Claims for Patent: 10,558,394

Summary for Patent: 10,558,394

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):	Richard L. Norton, Andrew Watkins, Mingxing Zhou
Assignee:	Indivior UK Ltd
Application Number:	US15/820,048
Patent Claims:	1. An injectable flowable composition comprising: (i) 10 wt % to about 50 wt % of buprenorphine in the form of a free base or a pharmaceutically acceptable salt; (ii) about 5 wt % to about 70 wt % of a poly(lactide-co-glycolide) copolymer; and (iii) N-methyl-2-pyrrolidone. 2. The composition of claim 1, comprising from 10 wt % to about 30 wt % of the buprenorphine. 3. The composition of claim 1, comprising from about 15 wt % to about 20 wt % of the buprenorphine. 4. The composition of claim 1, comprising from about 15 wt % to about 70 wt % of the poly(lactide-co-glycolide) copolymer. 5. The composition 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. 6. The composition of claim 1, wherein the poly(lactide-co-glycolide) copolymer is a 50/50 poly(lactide-co-glycolide) copolymer. 7. The composition of claim 1, wherein the buprenorphine is in the form of the free base. 8. The composition of claim 1, comprising from about 3 mg to about 300 mg of the buprenorphine free base. 9. An injectable flowable 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. 10. The composition of claim 9, wherein the poly(lactide-co-glycolide) copolymer has a carboxy terminal group. 11. The composition of claim 9, wherein the poly(lactide-co-glycolide) copolymer has an average molecular weight from about 5,000 Daltons to about 20,000 Daltons. 12. The composition of claim 9, 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 from about 5,000 Daltons to about 20,000 Daltons. 13. The composition of claim 9, wherein the composition transforms in situ into an implant by contact with water, a bodily fluid, or other aqueous medium. 14. The composition of claim 9, wherein the composition comprises from about 3 mg to about 300 mg of buprenorphine free base. 15. The composition of claim 14 having a volume of about 0.5 mL. 16. The composition of claim 9, wherein the composition comprises from about 9 mg to about 900 mg of buprenorphine free base. 17. The composition of claim 16 having a volume of about 1.5 mL. 18. The composition of claim 9 having a volume from about 0.10 mL to about 2.0 mL. 19. A syringe comprising the composition of claim 9. 20. A container comprising the composition of claim 9. 21. An injectable flowable pharmaceutical composition comprising about 15 wt % to about 30 wt % of buprenorphine free base; about 5 wt % to about 50 wt % of a poly(lactide-co-glycolide) copolymer; and about 30 wt % to about 70 wt % of N-methyl-2-pyrrolidone. 22. The composition of claim 21, wherein the composition transforms in situ into an implant by contact with water, a bodily fluid, or other aqueous medium. 23. The composition of claim 21, wherein the biodegradable thermoplastic polymer is a poly(lactide-co-glycolide) copolymer having an average molecular weight of about 5,000 Daltons to about 20,000 Daltons. 24. An injectable flowable pharmaceutical composition comprising about 15 wt % to about 30 wt % of buprenorphine free base; about 5 wt % to about 50 wt % of a poly(lactide-co-glycolide) copolymer; and about 30 wt % to about 70 wt % of a biocompatible organic liquid comprising: (i) N-methyl-2-pyrrolidone and (ii) glycerin, propylene glycol, polyethylene glycol, or a combination of two or more thereof. 25. The composition of claim 24, wherein the composition transforms in situ into an implant by contact with water, a bodily fluid, or other aqueous medium. 26. The composition of claim 21, comprising about 18 wt % of buprenorphine free base. 27. The composition of claim 24, comprising about 18 wt % of buprenorphine free base. 28. The container of claim 19, wherein the composition transforms in situ into an implant by contact with water, a bodily fluid, or other aqueous medium.