IP Library Granted Patent US 9,056,086
Granted Patent B2
US 9,056,086 · App. 13/622,120 · Granted Jun 16, 2015

Pharmaceutical compositions comprising DGLA, 15-HEPE, and/or 15-HETrE and methods of use thereof

Inventors: Mehar Manku (Birmingham, GB); John Climax (Dublin, IE); David Coughlan (Dublin, IE)
Assignee: Dignity Sciences Limited
A61K31/202A61K31/19A61K31/192A61K31/327A61K45/06A61K9/0014A61K8/361A61K8/368A61K8/38A61K8/4946A61K8/675A61Q19/00
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Quick Facts
Patent No.
US 9,056,086
App. No.
13/622,120
Granted
Jun 16, 2015
Kind
B2
Abstract

The present disclosure provides compositions comprising fatty acids, or derivatives thereof (e.g., C1-C4 esters) including, for example, DGLA, 15-OHEPA and/or 15-HETrE, used singly or in combination with anti-bacterial agents for the treatment of disease and/or disorders such as acne or atopic dermatitis.

Claims (44)

1. A method for treating acne in a subject in need thereof, the method comprising: administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of 15-hydroxy-eicosapentaenoic acid (“15-HEPE”) or 15-hydroxy-eicosatrienoic acid (“15-HETrE”).

2. The method of claim 1 , wherein the pharmaceutical composition comprises about 0.1 wt. % to about 20 wt. % of 15-HEPE or 15-HETrE.

3. A method of treating acne in a subject in need thereof, the method comprising: topically administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of dihomo-gamma-linolenic acid (“DGLA”), 15-HEPE, or 15-HETrE, wherein the pharmaceutical composition further comprises about 1.65 wt. % steareth-2, about 1.35 wt. % steareth-21, about 0.5 wt. % cetyl alcohol, about 0.2 wt. % ascorbyl palmitate, about 0.15 wt. % a-tocopherol, about 2.0 wt. % medium-chain triglycerides, about 2.0 wt. % myristyl myristate, about 4.0 wt. % isopropryl palmitate, about 1.0 wt. % glycerin, about 1.0 wt. % phenoxyethanol, about 0.1 wt. % ascorbic acid, about 0.8 wt. % carbomer, about 0.4 wt. % xanthan gum, about 0.5 wt. % liquid soy lecithin, and about 0.05 wt. % Mild Care 345 fragrance.

4. The method of claim 2 , wherein the pharmaceutical composition comprising 15-HEPE further includes a therapeutically effective amount of benzoyl peroxide.

5. The method of claim 4 , wherein the pharmaceutical composition comprises about 1.25% to about 10 wt. % of benzoyl peroxide.

6. The method of claim 2 , wherein the pharmaceutical composition comprising 15-HETrE further includes a therapeutically effective amount of adapalene.

7. The method of claim 6 , wherein the pharmaceutical composition comprises about 0.05 wt. % to about 0.3 wt. % of adapalene.

8. The method of claim 3 , wherein the step of administering comprises topically applying the composition to an area of the skin afflicted with acne lesions.

9. The method of claim 8 , wherein the area of the skin afflicted with acne lesions is first washed prior to application of the pharmaceutical composition.

10. The method of claim 8 , wherein the acne lesions are inflammatory type and/or non-inflammatory type lesions.

11. The method of claim 10 , wherein applying the composition results in about a 10%, 20%, 30%, 40%, 50% 50%, 70%, 80%, 90% or more reduction in number of acne lesions.

12. The method of claim 3 , wherein the acne is associated with Propionibacterium acnes.

13. The method of claim 3 , wherein the pharmaceutical composition is administered to the subject once a day, twice a day, or three times a day.

14. The method of claim 3 , wherein the pharmaceutical composition is a cream.

15. The method of claim 3 , wherein the subject previously exhibited acne lesions.

16. A method of treating acne vulgaris or acne necrotica in a subject in need thereof, the method comprising: topically administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of DGLA, wherein the pharmaceutical composition further comprises about 1.65 wt. % steareth-2, about 1.35 wt. % steareth-21, about 0.5 wt. % cetyl alcohol, about 0.2 wt. % ascorbyl palmitate, about 0.15 wt. % a-tocopherol, about 2.0 wt. % medium-chain triglycerides, about 2.0 wt. % myristyl myristate, about 4.0 wt. % isopropryl palmitate, about 1.0 wt. % glycerin, about 1.0 wt. % phenoxyethanol, about 0.1 wt. % ascorbic acid, about 0.8 wt. % carbomer, about 0.4 wt. % xanthan gum, about 0.5 wt. % liquid soy lecithin, and about 0.05 wt. % Mild Care 345 fragrance.

17. The method of claim 16 , wherein the pharmaceutical composition comprising DGLA further includes a therapeutically effective amount of benzoyl peroxide.

18. The method of claim 17 , wherein the pharmaceutical composition comprises about 1.25% to about 10 wt. % of benzoyl peroxide.

19. The method of claim 16 , wherein the step of administering comprises topically applying the composition to an area of the skin afflicted with acne lesions.

20. The method of claim 19 , wherein the area of the skin afflicted with acne lesions is first washed prior to application of the pharmaceutical composition.

21. The method of claim 19 , wherein the acne lesions are inflammatory type and/or non-inflammatory type lesions.

22. The method of claim 21 , wherein the composition reduces about 10%, 20%, 30%, 40%, 50% 50%, 70%, 80%, 90% or more of the acne lesions.

23. The method of claim 16 , wherein the acne is associated with Propionibacterium acnes.

24. The method of claim 16 , wherein the pharmaceutical composition is administered to the subject once a day, twice a day, or three times a day.

25. The method of claim 16 , wherein the pharmaceutical composition is a cream.

26. The method of claim 16 , wherein the subject previously exhibited acne lesions.

27. A method for improving antimicrobial activity of an agent used in the treatment of acne, the method comprising: adding a composition comprising one or more of 15-HEPE or 15-HETrE to the agent.

28. The method of claim 27 , wherein the composition comprises about 0.1 wt. % to about 20 wt. % of 15-HEPE or 15-HETrE.

29. A method for improving antimicrobial activity of an agent in the treatment of acne, the method comprising: adding a topically deliverable composition comprising one or more of DGLA, 15-HEPE, or 15-HETrE, wherein the composition further comprises about 1.65 wt. % steareth-2, about 1.35 wt. % steareth-21, about 0.5 wt. % cetyl alcohol, about 0.2 wt. % ascorbyl palmitate, about 0.15 wt. % a-tocopherol, about 2.0 wt. % medium-chain triglycerides, about 2.0 wt. % myristyl myristate, about 4.0 wt. % isopropryl palmitate, about 1.0 wt. % glycerin, about 1.0 wt. % phenoxyethanol, about 0.1 wt. % ascorbic acid, about 0.8 wt. % carbomer, about 0.4 wt. % xanthan gum, about 0.5 wt. % liquid soy lecithin, and about 0.05 wt. % Mild Care 345 fragrance.

30. The method of claim 29 , wherein the composition comprising DGLA further includes a therapeutically effective amount of benzoyl peroxide.

31. The method of claim 30 , wherein the composition comprises about 1.25 wt. % to about 10 wt. % of benzoyl peroxide.

32. The method of claim 28 , wherein the composition comprising 15-HEPE further includes a therapeutically effective amount of benzoyl peroxide.

33. The method of claim 32 , wherein the composition comprises about 1.25% to about 10 wt. % of benzoyl peroxide.

34. The method of claim 28 , wherein the composition comprising 15-HETrE further includes a therapeutically effective amount of adapalene.

35. The method of claim 34 , wherein the composition comprises about 0.05 wt. % to about 0.3 wt. % of adapalene.

36. A method of inhibiting Propionibacterium acnes , the method comprising: contacting Propionibacterium acnes with a pharmaceutical composition comprising 15-HEPE or 15-HETrE.

37. The method of claim 36 , wherein the pharmaceutical composition comprises about 0.1 wt. % to about 20 wt. % of 15-HEPE or 15-HETrE.

38. A method of inhibiting Propionibacterium acnes , the method comprising: contacting Propionibacterium acnes with a pharmaceutical composition comprising DGLA, 15-HEPE, or 15-HETrE, wherein the pharmaceutical composition further comprises about 1.65 wt. % steareth-2, about 1.35 wt. % steareth-21, about 0.5 wt. % cetyl alcohol, about 0.2 wt. % ascorbyl palmitate, about 0.15 wt. % a-tocopherol, about 2.0 wt. % medium-chain triglycerides, about 2.0 wt. % myristyl myristate, about 4.0 wt. % isopropryl palmitate, about 1.0 wt. % glycerin, about 1.0 wt. % phenoxyethanol, about 0.1 wt. % ascorbic acid, about 0.8 wt. % carbomer, about 0.4 wt. % xanthan gum, about 0.5 wt. % liquid soy lecithin, and about 0.05 wt. % Mild Care 345 fragrance.

39. The method of claim 38 , wherein the pharmaceutical composition comprising DGLA further includes a therapeutically effective amount of benzoyl peroxide.

40. The method of claim 39 , wherein the pharmaceutical composition comprises about 1.25% to about 10 wt. % of benzoyl peroxide.

41. The method of claim 37 , wherein the pharmaceutical composition comprising 15-HEPE further includes a therapeutically effective amount of benzoyl peroxide.

42. The method of claim 41 , wherein the pharmaceutical composition comprises about 1.25% to about 10 wt. % of benzoyl peroxide.

43. The method of claim 37 , wherein the pharmaceutical composition comprising 15-HETrE further includes a therapeutically effective amount of adapalene.

44. The method of claim 43 , wherein the pharmaceutical composition comprises about 0.05% to about 0.3 wt. % of adapalene.

Assignments (2)
CHANGE OF NAME Recorded Jul 31, 2017
From: DIGNITY SCIENCES LIMITED
To: DS BIOPHARMA LIMITED
Reel/Frame 043147/0143 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 4, 2012
From: MANKU, MEHAR; CLIMAX, JOHN; COUGHLAN, DAVID
To: DIGNITY SCIENCES LIMITED
Reel/Frame 029399/0222 →
Continuity (3)
Continuation 13478982 · May 23, 2012
Provisional Application 61549018 · Oct 19, 2011
Related Publication 20130102575A1 · Apr 25, 2013