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WO2001049285A1 - Flavonoide et forme posologique, production et utilisation associees - Google Patents

Flavonoide et forme posologique, production et utilisation associees Download PDF

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Publication number
WO2001049285A1
WO2001049285A1 PCT/FI2001/000001 FI0100001W WO0149285A1 WO 2001049285 A1 WO2001049285 A1 WO 2001049285A1 FI 0100001 W FI0100001 W FI 0100001W WO 0149285 A1 WO0149285 A1 WO 0149285A1
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WIPO (PCT)
Prior art keywords
flavonoids
dosage form
flavonoid
apple
onion
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/FI2001/000001
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English (en)
Inventor
Lasse Kurppa
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SLK Foundation
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SLK Foundation
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Filing date
Publication date
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Priority to AU26824/01A priority Critical patent/AU2682401A/en
Publication of WO2001049285A1 publication Critical patent/WO2001049285A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105—Plant extracts, their artificial duplicates or their derivatives
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • 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
    • A61K36/13—Coniferophyta (gymnosperms)
    • A61K36/15—Pinaceae (Pine family), e.g. pine or cedar
    • 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
    • A61K36/16—Ginkgophyta, e.g. Ginkgoaceae (Ginkgo family)
    • 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)
    • A61K36/73—Rosaceae (Rose family), e.g. strawberry, chokeberry, blackberry, pear or firethorn
    • 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)
    • A61K36/82—Theaceae (Tea family), e.g. camellia
    • 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)
    • A61K36/87—Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
    • 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)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/896—Liliaceae (Lily family), e.g. daylily, plantain lily, Hyacinth or narcissus
    • A61K36/8962—Allium, e.g. garden onion, leek, garlic or chives
    • 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
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/11—Encapsulated compositions
    • 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
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    • 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
    • A61K8/9755—Gymnosperms [Coniferophyta]
    • A61K8/9767—Pinaceae [Pine family], e.g. pine or cedar
    • 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
    • A61K8/9771—Ginkgophyta, e.g. Ginkgoaceae [Ginkgo family]
    • 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
    • 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]
    • A61K8/9794—Liliopsida [monocotyledons]
    • 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
    • A61P39/06—Free radical scavengers or antioxidants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
    • 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
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/52—Stabilizers
    • A61K2800/522—Antioxidants; Radical scavengers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4875—Compounds of unknown constitution, e.g. material from plants or animals

Definitions

  • Flavonoid drug and dosage form its production and use
  • the present invention relates to a flavonoid drug, a flavonoid dosage form, their production and use.
  • the dosage form include products used as food additives or alimentary products.
  • the flavonoid drug and the flavonoid dosage form of the present invention is useful for the therapeutic, prophylactic and/or palliative treatment of cancer, psoriasis, diabetes, rheumatism, cardiovascular diseases, elevated blood pressure, elevated cholesterol levels, caries, and colds. , in general for the treatment of disorders and disease related to aging.
  • the drug of the present invention is also useful as medicament for the protection and control of cholesterol and human DNA, RNA, lipids, enzymes, hormones in order to reduce and/or prevent the undesired oxidation thereof and as an antibiotic or cosmetic preparation which composition contains at least one flavonoid as the active ingredient.
  • the preparation of this invention is suitable for the treatment of all kinds of disorders and disease related to aging including medicinal and cosmetic treatment.
  • the dosage form of the invention especially include food additive products and alimentary products freely sold and having the above mentioned effects.
  • the dosage form of the present invention is suitable for oral, parenteral or topical administrationand and may be prepared as capsules, powders, tablets, liquids and alike.
  • Flavonoids are one of the widest found groups of vegetable chemical compounds. They are polyphenolic antioxidants naturally present in vegetables, fruits, and beverages such as tea and wine. More than 3000 flavonoids have been found and identified. All flavonoids have a common biosynthetic origin and they therefore possess the same basic structural element, namely a 2-phenyl chromane skeleton. Flavonoids occur mainly as glycosides but they may also be in the form of free phenols and sulphates.
  • Oxidation of low density lipoproteins by free radicals is thought to play a central part in the development of atherosclerosis. Antioxidants may thus delay the onset of atherogenesis.
  • Several flavonoid compounds have been shown to have antioxidant properties in vitro, inhibiting the oxidation of low density lipoproteins and reducing thrombotic tendencies by inhibiting platelet aggregation.
  • Patent application WO 98/18348 by the same inventor relates to the use of flavonoids as flavoring agents, especially for replacing table salt.
  • a mixture of the flavonoids of green tea, onion and apple are described as a preferred, flavoring mixture.
  • flavonoids In the prior art the intake of flavonoids was mainly provided by people eating flavonoid-containing fruits and vegetables or drinking flavonoid-rich beverages such as tea and wine.
  • the present invention is based on the realization that flavonoids may be extracted and/or powdered and made into a drug or dosage form which may be used for the therapeutic, prophylactic and/or palliative treatment of serious disorders such as cancer.
  • the product also potentially has an activity against psoriasis, diabetes and rheumatism. It can reduce blood, pressure and cholesterol levels. It can reduce the risk for stroke and heart diseases. It may also provide protection against influenza. It is potentially useful for combatting disorders caused by stress. It can further successfully be used as an antioxidant for reducing or preventing the undesired oxidation of cholesterol and DNA in humans
  • the drug and dosage form according to the invention has little or no toxic effects. It can be administered orally, parenterally and/or topically. It has a good human acceptance and low cost of preparation.
  • the flavonoid drug and the dosage form of the present invention is easy to use and is suitable for both home use and hospital care.
  • the aim of the invention is to prevent (presented by a dotted line in the scheme above) the undesired oxidation of the species.
  • the present invention is directed to a medicament and a dosage form for the therapeutic, prophylactic and/or palliative treatment of cancer, psoriasis, diabetes, rheumatism, cardiovascular diseases, elevated blood pressure, elevated cholesterol levels, caries, and colds, which comprises a composition containing at least one flavonoid as the active ingredient.
  • the present invention is further directed to a medicament for the protection and control of cholesterol and human DNA, RNA, lipids, enzymes, hormones in order to reduce and/or prevent the undesired oxidation thereof and as an antibiotic or cosmetic preparation which composition contains at least one flavonoid as the active ingredient
  • the preferred medicament comprises a mixture of at least two, and preferably three flavonoids in an orally, parenterally or topically administrable dosage form.
  • the preferred flavonoids are selected from flavonoids of onion, green and black tea, apple, grape, bark of Ginko Biloba and Maritime pine. Especially preferred are quercetin and its derivatives, epigallocatechin and its derivatives, especially epigallocatechin-3-gallate, and myricetin.
  • the preferred flavonoid is epigallocatchin gallate. It is most preferably used in combination with quercetin and vitamin C, possibly also vitamin E. Vitamin C is believed to prevent oxidation of polyphenols and to reactivate vitamin E.
  • the medicament and food additive of the present invention preferably contains querectin and/or its derivatives in an amount of 10 to 30 mg/100 g and epigallocatechin-3-gallate 80 to 200 mg/100 g calculated on the weight of the product.
  • the dosage form according to the present invention is suitable for the therapeutic, prophylactic and/or palliative treatment of cancer, and it is formulated into a capsule, pill, tablet, cream, ointment, liquid or an injectable fluid which contains at least one flavonoid as the active ingredient. It preferably contains a mixture of at least two, and preferably three flavonoids selected from flavonoids of onion, green and black tea, apple, grape, bark of Ginko Biloba and Maritime pine.
  • the dosage form according to the invention preferably contains an antioxidant, such as C-vitamin and/or E-vitamin, for preventing polyphenol oxidation from taking place in the preparation.
  • an antioxidant such as C-vitamin and/or E-vitamin
  • the dosage form of the present invention can be produced by mixing a powder and/or an extract of onion, green black tea and/or apple and/or grape and/or extract of fresh bark of Ginko Biloba and/or Maritime pine with at least one pharmaceutically acceptable carrier and formulating it into a dosage form for oral, parenteral or topical administration.
  • An antioxidant such as C-vitamin and/or E-vitamin is preferably included in the formulation.
  • the drug of the present invention is preferably used for clinical nutrition. It can be easily administered orally in the form of a tablet, pill or capsule or it can be in the form of a liquid or a powder to be dissolved in a liquid. It can be drunk as a juice for thirst or as a table drink. It can also be administered by a tube directly into the stomach.
  • the last mentioned adminstration form is especially suitable for cancer/geriatric and other chronic patients.
  • topically administrable creams, lotions and ointments can be used for prophylaxis, palliation and treatment of excessive exposure to UV radiation and/or melanoma.
  • Cosmetic type lotions or shampoos may be used to prevent and cure psoriasis, but also other more cosmetic dermatological disorders may be treated.
  • the preferred flavonoids are selected from flavonoids of onion, tea and apple, and an especially preferred mixture comprises a mixture containing onion powder (about 35 to 50 %), green and/or black tea extract (about 30 to 40 %), and apple powder (about 20 to 30 %).
  • Preferred flavonoides may further be selected from flavonoids derived from onion, green tea, apple, grape, Ginko Biloba and Maritime pine as follows: onion powder 20 to 50 %, tea extract 10 to 40 %, apple powder 10 to 30 %, grape powder 10 to 40 %, Ginko Biloba powder 10 to 30 % and Maritime pine powder 10 to 30 %.
  • the mixture may be formulated with pharmaceutically acceptable carriers such as di- or tricalcium phosphate and/or silicon dioxide.
  • the preferred embodiment according to the invention comprises a mixture of flavonoids derivable from these natural sources, such as onion powder, green tea extract, apple powder, grape powder, Ginko Biloba powder and Maritime pine powder.
  • the beneficial flavonoids are mainly quercetin and its derivatives, epigallocatechin-3-gallate and myricetin. It has been found that green tea extract can be provided with a very high level of epigallocatechin-3-gallate which has been found to have a beneficial effect on serious disorders such as cancer. Thus, epigallocatechin-3-gallate has an ability to inhibit the growth of cancer cells and it has been shown to reduce the size of malignant tumors. In combination with quercetin or its derivatives, the beneficial effect is enhanced. Myricetin has a similar effect.
  • Vitamin C When these naturally occurring flavonoid sources are combined with Vitamin C, the result is a medicament which has a good storage capacity and a surprisingly active therapeutic, prophylactic and palliative effect as deseribed above.
  • Green tea extract which is enriched in epigallocatechin gallate is commercially available and is suitable for use in the present invention.
  • the flavonoid components may be present in the drug in the form of powders, liquids and/or extracts.
  • the flavonoid components may be crystallized or concentrated.
  • a daily dosage of the flavonoid drug will depend on the formulation and- the disease in question.
  • the flavonoid drug is non-toxic and based on naturally occurring sources. Therefore overdosing is hardly likely to occur.
  • the beneficial effect of the drug according to the invention on health is based on the flavonoids, especially a combination of flavonoids from apple, onion, green tea, grape, Ginko Biloba and/or Maritime pine, which the product contains.
  • the natural protective agents are in the right proportion to each other and are combined, with Vitamin C to prevent oxidation.
  • the drug according to the invention may also contain other components, such as further flavonoids, vitamins, and pharmaceutically acceptable carriers.
  • the drug according to the invention may be mixed with pharmaceutically acceptable carrier or filler compounds which are easily powdered and which add body to the drug.
  • Such carriers are preferably inert compounds such as calcium phosphate and/or silica.
  • the drug may he provided in a capsule or be produced in powder, tablet, liquid or cream form.
  • One aim of the present invention is also to provide a method for the reduction or prevention of the undesired oxidation of human cholesterol and/or DNA, in which the composition containing an effective amount of at least one flavonoid as the active ingredient is given to the person to be treated.
  • said composition contains at least two, perferably three, flovonoids selected from the flavoinoids of onion, green tea, apple, grape, Ginko Biloba and Maritime pine.
  • said flavonoids contained in the composition are selected from querectin and its derivatives, epigallocatechin- 3-gallate and/or myricetin. Perferred amounts are: quercetin and/or its derivatives 10 to 30 mg/100 g and epigallochatechin-3-gallate 80 to 200 mg/100 g calculated on the weight of the product.
  • Each capsule contained: gelatine 60 mg 23.1 % microcrystalline cellulose (E 460) 46 mg onion powder 45 mg 17.3 % dicalcium phosphate (E 540) 46 mg tea extract 36 mg 13.8 % apple powder 27 mg 10.4 % ascorbic acid (E 300) 2 mg silicium oxide (E 551) 2 mg magnesium stearate 2 mg
  • the capsule was tested for presence of flavonoids by HPLC after acid hydrolysis.
  • the capsule according to the invention was compared with the flavonoid contents of Phytorome green tea extract and normal green tea extract (Natural Gunpowder).
  • a 4-fold extracted normal green tea contained less than 1.0 mg epigallocatechin gallate per 100 g of product.
  • the capsule of the present invention was produced from the Phytomore green tea extract and contained 3280 mg cpigaflocatechin gallate per 100 g of product.
  • A stands for a capsule of the present invention
  • B stands for Phytomore green tea extract M 4115
  • C stands for 4-fold water extracted Natural Gunpowder Tea.
  • Flavonoids (m ⁇ /1 OO ⁇ fresh weight*) A B C epigallocatechin - epigallocatechin gallate 4870 6100 -
  • Flavonoids (mg/10Qg fresh weight*) A B C isovitexin - - 85.8 vitexin - - 91.6
  • the Table II shows that the capsule of the present invention contains a large proprotion of beneficial flavonoids.
  • Table III reveals the composition of another "Flavomare” capsule and extract according to the invention.
  • Flavanols epigallocatechin 23300 epigallocatechin gallate 4097 8,19 750
  • LDL-TRAP LDL antioxidant potential
  • LDL baseline diene conjugation was based on spectrophotometric determination of conjugated dienes in lipids extracted from LDL.
  • Determination of LDL antioxidant potential was based on luminometric measurement of the ability of LDL sample to resist chemically- induced lipid peroxidation. Serum total, LDL and HDL cholesterol were assayed by commercial kits (Boeh nger-Mannheim).
  • LDL-BDC baseline diene conjugation method
  • LDL-TRAP Flavomare on LDL antioxidant potential
  • Flavomare (i) can act as an antioxidant in human body and (ii) prevents LDL oxidation in vivo.

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  • Medicines Containing Plant Substances (AREA)

Abstract

L'invention concerne un médicament, une forme posologique et un additif alimentaire utilisés dans le traitement thérapeutique, prophylactique et/ou palliatif de maladies et de troubles de santé et cosmétique, comprenant une composition contenant au moins un, et de préférence au moins deux, flavonoïdes comme principe actif. L'invention concerne également l'utilisation de ces produits dans des procédés de traitement.
PCT/FI2001/000001 2000-01-03 2001-01-02 Flavonoide et forme posologique, production et utilisation associees Ceased WO2001049285A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU26824/01A AU2682401A (en) 2000-01-03 2001-01-02 Flavonoid drug and dosage form, its production and use

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FI20000004A FI20000004A0 (fi) 2000-01-03 2000-01-03 Flavonoidilääke...
FI20000004 2000-01-03

Publications (1)

Publication Number Publication Date
WO2001049285A1 true WO2001049285A1 (fr) 2001-07-12

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PCT/FI2001/000001 Ceased WO2001049285A1 (fr) 2000-01-03 2001-01-02 Flavonoide et forme posologique, production et utilisation associees

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AU (1) AU2682401A (fr)
FI (1) FI20000004A0 (fr)
WO (1) WO2001049285A1 (fr)

Cited By (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002009699A3 (fr) * 2000-07-28 2003-01-03 Immupharm Aps Procede pour traiter les symptomes du rhume, la rhinite allergique et les infections liees aux voies respiratoires
WO2003011339A1 (fr) * 2001-07-30 2003-02-13 Dsm Ip Assets B.V. Composition de l'epigallocatechin gallate
WO2003015737A1 (fr) * 2001-08-14 2003-02-27 Beiersdorf Ag Utilisation d'oroxyline a pour fabriquer des preparations cosmetiques ou dermatologiques destinees a la prophylaxie et au traitement d'etats inflammatoires cutanes et / ou a la protection de la peau en cas de peau sensible et seche
US6576660B1 (en) 1997-10-31 2003-06-10 Arch Development Corporation Methods and compositions for regulation of 5-α-reductase activity
WO2003057700A1 (fr) * 2001-12-28 2003-07-17 Sansho Seiyaku Co., Ltd. Compositions contenant un inhibiteur de pigmentation, utilisation desdites compositions et leur procede de production
US6610320B2 (en) 2000-04-14 2003-08-26 Mars, Incorporated Compositions and methods for improving vascular health
WO2003094878A1 (fr) * 2002-05-10 2003-11-20 Suntory Limited Composition de gallocatechine contenant du gallate
WO2002072086A3 (fr) * 2001-03-12 2004-02-19 Consorzio Per Gli Studi Uni Utilisation de l'epigallocatechin-3-gallate ou des derives de celui-ci dans la prevention et le traitement de maladies neurodegeneratives
US6696484B2 (en) 1997-10-31 2004-02-24 University Of Chicago Office Of Technology And Intellectual Property Method and compositions for regulation of 5-alpha reductase activity
WO2004045605A1 (fr) * 2002-11-18 2004-06-03 N.V. Nutricia Utilisation de flavonoide pour le traitement de la surcharge ponderale et la reduction de l'appetit chez un mammifere
WO2007029982A1 (fr) * 2005-09-08 2007-03-15 Amorepacific Corporation Composition d'une application a usage externe pour la peau anti-vieillissement
WO2007029983A1 (fr) * 2005-09-08 2007-03-15 Amorepacific Corporation Composition cosmetique pour eliminer le sebum contenant des catechines et des flavonols
WO2007032624A1 (fr) * 2005-09-16 2007-03-22 Amorepacific Corporation Composition pour application cutanee externe, contenant du gallocatechine gallate, ayant un effet hydratant sur la peau
US7238376B2 (en) 2000-11-15 2007-07-03 Rutgers, The State University Black tea extract for prevention of disease
WO2008096040A1 (fr) * 2007-02-07 2008-08-14 Slk Foundation Composition de parfum
WO2009003832A3 (fr) * 2007-07-05 2009-03-19 Unilever Nv Composition comprenant des polyphénols
WO2009003838A3 (fr) * 2007-07-05 2009-03-19 Unilever Nv Composition comprenant des polyphénols
US7585890B2 (en) 2002-10-24 2009-09-08 Immunpharm A/S Pharmaceutical compositions comprising flavonoids and menthol
GB2463080A (en) * 2008-09-02 2010-03-03 Nicholas John Larkins Pharmaceutical preparation
ITMI20090747A1 (it) * 2009-04-30 2010-11-01 Giuliani Spa Composizione farmaceutica o dermatologica o nutrizionale o cosmetica per combattere l'azione di immunosoppressione provocata sulla pelle da agenti aggressivi
US7947733B2 (en) * 2007-07-31 2011-05-24 Limerick Biopharma Phosphorylated pyrone analogs and methods
EP2068902A4 (fr) * 2006-09-21 2012-03-21 Jack F Bukowski Compositions dérivées du thé et procédés d'utilisation de celles-ci pour améliorer l'état de santé cardiovasculaire
KR101149686B1 (ko) * 2005-09-08 2012-05-23 (주)아모레퍼시픽 카테킨류 및 캄페롤 성분을 함유하는 피지억제용 화장료조성물
US20120171282A1 (en) * 2009-07-28 2012-07-05 Velleja Research S.R.L. Ginkgo biloba extract with a standardised ginkgo flavone glycosides content deprived of the paf-antagonist terpenic fraction, and compositions containing it, for the prevention and treatment of circulatory, cognitive, geriatric and sensory disorders
WO2010121213A3 (fr) * 2009-04-16 2012-08-09 Forsyth Dental Infirmary For Children Compositions antibactériennes
ES2524870A1 (es) * 2013-06-12 2014-12-15 Universidad De Burgos Sazonador de origen vegetal con propiedades conservantes, sustitutivo de la sal, y procedimiento de obtención del mismo
US20150313999A1 (en) * 2012-11-29 2015-11-05 Nestec S.A. Increasing the bioavailability of flavan-3-ols by polyphenols
DE102014010826A1 (de) * 2014-07-23 2016-01-28 Innotec Research Ug (Haftungsbeschränkt) Optimierte chemische oder physikalische Kombination von Grüntee-Extrakt mit weiteren Hilfsstoffen zur gleichzeitigen Stabilisierung des Grüntee-Extrakts und zur Modulierung körpereigener Prozesse.
US9517249B2 (en) 2012-11-26 2016-12-13 Access Business Group International Llc Antioxidant dietary supplement and related method
EP3682865A1 (fr) * 2019-01-15 2020-07-22 Amorepacific Corporation Composition de blanchiment de la peau ou de prévention ou d'amélioration des rides comprenant un extrait de thé vert contenant des quantités d'ingrédients modifiées
CN115803040A (zh) * 2020-05-29 2023-03-14 韦德森诺氏印度私人有限公司 用于处理covid-19和相关病症的组合物

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Cited By (49)

* Cited by examiner, † Cited by third party
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US6576660B1 (en) 1997-10-31 2003-06-10 Arch Development Corporation Methods and compositions for regulation of 5-α-reductase activity
US6696484B2 (en) 1997-10-31 2004-02-24 University Of Chicago Office Of Technology And Intellectual Property Method and compositions for regulation of 5-alpha reductase activity
US6610320B2 (en) 2000-04-14 2003-08-26 Mars, Incorporated Compositions and methods for improving vascular health
WO2002009699A3 (fr) * 2000-07-28 2003-01-03 Immupharm Aps Procede pour traiter les symptomes du rhume, la rhinite allergique et les infections liees aux voies respiratoires
US8003688B2 (en) 2000-07-28 2011-08-23 Immupharm Aps Method of treating symptoms of common cold, allergic rhinitis and infections relating to the respiratory tract
EA008612B1 (ru) * 2000-07-28 2007-06-29 Иммуфарм Апс Способ лечения обычной простуды, аллергического ринита и инфекций дыхательных путей
US7238376B2 (en) 2000-11-15 2007-07-03 Rutgers, The State University Black tea extract for prevention of disease
WO2002072086A3 (fr) * 2001-03-12 2004-02-19 Consorzio Per Gli Studi Uni Utilisation de l'epigallocatechin-3-gallate ou des derives de celui-ci dans la prevention et le traitement de maladies neurodegeneratives
CN1325049C (zh) * 2001-07-30 2007-07-11 Dsmip资产有限公司 含有表没食子儿茶素没食子酸酯的组合物
WO2003011339A1 (fr) * 2001-07-30 2003-02-13 Dsm Ip Assets B.V. Composition de l'epigallocatechin gallate
WO2003015737A1 (fr) * 2001-08-14 2003-02-27 Beiersdorf Ag Utilisation d'oroxyline a pour fabriquer des preparations cosmetiques ou dermatologiques destinees a la prophylaxie et au traitement d'etats inflammatoires cutanes et / ou a la protection de la peau en cas de peau sensible et seche
WO2003057700A1 (fr) * 2001-12-28 2003-07-17 Sansho Seiyaku Co., Ltd. Compositions contenant un inhibiteur de pigmentation, utilisation desdites compositions et leur procede de production
WO2003094878A1 (fr) * 2002-05-10 2003-11-20 Suntory Limited Composition de gallocatechine contenant du gallate
EP1504754A4 (fr) * 2002-05-10 2006-03-15 Suntory Ltd Composition de gallocatechine contenant du gallate
US7671086B2 (en) 2002-10-24 2010-03-02 Immupharm A/S Pharmaceutical compositions comprising flavonoids and menthol
US7585890B2 (en) 2002-10-24 2009-09-08 Immunpharm A/S Pharmaceutical compositions comprising flavonoids and menthol
WO2004045605A1 (fr) * 2002-11-18 2004-06-03 N.V. Nutricia Utilisation de flavonoide pour le traitement de la surcharge ponderale et la reduction de l'appetit chez un mammifere
WO2007029983A1 (fr) * 2005-09-08 2007-03-15 Amorepacific Corporation Composition cosmetique pour eliminer le sebum contenant des catechines et des flavonols
WO2007029982A1 (fr) * 2005-09-08 2007-03-15 Amorepacific Corporation Composition d'une application a usage externe pour la peau anti-vieillissement
US10092493B2 (en) 2005-09-08 2018-10-09 Amorepacific Corporation Composition of skin external application for anti-aging
KR101149686B1 (ko) * 2005-09-08 2012-05-23 (주)아모레퍼시픽 카테킨류 및 캄페롤 성분을 함유하는 피지억제용 화장료조성물
WO2007032624A1 (fr) * 2005-09-16 2007-03-22 Amorepacific Corporation Composition pour application cutanee externe, contenant du gallocatechine gallate, ayant un effet hydratant sur la peau
US8518458B2 (en) 2006-09-21 2013-08-27 Immune Guard, LLC Tea-derived compositions and methods of using same for cardiovascular health
EP2068902A4 (fr) * 2006-09-21 2012-03-21 Jack F Bukowski Compositions dérivées du thé et procédés d'utilisation de celles-ci pour améliorer l'état de santé cardiovasculaire
WO2008096040A1 (fr) * 2007-02-07 2008-08-14 Slk Foundation Composition de parfum
WO2009003832A3 (fr) * 2007-07-05 2009-03-19 Unilever Nv Composition comprenant des polyphénols
WO2009003838A3 (fr) * 2007-07-05 2009-03-19 Unilever Nv Composition comprenant des polyphénols
US7947733B2 (en) * 2007-07-31 2011-05-24 Limerick Biopharma Phosphorylated pyrone analogs and methods
GB2463080A (en) * 2008-09-02 2010-03-03 Nicholas John Larkins Pharmaceutical preparation
US8399220B2 (en) 2009-04-16 2013-03-19 Forsyth Dental Infirmary For Children Antibacterial compositions
US8802105B2 (en) 2009-04-16 2014-08-12 Forsyth Dental Infirmary For Children Antibacterial compositions
WO2010121213A3 (fr) * 2009-04-16 2012-08-09 Forsyth Dental Infirmary For Children Compositions antibactériennes
WO2010125541A1 (fr) * 2009-04-30 2010-11-04 Giuliani S.P.A. Composition pharmaceutique, dermatologique, nutritionnelle ou cosmétique pour combattre l'action immunosuppressive d'agents agressifs sur la peau
ITMI20090747A1 (it) * 2009-04-30 2010-11-01 Giuliani Spa Composizione farmaceutica o dermatologica o nutrizionale o cosmetica per combattere l'azione di immunosoppressione provocata sulla pelle da agenti aggressivi
AU2010243181B2 (en) * 2009-04-30 2013-12-05 Giuliani S.P.A. A pharmaceutical, dermatological, nutritional or cosmetic composition for combating the immunosuppressive action of aggressive agents on the skin
JP2012525375A (ja) * 2009-04-30 2012-10-22 ギウリアニ ソシエタ ペル アチオニ 皮膚の攻撃的な作用因子の免疫抑制作用に対抗するための医薬用、皮膚用、栄養用又は化粧品用組成物
US9138394B2 (en) 2009-04-30 2015-09-22 Giuliani S.P.A. Pharmaceutical, dermatological, nutritional or cosmetic composition for combating the immunosuppresive action of aggressive agents on the skin
US20120171282A1 (en) * 2009-07-28 2012-07-05 Velleja Research S.R.L. Ginkgo biloba extract with a standardised ginkgo flavone glycosides content deprived of the paf-antagonist terpenic fraction, and compositions containing it, for the prevention and treatment of circulatory, cognitive, geriatric and sensory disorders
US9517249B2 (en) 2012-11-26 2016-12-13 Access Business Group International Llc Antioxidant dietary supplement and related method
US10201583B2 (en) 2012-11-26 2019-02-12 Access Business Group International Llc Antioxidant dietary supplement and related method
US20150313999A1 (en) * 2012-11-29 2015-11-05 Nestec S.A. Increasing the bioavailability of flavan-3-ols by polyphenols
US10722584B2 (en) * 2012-11-29 2020-07-28 Societe Des Produits Nestle S.A. Increasing the bioavailability of flavan-3-ols by polyphenols
ES2524870A1 (es) * 2013-06-12 2014-12-15 Universidad De Burgos Sazonador de origen vegetal con propiedades conservantes, sustitutivo de la sal, y procedimiento de obtención del mismo
DE102014010826A1 (de) * 2014-07-23 2016-01-28 Innotec Research Ug (Haftungsbeschränkt) Optimierte chemische oder physikalische Kombination von Grüntee-Extrakt mit weiteren Hilfsstoffen zur gleichzeitigen Stabilisierung des Grüntee-Extrakts und zur Modulierung körpereigener Prozesse.
EP3682865A1 (fr) * 2019-01-15 2020-07-22 Amorepacific Corporation Composition de blanchiment de la peau ou de prévention ou d'amélioration des rides comprenant un extrait de thé vert contenant des quantités d'ingrédients modifiées
US11896640B2 (en) 2019-01-15 2024-02-13 Amorepacific Corporation Composition for skin-whitening or preventing or improving skin wrinkles comprising green tea extract which has modified amounts of ingredients
US12178837B2 (en) 2019-01-15 2024-12-31 Amorepacific Corporation Composition for skin-whitening or preventing or improving skin wrinkles comprising green tea extract which has modified amounts of ingredients
CN115803040A (zh) * 2020-05-29 2023-03-14 韦德森诺氏印度私人有限公司 用于处理covid-19和相关病症的组合物
CN115803040B (zh) * 2020-05-29 2024-04-12 韦德森诺氏印度私人有限公司 用于处理covid-19和相关病症的组合物

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