IP Library Granted Patent US 11,517,543
Granted Patent B2
US 11,517,543 · App. 17/525,339 · Granted Dec 6, 2022

Bupropion as a modulator of drug activity

Inventor: Herriot Tabuteau (New York, NY)
Assignee: ANTECIP BIOVENTURES II LLC
A61K31/138A61K9/0053A61K31/137A61K31/485A61P25/24
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Quick Facts
Patent No.
US 11,517,543
App. No.
17/525,339
Granted
Dec 6, 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 (23)

1. A method of treating major depressive disorder, comprising:

orally administering, to an adult human suffering from major depressive disorder, a dosage form comprising:

about 105 mg of bupropion hydrochloride, formulated for sustained release and

about 45 mg of a dextromethorphan, formulated for immediate release, as the only therapeutically active compounds in the dosage form;

wherein the dosage form is administered once a day for the first three days, and twice a day thereafter so that the 105 mg of bupropion hydrochloride and the 45 mg of the dextromethorphan are administered once a day or twice a day for at least 14 days.

2. The method of claim 1 , wherein the dextromethorphan is dextromethorphan hydrobromide.

3. The method of claim 1 , wherein the adult human has a C max of bupropion that is about 90 ng/mL after 8 days of dosing.

4. The method of claim 1 , wherein the adult human has an AUC 0-12 of bupropion that is about 600 ng·hr/mL after 8 days of dosing.

5. The method of claim 1 , wherein the adult human has an AUC 0-12 of bupropion that is about 700 ng·hr/mL after 8 days of dosing.

6. The method of claim 1 , wherein the adult human has an AUC 0-12 of bupropion that is about 600 ng·hr/mL to about 700 ng·hr/mL after 8 days of dosing.

7. The method of claim 1 , wherein the adult human is suffering from treatment-resistant major depressive disorder.

8. The method of claim 1 , wherein the dosage form further comprises microcrystalline cellulose.

9. The method of claim 1 , wherein the dosage form further comprises magnesium stearate.

10. The method of claim 1 , wherein the adult human has a T max of dextromethorphan that is about 4 hours after 8 days of dosing.

11. The method of claim 1 , wherein the administration of the dosage form yields an increased elimination half-life of dextromethorphan as compared to a corresponding elimination half-life of dextromethorphan, were the dextromethorphan administered alone.

12. The method of claim 1 , wherein administration of the dosage form results in the adult human experiencing an improvement of a depressive symptom.

13. The method of claim 12 , wherein the depressive symptom comprises sadness.

14. The method of claim 12 , wherein the depressive symptom comprises reduced sleep.

15. The method of claim 12 , wherein the depressive symptom comprises reduced appetite.

16. The method of claim 12 , wherein the depressive symptom comprises difficulty concentrating.

17. The method of claim 12 , wherein the depressive symptom comprises lassitude.

18. The method of claim 12 , wherein the depressive symptom comprises pessimism.

19. The method of claim 1 , wherein the administration of the dosage form yields higher systemic exposure to dextromethorphan as compared to a corresponding systemic exposure to dextromethorphan, were the 45 mg of the dextromethorphan administered alone.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 30, 2021
From: TABUTEAU, HERRIOT
To: ANTECIP BIOVENTURES II LLC
Reel/Frame 058246/0668 →