# US 11,439,650 B2 · Thermo-kinetic mixing for pharmaceutical applications > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,439,650 B2 - Document ID: US11439650B2 - Status: Granted - Kind: B2 - Application number: 16/866,676 - Filed: 2020-05-05 - Published: 2020-08-20 - Granted: 2022-09-13 - Earliest claimed: 2007-08-21 - Assignees: Board of Regents, The University of Texas System; Dispersol Technologies, LLC - Applicants: Board of Regents, the University of Texas System; Dispersol Technologies, LLC - Inventors: Chris Brough; James W. McGinity; Dave A. Miller; James C. DiNunzio; Robert O. Williams, III - Web page: https://patentgrep.com/patent/US11439650B2 ## CPC - A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone - A61J 3/00: Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms - A61J 3/07: into the form of capsules or similar small containers for oral use - A61J 3/10: into the form of compressed tablets (tablet presses B30B11/00) - A61K 9/146: {with organic macromolecular compounds} - A61K 9/1694: {resulting in granules or microspheres of the matrix type containing more than 5% of excipient} - A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets} - A61K 31/343: condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone - A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin - A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone} - A61K 47/38: Cellulose; Derivatives thereof - A61P 31/10: Antimycotics - 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) - A61J: CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract Compositions and methods for making a pharmaceutical dosage form include making a pharmaceutical composition that includes one or more active pharmaceutical ingredients (API) with one or more pharmaceutically acceptable excipients by thermokinetic compounding into a composite. Compositions and methods of preprocessing a composite comprising one or more APIs with one or more excipients include thermokinetic compounding, comprising thermokinetic processing the APIs with the excipients into a composite, wherein the composite can be further processed by conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding. ## Claims ### Claim 1 A pharmaceutical composition comprising at least one active pharmaceutical ingredient (API) with at least one pharmaceutically acceptable excipient thermokinetically processed into a composite, wherein the at least one API comprises a thermally labile or poorly water-soluble API, and wherein the composite is processed at an average temperature that is at or below a glass transition temperature or a melting point of the at least one API. ### Claim 2 (depends on 1) The pharmaceutical composition of claim 1, wherein the at least one pharmaceutically acceptable excipient comprises a polymer having a high melt viscosity. ### Claim 3 (depends on 1) The pharmaceutical composition of claim 1, wherein the at least one pharmaceutically acceptable excipient comprises a polymer selected from the group consisting of methylcellulose, ethylcellulose, hydroxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxybutylcellulose, hydroxyethyl methylcellulose, hydroxypropyl methylcellulose, carboxymethylcellulose, hydroxypropyl methylcellulose acetate succinate, cellulose acetate phthalate, cellulose acetate trimellate, hydroxypropyl methylcellulose phthalate, cellulose acetate butyrate, polyvinylpyrrolidones, polyacrylates, polymethacrylates, polyvinyl alcohols, polyethylene glycols, polyvinyl acetate polyvinylpyrrolidone copolymers, polyethylene oxides, dimethylaminoethyl methacrylate-methacrylic acid ester copolymers, ethylacrylate-methylmethacrylate copolymers, poly(methyacrylate ethylacrylate) copolymers, poly(methacrylate methylmethacrylate) copolymers, starches, pectins, polysaccharides, gum arabic, guar gum, and xanthan gum. ### Claim 4 (depends on 1) The pharmaceutical composition of claim 1, wherein the composition comprises less than about 1.0% degradation products of the at least one API. ### Claim 5 (depends on 1) The pharmaceutical composition of claim 1, wherein, after processing, the at least one API has at least about 94% drug potency as compared to the at least one API before processing. ### Claim 6 (depends on 1) The pharmaceutical composition of claim 1, wherein the pharmaceutical composition does not comprise a processing agent. ### Claim 7 (depends on 1) The pharmaceutical composition of claim 1, wherein the composite is a single phase, amorphous composite. ### Claim 8 (depends on 1) The pharmaceutical composition of claim 1, wherein the at least one API comprises a molecule selected from the group consisting of a small organic molecule, a protein, a peptide, and a polynucleic acid. ### Claim 9 (depends on 1) The pharmaceutical composition of claim 1, wherein the composite is further processed by hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding. ### Claim 10 (depends on 1) The pharmaceutical composition of claim 1, wherein the composite is shaped into a dosage form that is a tablet, a capsule, or a pellet.