IP Library Granted Patent US 11,793,786
Granted Patent B2
US 11,793,786 · App. 17/228,514 · Granted Oct 24, 2023

Administration of benzodiazepine compositions

Inventors: Steve Cartt (Hillsborough, CA); David Medeiros (Sparks, NV); Garry Thomas Gwozdz (Jim Thorpe, PA); Andrew Loxley (Brussels, BE); Mark Mitchnick (East Hampton, NY); David F. Hale (San Diego, CA); Edward T. Maggio (San Diego, CA)
Assignee: Neurelis, Inc.
A61K31/355A61K9/008A61K9/0043A61K31/5513
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Quick Facts
Patent No.
US 11,793,786
App. No.
17/228,514
Granted
Oct 24, 2023
Kind
B2
Abstract

The invention relates to pharmaceutical compositions comprising one or more benzodiazepine drugs for nasal administration, methods for producing and for using such compositions.

Claims (35)

1. A pharmaceutical solution for nasal administration consisting of:

a therapeutically effective amount of diazepam or a pharmaceutically acceptable salt thereof;

one or more natural or synthetic tocopherols or tocotrienols selected from the group consisting of α-tocopherol, β-tocopherol, γ-tocopherol, δ-tocopherol, α-tocotrienol, β-tocotrienol, γ-tocotrienol, δ-tocotrienol, tocophersolan, any isomers thereof, any esters thereof, and any combinations thereof, in an amount from 30% to 95% (w/w);

one or more alcohols in an amount from 10% to 70% (w/w), wherein the one or more alcohols comprises benzyl alcohol; and

n-dodecyl beta-D-maltoside.

2. The pharmaceutical solution of claim 1 , wherein the therapeutically effective amount of diazepam or pharmaceutically acceptable salt thereof is present in the pharmaceutical solution in a concentration from 1 to 20% (w/v).

3. The pharmaceutical solution of claim 1 , wherein the therapeutically effective amount of diazepam or pharmaceutically acceptable salt thereof is present in the pharmaceutical solution in a concentration from 10 mg/mL to 250 mg/mL.

4. The pharmaceutical solution of claim 3 , wherein the therapeutically effective amount of diazepam or pharmaceutically acceptable salt thereof is present in the pharmaceutical solution in a concentration from 20 mg/mL to 50 mg/mL.

5. The pharmaceutical solution of claim 1 , wherein the one or more natural or synthetic tocopherols or tocotrienols is in an amount from 45% to 85% (w/w).

6. The pharmaceutical solution of claim 5 , wherein the one or more natural or synthetic tocopherols or tocotrienols is in an amount from 60% to 75% (w/w).

7. The pharmaceutical solution of claim 1 , wherein the one or more alcohols is benzyl alcohol and a second alcohol selected from ethanol, propyl alcohol, butyl alcohol, pentanol, any isomers thereof, and any combinations thereof.

8. The pharmaceutical solution of claim 1 , wherein the one or more alcohols are in an amount from 15% to 55% (w/w).

9. The pharmaceutical solution of claim 8 , wherein the one or more alcohols are in an amount from 25% to 40% (w/w).

10. The pharmaceutical solution of claim 1 , wherein the solution consists of diazepam, vitamin E, benzyl alcohol, and n-dodecyl beta-D-maltoside.

11. A pharmaceutical solution for nasal administration consisting of:

a therapeutically effective amount of diazepam or a pharmaceutically acceptable salt thereof;

one or more natural or synthetic α-tocopherols selected from the group consisting of tocopherol, β-tocopherol, γ-tocopherol, δ-tocopherol, tocophersolan, any isomers thereof, any esters thereof, and any combinations thereof, in an amount from 30% to 95% (w/w);

one of more alcohols in an amount from 10% to 70% (w/w)), wherein the one or more alcohols comprises benzyl alcohol; and

n-dodecyl beta-D-maltoside.

12. The pharmaceutical solution of claim 11 , wherein the therapeutically effective amount of diazepam or pharmaceutically acceptable salt thereof is present in the pharmaceutical solution in a concentration from 1 to 20% (w/v).

13. The pharmaceutical solution of claim 11 , wherein the therapeutically effective amount of diazepam or pharmaceutically acceptable salt thereof is present in the pharmaceutical solution in a concentration from 10 mg/mL to 250 mg/mL.

14. The pharmaceutical solution of claim 13 , wherein the therapeutically effective amount of diazepam or pharmaceutically acceptable salt thereof is present in the pharmaceutical solution in a concentration from 20 mg/mL to 50 mg/mL.

15. The pharmaceutical solution of claim 11 , wherein the one or more natural or synthetic tocopherols is in an amount from 45% to 85% (w/w).

16. The pharmaceutical solution of claim 15 , wherein the one or more natural or synthetic tocopherols is in an amount from 60% to 75% (w/w).

17. The pharmaceutical solution of claim 11 , wherein the one or more alcohols is benzyl alcohol and a second alcohol selected from ethanol, propyl alcohol, butyl alcohol, pentanol, any isomers thereof, and any combinations thereof.

18. The pharmaceutical solution of claim 11 , wherein the one or more alcohols are in an amount from 15% to 55% (w/w).

19. The pharmaceutical solution of claim 18 , wherein the one or more alcohols are in an amount from 25% to 40% (w/w).

20. The pharmaceutical solution of claim 1 , wherein the therapeutically effective amount of diazepam or pharmaceutically acceptable salt thereof present in the pharmaceutical solution is from about 5 to about 20 mg.

21. The pharmaceutical solution of claim 11 , wherein the therapeutically effective amount of diazepam or pharmaceutically acceptable salt thereof present in the pharmaceutical solution is from about 1 mg to about 20 mg.

22. The pharmaceutical solution of claim 1 , wherein the n-dodecyl beta-D-maltoside is present in the pharmaceutical solution in an amount from about 0.01% (w/v) to about 1% (w/v).

23. The pharmaceutical solution of claim 11 , wherein the n-dodecyl beta-D-maltoside is present in the pharmaceutical solution in an amount from about 0.01% (w/v) to about 1% (w/v).

24. The pharmaceutical solution of claim 1 , wherein the n-dodecyl beta-D-maltoside is present in the pharmaceutical solution in an amount from about 0.125% (w/v) to about 0.5% (w/v).

25. The pharmaceutical solution of claim 11 , wherein the n-dodecyl beta-D-maltoside is present in the pharmaceutical solution in an amount from about 0.125% (w/v) to about 0.5% (w/v).

26. The pharmaceutical solution of claim 1 , wherein the α-tocopherol is Vitamin E USP.

27. The pharmaceutical solution of claim 11 , wherein the α-tocopherol is Vitamin E USP.

Assignments (4)
RELEASE OF SECURITY INTEREST Recorded Nov 14, 2024
From: ORBIMED ROYALTY & CREDIT OPPORTUNITIES III, LP
To: NEURELIS, INC.; AEGIS THERAPEUTICS, LLC
Reel/Frame 069359/0921 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 13, 2021
From: CARTT, STEVE; MEDEIROS, DAVID; GWOZDZ, GARRY THOMAS; LOXLEY, ANDREW; MITCHNICK, MARK; HALE, DAVID F.; MAGGIO, EDWARD T.
To: HALE BIOPHARMA VENTURES, LLC
Reel/Frame 058369/0257 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 13, 2021
From: HALE BIOPHARMA VENTURES, LLC
To: NEURELIS, INC.
Reel/Frame 058369/0292 →
SECURITY INTEREST Recorded Aug 6, 2021
From: NEURELIS, INC.; AEGIS THERAPEUTICS, LLC
To: ORBIMED ROYALTY & CREDIT OPPORTUNITIES III, LP
Reel/Frame 057111/0242 →
Cited By (1)
US 12,521,400