Claims for Patent: 10,406,160

Summary for Patent: 10,406,160

Title:	Sustained release small molecule drug formulation
Abstract:	An injectable depot formulation includes a biocompatible polymer, an organic solvent combined with the biocompatible polymer to form a viscous gel, and a small molecule drug incorporated in the viscous gel such that the formulation exhibits an in vivo release profile having a C.sub.max to C.sub.min ratio of less than 200 and a lag time less than 0.2.
Inventor(s):	Luk; Andrew S. (Castro Valley, CA), Junnarkar; Gunjan H. (Palo Alto, CA), Chen; Guohua (Sunnyvale, CA)
Assignee:	INDIVIOR UK LIMITED (Hull, GB)
Application Number:	16/044,259
Patent Claims:	1. An injectable pharmaceutical composition comprising from about 10 wt % to about 30 wt % of risperidone base suspended in gel comprising: (i) from about 40 wt % to about 60 wt % of a copolymer of lactic acid and glycolic acid, wherein the lactic acid to glycolic acid monomer ratio is from about 100:0 to about 60:40, and wherein the copolymer has a number average molecular weight from about 5,000 Daltons to about 30,000 Daltons, and (ii) N-methyl-2-pyrrolidone. 2. The composition of claim 1, wherein the gel consists of (i) and (ii). 3. An injectable pharmaceutical composition comprising from about 1 wt % to about 50 wt % of risperidone base suspended in a gel comprising: (i) from about 5 wt % to about 80 wt % of a copolymer of lactic acid and glycolic acid, and (ii) N-methyl-2-pyrrolidone. 4. The composition of claim 3, comprising from about 5 wt % to about 40 wt % of risperidone base. 5. The composition of claim 4, comprising from about 5 wt % to about 30 wt % of risperidone base. 6. The composition of claim 5, comprising from about 10 wt % to about 30 wt % of risperidone base. 7. The composition of claim 3, wherein the gel comprises: (i) from about 20 wt % to about 70 wt % of a copolymer of lactic acid and glycolic acid, and (ii) N-methyl-2-pyrrolidone. 8. The composition of claim 7, wherein the gel comprises: (i) from about 40 wt % to about 60 wt % of a copolymer of lactic acid and glycolic acid, and (ii) N-methyl-2-pyrrolidone. 9. The composition of claim 3, wherein the lactic acid to glycolic acid monomer ratio in the copolymer is from about 100:0 to 60:40. 10. The composition of claim 9, wherein the lactic acid to glycolic acid monomer ratio in the copolymer is from about 100:0 to 75:25. 11. The composition of claim 3, wherein the copolymer has a number average molecular weight from about 1,000 Daltons to about 120,000 Daltons. 12. The composition of claim 11, wherein the copolymer has a number average molecular weight from about 5,000 Daltons to about 30,000 Daltons. 13. The composition of claim 3, wherein the gel consists of (i) and (ii). 14. An injectable pharmaceutical composition comprising risperidone base suspended in a gel comprising: (i) a copolymer of lactic acid and glycolic acid, and (ii) N-methyl-2-pyrrolidone. 15. A method of administering risperidone base to a subject in need thereof, the method comprising subcutaneously injecting the composition of claim 1 into the subject once per month. 16. A method of administering risperidone base to a subject in need thereof, the method comprising subcutaneously injecting the composition of claim 3 into the subject once per month. 17. A method of administering risperidone base to a subject in need thereof, the method comprising subcutaneously injecting the composition of claim 14 into the subject once per month. 18. A syringe comprising the composition of claim 1. 19. A syringe comprising the composition of claim 3. 20. A syringe comprising the composition of claim 14.