IP Library Granted Patent US 10,471,014
Granted Patent B2
US 10,471,014 · App. 16/001,697 · Granted Nov 12, 2019

Pharmaceutical compositions comprising meloxicam

Inventor: Herriot Tabuteau (New York, NY)
Assignee: AXSOME THERAPEUTICS, INC.
A61K9/2009A61K9/0053A61K9/205A61K9/209A61K9/2086A61K31/4196A61K31/5415A61K47/02A61K47/40A61K47/6951A61P25/06C08B37/0015
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Quick Facts
Patent No.
US 10,471,014
App. No.
16/001,697
Filed
Jun 6, 2018
Granted
Nov 12, 2019
Kind
B2
Art Unit
1628
USPC
514/226.5
Abstract

Disclosed herein are compositions comprising a drug such as a triptan (e.g. rizatriptan) and/or an NSAID (e.g. 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 drug for the treatment of conditions such as pain.

Claims (19)

1. A method of treating migraine, comprising administering a solid oral dosage form comprising a complex of meloxicam with a sulfobutyl ether β-cyclodextrin (SBEβCD), at least 400 mg of a bicarbonate, and rizatriptan to a human being suffering from migraine.

2. The method of claim 1 , wherein about 8 mg to about 13 mg of the rizatriptan is present in the dosage form based upon the weight of the rizatriptan in the free base form.

3. The method of claim 1 , wherein the rizatriptan is present in a salt form in an amount that is a molar equivalent to about 10 mg of the rizatriptan in the free base form.

4. The method of claim 3 , wherein the rizatriptan is present as rizatriptan benzoate.

5. The method of claim 1 , wherein the dosage form contains about 15 mg to about 25 mg of meloxicam.

6. The method of claim 1 , wherein the dosage form contains about 20 mg of meloxicam.

7. The method of claim 1 , wherein the dosage form contains about 100 mg to about 175 mg of the SBEβCD.

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

9. The method of claim 1 , wherein the bicarbonate comprises sodium bicarbonate.

10. The method of claim 1 , wherein the dosage form contains about 400 mg to about 600 mg of the bicarbonate.

11. The method of claim 1 , wherein the dosage form contains about 500 mg of sodium bicarbonate.

12. The method of claim 1 , wherein the bicarbonate improves solubility of meloxicam in the dosage form in a greater extent than a carbonate would in a reference dosage form containing: (1) about same amount of meloxicam, and (2) an amount of carbonate that would achieve same pH as the bicarbonate.

13. The method of claim 1 , wherein 15 minutes after the dosage form is orally administered, the amount of the meloxicam dissolved in the stomach fluid of the human being is greater than the amount of the meloxicam that would be dissolved in the stomach fluid of the human being as a result of orally administering to the human being a reference dosage form containing: 1) the same amount of meloxicam, and 2) no bicarbonate.

14. The method of claim 1 , wherein 15 minutes after the dosage form is orally administered, the amount of the rizatriptan dissolved in the stomach fluid of the human being is greater than the amount of the rizatriptan that would be dissolved in the stomach fluid of the human being as a result of orally administering to the human being a reference dosage form containing: 1) the same amount of meloxicam, and 2) no bicarbonate.

15. The method of claim 1 , wherein the human being experiences pain relief sooner than would be experienced as a result of orally administering to the human being a reference dosage form containing: 1) the same amount of meloxicam, and 2) no bicarbonate.

16. The method of claim 1 , wherein 30 minutes after the dosage form is orally administered, at least about 50% of the rizatriptan in the dosage form is dissolved in the stomach fluid of the human being.

17. The method of claim 1 , wherein 30 minutes after the dosage form is orally administered, at least about 50% of the meloxicam in the dosage form is dissolved in the stomach fluid of the human being.

18. The method of claim 1 , wherein the dosage form provides a T max of meloxicam in the human being that is less than about 2 hours.

19. The method of claim 1 , wherein the dosage form provides a T max of meloxicam in the human being that is less than about 3 hours.

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 046310/0559 →
Cited By (16)
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