IP Library Granted Patent US 10,485,871
Granted Patent B2
US 10,485,871 · App. 16/372,958 · Granted Nov 26, 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 10,485,871
App. No.
16/372,958
Granted
Nov 26, 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 or pharmacokinetics of the NSAID for the treatment of conditions such as pain.

Claims (24)

1. A method of treating pain comprising: orally administering a solid dosage form to a human being for at least six consecutive days, wherein the solid dosage form comprises: 1) a complex of meloxicam and a sulfobutyl ether β-cyclodextrin (SBEβCD), 2) a bicarbonate, and 3) esomeprazole, wherein orally administering the solid dosage form to the human being results in a T max of meloxicam that is shorter than a T max of a reference solid dosage form that: 1) contains the same amount of meloxicam, 2) does not contain an SBEβCD, and 3) does not contain a bicarbonate, and wherein the average gastric pH of the human being on the sixth consecutive day is at least 3.5.

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

3. The method of claim 1 , wherein the solid dosage form comprises about 1 mg to about 50 mg of meloxicam.

4. The method of claim 3 , wherein the solid dosage form comprises about 15 mg of meloxicam.

5. The method of claim 3 , wherein the solid dosage form comprises about 20 mg of meloxicam.

6. The method of claim 1 , wherein the bicarbonate is sodium bicarbonate or potassium bicarbonate.

7. The method of claim 6 , wherein the solid dosage form comprises 400 mg to 900 mg of sodium bicarbonate.

8. The method of claim 6 , wherein the solid dosage form comprises 450 mg to 550 mg of sodium bicarbonate.

9. The method of claim 6 , wherein the solid dosage form comprises 500 mg of sodium bicarbonate.

10. The method of claim 1 , wherein about 30 mg to about 50 mg of esomeprazole is present in the solid dosage form.

11. The method of claim 1 , wherein about 40 mg of esomeprazole is present in the solid dosage form.

12. The method of claim 1 , wherein the SBEβCD has about 6 to about 7 sulfobutyl ether groups for each molecule of β-cyclodextrin.

13. The method of claim 1 , wherein the solid dosage form contains about 75 mg to about 150 mg of the SBEβCD.

14. The method of claim 1 , wherein the solid dosage form contains about 100 mg to about 140 mg of the SBEβCD.

15. The method of claim 14 , wherein the solid dosage form contains about 100 mg of the SBEβCD.

16. The method of claim 1 , wherein the solid dosage form has been shown to have a median T max of meloxicam that is less than about 2 hours in fasted human subjects.

17. The method of claim 1 , wherein the solid dosage form has been shown to have a median T max of meloxicam that is within about 80 minutes in fasted human subjects.

18. The method of claim 1 , wherein the solid dosage form has been shown to have a median T max of meloxicam that is less than about 1 hour in fasted human subjects.

19. The method of claim 1 , wherein the solid dosage form has been shown to have a median time to half-maximal plasma concentration of meloxicam that is less than about 30 minutes in fasted human subjects.

20. The method of claim 1 , wherein the solid dosage form has been shown to have a median T max of meloxicam that is at least 5 times shorter as compared to the reference solid dosage form in fasted human subjects.

21. The method of claim 1 , wherein the solid dosage form has been shown to have a median C max of meloxicam that is at least 1800 ng/mL in fasted human subjects.

22. The method of claim 1 , wherein the solid dosage form has been shown to have a median C max of meloxicam that is about 2000 ng/mL to about 2500 ng/mL in fasted human subjects.

23. The method of claim 1 , wherein the pain is inflammatory pain.

24. The method of claim 1 , wherein the solid dosage form is orally administered to the human being to treat pain associated with osteoarthritis, rheumatoid arthritis, or juvenile rheumatoid arthritis.

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 May 29, 2019
From: TABUTEAU, HERRIOT
To: AXSOME THERAPEUTICS, INC.
Reel/Frame 049305/0160 →
Continuity (10)
Continuation 15984055 · May 18, 2018
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 20190224320A1 · Jul 25, 2019
Cited By (16)
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