IP Library Granted Patent US 11,478,468
Granted Patent B2
US 11,478,468 · App. 17/705,930 · Granted Oct 25, 2022

Bupropion as a modulator of drug activity

Inventor: Herriot Tabuteau (New York, NY)
Assignee: ANTECIP BIOVENTURES II LLC
A61K31/485A61K9/0053A61K31/135A61K31/137A61K31/15A61K31/343A61K31/381
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Quick Facts
Patent No.
US 11,478,468
App. No.
17/705,930
Granted
Oct 25, 2022
Kind
B2
Abstract

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan.

Claims (19)

1. A method of treating major depressive disorder, comprising administering a dosage form by mouth once daily or twice daily to a human patient in need thereof for at least 8 consecutive days, wherein the dosage form comprises about 105 mg of bupropion hydrochloride and about 45 mg of a dextromethorphan salt as the only therapeutically active compounds in the dosage form and the dosage form is formulated for sustained release of bupropion hydrochloride and immediate release of the dextromethorphan salt, and wherein the human being experiences an improvement of depressive symptoms after the dosage form is administered by mouth to the human patient.

2. The method of claim 1 , wherein each of the depressive symptoms is selected from the group consisting of feelings of sadness, inner tension, reduced sleep or appetite, difficulty concentrating, pessimism, and a combination thereof.

3. The method of claim 2 , wherein the dosage form is a tablet, bupropion hydrochloride is in a sustained release formulation, the dextromethorphan salt is in an immediate release formulation, the human patient is an extensive CYP2D6 metabolizer, the dosage form is administered once daily by mouth for three days followed by twice daily by mouth thereafter for a total of at least 8 days, and wherein on the eighth day that the dosage form is administered, the C max of bupropion is about 9×10 1 ng/mL in the human patient and the AUC 0-12 of bupropion in the human patient is about 7×10 2 ng·hr/mL.

4. The method of claim 3 , wherein the dextromethorphan salt is dextromethorphan hydrobromide.

5. The method of claim 1 , wherein one of the depressive symptoms is feelings of sadness.

6. The method of claim 5 , wherein the dosage form is a tablet, bupropion hydrochloride is in a sustained release formulation, the dextromethorphan salt is in an immediate release formulation, the human patient is an extensive CYP2D6 metabolizer, the dosage form is administered once daily by mouth for three days followed by twice daily by mouth thereafter for a total of at least 8 days, and wherein on the eighth day that the dosage form is administered, the C max of bupropion in the human patient is about 9×10 1 ng/mL and the AUC 0-12 of bupropion in the human patient is about 7×10 2 ng·hr/mL.

7. The method of claim 6 , wherein the dextromethorphan salt is dextromethorphan hydrobromide.

8. The method of claim 1 , wherein one of the depressive symptoms is inner tension.

9. The method of claim 8 , wherein the dosage form is a tablet, bupropion hydrochloride is in a sustained release formulation, the dextromethorphan salt is in an immediate release formulation, the human patient is an extensive CYP2D6 metabolizer, the dosage form is administered once daily by mouth for three days followed by twice daily by mouth thereafter for a total of at least 8 days, and wherein on the eighth day that the dosage form is administered, the C max of bupropion in the human patient is about 9×10 1 ng/mL and the AUC 0-12 of bupropion in the human patient is about 7×10 2 ng·hr/mL.

10. The method of claim 9 , wherein the dextromethorphan salt is dextromethorphan hydrobromide.

11. The method of claim 1 , wherein one of the depressive symptoms is reduced sleep or appetite.

12. The method of claim 11 , wherein the dosage form is a tablet, bupropion hydrochloride is in a sustained release formulation, the dextromethorphan salt is in an immediate release formulation, the human patient is an extensive CYP2D6 metabolizer, the dosage form is administered once daily by mouth for three days followed by twice daily by mouth thereafter for a total of at least 8 days, and wherein on the eighth day that the dosage form is administered, the C max of bupropion in the human patient is about 9×10 1 ng/mL and the AUC 0-12 of bupropion in the human patient is about 7×10 2 ng·hr/mL.

13. The method of claim 12 , wherein the dextromethorphan salt is dextromethorphan hydrobromide.

14. The method of claim 1 , wherein one of the depressive symptoms is difficulty concentrating.

15. The method of claim 14 , wherein the dosage form is a tablet, bupropion hydrochloride is in a sustained release formulation, the dextromethorphan salt is in an immediate release formulation, the human patient is an extensive CYP2D6 metabolizer, the dosage form is administered once daily by mouth for three days followed by twice daily by mouth thereafter for a total of at least 8 days, and wherein on the eighth day that the dosage form is administered, the C max of bupropion in the human patient is about 9×10 1 ng/mL and the AUC 0-12 of bupropion in the human patient is about 7×10 2 ng·hr/mL.

16. The method of claim 15 , wherein the dextromethorphan salt is dextromethorphan hydrobromide.

17. The method of claim 1 , wherein one of the depressive symptoms is pessimism.

18. The method of claim 17 , wherein the dosage form is a tablet, bupropion hydrochloride is in a sustained release formulation, the dextromethorphan salt is in an immediate release formulation, the human patient is an extensive CYP2D6 metabolizer, the dosage form is administered once daily by mouth for three days followed by twice daily by mouth thereafter for a total of at least 8 days, and wherein on the eighth day that the dosage form is administered, the C max of bupropion in the human patient is about 9×10 1 ng/mL and the AUC 0-12 of bupropion in the human patient is about 7×10 2 ng·hr/mL.

19. The method of claim 18 , wherein the dextromethorphan salt is dextromethorphan hydrobromide.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 26, 2022
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 059737/0164 →
Continuity (14)
Continuation In Part 17191014 · Mar 3, 2021
Continuation In Part 16822697 · Mar 18, 2020
Continuation In Part 16359958 · Mar 20, 2019
Continuation In Part 15821563 · Nov 22, 2017
Continuation In Part 15645939 · Jul 10, 2017
Continuation In Part 15263138 · Sep 12, 2016
Continuation 15164746 · May 25, 2016
Continuation In Part 14879002 · Oct 8, 2015
Continuation 14554988 · Nov 26, 2014
Continuation 14550618 · Nov 21, 2014
Continuation In Part PCTUS2014064184 · Nov 5, 2014
Provisional Application 61900354 · Nov 5, 2013
Provisional Application 62576538 · Oct 24, 2017
Related Publication 20220218698A1 · Jul 14, 2022
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