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CN-121985938-A - Nicotine disintegrating tablet

CN121985938ACN 121985938 ACN121985938 ACN 121985938ACN-121985938-A

Abstract

A nicotine disintegrating tablet for rapid relief of nicotine craving is disclosed, the tablet comprising nicotine, a disintegrant and at least one sugar alcohol, wherein the tablet comprises an amount of dissolution modifying wherein the amount of dissolution modifying is not more than 2% by weight of the tablet.

Inventors

  • CARLSON ROY F.
  • K.A. Nelson
  • B. P. Nielsen
  • H Martin n.

Assignees

  • 费尔廷制药公司

Dates

Publication Date
20260505
Application Date
20240912
Priority Date
20230912

Claims (20)

  1. 1. A nicotine disintegrating tablet for rapid relief of nicotine craving, the tablet comprising nicotine, a disintegrant and at least one sugar alcohol, wherein the tablet comprises an amount of dissolution modifying wherein the amount of dissolution modifying is not more than 2% by weight of the tablet.
  2. 2. The nicotine disintegrating tablet of claim 1, wherein the dissolution modifying agent is selected from the group consisting of xanthan gum, guar gum, konjac gum, tara gum, gellan gum, locust bean gum, acacia gum, pullulan, tragacanth gum, karaya gum, fenugreek gum, cassia gum, carrageenan, agar, alginic acid and monovalent salts thereof, and any combination thereof.
  3. 3. The nicotine disintegrating tablet of claim 1 or 2, wherein the dissolution modifying agent comprises at least one dissolution modifying agent selected from guar gum, xanthan gum, monovalent alginate salts, and any combination thereof.
  4. 4. A nicotine disintegrating tablet according to any one of claims 1-3, wherein the amount of dissolution modifying means is at most 1% by weight of the tablet, such as at most 0.5% by weight of the tablet, such as at most 0.25% by weight of the tablet, such as at most 0.1% by weight of the tablet.
  5. 5. The nicotine disintegrating tablet of any one of claims 1-4, wherein the disintegrating tablet has a disintegration time of 1 to 8 minutes, such as 1 to 7 minutes, such as 2 to 5 minutes, such as 3 to 5 minutes.
  6. 6. The nicotine disintegrating tablet of any one of claims 1-5, wherein the tablet has an in vitro disintegration time of 1 to 8 minutes, such as 1 to 7 minutes, such as 2 to 5 minutes, such as 3 to 5 minutes.
  7. 7. The nicotine disintegrating tablet of claim 6, wherein the in vitro disintegration time is measured according to the european pharmacopoeia 9.0 section 2.9.1 "disintegration of tablets and capsules".
  8. 8. The nicotine disintegrating tablet of any one of claims 1-7, wherein the tablet comprises at least one sugar alcohol in an amount of at least 40% by weight of the tablet, such as at least 50% by weight of the tablet, such as at least 60% by weight of the tablet, such as at least 70% by weight of the tablet, such as at least 80% by weight of the tablet.
  9. 9. The nicotine disintegrating tablet of any one of claims 1-8, wherein the at least one sugar alcohol comprises a sugar alcohol selected from the group consisting of xylitol, maltitol, mannitol, erythritol, isomalt, sorbitol, lactitol, and any combination thereof.
  10. 10. The nicotine disintegrating tablet of any one of claims 1-9, wherein the tablet comprises at least 0.5% of the tablet weight of the disintegrant, such as at least 1% of the tablet weight, such as at least 2% of the tablet weight, such as at least 3% of the tablet weight, such as at least 5% of the tablet weight.
  11. 11. The nicotine disintegrating tablet of any one of claims 1-10, wherein the disintegrant is selected from the group consisting of starch, pregelatinized starch, modified cellulose, ion exchange resin, calcium silicate, crosslinked cellulose, crosslinked polyvinylpyrrolidone, crosslinked starch, crosslinked alginate, and combinations thereof.
  12. 12. The nicotine disintegrating tablet of any one of claims 1-11, wherein the disintegrant comprises pregelatinized starch.
  13. 13. The nicotine disintegrating tablet of any one of claims 1-12, wherein the disintegrant consists of pregelatinized starch.
  14. 14. The nicotine disintegrating tablet of any one of claims 1-13, wherein the disintegrant comprises a super disintegrant.
  15. 15. The nicotine disintegrating tablet of claim 14, wherein the superdisintegrant comprises one or more crosslinked polymers.
  16. 16. Nicotine disintegrating tablet according to claim 14 or 15, wherein the tablet comprises at least 0.5% of the tablet weight of the superdisintegrant, such as at least 1% of the tablet weight, such as at least 2% of the tablet weight, such as at least 3% of the tablet weight, such as at least 5% of the tablet weight.
  17. 17. The nicotine disintegrating tablet of any one of claims 14-16, wherein the superdisintegrant is selected from the group consisting of crosslinked cellulose, crosslinked polyvinylpyrrolidone, crosslinked starch, crosslinked alginate, and any combination thereof.
  18. 18. The nicotine disintegrating tablet of any one of claims 1-17, wherein the disintegrant is a superdisintegrant selected from the group consisting of crosslinked cellulose, crosslinked polyvinylpyrrolidone (PVP), crosslinked starch, and any combination thereof.
  19. 19. The nicotine disintegrating tablet of any one of claims 1-18, wherein the disintegrant is a superdisintegrant selected from the group consisting of crosslinked polyvinylpyrrolidone, croscarmellose, sodium carboxymethyl starch, and any combination thereof.
  20. 20. The nicotine disintegrating tablet of any one of claims 1-19, wherein the tablet is a compressed tablet.

Description

Nicotine disintegrating tablet Technical Field The present invention relates to a nicotine disintegrating tablet (DISINTEGRATING NICOTINE TABLET) according to the claims. Background Nicotine sustained release tablets for releasing nicotine into the oral cavity of a user over a period of time are well known. The prior art has put much effort into simulating nicotine release and buccal feel when a user smokes, which means that the prior art has conducted intensive research into the release characteristics of nicotine tablets. However, a non-competing fact is that there is currently no means other than cigarettes (cigarette) to fully simulate smoking. Furthermore, the user's perception of nicotine tablets may be improved, for example, because the release of nicotine is accompanied by a bad stimulation of the throat, a side effect called nicotine burning sensation (nicotine burning) or simply burning sensation. PCT application WO 2019/110072 A1 by fertin pharmaceutical company (FERTIN PHARMA A/S) relates to an example of an orally disintegrating nicotine tablet which disintegrates within 60 seconds after oral administration. Summary of The Invention The present invention relates to a nicotine disintegrating tablet for rapid relief of nicotine craving (nicotine craving), said tablet comprising nicotine, a Disintegrant (DISINTEGRANT) and at least one sugar alcohol, wherein said tablet comprises an amount of dissolution modifying agent (dissolution modifier), wherein the amount of dissolution modifying agent is not more than 2% by weight of the tablet. An advantage of the present invention is that a desirable mouthfeel is obtained by adding a dissolution modifying agent. At the same time, another advantage of the present invention is that the tablet unexpectedly disintegrates rapidly in the oral cavity despite the addition of dissolution modifying agents, which allows for faster delivery of nicotine than intended, thereby rapidly alleviating nicotine cravings. Thus, the present invention advantageously improves both mouthfeel and promotes unexpectedly rapid relief of nicotine cravings. In the present context, the term "fast relief of nicotine cravings" may refer to relief of nicotine cravings for a period of time of no more than 8 minutes (e.g. no more than 7 minutes, such as no more than 5 minutes, such as no more than 3 minutes, such as no more than 2 minutes, such as no more than 1 minute). The desired mouthfeel obtained may be, for example, the smooth feel experienced by the tablet during disintegration in the oral cavity. In particular, tablets composed of powder ingredients generally tend to exhibit a rough surface texture, but the inventors have unexpectedly found that the surface texture of the tablets of the present invention is smooth and very attractive. Another advantage of the present invention is that the use of the tablet helps to quickly relieve nicotine cravings. Because the tablet is unexpectedly rapidly disintegrated in the presence of the dissolution modifying agent, the resulting release of nicotine not only helps to relieve nicotine cravings, but also brings a very pleasant mouthfeel. The inventors found that too high an amount of dissolution modifying agent resulted in slow dissolution of the tablet, which was disadvantageous in this study. On the other hand, the inventors have found that the addition of dissolution modifying agents advantageously provides improved mouthfeel, in particular improved smoothness. Thus, the inventors have found that when the content of dissolution modifying agent is less than 2% by weight of the tablet, a balance can be achieved between dissolution time and resulting craving relief of nicotine on the one hand and mouthfeel on the other hand. Notably, the nicotine disintegrating tablet to be protected contains a certain amount of dissolution modifying agent, and thus it excludes tablets that do not contain dissolution modifying agent. In this context, the term "dissolution modifying agent" refers to a substance that is commonly used in, for example, a lozenge (lozenges) to delay dissolution. Thus, dissolution modifying agents may also be referred to as dissolution retarders. Notably, in the context of the present invention, dissolution modifying agents do not include disintegrants (disintegrants are capable of promoting rapid disintegration of the drug). According to an advantageous embodiment of the invention, the dissolution modifying agent is selected from xanthan gum (xanthon gum), guar gum (guar gum), konjac gum (konjac gum), tara gum (tara gum), gellan gum (gellan gum), locust bean gum (locust bean gum), acacia gum (gum arabic), pullulan (pullulan), tragacanth gum (TRAGACANTH GUM), karaya gum (gum karaya), fenugreek gum (fenugreek gum), cassia gum (cassia gum), carrageenan (carageenan), agar, alginic acid (ALGINIC ACID) and monovalent salts thereof, and any combination thereof. It is noted that in this context, the terms "monovalent alginate salt", "monoval