# US 11,077,112 B2 · Formulation and treatment methods > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,077,112 B2 - Document ID: US11077112B2 - Status: Granted - Kind: B2 - Application number: 15/764,247 - Filed: 2016-09-29 - Published: 2018-08-23 - Granted: 2021-08-03 - Earliest claimed: 2015-09-29 - Assignees: Prodrugxtend Pty Ltd - Applicants: Prodrugxtend Pty Ltd - Inventors: Timothy Florin; Amirali Popat; Siddharth Jambhrunkar - Web page: https://patentgrep.com/patent/US11077112B2 ## CPC - A61K 31/52: Purines, e.g. adenine - A61K 9/0031: {Rectum, anus} - A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration} - A61K 9/08: Solutions {(composition of solutions A61K47/00)} - A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} - 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 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin} - A61K 9/28: Dragees; Coated pills or tablets {, e.g. with film or compression coating (A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209)} - A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system - 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 invention relates to pharmaceutical compositions comprising 6-thioguanidine (6-TG) wherein the composition is formulated for release of 6-TG in the distal intestine. Methods for treating a disease or condition of the distal ileum that responds to 6-TG wherein the 6-TG is released in the distal intestine are also disclosed. ## Claims ### Claim 1 A pharmaceutical composition comprising 6-TG and a homogeneous erodible hydrophilic polymer matrix, wherein the composition is formulated for oral administration and provides release of at least 35% of the 6-TG in vitro at about pH 6 to about pH 7.5 after approximately 12 hours. ### Claim 2 (depends on 1) A pharmaceutical composition according to claim 1 in solid dosage form. ### Claim 3 (depends on 1) A pharmaceutical composition according to claim 1 comprising an enteric coating. ### Claim 4 (depends on 1) A pharmaceutical composition according to claim 1 wherein the composition is adapted to provide substantially zero order kinetics of 6-TG release between approximately 12 hours and 24 hours from oral administration. ### Claim 5 (depends on 1) A pharmaceutical composition according to claim 1 wherein the composition provides release of at least 60% of the 6-TG in vitro at about pH 6 to about pH 7.5 after approximately 12 hours. ### Claim 6 (depends on 1) A pharmaceutical composition according to claim 1, wherein the composition is adapted to avoid substantial systemic concentrations of 6-TG. ### Claim 7 (depends on 1) The pharmaceutical composition according to claim 1, wherein the composition provides release of at least 50%, 55%, 60%, 65%, 70%, 75%, 80%, 85%, 90% or 95% of the 6-TG in vitro at about pH 6 to about pH 7.5 after approximately 12 hours. ### Claim 8 (depends on 1) A pharmaceutical composition according to claim 1 in microparticulate dosage form. ### Claim 9 (depends on 1) The pharmaceutical composition according to claim 1 wherein the composition provides release of at least 45% of the 6-TG in vitro at about pH 6 to about pH 7.5 after approximately 12 hours. ### Claim 10 (depends on 1) A pharmaceutical composition according to claim 1, wherein the pH is about 6. ### Claim 11 (depends on 1) A pharmaceutical composition according to claim 1, wherein the pH is about 7.5. ### Claim 12 (depends on 1) A pharmaceutical composition according to claim 1, wherein the homogeneous erodible hydrophilic polymer matrix comprises polyethylene oxides. ### Claim 13 (depends on 1) A pharmaceutical composition according to claim 1, wherein the homogeneous erodible hydrophilic polymer matrix comprises both a hydrophilic and a hydrophobic polymer. ### Claim 14 (depends on 13) A pharmaceutical composition according to claim 13, wherein the homogeneous erodible hydrophilic polymer matrix comprises ethyl cellulose. ### Claim 15 (depends on 1) A pharmaceutical composition according to claim 1, wherein the homogeneous erodible hydrophilic polymer matrix comprises polyethylene oxides and the pharmaceutical composition comprises an enteric coating. ### Claim 16 (depends on 1) A pharmaceutical composition according to claim 1, wherein the homogeneous erodible hydrophilic polymer matrix comprises polyethylene oxides and ethyl cellulose, and the pharmaceutical composition comprises an enteric coating.