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Claims for Patent: 9,259,421

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Claims for Patent: 9,259,421

Title:Abuse-resistant pharmaceutical composition for the treatment of opioid dependence
Abstract: There is provided pharmaceutical compositions for the treatment of e.g. opioid dependency comprising microparticles of a pharmacologically-effective amount of buprenorphine, or a pharmaceutically-acceptable salt thereof, in associative admixture with particles comprising a weak acid, or particles comprising weakly-acidic buffer forming materials. The composition may further comprise a disintegrant and/or particles of a pharmacologically-effective amount of naloxone, or a pharmaceutically-acceptable salt thereof. The compositions are useful in the treatment of opioid dependency/addiction and/or pain.
Inventor(s): Fischer; Andreas (Uppsala, SE)
Assignee: Orexo AB (Uppsala, SE)
Application Number:14/668,973
Patent Claims: 1. A pharmaceutical composition in the form of a tablet comprising: buprenorphine, or a pharmaceutically acceptable salt thereof, provided in the form of microparticles, a weak acid, provided in the form of particles, which particles are separate from the microparticles of buprenorphine, or a pharmaceutically acceptable salt thereof, a disintegrant, and naloxone or a pharmaceutically acceptable salt thereof, wherein the buprenorphine or salt thereof and naloxone or salt thereof are present in about a 4:1 buprenorphine:naloxone dose ratio (calculated as free bases), and wherein, when an aqueous USP/NF potassium phosphate buffer with a pH of 6.8 is dripped at a rate of about 2 mL per minute through a tube with an inner diameter of about 3 mm onto said tablet composition placed on top of a Porosity 1 20 mm diameter silica filter in a glass funnel with an upper inner diameter of 55 mm, in which the distance between the end of the tube and the silica filter in the funnel is about 7.5 cm, the pH of the resultant drips, measured from the start of dripping at the outlet of the glass funnel, exhibits a maximum drop from 6.8 of between 0.5 to 5 pH units within about 1 minute immediately followed by maintenance of pH within that range for no more than about 3 minutes.

2. The composition as claimed in claim 1 in which said microparticles of buprenorphine or pharmaceutically acceptable salt thereof are presented upon the surfaces of larger carrier particles, which carrier particles are distinct from the particles of weak acid.

3. The composition as claimed in claim 2 in which said particles of the weak acid are presented upon the surfaces of, and/or between, said carrier particles.

4. The composition as claimed in claim 1 wherein the disintegrant is selected from the group croscarmellose sodium, sodium starch glycolate, crosslinked polyvinylpyrrolidone and mixtures thereof.

5. The composition as claimed in claim 1, wherein the naloxone or pharmaceutically acceptable salt thereof is provided in the form of particles.

6. A pharmaceutical composition in the form of a tablet comprising: about 0.1% to about 10% by weight, based upon the total weight of the composition, of buprenorphine, or a pharmaceutically acceptable salt thereof, provided in the form of microparticles; about 0.125% to about 5% by weight, based upon the total weight of the composition, of naloxone or a pharmaceutically acceptable salt thereof, provided in the form of particles, wherein the buprenorphine or salt thereof and naloxone or salt thereof are present in about a 4:1 buprenorphine:naloxone dose ratio (calculated as free bases); either about 1% to about 10% by weight, based upon the total weight of the composition, of a weak acid provided in the form of particles, or about 1% to about 15% by weight, based upon the total weight of the composition, of a weakly-acidic buffer forming material provided in the form of particles; about 0.5% to about 15% by weight, based upon the total weight of the composition, of a disintegrant; about 0.5 to 20% by weight, based upon the total weight of the composition, of a binder; and water-soluble carrier particles; wherein the particles of weak acid or weakly-acidic buffer forming material are separate from the microparticles of buprenorphine, or a pharmaceutically acceptable salt thereof; wherein, when an aqueous USP/NF potassium phosphate buffer with a pH of 6.8 is dripped at a rate of about 2 mL per minute through a tube with an inner diameter of about 3 mm onto said tablet composition placed on top of a Porosity 1 20 mm diameter silica filter in a glass funnel with an upper inner diameter of 55 mm, in which the distance between the end of the tube and the silica filter in the funnel is about 7.5 cm, the pH of the resultant drips, measured from the start of dripping at the outlet of the glass funnel, exhibits a maximum drop from 6.8 of between 0.5 to 5 pH units within about 1 minute immediately followed by maintenance of pH within that range for no more than about 3 minutes.

7. The composition as claimed in claim 6, wherein the water-soluble carrier particles are of a size, based on a weight based mean diameter, of about 100 .mu.m to about 800 .mu.m.

8. The composition as claimed in claim 6, wherein the water-soluble carrier particles comprise a sugar or sugar alcohol.

9. The composition as claimed in claim 8, wherein the water-soluble carrier particles comprise mannitol.

10. The composition as claimed in claim 6, wherein the microparticles of buprenorphine or salt thereof and the particles of naloxone or salt thereof each have a weight based mean diameter of between about 0.5 .mu.m and about 15 .mu.m.

11. The composition as claimed in claim 6, wherein the particles of weak acid are from about 1 .mu.m to about 1000 .mu.m.

12. The composition as claimed in claim 6, wherein the weak acid is provided and the weak acid is selected from the group consisting of citric acid, malic acid, tartaric acid, fumaric acid, adipic acid, succinic acid, lactic acid, acetic acid, oxalic acid, maleic acid, ammonium chloride, and a combination of such acids.

13. The composition as claimed in claim 6, wherein the particles of weakly-acidic buffer forming material are from about 1 .mu.m to about 1000 .mu.m.

14. The composition as claimed in claim 6, wherein the weakly-acidic buffer forming material is provided and comprises a combination of: (i) an acid selected from the group consisting of citric acid, malic acid, tartaric acid, fumaric acid, adipic acid, succinic acid, lactic acid, acetic acid, oxalic acid, maleic acid, ammonium chloride, and a combination of such acids; and (ii) an alkaline salt of citric acid, malic acid, tartaric acid, fumaric acid, adipic acid, succinic acid, lactic acid, acetic acid, oxalic acid, or maleic acid.

15. The composition as claimed in claim 6, wherein the disintegrant is present in an amount of about 2 to about 7% by weight.

16. The composition as claimed in claim 6, wherein the disintegrant is in particulate form, having a weight based mean diameter of between about 0.1 .mu.m and about 100 .mu.m.

17. The composition as claimed in claim 6, wherein the disintegrant is cross-linked polyvinylpyrrolidone, sodium starch glycolate, croscarmellose sodium, or combinations thereof.

18. The composition as claimed in claim 6, where the per tablet dosage of buprenorphine or salt thereof is about 0.1 mg to about 15 mg (calculated as free base).

19. The composition as claimed in claim 6, wherein the per tablet dosages of buprenorphine and naloxone are, respectively, about 11.4 mg and about 2.9 mg; about 8.6 mg and about 2.2 mg; about 5.7 mg and about 1.4 mg; about 2.9 mg and about 0.7 mg; or about 1.4 mg and about 0.4 mg (calculated as free bases).

20. The composition as claimed in claim 6, wherein the binder is present in an amount of about 2.0 to about 12% by weight.

21. The composition as claimed in claim 6, wherein the binder is a cellulose gum or microcrystalline cellulose.

22. The composition as claimed in claim 6, wherein the tablet has a crushing strength in the range of about 10 N to about 100 N.

23. The composition as claimed in claim 1, wherein the pH of the resultant drips, measured from the start of dripping at the outlet of the glass funnel, exhibits a maximum drop from 6.8 of between 0.55 to 5 pH units within about 1 minute.

24. The composition as claimed in claim 1, wherein the pH of the resultant drips, measured from the start of dripping at the outlet of the glass funnel, exhibits a maximum drop from 6.8 of between 0.55 to 4.5 pH units within about 1 minute.
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