Methods for the treatment of peripheral neural and vascular ailments

• US 20040087516A1
• Filed: 11/06/2002
• Published: 05/06/2004
• Est. Priority Date: 11/06/2002
• Status: Active Grant

• Current Assignee: The Quigley Corporation
• Original Assignee: The Quigley Corporation
• Inventors: Rosenbloom, Richard A..
• Granted Patent: US 7,083,813 B2
• Time in Patent Office: Days
• US Class Current: 514/27
• CPC Class Codes: A61K 31/121 acyclic
• CPC Class Codes: A61K 31/352 condensed with carbocyclic rings, e.g. methantheline cannabinoids A61K31/658
• CPC Class Codes: A61K 31/353 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
• CPC Class Codes: A61K 31/7048 having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin , digitoxin or digoxin

Abstract

Compositions and methods for the treatment of peripheral neural and vascular ailments are disclosed. The method comprises administering a flavonoid compound with antioxidant properties, optionally formulated in a acceptable carrier. This compound or combination of compounds provides significant, effective relief of the symptoms of peripheral neural or vascular ailments. In addition, the compositions, when used according to the methods of the present invention, do not exhibit the severe side effects of many prior art compositions proposed for treatment of these ailments.

Claims

1. A method of treating peripheral neural and vascular ailments comprising the step of administering to a patient having a peripheral neural or vascular ailment a composition formulated from a therapeutically effective amount of a flavonoid having antioxidant properties;

and, optionally, an acceptable carrier.

2. The method of claim 1, wherein treating peripheral neural and vascular ailments comprises treating a systemic effect of the peripheral neural and vascular ailment.

3. The method of claim 1, wherein treating peripheral neural and vascular ailments comprises treating a local effect of the peripheral neural and vascular ailment.

4. The method of claim 1, wherein treating a peripheral neural and vascular ailment is selected from the group consisting of decreasing pain, decreasing tingling, normalizing sensitivity to heat or cold, decreasing cramping, decreasing muscle weakness, decreasing numbness, decreasing hair loss, promoting angiogenesis, regenerating damaged nerves, generating new nerves and improving peripheral circulation.

5. The method of claim 1, wherein the flavonoid having antioxidant properties is selected from the group consisting of (−

)-epigallocatechin;

(−

)-epigallocatechin-gallate;

1,2,3,6-tetra-o-gallyol-β

-d-glucose;

2′

o-acetylacetoside;

3,3′

,4-tri-o-methyl-ellagic acid;

6,3′

,4′

-trihydroxy-5,7,8-trimethoxyflavone;

6-hydroxy-luteolin;

6-hydroxykaempferol-3,6-dimethyl ether;

7-o-acetyl-8-epi-loganic acid;

acacetin;

acetoside;

acetyl trisulfate quercetin;

amentoflavone;

apigenin;

apiin;

astragalin;

avicularin;

axillarin;

baicalein;

brazilin;

brevifolin carboxylic acid;

caryophyllene;

catechin;

chrysin;

chrysin-5,7-dihydroxyflavone;

chrysoeriol;

chrysosplenol;

chrysosplenoside-a;

chrysosplenoside-d;

cosmosiin;

6-cadinene;

curcumin;

dihydroquercetin;

dimethylmussaenoside;

diacerylcirsimaritin;

diosmetin;

dosmetin;

ellagic acid;

ebinin;

epicatechin;

ethyl brevifolin carboxylate;

flavocannibiside;

flavosativaside;

genistein;

ginkgo flavone glycosides;

ginkgo heterosides;

gossypetin;

gossypetin-8-glucoside;

haematoxylin;

hesperidine;

hispiduloside;

hyperin;

indole;

iridine;

isoliquiritigenin;

isoliquiritin;

isoquercitrin;

jionoside;

juglanin;

kaempferol;

kaempferol-3-rhamnoside;

kaempferol-3-neohesperidoside;

kolaviron;

licuraside;

linariin;

linarin;

lonicerin;

luteolin;

luteolin-7-glucoside;

luteolin-7-glucoronide;

macrocarpal-a;

macrocarpal-b;

macrocarpal-d;

macrocarpal-g;

maniflavone;

morin;

methyl scutellarein;

myricetin;

naringenin;

naringin;

nelumboside;

nepetin;

nepetrin;

nerolidol;

oligomeric proanthocyanidins;

oxyayanin-a;

pectolinarigenin;

pectolinarin;

quercetagetin;

quercetin;

quercimertrin;

quercitrin;

quercitryl-2″

acetate;

reynoutrin;

rhamnetin;

rhoifolin;

rutin;

scutellarein;

sideritoflavone;

silibin;

silydianin;

silychristine;

silymarin;

sophoricoside;

sorbarin;

spiraeoside;

trifolin;

vitexin;

wogonin; and

a component of green tea; and

pharmaceutically acceptable salts thereof.

6. The method of claim 1, wherein the flavonoid having antioxidant properties is selected from the group consisting of (−

)-epigallocatechin-3-gallate, catechin, rutin, quercetin, quercitrin, myricetin, kaempferol, myrecetrin luteolin, morin, fisetin, silymarin, apigenin, hesperitin, citrin, gossypetin, chrysin, oligomeric proanthocyanidins, polyphenols, biacalein, curcumin, epicatechin, dihydroquercetin, ginkgo flavone glycosides, ginkgo heterosides, silibin, silydianin, silychristine, a component of green tea, and pharmaceutically acceptable salts thereof.

7. The method of claim 1, wherein the flavonoid having antioxidant properties is selected from the group consisting of quercetin, quercitrin, myricetin, rutin, kaempferol, myrecetrin, galangin, monoHER, diHER, triHER, tetraHER, naringenin, naringin, taxifolin, diosmin, phloretin, phloridzin, cyanidin, pelargonidin, a component of green tea, and pharmaceutically acceptable salts thereof.

8. The method of claim 1, wherein the flavonoid having antioxidant properties is selected from the group consisting of quercetin, quercitrin, myricetin, rutin, kaempferol, myrecetrin, a component of green tea, and pharmaceutically acceptable salts thereof.

9. The method of claim 1, wherein the flavonoid having antioxidant properties comprises a component of green tea.

10. The method of claim 1, wherein the composition is further formulated from a non-flavonoid antioxidant compound.

11. The method of claim 10, wherein the non-flavonoid antioxidant compound is selected from the group consisting of ascorbyl palmitate, ascorbic acid, vitamin A, vitamin E and its pharmaceutically acceptable esters, α

-lipoic acid, coenzyme Q10, glutathione, a polyphenol, a component of green tea, and pharmaceutically acceptable salts thereof.

12. The method of claim 10, wherein the non-flavonoid antioxidant compound comprises glutathione.

13. The method of claim 10, wherein the non-flavonoid antioxidant compound comprises a component of green tea.

14. The method as claimed in claim 1, wherein the composition is further formulated from vitamin D₃, 1,25-dihydroxyvitamin D₃, I(S), 3(R)-dihydroxy-20(R)-(1-ethoxy-5-ethyl-5-hydroxy-2-heptyn-1-yl)-9,10-seco-pregna-5(Z), 7(E), 10(19)-triene, or a pharmaceutically acceptable salt thereof.

15. The method as claimed in claim 1, wherein the acceptable carrier comprises a sufficient amount of a panthenol selected from D-panthenol and DL-panthenol to promote penetration of one or more compounds of the composition into the skin.

16. The method of claim 1, wherein administering comprises oral administration.

17. The method of claim 16, wherein treating peripheral neural and vascular ailments comprises at least one of maintaining and/or supporting neural health, maintaining and/or supporting vascular health, maintaining and/or supporting circulation, maintaining and/or supporting muscular health, maintaining sensory integrity and supporting the health of the skin.

18. The method as claimed in claim 1, wherein the acceptable carrier comprises a sufficient amount of at least one non-U.S.P. hydrophilic ointment base to form a substantially topical composition.

19. The method of claim 13, wherein treating a peripheral neural and vascular ailment is selected from the group consisting of reducing or preventing redness of skin, reducing or preventing discoloration of skin, beautifying skin, improving appearance of skin, promoting attractiveness of skin, cleansing skin, removing dead or damaged skin or skin cells from skin and moisturizing skin.

20. The method of claim 13, wherein the step of applying comprises rubbing, pouring, spraying or sprinkling.

21. The method of claim 18, wherein the composition comprises a moisturizer, DL-panthenol, quercetin, and a further antioxidant.

22. The method of claim 18, wherein the composition comprises a hydrophilic ointment base, 2 to 100 g of sodium L-pyrrolidone carboxylic acid per pound of the composition, 1 to 10 cc of DL-panthenol per pound of the composition, 10 g to 50 g of quercetin per pound of the composition, and 18 to 50 g of a compound selected from the group consisting of glutathione and rutin, per pound of the composition.

23. A method of treating diabetic neuropathy comprising the step of administering to a patient having diabetic neuropathy a composition consisting of a therapeutically effective amount of a flavonoid having antioxidant properties and a acceptable carrier.

25. The method of claim 23, wherein the flavonoid having antioxidant properties is selected from the group consisting of quercetin, quercitrin, myricetin, rutin, kaempferol, myrecetrin, galangin, monoHER, diHER, triHER, tetraHER, naringenin, naringin, taxifolin, diosmin, phloretin, phloridzin, cyanidin, pelargonidin and pharmaceutically acceptable salts thereof.

26. The method of claim 23, wherein the flavonoid having antioxidant properties is selected from the group consisting of quercetin, quercitrin, myricetin, rutin, kaempferol, myrecetrin, and pharmaceutically acceptable salts thereof.

27. The method of claim 23, wherein the composition further comprises a non-flavonoid antioxidant.

28. The method of claim 23 wherein the non-flavonoid antioxidant is selected from the group consisting of ascorbyl palmitate, ascorbic acid, vitamin A, vitamin E and its pharmaceutically acceptable esters, α

-lipoic acid, coenzyme Q10, glutathione, and pharmaceutically acceptable salts thereof.

29. The method of claim 23 wherein the acceptable carrier further comprises a moisturizer and DL-panthenol.

24. A method of treating diabetic neuropathy comprising the step of administering to a patient having diabetic neuropathy a composition comprising a therapeutically effective amount of a flavonoid having antioxidant properties;

and, optionally, a acceptable carrier;

with the proviso that said composition does not include vitamin D₃ or a vitamin D₃ analog.