# US 12,005,058 B2 · Nicotine tablet > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,005,058 B2 - Document ID: US12005058B2 - Status: Granted - Kind: B2 - Application number: 18/348,891 - Filed: 2023-07-07 - Published: 2023-11-02 - Granted: 2024-06-11 - Earliest claimed: 2017-12-08 - Assignees: Fertin Pharma A/S - Applicants: Fertin Pharma A/S - Inventors: Bruno Provstgaard Nielsen; Kent Albin Nielsen - Web page: https://patentgrep.com/patent/US12005058B2 ## CPC - A61K 31/465: Nicotine; Derivatives thereof - 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 9/006: {Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays} - A61K 9/2009: {Inorganic compounds} - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 9/2095: {Tabletting processes} - A61P 25/34: Tobacco-abuse - 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 an orally disintegrating nicotine tablet for nicotine craving relief comprising a pressed powder formulation, the tablet being designed to disintegrate within a period of less than 60 seconds upon oral administration, the powder formulation comprising an amount of nicotine and a pH regulating agent. ## Claims ### Claim 1 An orally disintegrating nicotine tablet for nicotine craving relief comprising a pressed powder formulation, wherein the tablet disintegrates within a period of less than 210 seconds upon oral administration, wherein the pressed powder formulation comprises an amount of nicotine, a pH regulating agent, at least one polyol, and a disintegrant wherein the tablet comprises the polyol in an amount of more than 40% by weight of the tablet, wherein the tablet comprises the disintegrant in an amount of 1-10% by weight of the tablet, wherein the formulation provides a peak saliva pH of more than 7.6 during the first 120 seconds upon oral administration, wherein at least 40% by weight of the nicotine is absorbed through the oral mucosa, and wherein the tablet substantially reduces the side effect of burning. ### Claim 2 (depends on 1) The tablet according to claim 1, wherein the tablet is designed to disintegrate within a period of less than 60 seconds upon oral administration. ### Claim 3 (depends on 1) The tablet according to claim 1, wherein the tablet comprises nicotine in an amount of at least 0.5 mg. ### Claim 4 (depends on 1) The tablet according to claim 1, wherein said nicotine is provided as a nicotine salt. ### Claim 5 (depends on 4) The tablet according to claim 4, wherein the nicotine salt is selected from nicotine ascorbate, nicotine aspartate, nicotine benzoate, nicotine monotartrate, nicotine bitartrate, nicotine chloride, nicotine citrate, nicotine fumarate, nicotine gensitate, nicotine lactate, nicotine mucate, nicotine laurate, nicotine levulinate, nicotine malate nicotine perchlorate, nicotine pyruvate, nicotine salicylate, nicotine sorbate, nicotine succinate, nicotine zinc chloride, nicotine sulfate, nicotine tosylate, nicotine salt hydrates, and any combination thereof. ### Claim 6 (depends on 1) The tablet according to claim 1, wherein said nicotine is provided as a complex between nicotine and an ion exchange resin. ### Claim 7 (depends on 1) The tablet according to claim 1, wherein said nicotine is provided in ionic complex with at least one mucoadhesive water-soluble anionic polymer. ### Claim 8 (depends on 1) The tablet according to claim 1, wherein the tablet is a sublingual tablet. ### Claim 9 (depends on 1) The tablet according to claim 1, wherein the pressed powder comprises at least one polyol and wherein the polyol comprises more than 59% by weight of the tablet. ### Claim 10 (depends on 1) The tablet according to claim 1, wherein the tablet is pressed at a pressure of 2-20 kN. ### Claim 11 (depends on 1) The tablet according to claim 1, wherein the formulation provides a peak saliva concentration of nicotine of more than 0.3 mg/mL and a peak saliva pH of more than 8 during the first 120 seconds upon oral administration. ### Claim 12 (depends on 1) The tablet according to claim 1, wherein the tablet comprises sodium stearyl fumarate (SSF) as a lubricant. ### Claim 13 (depends on 1) The tablet according to claim 1, wherein the tablet comprises pH regulating agent in an amount of at least 2.7 percent by weight of said tablet. ### Claim 14 (depends on 1) The tablet according to claim 1, wherein the tablet has a weight of 25 to 200 mg. ### Claim 15 (depends on 1) The tablet according to claim 1, wherein the at least one polyol is selected from the group consisting of sorbitol, erythritol, xylitol, maltitol, mannitol, lactitol, isomalt, and any combination thereof. ### Claim 16 (depends on 1) The tablet according to claim 1, wherein the at least one polyol is mannitol. ### Claim 17 (depends on 1) The tablet according to claim 1, wherein the disintegrant is selected from the group consisting of starch, pregelatinated starch, modified starch, cellulose, microcrystalline cellulose, alginates, ion-exchange resin, superdisintegrants, and combinations thereof. ### Claim 18 (depends on 1) The tablet according to claim 1, wherein the disintegrant is selected from the group consisting of crosslinked cellulose, crosslinked polyvinyl pyrrolidone (PVP), crosslinked starch, crosslinked alginic acid, natural superdisintegrants, calcium silicate, and combinations thereof. ### Claim 19 (depends on 1) The tablet according to claim 1, wherein the disintegrant comprises at least one of crospovidone, sodium starch glycolate, and croscarmellose. ### Claim 20 An orally disintegrating nicotine tablet for nicotine craving relief comprising a pressed powder formulation, wherein the tablet disintegrates within a period of less than 210 seconds upon oral administration, wherein the pressed powder formulation comprises an amount of nicotine, a pH regulating agent, at least one polyol, and a disintegrant wherein the tablet comprises the polyol in an amount of more than 40% by weight of the tablet, wherein the tablet comprises the disintegrant in an amount of 1-10% by weight of the tablet, wherein the formulation provides a peak saliva pH of more than 7.6 during the first 120 seconds upon oral administration, wherein at least 40% by weight of the nicotine is absorbed through the oral mucosa, and wherein the tablet provides alleviation of nicotine craving within a period of no more than 300 seconds upon oral administration. ### Claim 21 An orally disintegrating nicotine tablet for nicotine craving relief comprising a pressed powder formulation, wherein the tablet disintegrates within a period of less than 210 seconds upon oral administration, wherein the pressed powder formulation comprises an amount of nicotine, a pH regulating agent, at least one polyol, and a disintegrant wherein the tablet comprises the polyol in an amount of more than 40% by weight of the tablet, wherein the tablet comprises the disintegrant in an amount of 1-10% by weight of the tablet, wherein the formulation provides a peak saliva pH of more than 7.6, wherein at least 40% by weight of the nicotine is absorbed through the oral mucosa, and wherein the tablet reduces the side effect of burning. ### Claim 22 (depends on 1) A method of alleviation of nicotine craving by administering said orally disintegrating nicotine tablet according to claim 1.