IP Library Granted Patent US 8,911,751
Granted Patent B2
US 8,911,751 · App. 12/078,317 · Granted Dec 16, 2014

Compositions for nasal delivery

Inventors: Elka Touitou (Jerusalem, IL); Biana Godin (Jerusalem, IL); Shaher Duchi (Kfar Rama, IL)
Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
A61K9/0043A61K47/24A61K31/196A61K31/05A61K9/0019A61K47/34A61K47/10A61K38/16A61K31/5513
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Quick Facts
Patent No.
US 8,911,751
App. No.
12/078,317
Granted
Dec 16, 2014
Kind
B2
Abstract

The present invention concerns a method of administering at least one active pharmaceutical agent to a patient in need thereof, which method comprises the intranasal administration of a composition comprising a therapeutically effective amount of this agent, phospholipids, one or more C2-C4 alcohols and water, wherein the concentrations of the phospholipids and the one or more alcohols in the composition are in the ranges of 0.2 to 10% and 12 to 30% by weight, respectively, with the water content of said composition being not less than 30% by weight, the phospholipids forming vesicles in said composition. Further are disclosed pharmaceutical compositions and combinations suitable for intranasal delivery.

Claims (40)

1. A method for the systemic administration of at least one active pharmaceutical agent, other than a nucleic acid, to a mammal, which method comprises administering to the mucous membranes of the nasal passage or nasal cavity of a mammal in need of the systemic administration of said agent, a composition comprising a therapeutically effective amount of said agent, phospholipids, one or more C2-C4 alcohols and water, wherein the concentrations of said phospholipids and said one or more alcohols in said composition are in the ranges of 0.2 to 10% and 12 to 30% by weight, respectively, with the water content of said composition being not less than 30% by weight, said phospholipids forming vesicles in said composition.

2. The method according to claim 1 , wherein said composition further includes one or more water-miscible polyols, wherein the concentration of said one or more polyols in said composition is in the range of 1 to 30% by weight.

3. The method according to claim 1 , wherein the C2-C4 alcohol is ethanol.

4. The method according to claim 2 , wherein the polyol is propylene glycol.

5. The method according to claim 1 , wherein the weight ratio between said C2-C4 alcohol and said phospholipids is not less than 2:1.

6. The method according to claim 1 , wherein said mammal is one in need of treatment of emesis, wherein said pharmaceutical agent is an anti-emetic agent.

7. The method of claim 6 , wherein said anti-emetic agent is granisetron.

8. The method according to claim 1 , wherein said mammal is one in need of treatment of diabetes, wherein said pharmaceutical agent is an anti-diabetic agent.

9. The method of claim 8 , wherein said anti-diabetic agent is insulin or derivative thereof.

10. The method according to claim 1 , wherein said mammal is one in need of treatment of malaria, wherein said pharmaceutical agent is an anti-malaria drug.

11. The method according to claim 1 , wherein said mammal is one in need of treatment of epileptic seizures, wherein said pharmaceutical agent is an anti-epileptic agent.

12. The method of claim 11 , wherein said anti-epileptic agent is diazepam.

13. The method according to claim 1 , wherein said mammal is one in need of treatment of depression and/or anxiety, wherein said pharmaceutical agent is an anti-depressant agent.

14. The method of claim 13 , wherein said anti-depressant agent is selected from group consisting of diazepam and buspirone hydrochloride.

15. The method according to claim 1 , wherein said mammal is one in need of treatment of obesity, wherein said pharmaceutical agent is an anti-obesity agent.

16. The method of claim 15 , wherein said anti-obesity agent is sibutramine.

17. The method according to claim 1 , wherein said mammal is one in need of treatment of depression and/or hot flushes, wherein said pharmaceutical agent is an anti-depression agent/anti-hot flushes agent.

18. The method of claim 17 , wherein said anti-depression/anti-hot flushes agent is paroxetine or a pharmaceutically acid addition salt thereof.

19. The method according to claim 1 , wherein said mammal is one in need of treatment of multiple sclerosis, wherein said pharmaceutical agent is an anti-multiple sclerosis agent.

20. The method of claim 19 , wherein said anti-multiple sclerosis agent is glatiramer acetate (GA).

21. The method according to claim 1 , wherein said mammal is one in need of treatment of dementia, wherein said pharmaceutical agent is an anti-dementia agent.

22. The method of claim 21 , wherein said dementia is Alzheimer disease.

23. The method of claim 22 , wherein said anti-dementia agent is rivastigmine.

24. The method according to claim 1 , wherein said mammal is one in need of treatment of pain, wherein said pharmaceutical agent is an analgesic agent.

25. The method of claim 24 , wherein said analgesic agent is tramadol.

26. The method according to claim 1 , wherein said mammal is one in need of induction of sleep, wherein said pharmaceutical agent is a hypnotic agent.

27. The method of claim 26 , wherein said hypnotic agent is brotizolam or any pharmaceutically acceptable salt thereof.

28. The method of claim 27 , wherein said hypnotic agent is diphenhydramine hydrochloride or any pharmaceutically acceptable salt thereof.

29. The method according to claim 1 , wherein said mammal is one in need of treatment of an inflammatory associated disease or disorder, wherein said pharmaceutical agent is a corticosteroid agent.

30. The method of claim 29 , wherein the inflammatory associated disease or disorder is an autoimmune disease.

31. The method of claim 30 , wherein said autoimmune disease is multiple sclerosis.

32. The method of claim 29 , wherein said corticosteroid agent is selected from the group consisting of dexamethasone and any pharmaceutically acceptable derivatives or salts thereof.

33. The method of claim 29 , wherein said corticosteroid agent is selected from the group consisting of prednisolone and any pharmaceutically acceptable derivatives or salts thereof.

34. The method according to claim 1 , wherein said mammal is one in need of treatment of Parkinson, wherein said pharmaceutical agent is an anti-parkinson agent.

35. The method of claim 34 , wherein said anti-parkinson agent is apomorphine.

36. The method of claim 19 , wherein said C2-C4 alcohol is ethanol.

37. The method of claim 24 , wherein said C2-C4 alcohol is ethanol.

38. The method according to claim 1 , wherein said mammal is one in need of treatment of multiple sclerosis, wherein said pharmaceutical agent is a combination of glatiramer acetate and cannabidiol.

39. The method according to claim 1 , wherein said mammal is one in need of regeneration of neurons and/or cells in a brain of a mammal, wherein said pharmaceutical agent is a combination of glatiramer acetate and cannabidiol.

40. The method according to claim 1 , wherein said mammal is one in need of treatment of pain, wherein said pharmaceutical agent is a combination of diazepam and diclofenac.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 22, 2008
From: TOUITOU, ELKA; GODIN, BIANA; DUCHI, SHAHER
To: YISSUM, RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
Reel/Frame 021270/0001 →
Continuity (4)
Continuation In Part PCTIL2006001187 · Oct 15, 2006
Provisional Application 60907340 · Mar 29, 2007
Provisional Application 60724904 · Oct 11, 2005
Related Publication 20090047234A1 · Feb 19, 2009