Granted Patent B2

US 12,208,160 · App. 17/390,331 · Granted Jan 28, 2025

Inventors: Rosaleen Mclaughlin (Swindon, GB); Simon Andrew Martyn Howes (Swindon, GB); Craig Wheadon (Swindon, GB); Jonathon Whitehouse (Herne Bay, GB); Adam Parker (Swindon, GB); Michael John Hutchinson (Lisburn, GB)

Assignee: Catalent U.K. Swindon Zydis Limited

A61K9/0056A61K9/2813A61K9/2826A61K9/2873A61K9/2893

Abstract

Claims (39)

1. A pharmaceutical composition comprising:

60-85% w/w API;

10-30% w/w a water insoluble material surrounding the API to form a first coating on the API;

0.5-3% w/w silica surrounding the first coating of the API to form a second coating on the first coating of the API, wherein the silica produces a slower dissolution profile for the API as compared to API without silica;

3-7% w/w matrix former; and

2-6% w/w structure former.

2. The pharmaceutical composition of claim 1 , wherein the water insoluble material comprises a wax.

3. The pharmaceutical composition of claim 2 , wherein the wax comprises carnauba wax.

4. The pharmaceutical composition of claim 1 , wherein the silica comprises hydrophobic silica.

5. The pharmaceutical composition of claim 1 , wherein the matrix former comprises gelatin.

6. The pharmaceutical composition of claim 1 , wherein the structure former comprises mannitol.

7. The pharmaceutical composition of claim 1 , further comprising a viscosity modifier.

8. The pharmaceutical composition of claim 7 , wherein the pharmaceutical composition comprises 0.1-1% w/w viscosity modifier.

9. The pharmaceutical composition of claim 7 , wherein the viscosity modifier comprises xanthan gum.

10. The pharmaceutical composition of claim 1 , further comprising a sweetener.

11. The pharmaceutical composition of claim 10 , wherein the pharmaceutical composition comprises 0.1-2% w/w sweetener.

12. The pharmaceutical composition of claim 10 , wherein the sweetener is sucralose.

13. The pharmaceutical composition of claim 1 , further comprising a flavoring agent and/or an anti-aeration agent.

14. The pharmaceutical composition of claim 13 , wherein the pharmaceutical composition comprises 0.5-3% w/w flavoring agent and/or anti-aeration agent.

15. The pharmaceutical composition of claim 13 , wherein the flavoring agent and/or anti-aeration agent comprises terpene and/or terpinol.

16. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition has a mid volume 60-minute dissolution test result less than or equal to 70% after 15 minutes.

17. A method of preparing coated API comprising:

sieving raw API;

mixing sieved raw API and a water insoluble material in a vessel;

applying mechanical energy to the vessel and heating the vessel to a temperature greater than or equal to 50° C.; and

adding silica to the vessel while continuing to apply the mechanical energy and maintaining the temperature of the vessel to form coated API comprising at least one coating comprising water insoluble material and silica, wherein the coated API comprises 40-85% w/w API, 10-60% w/w water insoluble material surrounding the API to form a first coating on the API, and 0.5-5% w/w silica surrounding the first coating of the API to form a second coating on the first coating of the API, wherein the silica produces a slower dissolution profile for the API as compared to API without silica.

18. The method of claim 17 , wherein sieving the raw API comprises sieving the raw API to an average particle size of 75-250 microns.

19. The method of claim 17 , further comprising sieving the coated API.

20. The method of claim 19 , wherein sieving the coated API comprises sieving the coated API to an average particle size of 75-250 microns.

21. The method of claim 17 , wherein the ratio of the at least one coating to the API of the API comprising at least one coating is 15-40:60-85.

22. The method of claim 17 , wherein the coated API has a low volume 60 minute dissolution test result less than or equal to 70% after 15 minutes.

23. A method of preparing a pharmaceutical composition comprising:

forming a pharmaceutical suspension comprising:

30-50% w/w API comprising at least one coating, wherein the at least one coating comprises a water insoluble material and silica;

1-5% w/w a matrix former;

1-3% w/w a structure former; and

a solvent;

dosing the pharmaceutical suspension into a mold; and

freeze drying the dosed pharmaceutical suspension in the mold to form the pharmaceutical composition, wherein the pharmaceutical composition comprises 60-85% w/w API, 10-30% w/w water insoluble material surrounding the API to form a first coating on the API, 0.5-3% w/w silica surrounding the first coating of the API to form a second coating on the first coating of the API, wherein the silica produces a slower dissolution profile for the API as compared to API without silica.

Assignments (1)

Continuity (2)

References Cited (188)