Pharmaceutical compositions and methods for fabrication of solid masses comprising glucose regulating proteins
View Patent ↗Embodiments of the invention provide shaped masses comprising one or more drugs such as proteins or polypeptides and methods for forming such shaped masses. One embodiment provides a shaped mass comprising a drug such as a protein or polypeptide having a biological activity in the body of a mammal. The shaped mass is formed by compression of a precursor material comprising the drug wherein an amount of biologically active drug in the mass is a preserved above a minimum level. Drugs which may be incorporated into the shaped mass may include one or more glucose regulating proteins such as insulin, incretins; and immunoglobulins such as TNF-inhibiting antibodies or interleukin neutralizing antibodies. Embodiments of the shaped mass may be incorporated into a tissue penetrating member which is inserted into the intestinal wall allowing for the oral delivery of proteins and peptides which would otherwise be degraded in the intestinal tract.
1. A shaped mass comprising insulin, the shaped mass formed by compression of a precursor material comprising insulin, wherein at least about 80% of the insulin in the shaped mass is biologically active, the shaped mass having a density in a range of about 0.95 to about 1.15 mg/mm 3 , and wherein the weight percentage of insulin in the shaped mass is in a range of about 80% to 95%, wherein the shaped mass comprises a pharmaceutical excipient.
2. The shaped mass of claim 1 , wherein the density is in a range of about 0.98 to about 1.10 mg/mm 3 .
3. The shaped mass of claim 1 , wherein at least about 95% of the insulin in the shaped mass is biologically active.
4. The shaped mass of claim 1 , wherein the shaped mass comprises between about 0.2 to about 0.8 mg of insulin.
5. The shaped mass of claim 1 , wherein the insulin comprises human insulin.
6. The shaped mass of claim 1 , wherein the compression is performed in a mold.
7. The shaped mass of claim 1 , wherein the shaped mass is formed by compression of a powder comprising insulin.
8. The shaped mass of claim 1 , wherein the shaped mass has a pellet or cylindrical shape.
9. The shaped mass of claim 1 , wherein the shaped mass has a tablet shape.
10. The shaped mass of claim 1 , wherein the shaped mass has a tissue penetrating shape.
11. The shaped mass of claim 1 , wherein the shaped mass comprises a biodegradable material which breaks down in a wall of a small intestine so as to release the insulin.
12. The shaped mass of claim 1 , wherein the pharmaceutical excipient comprises at least one of a lubricant, a binding agent, a bulking agent or PEG.
13. The shaped mass of claim 12 , wherein the binder is povidone.
14. The shaped mass of claim 12 , wherein the bulking agent is mannitol.
15. The shaped mass of claim 12 , wherein the lubricant is PEG.
16. The shaped mass of claim 12 , wherein the lubricant is PEG, the bulking agent is mannitol and the binder is povidone.
17. A shaped mass comprising insulin, wherein:
i) at least about 80% of the insulin in the shaped mass is biologically active;
ii) the shaped mass has a density in a range of about 0.95 to about 1.15 mg/mm 3 ;
iii) the weight percentage of insulin in the shaped mass is in a range of about 80% to 95%; and;
iv) the shaped mass degrades in a tissue to release insulin into a bloodstream to treat a blood glucose regulation disorder, and
wherein the shaped mass comprises a pharmaceutical excipient.
18. The shaped mass of claim 17 , wherein the tissue is an intestinal tissue or an intestinal wall tissue.
19. The shaped mass of claim 18 , where the intestinal wall is a wall of a small intestine.
20. The shaped mass of claim 17 , wherein the tissue is an intramuscular tissue.
21. The shaped mass of claim 17 , wherein the density is in a range of about 0.98 to about 1.10 mg/mm 3 .
22. The shaped mass of claim 17 , wherein the blood glucose regulation disorder is diabetes.
23. The shaped mass of claim 17 , wherein the shaped mass comprises about 0.2 to about 0.8 mg of insulin.
24. The shaped mass of claim 17 , wherein the insulin comprises human insulin.