Injectable flowable composition comprising buprenorphine
View Patent ↗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.
1. An injectable flowable composition comprising:
(i) 8 wt% to about 30 wt% of buprenorphine in the form of a 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;
wherein the composition is transformed in situ into a solid implant by contact with water, body fluid, or other aqueous medium.
2. The composition of claim 1 , wherein the composition comprises from about 3 milligrams to about 300 milligrams of buprenorphine in the form of the free base or the pharmaceutically acceptable salt.
3. The composition of claim 1 , wherein the polymer is a 50/50 poly (DL-lactide-co-glycolide) copolymer.
4. The composition of claim 1 , wherein the poly(DL-lactide-co-glycolide) copolymer has an average molecular weight from about 5,000 Daltons to about 40,000 Daltons.
5. An injectable flowable composition consisting of:
(i) 8 wt% to about 30 wt% of buprenorphine in the form of a 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;
wherein the composition is transformed in situ into a solid implant by contact with water, body fluid, or other aqueous medium.
6. The composition of claim 5 , wherein the poly(DL-lactide-co-glycolide) copolymer is a 50/50 poly(DL-lactide-co-glycolide) copolymer.
7. The composition of claim 5 , wherein the poly(DL-lactide-co-glycolide) copolymer has an average molecular weight from about 5,000 Daltons to about 40,000 Daltons.
8. The composition of claim 5 , wherein the flowable composition comprises from about 3 milligrams to about 300 milligrams of buprenorphine in the form of a free base or pharmaceutically acceptable salt.
9. The composition of claim 5 , wherein poly(DL-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(DL-lactide-co-glycolide) copolymer.
10. An injectable flowable composition comprising:
(i) 8 wt% to about 30 wt% of buprenorphine in the form of a 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.
11. A method for treating a patient having an opioid dependency comprising parenterally administering to the patient a therapeutically effective amount of the composition of claim 1 once per month to treat the opioid dependency.
12. A method for treating a patient having an opioid dependency comprising parenterally administering to the patient a therapeutically effective amount of the composition of claim 5 once per month to treat the opioid dependency.
13. A method for treating a patient having an opioid dependency comprising parenterally administering to the patient a therapeutically effective amount of the composition of claim 10 once per month to treat the opioid dependency.
14. An injectable flowable composition consisting of:
(i) 8 wt% to about 30 wt% of buprenorphine in the form of a 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.
15. A method for treating a patient having an opioid dependency comprising parenterally administering to the patient a therapeutically effective amount of the composition of claim 14 once per month to treat the opioid dependency.