PHARMACEUTICAL COMPOSITIONS AND METHODS FOR FABRICATION OF SOLID MASSES COMPRISING POLYPEPTIDES AND/OR PROTEINS
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 - 20 . (canceled)
21 . A shaped mass comprising a biologically active incretin and a pharmaceutical excipient, the shaped mass formed by compression of a precursor material comprising the biologically active incretin, wherein an amount of biologically active incretin in the shaped mass is at least 70% of that in the precursor material, the shaped mass having a density in a range of about 0.80 mg/mm 3 to about 1.15 mg/mm 3 .
22 . The shaped mass of claim 21 , wherein the density is in a range of about 0.86 mg/mm 3 to about 1.05 mg/mm 3 .
23 . The shaped mass of claim 21 , wherein the precursor material has a particle size in the range of about 50 μm to about 450 μm.
24 . The shaped mass of claim 21 , wherein the shaped mass comprises a degradable material.
25 . The shaped mass of claim 21 , wherein the precursor material is a powder comprising the incretin.
26 . The shaped mass of claim 21 , wherein the precursor material is a slurry comprising the incretin.
27 . The shaped mass of claim 21 , wherein the incretin comprises exenatide.
28 . The shaped mass of claim 21 , wherein the shaped mass has a pellet or cylindrical shape.
29 . The shaped mass of claim 21 , wherein the shaped mass has a tablet shape.
30 . The shaped mass of claim 21 , wherein the shaped mass has a tissue-penetrating shape.
31 . The shaped mass of claim 21 , wherein the shaped mass is configured to degrade in a wall of a small intestine so as to release the incretin.
32 . The shaped mass of claim 21 , wherein the pharmaceutical excipient comprises at least one of a lubricant, a binding agent, or a bulking agent.
33 . The shaped mass of claim 27 , wherein the shaped mass comprises from about 0.2 mg to about 5 mg of exenatide.
34 . The shaped mass of claim 27 , wherein the shaped mass comprises from about 0.2 mg to about 1 mg of exenatide.
35 . The shaped mass of claim 27 , wherein the density of the shaped mass is in a range of 1.04±0.10 mg.
36 . A shaped mass comprising a biologically active incretin and a pharmaceutical excipient, the shaped mass formed by compression of a precursor material comprising the biologically active incretin, wherein a percentage by weight of biologically active incretin in the shaped mass is at least 70% relative to that of the precursor material prior to formation of the shaped mass, the shaped mass having a density in a range of about 0.80 mg/mm 3 to about 1.15 mg/mm 3 .
37 . The shaped mass of claim 36 , wherein the incretin comprises exenatide.
38 . A shaped mass comprising a biologically active incretin and a pharmaceutical excipient, the shaped mass formed by compression of a precursor material comprising the biologically active incretin, wherein an amount of biologically active incretin in the shaped mass is at least 80% relative to that in the precursor material prior to formation of the shaped mass, the shaped mass having a density in a range of about 0.80 mg/mm 3 to about 1.15 mg/mm 3 .
39 . The shaped mass of claim 38 , wherein the incretin comprises exenatide.