Residence structures and related methods

Patent metadata

Field	Value
Publication number	US-10517820-B2
Application number	US-201916379727-A
Country	US
Kind code	B2
Filing date	Apr 9, 2019
Priority date	Jun 11, 2014
Publication date	Dec 31, 2019
Grant date	Dec 31, 2019

Abstract

Described are methods of making a gastric residence structure including an active substance. The methods may include forming one or more arms comprising a loadable polymeric component, wherein the loadable polymeric component includes one or more polymeric materials and at least one active substance. The methods may also include connecting the one or more arms to an elastic polymeric component using a separate linker component. The gastric residence structures may be configured to be folded and physically constrained during administration and may be configured to assume an open retention shape upon removal of a constraint. The change between the folded shape and the open retention shape may be mediated by the elastic polymeric component that undergoes elastic deformation when the residence structure is in the folded shape and recoils when the gastric residence structure assumes the open retention shape.

First claim

What is claimed is:

1. A method of making a gastric residence structure comprising an active substance comprising:
forming one or more arms comprising a loadable polymeric component, wherein the loadable polymeric component comprises one or more polymeric materials and at least one active substance; and
connecting the one or more arms to an elastic polymeric component using a separate linker component;
wherein the gastric residence structure is configured to be folded and physically constrained during administration and is configured to assume an open retention shape upon removal of a constraint, wherein change between the folded shape and the open retention shape is mediated by the elastic polymeric component that undergoes elastic deformation when the residence structure is in the folded shape and recoils when the gastric residence structure assumes the open retention shape; and
wherein the linker degrades, dissolves, disassociates, or mechanically weakens in a gastric environment which results in loss of retention shape integrity and passage out of a gastric cavity.

2. The method of claim 1 , wherein the loadable polymeric component comprises polycaprolactone (PCL).

3. The method of claim 1 , wherein the loadable polymeric component comprises, poly(ethylene-co-vinyl acetate) or polyethylene glycol (PEG).

4. The method of claim 1 , wherein the loadable polymeric component comprises at least 10 wt % active substance of the total weight of the loadable polymeric component.

5. The method of claim 1 , wherein the loadable polymeric component comprises 10-50 wt % active substance of the total weight of the loadable polymeric component.

6. The method of claim 1 , wherein the gastric residence structure comprises a plurality of active substances.

7. The method of claim 1 , wherein the at least one active substance comprises a therapeutic agent or a diagnostic agent.

8. The method of claim 1 , wherein the at least one active substance comprises an antiviral agent.

9. The method of claim 1 , wherein the at least one active substance comprises an antiretroviral agent.

10. The method of claim 1 , wherein the at least one active substance comprises an antipsychotic agent.

11. The method of claim 1 , wherein the at least one active substance comprises an immunosuppresive agent.

12. The method of claim 1 , wherein the at least one active substance comprises a neuroprotective agent.

13. The method of claim 1 , wherein the at least one active substance comprises memantine.

14. The method of claim 1 , wherein the at least one active substance comprises buprenorphine.

15. The method of claim 1 , wherein the at least one active substance comprises risperidone.

16. The method of claim 1 , wherein the linker component comprises an enteric polymer.

17. A method of making an orally administrable gastric residence system comprising an active substance comprising: forming one or more arms comprising a loadable polymeric component, wherein the loadable polymeric component comprises one or more polymeric materials and at least one active substance; and connecting the one or more arms to an elastic polymeric component using a separate linker component to form a gastric residence structure, said linker connecting the loadable polymeric component with the elastic polymeric component; wherein the gastric residence structure is configured to be folded and physically constrained during administration and is configured to assume an open retention shape upon removal of a constraint, wherein change between the folded shape and the open retention shape is mediated by the elastic polymeric component that undergoes elastic deformation when the residence structure is in the folded shape and recoils when the gastric residence structure assumes the open retention shape; wherein the linker degrades, dissolves, disassociates, or mechanically weakens in a gastric environment which results in loss of retention shape integrity and passage out of a gastric cavity; and inserting the gastric residence system in the folded shape into a capsule to form an administrable gastric residence system.

18. The method of claim 17 , wherein forming a loadable polymeric component from one or more polymeric materials and at least one active substance comprises powder mixing, solvent loading, melt loading, or physical blending the one or more polymeric materials with the at least one active substance.

19. The method of claim 17 , wherein the loadable polymeric component comprises polycaprolactone (PCL).

20. The method of claim 17 , wherein the loadable polymeric component comprises poly(ethylene-co-vinyl acetate), or polyethylene glycol (PEG).

21. The method of claim 17 , wherein the loadable polymeric component comprises at least 10 wt % active substance of the total weight of the loadable polymeric component.

22. The method of claim 17 , wherein the loadable polymeric component comprises 10-50 wt % active substance of the total weight of the loadable polymeric component.

23. The method of claim 17 , wherein the gastric residence structure comprises a plurality of active substances.

24. The method of claim 17 , wherein the at least one active substance comprises a therapeutic agent or a diagnostic agent.

25. The method of claim 17 , wherein the at least one active substance comprises an antiviral agent.

26. The method of claim 17 , wherein the at least one active substance comprises an antiretroviral agent.

27. The method of claim 17 , wherein the at least one active substance comprises an antipsychotic agent.

28. The method of claim 17 , wherein the at least one active substance comprises an immunosuppresive agent.

29. The method of claim 17 , wherein the at least one active substance comprises a neuroprotective agent.

30. The method of claim 17 , wherein the at least one active substance comprises memantine.

31. The method of claim 17 , wherein the at least one active substance comprises buprenorphine.

32. The method of claim 17 , wherein the at least one active substance comprises risperidone.

33. The method of claim 17 , wherein the linker component comprises an enteric polymer.

34. The method of claim 17 , wherein the capsule is a 000 capsule, a 00 capsule, a 0 capsule, a 1 capsule, a 2 capsule, a 3 capsule, a 4capsule, or a 5 capsule.

35. A method of making a gastric residence structure comprising an active substance comprising:
forming one or more arms comprising a loadable polymeric component, wherein each polymeric component is formed from one or more polymeric materials and at least one active substance, and forming the loadable polymeric component comprises powder mixing, solvent loading, melt loading, or physical blending the one or more polymeric materials with the at least one active substance; and
connecting the one or more arms to an elastic polymeric component using a separate linker component;
wherein the gastric residence structure is configured to be folded and physically constrained during administration and is configured to assume an open retention shape upon removal of a constraint, wherein change between the folded shape and the open retention shape is mediated by the elastic polymeric component that undergoes elastic deformation when the residence structure i

Assignees

• Massachusetts Inst Technology
• Brigham & Womens Hospital Inc
• Tokitae Llc

Inventors

• Bellinger Andrew
• Zhang Shiyi
• Traverso Carlo Giovanni
• Langer Robert S
• Mo Stacy
• Grant Tyler
• Jafari Mousa
• Glettig Dean Liang
• Diciccio Angela
• Wood Jr Lowell L
• Eckhoff Philip A

Classifications

• A61K47/6901

  Conjugates being cells, cell fragments, viruses, ghosts, red blood cells or viral vectors · CPC title

• A61K47/32

  Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone} · CPC title

• A61K31/65

  Tetracyclines · CPC title

• A61K47/58

  obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin · CPC title

• C08G83/006

  After treatment of hyperbranched macromolecules · CPC title