Oral delivery vehicle containing nicotine

Patent metadata

Field	Value
Publication number	US-10543205-B2
Application number	US-201615356175-A
Country	US
Kind code	B2
Filing date	Nov 18, 2016
Priority date	Nov 18, 2016
Publication date	Jan 28, 2020
Grant date	Jan 28, 2020

Abstract

The invention relates an oral delivery vehicle tablet containing nicotine, the delivery vehicle tablet being formed by compression of a plurality of particles, the oral delivery vehicle tablet comprising nicotine, the oral delivery vehicle tablet comprising sugar alcohol(s) in an amount of 40 to 100% by weight of the delivery vehicle tablet, wherein at least 10% by weight of the delivery vehicle tablet comprises a plurality of particles consisting of erythritol and wherein the delivery vehicle tablet comprises a plurality of further sugar alcohol particles in an amount of at least 10% by weight of the delivery vehicle tablet, wherein said further sugar alcohol particles comprise at least one sugar alcohol and wherein said further sugar alcohols particles have a composition which is different from said particles consisting of erythritol.

First claim

What is claimed is:

1. An oral delivery vehicle tablet, the oral delivery vehicle tablet having been formed by direct compression of a plurality of particles, and the oral delivery vehicle tablet comprising:
nicotine;
a plurality of non-directly compressible (non-DC) grade erythritol particles in an amount of at least 10% by weight of the oral delivery vehicle tablet; and
a plurality of further sugar alcohol particles in an amount of at least 10% by weight of the oral delivery vehicle tablet,
wherein a weight ratio between said plurality of non-DC grade erythritol particles and said plurality of further sugar alcohol particles is between 0.3 and 0.7,
wherein said further sugar alcohol particles are different from said non-DC grade erythritol particles, and
wherein said non-DC grade erythritol particles are particles that have not been subject to granulation or agglomeration steps prior to said direct compression.

2. The oral delivery vehicle tablet according to claim 1 , wherein said non-DC grade erythritol particles are defined as non-DC grade particles with reference to the Compressibility Index according to European Pharmacopeia 6.0, and wherein said non-DC grade erythritol particles have a compressibility index which is greater than 21%.

3. The oral delivery vehicle tablet according to claim 1 , wherein said non-DC grade erythritol particles are defined as non-DC grade with reference to the Compressibility Index according to European Pharmacopeia 6.0, and wherein said non-DC grade erythritol particles have a compressibility index which is greater than 21% and less than 37%.

4. The oral delivery vehicle tablet according to claim 1 , wherein said further sugar alcohol particles are directly compressible (DC) grade particles.

5. The oral delivery vehicle tablet according to claim 1 , wherein said further sugar alcohol particles are defined as directly compressible (DC) grade particles with reference to the Compressibility Index according to European Pharmacopeia 6.0, and wherein said further sugar alcohol particles have a compressibility index which is less than 21%.

6. The oral delivery vehicle tablet according to claim 4 , wherein said further sugar alcohol particles comprise sugar alcohols selected from the group consisting of sorbitol, erythritol, xylitol, lactitol, maltitol, mannitol or isomalt or any combination thereof.

7. The oral delivery vehicle tablet according to claim 1 , wherein friability of the oral delivery vehicle tablet is less than 2%, and wherein friability is measured according to European Pharmacopoeia 9.1, test method 2.9.7. by using a pharmaceutical friability-tester PTF 10E from Pharma Test.

8. The oral delivery vehicle tablet according to claim 1 , wherein friability of the oral delivery vehicle tablet is greater than 0.2%, and wherein friability is measured according to European Pharmacopoeia 9.1, test method 2.9.7. by using a pharmaceutical friability-tester PTF 10E from Pharma Test.

9. The oral delivery vehicle tablet according to claim 1 , wherein said non-DC grade erythritol particles have an average particle size which is larger than the average particle size of said further sugar alcohol particles, and wherein the average particle size is determined according to the European Pharmacopoeia 9.1 when using test method 2.9.38 particle size distribution estimation by analytical sieving.

10. The oral delivery vehicle tablet according to claim 1 , wherein a particle size of at least 80% of said non-DC grade erythritol particles is greater than 200 micron, and wherein the particle size is determined according to European Pharmacopoeia 9.1 when using test method 2.9.38 particle size distribution estimation by analytical sieving.

11. The oral delivery vehicle tablet according to claim 1 , wherein a particle size of less than 20% of said non-DC grade erythritol particles is smaller than 250 micron, and wherein the particle size is determined according to European Pharmacopoeia 9.1 when using test method 2.9.38 particle size distribution estimation by analytical sieving.

12. The oral delivery vehicle tablet according to claim 1 , wherein the resistance to crunching of the oral delivery vehicle tablet is greater than 60N, and wherein the resistance to crunching is determined according to European Pharmacopoeia 9.1, test method 2.9.8. by using a pharmaceutical resistance to crunching tester model Pharma Test type PTB 311.

13. The oral delivery vehicle tablet according to claim 1 , wherein the oral delivery vehicle tablet comprises at least one module, wherein the module comprises more than 10% by weight of compressed non-DC grade erythritol particles, wherein the resistance to crunching of the module is greater than 60N, and wherein the resistance to crunching is determined according to the European Pharmacopoeia 9.1, test method 2.9.8. by using a pharmaceutical resistance to crunching tester model Pharma Test type PTB 311.

14. The oral delivery vehicle tablet according to claim 13 , wherein the oral delivery vehicle tablet comprises, in addition to the at least one module, one or more additional modules, wherein each of the at least one module and the one or more additional modules are comprised of compressed particles.

15. The oral delivery vehicle tablet according to claim 14 , wherein the oral delivery vehicle tablet comprises at least two modules, wherein the resistance to crunching of a first module comprising non-DC grade erythritol particles is less than 150N, wherein the resistance to crunching of a second module is more than 100N and more than the resistance to crunching of the first module, wherein the second module comprises less non-DC grade erythritol particles with respect to weight than the first module, wherein the resistance to crunching of the oral delivery vehicle tablet is higher than the resistance to crunching of the second module when the second module is separated from the oral delivery vehicle tablet, and wherein the resistance to crunching is determined according to European Pharmacopoeia 9.1, test method 2.9.8. by using a pharmaceutical resistance to crunching tester model Pharma Test type PTB 311.

16. The oral delivery vehicle tablet according to claim 1 , further comprising 0-60 percent by weight of gum base.

17. The oral delivery vehicle tablet according to claim 1 , wherein the oral delivery vehicle tablet is free of gum base.

18. An oral delivery vehicle tablet, the oral delivery vehicle tablet having been formed by direct compression of a plurality of particles, and the oral delivery vehicle tablet comprising:
nicotine;
a plurality of non-directly compressible (non-DC) grade erythritol particles in an amount of at least 10% by weight of the oral delivery vehicle tablet; and
a plurality of further sugar alcohol particles in an amount of at least 10% by weight of the oral delivery vehicle tablet,
wherein a weight ratio between said plurality of non-DC grade erythritol particles and said plurality of further sugar alcohol particles is between 0.3 and 0.7,
wherein said further sugar alcohol particles are different from said non-DC grade erythritol particles,
wherein the total amount of sugar alcohols of the oral delivery vehicle tablet is at least 40% by weight of the oral delivery vehicle tablet, and
wherein said non-DC grade erythritol particles are particles that have not been subject to granulation or agglomeration steps with said further sugar alcohol particles, other sugar alcohols, or binders prior to said direct compression.

19. An oral delivery vehicle tablet, the oral delivery v

Assignees

• Wittorff Helle
• Bruun Heidi Ziegler
• Boesen Dorthe Schackinger
• Fertin Pharma As

Inventors

• Wittorff Helle
• Bruun Heidi Ziegler
• Boesen Dorthe Schackinger

Classifications

• A61K9/2086

  Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat (active cores with a complete drug-free outer coat A61K9/28) · CPC title

• A61K9/2018

  Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates · CPC title

• A61K31/465 Primary

  Nicotine; Derivatives thereof · CPC title

• A61K9/2095

  Tabletting processes · CPC title