Formulation of a mixture of free-B-ring flavonoids and flavans as a therapeutic agent

Patent metadata

Field	Value
Publication number	US-9370544-B2
Application number	US-201314078053-A
Country	US
Kind code	B2
Filing date	Nov 12, 2013
Priority date	Apr 30, 2002
Publication date	Jun 21, 2016
Grant date	Jun 21, 2016

Abstract

The present invention provides a novel composition of matter comprised of a mixture of two specific classes of compounds—Free-B-ring flavonoids and flavans—for use in the prevention and treatment of diseases and conditions mediated by the COX-2 and 5-LO pathways. The present invention further provides a novel method for simultaneously inhibiting the cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LO) enzymes, and reducing cox-2 mRNA production. Finally, the present invention includes a method for weight loss and blood glucose control. The methods of this invention are comprised of administering to a host in need thereof an effective amount of the composition of this invention together with a pharmaceutically acceptable carrier. This invention relates generally to the prevention and treatment of diseases and conditions mediated by the cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LO) pathways, including but not limited to the relief joint discomfort and pain associated with conditions such as osteoarthritis, rheumatoid arthritis, and other injuries that result from overuse.

First claim

The invention claimed is:

1. A capsule, tablet, pill, or microcapsule formulation for alleviating joint pain and/or joint stiffness in a human consisting essentially of a therapeutically effective amount of a combination of a Scutellaria extract, an Acacia extract, and a component selected from the group consisting of silica, boron, glucosamine sulfate, chondroitin sulfate, carboxymethylcellulose, copper gluconate, dextrose, saline, vitamin D, shark cartilage and bovine cartilage.

2. The formulation of claim 1 , wherein the Scutellaria extract is a partially purified Scutellaria extract enriched for Free-B-ring flavonoids containing baicalin.

3. The formulation of claim 1 , wherein the Acacia extract is a partially purified Acacia extract enriched for flavans containing catechin, epicatechin or both.

4. The formulation of claim 1 , wherein the Scutellaria extract is a partially purified Scutellaria extract enriched for Free-B-ring flavonoids containing baicalin, and the Acacia extract is a partially purified Acacia extract enriched for flavans containing catechin, epicatechin or both.

5. The formulation of claim 1 , wherein the Scutellaria extract is from a Scutellaria plant species selected from Scutellaria baicalensis, Scutellaria orthocalyx , or both.

6. The formulation of claim 1 , wherein the Acacia extract is from an Acacia plant species selected from Acacia catechu, Acacia concinna, Acacia farnesiana, Acacia Senegal, Acacia speciosa, Acacia arabica, Acacia caesia, Acacia pennata, Acacia sinuata, Acacia mearnsii, Acacia picnantha, Acacia dealbata, Acacia auriculiformis, Acacia holoserecia, Acacia mangium , or a combination thereof.

7. The formulation of claim 1 , wherein the Scutellaria extract is from Scutellaria baicalensis and the Acacia extract is from Acacia catechu.

8. The formulation of claim 1 , wherein the partially purified Scutellaria extract enriched for Free-B-ring flavonoids is from Scutellaria baicalensis and the partially purified Acacia extract enriched for flavans is from Acacia catechu.

9. The formulation of claim 1 , wherein the Scutellaria extract and the Acacia extract are each from a plant part selected from the group consisting of stems, stem barks, trunks, trunk barks, twigs, tubers, roots, root barks, young shoots, seeds, rhizomes, flowers, leaves, and any combination thereof.

10. The formulation of claim 4 , wherein the ratio of Free-B-ring flavonoids to flavans in the formulation ranges from about 90:10 to about 10:90.

11. The formulation of claim 8 , wherein the ratio of Free-B-ring flavonoids to flavans in the formulation ranges from about 90:10 to about 10:90.

12. The formulation of claim 4 , wherein the ratio of Free-B-ring flavonoids to flavans in the formulation ranges from about 85:15 to about 20:80.

13. The formulation of claim 4 , wherein the ratio of Free-B-ring flavonoid to flavans in the formulation is about 85:15.

14. The formulation of claim 4 , wherein at least 80% of the total weight of the formulation is Free-B-ring flavonoids and flavans.

15. The formulation of claim 4 , wherein the Free-B-ring flavonoids are major active components of the formulation.

16. The formulation of claim 4 , wherein the flavans are major active components of the formulation.

17. The formulation of claim 4 , wherein the Free-B-ring flavonoids and the flavans are major active components of the formulation.

18. The formulation of claim 8 , wherein the Free-B-ring flavonoids and the flavans are major active components of the formulation.

19. The formulation of claim 4 , wherein baicalin, catechin or both are major active ingredients of the formulation.

20. The formulation of claim 4 , wherein the formulation is a capsule.

Assignees

• Unigen Inc

Inventors

• Jia Qi

Classifications

• A61P9/10

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• A61P37/02

  Immunomodulators · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title