Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Reexamination Certificate
1998-09-28
2001-06-05
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
C424S195110
Reexamination Certificate
active
06242005
ABSTRACT:
The present invention concerns the use of residual fractions of crushed grapes for preparing an absorbable prophylactic composition providing protection against ionising or non-ionising electromagnetic waves.
The production of free radicals and, in particular, of oxygenated free radicals is a normal physiological process at the cellular level not normally having deleterious consequences since the human organism is provided with protective systems: these protective systems are constituted either by enzymatic systems that trap oxygenated free radicals, such as SOD, or capable of decomposing secondary toxic products (H
2
O
2
) such as catalase, or by non-enzymatic systems such as vitamin E or glutathione.
It may happen, however, that the level of production of the oxygenated free radicals exceeds the capacities of the protective systems and they react with other molecules of the living cells, the consequences of which may be profound disturbances of the membranal integrity, the inactivation of many enzymatic systems, and profound modifications to the structure of the nucleic acids.
This hyper-production of oxygenated free radicals may result :
either from activation of endogenous mechanisms known to be generators of oxygenated free radicals, such as the energetic metabolism at the level of the respiratory chains or the activity of the macrophages particularly stimulated in the case of inflammation,
or from genesis induced by exogenous factors such as electromagnetic waves (ionising or non-ionising radiation) or hyper-oxygenation.
Among the mechanisms induced by excessive production of oxygenated free radicals, scientists are in agreement in considering that the most important is lipoperoxidation which corresponds to the degradation under the effect of radical reactions of the polyunsaturated fatty acids present in the phospholipids constituting the membranes of living cells; as a consequence, these molecular species are the privileged target of the radical attacks.
It has been possible to determine experimentally that under the effect of oxygenated free radicals, the molecules of polyunsaturated fatty acid tend to oxidise and to generate numerous degradation products, among which the most important are aldehydes, especially malondialdehyde. The consequence of this catabolism is a loss of the integrity and the stability of the polyunsaturated fatty acids, which manifests itself in a profound change in the cellular integrity.
It is generally accepted that these phenomena are involved in pathologies ass varied as rheumatoid polyarthritis, certain cancers, certain neuro-degenerative diseases (Alzheimers's, Parkinson's), cerebral and cardiac ischemias and, in general terms, ageing and cell death.
Besides the above-mentioned classic protective systems (SOD, catalase, vitamin E, . . .), it has been known for several years that certain flavonoids of vegetable origin are excellent at trapping free radicals. It has been possible to ascertain that in this group the most interesting appear to be the procyanidols or proanthocyanidines which correspond to hydrolysable tannins constituted by a glucidic molecule on which is esterified gallic acid or one of its derivatives and which are capable of liberating cyanidol by hydrolysis in an acid medium.
According to their degree of increasing polymerisation, the procyanidols are characterised by the following terms: monomers, dimers, trimers, tetramers, oligomers and condensates; among the monomers, the most common are epigallocatechin and epigallocatechin gallate. It has in fact been found that these compounds have a very high intrinsic efficacy and in particular are markedly more active than vitamin E.
Starting from this general knowledge, there has already been proposed, according to the publication JP-A-04/164 030, a prophylactic composition for protection against disorders linked to radioactivity—such as may occur for example in patients who are treated with radio-therapy, or in permanent operators of apparatus emitting radioactive radiation—capable of being absorbed orally and the active constituents of which are previously purified epigallocatechin or epigallocatechin gallate monomers. This Japanese publication indicates that this prophylactic composition may be constituted by a mixture of epigallocatechin and epigallocatechin gallate in a ratio of ⅓ obtained from leaves of green tea.
The preparation of this composition, however, has the drawback of requiring extraction and purification operations which are long and expensive, and therefore particularly inconvenient.
According to the invention, the idea was conceived of remedying these drawbacks by the use, for preparing an absorbable prophylactic composition providing protection against ionising or non-ionising radiation, not of a composition based on previously isolated constituents but of a crude extract of the residual fractions of crushed grapes, that is to say, of a product available in large quantities and therefore not difficult to obtain.
According to the invention, such a crude extract may contain pips and/or stalks and/or skins. It may also be obtained from residual press cakes from the manufacture of grapeseed oil.
It should be noted that in the course of wine-making operation the bunches of grapes are squashed, that is to say, partially crushed in order to liberate the must which contains approximately 80% juice and 20% solid matter essentially constituted by the pips, stalks and skins. This must is then transferred to a fermentation vat in which occur the different chemical reactions of maceration and fermentation which permit the transformation of the grape into wine. In the course of these reactions, part of the constituents initially contained in the solid matter diffuses into the juice. The residual solid matter is then separated from the juice then pressed so as to obtain a wine known as “press” wine, and a residue termed “marc”.
This residue may be distilled to produce brandy, or be used for animal feed.
Another outlet for more or less dried wine-making marcs corresponds to the manufacture of grapeseed oil by a pressing operation during the course of which the fatty part is separated from a press cake.
It should be noted that it has already been proposed to use by-products or wine-making for the preparation, after purification, of a medicament intended for the treatment of venous circulation problems: Endotelon®.
In spite of the various possibilities mentioned above, the major part of the wine-making marcs and of the press cakes from the manufacture of grapeseed oil is at present poorly exploited.
However, different earlier studies have made it possible to demonstrate that the grape pips present in these residues are particularly rich in procyanidols and contain, in particular, large amounts of epigallocatechin and epigallocatechin gallate which can be found in monomer form but also in dimer, trimer and oligomer form.
According to the invention, it has been ascertained that these procyanidols are also at least partially present in the above-mentioned by-products of wine-making, besides other constituents such as catechin, or even gallic acid or caffeic acid.
It has consequently been proposed to use a crude extract of all or parts of the residual fraction of crushed grapes for preparing an absorbable prophylactic composition providing protection against ionising or non-ionising electromagnetic waves.
It has been found that such a crude extract, surprisingly, has a markedly greater efficacy than that which epigallocatechin and epigallocatechin gallate which are isolated, or even associated with each other, have on the prevention of lipidic changes induced by radiation.
Taking into account the foregoing, the use according to the invention has the advantage of making it possible to derive value from the by-products of wine-making vines.
The invention also relates to an absorbable prophylactic composition providing protection against ionising or non-ionising electromagnetic waves.
According to the invention, this prophylactic composition is characterised in tha
Bouhamidi Rachid
Legrand Charles
Hughes Robert B.
Hughes & Schacht, PLLC
Page Thurman K.
Seidleck Brian K.
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