Method and compositions for administering resveratrol and pterostilbene

a technology of resveratrol and pterostilbene, which is applied in the direction of drug compositions, chewing gum, dispersed delivery, etc., can solve the problems of resveratrol not being bioavailable, affecting the rate of sulfate conjugation, and unclear whether drugs reach the proposed site of action,

Inactive Publication Date: 2009-07-09
RUBIN DAVID +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it is not clear whether the drugs reach the proposed sites of action in vivo after oral administration, especially in humans.
However, the resveratrol is rapidly transformed in the liver to the glucurunide, which makes the resveratrol not bioavailable.
However, it is not clear if the drug reaches the proposed sites of action in vivo after oral ingestion, especially in humans.
Extremely rapid sulfate conjugation by the intestine / liver appears to be the rate-limiting step in the bioavailability of resveratrol and related compounds such as pterostilbene.

Method used

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Embodiment Construction

[0009]Significant reductions in cardiovascular disease risk have been associated with moderate consumption of alcoholic beverages (43). This “French Paradox”, the observation that mortality from coronary heart disease is relatively low in France despite relatively high levels of dietary saturated fat and cigarette smoking, suggested that the regular consumption of red wine could provide additional protection from cardiovascular disease (44, 45). Red wine contains resveratrol and even higher levels of flavonoids. These polyphenolic compounds have antioxidant, anti-inflammatory, and other potentially anti-atherogenic effects in the test tube and in some animal modes of atherosclerosis (46). Results of epidemiological studies addressing the value of these polyphenolic compound has been inconsistent. While some large prospective studies found that wine drinkers were at lower risk of cardiovascular disease than been or liquor drinkers (47-49), others fond no difference (50-52). Several s...

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Abstract

Resveratrol and/or pterostilbene are added to a chewable carrier, to enhance absorption of resveratrol and/or pterostilbene buccally or through the mucous membranes of the mouth. The composition containing the resveratrol and/or pterostilbene is designed to be retained in the mouth for at least 20 seconds and up to 20 minutes to ensure absorption of the resveratrol and/or pterostilbene through the mucous membranes of the mouth.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS [0001]The present application claims priority from provisional application 61 / 019,745, filed Jan. 8, 2008.FIELD OF THE INVENTION [0002]The present invention relates to methods and compositions for administering resveratrol and pterostilbene.BACKGROUND OF THE INVENTION [0003]Resveratrol and its analogs, pterostilbene (3,5-dimethoxy-4′-hydroxy-trans-stilbene), TMS (3,4′,5-reimwrhoxzy-trans-stilbene), 3,4′,4-DH-5-MS (3,4′-dihydroxy5-methoxy-trans-stilbnene) and 3,5-DH-4′MS(3,5-dihydroxy-4′-,ethoxy-trans-stilbene), have been shown to have chemopreventaive activity against cardiovascular disease and a variety of cancers in model systems. However, it is not clear whether the drugs reach the proposed sites of action in vivo after oral administration, especially in humans.[0004]Walle et al., in Drug Metabolism and Disposition 32: 1377-1382, 2004, examined the absorption, bioavailability and metabolism of 14C-resveratrol after oral and intravenous dose...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/68A61K31/047A61K31/09
CPCA23G3/364A23G3/48A23G4/068A23G4/12A61K31/09A61K9/0058A61K9/006A61K9/0095A61K31/047A61K9/0056A23K20/111A61P35/00C12G1/02C12G2200/21C12H1/14
Inventor RUBIN, DAVIDRUBIN, TAL
Owner RUBIN DAVID
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