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EP-4739285-A1 - DISSOLVABLE ORALLY ADHERING TABLET

EP4739285A1EP 4739285 A1EP4739285 A1EP 4739285A1EP-4739285-A1

Abstract

A dissolvable orally adhering tablet for sustained release is disclosed, the tablet comprising an active ingredient, wherein the tablet is a multilayer tablet comprising a first layer and a second layer, the first layer being a mucoadhesive layer comprising a natural gum mucoadhesive and the second layer comprising at least one sugar alcohol.

Inventors

  • WITTORFF, HELLE

Assignees

  • Fertin Pharma A/S

Dates

Publication Date
20260513
Application Date
20240708

Claims (20)

  1. 1. A dissolvable orally adhering tablet for sustained release, the tablet comprising an active ingredient, wherein the tablet is a multilayer tablet comprising a first layer and a second layer, the first layer being a mucoadhesive layer comprising a natural gum mucoadhesive and the second layer comprising at least one sugar alcohol.
  2. 2. The tablet according to claim 1, wherein the tablet adheres to the gum.
  3. 3. The tablet according to claim 1 or 2, wherein the tablet is a compressed tablet.
  4. 4. The tablet according to any of claims 1-3, wherein the tablet is composed of a plurality of compressed particles.
  5. 5. The tablet according to any of claims 1-4, wherein the first and the second layers are fused by compression.
  6. 6. The tablet according to any of claims 1-5, wherein the active ingredient comprises a buccally absorbable active ingredient
  7. 7. The tablet according to any of claims 1-6, wherein the active ingredient comprises an active pharmaceutical ingredient.
  8. 8. The tablet according to any of claims 1-7, wherein the active ingredient is selected from the group consisting of caffeine, melatonin, nicotine, and combinations of nicotine and caffeine.
  9. 9. The tablet according to any of claims 1-8, wherein the active ingredient is selected from the group consisting of caffeine, nicotine, and any combination thereof.
  10. 10. The tablet according to any of claims 1-9, wherein the active ingredient comprises melatonin.
  11. 11. The tablet according to any of claims 1-10, wherein the active ingredient comprises caffeine.
  12. 12. The tablet according to any of claims 1-11, wherein the active ingredient comprises nicotine.
  13. 13. The tablet according to any of claims 1-12, wherein the active ingredient comprises paraxanthine.
  14. 14. The tablet according to any of claims 1-13, wherein the tablet comprises paraxanthine in an amount of at least 10 mg, such as at least 20 mg.
  15. 15. The tablet according to any of claims 1-14, wherein the active ingredient comprises one or more probiotics.
  16. 16. The tablet according to any of claims 1-15, wherein the tablet comprises said one or more probiotics in an amount of at least 2 mg, such as at least 5 mg.
  17. 17. The tablet according to any of claims 1-16, wherein the tablet comprises caffeine in an amount of at least 10 mg, such as at least 20 mg.
  18. 18. The tablet according to any of claims 1-17, wherein the tablet comprises melatonin in an amount of at least 0.5 mg, such as at least 1 mg.
  19. 19. The tablet according to any of claims 1-18, wherein the tablet comprises nicotine in an amount of at least 0.5 mg, such as at least 1 mg.
  20. 20. The tablet according to any of claims 1-19, wherein the tablet has a weight ratio between content of the active ingredient and the content of the sugar alcohol of the tablet, wherein said weight ratio is at least 1 :600, such as at least 1 :400, such as at least 1 :200, such as at least 1 : 100.

Description

DISSOLVABLE ORALLY ADHERING TABLET FIELD OF INVENTION The invention relates to a dissolvable orally adhering tablet for sustained release according to the claims. BACKGROUND Several tablets are known to provide sustained release of some active ingredients. However, such tablets may be inconvenient for the user due to the slow dissolution of the tablets. Additionally, slow dissolution may result in an unintended swallowing of active ingredients, which further would result in an unpleasant experience for the user. Besides being an unpleasant experience, unintended swallowing would prohibit buccal absorption of active ingredients. Thus, a lowered efficacy and undesired side effects such as off-taste, throat irritation and/or hiccups may be expected. At the same time, due to the slow dissolution, providing tablets with a good mouthfeel is desirable, as users may otherwise discourage from use, or may eject the tablets prematurely due to discomfort. It is an object of the present invention to overcome the disadvantages of the prior art. SUMMARY The invention relates to a dissolvable orally adhering tablet for sustained release, the tablet comprising an active ingredient, wherein the tablet is a multilayer tablet comprising a first layer and a second layer, the first layer being a mucoadhesive layer comprising a natural gum mucoadhesive and the second layer comprising at least one sugar alcohol. An advantage of the invention may be that a desirable sustained delivery of active ingredients may be obtained. Specifically, by including a natural gum mucoadhesive selectively in the first layer, the tablet may after insertion between the gum and the lip adhere to the mucosal surface of the gum or to the lip, whereby the tablet is immobilized. This immobilization facilitates sustained release, as the tablet is inserted into a low exposure region of the oral cavity with low saliva flux and minimum interaction with the tongue. Thereby the disintegration time of the tablet may be significantly prolonged. On the other hand, the adhesion either to the gum or to the lip facilitates a significant improvement in the mouthfeel for the user, as simultaneous adhesion to the gum and the lip is perceived as unpleasant, e.g. since it prevents the gum and the lip to move freely relative to each other. Based on this insight, the tablet comprises both a first layer being a mucoadhesive layer and a second layer comprising sugar alcohol. Furthermore, by using natural gum mucoadhesive, the release profile of the active ingredient may be altered as desired. A further advantage of the present invention may be a desirable mouthfeel and release, facilitated by the use of natural gum mucoadhesives. A further advantage of the invention may be that the natural gum mucoadhesive upon swallowing may offer health benefits, e.g. in the bowel system due to its prebiotic properties. It is noted that the intended use of the tablet is insertion between the gum and the lip, with the first layer facing the gum or the lip, preferably the gum, whereby the first layer adheres to the gum or lip to facilitate immobilization of the tablet. Thus, the layered structure of the tablet with the mucoadhesive layer on one side facilitates this advantageous use. In the present context, the term “gum” refers to the gingiva, i.e. the mucosal tissue that covers the tooth. It is noted that the term ”gum” is of course not to be confused with the term ’’natural gum mucoadhesive”. According to an advantageous embodiment of the invention, the tablet adheres to the gum. In a preferred embodiment according to the invention the tablet adheres to the gum. In this embodiment the first layer adheres to the gum. It is noted within the present context that the term “dissolvable orally adhering tablet” refers to a tablet for oral administration, which is able to adhere to a mucosal surface of the oral cavity, particularly the gum or lip, preferably the gum, by means of the mucoadhesive layer. The tablet is overall dissolvable, particularly in saliva or water, in the sense that the main constituents are dissolvable in water. For the avoidance of doubt it is noted that the tablet according to the present invention is a non-chewing gum tablet, i.e. the tablet according to the present invention does not comprise gum base, and the tablet according to the present invention is not a chewing gum. As used herein, the term “dissolve” is the process where a solid substance enters a solvent (oral saliva) to yield a solution. Unless otherwise stated, dissolving implies a full dissolving of the compound in question. It is noted within the present context that the term “sustained release” refers to release of the active ingredient over a prolonged period of time, in particular over period of at least 30 minutes, such as at least 45 minutes, such as at least 1 hour. It is noted that sustained release may sometimes also be referred to as controlled release or extended release. According to an embodime