IP Library › Granted Patent US 12,337,061
Granted Patent B2
US 12,337,061 · App. 17/721,595 · Granted Jun 24, 2025

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 Hale (San Diego, CA); Edward T. Maggio (San Diego, CA)
Assignee: Neurelis, Inc.
A61K9/0043A61K9/008A61K9/08A61K9/10A61K31/355A61K31/5513A61K45/06A61K47/10A61K47/22A61K47/26
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Quick Facts
Patent No.
US 12,337,061
App. No.
17/721,595
Granted
Jun 24, 2025
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 (116)

1. A method of treating bouts of intermittent and stereotypic episodes of increased seizure activity in an epilepsy patient that is distinguishable from other seizures suffered by the patient consisting of:

administering a single spray of 100 μL of a stable pharmaceutical solution to a nostril of the patient, the pharmaceutical solution containing:

14.47 mg of vitamin E USP;

10 mg of diazepam;

0.25 mg of dodecyl maltoside;

0.50 mg of benzyl alcohol; and

a sufficient quantity of ethanol;

wherein administering the single spray of the pharmaceutical solution achieves 96% to 97% of the bioavailability of an equivalent dose of diazepam administered intravenously;

wherein administering the single spray of the pharmaceutical solution is safe and effective in treating the bouts of intermittent and stereotypic episodes of increased seizure activity in the patient; and

wherein administering the single spray of the pharmaceutical solution results in a treatment selected from the group consisting of a reduction in the severity of the seizure, a reduction in the probability that the patient will experience a repeat seizure, an increase in the interval between a current seizure and a next seizure in the patient, a reduction in the frequency of seizure in the patient and combinations thereof.

2. The method of claim 1 , wherein the pharmaceutical solution is stable at 25° C. and 60% relative humidity for at least 3 months.

3. The method of claim 1 , wherein administering the single spray of the pharmaceutical solution results in treatment in less than about 5 minutes.

4. The method of claim 3 , wherein administering the single spray of the pharmaceutical solution results in treatment over about 24 hours.

5. A method of treating bouts of intermittent and stereotypic episodes of increased seizure activity in an epilepsy patient that is distinguishable from other seizures suffered by the patient consisting of:

administering a single spray of 100 μL of a stable pharmaceutical solution to a nostril of the patient and administering a second single spray of 100 μL of the pharmaceutical solution to a second nostril of the patient, each of the 100 μL of the pharmaceutical solution containing:

14.47 mg of vitamin E USP;

10 mg of diazepam;

0.25 mg of dodecyl maltoside;

0.50 mg of benzyl alcohol; and

a sufficient quantity of ethanol;

wherein administering the single spray and administering the second single spray of the pharmaceutical solution achieves 96% to 97% of the bioavailability of an equivalent dose of diazepam administered intravenously;

wherein administering the single spray and administering the second single spray of the pharmaceutical solution is safe and effective in treating the bouts of intermittent and stereotypic episodes of increased seizure activity in the patient; and

wherein administering the single spray and administering the second single spray of the pharmaceutical solution results in a treatment selected from the group consisting of a reduction in the severity of the seizure, a reduction in the probability that the patient will experience a repeat seizure, an increase in the interval between a current seizure and a next seizure in the patient, a reduction in the frequency of seizure in the patient and combinations thereof.

6. The method of claim 5 , wherein the pharmaceutical solution is stable at 25° C. and 60% relative humidity for at least 3 months.

7. The method of claim 5 , wherein administering the single spray and administering the second single spray of the pharmaceutical solution results in treatment in less than about 5 minutes.

8. The method of claim 7 , wherein administering the single spray and administering the second single spray of the pharmaceutical solution results in treatment over about 24 hours.

9. The method of claim 1 , wherein the single spray of 100 μL is administered to a nostril of the patient as a single metered spray.

10. The method of claim 5 , wherein the single spray of 100 μL and the second single spray of 100 μL are each administered to a nostril of the patient as a single metered spray.

11. The method of claim 1 , wherein the ethanol is dehydrated ethanol.

12. The method of claim 5 , wherein the ethanol is dehydrated ethanol.

13. The method of claim 1 , wherein the dodecyl maltoside is n-dodecyl-B-D-maltoside.

14. The method of claim 5 , wherein the dodecyl maltoside is n-dodecyl-B-D-maltoside.

15. The method of claim 1 , wherein the pharmaceutical solution exhibits an approximate area under a blood plasma concentration curve measuring total drug exposure across time (AUC 0-∞ ) of 7338 hours*ng/ml.

16. The method of claim 5 , wherein the pharmaceutical solution exhibits an approximate area under a blood plasma concentration curve measuring total drug exposure across time (AUC 0-∞ ) of 7338 hours*ng/mL.

17. The method of claim 1 , wherein the pharmaceutical solution exhibits an approximate C max of 272 ng/mL.

18. The method of claim 5 , wherein the pharmaceutical solution exhibits an approximate C max of 272 ng/mL.

19. The method of claim 1 , wherein the pharmaceutical solution exhibits an approximate T max of 1.5 hours.

20. The method of claim 5 , wherein the pharmaceutical solution exhibits an approximate T max of 1.5 hours.

21. A method of treating bouts of intermittent and stereotypic episodes of increased seizure activity in an epilepsy patient that is distinguishable from other seizures suffered by the patient comprising:

administering a single spray of 100 μL +/−5% of a stable pharmaceutical solution to a nostril of the patient, the pharmaceutical solution containing:

14.47 mg of vitamin E USP +/−5%;

10 mg of diazepam;

0.25 mg of dodecyl maltoside +/−5%;

10.50 mg of benzyl alcohol +/−5%; and

a sufficient quantity of ethanol;

wherein administering the single spray of the pharmaceutical solution achieves 92.5% to 107.5% of the bioavailability of an equivalent dose of diazepam administered intravenously;

wherein administering the single spray of the pharmaceutical solution is safe and effective in treating the bouts of intermittent and stereotypic episodes of increased seizure activity in the patient; and

wherein administering the single spray of the pharmaceutical solution results in a treatment selected from the group consisting of a reduction in the severity of the seizure, a reduction in the probability that the patient will experience a repeat seizure, an increase in the interval between a current seizure and a next seizure in the patient, a reduction in the frequency of seizure in the patient and combinations thereof.

22. The method of claim 21 , wherein the pharmaceutical solution is stable at 25° C. and 60% relative humidity for at least 3 months.

23. The method of claim 21 , wherein administering the single spray of the pharmaceutical solution results in treatment in less than about 5 minutes.

24. The method of claim 21 , wherein administering the single spray of the pharmaceutical solution results in treatment over about 24 hours.

25. The method of claim 21 , wherein the single spray of 100 μL is administered to a nostril of the patient as a single metered spray.

26. The method of claim 21 , wherein the ethanol is dehydrated ethanol.

27. The method of claim 21 , wherein the dodecyl maltoside is n-dodecyl-B-D-maltoside.

28. The method of claim 21 , wherein the pharmaceutical solution exhibits an approximate area under a blood plasma concentration curve measuring total drug exposure across time (AUC 0-∞ ) of 7338 hours*ng/mL.

29. The method of claim 21 , wherein the pharmaceutical solution exhibits an approximate C max of 272 ng/mL.

30. The method of claim 21 , wherein the pharmaceutical solution exhibits an approximate T max of 1.5 hours.

31. The method of claim 21 , wherein the pharmaceutical solution exhibits a half-life of about 49.2 hours.

32. The method of claim 21 , wherein the absolute bioavailability is 96% to 97%.

33. A method of treating bouts of intermittent and stereotypic episodes of increased seizure activity in an epilepsy patient that is distinguishable from other seizures suffered by the patient comprising:

administering a single spray of 100 μL +/−5% of a stable pharmaceutical solution to a nostril of the patient and administering a second single spray of 100 μL +/−5% of the pharmaceutical solution to a second nostril of the patient, each of the 100 μL +/−5% of the pharmaceutical solution containing:

14.47 mg of vitamin E USP +/−5%;

10 mg of diazepam;

0.25 mg of dodecyl maltoside +/−5%;

10.50 mg of benzyl alcohol +/−5%; and

a sufficient quantity of ethanol;

wherein administering the single spray and administering the second single spray of the pharmaceutical solution achieves 92.5% to 107.5% of the bioavailability of an equivalent dose of diazepam administered intravenously;

wherein administering the single spray and administering the second single spray of the pharmaceutical solution is safe and effective in treating the bouts of intermittent and stereotypic episodes of increased seizure activity in the patient; and

wherein administering the single spray and administering the second single spray of the pharmaceutical solution results in a treatment selected from the group consisting of a reduction in the severity of the seizure, a reduction in the probability that the patient will experience a repeat seizure, an increase in the interval between a current seizure and a next seizure in the patient, a reduction in the frequency of seizure in the patient and combinations thereof.

34. The method of claim 33 , wherein the pharmaceutical solution is stable at 25° C. and 60% relative humidity for at least 3 months.

35. The method of claim 33 , wherein administering the single spray and the second single spray of the pharmaceutical solution results in treatment in less than about 5 minutes.

36. The method of claim 33 , wherein administering the single spray and the second single spray of the pharmaceutical solution results in treatment over about 24 hours.

37. The method of claim 33 , wherein the single spray of 100 μL +/−5% and the second single spray of 100 μL +/−5% are each administered to a nostril of the patient as a single metered spray.

38. The method of claim 33 , wherein the ethanol is dehydrated ethanol.

39. The method of claim 33 , wherein the dodecyl maltoside is n-dodecyl-B-D-maltoside.

40. The method of claim 33 , wherein the pharmaceutical solution exhibits an approximate T max of 1.5 hours.

41. The method of claim 33 , wherein the pharmaceutical solution exhibits a half-life of about 49.2 hours.

42. The method of claim 33 , wherein the absolute bioavailability is 96% to 97%.

43. A method of treating bouts of intermittent and stereotypic episodes of increased seizure activity in an epilepsy patient that is distinguishable from other seizures suffered by the patient comprising:

administering a single spray of 100 μL +/−5% of a stable pharmaceutical solution to a nostril of the patient and administering a second single spray of 100 μL +/−5% of the pharmaceutical solution to a second nostril of the patient, each of the 100 μL +/−5% of the pharmaceutical solution containing:

14.47 mg of vitamin E USP +/−5%;

7.5 mg of diazepam;

0.25 mg of dodecyl maltoside +/−5%;

10.50 mg of benzyl alcohol +/−5%; and

a sufficient quantity of ethanol;

wherein administering the single spray and administering the second single spray of the pharmaceutical solution achieves 92.5% to 107.5% of the bioavailability of an equivalent dose of diazepam administered intravenously;

wherein administering the single spray and administering the second single spray of the pharmaceutical solution is safe and effective in treating the bouts of intermittent and stereotypic episodes of increased seizure activity in the patient; and

wherein administering the single spray and administering the second single spray of the pharmaceutical solution results in a treatment selected from the group consisting of a reduction in the severity of the seizure, a reduction in the probability that the patient will experience a repeat seizure, an increase in the interval between a current seizure and a next seizure in the patient, a reduction in the frequency of seizure in the patient and combinations thereof.

44. The method of claim 43 , wherein the pharmaceutical solution is stable at 25° C. and 60% relative humidity for at least 3 months.

45. The method of claim 43 , wherein administering the single spray and the second single spray of the pharmaceutical solution results in treatment in less than about 5 minutes.

46. The method of claim 43 , wherein administering the single spray and the second single spray of the pharmaceutical solution results in treatment over about 24 hours.

47. The method of claim 43 , wherein the single spray of 100 μL +/−5% and the second single spray of 100 μL +/−5% are each administered to a nostril of the patient as a single metered spray.

48. The method of claim 43 , wherein the ethanol is dehydrated ethanol.

49. The method of claim 43 , wherein the dodecyl maltoside is n-dodecyl-B-D-maltoside.

50. The method of claim 43 , wherein the pharmaceutical solution exhibits an approximate T max of 1.5 hours.

51. The method of claim 43 , wherein the pharmaceutical solution exhibits a half-life of about 49.2 hours.

52. The method of claim 43 , wherein the absolute bioavailability is 96% to 97%.

53. A method of treating bouts of intermittent and stereotypic episodes of increased seizure activity in an epilepsy patient that is distinguishable from other seizures suffered by the patient comprising:

administering a single spray of 100 μL +/−5% of a stable pharmaceutical solution to a nostril of the patient, the pharmaceutical solution containing:

14.47 mg of vitamin E USP +/−5%;

5 mg of diazepam;

0.25 mg of dodecyl maltoside +/−5%;

10.50 mg of benzyl alcohol +/−5%; and

a sufficient quantity of ethanol;

wherein administering the single spray of the pharmaceutical solution achieves 92.5% to 107.5% of the bioavailability of an equivalent dose of diazepam administered intravenously;

wherein administering the single spray of the pharmaceutical solution is safe and effective in treating the bouts of intermittent and stereotypic episodes of increased seizure activity in the patient; and

wherein administering the single spray of the pharmaceutical solution results in a treatment selected from the group consisting of a reduction in the severity of the seizure, a reduction in the probability that the patient will experience a repeat seizure, an increase in the interval between a current seizure and a next seizure in the patient, a reduction in the frequency of seizure in the patient and combinations thereof.

54. The method of claim 53 , wherein the pharmaceutical solution is stable at 25° C. and 60% relative humidity for at least 3 months.

55. The method of claim 53 , wherein administering the single spray of the pharmaceutical solution results in treatment in less than about 5 minutes.

56. The method of claim 53 , wherein administering the single spray of the pharmaceutical solution results in treatment over about 24 hours.

57. The method of claim 53 , wherein the single spray of 100 μL is administered to a nostril of the patient as a single metered spray.

58. The method of claim 53 , wherein the ethanol is dehydrated ethanol.

59. The method of claim 53 , wherein the dodecyl maltoside is n-dodecyl-β-D-maltoside.

60. The method of claim 53 , wherein the pharmaceutical solution exhibits an approximate T max of 1.5 hours.

61. The method of claim 53 , wherein the pharmaceutical solution exhibits a half-life of about 49.2 hours.

62. The method of claim 53 , wherein the absolute bioavailability is 96% to 97%.

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 →
SECURITY INTEREST Recorded Jun 3, 2022
From: NEURELIS, INC.; AEGIS THERAPEUTICS, LLC
To: ORBIMED ROYALTY & CREDIT OPPORTUNITIES III, LP
Reel/Frame 060096/0039 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 15, 2022
From: CARTT, STEVE; MEDEIROS, DAVID; GWOZDZ, GARRY THOMAS; LOXLEY, ANDREW; MITCHNICK, MARK; HALE, DAVID; MAGGIO, EDWARD T.
To: HALE BIOPHARMA VENTURES, LLC
Reel/Frame 059609/0658 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 15, 2022
From: HALE BIOPHARMA VENTURES, LLC
To: NEURELIS, INC.
Reel/Frame 059609/0702 →
Continuity (7)
Continuation 17336389 · Jun 2, 2021
Continuation 15470498 · Mar 27, 2017
Continuation 14527613 · Oct 29, 2014
Continuation 13495942 · Jun 13, 2012
Provisional Application 61570110 · Dec 13, 2011
Provisional Application 61497017 · Jun 14, 2011
Related Publication 20220241187A1 · Aug 4, 2022
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