Claims for Patent: 12,539,299

Summary for Patent: 12,539,299

Title:	Oral formulation of a therapeutic compound
Abstract:	The present invention provides a pharmaceutical tablet formulation of tenapanor that is chemically stable and soluble comprising greater than about 6% w/w of amorphous tenapanor in its bis-HCl form, an acidifying agent, an antioxidant, a disintegrant, a lubricant, a glidant, a filler, and an immediate release coating, wherein the total chloride content of the active ingredient is greater than 5.82% and the particle diameter distribution D50 is from about from about 18 μm to about 22 μm.
Inventor(s):	Cecilia Gunnarsson, Magnus Swenson, Hanna MATIC, John Salomonsson, Eva Karlsson
Assignee:	AstraZeneca AB
Application Number:	US18/265,173
Patent Claims:	1. A process comprising: providing a first blend by blending tenapanor, propyl gallate and tartaric acid with hydroxypropyl cellulose; milling said first blend to remove lumps; and providing a second blend by adding stearic acid to said first blend during or after the milling step and optionally blending said second blend; to provide a pharmaceutical formulation, wherein the pharmaceutical formulation comprises greater than 6% w/w of tenapanor bis-HCl as an active ingredient and a pharmaceutically acceptable excipient, wherein the total chloride content of said active ingredient is greater than 5.82%. 2. The process of claim 1, further comprising compressing the second blend into tablets. 3. The process of claim 2, wherein said tablets comprise 30 mg of tenapanor. 4. The process of claim 2, wherein said tablets comprise 50 mg of tenapanor. 5. The process of claim 1, further comprising compacting said second blend. 6. The process of claim 5, wherein the second blend is roller compacted. 7. The process of claim 6, wherein the compacted second blend is milled. 8. The process of claim 7, wherein further stearic acid is added to the milled second blend to provide a third blend. 9. The process of claim 8, further comprising compressing said third blend into tablets. 10. The process of claim 1, wherein tenapanor is spray-dried. 11. The process of claim 10, wherein tenapanor is spray-dried using a water ethanol solvent mixture. 12. The process of claim 1, wherein tenapanor is a bis-HCl salt in amorphous form. 13. The process of claim 1, further comprising administering the pharmaceutical formulation to a human to treat irritable bowel syndrome. 14. The process of claim 1, further comprising administering the pharmaceutical formulation to a human in need of phosphate lowering to inhibit phosphate uptake in the gastrointestinal tract of the human. 15. A pharmaceutical formulation prepared by the process of claim 1.