# US 2019/0167643 A1 · Formulations of deferasirox and methods of making the same > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2019/0167643 A1 - Document ID: US20190167643A1 - Status: Published application - Kind: A1 - Application number: 16/268,785 - Filed: 2019-02-06 - Published: 2019-06-06 - Earliest claimed: 2015-06-17 - Assignees: Dispersol Technologies, LLC - Applicants: Dispersol Technologies, LLC - Inventors: Dave A. MILLER; Justin M. KEEN; Sandra U. KUCERA - Web page: https://patentgrep.com/patent/US20190167643A1 ## CPC - A61K 31/4196: 1,2,4-Triazoles - A61K 9/146: {with organic macromolecular compounds} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61P 39/04: Chelating agents - 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 ## Abstract The disclosure provides for improved pharmaceutical compositions containing deferasirox (DFX) and methods of manufacturing the same. In particular, the compositions are prepared using thermokinetic compounding and provide improved properties as well as more efficient methods of manufacture. ## Claims ### Claim 1 A method of making a pharmaceutical composition comprising: (a) providing crystalline deferasirox (DFX) and one or more pharmaceutically acceptable excipients; (b) compounding the materials of step (a) in a thermokinetic mixer at less than or equal to 200° C. for less than about 300 seconds, wherein the thermokinetic compounding of DFX and the one or more pharmaceutically acceptable excipients forms a melt blended pharmaceutical composite. ### Claim 2 (depends on 1) The method of claim 1, wherein said pharmaceutical comprises a second active pharmaceutical ingredient in addition to DFX. ### Claim 3 (depends on 1) The method of claim 1, wherein the one or more pharmaceutically acceptable excipients comprises a pharmaceutical polymer. ### Claim 4 (depends on 1) The method of claim 1, wherein the one or more pharmaceutically acceptable excipients comprises a surfactant. ### Claim 5 (depends on 1) The method of claim 1, wherein the one or more pharmaceutically acceptable excipients comprises one or more surfactants and one or more polymer carriers. ### Claim 6 (depends on 1) The method of claim 1, wherein said composite is an amorphous dispersion. ### Claim 7 (depends on 3) The method of claim 3, wherein the pharmaceutical polymer comprises an agent selected from the group consisting of poly(vinyl acetate)-co-poly(vinylpyrrolidone) copolymer, ethylcellulose, hydroxypropylcellulose, cellulose acetate butyrate, poly(vinylpyrrolidone), poly(ethylene glycol), poly(ethylene oxide), poly(vinyl alcohol), hydroxypropyl methylcellulose, hydroxyethylcellulose, sodium carboxymethyl-cellulose, dimethylaminoethyl methacrylate-methacrylic acid ester copolymer, ethylacrylate-methylmethacrylate copolymer, cellulose acetate phthalate, cellulose acetate trimelletate, poly(vinyl acetate) phthalate, hydroxypropylmethylcellulose phthalate, poly(methacrylate ethylacrylate) (1:1) copolymer, poly(methacrylate methylmethacrylate) (1:1) copolymer, poly(methacrylate methylmethacrylate) (1:2) copolymer, hydroxypropylmethylcellulose acetate succinate and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. ### Claim 8 (depends on 4) The method of claim 4, wherein the one or more surfactants comprises an agent selected from the group consisting of sodium dodecyl sulfate, dioctyl sodium sulphosuccinate, polyoxyethylene (20) sorbitan monooleate, glycerol polyethylene glycol oxystearate-fatty acid glycerol polyglycol esters-polyethylene glycols-glycerol ethoxylate, glycerol-polyethylene glycol ricinoleate-fatty acid esters of polyethyleneglycol-polyethylene glycols-ethoxylated glycerol, vitamin E TPGS and sorbitan laurate. ### Claim 9 (depends on 5) The method of claim 5, wherein the surfactant comprises an agent selected from the group consisting of sodium dodecyl sulfate, dioctyl sodium sulphosuccinate, polyoxyethylene (20) sorbitan monooleate, glycerol polyethylene glycol oxystearate-fatty acid glycerol polyglycol esters-polyethylene glycols-glycerol ethoxylate, glycerol-polyethylene glycol ricinoleate-fatty acid esters of polyethyleneglycol-polyethylene glycols-ethoxylated glycerol, vitamin E TPGS, and sorbitan laurate, and the pharmaceutical polymer comprises an agent selected from a group consisting of poly(vinyl acetate)-co-poly(vinylpyrrolidone) copolymer, ethylcellulose, hydroxypropylcellulose, cellulose acetate butyrate, poly(vinylpyrrolidone), poly(ethylene glycol), poly(ethylene oxide), poly(vinyl alcohol), hydroxypropyl methylcellulose, hydroxyethylcellulose, sodium carboxymethyl-cellulose, dimethylaminoethyl methacrylate-methacrylic acid ester copolymer, ethylacrylate-methylmethacrylate copolymer, cellulose acetate phthalate, cellulose acetate trimelletate, poly(vinyl acetate) phthalate, hydroxypropylmethylcellulose phthalate, poly(methacrylate ethylacrylate) (1:1) copolymer, poly(methacrylate methylmethacrylate) (1:1) copolymer, poly(methacrylate methylmethacrylate) (1:2) copolymer, hydroxypropylmethylcellulose acetate succinate and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. ### Claim 10 (depends on 1) The method of claim 1, wherein said composition remains amorphous per x-ray diffraction analysis following storage in an open container at about 40° C., relative humidity of about 75%, at five weeks. ### Claim 11 (depends on 1) The method of claim 1, wherein the composition comprises about 30%-60% DFX, about 40%-60% DFX, about 30% DFX, 35% DFX, 40% DFX, 45% DFX, 50% DFX, 55% DFX, or 60% DFX. ### Claim 12 (depends on 1) The method of claim 1, wherein the one or more pharmaceutically acceptable excipients comprises a processing agent, such as a plasticizer. ### Claim 13 (depends on 1) The method of claim 1, wherein step (b) is performed at a temperature of about 100° C., about 125° C., about 150° C., about 180° C., or about 100° C. to 200° C. ### Claim 14 (depends on 1) The method of claim 1, wherein the one or more pharmaceutically acceptable excipients comprises a water soluble pharmaceutical polymer. ### Claim 15 (depends on 14) The method of claim 14, wherein the water soluble pharmaceutical polymer comprises a polymer selected from a group consisting of poly(vinyl acetate)-co-poly(vinylpyrrolidone) copolymer, poly(vinylpyrrolidone), cellulose acetate phthalate, poly(vinyl acetate) phthalate, hydroxypropylmethylcellulose phthalate, poly(methacrylate ethylacrylate) (1:1) copolymer, poly(methacrylate methylmethacrylate) (1:1) copolymer, poly(methacrylate methylmethacrylate) (1:2) copolymer, hydroxypropyl methylcellulose, hydroxypropylmethylcellulose acetate succinate, poly(vinyl alcohol), and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. ### Claim 16 (depends on 1) The method of claim 1, wherein the one or more pharmaceutically acceptable excipients comprises a cross-linked pharmaceutical polymer. ### Claim 17 (depends on 16) The method of claim 16, wherein the cross-linked pharmaceutical polymer is, carbomer, crospovidone, or croscarmellose sodium. ### Claim 18 (depends on 1) The method of claim 1, wherein the one or more pharmaceutically acceptable excipients comprises a pharmaceutical polymer of high melt viscosity. ### Claim 19 (depends on 1) The method of claim 1, wherein the one or more pharmaceutically acceptable excipients comprises a thermally labile pharmaceutical polymer. ### Claim 20 (depends on 1) The method of claim 1, wherein the one or more pharmaceutically acceptable excipients comprises poly(methacrylate ethylacrylate) (1:1) copolymer or poly(vinyl acetate)-co-poly(vinylpyrrolidone). ### Claim 21 (depends on 1) The method of claim 1, wherein the one or more pharmaceutically acceptable excipients comprises poly(methacrylate ethylacrylate) (1:1) copolymer and poly(vinyl acetate)-co-poly(vinylpyrrolidone). ### Claim 22 (depends on 1) The method of claim 1, wherein the one or more pharmaceutically acceptable excipients comprises poly(vinyl acetate)-co-poly(vinylpyrrolidone) and hydroxypropylmethylcellulose acetate succinate. ### Claim 23 (depends on 1) The method of claim 1, wherein said composition has a single glass transition temperature. ### Claim 24 (depends on 1) The method of claim 1, wherein the purity of DFX in said composition is about 95%, is about 99%, is about 99.5%, or is about 95% to about 100%. ### Claim 25 (depends on 1) The method of claim 1, wherein the DFX to pharmaceutical polymer ratio is about 2:8 to about 7:3, including about 1:1. ### Claim at position 26 26-138. (canceled)