Multi-Portion Intra-Oral Dosage Form With Organoleptic Properties

• US 20100247586A1
• Filed: 04/27/2009
• Published: 09/30/2010
• Est. Priority Date: 03/27/2009
• Status: Abandoned Application

• Current Assignee: McNeil AB (Johnson & Johnson)
• Original Assignee: McNeil AB (Johnson & Johnson)
• Inventors: Nicklasson, Fredrik, Hugerth, Andreas, Lindell, Katarina, Thyresson, Kristina
• Application Number:
  US12/430,238
• Publication Number:
  US 20100247586A1
• Time in Patent Office: Days
• US Class Current: 424/401
• CPC Class Codes: A23G 1/32 characterised by the composition containing organic or inorganic compounds
• CPC Class Codes: A23G 3/36 characterised by the composition containing organic or inorganic compounds
• CPC Class Codes: A23G 4/06 characterised by the composition containing organic or inorganic compounds
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/05 Phenols cannabinoids A61K31/658
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/19 Carboxylic acids, e.g. valproic acid salicylic acid A61K31/60
• CPC Class Codes: A61K 31/198 Alpha-amino acids, e.g. alanine or edetic acid [EDTA] betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00
• CPC Class Codes: A61K 31/4545 containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• CPC Class Codes: A61K 31/465 Nicotine; Derivatives thereof
• CPC Class Codes: A61K 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 31/55 having seven-membered rings, e.g. azelastine, pentylenetetrazole
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 8/02 characterised by special physical form
• CPC Class Codes: A61K 8/0216 Solid or semisolid forms
• 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 9/0058 Chewing gums non-medicinal aspects, preparing chewing gum A23G4/00; chewing gum for care of the teeth or oral cavity, e.g. with breath freshener A61Q11/00
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00
• CPC Class Codes: A61K 9/4808 characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084
• CPC Class Codes: A61P 25/34 : Tobacco-abuse
• CPC Class Codes: A61Q 11/00 : Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Abstract

A multi portion intra-oral dosage form has at least one pharmaceutically active agent or health promoting agent with at least one portion comprises a component for creating a noticeable organoleptic sensation. The sensory markers or signals are conceptual aids for a subject using the dosage form where the organoleptic sensation is such that it facilitates the subject to identify a portion and differentiate between different portions. Also contemplated are a dosage form, a method and a system for delivering active agents, such as nicotine and/or metabolites thereof, such as cotinine, nicotine N′-oxide, nomicotine, (S)-nicotine-N-β-glucuronide and mixtures, isomers, salts and complexes thereof as well as use and production of said dosage forms.

Claims

1. A multi portion intra-oral dosage form comprising at least one pharmaceutically active agent or health promoting agent, wherein there is a discernable difference in organoleptic sensation between at least two portions and said discernable difference in organoleptic sensation facilitates differentiation between said at least two portions and each portion comprises at least one item selected from the group consisting of a pharmaceutically active agent, a pH-buffering component, a pH-regulating component, a barrier component, an adhesive component, a taste masking agent, a health promoting agent, a tooth whitening agent, a breath freshening agent, an oral health promoting agent, and an anti-caries agent.

2. The multi portion intra-oral dosage form according to claim 1, wherein said organoleptic sensations is selected from the group consisting of perception of flavor, cooling, burning, warming, heating, tingling, crunchiness, crumbliness, flakiness, fusing, mouth watering, a color component, size, shape, auditive effect, effervescence, visual effect, stickiness, fragrance, olfactory sensation, bubbling, foaming, viscosity, elasticity, rheology, hardness, softness, mouth feel, smoothness, roughness, embossing, engravings and difference in dissolution rate.

3. The multi portion intra-oral dosage form according to claim 1, wherein said organoleptic sensation comprises a change in flavor.

4. The multi portion intra-oral dosage form according to claim 1, wherein said organoleptic sensation is delivered from a portion as a signal to inform a subject using said dosage form that said at least one pharmaceutically active agent or health promoting agent present in said portion has started to be released there from.

5. The multi portion intra-oral dosage form according to claim 1, wherein said organoleptic sensation is provided from a portion as a signal to inform a subject using said dosage form that all of or a fraction of said pharmaceutically active agent or health promoting agent being present in said portion has been released there from.

6. The multi portion intra-oral dosage form according to claim 1, where said pharmaceutically active agent is selected from the group consisting of nicotine and a nicotine mimicking agent.

7. The multi portion intra-oral dosage form according to claim 1, wherein said at least two portions have different dissolution rates including at least one portion with a slower dissolution rate and at least one portion with a faster dissolution rate.

8. The multi portion intra-oral dosage form according to claim 7, where at least one portion disintegrates more rapidly than at least one other portion, and where each portion comprises at least one item selected from a component for treating tobacco dependence, a pharmaceutically active component, a nicotine mimicking component, a pH-buffering component, a pH-regulating component, a flavor, a barrier component, a color component, an adhesive component, a taste masking agent, a tooth whitening agent, a breath freshening agent, an oral health promoting agent, and an anti-caries agent.

9. The multi portion intra-oral dosage form according to claim 7, where the dissolution time for the portion with the slower dissolution rate is at least two times longer than the portion with the faster dissolution rate.

10. The multi portion intra-oral dosage form according to claim 9, wherein said dissolution time for the portion with the slower dissolution rate is 3-10 times longer than the dissolution rate for the portion with a faster dissolution rate.

11. The multi portion intra-oral dosage form according to 7, further comprising at least two rapidly dissolving portions and at least one slowly dissolving portion.

12. The multi portion intra-oral dosage form according to claim 11, wherein said at least two rapidly dissolving portions at least partly covers the at least one slowly dissolving portion.

13. The multi portion intra-oral dosage form according to claim 7, wherein said at least one slower dissolving portion covers at least 20% of the surface of said rapidly dissolving portion.

14. The multi portion intra-oral dosage form according to claim 1, further comprising a member selected from the group consisting of a buffer and a pH-adjusting agent, which upon administration to a subject transiently changes the pH of the saliva of the subject by 0.1-4 pH units.

15. The multi portion intra-oral dosage form according to claim 1 comprising a nicotine compound selected from the group consisting of a nicotine salt, the free base form of nicotine, a nicotine derivative, a nicotine cation exchanger, a nicotine inclusion complex, nicotine in any non-covalent binding, nicotine bound to zeolites, nicotine bound to cellulose.

16. The multi portion intra-oral dosage form according to claim 1, comprising a component for treating tobacco dependence selected from the group consisting of a nicotine pro-drug, cotinine, nicotine N′

-oxide, nornicotine, (S)-nicotine-N-β

-glucuronide, isomers thereof and mixture thereof.

17. The multi portion intra-oral dosage form according to claim 15, wherein the nicotine compound is present in an amount of 0.05-12 mg calculated as the free base form of nicotine per unit dose.

18. The multi portion intra-oral dosage form according to claim 7, wherein said at least one portion with a faster dissolution rate comprises a compressible excipient selected from isomalt, dextrose monohydrate, maltodextrin, lactose monohydrate, dextrin, mannitol, lactitol, sorbitol, xylitol, erythritol, sucrose, and lactose, and mixtures or derivatives thereof.

19. The multi portion intra-oral dosage form according to claim 18, wherein said at least one portion with a faster dissolution rate comprises from about 5 to about 90 percent by weight of one or more of the compressible excipients based on the total weight of said at least one portion with a faster dissolution rate.

20. A multi portion intra-oral dosage form according to claim 1, being a lozenge, a tablet, an oral film, a chewing gum, a sublingual tablet, a troche, a lolly pop, a hard boiled candy, a chocolate lens, a micro bead, a wine gum, a semi solid, or a combination thereof.