KR-20260065796-A - Dissolvable oral adhesive tablets

Abstract

A soluble oral adhesive tablet for sustained release is disclosed, the tablet comprises an active ingredient, the tablet is a multilayer tablet comprising a first layer and a second layer, the first layer is a mucosal adhesive layer comprising a natural gum mucosal adhesive, and the second layer comprises at least one sugar alcohol.

Inventors

• 비토르프, 헬레

Assignees

• 페르틴 파르마 에이/에스

Dates

Publication Date

20260511

Application Date

20240708

Priority Date

20231107

Claims (20)

1. As a soluble oral adhesive tablet for sustained release, The tablet contains an active ingredient, The tablet is a multilayer tablet comprising a first layer and a second layer, and A tablet, wherein the first layer is a mucosal adhesive layer comprising a natural gum mucosal adhesive, and the second layer comprises at least one sugar alcohol.
2. In paragraph 1, the tablet is a tablet that adheres to the gums.
3. In paragraph 1 or 2, the tablet is a compressed tablet.
4. In any one of paragraphs 1 to 3, the tablet is composed of a plurality of compressed particles.
5. A tablet according to any one of paragraphs 1 to 4, wherein the first and second layers are fused by compression.
6. A tablet according to any one of claims 1 to 5, wherein the active ingredient comprises an active ingredient that can be absorbed via the buccal side.
7. A tablet according to any one of paragraphs 1 to 6, wherein the active ingredient comprises an effective pharmaceutical ingredient.
8. A tablet according to any one of claims 1 to 7, wherein the active ingredient is selected from the group consisting of caffeine, melatonin, nicotine, and combinations of nicotine and caffeine.
9. A tablet according to any one of claims 1 to 8, wherein the active ingredient is selected from the group consisting of caffeine, nicotine, and any combination thereof.
10. A tablet according to any one of claims 1 to 9, wherein the active ingredient comprises melatonin.
11. A tablet according to any one of claims 1 to 10, wherein the active ingredient comprises caffeine.
12. A tablet according to any one of claims 1 to 11, wherein the active ingredient comprises nicotine.
13. A tablet according to any one of claims 1 to 12, wherein the active ingredient comprises paraxanthin.
14. A tablet according to any one of claims 1 to 13, wherein the tablet contains paraxanthine in an amount of at least 10 mg, e.g., at least 20 mg.
15. A tablet according to any one of claims 1 to 14, wherein the active ingredient comprises one or more probiotics.
16. A tablet according to any one of claims 1 to 15, wherein the tablet comprises one or more of the above probiotics in an amount of at least 2 mg, e.g., at least 5 mg.
17. A tablet according to any one of claims 1 to 16, wherein the tablet contains caffeine in an amount of at least 10 mg, e.g., at least 20 mg.
18. A tablet according to any one of claims 1 to 17, wherein the tablet contains melatonin in an amount of at least 0.5 mg, e.g., at least 1 mg.
19. A tablet according to any one of claims 1 to 18, wherein the tablet contains nicotine in an amount of at least 0.5 mg, e.g., at least 1 mg.
20. A tablet according to any one of claims 1 to 19, wherein the tablet has a weight ratio between the content of the active ingredient of the tablet and the content of the sugar alcohol, said weight ratio being at least 1:600, e.g., at least 1:400, e.g., at least 1:200, e.g., at least 1:100.

Description

Dissolvable oral adhesive tablets The present invention relates to a dissolvable orally adhering tablet for sustained release according to the claims. Several tablets are known to provide sustained release of certain active ingredients. However, these tablets can be inconvenient for users due to their slow dissolution. Additionally, slow dissolution leads to unintended swallowing of the active ingredient, which can result in an further unpleasant experience for the user. Unintended swallowing is not only an unpleasant experience but can also interfere with the buccal absorption of the active ingredient. Consequently, efficacy is reduced, and unwanted side effects such as taste abnormalities, throat irritation, and/or hiccups may occur. At the same time, it is desirable to provide a tablet that feels good in the mouth due to slow dissolution, because otherwise, users may not use the tablet or may spit it out prematurely due to discomfort. The objective of the present invention is to overcome the disadvantages of the prior art. The present invention relates to a soluble oral adhesive tablet for sustained release, wherein The tablet contains an active ingredient, The tablet is a multilayer tablet comprising a first layer and a second layer, and The first layer is a mucosal adhesive layer comprising a natural gum mucosal adhesive, and the second layer comprises at least one sugar alcohol. An advantage of the present invention may be that desirable sustained delivery of the active ingredient can be obtained. Specifically, by optionally including a natural gum mucosal adhesive in the first layer, the tablet can be fixed by adhering to the mucosal surface of the gum or the lip after being inserted between the gum and the lip. This fixation facilitates sustained release by inserting the tablet into a low-exposure area of the oral cavity where salivary flow is low and interaction with the tongue is minimized. Thus, the disintegration time of the tablet can be significantly extended. On the other hand, adhesion to either the gum or the lip significantly improves the user's oral sensation, as simultaneous adhesion to both the gum and the lip is perceived as unpleasant, for example, because it prevents the gum and the lip from moving freely relative to each other. Based on this insight, the tablet comprises both a first layer, which is a mucosal adhesive layer, and a second layer containing a sugar alcohol. Furthermore, by using natural gum adhesives, the release profile of the active ingredient can be changed as desired. An additional advantage of the present invention may be that the use of a natural gum mucosal adhesive can facilitate a desirable oral sensation and release. An additional advantage of the present invention is that the natural gum mucosal adhesive can provide health benefits, for example in the intestinal system, due to its prebiotic properties during swallowing. It is noted that the intended use of the tablet is to insert it between the gum and the lip with the first layer facing the gum or lip, preferably the gum, so that the first layer adheres to the gum or lip, thereby facilitating the fixation of the tablet. Accordingly, the layered structure of the tablet having a mucosal adhesive layer on one side facilitates this advantageous use. In this context, the term "gum" refers to the gingiva, that is, the mucosal tissue covering the teeth. The term "gum" should not be confused with the term "natural gum mucosal adhesive." According to an advantageous embodiment of the present invention, the tablet adheres to the gums. In a preferred embodiment according to the present invention, the tablet adheres to the gums. In this embodiment, the first layer adheres to the gums. It is noted that in this context, the term “soluble oral adhesive tablet” refers to a tablet for oral administration that can be adhered to the mucosal surface of the oral cavity, particularly the gums or lips, preferably the gums, by means of a mucosal adhesive layer. The tablet is soluble in saliva or water in general, in that the main component is soluble in water. To avoid any doubt, it is noted that the tablet according to the present invention is a tablet that is not chewing gum, that is, the tablet according to the present invention does not contain a gum base, and the tablet according to the present invention is not chewing gum. As used herein, the term "dissolve" is the process by which a solid substance enters a solvent (oral saliva) to form a solution. Unless otherwise specified, dissolution means the complete dissolution of the compound in question. It is noted that in this context, the term “sustained release” refers to the release of an active ingredient over a long period, particularly over at least 30 minutes, e.g., at least 45 minutes, e.g., at least 1 hour. It is noted that sustained release may also sometimes be referred to as controlled release or sustained release. According to one embodiment of the present invention,