Compositions comprising flavonoids and tocotrienols and methods thereof

• US 20060013901A1
• Filed: 05/24/2005
• Published: 01/19/2006
• Est. Priority Date: 05/26/2004
• Status: Abandoned Application

• Current Assignee: KGK Synergize Incorporated
• Original Assignee: KGK Synergize Incorporated
• Inventors: Guthrie, Najla
• Application Number:
  US11/135,693
• Publication Number:
  US 20060013901A1
• Time in Patent Office: Days
• US Class Current: 424/736
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/353 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
• CPC Class Codes: A61K 31/355 Tocopherols, e.g. vitamin E
• CPC Class Codes: A61K 31/7048 having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin , digitoxin or digoxin
• CPC Class Codes: A61K 36/752 Citrus, e.g. lime, orange or lemon
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 7/00 Drugs for disorders of the blood or the extracellular fluid
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

Disclosed in certain embodiments is a pharmaceutical formulation comprising a pharmaceutical ingredient comprising an active agent combination comprising flavonoids and tocotrienols in a ratio of about 75:25 to about 95:5 and at least one pharmaceutically acceptable excipient.

Claims

1. A pharmaceutical ingredient comprising an active agent combination comprising polymethoxylated flavonoids and tocotrienols in a ratio of about 75:

25 to about 95;

5, the pharmaceutical composition selected from the group consisting of an essence oil isolated from a citrus fruit, a peel oil isolated from a citrus fruit, a peel isolated from a citrus fruit, decharacterized citrus fruit, and combinations thereof.

2. The pharmaceutical ingredient according to claim 1, wherein the active agent combination comprises flavonoids and tocotrienols in a ratio of about 90:

10.

3. The pharmaceutical ingredient according to claim 1, wherein the active agent combination comprises flavonoids and tocotrienols in a ratio of about 80:

20.

4. The pharmaceutical ingredient according to claim 1, wherein the active agent combination comprises flavonoids and tocotrienols in a ratio of about 95:

5.

5. The pharmaceutical ingredient according to claim 1, comprising from about 50% to about 90% of the active agent combination.

6. The pharmaceutical ingredient according to claim 1, comprising from about 60% to about 80% of the active agent combination.

7. The pharmaceutical ingredient according to claim 1, comprising from about 70% of the active agent combination.

8. The pharmaceutical ingredient according to claim 1, wherein the flavonoid comprises a member consisting of naringenin, hesperetin, nobiletin, and tangeretin.

9. The pharmaceutical ingredient according to claim 1, wherein the tocotrienol is selected from the group consisting of alpha-tocotrienol, gamma-tocotrienol, and delta-tocotrienol.

10. A pharmaceutical formulation comprising a pharmaceutical ingredient comprising an active agent combination comprising flavonoids and tocotrienols in a ratio of about 75:

25 to about 95;

5 and at least one pharmaceutically acceptable excipient.

21. The pharmaceutical formulation according to claim 10, wherein the formulation lowers total cholesterol by at least 10%.

22. The pharmaceutical formulation according to claim 21, wherein the formulation lowers total cholesterol by at least 10% in a single patient.

23. The pharmaceutical formulation according to claim 21, wherein the formulation lowers total cholesterol by at least 10% in a patient population

30. The pharmaceutical formulation according to claim 10, wherein the formulation lowers triacylglycerols by at least 15%.

31. The pharmaceutical formulation according to claim 30, wherein the formulation lowers triacylglycerols by at least 15% in a single patient.

32. The pharmaceutical formulation according to claim 30, wherein the formulation lowers triacylglycerols by at least 15% in a patient population

39. The pharmaceutical formulation according to claim 10, wherein the formulation lowers LDL cholesterol by at least 10%.

40. The pharmaceutical formulation according to claim 39, wherein the formulation lowers LDL cholesterol by at least 10% in a single patient.

41. The pharmaceutical formulation according to claim 39, wherein the formulation lowers LDL cholesterol by at least 10% in a patient population

48. The pharmaceutical formulation according to claim 10, wherein the formulation lowers Apo B by at least 10%.

49. The pharmaceutical formulation according to claim 48, wherein the formulation lowers Apo B by at least 10% in a single patient.

50. The pharmaceutical formulation according to claim 48, wherein the formulation lowers Apo B by at least 10% in a patient population.

61. A method of treating a human subject at risk of or suffering from cardiovascular disease comprising administering an effective amount of a pharmaceutical formulation according to claim 10.

62. The method of claim 61, wherein the cardiovascular disease is hypercholesterolemia or atherosclerosis.

11-20. -20. (canceled)

24-29. -29. (canceled)

33-38. -38. (canceled)

42-47. -47. (canceled)

51-56. -56. (canceled)

57. A pharmaceutical formulation comprising a pharmaceutical ingredient comprising an active agent combination comprising flavonoids and tocotrienols and an additional active agent selected from the group consisting of soy protein, soy isoflavones, grapeseed extract, pine bark extract, gugulipids, policosinols, pantesine, niacin, alpha lipoic acid, tea flavins, coenzyme q10, lutein, statins, and combimations thereof.

58-60. -60. (canceled)

63-77. -77. (canceled)

78. A pharmaceutical formulation comprising a pharmaceutical ingredient comprising an active agent combination comprising flavonoids and tocotrienols and at least one pharmaceutically acceptable excipient, the formulation lowering total cholesterol by at least 10% after administration.

79-85. -85. (canceled)