# US 12,214,019 B2 · Pharmaceutical compositions and methods for fabrication of solid masses comprising polypeptides and/or proteins > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,214,019 B2 - Document ID: US12214019B2 - Status: Granted - Kind: B2 - Application number: 17/694,507 - Filed: 2022-03-14 - Published: 2022-06-30 - Granted: 2025-02-04 - Earliest claimed: 2014-05-15 - Assignees: Rani Therapeutics, LLC - Applicants: Rani Therapeutics, LLC - Inventors: Mercedes Morales; Mir Imran; Radhika Korupolu; Mir Hashim - Web page: https://patentgrep.com/patent/US12214019B2 ## CPC - A61K 38/28: Insulins - A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates} - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 9/2031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers} - A61K 9/2072: {characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms (A61K9/0004, A61K9/0056, A61K9/0065 take precedence)} - A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets} - A61K 38/26: Glucagons - A61P 3/10: for hyperglycaemia, e.g. antidiabetics - A61P 35/00: Antineoplastic agents - C07K 16/00: Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies - C07K 16/241: {Tumor Necrosis Factors} - C07K 16/244: {Interleukins [IL]} - C07K 2317/21: from primates, e.g. man - C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered - C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00) ## Abstract 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. ## Claims ### Claim 1 A shaped mass comprising a biologically active protein or polypeptide and a pharmaceutical excipient, the shaped mass formed by compression of a precursor material comprising the biologically active protein or polypeptide, wherein an amount of biologically active protein or polypeptide 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/mm3 to about 1.15 mg/mm3. ### Claim 2 (depends on 1) The shaped mass of claim 1, wherein the density is in a range of about 0.86 mg/mm to about 1.05 mg/mm3. ### Claim 3 (depends on 1) The shaped mass of claim 1, wherein the precursor material has a particle size in the range of about 50 μm to about 450 μm. ### Claim 4 (depends on 1) The shaped mass of claim 1, wherein the shaped mass comprises a degradable material. ### Claim 5 (depends on 1) The shaped mass of claim 1, wherein the precursor material is a powder comprising the protein or polypeptide. ### Claim 6 (depends on 1) The shaped mass of claim 1, wherein the precursor material is a slurry comprising the protein or polypeptide. ### Claim 7 (depends on 1) The shaped mass of claim 1, wherein the protein or polypeptide comprises an immunoglobulin. ### Claim 8 (depends on 7) The shaped mass of claim 7, wherein the immunoglobulin comprises an antibody. ### Claim 9 (depends on 1) The shaped mass of claim 1, wherein the protein or polypeptide has an affinity for an antigen. ### Claim 10 (depends on 1) The shaped mass of claim 1, wherein the shaped mass has a pellet or cylindrical shape. ### Claim 11 (depends on 1) The shaped mass of claim 1, wherein the shaped mass has a tablet shape. ### Claim 12 (depends on 1) The shaped mass of claim 1, wherein the shaped mass has a tissue-penetrating shape. ### Claim 13 (depends on 1) The shaped mass of claim 1, wherein the shaped mass is configured to degrade in a wall of a small intestine so as to release the protein or polypeptide. ### Claim 14 (depends on 1) The shaped mass of claim 1, wherein the pharmaceutical excipient comprises at least one of a lubricant, a binding agent, or a bulking agent. ### Claim 15 (depends on 1) The shaped mass of claim 1, wherein the shaped mass comprises a TNF inhibiting antibody. ### Claim 16 (depends on 15) The shaped mass of claim 15, wherein the TNF inhibiting antibody comprises adalimumab. ### Claim 17 (depends on 16) The shaped mass of claim 16, wherein the shaped mass comprises from about 1 mg to about 4 mg of adalimumab. ### Claim 18 A shaped mass comprising a biologically active protein or polypeptide and a pharmaceutical excipient, the shaped mass formed by compression of a precursor material comprising the biologically active protein or polypeptide, wherein a percentage by weight of biologically active protein or polypeptide 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/mm3 to about 1.15 mg/mm3. ### Claim 19 A shaped mass comprising a biologically active protein or polypeptide and a pharmaceutical excipient, the shaped mass formed by compression of a precursor material comprising the biologically active protein or polypeptide, wherein an amount of biologically active protein or polypeptide 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/mm3 to about 1.15 mg/mm3.