Combination of carnitines and resveratrol for prevention or...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai

Reexamination Certificate

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C514S025000, C514S470000, C514S556000, C514S733000, C514S822000, C560S196000, C562S567000

Reexamination Certificate

active

06515020

ABSTRACT:

The present invention relates to a new use of a combination composition of L-carnitine or an alkanoyl L-carnitine and a trihydroxy or tetrahydroxystilbene for the preventive or therapeutic treatment of cerebral disorders brought about by ageing and use of neurotoxic drugs.
Accordingly, the composition may take the form and exert the action of a dietary supplement or of an actual medicine, depending upon the support or preventive action, or the strictly therapeutic action, which the composition is intended to exert in relation to the particular individuals it is to be used in.
The use of the combination of (A) L-carnitine or alkanoyl L-carnitine in which the straight or branched-chain alkanoyl group contains 2-8 carbon atoms, or a pharmacologically acceptable salt thereof and (B) a trihydroxy or tetrahydroxystilbene, typically resveratrol, in the prevention and therapeutic treatment of a number of different pathologies is already known. U.S. Pat. No. 5,747,536, in fact, describes the use of the aforesaid combination for the prevention and treatment of diabetic neuropathy and atheroslerotic lesions and for the inhibition of platelet aggregation.
The use according to the present invention is in no way related to or deducible from such already known use.
In its broader aspect, the present invention relates to the coordinated use of L-carnitine or alkanoyl L-carnitine or their pharmacologically acceptable salts and of a trihydroxy or tetrahydroxystilbene for the prevention or treatment of the above-mentioned pathologies, where what is meant by the “coordinated use” of these active ingredients is indifferently either their co-administration, i.e. the practically simultaneous administration of L-carnitine or alkanoyl L-carnitine or their pharmacologically acceptable salts and trihydroxy- or tetrahydroxystilbene, or the administration of a composition containing a mixture of said active ingredients.
Here below, for the sake of brevity and simplicity of presentation, reference will be made only to L-carnitine, it being understood that the description also applies to the above-mentioned alkanoyl L-carnitines and their pharmacologically acceptable salts. Equally, here below, reference will be made only to resveratrol (trans-3,4′,5-trihydroxy-stilbene), it being understood, however, that the description applies not only to cis-resveratrol and to the respective trans- and cis-glycosides, but also to the trihydroxy- and tetrahydroxystilbenes in general.
Resveratrol is to be found in grapes and in particular in grape skins, seeds, stalks and vine leaves, particularly of
Vitis vinifera, Vitis rotundifolia
and
Vitis labrusca
and, obviously, in the wines obtained from their grapes and in the extracts and powders of the above-mentioned natural products. Resveratrol is also present in the roots of a number of species of the
Polygonum
genus (
Polygonaceae
family), such as
Polygonum cuspidatum
and
Polygonum multiflorum.
For the purposes of the present invention, what is meant by “resveratrol” is both trans-3,4′-5-trihydroxystilbene (i.e. resveratrol proper) and the cis isomer, the respective glycosides and extracts and powders containing resveratrol obtained from any suitable plant species.
The natural polyphenols present in grapes and wine have recently claimed the attention of numerous groups of researchers following epidemiological studies which have demonstrated that populations which consume moderate amounts of wine in their habitual diet present a much lower percentage of cardiovascular accidents than do populations whose dietary habits do not include the consumption of wine. Among the various polyphenols studied, resveratrol has proved to be the most interesting in that it is capable of exerting a significant action against platelet aggregation as well as a significant anti-inflammatory and vasoprotective action.
Another aspect of resveratrol and the polyphenols present in wine is that related to the significant reduction in the incidence of pre-senile and senile dementia which moderate consumption of wine is capable of inducing, particularly in the elderly population. A recent epidemiological study conducted in a large population has confirmed what a similar previous study had already indicated with regard to the mortality due to cerebral stroke, which is lower in moderate wine drinkers than in non-drinking subjects.
As regards the already known therapeutic uses of L-carnitine, this substance is used for example in the cardiovascular field for the treatment of acute and chronic myocardial ischaemia, angina pectoris, heart failure and cardiac arrhythmias and for peripheral vasculo-pathies. In the nephrological field, L-carnitine is administered to chronic uraemic patients undergoing regular haemodialytic treatment to combat muscular asthenia and the onset of muscle cramps. Other therapeutic uses relate to the normalisation of the HDL/LDL+VLDL ratio and total parenteral nutrition. The use of L-carnitine is also known in the treatment of certain myopathies and muscular dystrophies.
It has now been found surprisingly that a composition containing a combination of the following as its characterising components:
(A) L-carnitine or an alkanoyl L-carnitine wherein the alkanoyl is a straight or branched-chain alkanoyl group containing 2-8 carbon atoms, or a pharmacologically acceptable salt thereof; and
(B) a trihydroxy or tetrahydroxystilbene is extremely effective in the prevention and/or therapeutic treatment of cerebral disorders caused by ageing or by the use of neurotoxic drugs, as a result of the potent synergistic effect exerted by its components.
Therefore, the present invention relates to the use of (A) L-carnitine or an alkanoyl L-carnitine wherein the alkanoyl is a straight or branched-chain group containinig 2-8 carbon atoms, or a pharmacologically acceptable salt thereof, and (B) a trihydroxy or tetrahydroxystilbene to prepare a pharmaceutical product in which (A) and (B) are admixed together or separately packaged for the prevention and treatment of disease forms related to neuronal or cerebral disorders. That the active ingredients (A) and (B) can be admixed together or separately packaged is consistent with what has been said above with regard to the “co-ordinated use” of said ingredients.
Preferably, the alkanoyl group contains 2-6 carbon atoms and, even more preferably, is selected from the group consisting of acetyl, propionyl, butyryl, valeryl and isovaleryl L-carnitine.
Component (B) is preferably 3,4′,5-trihydroxystilbene (resveratrol) or 3,4′,5-trihydroxy-3-&bgr;-mono-D-glucoside or one of their pharmacologically acceptable salts. The resveratrol can be the synthetically prepared form or can be the form extracted from
Vitis vinifera, Vitis rotundifolia, Vitis labrusca
or from the roots of
Polygonum cuspidatum
or
Polygonum multiflorum.
Component (B) can also consist in extracts or powders of natural products containing resveratrol, such as extracts or powders of grape skins, seeds or stalks of
Vitis vinifera, Vitis rotundifolia, Vitis labrusca
or from the roots of
Polygonum cuspidatum
or
Polygonum multiflorum.
The (B):(A) weight-to-weight ratio ranges from 1:1 to 1;1,000, and preferably from 1:1 to 1:500.
The cerebral disorders caused by ageing prophylactically and therapeutically treated according to the present invention include particularly cerebral stroke, pre-senile and senile dementia and Alzheimer's disease.
An example of a neurotoxic drug against the effects of which the “co-ordinated” use according to the invention proves potently effective is cisplatin.
The unexpected synergism exerted by components (A) and (B) at cerebral nerve level is demonstrated by the results obtained with experimental models well recognised as being indicative of a protective action at central nervous system level and as being predictive of the effective use of the combination to combat cerebral nerve abnormalities in human subjects.
Toxicology
Tests conducted both in mice and in rats, administering combinations of high doses both of L-

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