Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/31—Brassicaceae or Cruciferae (Mustard family), e.g. broccoli, cabbage or kohlrabi
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/01—Hydrocarbons
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
  • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
  • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• • 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
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P39/00—General protective or antinoxious agents
  • A61P39/04—Chelating agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
• • 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

Definitions

• the present invention relates to compositions, in particular for dietetic purposes (food supplement), cosmetic or medical, based on natural products, that is to say products found in plants or extracts of such plants.
• pectins have long been used as gelling agents or thickeners in the food industry. Furthermore, we now know that pectins are capable of binding heavy metals and their radionuclides and ensuring their excretion out of the body.
• Carotenoids are also known and used for their pigmentary and antioxidant (anti-free radical) properties in the field of sun creams and cosmetic supplements (capsules, for example). Mention may be made of alpha- and beta-carotenes and lycopene, the most powerful of these compounds, which is extracted from tomatoes (tomato oleoresin).
• GB-B-1 041 890 describes emulsions which can be used in human medicine, for example as a vehicle for the administration of medicinal substances via food.
• These emulsions can comprise on the one hand a substance such as a fat-soluble vitamin, a fat-soluble derivative of a water-soluble vitamin, a carotenoid or their mixtures, and on the other hand a nonionic emulsifier and an ionic wetting agent, the aqueous phase.
• a hydrocolloid such as pectin.
• SU-A-1 786 531 describes a drink produced from the juice of several fruits and which can therefore contain, among other things, carotene and pectin.
• pectins can be very advantageously combined with carotenoids, in particular lycopene, or with broccoli or broccoli extracts. , and preferably to these two types of compounds, and that this combination allowed the different compounds to perform their above functions (fixation and elimination of heavy metals, antioxidant and anti-radical action and beneficial action on cell regeneration ) under more favorable conditions than when they are alone.
• the pectins favor the availability and the transport of the associated compounds, so that the individual efficacy of the various compounds is thereby increased.
• the combination administered orally allows better transport and better bioavailability of the associated compounds (carotenoid and / or broccoli or extract).
• the association acts synergistically on the aggressions against the cells of the epidermis by pollution and solar rays.
• the present invention therefore relates to a composition, in particular for dietetic, medical or cosmetic purposes, comprising at least one heteropolysaccharide, preferably esterified, in particular a polygalacturonic acid or ester, preferably a pectin, and a compound chosen from the group consisting of carotenoids, preferably lycopene, and glucosinolate and / or sulphoraphane, in particular plant extract, in particular from cruciferous plants, preferably broccoli, containing them, and mixtures thereof.
• a heteropolysaccharide preferably esterified, in particular a polygalacturonic acid or ester, preferably a pectin
• a compound chosen from the group consisting of carotenoids, preferably lycopene, and glucosinolate and / or sulphoraphane in particular plant extract, in particular from cruciferous plants, preferably broccoli, containing them, and mixtures thereof.
• compositions according to the invention have an excellent preventive action with respect to the action of pollutants such as in particular heavy metals (in particular mercury, lead, arsenic, cadmium) and their radionucleides.
• pollutants such as in particular heavy metals (in particular mercury, lead, arsenic, cadmium) and their radionucleides.
• In vitro tests have in particular demonstrated a protective effect with respect to metals such as arsenic and cadmium which can exceed 80% and reach 100%.
• In vivo tests in rats have also demonstrated a very high protective and preventive protective effect against mercury.
• the composition comprises the three types of compounds.
• the invention extends, with respect to pectin functionality, to heteropolysaccharides, preferably esterified to various degrees, to mixtures of such compounds, for example of various degrees of esterification, and among these heteropolysaccharides, preferably polygalacturonic acids and their esters to which pectins belong.
• heteropolysaccharides preferably polygalacturonic acids and their esters to which pectins belong.
• they are methyl, ethyl or propyl esters.
• the essential compounds are glucosinolates, found in particular in crucifers, and capable of transforming into sulphoraphanes.
• the invention therefore extends to the use of glucosinolates and sulphoraphanes, of extraction or of synthesis, including produced by microorganisms, as well as to plants or plant extracts containing them, in particular cruciferous or extracts of cruciferous, preferably broccoli or broccoli extract.
• Carotenoids and their derivatives can be used. We will prefer lycopene.
• compositions according to the invention can comprise at least one plant extract including at least one of the compounds chosen from the heteropolysaccharide, carotenoid, glucosinolate and / or sulphoraphane group. These compositions can therefore be formed, with regard to the compounds of the invention, partially or exclusively of plant extracts.
• compositions according to the invention are preferably in the following forms: - for a therapeutic or non-therapeutic application, eg dietetic, preferably by oral route: in liquid or dry form or any other intermediate form comprising all extractable forms of said components: fluid extract, lyophilisate, atomiser, plant powder; formulated for example in capsules, drinks, tablets, etc. - for a cosmetic application: topical or transcutaneous route, for epidermal distribution, or oral application.
• a therapeutic or non-therapeutic application eg dietetic, preferably by oral route: in liquid or dry form or any other intermediate form comprising all extractable forms of said components: fluid extract, lyophilisate, atomiser, plant powder; formulated for example in capsules, drinks, tablets, etc.
• - for a cosmetic application topical or transcutaneous route, for epidermal distribution, or oral application.
• compositions advantageously comprise in%:
• an extract containing glucosinolate and / or sulphorophane e.g. broccoli extract (such an extract contains from 2000 to 5000 ppm / kg).
• extract containing carotenoid e.g. lycopene, (such an extract contains from 3 to 6% of carotenoid)
• extract containing carotenoid e.g. lycopene, (such an extract contains from 3 to 6% of carotenoid)
• extract containing glucosinolate and / or sulphorophane e.g. broccoli extract (such an extract contains from 2000 to 5000 ppm / kg).
• the present invention is intended to apply to both the therapeutic and non-therapeutic fields according to the regulations in force, methods of use and doses administered. It can in particular be used in the non-therapeutic field both in cosmetics and in dietetics, the objective then being essentially preventive and the use left to the free choice of the user.
• dietary compositions in particular based exclusively or partially on plant extracts, or in the cosmetic field in the form of ointments and analogues applied to the skin, or in the form of oral hygiene products. , such as toothpaste, dental solution, etc.
• compositions may be used in curative treatment, for example in the event of intoxication with heavy metals, or also as a preventive measure in a medical context in subjects at risk, such as people working in contact with heavy metals ( eg in the paint industry) or in nuclear power plants.
• the present invention therefore also relates to the use of the compositions according to the invention, preferably tri-components, for the preparation of a medicament, for example a medicament intended for trapping heavy metals, in particular lead, mercury, cadmium. , nickel and their radionucleides, especially mercury.
• a medicament for example a medicament intended for trapping heavy metals, in particular lead, mercury, cadmium. , nickel and their radionucleides, especially mercury.
• a subject of the invention is therefore also such a medicament, eg intended for trapping heavy metals and their radionucleides, in particular mercury, comprising a composition according to the invention, preferably tri-components, and a pharmaceutically acceptable excipient, in particular for a oral administration, this pharmaceutical excipient being able to be any usual excipient, in particular solid or liquid, preferably adapted for an oral administration. It may in particular be granules, or any other solid or liquid form, comprising from 15 to 40%, in particular from 20 to 30%, eg 25% of bi- or tri-component composition as described above, and a QSP100 excipient.
• the subject of the invention is also a method of therapeutic, curative or preventive treatment, preferably curative, in particular intended to trap the heavy metals and their radionucleides, comprising the administration of such a drug.
• the medicament may be administered in particular at a rate of 8 to 30 g of two- or three-component composition per day, preferably from 15 to 25 g / day.
• a subject of the invention is also the use of the compositions according to the invention for the preparation of external cosmetic preparations, in particular for their antioxidant and anti-radical action as well as their beneficial action on cell regeneration.
• an external cosmetic preparation comprising a composition according to the invention and an appropriate cosmetic excipient in particular suitable for topical application, in particular in the form of a lotion, ointment, body cream, etc.
• compositions according to the invention for the preparation of cosmetic products for oral hygiene, in particular mouthwashes, toothpastes, dental solutions or gels, in particular for trapping heavy metals, in particular the mercury contained in dental amalgams.
• compositions according to the invention are also relates to these cosmetic oral hygiene products comprising a composition according to the invention and the usual excipients of the type of product concerned (e.g. mouthwash, toothpaste, dental gel or solution).
• excipients of the type of product concerned e.g. mouthwash, toothpaste, dental gel or solution.
• the incorporation of the compositions according to the invention, as associated active ingredient, in oral hygiene products also comes within the scope of the present invention.
• a subject of the invention is also the use of the compositions according to the invention for the preparation of dietetic products, in particular food supplements, for all the beneficial actions which have been mentioned above and these products will then preferably be in the form oral compositions, liquids or solids.
• the dietetic use essentially aims to take advantage of the preventive properties of the compositions according to the invention, eg with respect to heavy metals and their radionucleides, and antioxidant and anti-radical action.
• the invention therefore also relates to dietetic products comprising a composition according to the invention and optionally an excipient suitable for administration by the oral route.
• the incorporation of the compositions according to the invention, as associated active principle, in dietetic products, in particular food supplements also comes within the scope of the invention. It also relates to the method consisting in administering, in particular orally, to humans, such a dietetic product.
• the dietetic products are administered orally at a rate of less than 8 g / d, eg from 1.5 to 6 g, in particular from 1.5 to 3.5 g, of bi-or tri-component composition, preferably based essentially on plant extracts as seen above, per day, in particular divided into several daily intakes. For example, take 3 to 6 capsules of 300 to 400 mg per day, the daily dose can be increased to 15 capsules.
• the cosmetic products are applied to the area to be treated at a rate of 10 to 100 mg per application, in particular at a rate of 2 to 3 applications per day.
• the network-forming properties of heteropolysaccharides and in particular pectins can be used in other combinations of active compounds to promote their bioavailability and their transport.
• the invention therefore also relates to such a use of this type of compound for the production in particular of dietetic, cosmetic or medical compositions. It also relates to any dietetic, cosmetic or medical composition comprising this type of compound encapsulating one or more other active compounds.
• Example 1 Sources of compounds
• Pectin can be obtained from any plant containing it, in particular apple, citrus, by known techniques. It is also possible to use commercially available pectins, in particular those sold by Herbstreith & Fox, in particular the pectin sold under the name Pectin Classic. AU 701 You can also use a plant extract, eg apple or citrus, naturally containing pectin which can be enriched by a supply of purified or synthesized pectin
• Lycopene or psi-carotene (Cl n ° 75125, E160 (d) (trans), CAS n ° 502- 65-8) is extracted from the tomato according to methods known to those skilled in the art
• broccoli is also a source of beta-carotene and therefore that the use of an appropriate broccoli extract will advantageously supplement the composition according to the invention with a carotenoid.
• Broccoli is a vegetable belonging to the cruciferous family, which contains substances very sensitive to the phenomenon of redox as well as to the phenomenon of enzymatic lysis. Like its sisters in the cruciferous family, it has the particularity of containing sulfur glucosides (glucosinolates) which under the attack of certain enzymes (myrosinases, catalases) transform this compound into isothyocyanates or derivatives (sulphoraphanes) which are responsible for very characteristic smell of this family. These compounds are very volatile and oxidize quickly, making any preparation of dry plants ineffective.
• the applicant was able to develop an appropriate procurement process.
• cryogenic grinding using any cryogenic source, e.g. liquid nitrogen
• micronized powder is obtained which is then lyophilized.
• the broccoli powder is then collected and mixed with the other ingredients of the preparation.
• the evaporation water from the freeze-dryer freeze trap is then recovered, it is concentrated by reverse osmosis at a temperature not exceeding 15 ° C.
• the volume of concentrated solution is reduced to the proportion of 1/100 (1 liter of concentrate for 100 liters of RO water).
• This water contains part of the volatile substances of the plant; it is then reintroduced into the final preparation according to the process described below.
• the mixing of pectins of various esterifications is carried out in a band mixer (Comia Fao type) or any other type of mixer; when the mixture is homogeneous, the tomato oleoresin is added in small portions, then the broccoli osmosis water.
• This addition has the particularity of creating a network at the fiber level which very advantageously leads to an encapsulation of the active substances (which in particular makes it possible to ensure the bioavailability of the added compounds (eg carotenoid and / or glucosinolate and / or sulphoraphane, etc.). .) and their transport); the lyophilized broccoli powder is then added, then finally a colloidal silica-type substance (eg AEROSIL) allowing the preparation to be dehydrated.
• AEROSIL colloidal silica-type substance
• the mixture thus prepared is ready for the various applications.
• Example 5 Cosmetic composition Product with depolluting action and cellular protector
• Example 7 Effect of a composition according to the invention on the toxicity of mercury in rats.
• the preventive and curative properties of a composition according to the invention were evaluated with respect to mercury. in rats.
• the preventive properties were evaluated by simultaneously administering HgCI 2 and the composition.
• the healing properties were evaluated by administering HgCI 2 alone to rats for 2 weeks, then by treating with the composition for the following 2 weeks.
• Duration of treatment 28 days. Non-lethal doses of mercury were administered and no direct deaths were observed. On the other hand, mortality was observed during anesthesia performed on certain rats not treated with the composition. The composition, on the other hand, protected the treated rats; the action of mercury on anesthesia was inhibited by the composition.
• composition significantly reduces blood mercury concentrations, both preventive and curative.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Natural Medicines & Medicinal Plants (AREA)
• Epidemiology (AREA)
• Pharmacology & Pharmacy (AREA)
• Medicinal Chemistry (AREA)
• Chemical & Material Sciences (AREA)
• Biotechnology (AREA)
• Botany (AREA)
• Microbiology (AREA)
• Mycology (AREA)
• Engineering & Computer Science (AREA)
• Dermatology (AREA)
• Birds (AREA)
• Medical Informatics (AREA)
• Alternative & Traditional Medicine (AREA)
• Molecular Biology (AREA)
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• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Cosmetics (AREA)
• Medicines Containing Plant Substances (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Coloring Foods And Improving Nutritive Qualities (AREA)
• Medicinal Preparation (AREA)

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• 1997
  • 1997-10-17 FR FR9713258A patent/FR2769837B1/fr not_active Expired - Fee Related
• 1998
  • 1998-10-16 AU AU95464/98A patent/AU9546498A/en not_active Abandoned
  • 1998-10-16 JP JP2000516645A patent/JP2001520181A/ja active Pending
  • 1998-10-16 CA CA002306414A patent/CA2306414A1/fr not_active Abandoned
  • 1998-10-16 WO PCT/FR1998/002232 patent/WO1999020242A1/fr not_active Ceased
  • 1998-10-16 BR BR9813083-8A patent/BR9813083A/pt not_active Application Discontinuation
  • 1998-10-16 EP EP98949074A patent/EP1023040A1/de not_active Withdrawn

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