Modified hydrolyzed vegetable protein microspheres and methods for preparation and use thereof

• US 5,972,387 A
• Filed: 11/21/1994
• Issued: 10/26/1999
• Est. Priority Date: 12/21/1992
• Status: Expired due to Fees

• Current Assignee: Emisphere Technologies, Inc. (Novo Nordisk A/S)
• Original Assignee: Emisphere Technologies, Inc. (Novo Nordisk A/S)
• Inventors: Milstein, Sam J., Barantsevitch, Evgueni N.
• Primary Examiner(s): Chan, Christina Y.
• Assistant Examiner(s): LUBET, MARTHA T
• Application Number:
  US08/342,900
• Time in Patent Office: 1,800 Days
• Field of Search: 424/450, 424/451, 424/464, 424/484, 424/488, 424/489, 424/490, 424/491, 424/130.1, 424/164.1, 424/198.1, 424/195.11, 514/12, 530/303, 530/307, 530/316, 530/324, 530/350, 530/345, 530/357, 530/370, 530/378, 530/387.1
• US Class Current: 424/491
• CPC Class Codes: A61K 9/1658 Proteins, e.g. albumin, gelatin

Abstract

Modified hydrolyzed vegetable protein microspheres and methods for their preparation and use as oral delivery systems for pharmaceutical agents are described.

Claims

1. A microsphere comprising

(a) a hydrolyzed vegetable protein modified with a monofunctional amine reactive modifying agent;

and

(b) a biologically active agent;

wherein said microsphere is hollow and said biologically active agent is encapsulated therein.

2. A microsphere according to claim 1, wherein said amine reactive modifying agent is selected from the group consisting of benzene sulfonyl chloride and benzoyl chloride.

3. A microsphere according to claim 1, wherein said biologically-active agent is selected from the group consisting of a protein, a polysaccharide, an antigen, a monoclonal antibody, insulin, calcitonin, and erythropoietin.

4. A microsphere according to claim 1, wherein said biologically-active agent comprises a protein.

5. A microsphere according to claim 4, wherein said protein comprises insulin.

6. A microsphere according to claim 4, wherein said protein comprises human growth hormone.

7. A microsphere according to claim 4, wherein said protein comprises bovine growth hormone.

8. A microsphere according to claim 4, wherein said protein comprises interferon.

9. A microsphere according to claim 4, wherein said protein comprises interleukin II.

10. A microsphere according to claim 4, wherein said protein comprises atrial naturetic factor.

11. A microsphere according to claim 4, wherein said protein comprises calcitonin.

12. A microsphere according to claim 1, wherein said biologically active agent comprises a polysaccharide.

13. A microsphere according to claim 12, wherein said polysaccharide comprises heparin.

14. A microsphere according to claim 1, wherein said biologically active agent comprises an antigen.

15. A microsphere according to claim 1, wherein said biologically active agent comprises a monoclonal antibody.

16. A microsphere according to claim 1, wherein said biologically active agent comprises aspirin.

17. A microsphere according to claim 1, wherein said biologically active agent comprises erythropoietin.

18. A microsphere according to claim 1, where in said biologically active agent comprises a nonsteroidal anti-inflammatory drug.

19. A microsphere according to claim 1, wherein said biologically active agent comprises an antimicrobial agent.

20. A microsphere according to claim 1, wherein said biologically active agent comprises quinolone.