# US 9,867,780 B2 · Optimized pharmaceutical formulation for the treatment of inflammatory conditions of the esophagus > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 9,867,780 B2 - Document ID: US9867780B2 - Status: Granted - Kind: B2 - Application number: 15/107,735 - Filed: 2014-12-18 - Published: 2016-11-10 - Granted: 2018-01-16 - Earliest claimed: 2013-12-23 - Assignees: Dr. Falk Pharma GmbH - Applicants: Dr. Falk Pharma GmbH - Inventors: Roland Greinwald; Ralph Mueller; Markus Proels; Rudolf Wilhelm - Web page: https://patentgrep.com/patent/US9867780B2 ## CPC - A61K 9/0056: {Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals} - A61K 9/0007: {Effervescent (A61K9/0065 takes precedence)} - A61K 9/2013: {Organic compounds, e.g. phospholipids, fats} - A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048}) - A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system - A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - 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 Disclosed is an optimized pharmaceutical formulation for the treatment of inflammatory conditions of the esophagus. A pharmaceutical formulation in the form of an orodispersible effervescent tablet is stable, easy to produce, and can be used without dissolving same in a liquid. It is not necessary to drink anything with the tablet as this would reduce the time that the budesonide solution remains in the affected regions of the esophagus. The effervescent tablet of the invention surprisingly resulted in an unexpectedly high rate of histological remission in patients with active eosinophilic esophagitis. ## Claims ### Claim 1 An orodispersible effervescent tablet containing: (a) 0.25 mg to 5 mg of budesonide; (b) a salt of at least one pharmacologically acceptable acid that, in an aqueous environment, can release a gas with a further acid, wherein said salt is selected from the group consisting of NaHCO3, Na2CO3, KHCO3, K2CO3, CaCO3, and mixtures thereof; (c) a pharmaceutically acceptable weak acid or salt thereof that decreases the pH value in an aqueous solution, wherein said weak acid is selected from the group consisting of disodium citrate, monosodium citrate, and mixtures thereof; and (d) sucralose in an amount of 0.1 to 1.0% by weight, based on the weight of the finished tablet; wherein: the effervescent tablet has a mass of 100 mg to 200 mg. ### Claim 2 (depends on 1) The orodispersible effervescent tablet according to claim 1, wherein said tablet has a diameter of 5 to 10 mm. ### Claim 3 (depends on 1) The orodispersible effervescent tablet according to claim 1, wherein said tablet has a height of 1.5 to 3.0 mm. ### Claim 4 (depends on 1) The orodispersible effervescent tablet according to claim 1, wherein said tablet has a fracture strength of 10 N to 100 N. ### Claim 5 (depends on 1) The orodispersible effervescent tablet according to claim 1, wherein said tablet has a friability of at most 5%. ### Claim 6 (depends on 1) The orodispersible effervescent tablet according to claim 1, wherein said tablet further contains 0.5 to 10% by weight polyvinylpyrrolidone, based on the weight of the finished tablet. ### Claim 7 (depends on 1) The orodispersible effervescent tablet according to claim 1, wherein said tablet further contains 0.01 to 0.2% by weight docusate Na, based on the weight of the finished tablet. ### Claim 8 (depends on 1) The orodispersible effervescent tablet according to claim 1, wherein said tablet further contains 2.0 to 10.0% by weight mannitol, based on the weight of the finished tablet. ### Claim 9 (depends on 1) The orodispersible effervescent tablet according claim 1, wherein said tablet further contains 1.0 to 10.0% by weight macrogol 6000, based on the weight of the finished tablet. ### Claim 10 (depends on 1) The orodispersible effervescent tablet according to claim 1, wherein said tablet further contains 0.05 to 0.5% by weight magnesium stearate, based on the weight of the finished tablet. ### Claim 11 (depends on 1) A method of treating an inflammatory condition of the esophagus, said method comprising the step of administering the orodispersible effervescent tablet according to claim 1 to a patient in need thereof. ### Claim 12 (depends on 11) The method of claim 11, wherein the inflammatory condition of the esophagus being treated is eosinophilic esophagitis.