Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/34—Alcohols
  • A61K8/347—Phenols
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
  • A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
  • A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/60—Sugars; Derivatives thereof
  • A61K8/602—Glycosides, e.g. rutin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
  • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
  • A61K8/9783—Angiosperms [Magnoliophyta]
  • A61K8/9789—Magnoliopsida [dicotyledons]
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/08—Anti-ageing preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
  • A61K2800/92—Oral administration

Definitions

• the present invention relates to a composition
• a composition comprising an extract of polygonum cuspidatum and a polyphenolic extract of red vitis vinifera.
• free radicals which may be endogenous (products of cellular metabolism or of external origin (high concentrations of oxygen, generators of radicals present in the environment, including smoke, sunlight and the like) and which are responsible for acute or chronic pathological conditions, such as, in particular, ageing, of an intrinsic nature (caused by the free radicals generated by the normal cellular oxidative metabolism, and of an extrinsic nature (produced by free radicals generated by environmental factors outside the organism) .
• the ageing process is in fact a natural phenomenon caused by the accumulation, in old cells, of altered molecules and organelles, said accumulation producing a consequent reduction of the metabolism and the functions of all the cells and all the tissues .
• This reduction is determined by the speed of said accumulation, which varies from person to person depending on the respective cellular defences, and increases with age, in all individuals, since the generation of free radicals increases with the number of altered mitochondria and peroxisomes which, in turn, increase with age, while the cellular defences decline.
• Stilbenes include resveratrol (trans-3 , 4 ' , 5- trihydroxystilbene) , a natural, non-flavonoid, polyphenolic antioxidant derived from many plants, including grapes, berries, peanuts and contained in wine, in particular red wine.
• the plants which contain resveratrol in high concentrations include also Polygonum Cuspidatum. ⁇ Rocha-Gonzalez HI, Ambriz-Tututi M, Granados-Soto V. Resveratrol: a natural compound with pharmacological potential in neurodegenerative diseases. CNS Neurosci Ther. 2008 Fall ; 14 (3): 234- 47. Epub 2008 Jul 29)
• Resveratrol is considered to be a promising natural bioactive molecule with phytotherapeutic and pharmacological potential (Shils ME, Shike M, Ross AC, Caballero B, Cousins RJ Modern Nutrition in Health and Disease, 10 th ed, p. 1796, Lippincott Williams & Wilkins, Baltimore, 2006) .
• Resveratrol has been the subject of many in vitro and in vivo investigations aimed at understanding biological activities, including anti-oxidant and anti-inflammatory, anti-aggregating, anti -atherogenous , phyto- estrogenous, cell-proliferation-inhibiting and immunomodulating activities (Pervaiz S, Holme AL. Resveratrol: Its Biological Targets and Functional Activity. Antioxid Redox Signal. 2009 May 11. [Epub ahead of print]). Resveratrol provides protection against diabetes (Subramanian S Resveratrol, a natural phytoalexin, normalizes hyperglycemia in streptozotocin-nicotinamide induced experimental diabetic rats. Bio ed Pharmacother.
• Resveratrol may also have cardioprotective and chemopreventive properties.
• resveratrol may in fact strengthen the death signals, depressing the redox proteins and strengthening the apoptotic proteins ⁇ Dudley J, Das S, Mukherjee S, Das DK.
• Resveratrol a unique phytoalexin present in red wine, delivers either survival signal or death signal to the ischemic myocardium depending on dose. J Nutr Biochem. 2009 Jun;20 (6) : 443 -52) .
• resveratrol is a phytoalexin, i.e. a defensive substance produced by plants in response to environmental stresses and pathogenic microorganism infections; in basic conditions resveratrol is absent or present in very low concentrations which may increase in a significantly rapid manner in the case of a more general defensive response (Zamboni A, Gatto P, Cestaro A, Pilati S, Viola R, Mattivi F, Moser C, Velasco R. Grapevine cell early activation of specific responses to DIMEB, a resveratrol elicitor BMC Genomics . 2009 Aug 6 / 10(1) :363. [Epub ahead of print]) ⁇ it follows that resveratrol is an additional defence which operates always in the presence of - and most probably in co-operation with - other defences which are always present in the cells.
• FR2867977 cosmetic, pharmaceutical and derrao- pharmaceutical compositions (not in the form of tablets) for combating wrinkles and skin lines, containing resveratrol (0.001-40%) in water- insoluble form or vegetable derivatives and extracts or mixtures thereof, which are active owing to the relaxing action of these compositions on the skin muscles.
• FR2923717 compositions containing derivatives obtained by means of alkylation of at least one stabilized phenolic function by means of esterification with mainly unsaturated fatty acids of polyphenols and stilbenes extracted from vitis vinifera or polygonum cuspidatum which are used for combating illnesses and ageing in human beings and in particular for cosmetic, dietary and therapeutic applications.
• WO2004/006881 cosmetic preparations in the form of a cream, ointment, emulsions, liposomes, gel, lotions and sprays which are able to clarify the skin and eliminate blemishes and which contain epsilon-viniferin optionally in combination with resveratrol and polyphenols in oligo or polymer form.
• WO2007/146318 describes fluid compositions containing trans-resveratrol and polyphenols able to provide users who cannot tolerate alcohol with beverages which are alcohol -free or have a low alcohol content and which contain trans -resveratirol and polyphenols in concentrations comparable to or greater than those of red wine in packaging able to protect the trans-resveratrol from oxidation by the oxygen in the atmosphere .
• the document also describes beverages containing trans-resveratrol in concentrations ranging from 5 to 300 mg/1 with or without stabilizers, vitamin A,. E and C, substances which absorb UV rays, one or more polyphenols, . proteins, minerals, tea, coffee and aromas .
• WO2008/114141 compositions capable of inhibiting 5 -alpha-reductase , containing a combination of omega- 6 fatty acids and rutin in concentrations ranging between 0.1 and 15%, in a suitable vehicle, useful for regulating nutrition of the hair bulbs and the production of sebum, formulated as a pharmaceutical, dietary or cosmetic product for treating hair loss.
• WO2009/53802 alimentary alcohol-free beverages for anti-ageing use, containing trans-resveratrol, citric acid, fructose, polyphenols extracted from black grape, extract of green tea, vitamin E, vitamin C and niacin, associated with edible-fruit juices ; US2004/02412261 (EP 1284133), products which exploit the effects of combinations in synergic proportions of the following natural anti -oxidants : a) polyphenols, in particular catechols; b) quercetin; c) resveratrol, able to develop a particularly active action as inhibitors of metalloproteinases .
• the preparations, in addition to the combination of pure substances, may be derived from the combination of extracts - of an aqueous or hydroalcoholic nature obtained via conventional techniques - of the following:
• the products may therefore contain up to 75% by weight of the mixture of the three extracts and contain quantities of resveratrol less than 5% by weight .
• XP-002593863 cosmeceutical products derived from grass and also extracts of grape seeds (vitis vinifera) and active principles contained therein, including resveratrol;
• XP-002593864 this deals with the protective action of many vegetable phenolic compounds against photo- ageing and UV-ray skin cancer, summarising the results achieved in- the sector up to 2003. More generally it describes the beneficial dermatological effects of grape seed extracts.
• the technical problem which is posed, therefore, is that of developing a composition which comprises resveratrol in combination with other components, able to produce a defensive action in the human body against cell and tissue ageing, without the negative consequences of an increase in the degenerative effects of ageing.
• composition according to the present invention comprises an extract of polygonum cuspidatum containing trans-resveratrol
• extract is understood as meaning a phyto-composite comprising all the components present in red vitis vinifera with their natural balance .
• extraction is performed using a hydroalcoholic method which does not introduce chemical molecules which are damaging for human health .
• This definition therefore includes polyphenols which are produced naturally (for example by means of extraction from red wine or red grape) , but not the polyphenols obtained synthetically.
• the hydrosoluble extract of polygonum cuspidatum has a content of trans-resveratrol of not less than 20%.
• the composition comprises trans-resveratrol added in an amount ranging between 0.1 and 5% by weight of the content of polyphenolic extract of red vitis vinifera.
• composition according to the present invention may also be associated with ubiquinol and/or ubiquinone and/or liposoluble vitamins with an anti -radical action such as vitamen E and vitamin F (Omega 3) which improve the absorption and stabilize and prolong the protective effects of the composition .
• ubiquinol and/or ubiquinone and/or liposoluble vitamins with an anti -radical action such as vitamen E and vitamin F (Omega 3) which improve the absorption and stabilize and prolong the protective effects of the composition .
• compositions may be associated with dolichol and/or with vegetable polyprenols from which dolichol may be synthesized, in order to improve protection of the skin against the acute and chronic damage produced by exposure to sunlight .
• composition according to the invention may be administered both systemically, preferably orally, and topically.
• said oral form may be formulated in the form of a capsule, coated or uncoated tablet, granular product or emulsion; the topical form may in turn be preferably formulated as a cream, gel or ointment .
• the preloading was carried out incubating the isolated liver cells (20 mg/ml) in 24 ml of solutions containing the polyphenols (RWP) in the final concentration of 0 , 50, 250 and 500 mg/100 ml for 10 minutes.
• RWP polyphenols
• the cells were centrifuged, separated from the supernatant and re-suspended in the final concentration of 6 mg/ml.
• Fig. 3 which shows the standard error ( ⁇ ) of the mean of 8 samples
• the MDA production values obtained, expressed in nmols/mg cells show that, in the presence of polyphenols of red wine, the resveratrol always has (both in low concentrations and in high concentrations) a significant capacity for protection against photo- lipoperoxidation .
• composition according to the invention is determined by the combination of complex natural extracts, naturally balanced both individually and in combination, without preliminary separation and recombination of the active components as indicated by the prior art.
• the choice of polygonum cuspidatum and vitis vinifera for obtaining the extracts according to the present invention provides a selection thereof such as to determine the special relative weight ratios of resveratrol , and complex polyphenols considered to be effective for the predefined aims, avoiding pretreatment and recombination which may give rise to alteration of the active components with a consequent reduction in their effectiveness.

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• Health & Medical Sciences (AREA)
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• General Health & Medical Sciences (AREA)
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• Public Health (AREA)
• Animal Behavior & Ethology (AREA)
• Epidemiology (AREA)
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• Emergency Medicine (AREA)
• Engineering & Computer Science (AREA)
• Biotechnology (AREA)
• Botany (AREA)
• Microbiology (AREA)
• Mycology (AREA)
• Gerontology & Geriatric Medicine (AREA)
• Dermatology (AREA)
• Medicines Containing Plant Substances (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Distillation Of Fermentation Liquor, Processing Of Alcohols, Vinegar And Beer (AREA)

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• 2009
  • 2009-11-05 IT IT001940A patent/ITMI20091940A1/it unknown
• 2010
  • 2010-11-04 EP EP10798587A patent/EP2496206A2/de not_active Ceased
  • 2010-11-04 WO PCT/IB2010/002812 patent/WO2011055222A2/en active Application Filing

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