# US 10,307,400 B2 · Orally disintegrating tablet containing asenapine > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,307,400 B2 - Document ID: US10307400B2 - Status: Granted - Kind: B2 - Application number: 15/426,462 - Filed: 2017-02-07 - Published: 2017-05-25 - Granted: 2019-06-04 - Earliest claimed: 2012-12-11 - Assignees: Alfred E. Tiefenbacher (GmbH & Co. KG) - Applicants: Alfred E. Tiefenbacher (GmbH & Co. KG) - Inventors: Chaitanya Yogananda Gujjar; Bala Ramesha Chary Rallabandi; Pradip Shivraj Patwari; Ansgar Fitzner - Web page: https://patentgrep.com/patent/US10307400B2 ## CPC - A61K 31/407: condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine - A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration} - 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 9/2013: {Organic compounds, e.g. phospholipids, fats} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin} - A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets} - A61K 9/2095: {Tabletting processes} - 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) ## Abstract The present invention relates to an orally disintegrating tablet (ODT) containing asenapine maleate and to a process for preparing the ODT. In a first aspect, the present invention relates to an ODT containing asenapine maleate and low substituted hydroxypropylcellulose. In a second aspect, the present invention relates to an ODT containing crystalline asenapine maleate and the ODT is prepared using conventional tabletting techniques as direct compression and granulation. In a third aspect, the present invention relates to an ODT containing asenapine maleate and a carboxylic acid, and to the use of a carboxylic acid for enhancing storage stability of an asenapine maleate containing ODT. ## Claims ### Claim 1 An orally disintegrating tablet comprising asenapine maleate, a carboxylic acid in an amount of 0.2 to 2.0% by weight based on total weight of the tablet, and one or more pharmaceutical excipients, wherein said tablet is stable at 40° C. and 75% rH for at least 3 months compared to a tablet having no carboxylic acid. ### Claim 2 (depends on 1) The orally disintegrating tablet according to claim 1, wherein the tablet is prepared by dry granulation. ### Claim 3 (depends on 1) The orally disintegrating tablet according to claim 1, wherein the tablet is prepared by wet granulation. ### Claim 4 (depends on 1) The orally disintegrating tablet according to claim 1, wherein said carboxylic acid is a branched or unbranched, saturated or unsaturated carboxylic acid containing 2 to 10 carbon atoms optionally substituted with one or more hydroxy (—OH), amino (—NH2) and/or mercapto (—SH) groups. ### Claim 5 (depends on 1) The orally disintegrating tablet according to claim 1, wherein the carboxylic acid is selected from monocarboxylic acid, dicarboxylic acid, tricarboxylic acid, and mixtures thereof. ### Claim 6 (depends on 1) The orally disintegrating tablet according to claim 1, wherein the carboxylic acid is selected from glycolic acid, oxalic acid, malonic acid, succinic acid, maleic acid, fumaric acid, tartaric acid, malic acid, glutaric acid, citric acid and gluconic acid. ### Claim 7 (depends on 1) The orally disintegrating tablet according to claim 1, wherein the carboxylic acid is a C4 dicarboxylic acid optionally substituted with hydroxy. ### Claim 8 (depends on 1) The orally disintegrating tablet according to claim 1, wherein the carboxylic acid is contained in the tablet in an amount of 0.5 to 1.5% by weight, based on the total weight of the tablet. ### Claim 9 (depends on 7) The orally disintegrating tablet according to claim 7, wherein the C4 dicarboxylic acid is tartaric acid. ### Claim 10 (depends on 1) The orally disintegrating tablet according to claim 1, wherein said excipients comprise one or more disintegrants, surfactants, glidants, lubricants, fillers, flavorants and sweeteners. ### Claim 11 (depends on 1) The orally disintegrating tablet according to claim 1, containing crystalline asenapine maleate. ### Claim 12 (depends on 11) The orally disintegrating tablet according to claim 11, wherein said crystalline asenapine maleate is monoclinic asenapine maleate (form H). ### Claim 13 (depends on 1) The orally disintegrating tablet according to claim 1, wherein said asenapine maleate is in a micronized form and has a particle size distribution in which D(90) is equal or less than 90 μm, D(50) is equal or less than 20 μm and D(10) is equal or less than 10 μm. ### Claim 14 (depends on 8) The orally disintegrating tablet according to claim 8 wherein the carboxylic acid is contained in the tablet in an amount of 0.5 to 1.5% by weight based on the total weight of the tablet. ### Claim 15 (depends on 8) The orally disintegrating tablet according to claim 8 wherein the carboxylic acid is contained in the tablet in an amount of 0.75 to 1.25% by weight, based on the total weight of the tablet. ### Claim 16 An orally disintegrating tablet comprising asenapine maleate, a carboxylic acid in an amount of 0.75 to 2.5% by weight based on total weight of the tablet, and one or more pharmaceutical excipients, wherein said tablet is stable at 40° C. and 75% rH for at least 3 months compared to a tablet having no carboxylic acid.