suspension agent comprises fumed silica, fumed alumina, or mixtures thereof.

35. The composition of claim 1, wherein the soft capsule shell comprises:

(a) about 25-50% of at least one film-forming polymer;

(b) about 15-25% of at least one plasticizer; and

(c) about 20-40% of a solvent.

46. A method for reducing the ability of a subject to extract an active pharmaceutical ingredient from a pharmaceutical composition though crushing, grating, grinding, cutting, or solvating or dissolving the matrix comprising:

providing the composition of claim 1, wherein the composition is resistant to crushing, grating, grinding, cutting, solvation, or dissolution.

21-22. -22. (canceled)

23. An abuse deterrent oral pharmaceutical composition comprising a tamper resistant controlled release matrix comprising:

(a) about 45% to about 52% soybean oil;

(b) about 1.5% to about 5% Gelucire®

43/01;

(c) about 1.8% to about 4% bee'"'"'s wax;

(d) about 2% to about 8% Kollidon®

90 F;

(e) about 0.5% to about 4% Carbopol®

971 A;

(f) about 2% to about 8% EUDRAGIT®

EPO;

(g) about 0.5% to about 5% Aerosil 200; and

(h) about 5% to about 30% tapentadol hydrochloride;

wherein the matrix is resistant to tampering and is encapsulated in a soft capsule shell comprising;

at least one film forming polymer, at least one plasticizer, and at least one solvent.

24. An abuse deterrent oral pharmaceutical composition comprising a tamper resistant controlled release matrix comprising:

(a) about 45% to about 52% soybean oil;

(b) about 1.8% to about 4% Gelucire®

43/01;

(c) about 1.8% to about 4% bee'"'"'s wax;

(d) about 5% to about 15% polyethylene oxide;

(e) about 0.5% to about 4% Carbopol®

971 A;

(f) about 2% to about 8% EUDRAGIT®

EPO;

(g) about 0.5% to about 5% Aerosil 200; and

(h) about 5% to about 30% tapentadol hydrochloride;

wherein the matrix is resistant to tampering and is encapsulated in a soft capsule shell comprising;

at least one film forming polymer, at least one plasticizer, and at least one solvent.

25-34. -34. (canceled)

36-45. -45. (canceled)

47-48. -48. (canceled)