EP1786384A1 - Utilisation d'au moins un triene d'acide gras conjugue pour la preparation d'un medicament destine au traitement de l'inflammation - Google Patents
Utilisation d'au moins un triene d'acide gras conjugue pour la preparation d'un medicament destine au traitement de l'inflammationInfo
- Publication number
- EP1786384A1 EP1786384A1 EP05790724A EP05790724A EP1786384A1 EP 1786384 A1 EP1786384 A1 EP 1786384A1 EP 05790724 A EP05790724 A EP 05790724A EP 05790724 A EP05790724 A EP 05790724A EP 1786384 A1 EP1786384 A1 EP 1786384A1
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- EP
- European Patent Office
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- 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.)
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- 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)
- A61K36/84—Valerianaceae (Valerian family), e.g. valerian
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
Definitions
- the subject of the invention is the use of at least one conjugated and optionally oxygenated fatty acid triene of synthetic and / or natural origin for the manufacture of a medicinal product intended for the treatment of inflammatory diseases and / or metabolic disorders. consecutive to inflammation.
- ⁇ -linolenic acid The most common trienoic fatty acid found in plants is ⁇ -linolenic acid.
- Several conjugated isomers of ⁇ -linolenic acid may be found in certain plant formulas and sometimes become major constituents of these vegetable oils. Catalysts of catalpa ovata, punicic acid of punica granatum, jacaric acid of jacaranda ninosisonia and calendulic acid of calendula officinalis, pomégranate (Punica granatum L.), catalpa (Catalpa ovata G .), balsam, ...
- Conjugated fatty acid trienes such as ⁇ -linolenic acid or calendrical acid, have already been used in pharmaceutical compositions for treating and / or preventing cholesterol.
- the inflammatory process is the set of reaction phenomena triggered, in a multicellular living organism, by the aggression of any pathogenic agent. It is an omni-tissue phenomenon taking place preferentially in the connective tissue which normally tends to limit and repair the effects of aggression. It ends with repair or healing of the lesion.
- Inflammation can be caused by physical aggressions (such as hot, cold, ionizing radiation), chemical (caused by acidic or basic compounds, bacterial toxins). It may be the consequence of an infection related to the presence in the body of living pathogenic organisms such as bacteria, viruses, parasites or fungi. It can be caused by an immune reaction secondary to reintroduction into the body of an antigen. She can finally be the consequence of a tissue necrosis, itself secondary to many causes, for example an arterial occlusion.
- the causes are multiple and represent the pathogens. They determine cellular or tissue lesions that will trigger inflammation: - physical causes (trauma, heat, cold, radiation, electric current);
- the pathogen may be endogenous or exogenous and infectious causes (microorganisms) are only a small part of the causes of inflammation. Some causes determine lesions whose morphology is peculiar, hence the notion of specific inflammation. On the other hand, the same pathogen can cause different inflammatory reactions depending on the host hence the importance of factors related to the host (contributing factors or protective factors). The course of the inflammatory process evolves in three successive stages:
- UV radiation reaches the skin, part of it is reflected from the surface. The rest of the radiation is scattered in the tissues just below the surface of the skin. A fraction of this radiation is absorbed by the living cells of the skin. Ultraviolet radiation absorbed by living cells damages sensitive substances that affect the normal development and appearance of the skin. Damage can lead to sunburn, accelerated aging of the skin and / or skin cancer.
- Sunburn is the most known and immediate effect of ultraviolet radiation on the skin. It is an inflammation caused by increased blood flow under the skin. A brief, intense exposure can cause severe sunburn in people who are not used to the strong sun. There is evidence that this type of exposure, as well as long-term exposures can lead to the development of skin cancers. A repetition exposed to the ultraviolet radiation of the sun participates also to the aging process. The skin thins in places and loses its elasticity; imperfections, hyper-pigmentation and wrinkles also appear. These changes can occur after many years of exposure, but when they do occur, the damage is irreversible. If sun exposure continues for several years, damaged skin is at greater risk of developing one of the forms of skin cancer. Exposure to ultraviolet radiation increases the risk of developing these cancers.
- Patent Application FR 2,630,648 describes a topical anti-inflammatory or anti-irritant composition comprising a zinc salt of one or more compounds selected from unsaturated fatty acids, polyunsaturated fatty acids and their cyclic derivatives, in which an approved excipient in a pharmacy.
- This application also teaches that derivatives of certain unsaturated or polyunsaturated fatty acids or protenoic acid may exhibit anti-inflammatory activity; possible anti-inflammatory activity of polyunsaturated fatty acids is neither described nor suggested.
- conjugated and optionally oxygenated fatty acid trienes of synthetic and / or natural origin can be used in the treatment of inflammation and / or to promote healing.
- the subject of the present invention is therefore the use of a composition comprising at least one fatty acid chosen from the group consisting of alpha-eleostearic acid, catalpic acid, calendrical acid, jacaric acid, licanic acid and beta-eleostearic acid, for the manufacture of a medicament for the prevention and / or treatment of inflammatory diseases and / or metabolic disorders resulting from inflammation of the skin, mucous membranes and / or cartilage .
- the composition may comprise alpha-linolenic acid, alone or in admixture with at least one conjugated fatty acid.
- metabolic disorders consecutive to an inflammation of the skin, mucous membranes and / or cartilage is understood to mean all diseases related to a disturbance of the metabolism, said disturbance of the metabolism being induced. or following inflammation. These metabolic disorders therefore have in common inflammation of the skin, mucous membranes and / or cartilage and they correspond to the main or secondary effects of said inflammation.
- the mucous membranes are advantageously chosen from the group consisting of oral, gingival, broncho-pulmonary, auricular, nasal, rectal or vaginal intestinal mucosa.
- Alpha-eleostearic acid has the following formula:
- the catalpic acid has the following formula:
- the calendrical acid has the following formula:
- the jacaric acid corresponds to the following formula:
- Punic acid has the following formula:
- the licanic acid has the following general formula:
- Beta-eleostearic acid has the following formula:
- the composition according to the invention comprises at least ⁇ -eleostearic acid and / or catalpic acid.
- the conjugated fatty acid is chosen from the group consisting of alpha-eleostearic acid and catalpic acid, alone or as a mixture.
- the inflammation may have a physical origin (heat, cold, ionizing radiation, infra-red radiation, solar radiation), mechanical (friction), chemical (contact with irritants or allergens such as a perfume or chemicals) or biological (microbe, mushroom).
- the medicament is intended for the prevention and / or treatment of allergic and / or irritative reactions of the skin and / or mucous membranes.
- the drug according to the invention is also suitable for promoting healing, in normal or pathological healing processes, such as ulcers and pressure ulcers.
- the drug according to the invention is advantageously intended for the prevention and / or treatment of diseases selected from the group consisting of atopic eczema, inflammatory dermatoses such as psoriasis, irritative dermatitis, acne, seborrheic dermatitis, nummular eczema, dyshidrotic eczema,
- diseases selected from the group consisting of atopic eczema, inflammatory dermatoses such as psoriasis, irritative dermatitis, acne, seborrheic dermatitis, nummular eczema, dyshidrotic eczema,
- the drug is advantageously intended for the prevention and / or treatment of diseases selected from the group consisting of gingivitis and periodontitis.
- the medicament is also advantageously intended for the prevention and / or treatment of diseases selected from the group consisting of vulvitis and vaginitis.
- the drug is also advantageously intended for the prevention and / or treatment of diseases selected from the group consisting of arthritis and osteoarthritis.
- Alpha linolenic acid has already been described as an anti-inflammatory agent (EP 0 226 468). The inventors have discovered that it can also be used for the manufacture of a medicament for the prevention and / or treatment of inflammatory diseases and / or metabolic disorders resulting from inflammation of the body. skin, mucous membranes and / or cartilage.
- alpha-linolenic acid can be used for the manufacture of a medicament for treatment:
- atopic eczema inflammatory dermatoses such as psoriasis, irritative dermatitis, acne, seborrheic dermatitis, nummular eczema, dyshidrotic eczema, Pytiriasis alba, eczema crackling, nutritional eczema, urticaria, parasitic dermatoses, viral dermatoses, fungal or bacterial dermatoses, intertrigo, inflammatory topical vascularization disorders, foot ulcer and / or insect bites; - gingivitis and periodontitis;
- the present invention also relates to the use of a composition comprising at least one fatty acid selected from the group consisting of alpha-eleostearic acid, catalpic acid, calendrical acid, jacaric acid, licanic acid and beta-eleostearic acid, for the cosmetic treatment of skins and / or mucous membranes that are sensitive, irritated, intolerant, have an allergic tendency, are aged, have a skin barrier disorder, have skin rashes or have an immunological imbalance non-pathological related to intrinsic aging, extrinsic or hormonal.
- a composition comprising at least one fatty acid selected from the group consisting of alpha-eleostearic acid, catalpic acid, calendrical acid, jacaric acid, licanic acid and beta-eleostearic acid
- Alpha-linolenic acid may also be used in a cosmetic composition for the cosmetic treatment of skins and / or mucous membranes that are sensitive, irritated, intolerant, have an allergic tendency, are elderly, have a cutaneous barrier disorder, have cutaneous redness or exhibit a non-pathological immunological imbalance related to intrinsic, extrinsic or hormonal aging.
- the cosmetic treatment may consist of the application or the ingestion of a cosmetic or nutraceutical composition respectively.
- the subject of the present invention is also the use of a composition comprising at least one conjugated fatty acid chosen from the group consisting of alpha-eleostearic acid, catalpic acid, calendrical acid, jacaric acid, licanic acid and beta-eleostearic acid, for the cosmetic treatment of cellulite.
- a composition comprising at least one conjugated fatty acid chosen from the group consisting of alpha-eleostearic acid, catalpic acid, calendrical acid, jacaric acid, licanic acid and beta-eleostearic acid, for the cosmetic treatment of cellulite.
- Alpha linolenic acid can also be used in a cosmetic composition for the cosmetic treatment of cellulite.
- Cellulite is an inflammation of the cell tissue located mainly under the skin in predisposed areas (thighs, hips, buttocks).
- Cellulitis is an inflammation of the subcutaneous cell tissue, and is manifested by induration of the affected area. This phenomenon may be due to insufficient flow of the local microcirculation which alters the exchanges between the blood and the cellular tissues, which leads to an excessive fixation of water, fat, and an accumulation of waste at the level of the cells.
- the composition comprising at least one conjugated fatty acid selected from the group consisting of alpha-eleostearic acid, catalpic acid, calendrical acid, jacaric acid, licanic acid and Beta-eleostearic acid can be formulated in the form of various preparations suitable for topical, oral, rectal, vaginal, nasal, atrial, bronchial, or parenteral administration.
- the composition according to the invention is advantageously formulated for topical or oral administration.
- the composition may comprise alpha-linolenic acid, alone or in admixture with at least one conjugated fatty acid.
- the various formulations may include creams, ointments, lotions, oils, patches, sprays or any other products for external application.
- the composition to be administered topically advantageously comprises 0.001 to 50% by weight, still more preferably 0.5 to 20% by weight, of at least one conjugated fatty acid selected from the group consisting of ⁇ -eleostearic acid. , catalpic acid, calendrical acid, jacaric acid, licanic acid and ⁇ -eleostearic acid, relative to the total weight of said composition.
- the composition administered topically comprises 0.001 to 50% by weight, advantageously 0.5 to 20% by weight, still more advantageously 1 to 10% by weight, of alpha-eleostearic acid and 0.001 to
- the composition administered topically advantageously comprises 0.001 to 50% by weight, advantageously 0.5 to 20% by weight, still more advantageously 1 to 10% by weight, of alpha-eleostearic acid. , relative to the total weight of said composition.
- the drug or the cosmetic composition may be administered in unit or multidose administration forms in admixture with suitable pharmaceutical or cosmetic carriers known to those skilled in the art.
- suitable unit dosage forms include, optionally, scored tablets, capsules, powders, granules and oral solutions or suspensions.
- Suitable multidose forms of administration include oral drops, emulsions and syrups.
- the composition may be formulated as a dietary supplement.
- the conjugated fatty acid (s) according to the invention are mixed with a pharmaceutically or cosmetically acceptable vehicle such as, in particular, gelatin, talc, starch, lactose, magnesium stearate, gum arabic or their analogues.
- a pharmaceutically or cosmetically acceptable vehicle such as, in particular, gelatin, talc, starch, lactose, magnesium stearate, gum arabic or their analogues.
- the tablets may optionally be coated, that is to say covered with several layers of various substances such as sucrose, to facilitate the setting or storage.
- the tablets may still have a more or less complex formulation intended to modify the rate of release of the active ingredient.
- the release of the active ingredient of said tablet can be accelerated, slowed down or delayed depending on the desired absorption.
- a preparation in capsules is obtained by mixing the conjugated fatty acid (s) according to the invention with a diluent.
- a syrup preparation may contain the conjugated fatty acid (s) according to the invention together with a sweetener, preferably a sweetener, a flavoring agent and a suitable dye.
- the water-dispersible powders or granules may comprise the conjugated fatty acid (s) according to the invention in admixture with dispersants or wetting agents, suspending agents, such as polyvinypyrrolidone, or sweeteners or preservatives. taste correctors.
- the composition administered orally advantageously comprises 0.001% to
- the composition administered orally comprises 0.001 to 100% by weight, advantageously 1 to 50% by weight. weight, alpha-eleostearic acid, and 0.001 to 100% by weight, preferably 1 to 50% by weight, of catalpic acid, relative to the total weight of said composition.
- the composition administered orally comprises 0.001 to 100% by weight, advantageously 1 to 50% by weight, of alpha-eleostearic acid, relative to the total weight of said composition.
- composition according to the invention when the composition according to the invention is formulated in the form of a dietary supplement, said dietary supplement may comprise up to 100% by weight of active ingredients according to the invention, ie particular fatty acids defined in the present invention. invention.
- the amount of active ingredients that will comprise the composition according to the invention depends primarily on the mode of administration and the chosen dosage form.
- the modes of administration, the dosages and the optimum dosage forms of the compositions according to the invention can be determined according to the criteria generally taken into account in the establishment of a pharmaceutical treatment, in particular a dermatological treatment, or a cosmetic treatment adapted to a patient such as eg age or body weight of patient, severity of general condition, tolerance to treatment, the side effects noted, the type of skin.
- a pharmaceutical treatment in particular a dermatological treatment, or a cosmetic treatment adapted to a patient such as eg age or body weight of patient, severity of general condition, tolerance to treatment, the side effects noted, the type of skin.
- the drug and / or the active compounds according to the invention may further comprise at least one pharmaceutically acceptable excipient, in particular dermatologically acceptable, or cosmetically acceptable.
- an excipient suitable for topical external or oral administration is used.
- the medicament or the cosmetic composition according to the present invention may further comprise at least one adjuvant which is pharmaceutically or cosmetically known to those skilled in the art, chosen from thickeners, preservatives, perfumes, dyes, chemical or mineral filters, moisturizers, thermal waters, etc.
- the medicament according to the invention is intended for the treatment and / or prevention of diseases that may affect humans and / or animals, especially mammals.
- the medicament or the cosmetic composition according to the invention may further comprise, in combination, advantageously with a synergistic effect, at least one compound chosen from the group consisting of emollients, moisturizing active agents, activators of keratin synthesis, keratoregulators, keratolytics, skin barrier restructuring agents (activators of cutaneous lipid synthesis), activators of differentiation of keratinocytes (retinoids or retinoids like, calcidone®, calcium), modulators of the differentiation of the epidermis, agents strengthening the epidermal dermal junction, antibiotics, anti-bacterial agents, antifungal compounds, anti-viral agents, stimulants of innate immunity (natural antibiotic peptides) or acquired, the sebo-regulators , such as the 5-alpha reductase inhibitors, in particular the 5-alpha Avocuta® active agent marketed by Laborato Expanscience or the salts of zinc and sabal (Sabalinae of the subfamily Coryphoideae), immunomodul
- the composition comprises, in combination, advantageously with a synergistic effect, active principles chosen from the group consisting of anti-inflammatory agents.
- the activators of keratin synthesis that can be used in combination, advantageously with a synergistic effect, with the conjugated fatty acids are advantageously retinoids or retinoids like, the lupine peptides marketed by Silab, key proteins of the stratum corneum. or granulosum (keratins).
- the antibiotics that can be used in combination, advantageously with a synergistic effect, with the conjugated fatty acids are advantageously fucidic acid, penicillin, tetracyclines, pristinamycin, erythromycin, clindamycin, mupirocine, minocycline, doxycycline.
- the anti-viral agents that can be used in combination with the conjugated fatty acids are advantageously acyclovir and valacyclovir.
- anti-irritant agents that can be used in the context of the present invention in combination, advantageously with a synergistic effect, with the conjugated fatty acids are advantageously glycine, sugars and / or peptides of lupine, sugars and / or peptides described in patent applications FR0404635 and
- the soothing agents that can be used in combination, advantageously with a synergistic effect, with the conjugated fatty acids are advantageously alpha bisabolol, licorice derivatives, enoxolone (3-beta-hydroxy-1-oxo-olean acid). 12-en-30-oic, CAS No. 471-53-4).
- the kératorégulados that can be used in combination with the conjugated fatty acids are advantageously alpha hydroxy acids and their derivatives.
- the keratolytics that may especially be used in combination with the conjugated fatty acids are salicylic acid and its derivatives: lipohydroxyacids.
- the antioxidant agents that may be used in combination with the conjugated fatty acids are advantageously vitamins (C, E), trace elements (copper, zinc, selenium) and anti-oxidant enzymes.
- the growth factors that can advantageously be used in combination with a synergistic effect with the conjugated fatty acids are advantageously becaplermine and TGF-beta (Transforming Growth Factor beta).
- the healing agents which can advantageously be used in combination with a synergistic effect, with the conjugated fatty acids are advantageously vitamin A, panthenol, avocadofurane®, zinc oxide, magnesium, silicon, acid madécassique or Asian, the polysaccharides of all origins and in particular of marine thermal origin or the derivatives of pearl oyster.
- the medicaments that can be used in the context of the present invention, in combination, advantageously with a synergistic effect, with the conjugated fatty acids are advantageously the drugs, suitable for administration for the topical or oral route, for the prevention and / or the treatment of atopy (corticosteroids, emollients, immunomodulators), acne (antibiotics, benzoyl peroxide, topical and oral retinoids, azelaic acid, vitamin PP, zinc, cyclins), eczema (immunomodulators, emollients, fish oil, borage, meadow and pro - biotic) or psoriasis (corticosteroids, calcipotriol, calcitriol, tazarotene, cade oil, acitretin, PUVA therapy, vitamin D derivatives).
- the drug may also include antibiotic peptide stimulants such as avocado sugars and avocado peptides.
- anti-inflammatory agents that can be used in combination, advantageously with a synergistic effect, with the conjugated fatty acids are advantageously steroidal anti-inflammatory agents (AIS), such as steroids, or non-steroids (NSAIDs) and anti-inflammatory agents.
- AIS steroidal anti-inflammatory agents
- NSAIDs non-steroids
- Cox 2 celecoxib
- the restructuring agents of the cutaneous barrier which make it possible to stimulate the synthesis of the key lipids of the epidermis, and which can be used in combination, advantageously with a synergistic effect, with the conjugated fatty acids are advantageously concentrates of sunflower, even more advantageously concentrates.
- linoleic sunflower seeds such as the active ingredient marketed by Laboratoires Expanscience, Soline® (see international application WO 01/21150), vegetable oil unsaponifiables, such as Avocadofurane® (see international application WO 01 / 21150), PPAR agonists alpha, beta, gamma and delta (rosiglitazone, pioglitazone).
- the RXR and RAR agonists vitamin D receptors.
- the antifungal compounds that can be used in combination with the conjugated fatty acids are advantageously Peconazole, ketoconazole and climbazole. It is also possible to use reducing agents such as ichthyol in combination.
- the antiseptic preservatives that can be used in combination, advantageously with a synergistic effect, with the conjugated fatty acids may be triclosan, chlorhexidine or quaternary ammoniums.
- the immunomodulators which can be used in combination, advantageously with a synergistic effect, with the conjugated fatty acids are advantageously tacrolimus, pimecrolimus and oxazolines.
- oxazolines which can be used in the context of the present invention are advantageously oxazolines chosen from the group consisting of 2-undecyl-4-hydroxymethyl-4-methyl-1,3-oxazoline and 2-undecyl-4,4-dimethylamine. dimethyl-1,3-oxazoline, the
- the compounds containing vegetable oil unsaponifiables that can be used in combination, advantageously with a synergistic effect, with the conjugated fatty acids are advantageously chosen from the group consisting of avocado furan lipids, avocado and soya unsaponifiables. , lupine oil concentrates, sunflower oil concentrates and mixtures thereof.
- the furanic lipids of avocado that can be used in the context of the present invention are advantageously natural 2-alkyl furans, in particular the active Avocadofurane® sold by Laboratoires Expanscience, obtainable by the process described in international application WO 01 / 21605.
- the avocado and soya unsaponifiables which can be used in combination with the conjugated fatty acids are advantageously a mixture of unsaponifiables of furanic avocado and unsaponifiable soya, in a respective ratio of approximately 1 / 3-2 / 3 .
- the unsaponifiable avocado and soya are even more advantageously the product Piasclédine®, marketed by Laboratoires Expanscience.
- the lupine oil concentrates that may be used are advantageously concentrates obtained by molecular distillation of lupine oil, advantageously sweet white lupine oil, such as those described in the international application WO 98/47479. They advantageously contain about 60% by weight of unsaponifiables.
- the sunflower oil concentrates that can be used are advantageously linoleic sunflower concentrates, such as the active ingredient marketed by Laboratoires Expanscience, Soline® (see the international application WO
- the source of conjugated fatty acid is a lipid extract of at least one plant selected from the group consisting of plants of the family Cucurbitaceae, Punicaceae, Bignoniaceae, Euphorbiaceae, Composites (Asteraceae), Balsaminaceae, Rosaceae, Chrysobalanaceae, Ricinocarpus and Chilopsis.
- the conjugated fatty acid source is a lipid extract of at least one plant selected from the group consisting of green, white, pearly and wild Mormordica, Catalpa, Peerites, Euphorbia, Parinarium, Licania, Parinarium, Calendula, Punica, Pomegranate, Chinese Wood, Balsam, Trichosanthes and Centrarus, Jacaranda.
- the source of alpha-eleostearic acid is advantageously virgin and / or refined oils of at least one plant selected from the group consisting of Momordica charantia, Aleuritippo montana and Aleuritippo fordii, Parinarium montanum, Parinarium excelsum , Parinarium macrophyllum, Parinarium holstii, Licania rigida and Ricinocarpus bowmanii.
- the source of catalpic acid is advantageously virgin and / or refined oils of at least one plant selected from the group consisting of Catalpa ovata, Catalpa hignoniodes and Chilopsis linearis.
- the source of calandic acid is advantageously a virgin and purified oil of Calendula officinalis.
- the source of punicic acid is advantageously virgin and / or refined oils of at least one plant selected from the group consisting of Punica granatum, Trichosanthes nervifolia and Momordica balsamina.
- the source of beta-eleostearic acid is advantageously a virgin and purified oil of Centratus ruber.
- the source of licanic acid is advantageously Oitica, Licania or Parinarium oil.
- the virgin and / or refined oils mentioned above do not contain any trace of detectable protein.
- the source of alpha-eleostearic acid and catalpic acid is more particularly a lipid extract of Mormordica seeds, advantageously seeds of Momordica charantia.
- the composition according to the invention administered topically comprises 0.001% to 50% by weight of a lipid extract of momordic seeds, advantageously 0.001% to 50% by weight, even more advantageously 2 at 20% by weight, of a lipid extract of Momordica charantia seeds, relative to the total weight of the composition.
- the composition according to the invention administered orally comprises 0.001% to 100% by weight of a lipid extract of momordic seeds, advantageously 0.001% to 100% by weight of lipid extract seed of Momordica charantia, more advantageously 1 to 50% by weight of a lipid extract of Momordica charantia seeds, relative to the total weight of the composition.
- the lipid extract of Momordica charantia seeds advantageously comprises at least 20% by weight of alpha-eleostearic acid and of catalpic acid, advantageously at least 40% by weight of alpha-eleostearic acid and of catalpic acid, and even more advantageously about 45% by weight of alpha-eleostearic acid and catalpic acid.
- the mixture of alpha-eleostearic acid and catalpic acid advantageously comprises at least 50% by weight of alpha-eleostearic acid, advantageously at least 90% by weight of alpha-eleostearic acid, still more advantageously at least 98% by weight. weight of alpha-eleostearic acid.
- the Margoze of the genus Momordica charantia is a tropical cucurbit that comes from India but is also grown on the island of Reunion. It is an annual herb, which can give lianas 2 meters long, and whose oblong fruits of green color contain flat seeds. The lipid content of these seeds is about 30% by weight.
- the lipid extract of Momordica charantia is obtainable by a process consisting in extracting the total lipids from the seeds of Momordica charantia previously dried and crushed, using a solvent of the oils, then evaporating said solvent or according to the process of extracting the lipids from the seeds of Momordica charantia by mechanical pressure of the seeds cold.
- the oil of the seeds of Momordica charantia can be obtained according to the process of extracting the total lipids from the seeds of cucurbitaceae previously dried and crushed, with the aid of a solvent of the oils, then to evaporate the solvent.
- the seeds of Momordica charantia according to the present invention are milled for example using a roller mill or hammers.
- the oil solvent used to extract the total lipids from the oil-forming seeds is a conventional organic lipid extraction solvent.
- the solvent is advantageously chosen from the group consisting of aliphatic alkanes, aromatic alkanes, aliphatic alcohols and their halogenated derivatives. Even more advantageously according to the present invention, the organic solvent is hexane.
- the extraction of the total lipids from the seeds of Momordica charantia is advantageously carried out by a Soxhlet extraction which is a technology well known to those skilled in the art.
- the organic solvent is evaporated, preferably by evaporation under vacuum.
- the seed oil of Momordica charantia can be obtained by the process of extracting the lipids from cucurbitaceae seeds by mechanical pressure of the cold seeds, advantageously with using a continuous screw press, to conduct, after filtration, virgin oils of first pressure.
- the lipid extracts of the other plants according to the present invention are capable of being obtained by methods similar to the processes described above.
- the oils of the plant (s) according to the present invention can be used raw or refined.
- refining is understood to mean the unitary lipid purification operations of plant origin well known to those skilled in the art, among which may be mentioned in particular chemical neutralization, degumming, decolourisation, deodorization. and frigmentation.
- the oils extracted from Momordica charantia seeds have the additional advantage of being cosmetically acceptable, non-aggressive to the skin, non-toxic and hypoallergenic.
- Example 1 Cosmetic Formulations Based on a Momordica Charantia Extract
- QSP Sufficient Quantity For
- QS Sufficient quantity (Anti-acne cream n ° 2
- QSP Sufficient Quantity For
- QS Sufficient quantity
- Example 4 Study of the effect of an extract of Momordica charantia in a model of mechanically induced cutaneous inflammation (shaving) in the wild Balb / c mouse. Protocol
- mice Female Balb / c mice aged 6 weeks. Each group of mice consists of 8 mice. At OJ, the mice are shaved on their backs
- Momordica charantia is applied at a dose of 2%, twice daily. At day 4, ie after 2 days of topical application of Momordica charantia extract, skin biopsies are performed. Histological analysis is performed by staining the haematoxylin / eosin sections.
- the extract of Momordica charantia used includes by weight:
- the vehicle-treated group (acetone / olive oil) has a skin thickness at J4, statistically higher than that of the group treated with 2% Momordica charantia extract for 2 days ( Figure 1).
- an extract of Momordica charantia has anti-inflammatory properties in a mechanically induced skin inflammation model in mice.
- FIG. 1 represents, on the ordinate, the thickness of the skin, in microns at day 4, measured in each of the treated groups (vehicle: acetone / olive oil or Momordica charantia extract).
- Example 5 Study of the effect of an extract of Momordica charantia, applied topically at the dose of 2% in the Balb / c wild-type mouse, on the proliferation of keratinocytes. Protocol The study was performed on female Balb / c mice aged 6 weeks.
- mice Each group of mice consists of 8 mice. At OJ, the mice are shaved on the back (surface of about 2 cm 2 ). At J2, a first group of mice is used to obtain the basic values.
- Momordica charantia extract is applied at 2% for 30 days, twice daily.
- the extract of Momordica charantia used is the same as that of Example 4.
- FIG. 2 represents the percentage of Ki-67 positive cells relative to the total number of cells measured at J30 in each of the treated groups (vehicle: acetone / olive oil or Momordica charantia extract).
- an extract of Momordica charantia causes an increase in the proliferation of keratinocytes in vivo in the mouse.
- Momordica charantia extract has healing and eutrophic properties.
- the said eutrophic properties are advantageous especially in the context of cutaneous pathologies characterized by a skin barrier disorder.
- the extract of Momordica charantia used is the same as that of Example 4. Culture conditions
- Momordica charantia extract does not induce any interference with radiolabeling.
- the reference molecule, cerulin (FAS inhibitor, Fatty Acid Synthase) tested at 10 ⁇ M inhibits the incorporation of acetate (75% inhibition / control). This result validates the test.
- the extract of Momordica charantia tested at 2 and 20 ppm significantly reduces the incorporation of acetate into the lipids (respectively 25 and 30% of the control).
- Momordica charantia extract shows a significant inhibitory activity of lipid synthesis.
- the extract of Momordica charantia is therefore capable of inhibiting lipogenesis in human adipocytes in culture. This experience shows quite unexpectedly the interest of the product in the management of cellulite.
- FIG. 3 attached illustrates the effect of Momordica charantia extract on the incorporation of radiolabelled acetate into adipocyte lipids. The results are significant (p ⁇ 0.01).
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Abstract
Description
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Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR0408230A FR2873295B1 (fr) | 2004-07-26 | 2004-07-26 | Utilisation d'au moins un triene d'acide gras conjugue pour la preparation d'un medicament destine au traitement de l'inflammation |
PCT/FR2005/001859 WO2006021660A1 (fr) | 2004-07-26 | 2005-07-20 | Utilisation d'au moins un triene d'acide gras conjugue pour la preparation d'un medicament destine au traitement de l'inflammation |
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Publication Number | Publication Date |
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EP1786384A1 true EP1786384A1 (fr) | 2007-05-23 |
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ID=34949333
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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EP05790724A Withdrawn EP1786384A1 (fr) | 2004-07-26 | 2005-07-20 | Utilisation d'au moins un triene d'acide gras conjugue pour la preparation d'un medicament destine au traitement de l'inflammation |
Country Status (4)
Country | Link |
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US (1) | US20080045594A1 (fr) |
EP (1) | EP1786384A1 (fr) |
FR (1) | FR2873295B1 (fr) |
WO (1) | WO2006021660A1 (fr) |
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US8343753B2 (en) | 2007-11-01 | 2013-01-01 | Wake Forest University School Of Medicine | Compositions, methods, and kits for polyunsaturated fatty acids from microalgae |
CA2704371A1 (fr) * | 2007-11-01 | 2009-05-07 | Wake Forest University School Of Medicine | Compositions et procedes de prevention et de traitement de maladies touchant des mammiferes |
FR2929515B1 (fr) * | 2008-04-08 | 2014-03-07 | Lr Beva | Utilisation d'acides gras comprenant un diene conjugue n-5cis, n-7trans ou un triene conjugue n-5cis, n-7trans, n-9cis en tant que medicament |
GB0814105D0 (en) * | 2008-08-01 | 2008-09-10 | Springdale Sustainable Develop | Composition for accelerated production of collagen |
JP5542143B2 (ja) | 2008-10-24 | 2014-07-09 | ユニリーバー・ナームローゼ・ベンノートシヤープ | A.indicaおよびm.charantiaまたはs.indicumの抽出物を含む外用組成物 |
GB0902040D0 (en) * | 2009-02-06 | 2009-03-11 | Seeds Lp | Composition for treatment of skin |
FR2949044B1 (fr) | 2009-08-12 | 2021-05-07 | Expanscience Lab | Composition comprenant une fraction d'insaponifiable |
KR100985719B1 (ko) | 2009-09-15 | 2010-10-06 | (주)지에프씨 | 노나무와 무궁화 추출물을 유효성분으로 하는 화장료 조성물 |
FR2984730A1 (fr) * | 2011-12-22 | 2013-06-28 | Diverchim | Nouvelles compositions cosmetiques anti-age et depigmentantes |
IT201700037319A1 (it) | 2017-04-05 | 2018-10-05 | Moss S P A | Composizione naturale per uso in ginecologia |
EP3714029A1 (fr) | 2017-11-22 | 2020-09-30 | Moss S.p.A. | Procédé de production d'une huile végétale ozonée |
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AU616502B2 (en) * | 1988-04-22 | 1991-10-31 | Medvet Science Pty. Ltd. | Treatment of inflammatory disorders in humans |
FR2762512B1 (fr) * | 1997-04-24 | 2000-10-13 | Pharmascience Lab | Compositions a base d'huile de lupin, notamment a base d'huile de lupin et d'huile de germe de ble et leur utilisation en cosmetologie, en pharmacie et en tant que complement alimentaire |
KR100480958B1 (ko) * | 1999-07-15 | 2005-04-07 | 칸나 푸시파 | 모모르디카 카란티아 엘 오일, 그의 제조 방법 및 용도 |
FR2798667B1 (fr) * | 1999-09-22 | 2001-12-21 | Pharmascience Lab | Procede d'extraction des composes furaniques et alcools gras polyhydroxyles de l'avocat, composition a base de et utilisation de ces composes en therapeutique, cosmetique et alimentaire |
CA2408357A1 (fr) * | 2000-05-09 | 2001-11-15 | Bioriginal Food & Science Corp. | Production d'acides linoleiques et d'acides linoleiques conjugues dans des plantes |
EP1407679A4 (fr) * | 2001-06-21 | 2005-06-15 | Kyowa Hakko Kogyo Kk | Procede permettant de produire un extrait vegetal contenant une poudre vegetale |
FR2826579B1 (fr) * | 2001-06-29 | 2005-08-05 | Pharmascience Lab | Composition cosmetique contenant au moins une huile extraite de graines de cucurbitacees, son utilisation cosmetique, therapeutique et alimentaire |
DE10158046A1 (de) * | 2001-11-27 | 2003-06-05 | Basf Ag | Formulierung für den Einsatz in Lebensmitteln, Nahrungsergänzungsmitteln, Futtermitteln, Futterzusatzstoffen, pharmazeutischen und kosmetischen Zubereitungen sowie Verfahren zu deren Herstellung |
CA2486967A1 (fr) * | 2002-05-24 | 2003-12-04 | Neopharm, Inc. | Compositions de cardiolipine, leurs procedes de preparation et d'utilisation |
US20040235925A1 (en) * | 2002-12-17 | 2004-11-25 | Pharmacia Corporation | Method for the treatment, prevention, or inhibition of a CNS disorder and/or pain and inflammation using a combination of duloxetine, venlafaxine or atomoxetine and a cyclooxygenase-2 selective inhibitor and compositions thereof |
-
2004
- 2004-07-26 FR FR0408230A patent/FR2873295B1/fr not_active Expired - Lifetime
-
2005
- 2005-07-20 EP EP05790724A patent/EP1786384A1/fr not_active Withdrawn
- 2005-07-20 WO PCT/FR2005/001859 patent/WO2006021660A1/fr active Application Filing
- 2005-07-20 US US11/572,769 patent/US20080045594A1/en not_active Abandoned
Non-Patent Citations (1)
Title |
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See references of WO2006021660A1 * |
Also Published As
Publication number | Publication date |
---|---|
WO2006021660A1 (fr) | 2006-03-02 |
FR2873295B1 (fr) | 2006-12-01 |
FR2873295A1 (fr) | 2006-01-27 |
WO2006021660A8 (fr) | 2006-04-27 |
US20080045594A1 (en) | 2008-02-21 |
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