Rhamnan sulphate composition for treatment of endothelial dysfunction

• US 20040116377A1
• Filed: 12/16/2002
• Published: 06/17/2004
• Est. Priority Date: 12/16/2002
• Status: Active Grant

• Current Assignee: Bruce A. Daniels, Endomatrix, Inc.
• Original Assignee: Endomatrix, Inc.
• Inventors: Daniels, Bruce Alan
• Granted Patent: US 6,797,705 B2
• Time in Patent Office: Days
• US Class Current: 514/54
• CPC Class Codes: A61K 31/715 Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
• CPC Class Codes: A61K 31/727 Heparin; Heparan

Abstract

The invention described is a method and composition for inducing cell surface anti-thrombotic activity in endothelial cells comprising administering to a patient a therapeutically-effective amount of Rhamnan Sulphate. The dose of Rhamnan Sulphate is equivalent to between approximately 8,000 IU and 12,000 IU of heparin activity daily on variable schedule or optionally at single dosage of 7.5 mg/kg, that is repeated on a daily basis as needed, to lower the incidence of thrombus formation or to lower the incidence of hard clot formation.

Claims

1. A method for treatment of the mammalian cellular environment for the prevention of endothelial dysfunction comprising the step of administering to a patient a therapeutically-effective amount of Rhamnan Sulphate, or its physiologically acceptable salts, in therapeutic proportions.

2. The method of claim 1 wherein the anticoagulation activity in the blood plasma of a patient is not appreciably increased.

3. The method of claim 1 wherein the Rhamnan Sulphate is extracted from algae.

4. The method of claim 1 wherein the dose of Rhamnan Sulphate is equivalent to between approximately 2,000 IU and 200,000 IU of heparin activity on a daily basis.

5. The method of claim 1 wherein the dose of Rhamnan Sulphate is equivalent to between approximately 5,000 IU and 20,000 IU of heparin activity on a daily basis.

6. The method of claim 1 wherein the dose of Rhamnan Sulphate is equivalent to between approximately 8,000 IU and 12,000 IU of heparin activity on a daily basis.

7. The method of claim 1 wherein the dose of Rhamnan Sulphate is approximately 7.5 mg/kg as a single dose.

8. The method of claim 1 wherein the dose of Rhamnan Sulphate is repeated daily to prevent the incidence of thrombosis.

9. The method of claim 1 wherein the dose of Rhamnan Sulphate is repeated daily to prevent the incidence of hard clots.

10. The method of claim 1 wherein Rhamnan Sulphate is substituted for by its functional analogs.

11. The method of claim 1 further comprising the co-administration of L-Arginine.

12. The method of claim 1 wherein the endothelial dysfunction is cardiovascular disease.

13. The method of claim 1 wherein the endothelial dysfunction is atherosclerosis.

14. The method of claim 1 wherein the endothelial dysfunction is arteriosclerosis.

15. A method of inducing cell surface anti-thrombotic activity in endothelial cells comprising the step of administering to a patient a therapeutically-effective amount of Rhamnan Sulphate, or its physiologically acceptable salts, in therapeutic proportions.

16. The method of claim 15 wherein the anticoagulation activity in the blood plasma of a patient is not appreciably increased.

17. The method of claim 15 wherein the dose of Rhamnan Sulphate is equivalent to between approximately 2,000 IU and 200,000 IU of heparin activity daily.

18. The method of claim 15 wherein the dose of Rhamnan Sulphate is equivalent to between approximately 5,000 IU and 20,000 IU of heparin activity daily.

19. The method of claim 15 wherein the dose of Rhamnan Sulphate is equivalent to between approximately 8,000 IU and 12,000 IU of heparin activity daily.

20. The method of claim 15 wherein Rhamnan Sulphate is substituted for by its functional analogs.

21. The method of claim 15 wherein the dose of Rhamnan Sulphate is repeated daily to prevent the incidence of thrombosis.

22. The method of claim 15 wherein the dose of Rhamnan Sulphate is repeated daily to prevent the incidence of hard clots.

23. The method of claim 15 further comprising the co-administration of L-Arginine.

24. A composition for treatment of the mammalian cellular environment for the prevention of endothelial dysfunction comprising of Rhamnan Sulphate other than normally ingested as food, or its functional analog or its physiologically acceptable salts, in therapeutic proportions.

25. The composition of claim 24 wherein the anticoagulation activity in the blood plasma of a patient is not appreciably increased.

26. The composition of claim 24 wherein the Rhamnan Sulphate is extracted from algae.

27. The composition of claim 24 wherein the disease is cardiovascular disease.

28. The composition of claim 24 wherein the disease is atherosclerosis.

29. The composition of claim 24 wherein the disease is arteriosclerosis.

30. The composition of claim 24 wherein the dose of Rhamnan Sulphate is repeated daily to prevent the incidence of thrombosis.

31. The composition of claim 24 wherein the dose of Rhamnan Sulphate is repeated daily to prevent the incidence of hard clots.

32. The composition of claim 24 further comprising L-Arginine.

33. The composition of claim 32 wherein the Rhamnan Sulphate and L-Arginine are formed into a Rhamnan Sulphate-L-Arginine complex.

34. A composition for inducing cell surface anti-thrombin activity in endothelial cells for treatment of cardiovascular disease without increasing the risk of hemorrhaging in patients, comprising a therapeutically-effective amount of Rhamnan Sulphate, or its physiologically acceptable salts, in therapeutic proportions.

35. The composition of claim 34 comprising a mixture of functional analogs or physiologically acceptable salts of Rhamnan Sulphate.

36. The composition of claim 34 wherein the dose of Rhamnan Sulphate is equivalent to between approximately 2,000 IU and 200,000 IU of heparin activity on a daily basis.

37. The composition of claim 34 wherein the dose of Rhamnan Sulphate is equivalent to between approximately 5,000 IU and 20,000 IU of heparin activity on a daily basis.

38. The composition of claim 34 wherein the dose of Rhamnan Sulphate is equivalent to between approximately 8,000 IU and 12,000 IU of heparin activity on a daily basis.

39. The composition of claim 34 wherein the dose of Rhamnan Sulphate is repeated daily to prevent the incidence of thrombosis.

40. The composition of claim 34 wherein the dose of Rhamnan Sulphate is repeated daily to prevent the incidence of hard clots.

41. The composition of claim 34 wherein Rhamnan Sulphate is substituted for by its functional analogs.

42. The composition of claim 34 further comprising L-Arginine.

43. The composition of claim 42 wherein the Rhamnan Sulphate and L-Arginine are formed into a Rhamnan Sulphate-L-Arginine complex.

44. A composition for inducing surface anti-thrombotic activity in endothelial cells for treatment of cardiovascular disease associated with endothelial dysfunction, without increasing the risk of hemorrhaging in patients, comprising the step of oral administration to a patient a therapeutically-effective amount of Rhamnan Sulphate, or its physiologically acceptable salts.