Injectable buprenorphine formulation

1. A method for the treatment of pain, for opioid maintenance therapy, or for the treatment of opioid dependence by detoxification and/or maintenance or for the treatment of the symptoms of opioid withdrawal and/or cocaine withdrawal, comprising the subcutaneous administration to a human or non-human animal subject in need thereof a therapeutically effective amount of an injectable liquid formulation comprising:

a) a lipid controlled-release matrix comprising at least 80% triglycerides;

b) at least one oxygen containing organic solvent; and

c) 50-600 mg of at least one active agent selected from buprenorphine and salts thereof, calculated as buprenorphine free base,

wherein the injectable liquid formulation is administered to the subject every 2 or 3 months,

wherein the injectable liquid formulation comprises at least 16% by weight of the active agent.

2. The method of claim 1 , wherein component a) comprises at least 90% triglycerides.

3. The method of claim 1 , wherein component a) comprises at least 95% triglycerides.

4. The method of claim 1 , wherein component a) further comprises:

i) at least one neutral diacyl lipid

ii) at least one tocopherol; and/or

iii) at least one phospholipid.

5. The method of claim 1 , wherein component a) comprises 10 to 60 wt. % of the total injectable liquid formulation.

6. The method of claim 1 , wherein component a) comprises at least 50 wt. % of triglycerides comprising C16 to C20 acyl groups having zero, one, or two unsaturations.

7. The method of claim 1 , wherein component a) comprises at least 60 wt. % of triglycerides comprising C16 to C18 acyl groups with zero, one, or two unsaturations.

8. The method of claim 1 , wherein component b) is present at 15 to 50 wt. % of the total injectable liquid formulation.

9. The method of claim 1 , wherein component b) comprises at least one amide and/or at least one sulphoxide.

10. The method of claim 9 , wherein component b) comprises N-methyl-2-pyrrolidone (NMP), dimethyl sulfoxide (DMSO), or mixtures thereof.

11. The method of claim 1 , wherein the injectable liquid formulation is in ready-to-administer form.

12. The method of claim 1 , wherein the injectable liquid formulation has a viscosity of 20 to 600 mPas at 20° C.

13. The method of claim 4 , wherein the ratio of triglyceride(s):phospholipid(s) (w/w) in the lipid controlled-release matrix a) is in the range of 90:10 to 100:0.

14. The method of claim 4 , wherein the level of phospholipid in the injectable liquid formulation as a whole is less than 8 wt. %.

15. The method of claim 1 , wherein component a) comprises greater than 90% triglycerides, and wherein component a) comprises at least 50 wt. % of triglycerides comprising C16 to C20 acyl groups having zero, one, or two unsaturations.

16. The method of claim 1 :

wherein component a) forms 10 to 70 wt. % of the total injectable liquid formulation,

wherein component b) is present at 10 to 60 wt. % of the total injectable liquid formulation,

wherein component b) comprises at least 50% N-methyl-2-pyrrolidone (NMP), dimethyl sulfoxide (DMSO), or mixtures thereof.

17. The method of claim 1 :

wherein component a) forms 10 to 60 wt. % of the total injectable liquid formulation,

wherein component b) is present at 15 to 50 wt. % of the total injectable liquid formulation,

wherein component b) comprises at least 70% N-methyl-2-pyrrolidone (NMP), dimethyl sulfoxide (DMSO), or mixtures thereof.

18. The method of claim 1 :

wherein component a) forms 15 to 64 wt. % of the total injectable liquid formulation,

wherein of component a) comprises at least 90% triglycerides,

wherein component b) is present at 20 to 45 wt. % of the injectable liquid formulation,

wherein component b) comprises at least 80% N-methyl-2-pyrrolidone (NMP), dimethyl sulfoxide (DMSO), or mixtures thereof.

19. The method of claim 1 :

wherein component a) forms 20 to 50 wt. % of the total injectable liquid formulation,

wherein component a) comprises at least 95% triglycerides,

wherein component b) is present at 25 to 40 wt. % of the injectable liquid formulation,

wherein component b) comprises at least 90% N-methyl-2-pyrrolidone (NMP), dimethyl sulfoxide (DMSO), or mixtures thereof.

20. The method of claim 19 , wherein component b) is NMP.

21. The method of claim 1 , wherein the injectable liquid formulation comprises 50-600 mg of the at least one active agent per dose.

22. The method of claim 1 , wherein the injectable liquid formulation comprises a single dose of 50-600 mg of the at least one active agent.