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Generated: December 18, 2017

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Title: Proteinoid microspheres and methods for preparation and use thereof
Abstract:Improved proteinoid microspheres and methods for their preparation and use as oral delivery systems for pharmaceutical agents are described. The proteinoid microspheres are soluble within selected pH ranges within the gastrointestinal tract and display enhanced stability towards at least one of photolysis or decomposition over time. The proteinoid microspheres are prepared from proteinoids having between 2 and 8 amino acids and having a molecular weight of about 1000 daltons.
Inventor(s): Milstein; Sam J. (Brooklyn, NY), Kantor; Martin L. (Mamaroneck, NY)
Assignee: Emisphere Technologies, Inc. (Hawthorne, NY)
Filing Date:Jul 27, 1992
Application Number:07/920,346
Claims:1. A composition comprising:

(A) a biologically active agent encapsulated within,

(B) a microsphere carrier, said carrier comprising a proteinoid comprising

(i) at least one monomer selected from the group consisting of tyrosine and phenylalanine;

(ii) at least one monomer selected from the group consisting of glutamic acid, pyroglutamic acid, glutamine, and aspartic acid; and

(iii) optionally at least one monomer selected from the group consisting of lysine, arginine, and ornithine,

said proteinoid being soluble within a selected pH range.

2. A composition as defined in claim 1, wherein said proteinoid forms a wall and said biologically active agent is encapsulated within said wall.

3. A composition as defined in claim 1, wherein said proteinoid is an acid-soluble proteinoid.

4. A composition as defined in claim 1, wherein said proteinoid is a base-soluble proteinoid.

5. A composition as defined in claim 1, wherein said biologically active agent is a monoclonal antibody.

6. A composition comprising a monoclonal antibody encapsulated within a proteinoid microsphere, said microsphere having a proteinoid wall comprising:

(i) at least one monomer selected from the group consisting of tyrosine and phenylalanine;

(ii) at least one monomer selected from the group consisting of glutamic acid, pyroglutamic acid, glutamine, and aspartic acid; and

(iii) optionally at least one monomer selected from the group consisting of lysine, arginine, and ornithine,

said proteinoid being soluble within a selected pH range.

7. The composition of claim 1, wherein said biologically active agent comprises at least one protein.

8. The composition of claim 7, wherein said protein comprises erythropoietin.

9. The composition of claim 7, wherein said protein comprises alpha interferon.

10. The composition of claim 7, wherein said protein comprises calcitonin.

11. The composition of claim 7, wherein said protein comprises insulin.

12. The composition of claim 7, wherein said protein comprises atrial naturetic factor.

13. The composition of claim 7, wherein said protein comprises interleukin II.

14. The composition of claim 7, wherein said protein comprises M-protein.

15. The composition of claim 7, wherein said protein comprises human growth factor.

16. The composition of claim 7, wherein said protein comprises bovine growth factor.

17. The composition of claim 1, wherein said biologically active agent comprises at least one polysaccharide.

18. The composition of claim 17, wherein said polysaccharide comprises heparin.

19. The composition of claim 1, wherein said biologically active agent comprises an antigen.

20. The composition of claim 1, wherein said biologically active agent comprises aspirin.

21. The composition of claim 1, wherein said biologically active agent comprises a quinolone.

22. The composition of claim 1, wherein said biologically active agent comprises an antimicrobial agent.

23. The composition of claim 3, wherein the monoclonal antibody in murine IgG.
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Federal Trade Commission

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