IP Library Granted Patent US 10,369,225
Granted Patent B2
US 10,369,225 · App. 16/006,692 · Granted Aug 6, 2019

Pharmaceutical compositions comprising meloxicam

Inventor: Herriot Tabuteau (New York, NY)
Assignee: AXSOME THERAPEUTICS, INC.
A61K47/02A61K9/0053A61K9/2009A61K31/4439A61K31/5415A61K45/06A61K47/40A61K47/6951C08B37/0012C08B37/0015
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Quick Facts
Patent No.
US 10,369,225
App. No.
16/006,692
Granted
Aug 6, 2019
Kind
B2
Abstract

Disclosed herein are compositions comprising an NSAID such as meloxicam in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability, solubility, or pharmacokinetics of the NSAID for the treatment of conditions such as pain.

Claims (25)

1. A method of improving the pharmacokinetics of meloxicam comprising orally administering a solid dosage form comprising meloxicam and 400 mg to 800 mg of a bicarbonate to a human being suffering from a condition known to be treatable by meloxicam, wherein the meloxicam dissolves more rapidly from the solid dosage form as compared with a reference solid dosage form that: a) contains the same amount of meloxicam, and b) does not contain a bicarbonate, wherein the T max of meloxicam in the human being is less than 1 hour.

2. The method of claim 1 , wherein the bicarbonate is sodium bicarbonate.

3. The method of claim 1 , wherein the bicarbonate is potassium bicarbonate.

4. The method of claim 1 , wherein the solid dosage form comprises 500 mg of sodium bicarbonate.

5. The method of claim 1 , wherein the solid dosage form further comprises an acid inhibitor.

6. The method of claim 5 , wherein the acid inhibitor is esomeprazole.

7. The method of claim 6 , wherein about 30 mg to about 50 mg of esomeprazole is present in the solid dosage form.

8. The method of claim 6 , wherein the solid dosage form contains about 40 mg of esomeprazole.

9. The method of claim 1 , wherein the solid dosage form comprises about 10 mg to about 20 mg of meloxicam.

10. The method of claim 1 , wherein the solid dosage form contains about 15 mg of meloxicam.

11. The method of claim 1 , wherein the solid dosage form further comprises one or more pharmaceutically acceptable excipients.

12. The method of claim 1 , wherein the solid dosage form is in a tablet form or a capsule form.

13. The method of claim 1 , wherein the solid dosage form is administered under fasting conditions.

14. The method of claim 1 , wherein the solid dosage form is administered once daily.

15. The method of claim 14 , wherein the solid dosage form is administered for at least 6 days.

16. The method of claim 1 , wherein the first time the solid dosage form is orally administered, the human being has a T max of meloxicam that is at least 5-fold shorter than the T max of meloxicam that would result from administering a reference dosage form that: 1) contains the same amount of meloxicam, and 2) does not contain a bicarbonate.

17. The method of claim 1 , wherein the first time the solid dosage form is orally administered, the human being has a T max of meloxicam that is at least 1.5-fold shorter than the T max of meloxicam that would result from administering a reference dosage form that: 1) contains the same amount of meloxicam, and 2) does not contain a bicarbonate.

18. The method of claim 1 , wherein administering the solid dosage form results in increased bioavailability of meloxicam as compared to the oral bioavailability of meloxicam that would result from administering a reference dosage form that: 1) contains the same amount of meloxicam; and 2) does not contain a bicarbonate, wherein the first time the solid dosage form is orally administered, the human being has an AUC 0-24 of meloxicam that is at least about 10 μg·hr/mL.

19. The method of claim 1 , wherein administering the solid dosage form results in an AUC 0-6 of meloxicam that is at least about 6 μg·hr/mL in the human being.

20. The method of claim 1 , wherein the solid dosage form is administered to the human being to treat pain.

21. The method of claim 1 , wherein the solid dosage form is administered to the human being to treat inflammatory pain.

22. The method of claim 1 , wherein the solid dosage form is administered to the human being to treat osteoarthritis.

23. The method of claim 1 , wherein the solid dosage form is administered to the human being to treat rheumatoid arthritis.

24. The method of claim 1 , wherein the solid dosage form is administered to the human being to treat juvenile rheumatoid arthritis.

25. The method of claim 1 , wherein the solid dosage form is administered to the human being to treat migraine.

Assignments (4)
RELEASE OF SECURITY INTEREST Recorded May 22, 2025
From: HERCULES CAPITAL, INC.
To: AXSOME THERAPEUTICS, INC.
Reel/Frame 071337/0004 →
SECURITY INTEREST Recorded May 9, 2025
From: AXSOME THERAPEUTICS, INC.; AXSOME MALTA LTD.
To: WILMINGTON TRUST, NATIONAL ASSOCIATION
Reel/Frame 071247/0836 →
INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Sep 25, 2020
From: AXSOME THERAPEUTICS, INC.
To: HERCULES CAPITAL, INC., AS AGENT
Reel/Frame 053941/0491 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 10, 2018
From: TABUTEAU, HERRIOT
To: AXSOME THERAPEUTICS, INC.
Reel/Frame 046309/0160 →
Continuity (9)
Continuation 15902770 · Feb 22, 2018
Continuation 15797955 · Oct 30, 2017
Continuation In Part 15132130 · Apr 18, 2016
Continuation PCTUS2016026991 · Apr 11, 2016
Provisional Application 62536466 · Jul 25, 2017
Provisional Application 62526884 · Jun 29, 2017
Provisional Application 62259993 · Nov 25, 2015
Provisional Application 62114215 · Feb 10, 2015
Related Publication 20180289808A1 · Oct 11, 2018
Cited By (18)
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