Claims for Patent: 9,272,044

Summary for Patent: 9,272,044

Title:	Injectable flowable composition buprenorphine
Abstract:	The present invention is directed to a buprenorphine sustained release delivery system capable of delivering buprenorphine, a metabolite, or a prodrug thereof for a duration of about 14 days to about 3 months. The buprenorphine sustained release delivery system includes a flowable composition and a solid implant for the sustained release of buprenorphine, a metabolite, or a prodrug thereof. The implant is produced from the flowable composition. The buprenorphine sustained release delivery system provides in situ 1-month and 3-month release profiles characterized by an exceptionally high bioavailability and minimal risk of permanent tissue damage and typically no risk of muscle necrosis.
Inventor(s):	Norton; Richard L. (Fort Collins, CO), Watkins; Andrew (Fort Collins, CO), Zhou; Mingxing (Fort Collins, CO)
Assignee:	Indivior UK Limited (Slough, GB)
Application Number:	14/610,818
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,272,044
Patent Claims:	1. A method for treating opioid addiction in a human in need thereof comprising administering a therapeutically effective amount of a pharmaceutical composition to the human to treat the opioid addiction; wherein the pharmaceutical composition comprises: (i) 8 wt % to about 30 wt % of buprenorphine in the form of the free base or a pharmaceutically acceptable salt; (ii) about 20 wt % to about 70 wt % of a poly(DL-lactide-co-glycolide) copolymer; and (iii) about 30 wt % to about 70 wt % of N-methyl-2-pyrrolidone. 2. The method of claim 1, wherein the composition comprises from about 3 milligrams to about 300 milligrams of buprenorphine in the form of a free base or pharmaceutically acceptable salt. 3. The method of claim 1, wherein the polymer is a 50/50 poly(DL-lactide-co-glycolide) copolymer having an average molecular weight of about 5,000 Daltons to about 40,000 Daltons. 4. The method of claim 1, wherein the polymer is a 50/50 poly(DL-lactide-co-glycolide) copolymer having an average molecular weight of about 10,000 Daltons to about 20,000 Daltons. 5. The method of claim 1, wherein the composition is transformed in situ into a solid implant after being parenterally administered to the human. 6. The method of claim 1, wherein the composition consists of (i), (ii), and (iii). 7. The method of claim 1, wherein the composition comprises (i) 8 wt % to about 22 wt % of buprenorphine in the form of the free base; (ii) about 25 wt % to about 50 wt % of a poly(DL-lactide-co-glycolide) copolymer having an average molecular weight of about 5,000 Daltons to about 40,000 Daltons; and (iii) about 30 wt % to about 70 wt % of N-methyl-2-pyrrolidone. 8. The method of claim 7, wherein the composition consists of (i), (ii), and (iii). 9. The method of claim 1, wherein the method comprises administering the pharmaceutical composition to the human once per month by injection. 10. The method of claim 1, wherein the method comprises administering the pharmaceutical composition to the human once every three months by injection. 11. The method of claim 1, wherein the method comprises administering the pharmaceutical composition to the human once every four months by injection. 12. The method of claim 1, wherein the method comprises administering the pharmaceutical composition to the human once every six months by injection. 13. The method of claim 1, wherein the pharmaceutical composition has a substantially linear release profile that lasts for 28 days after administration to the human. 14. The method of claim 1, wherein the therapeutically effective dose of buprenorphine is delivered to the human for at least about 15 days after administration; for at least about 28 days after administration; for at least about 45 days after administration; or for at least about 60 days after administration. 15. The method of claim 1, wherein the administration is a subcutaneous injection. 16. A method for treating opioid addiction in a human in need thereof comprising administering a therapeutically effective amount of a pharmaceutical composition to the human to treat the opioid addiction; wherein the pharmaceutical composition comprises: (i) 8 wt % to about 30 wt % of buprenorphine in the form of a free base or pharmaceutically acceptable salt; (ii) about 15 wt % to about 70 wt % of a biodegradable thermoplastic polymer; and (iii) about 10 wt % to about 90 wt % of an organic liquid selected from the group consisting of N-methyl-2-pyrrolidone, 2-pyrrolidone, acetic acid, lactic acid, methyl lactate, ethyl lactate, monomethyl succinate acid, monomethyl citric acid, glycofurol, glycerol formal, isopropylidene glycol, 2,2-dimethyl-1,3-dioxolone-4-methanol, solketal, dimethylformamide, dimethylacetamide, dimethylsulfoxide, dimethylsulfone, epsilon-caprolactone, butyrolactone, caprolactam, or a mixture of two or more thereof. 17. The method of claim 16, wherein the polymer is a polylactide, a polyglycolide, a polycaprolactone, a copolymer thereof, a terpolymer thereof, or any combination thereof. 18. A method for treating opioid addiction in a human in need thereof comprising subcutaneously injecting a pharmaceutical composition into the human once per month to treat the opioid addiction; wherein the pharmaceutical composition consists of: (i) 8 wt % to about 22 wt % of buprenorphine in the form of a free base; (ii) about 25 wt % to about 50 wt % of a poly(DL-lactide-co-glycolide) copolymer; and (iii) about 30 wt % to about 70 wt % of N-methyl-2-pyrrolidone; and wherein the composition comprises from about 3 milligrams to about 300 milligrams of the buprenorphine in the form of the free base. 19. A method for treating chronic pain in a human in need thereof comprising subcutaneously injecting a pharmaceutical composition into the human once per month to treat the chronic pain; wherein the pharmaceutical composition consists of: (i) 8 wt % to about 22 wt % of buprenorphine in the form of a free base; (ii) about 25 wt % to about 50 wt % of a poly(DL-lactide-co-glycolide) copolymer; and (iii) about 30 wt % to about 70 wt % of N-methyl-2-pyrrolidone; and wherein the composition comprises from about 3 milligrams to about 300 milligrams of buprenorphine in the form of the free base. 20. A method for treating pain in a human in need thereof comprising administering a therapeutically effective amount of a pharmaceutical composition to the human to treat the pain; wherein the pharmaceutical composition comprises: (i) 8 wt % to about 30 wt % of buprenorphine in the form of the free base or a pharmaceutically acceptable salt; (ii) about 20 wt % to about 70 wt % of a poly(DL-lactide-co-glycolide) copolymer; and (iii) about 30 wt % to about 70 wt % of N-methyl-2-pyrrolidone. 21. The method of claim 20, wherein the pain is chronic pain. 22. The method of claim 20, wherein the composition comprises from about 3 milligrams to about 300 milligrams of buprenorphine in the form of a free base or pharmaceutically acceptable salt. 23. The method of claim 20, wherein the polymer is a 50/50 poly(DL-lactide-co-glycolide) copolymer having an average molecular weight of about 5,000 Daltons to about 40,000 Daltons. 24. The method of claim 20, wherein the polymer is a 50/50 poly(DL-lactide-co-glycolide) copolymer having an average molecular weight of about 10,000 Daltons to about 20,000 Daltons. 25. The method of claim 20, wherein the composition is transformed in situ into a solid implant after being parenterally administered to the human. 26. The method of claim 20, wherein the composition consists of (i), (ii), and (iii). 27. The method of claim 20, wherein the composition comprises (i) 8 wt % to about 22 wt % of buprenorphine in the form of the free base; (ii) about 25 wt % to about 50 wt % of a poly(DL-lactide-co-glycolide) copolymer having an average molecular weight of about 5,000 Daltons to about 40,000 Daltons; and (iii) about 30 wt % to about 70 wt % of N-methyl-2-pyrrolidone. 28. The method of claim 27, wherein the composition consists of (i), (ii), and (iii). 29. The method of claim 20, wherein the method comprises administering the pharmaceutical composition to the human once per month by injection. 30. The method of claim 20, wherein the method comprises administering the pharmaceutical composition to the human once every three months by injection. 31. The method of claim 20, wherein the administration is a subcutaneous injection. 32. A method for treating pain in a human in need thereof comprising administering a therapeutically effective amount of a pharmaceutical composition to the human to treat the pain; wherein the pharmaceutical composition comprises: (i) 8 wt % to about 30 wt % of buprenorphine in the form of a free base or pharmaceutically acceptable salt; (ii) about 15 wt % to about 70 wt % of a biodegradable thermoplastic polymer; and (iii) about 10 wt % to about 90 wt % of an organic liquid selected from the group consisting of N-methyl-2-pyrrolidone, 2-pyrrolidone, acetic acid, lactic acid, methyl lactate, ethyl lactate, monomethyl succinate acid, monomethyl citric acid, glycofurol, glycerol formal, isopropylidene glycol, 2,2-dimethyl-1,3-dioxolone-4-methanol, solketal, dimethylformamide, dimethylacetamide, dimethylsulfoxide, dimethylsulfone, epsilon-caprolactone, butyrolactone, caprolactam, or a mixture of two or more thereof. 33. The method of claim 32, wherein the polymer is a polylactide, a polyglycolide, a polycaprolactone, a copolymer thereof, a terpolymer thereof, or any combination thereof. 34. The method of claim 16, wherein the composition consist of (i), (ii), and (iii). 35. The method of claim 32, wherein the composition consist of (i), (ii), and (iii).