IP Library Granted Patent US 9,301,936
Granted Patent B2
US 9,301,936 · App. 14/325,630 · Granted Apr 5, 2016

Pharmaceutical formulations of tranexamic acid and their use

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Quick Facts
Patent No.
US 9,301,936
App. No.
14/325,630
Granted
Apr 5, 2016
Kind
B2
Abstract

The present invention relates to pharmaceutical formulations comprising tranexamic acid, kits thereof, and methods for treating bleeding by local administration.

Claims (52)

1. A pharmaceutical composition consisting essentially of a therapeutically effective amount of:

(a) tranexamic acid;

(b) one or more antibiotic(s);

(c) optionally, one or more anesthetic(s);

(d) optionally, one or more non-steroid anti-inflammatory drug(s) selected from the group consisting of ketorolac, ketoprofen, flurbiprofen, bromfenac, diclofenac and combinations thereof; and

(e) an excipient or carrier that facilitates transdermal non-mucosal administration.

2. The pharmaceutical composition of claim 1 , wherein the therapeutically effective amount of tranexamic acid is between 1-70% by weight of the composition.

3. The pharmaceutical composition of claim 1 , wherein the one or more antibiotic(s) are selected from the group consisting of sulfacetamide, mupirocin, erythromycin, sulfadiazine, mafenide, tetracycline, bacitracin, neomycin, and polymyxin B.

4. The pharmaceutical composition of claim 1 , wherein the one or more antibiotic(s) are selected from the group consisting of bacitracin, neomycin, and polymyxin B.

5. The pharmaceutical composition of claim 1 , wherein the excipient or carrier permits the composition to remain in contact with a bleeding wound.

6. The pharmaceutical composition of claim 5 , wherein the excipient or carrier comprises an ointment, a cream, a liniment, a paste, a patch, a lotion, a gel, a shampoo, a hydrogel, a liposome, a spray, an aerosol, a solution, a sponge, a film, a plaster, a surgical dressing, a bandage, or an emulsion.

7. The pharmaceutical composition of claim 1 , wherein the one or more anesthetic(s) are selected from the group consisting of lidocaine, proparacaine, procaine, tetracaine and combinations thereof.

8. The pharmaceutical composition of claim 1 , wherein the transdermal non-mucosal composition is selected from the group consisting of an ointment, a gel, a liniment, a paste, a film, a hydrogel, a liposome, a cream, a patch, and a spray.

9. A method for treating bleeding in a subject in need thereof comprising transdermally non-mucosally administering to the subject a pharmaceutical composition of claim 1 .

10. The method of claim 9 , wherein the therapeutically effective amount of tranexamic acid is between 1-70% by weight of the composition.

11. The method of claim 9 , wherein the one or more antibiotics are selected from the group consisting of sulfacetamide, mupirocin, erythromycin, sulfadiazine, mafenide, tetracycline, bacitracin, neomycin, and polymyxin B.

12. The method of claim 9 , wherein the one or more antibiotics are bacitracin, neomycin, and/or polymyxin B.

13. The method of claim 9 , wherein an anticoagulant has been or is to be administered to the subject.

14. The method of claim 9 , wherein the excipient or carrier permits the composition to remain in contact with said bleeding wound.

15. The method of claim 14 , wherein the excipient or carrier comprises an ointment, a cream, a liniment, a paste, a patch, a lotion, a gel, a shampoo, a hydrogel, a liposome, a spray, an aerosol, a solution, a sponge, a film, a plaster, a surgical dressing, a bandage, or an emulsion.

16. The method of claim 9 , wherein the one or more anesthetic(s) are selected from the group consisting of lidocaine, proparacaine, procaine, tetracaine and combinations thereof.

17. The method of claim 9 , wherein the one or more non-steroid anti-inflammatory drug(s) are selected from the group consisting of ketorolac, ketoprofen, flurbiprofen, bromfenac, diclofenac and combinations thereof.

18. The method of claim 9 , wherein the transdermal non-mucosal composition is selected from the group consisting of an ointment, a gel, a liniment, a paste, a film, a hydrogel, a liposome, a cream, a patch and a spray.

19. A kit comprising:

the pharmaceutical composition of claim 1 ;

two or more containers for housing the composition; and

instructions for use.

20. A pharmaceutical composition consisting of a therapeutically effective amount of tranexamic acid and an excipient or carrier that facilitates transdermal non-mucosal administration.

21. The pharmaceutical composition of claim 20 , further comprising one or more antibiotics.

22. The pharmaceutical composition of claim 20 , wherein the therapeutically effective amount of tranexamic acid is between 1-70% by weight of the composition.

23. The pharmaceutical composition of claim 21 , wherein the one or more antibiotics are selected from the group consisting of sulfacetamide, mupirocin, erythromycin, sulfadiazine, mafenide, tetracycline, bacitracin, neomycin, and polymyxin B.

24. The pharmaceutical composition of claim 21 , wherein the one or more antibiotics are selected from the group consisting of bacitracin, neomycin, and polymyxin B.

25. The pharmaceutical composition of claim 20 , wherein the excipient or carrier permits the composition to remain in contact with a bleeding wound.

26. The pharmaceutical composition of claim 25 , wherein the excipient or carrier comprises an ointment, a cream, a liniment, a paste, a patch, a lotion, a gel, a shampoo, a hydrogel, a liposome, a spray, an aerosol, a solution, a sponge, a film, a plaster, a surgical dressing, a bandage, or an emulsion.

27. The pharmaceutical composition of claim 20 , wherein the composition is an ointment, a gel, a liniment, a paste, a film, a hydrogel, a liposome, a cream, a patch, or a spray.

28. A method for treating bleeding in a subject in need thereof comprising transdermally non-mucosally administering to the subject a pharmaceutical composition, wherein the composition consists of a therapeutically effective amount of tranexamic acid and an excipient or carrier that facilitates the transdermal non-mucosal administration.

29. The method of claim 28 , wherein the pharmaceutical composition further comprises one or more antibiotics.

30. The method of claim 28 , wherein the pharmaceutical composition consists essentially of a therapeutically effective amount of tranexamic acid, one or more antibiotics, and an excipient or carrier that facilitates transdermal non-mucosal administration.

31. The method of claim 28 , wherein the therapeutically effective amount of tranexamic acid is between 1-70% by weight of the composition.

32. The method of claim 29 , wherein the one or more antibiotics are selected from the group consisting of sulfacetamide, mupirocin, erythromycin, sulfadiazine, mafenide, tetracycline, bacitracin, neomycin, and polymyxin B.

33. The method of claim 29 , wherein the one or more antibiotics are bacitracin, neomycin, and/or polymyxin B.

34. The method of claim 28 , wherein an anticoagulant has been or is to be administered to the subject.

35. The method of claim 28 , wherein the excipient or carrier permits the composition to remain in contact with said bleeding wound.

36. The method of claim 35 , wherein the excipient or carrier comprises an ointment, a cream, a liniment, a paste, a patch, a lotion, a gel, a shampoo, a hydrogel, a liposome, a spray, an aerosol, a solution, a sponge, a film, a plaster, a surgical dressing, a bandage, or an emulsion.

37. The method of claim 28 , wherein the composition is an ointment, a gel, a liniment, a paste, a film, a hydrogel, a liposome, a cream, a patch, or a spray.

38. A kit comprising: a pharmaceutical composition comprising a therapeutically effective amount of tranexamic acid; an excipient or carrier that facilitates transdermal non-mucosal administration; two or more containers for housing the composition and the excipient or carrier; and instructions for use.

39. The pharmaceutical composition of claim 1 , consisting essentially of a therapeutically effective amount of:

(a) tranexamic acid;

(b) one or more antibiotic(s);

(c) one or more anesthetic(s);

(d) one or more non-steroid anti-inflammatory drug(s) selected from the group consisting of ketorolac, ketoprofen, flurbiprofen, bromfenac, diclofenac and combinations thereof; and

(e) an excipient or carrier that facilitates transdermal non-mucosal administration.

Assignments (10)
SECURITY INTEREST Recorded Sep 26, 2025
From: HARROW, INC.; HARROW IP, LLC
To: FIFTH THIRD BANK, NATIONAL ASSOCIATION, AS AGENT
Reel/Frame 072384/0781 →
RELEASE OF SECURITY INTEREST Recorded Sep 18, 2025
From: OAKTREE FUND ADMINISTRATION, LLC, AS ADMINISTRATIVE AGENT
To: HARROW IP, LLC
Reel/Frame 072299/0911 →
PATENT SECURITY AGREEMENT Recorded Mar 30, 2023
From: HARROW IP, LLC
To: OAKTREE FUND ADMINISTRATION, LLC, AS ADMINISTRATIVE AGENT
Reel/Frame 063205/0708 →
RELEASE OF SECURITY INTEREST Recorded May 7, 2021
From: SWK FUNDING LLC
To: HARROW IP, LLC
Reel/Frame 056174/0332 →
AMENDED AND RESTATED INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Nov 21, 2019
From: HARROW IP, LLC
To: SWK FUNDING LLC, AS COLLATERAL AGENT
Reel/Frame 051079/0453 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 12, 2019
From: IMPRIMIS PHARMACEUTICALS, INC.
To: HARROW IP, LLC
Reel/Frame 050985/0969 →
INTELLECTUAL PROPERTY SECURITY AGREEMENT Recorded Jul 19, 2017
From: IMPRIMIS PHARMACEUTICALS, INC.
To: SWK FUNDING LLC, AS COLLATERAL AGENT
Reel/Frame 043258/0581 →
RELEASE OF SECURITY INTEREST IN INTELLECTUAL PROPERTY COLLATERAL AT REEL/FRAME NO. 35923/0749 Recorded Jul 19, 2017
From: IMMY FUNDING LLC
To: IMPRIMIS PHARMACEUTICALS, INC.
Reel/Frame 043259/0434 →
SECURITY INTEREST Recorded Jun 16, 2015
From: IMPRIMIS PHARMACEUTICALS, INC.
To: IMMY FUNDING LLC
Reel/Frame 035923/0749 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 28, 2014
From: BUDERER, MATTHEW J.; ABRAMS, JEFFREY J.
To: IMPRIMIS PHARMACEUTICALS, INC.
Reel/Frame 033630/0620 →