WO2003061618A1 - Method for obtaining an active principle from agarum cribosum, particularly for prevention of pigmentation - Google Patents

Method for obtaining an active principle from agarum cribosum, particularly for prevention of pigmentation Download PDF

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Publication number
WO2003061618A1
WO2003061618A1 PCT/FR2003/000159 FR0300159W WO03061618A1 WO 2003061618 A1 WO2003061618 A1 WO 2003061618A1 FR 0300159 W FR0300159 W FR 0300159W WO 03061618 A1 WO03061618 A1 WO 03061618A1
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active principle
obtaining
active ingredient
active
pigmentation
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PCT/FR2003/000159
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French (fr)
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Jean-Jacques Paufique
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Societe Industrielle Limousine D'application Biologique (Silab)
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
    • 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
    • A61K8/9706—Algae
    • A61K8/9711—Phaeophycota or Phaeophyta [brown algae], e.g. Fucus
    • 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
    • A61K2800/74—Biological properties of particular ingredients
    • A61K2800/78—Enzyme modulators, e.g. Enzyme agonists
    • A61K2800/782—Enzyme inhibitors; Enzyme antagonists

Definitions

  • the present invention relates to the obtaining of an active ingredient from an alga known under the name of Agarum cribosum and the use, in cosmetic or dermatological compositions of this active ingredient.
  • the application relates more particularly to the fight against skin pigmentation.
  • the invention also covers cosmetic compositions including this active principle.
  • the color of the skin in humans is mainly due to the concentration in keratinocytes of the melanin produced by the melanocytes. These melanocytes synthesize melanin.
  • Tyrosinase is an enzyme involved in the reaction leading to the production of melanin.
  • the quantity of tyrosinase is appreciably constant from one person to another and yet the rate of melanin varies. It is concluded from this that variations in the activity of the melanogenesis reaction are caused by modifications in the activity of the essential enzyme, namely tyrosinase.
  • French patent application No. 2,655,268 provides for the obtaining of compositions having an anti-radical activity from algae of the variety Fucus vesiculosus.
  • the present invention provides for working from algae of the variety Agarum cribosum in order to extract an active ingredient having lightening properties for the pigmentation of the skin.
  • This variety of algae is of the type said laminar screened by the presence of holes in its leaf surface. It is particularly present at sea, in northern Canada.
  • brown alga is rich in marine polyphenols called phlorotannins.
  • the present invention provides for the use of the active principle extracted from this alga, Agarum cribosum, which has, in an unknown and surprising manner, anti-tyrosinase activity. This property can be used to at least partially block melanogenesis.
  • the present invention provides a process for obtaining an active ingredient from Agarum cribosum making it possible to combat pigmentation, in particular this pigmentation localized in the form of senescence spots, and presents tests showing the effectiveness of this active ingredient in its application.
  • the process consists of the following stages:
  • the hydrolysis conditions are: temperature between 45 ° C and 70 ° C, duration between 1 and 4 hours and a pH in a range of 2.0 to 7.0,
  • the solubilization medium is advantageously a water / butylene glycol mixture.
  • the concentration is advantageously carried out by ultrafiltration.
  • the inactivation of the enzymatic activity it is obtained thermally or by modification of the pH.
  • the dry matter content is between 5 and 100 g / 1, more particularly between 5 and 50 g / 1, the preferred dry matter content is between 16 and 32 g / 1.
  • This rate is obtained by passing through the oven at 105 ° C until a constant weight is obtained.
  • the pH value is between 4.0 and 8.0, more particularly between
  • the value is determined by the potentiometric method, at room temperature.
  • Polyphenolic compounds form colored complexes in the presence of potassium ferricyanide.
  • the intensity of the corresponding peaks can be detected at 715 nm.
  • the content of polyphenolic compounds in the solution analyzed can then be determined, the results being expressed in grams of gallic acid. in the extract thus analyzed, the value is greater than 0.5 g / 1.
  • the determination is semi-quantitative. It consists in putting the phlorotannins (1,3,5 substituted and 1,3 substituted form) in the presence of di ethoxybenzaldehyde (DMBA), which gives a specific garnet coloration at 510 nm.
  • DMBA di ethoxybenzaldehyde
  • the optical density is measured at 475 nm.
  • the protocol consists in treating reconstructed pigmented skins of the type sold under the name SkinEthic®. With emulsions containing 2 or 4% of active ingredient, for 4 days, After treatment, the melanin of these epidermis is quantified. The results are expressed in // g / ml of melanin and the depigmenting activity is determined relative to the control epidermis.
  • the active ingredient is introduced into a white emulsion with a 5% formulation.
  • Chromameter which allows, by digital conversion of colors in the spectrum of human vision, to indicate three parameters:
  • - L luminance, corresponding to the clarity, going from dark to pale.
  • - a chrominance, corresponding to variations in the area from green to red
  • ITA Individual Typological Angle
  • the ⁇ test focused on female volunteers aged 45 to 65 after 56 days of twice-daily application.
  • One hand is treated with white cream containing 5% of active ingredient and the other hand is treated with a white placebo cream.
  • the measurements are performed using the Chromameter on three senescence tasks.
  • the Active ingredient thus obtained, rich in polyphenols, helps fight against unsightly pigmentation of the skin.
  • this active principle can be incorporated in any suitable galenical form: cream, ointment, lotion, aqueous or fatty emulsion, milk, solution or gel.
  • the active principle can be introduced at a rate of 0.5 to 20%.
  • Stabilizers can be added so as to eliminate any risk of phase shift when necessary.
  • dosage forms may provide for the addition of perfume or smoothing agents or facilitating penetration through the epidermis, this at the discretion of the formulator.

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  • Life Sciences & Earth Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Dermatology (AREA)
  • Botany (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Cosmetics (AREA)

Abstract

The invention relates to a method for obtaining an active principle for cosmetic use as a depigmentation agent, an inhibitor of tyrosinase activity and inhibitor of melanin synthesis, characterised in that the above is obtained from the algae of the species Agarum cribosum. The invention further relates to the active principle obtained, the cosmetic compositions and use thereof as depigmentation and brightening agent.

Description

PROCEDE Ù 'OBTENTION ù 'UN PRINCIPE ACTIF A PARTIR Ù 'Agarum cribosum, NOTAMMENT POUR LUTTER CONTRE LA PIGMENTATION PROCESS OB 'OBTAINING INC AN ACTIVE INGREDIENT FROM Ag Agarum cribosum, ESPECIALLY TO FIGHT AGAINST PIGMENTATION
La présente invention concerne l'obtention d'un principe actif à partir d'une algue connue sous le nom d' Agarum cribosum et l'utilisation, dans des compositions cosmétiques ou dermatologiques de ce principe actif. L'application concerne plus particulièrement la lutte contre la pigmentation de la peau. L'invention couvre aussi des compositions cosmétiques incluant ce principe actif.The present invention relates to the obtaining of an active ingredient from an alga known under the name of Agarum cribosum and the use, in cosmetic or dermatological compositions of this active ingredient. The application relates more particularly to the fight against skin pigmentation. The invention also covers cosmetic compositions including this active principle.
La couleur de la peau chez l'homme est principalement due à la concentration en kératinocytes de la mélanine produite par les mélanocytes. Ces mélanocytes synthétisent la mélanine. La tyrosinase est une enzyme qui intervient dans la réaction conduisant à la production de mélanine. Or la quantité de tyrosinase est sensiblement constante d'une personne à une autre et pourtant le taux de mélanine varie. On en conclut que les variations de l'activité de la réaction de la mélanogénèse sont engendrées par des modifications de l'activité de l'enzyme essentielle à savoir la tyrosinase. On connaît des utilisations d'extraits d'algues pour la préparation de compositions cosmétiques, pharmaceutiques ou alimentaires. Ainsi la demande de brevet français N° 2 655 268 prévoit l'obtention de compositions ayant une activité anti-radicalaire à partir d'algues de la variété Fucus vesiculosus.The color of the skin in humans is mainly due to the concentration in keratinocytes of the melanin produced by the melanocytes. These melanocytes synthesize melanin. Tyrosinase is an enzyme involved in the reaction leading to the production of melanin. However the quantity of tyrosinase is appreciably constant from one person to another and yet the rate of melanin varies. It is concluded from this that variations in the activity of the melanogenesis reaction are caused by modifications in the activity of the essential enzyme, namely tyrosinase. There are known uses of algae extracts for the preparation of cosmetic, pharmaceutical or food compositions. Thus, French patent application No. 2,655,268 provides for the obtaining of compositions having an anti-radical activity from algae of the variety Fucus vesiculosus.
La présente invention prévoit de travailler à partir d'algues de la variété Agarum cribosum en vue d'extraire un principe actif ayant des propriétés éclaircissantes de la pigmentation de la peau. Cette variété d'algues est du type laminaire dit criblé par la présence de trous dans sa surface foliaire. Elle est présente notamment en mer, au nord du Canada.The present invention provides for working from algae of the variety Agarum cribosum in order to extract an active ingredient having lightening properties for the pigmentation of the skin. This variety of algae is of the type said laminar screened by the presence of holes in its leaf surface. It is particularly present at sea, in northern Canada.
Cette algue dite brune est riche en polyphénols marins dits phlorotannins .This so-called brown alga is rich in marine polyphenols called phlorotannins.
On connaît de nombreuses actions de ces polyphénols, spécifiquement des propriétés antioxydantes mais aussi antibactériennes.Many actions of these polyphenols are known, specifically antioxidant but also antibacterial properties.
Afin de lutter contre la pigmentation de la peau, notamment lorsqu'elle est localisée, la présente invention prévoit une utilisation du principe actif extrait de cette algue, Agarum cribosum , qui présente de façon inconnue et surprenante, une activité anti-tyrosinase. Cette propriété peut être mise à profit pour bloquer au moins partiellement la mélanogénèse.In order to combat pigmentation of the skin, in particular when it is localized, the present invention provides for the use of the active principle extracted from this alga, Agarum cribosum, which has, in an unknown and surprising manner, anti-tyrosinase activity. This property can be used to at least partially block melanogenesis.
On connaît l'effet disgracieux des tâches dites de sénescence qui apparaissent avec l'âge, en particulier sur les parties exposées de la peau, mains, visage ou cou.We know the unsightly effect of so-called senescence tasks that appear with age, in particular on the exposed parts of the skin, hands, face or neck.
La présente invention propose un procédé d'obtention d'un principe actif à partir d' Agarum cribosum permettant de lutter contre la pigmentation, notamment cette pigmentation localisée sous forme de tâches de sénescence, et présente des tests montrant l'efficacité de ce principe actif dans son application.The present invention provides a process for obtaining an active ingredient from Agarum cribosum making it possible to combat pigmentation, in particular this pigmentation localized in the form of senescence spots, and presents tests showing the effectiveness of this active ingredient in its application.
Le procédé est maintenant décrit en détail et le principe actif est caractérisé en lui-même tandis que les résultats obtenus sont regroupés dans des tableaux au fur et à mesure de la description.The process is now described in detail and the active principle is characterized in itself while the results obtained are grouped in tables as the description progresses.
PROCÉDÉ LV OBTENTIONLV PROCESS OBTAINING
Le procédé consiste en la succession des étapes suivantes :The process consists of the following stages:
- solubilisation de poudre d'algues de la variété Agarum cribosum dans un mélange eau/alcool.- solubilization of algae powder of the Agarum cribosum variety in a water / alcohol mixture.
- hydrolyse enzymatique- enzymatic hydrolysis
- décantation pour séparer les phases soluble et insoluble- decantation to separate the soluble and insoluble phases
- inactivation des enzymes - refroidissement à température ambiante,- inactivation of enzymes - cooling to room temperature,
- concentrations des phlorotannins et des protéines, et- concentrations of phlorotannins and proteins, and
- stérilisation de la phase active concentrée.- sterilization of the concentrated active phase.
Les conditions d'hydrolyse sont : température comprise entre 45°C et 70°C, durée comprise entre 1 et 4 heures et un pH compris dans une plage de 2,0 à 7,0,The hydrolysis conditions are: temperature between 45 ° C and 70 ° C, duration between 1 and 4 hours and a pH in a range of 2.0 to 7.0,
Le milieu de solubilisation est avantageusement un mélange eau/butylène glycol. La concentration est réalisée de façon avantageuse par ultraf iltration.The solubilization medium is advantageously a water / butylene glycol mixture. The concentration is advantageously carried out by ultrafiltration.
Quant à l'inactivation de l'activité enzymatique, elle est obtenue par voie thermique ou par modification du pH.As for the inactivation of the enzymatic activity, it is obtained thermally or by modification of the pH.
PRINCIPE ACTIF 1/ Taux de matière sècheACTIVE INGREDIENT 1 / Dry matter content
Le taux de matière sèche est compris entre 5 et 100 g/1, plus particulièrement entre 5 et 50 g/1, le taux de matière sèche préférentiel est compris entre 16 et 32 g/1.The dry matter content is between 5 and 100 g / 1, more particularly between 5 and 50 g / 1, the preferred dry matter content is between 16 and 32 g / 1.
Ce taux est obtenu par passage à l'étuve à 105°C jusqu'à obtention d'un poids constant.This rate is obtained by passing through the oven at 105 ° C until a constant weight is obtained.
2/ pH La valeur du pH est comprise entre 4,0 et 8,0 plus particulièrement entre2 / pH The pH value is between 4.0 and 8.0, more particularly between
5,0 et 6,0.5.0 and 6.0.
La valeur est déterminée par la méthode potentiométrique, à température ambiante.The value is determined by the potentiometric method, at room temperature.
3/ Teneur en polyphénols totaux3 / Content of total polyphenols
Les composés polyphénoliques forment des complexe colorés en présence de ferricyanure de potassium. L'intensité des pics correspondants peut être détectée à 715 nm. En comparant ces valeurs à une courbe étalon obtenue à partir d'une gamme étalon d'acide gallique allant de 0,04 à 0,12 g/1. On peut alors déterminer la teneur en composés polyphenoliques de la solution analysée, les résultats étant exprimés en grammes d'acide gallique. bans l'extrait ainsi analysé, la valeur est supérieure à 0,5 g/1 .Polyphenolic compounds form colored complexes in the presence of potassium ferricyanide. The intensity of the corresponding peaks can be detected at 715 nm. By comparing these values to a standard curve obtained from a standard range of gallic acid from 0.04 to 0.12 g / 1. The content of polyphenolic compounds in the solution analyzed can then be determined, the results being expressed in grams of gallic acid. in the extract thus analyzed, the value is greater than 0.5 g / 1.
Elle est plus particulièrement comprise entre 0,5 g/1 et 10,0 g/1It is more particularly between 0.5 g / 1 and 10.0 g / 1
4/ Identification des phlorotannins4 / Identification of phlorotannins
La détermination est semi-quantitative. Elle consiste à mettre les phlorotannins ( forme 1,3,5 substitués et 1,3 substitués) en présence de di éthoxybenzaldéhyde (DMBA), ce qui donne une coloration grenat spécifique à 510 nm.The determination is semi-quantitative. It consists in putting the phlorotannins (1,3,5 substituted and 1,3 substituted form) in the presence of di ethoxybenzaldehyde (DMBA), which gives a specific garnet coloration at 510 nm.
La densité optique de cette solution est mesurée en fonction de la concentration de principe actif. On obtient les résultats suivants :The optical density of this solution is measured as a function of the concentration of active ingredient. The following results are obtained:
Principe Actif Densité Optique Teneur en phlorotanninsActive Principle Optical Density Phlorotannin content
0,5% 014 Teneur moyenne0.5% 014 Average content
1,5% 0,17 Teneur moyenne1.5% 0.17 Average content
5,0% 0,29 Teneur forte5.0% 0.29 High content
10,0% 0,49 Teneur très forte10.0% 0.49 Very high content
EFFET DEPIGMENTANT 1/ Activité anti-tyrosinaseDEPIGMENTING EFFECT 1 / Anti-tyrosinase activity
L'effet anti-tyrosinase du principe actif est mesuré par la mise en œuvre du protocole suivant :The anti-tyrosinase effect of the active ingredient is measured by implementing the following protocol:
- dans une solution de L-DOPA, dihydroxyphénylalanine, (2mM), on ajoute 20μl de tyrosinase et 200 μl de principe actif, - on effectue un blanc avec de l'eau osmosée, et- in a solution of L-DOPA, dihydroxyphenylalanine, (2mM), 20 μl of tyrosinase and 200 μl of active principle are added, - a blank is made with osmosis water, and
- on mesure la densité optique à 475 nm.- the optical density is measured at 475 nm.
La formule suivante est utilisée o^ec DO comme abréviation de Densité Optique, to pour temps de départ, t_ pour temps de réaction et PA pour principe actif :The following formula is used o ^ ec DO as an abbreviation for Optical Density, to for start time, t_ for reaction time and PA for active principle:
(DOt-DOtσ)Blanc - (DOt-DOt0)PA(DOt-DOt σ ) White - (DOt-DOt 0 ) PA
% activité anti-tyrosinase =% anti-tyrosinase activity =
(DOt-DOtσ)Blanc(Dot-DOtσ) White
Cette formule donne les résultats regroupés dans le tableau qui suit :This formula gives the results grouped in the following table:
Figure imgf000006_0001
Figure imgf000006_0001
On constate une inhibition de 100 % de l'activité de la tyrosinase dès 2,0 % de principe actif.There is a 100% inhibition of the activity of tyrosinase from 2.0% of active ingredient.
2/ Etude ex vivo des effets dépigmentants Le protocole consiste à traiter des peaux reconstruites pigmentées du type commercialisée sous la dénomination SkinEthic®.avec des émulsions contenant 2 ou 4 % de principe actif, pendant 4 jours, Après traitement, on quantifie la mélanine de ces épidermes. Les résultats sont exprimés en //g/ml de mélanine et l'activité dépigmentante est déterminée par rapport à I epiderme témoin.2 / Ex vivo study of depigmenting effects The protocol consists in treating reconstructed pigmented skins of the type sold under the name SkinEthic®. With emulsions containing 2 or 4% of active ingredient, for 4 days, After treatment, the melanin of these epidermis is quantified. The results are expressed in // g / ml of melanin and the depigmenting activity is determined relative to the control epidermis.
Figure imgf000007_0001
Figure imgf000007_0001
3/ Etude cutanée des effets dépigmentants3 / Skin study of depigmenting effects
Cette étude porte sur les modifications de la couleur des tâches de sénescence sur le dos de la main de volontaires .This study focuses on the changes in the color of the spots on the back of the hand of volunteers.
Le principe actif est introduit dans une émulsion blanche avec une formulation à 5 % .The active ingredient is introduced into a white emulsion with a 5% formulation.
La mesure colorimétrique est réalisée à l'aide d'un appareillage du commerce connue sous la dénomination Chromamètre qui permet, par conversion numérique des couleurs dans le spectre de la vision humaine, d'indiquer trois paramètres :The colorimetric measurement is carried out using a commercial apparatus known under the name Chromameter which allows, by digital conversion of colors in the spectrum of human vision, to indicate three parameters:
- L : luminance, correspondant à la clarté, allant du sombre au pâle. - a : chrominance, correspondant aux variations dans la zone du vert au rouge- L: luminance, corresponding to the clarity, going from dark to pale. - a: chrominance, corresponding to variations in the area from green to red
- b : chrominance, correspondant aux variations dans la zone du bleu au jaune Dans la présente étude, ce sont les paramètres de luminance L et de chrominance b et l'Angle Typologique Individuel (ITA) qui sont retenus pour déterminer la pigmentation de la peau. L'ITA est obtenu avec la formule :- b: chrominance, corresponding to the variations in the blue to yellow zone In the present study, it is the parameters of luminance L and chrominance b and the Individual Typological Angle (ITA) which are used to determine the pigmentation of the skin. . The ITA is obtained with the formula:
ITA = [ Arc tan (L- 50)/b]x 180/ πITA = [Arc tan (L- 50) / b] x 180 / π
Plus ITA est élevé , plus la peau est claire. Le test α porté sur des volontaires féminins âgés de 45 à 65 ans après 56 jours d'application biquotidienne.The higher the ITA, the lighter the skin. The α test focused on female volunteers aged 45 to 65 after 56 days of twice-daily application.
Une main est traitée avec la crème blanche à 5 % de principe actif et l'autre main traitée avec une crème blanche placebo. Les mesures sont réalisées à l'aide du Chromamètre sur trois tâches de sénescence.One hand is treated with white cream containing 5% of active ingredient and the other hand is treated with a white placebo cream. The measurements are performed using the Chromameter on three senescence tasks.
Les résultats des moyennes obtenues de la luminance sont indiqués ci-après :The results of the averages obtained from the luminance are indicated below:
Figure imgf000008_0001
Figure imgf000008_0001
On constate ainsi une augmentation de la luminance de 1,92 %.There is thus an increase in luminance of 1.92%.
Les résultats des moyennes obtenues concernant la chrominance b sont indiqués ci-après :The results of the means obtained for chrominance b are shown below:
Figure imgf000008_0002
Figure imgf000008_0002
On constate ainsi une diminution de la chrominance de 4,06 %,There is thus a decrease in chrominance of 4.06%,
Les résultats des moyennes obtenues du paramètre ITA sont indiqués ci- apresThe results of the means obtained from the ITA parameter are shown below.
Figure imgf000008_0003
On constate ainsi une augmentation de l'Angle Typologique Individuel de plus de 11 %, qui est un paramètre essentiel puisqu'il représente le degré de pigmentation de la peau des volontaires. Le principe actif ainsi obtenu, riche en polyphénols, permet de lutter contre la pigmentation disgracieuse de la peau. Afin de pouvoir l'utiliser de façon pratique, ce principe actif peut être incorporé dans toute forme galénique adaptée : crème, onguent, lotion, émulsion aqueuse ou grasse, lait, solution ou gel.
Figure imgf000008_0003
There is thus an increase in the Individual Typological Angle of more than 11%, which is an essential parameter since it represents the degree of pigmentation of the skin of the volunteers. The active ingredient thus obtained, rich in polyphenols, helps fight against unsightly pigmentation of the skin. In order to be able to use it in a practical way, this active principle can be incorporated in any suitable galenical form: cream, ointment, lotion, aqueous or fatty emulsion, milk, solution or gel.
Dans de telles formulations cosmétiques, le principe actif peut être introduit à raison de 0,5 à 20 %.In such cosmetic formulations, the active principle can be introduced at a rate of 0.5 to 20%.
Des stabilisants peuvent être ajoutés en sorte de supprimer tout risque de déphasage lorsque cela est nécessaire.Stabilizers can be added so as to eliminate any risk of phase shift when necessary.
De même, les formes galéniques peuvent prévoir l'adjonction de parfum ou d'agents lissants ou facilitant la pénétration à travers l'épiderme, ceci à la discrétion du formulateur. Similarly, dosage forms may provide for the addition of perfume or smoothing agents or facilitating penetration through the epidermis, this at the discretion of the formulator.

Claims

R E V E N D I C A T I O N S
1. Procédé d'obtention d'un principe actif pour des usages cosmétiques comme agent dépigmentant, inhibiteur de l'activité de la tyrosinase et inhibiteur de la synthèse de la mélanine, caractérisé en ce qu'on réalise cette obtention à partir de l'algue de la variété Agarum cribosum par succession des étapes suivantes :1. Method for obtaining an active ingredient for cosmetic uses as a depigmenting agent, inhibitor of tyrosinase activity and inhibitor of melanin synthesis, characterized in that this is obtained from seaweed of the variety Agarum cribosum by succession of the following stages:
- solubilisation de poudre d'algues de la variété Agarum cribosum dans un mélange eau/alcool,- solubilization of algae powder of the Agarum cribosum variety in a water / alcohol mixture,
- hydrolyse enzymatique,- enzymatic hydrolysis,
- décantation pour séparer les phases soluble et insoluble, - inactivation des enzymes,- decantation to separate the soluble and insoluble phases, - inactivation of enzymes,
- refroidissement à température ambiante,- cooling to room temperature,
- concentrations des phlorotannins, et- concentrations of phlorotannins, and
- stérilisation de la phase active concentrée.- sterilization of the concentrated active phase.
2. Procédé d'obtention selon la revendication 1, caractérisé en ce que l'obtention alcoolique est réalisée dans un mélange eau/butylène glycol.2. Method of obtaining according to claim 1, characterized in that the alcoholic production is carried out in a water / butylene glycol mixture.
3. Procédé d'obtention selon l'une quelconque des revendications précédentes, caractérisé en ce que la température est comprise entre 45°C et 70°C, la durée est comprise entre 1 et 4 heures et le pH est compris dans une plage de 2,0 à 7,0. 3. Method of obtaining according to any one of the preceding claims, characterized in that the temperature is between 45 ° C and 70 ° C, the duration is between 1 and 4 hours and the pH is within a range of 2.0 to 7.0.
4. Principe actif obtenu par la mise en oeuvre du procédé selon l'une des revendications 1 à 3, caractérisé en ce qu'il présente les paramètres suivants :4. Active principle obtained by implementing the method according to one of claims 1 to 3, characterized in that it has the following parameters:
- matière sèche comprise entre 5 et 100 g/1,- dry matter between 5 and 100 g / 1,
- pH compris entre 4,0 et 8,0, et- pH between 4.0 and 8.0, and
- taux de polyphénols totaux supérieur à 0,5 g/1. 5. Principe actif selon la revendication 4, caractérisé en ce qu'il présente les paramètres suivants : - matière sèche comprise entre 5 et 50 g/l , plus particulièrement entre 16 et 32 g/1,- rate of total polyphenols greater than 0.5 g / 1. 5. Active ingredient according to claim 4, characterized in that it has the following parameters: - dry matter between 5 and 50 g / l, more particularly between 16 and 32 g / 1,
- pH compris entre 5,0 et 6,0, et- pH between 5.0 and 6.0, and
- taux de polyphénols totaux compris entre 0,- level of total polyphenols between 0,
5 g/1 et 10,0 g/1. 5 g / 1 and 10.0 g / 1.
6. Composition cosmétique comprenant le principe actif selon l'une des revendications 4 ou 5, ou obtenu par le procédé selon les revendications 1 à 3, caractérisée en ce qu'elle comprend de 0,5 à 20 % de principe actif dans une formulation cosmétique adaptée.6. Cosmetic composition comprising the active principle according to one of claims 4 or 5, or obtained by the process according to claims 1 to 3, characterized in that it comprises from 0.5 to 20% of active principle in a formulation adapted cosmetics.
7. Utilisation de la composition cosmétique selon la revendication 6, caractérisée en ce que l'on applique sur la peau cette composition sur les zones pigmentées en sorte d'obtenir des effets dépigmentant et éclaircissant. 7. Use of the cosmetic composition according to claim 6, characterized in that this composition is applied to the skin on the pigmented areas so as to obtain depigmenting and lightening effects.
PCT/FR2003/000159 2002-01-22 2003-01-20 Method for obtaining an active principle from agarum cribosum, particularly for prevention of pigmentation WO2003061618A1 (en)

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FR0200726A FR2834886B1 (en) 2002-01-22 2002-01-22 PROCESS FOR OBTAINING AN ACTIVE INGREDIENT FROM AGARUM CRIBOSUM, IN PARTICULAR TO FIGHT PIGMENTATION
FR02/00726 2002-01-22

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GB2422107A (en) * 2004-12-23 2006-07-19 Boots Co Plc Skin whitening composition
FR2913336A1 (en) * 2007-03-08 2008-09-12 Lvmh Rech USE OF ALGAE PHAEODACTYLUM EXTRACT FOR SKIN DEPIGMENTATION

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GB2422107A (en) * 2004-12-23 2006-07-19 Boots Co Plc Skin whitening composition
GB2422107B (en) * 2004-12-23 2008-12-17 Boots Co Plc Cosmetic compositions
FR2913336A1 (en) * 2007-03-08 2008-09-12 Lvmh Rech USE OF ALGAE PHAEODACTYLUM EXTRACT FOR SKIN DEPIGMENTATION
WO2008125789A2 (en) * 2007-03-08 2008-10-23 Lvmh Recherche Use of phaeodactylum algae extract for depigmenting the skin
WO2008125789A3 (en) * 2007-03-08 2008-12-18 Lvmh Rech Use of phaeodactylum algae extract for depigmenting the skin
US8372408B2 (en) 2007-03-08 2013-02-12 Lvmh Recherche Use of Phaeodactylum algae extract for depigmenting the skin

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FR2834886B1 (en) 2005-10-14

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