Claims for Patent: 10,198,218

Summary for Patent: 10,198,218

Title:	Injectable flowable composition comprising 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:	15/857,507
Patent Claims:	1. A method for treating opioid dependence in a subject in need thereof, the method comprising administering to the subject by subcutaneous injection a therapeutically effective amount of a pharmaceutical composition comprising: (i) 10 wt % to about 50 wt % of buprenorphine free base; (ii) 5 wt % to about 70 wt % of a poly(lactide-co-glycolide) copolymer; and (iii) N-methyl-2-pyrrolidone; to treat the opioid dependence. 2. The method of claim 1, comprising administering the composition once every twenty-eight days. 3. The method of claim 1, comprising administering the composition once per month. 4. The method of claim 1, wherein the composition comprises from 10 wt % to about 30 wt % of the buprenorphine free base. 5. The method of claim 1, wherein the composition comprises from about 15 wt % to about 20 wt % of the buprenorphine free base. 6. The method of claim 1, wherein the composition comprises about 18 wt % of the buprenorphine free base. 7. The method of claim 1, wherein the composition comprises from about 15 wt % to about 70 wt % of the poly(lactide-co-glycolide) copolymer. 8. The method of claim 1, wherein the composition comprises about 32 wt % of the poly(lactide-co-glycolide) copolymer. 9. The method of claim 1, wherein the poly(lactide-co-glycolide) copolymer is a 50/50, 55/45, 60/40, 65/35, 70/30, 75/25, 80/20, 85/15, 90/10, or 95/5 poly(lactide-co-glycolide) copolymer. 10. The method of claim 1, wherein the poly(lactide-co-glycolide) copolymer is a 50/50 poly(lactide-co-glycolide) copolymer. 11. The method of claim 1, wherein the composition comprises from about 10 wt % to about 70 wt % of the N-methyl-2-pyrrolidone. 12. The method of claim 1, wherein the composition comprises about 50 wt % of the N-methyl-2-pyrrolidone. 13. The method of claim 1, wherein the poly(lactide-co-glycolide) copolymer has an average molecular weight from about 5,000 Daltons to about 40,000 Daltons. 14. The method of claim 1, wherein the poly(lactide-co-glycolide) copolymer has an average molecular weight from about 10,000 Daltons to about 20,000 Daltons. 15. A method for treating opioid dependence in a patient, the method comprising administering to the patient, by subcutaneous injection, a pharmaceutical composition comprising about 18 wt % of buprenorphine free base, about 32 wt % of a poly(lactide-co-glycolide) copolymer, and about 50 wt % of N-methyl-2-pyrrolidone. 16. The method of claim 15, wherein the composition is transformed in situ into an implant by contact with body fluid of the patient. 17. The method of claim 15, wherein the composition provides sustained release of buprenorphine to the patient for at least 28 days. 18. The method of claim 15, wherein the composition provides sustained release of buprenorphine to the patient for at least 45 days. 19. The method of claim 15, wherein the composition provides sustained release of buprenorphine to the patient for at least 60 days. 20. The method of claim 15, wherein the pharmaceutical composition comprises about 3 mg to about 300 mg of the buprenorphine free base; and wherein the composition has a volume of about 0.5 mL. 21. The method of claim 15, wherein the pharmaceutical composition comprises about 9 mg to about 900 mg of the buprenorphine free base; and wherein the composition has a volume of about 1.5 mL. 22. The method of claim 15, wherein the poly(lactide-co-glycolide) copolymer is a 50:50 poly(lactide-co-glycolide) copolymer. 23. The method of claim 15, wherein the poly(lactide-co-glycolide) copolymer is a 50:50 poly(lactide-co-glycolide) copolymer having an average molecular weight of about 5,000 Daltons to about 40,000 Daltons. 24. The method of claim 15, wherein the poly(lactide-co-glycolide) copolymer is a 50:50 poly(lactide-co-glycolide) copolymer having a carboxy terminal group and an average molecular weight of about 10,000 Daltons to about 20,000 Daltons. 25. The method of claim 15, wherein the buprenorphine composition comprises from about 3 mg to about 300 mg of buprenorphine free base. 26. A method for treating opioid dependence in a patient in need thereof, the method comprising subcutaneously administering a buprenorphine composition to the patient once every two months; wherein the buprenorphine composition comprises about 18 wt % of buprenorphine free base; about 32 wt % of a poly(lactide-co-glycolide) copolymer; and about 50 wt % of N-methyl-2-pyrrolidone. 27. The method of claim 26, wherein the poly(lactide-co-glycolide) copolymer is a 50:50 poly(lactide-co-glycolide) copolymer. 28. The method of claim 26, wherein the poly(lactide-co-glycolide) copolymer is a 50:50 poly(lactide-co-glycolide) copolymer having an average molecular weight of about 5,000 Daltons to about 40,000 Daltons. 29. The method of claim 26, wherein the poly(lactide-co-glycolide) copolymer is a 50:50 poly(lactide-co-glycolide) copolymer having a carboxy terminal group and an average molecular weight of about 10,000 Daltons to about 20,000 Daltons. 30. The method of claim 26, wherein the buprenorphine composition comprises from about 3 mg to about 300 mg of buprenorphine free base. 31. A method for treating opioid dependence in a patient in need thereof, the method comprising subcutaneously administering a buprenorphine composition to the patient once every two months; wherein the buprenorphine composition comprises 10 wt % to about 50 wt % buprenorphine free base; 5 wt % to about 70 wt % of a poly(lactide-co-glycolide) copolymer; and N-methyl-2-pyrrolidone. 32. The method of claim 31, wherein the buprenorphine composition comprises about 8 wt % to about 30 wt % of buprenorphine free base; about 5 wt % to about 70 wt % of the poly(lactide-co-glycolide) copolymer; and about 30 wt % to about 70 wt % of N-methyl-2-pyrrolidone. 33. The method of claim 32, wherein the poly(lactide-co-glycolide) copolymer has an average molecular weight of about 5,000 Daltons to about 40,000 Daltons. 34. The method of claim 31, wherein the buprenorphine composition comprises about 10 wt % to about 30 wt % of buprenorphine free base; about 15 wt % to about 70 wt % of the poly(lactide-co-glycolide) copolymer, and about 30 wt % to about 70 wt % of N-methyl-2-pyrrolidone. 35. The method of claim 34, wherein the poly(lactide-co-glycolide) copolymer has an average molecular weight of about 5,000 Daltons to about 40,000 Daltons.