Pouch containing nicotine in free salt form

• US 9,161,908 B2
• Filed: 03/28/2012
• Issued: 10/20/2015
• Est. Priority Date: 03/29/2011
• Status: Active Grant

• Current Assignee: Helix Innovations GmbH, Nyz Ab
• Original Assignee: Tillce AB, Wm17 Holding AG
• Inventors: Nilsson, Per-Gunnar
• Primary Examiner(s): Justice, Gina
• Application Number:
  US14/008,367
• Publication Number:
  US 20140017286A1
• Time in Patent Office: 1,301 Days
• Field of Search: 424/489, 131/273
• US Class Current: 1/1
• CPC Class Codes: A24B 15/16 of tobacco substitutes
• CPC Class Codes: A61K 31/465 Nicotine; Derivatives thereof
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/22 Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: 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
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/009 Sachets, pouches characterised by the material or function of the envelope with gastric retention A61K9/0065; sachets which are not administered but function merely as a container are classified according to the content, e.g. sachets comprising powder for reconstitution of a drink A61K9/0095
• CPC Class Codes: A61K 9/145 with organic compounds
• CPC Class Codes: A61K 9/1611 Inorganic compounds
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61K 9/1635 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61P 25/34 Tobacco-abuse

Abstract

The invention relates to a product for oral delivery of nicotine containing a core comprising a powder of at least one free nicotine salt, at least one pH adjusting agent and at least one filler, and a water insoluble pouch, wherein said pouch is permeable for saliva and therein dissolved parts of the powder, wherein said product upon contact with purified water gives a pH of at least 6. The invention also relates to a method to manufacture such a product.

Claims

1. A product for oral delivery of nicotine containing a core comprising a powder of

a) at least one free nicotine salt

b) at least one pH adjusting agent

c) at least one filler

and a water insoluble pouch, wherein said pouch is permeable for saliva and therein dissolved parts of the powder, wherein said product upon contact with purified water gives a pH of at least 6 and wherein said powder being substantially free from adsorbed and/or absorbed nicotine.

2. The product according to claim 1, wherein said nicotine salt is water soluble.

3. The product according to claim 1, wherein said nicotine salt is selected from the group consisting of nicotine hydrochloride, nicotine dihydrochloride, nicotine monotartrate, nicotine bitartrate, nicotine bitartrate dihydrate, nicotine sulphate, nicotine zinc chloride monohydrate and nicotine salicylate, and mixtures thereof.

4. The product according to claim 3, wherein said nicotine salt is nicotine bitartrate dihydrate.

5. The product according to claim 1, wherein said pH adjusting agent is selected from the group consisting of carbonates including monocarbonate, bicarbonate and sesquicarbonate, acetates, glycinates, gluconates, borates, glycerophosphates or citrates of alkaline metals or ammonium, phosphate systems including monohydrogenphosphate, dihydrogenphosphate and trihydrogenphosphate, metal hydroxides such as sodium hydroxide and potassium hydroxide, and mixtures thereof.

6. The product according to claim 5, wherein said pH adjusting agent is sodium bicarbonate or sodium carbonate, and mixtures thereof.

7. The product according to claim 5, wherein said pH adjusting agent is encapsulated or embedded.

8. The product according to claim 7, wherein said pH adjusting agent is encapsulated or embedded with a polymer which physically separates the pH adjusting agent from the nicotine salt.

9. The product according to claim 1, wherein said filler is selected from the group consisting of polysaccharides, polyols, sugars, natural fibres, microcrystalline cellulose, cellulose and cellulose derivatives, and mixtures thereof.

10. The product according to claim 1, wherein said product comprises at least one filler which is a sweetener or a flavoring agent.

11. The product according to claim 10 wherein said sweetener is selected from the group consisting of mono- di- tri- and polysaccharides, polyols such as mannitol and maltitol, natural and synthetic sweeteners such as sucrose, glucose, dextrose, maltose, fructose, saccharin, aspartame, acesulfame, sucralose, saccharin and cyclamates, and mixtures thereof.

12. The product according to claim 10 wherein said flavoring agent is selected from the group consisting of bergamot, eucalyptus, orange, mandarin, citrus, lemon, peppermint, mint, menthol, liquorice, wintergreen, tobacco, coffee, vanilla, lime, apple, peach, and mixtures thereof.

13. The product according to claim 1, wherein said pouch is manufactured from material selected from the group consisting of pharmaceutically acceptable membrane materials.

14. The product according to claim 1, wherein said product comprises nicotine in an amount of from 0.1 to 10 mg per unit dose calculated as nicotine base.

15. The product according to claim 14, wherein said product comprises nicotine in an amount of 0.5, 1.0, 1.5, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 7.0, 8.0 or 9.0 mg per unit dose calculated as nicotine base.

16. The product according to claim 1, wherein said product comprises from 50 mg to 1000 mg of said powder.

17. The product according to claim 16, wherein said product comprises 100, 150, 200, 250, 300, 350, 400, 450, 500, 550, 600, 650, 700, 750, 800, 850, 900 or 950 mg of said powder.

21. The product according to claim 1, wherein said powder is granulated.

18. A method of making a product comprising the steps of

a) combining ingredients to form a powder, wherein the powder comprises at least one free nicotine salt wherein a substantial portion of the at least one free nicotine salt is not bound, at least one pH adjusting agent and at least one filler;

b) placing the powder in a water insoluble pouch thereby forming a product for oral delivery of nicotine, wherein said pouch is permeable for saliva and therein dissolved parts of the powder, wherein said product upon contact with purified water gives a pH of at least 6.

19. The method according to claim 18 wherein said method comprising the additional steps of encapsulating or embedding the pH adjusting agent.

20. The method according to claim 18 wherein said method comprising the additional step of granulating the powder.