IP Library Granted Patent US 11,266,598
Granted Patent B2
US 11,266,598 · App. 17/236,295 · Granted Mar 8, 2022

Orally administered corticosteroid compositions

Inventors: Stephen Perrett (Princeton, NJ); Fredric Jay Cohen (Washington Crossing, PA); Gopi M. Venkatesh (Vandalia, OH)
Assignee: ELLODI PHARMACEUTICALS, L.P.
A61K9/0065A61K9/006A61K9/0053A61K9/0056A61K9/08A61K31/56A61K31/569A61K31/58A61K45/06A61K47/38A61K9/06
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Quick Facts
Patent No.
US 11,266,598
App. No.
17/236,295
Granted
Mar 8, 2022
Kind
B2
Abstract

The present invention is directed to orally administered corticosteroid compositions. The present invention also provides a method for treating a condition associated with inflammation of the gastrointestinal tract in an individual. The method comprises administering to an individual in need thereof a pharmaceutical composition of the present invention.

Claims (38)

1. An orally disintegrating tablet comprising:

(i) about 1 mg to about 6 mg of fluticasone propionate; and

(ii) at least one disintegrant;

wherein upon administration a therapeutically effective amount of fluticasone propionate is deposited topically in the upper gastrointestinal tract, and

wherein the orally disintegrating tablet disintegrates within 60 seconds when tested using the USP <701>Disintegration Test.

2. The orally disintegrating tablet of claim 1 , comprising about 1 mg to about 2 mg of fluticasone propionate.

3. The orally disintegrating tablet of claim 1 , comprising about 3 mg of fluticasone propionate.

4. The orally disintegrating tablet of claim 1 , comprising a sugar alcohol and/or saccharide.

5. The orally disintegrating tablet of claim 1 , wherein the orally disintegrating tablet comprises drug particles and rapidly dispersing granules, wherein the drug particles comprise fluticasone propionate and at least one excipient, and the rapidly dispersing granules comprise the disintegrant and a sugar alcohol and/or saccharide.

6. The orally disintegrating tablet of claim 5 , wherein the rapidly dispersing granules have an average particle size of less than about 300 μm, and each of the disintegrant and sugar alcohol and/or saccharide have an average particle size of about 1-30 μm.

7. The orally disintegrating tablet of claim 5 , wherein the drug particles have an average particle size of about 100-400 μm.

8. The orally disintegrating tablet of claim 5 , the drug particles have an average particle size of about 100-400 μm, the rapidly dispersing granules have an average particle size of less than about 300 μm, and each of the disintegrant and sugar alcohol and/or saccharide have an average particle size of about 1-30 μm.

9. The orally disintegrating tablet of claim 5 , comprising about 1 mg to about 2 mg of fluticasone propionate.

10. The orally disintegrating tablet of claim 5 , comprising about 3 mg of fluticasone propionate.

11. The orally disintegrating tablet of claim 8 , comprising about 1 mg to about 2 mg of fluticasone propionate.

12. The orally disintegrating tablet of claim 8 , comprising about 3 mg of fluticasone propionate.

13. The orally disintegrating tablet of claim 1 , wherein the disintegrant is crospovidone, sodium starch glycolate, crosslinked carboxymethyl cellulose, low-substituted hydroxylpropylcellulose, mannitol, xylitol, sorbitol, maltol, maltitol, lactose, sucrose, maltose, or combinations thereof.

14. The orally disintegrating tablet of claim 13 , wherein the disintegrant is crospovidone.

15. The orally disintegrating tablet of claim 5 , wherein the sugar alcohol and/or saccharide is mannitol, sorbitol, xylitol, maltitol, arabitol, ribitol, dulcitol, iditol, isomalt, lactitol, erythritol, lactose, sucrose, maltose, or combinations thereof.

16. The orally disintegrating tablet of claim 15 , wherein the sugar alcohol is mannitol.

17. The orally disintegrating tablet of claim 5 , wherein the ratio of disintegrant to sugar alcohol, saccharide or mixture thereof in the rapidly dispersing microgranules ranges from about 90/10 to about 99/01.

18. The orally disintegrating tablet of claim 1 , wherein the orally disintegrating tablet disintegrates within 60 seconds when tested in simulated saliva fluid using the USP <701>Disintegration Test.

19. The orally disintegrating tablet of claim 1 , wherein the orally disintegrating tablet disintegrates within 30 seconds when tested using the USP <701>Disintegration Test.

20. An orally disintegrating tablet comprising:

(i) about 1 mg to about 3 mg of fluticasone propionate; and

(ii) rapidly dispersing granules comprising (a) at least one disintegrant and (b) at least one sugar alcohol, saccharide, or combination thereof;

wherein upon administration a therapeutically effective amount of the fluticasone propionate is deposited topically in the upper gastrointestinal tract, and

wherein the orally disintegrating tablet disintegrates within 60 seconds when tested using the USP <701>Disintegration Test.

21. The orally disintegrating tablet of claim 20 , wherein the orally disintegrating tablet comprises drug particles comprising the fluticasone propionate and at least one excipient.

22. The orally disintegrating tablet of claim 21 , wherein drug particles have an average particle size of about 100-400 μm, the rapidly dispersing granules have an average particle size of less than about 300 μm, the disintegrant and sugar alcohol and/or saccharide have an average particle size of about 1-30 μm, and the ratio of disintegrant to sugar alcohol and/or saccharide in the rapidly dispersing microgranules ranges from about 90/10 to about 99/01.

23. The orally disintegrating tablet of claim 22 , wherein the disintegrant is crospovidone.

24. The orally disintegrating tablet of claim 23 , wherein the sugar alcohol is mannitol.

25. The orally disintegrating tablet of claim 24 , comprising about 1 mg to about 2 mg of fluticasone propionate.

26. The orally disintegrating tablet of claim 24 , comprising about 3 mg of fluticasone propionate.

27. The orally disintegrating tablet of claim 26 , wherein the orally disintegrating tablet disintegrates within 30 seconds when tested using the USP <701>Disintegration Test.

28. A method for treating eosinophilic esophagitis comprising administering to a patient in need thereof the orally disintegrating tablet according to claim 1 .

29. The method of claim 28 , comprising about 1 mg to about 2 mg of fluticasone propionate.

30. The method of claim 28 , comprising about 3 mg of fluticasone propionate.

Assignments (6)
CHANGE OF NAME Recorded May 4, 2021
From: ADARE PHARMACEUTICALS US, L.P.
To: ELLODI PHARMACEUTICALS, L.P.
Reel/Frame 056126/0350 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 21, 2021
From: PERRETT, STEPHEN; COHEN, FREDRIC JAY; VENKATESH, GOPI
To: EURAND, INC.
Reel/Frame 055990/0685 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 21, 2021
From: ADARE PHARMACEUTICALS, INC.
To: ADARE DEVELOPMENT I, L.P.
Reel/Frame 055991/0241 →
CHANGE OF NAME Recorded Apr 21, 2021
From: EURAND, INC.
To: APTALIS PHARMATECH, INC.
Reel/Frame 055997/0201 →
CHANGE OF NAME Recorded Apr 21, 2021
From: APTALIS PHARMATECH, INC.
To: ADARE PHARMACEUTICALS, INC.
Reel/Frame 055997/0213 →
CHANGE OF NAME Recorded Apr 21, 2021
From: ADARE DEVELOPMENT I, L.P.
To: ADARE PHARMACEUTICALS US, L.P.
Reel/Frame 055997/0253 →
Continuity (7)
Continuation 16821464 · Mar 17, 2020
Continuation 15816154 · Nov 17, 2017
Continuation 15205390 · Jul 8, 2016
Continuation 14311732 · Jun 23, 2014
Division 12896005 · Oct 1, 2010
Provisional Application 61247642 · Oct 1, 2009
Related Publication 20210244660A1 · Aug 12, 2021
Cited By (4)
US 12,290,598 US 12,310,976 US 12,447,157 US 12,691,128