FR2848455A1 - Composition for treating greasy skin, useful in conditions associated with hyperseborrhea, particularly acne, contains an extract from plants of the family Clusiaceae - Google Patents

Abstract

Composition (A) for treating greasy skin contains an extract (I) from a plant of the family Clusiaceae.

Description

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USE OF A PLANT EXTRACT FROM THE FAMILY OF
CLUSIACEES IN THE PREPARATION OF A COMPOSITION
INTENDED TO CORRECT OR PREVENT ASSOCIATED DISORDERS
The present invention relates to the use of a plant extract of the clusiaceae family in the preparation of a composition intended to correct or prevent disorders associated with oily skin, in particular by an action of decreasing secretion. sebum. The invention is directed in particular to cosmetic compositions intended for oral or topical administration. The invention also relates to a cosmetic process for correcting or preventing disorders associated with hyperseborrhoea.

Hyper-seborrhoeic oily skin is characterized by excessive secretion and excretion of sebum. Classically, a sebum level greater than 200 μg / cm 2 measured at the forehead is considered to be characteristic of such oily skin.

Oily skin is often associated with a lack of desquamation, a glowing complexion, a thick skin texture.

In addition to these aesthetic disorders, excess sebum can serve as a support for the anarchic development of saprophytic bacterial flora (especially acnes) and cause comedones and / or acne lesions.

Sebum is the natural product of the sebaceous gland which is an appendage of the pilosebaceous unit. It is essentially a more or less complex mixture of lipids. Classically, the sebaceous gland produces squalene, triglycerides, aliphatic waxes,

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 cholesterol and possibly free cholesterol (Stewart, M.E., Semin Dermatol 11, 100-105 (1992)). The action of bacterial lipases converts a variable part of triglycerides, formed into free fatty acids.

The sebocyte constitutes the competent cell of the sebaceous gland. The production of sebum is associated with a program of terminal differentiation of this cell. During this differentiation, the metabolic activity of the sebocyte is essentially focused on the biosynthesis of lipids (lipogenesis) and more precisely on the neosynthesis of fatty acid.

The sebaceous secretion is under the control of different afferents of nervous origin. In particular, M. Cartlidge et al (Br J. Dermatol 1972, 86 (1), 61-63) specified the modulatory role of the cholinergic (para-lymphatic) system on seborrhea.

This secretion is also under endocrine control since the Applicant has demonstrated a negative regulatory activity of cortisol on sebaceous secretion.

This seboregulatory activity of cortisol demonstrated experimentally on sebocytes in culture confirms the work of Levèque et al. (Arch Dermatol Res 283, 372-6, (1991)) on the control of the hyperseborrhoeic state by topical application of glucocorticoids.

It is further described that the secretion of cortisol is, in particular, dependent on the serotonergic system. There is therefore a relationship between the nervous system, the endocrine system and seborrhea. This cortisol production is specifically dependent on the serotonin 5HT4 receptor (Lefevbre et al., Neurosci, 47, 999-1007 (1992)).

The serotonergic system is one of the main aminergic systems involved in neurotransmission.

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 that the other active substances of the plant could play in the anti-depressant activity of St. John's wort extract.

To the knowledge of the Applicant, it has never been suggested to use an extract of St. John's wort, and more generally, of the family of clusiaceae in the preparation of a composition for correcting or preventing disorders associated with a oily skin, especially by an action leading to decrease the secretion of sebum.

The subject of the invention is therefore the use of a plant extract of the clusiaceae family in the preparation of a composition intended for the treatment of oily skin.

The observed activity of improving the condition of oily skin as a result of the treatment can result in particular from the decrease in the secretion of sebum. The production of sebum at the level of the skin can be determined by measuring the level of sebum according to the process described by J. L. Levèque in the patent FR 2968708.

By decreasing the secretion of sebum is meant a significant decrease in the level of sebum in the skin, that is to say at least 10%, preferably at least 30% of the sebum level.

The species of clusiaceae chosen for the preparation of the plant extracts used in the compositions are preferably chosen from the species of the genus Hypericum.

In particular, the species Hypericum perforatum is mentioned.

In a particular embodiment, the extract is derived from St. John's wort (Hypericum perforatum). The extract can be obtained from the aerial parts of the plant, especially the leaves, the flower, the fruit, or the

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 seed or any other part of the plant. Preferably, the extract is obtained from the flower.

It is advantageous to use extracts containing hypericin and / or hyperforin which can be prepared according to the numerous methods described in the state of the art. Complete dried extracts of St. John's Wort or hyperforin-enriched dry extracts may in particular be obtained according to the process described in patent EP-A-0 599 307.

The serotonin reuptake inhibitory effect present in the plant extract that can be used according to the invention can in particular be determined by measuring the percentage of reuptake of serotonin according to the method described by Marcusson et al. (Neurochem 50: 1783-1790).

The extract is preferably obtained so as to have a serotonin reuptake inhibitory effect greater than or equal to that present in the plant before extraction.

In particular, an extract of plants of the clusiaceae family may be obtained by aqueous, alcoholic or hydro-alcoholic extraction, and preferably by alcoholic or hydro-alcoholic extraction.

The invention also relates to compositions comprising the plant extract of the clusiaceae family, intended to correct or prevent disorders associated with oily skin, in particular by an action for decreasing the secretion of sebum. The proportion of plant extract in the composition is of course determined according to the desired effect on the inhibition of the sebaceous function of the skin and the method of administration of the composition.

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In a particularly preferred embodiment, the composition is formulated for oral administration. In this case, it may be in any dosage form suitable for this mode of administration, for example, in the form of scored tablets or not, granules, capsules, capsules, solutes, suspensions or solutions comprising a appropriate excipient.

Preferably, a composition according to the invention is a nutritional supplement, presented in the form of a solid composition, of the tablet, granule, capsule or capsule type and comprising an extract of plants as defined above and a suitable adjuvant for oral administration.

In this regard, adjuvants for oral compositions, especially for food supplements, are known to those skilled in the art. Mention may be made, inter alia and in a purely illustrative manner, of lubricants such as magnesium stearate, products for instant solubilization, gelling agents, thickeners, humectants, fatty and / or aqueous components, preservatives, texturing agents, flavoring agents and the like. / or coating, antioxidants and dyes usual in the food field.

The composition according to the present invention may further comprise one or more vitamins and / or trace elements. As such, may for example be used alone or in combination the following assets: zinc and its salts including zinc sulfate and glucanate, vitamins B5, B6, B8, C, E or PP, p-carotene and carotenoids, garlic extracts especially in the form of allyl or ajoen sulphide, selenium, curcumin, curcuminoids, niacin, lithospermic acid and adenosine. It is understood that those skilled in the art will choose such assets and, where appropriate, combine them in the sense of an improvement of the expected effects of the composition object of the invention, avoiding that the activity of interest sought is either inhibited or attenuated.

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The composition for oral administration comprises a plant extract of the clusiaceae family in an amount of from 0.001% to 40% by weight of the composition, preferably from 0.05% to 5% by weight and more preferably from 0.1% to 1% by weight of the composition.

The invention also relates to a cosmetic process for the treatment of oily skin, for the prevention and / or treatment of disorders of the skin associated with hyperseborrhoea, and in particular acne lesions, consisting in administering orally a composition comprising an extract of plants of the clusiaceae family, and in particular a St. John's wort extract (Hypericum perforatum), as described above.

Daily doses of clusiaceae plant extract administered orally for the treatment of oily skin may be from 1 to 5000 mg / day, preferably. Preferentially, the plant extract of the clusiaceae family is included in the composition according to the invention in an amount allowing its administration at a dose of between 5 and 1000 mg / day, said dosage being carried out in one or more doses.

In another embodiment, the composition comprising a plant extract of the clusiaceae family is formulated for topical administration. In this case, the plant extract may be present in the composition in an amount ranging from 0.0001 to 20% by weight, and preferably from 0.001 to 10%.

A composition formulated for topical administration according to the invention contains a cosmetically or dermatologically acceptable medium, that is to say a medium that is compatible with the skin, the nails, the mucous membranes, the tissues and the hair. According to a preferred embodiment of

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 the invention has a pH preferably close to that of the skin, of between 4 and 7. The composition comprising a plant extract of the clusiaceae family is preferably applied topically to the face, the neck, hair, mucous membranes and nails or any other skin area of the body.

A cosmetic composition according to the invention may be in any galenical form normally used in the cosmetic and dermatological fields. It may especially be in the form of hydroalcoholic or oily solutions, dispersions of the lotion or serum type, anhydrous or oily gels, emulsions of liquid or semi-liquid consistency of the milk type, obtained by dispersion of a fatty phase in a aqueous phase (O / W) or conversely (W / O), or a triple emulsion (W / O / W or H / EH), suspensions or emulsions of soft, semi-solid or solid consistency of the type cream, gel, micro-emulsions, or micro-capsules, microparticles, or vesicular dispersions of ionic and / or nonionic type. These compositions are prepared according to the usual methods.

The compositions according to the invention can also be used for the hair in the form of alcoholic or aqueous-alcoholic solutions, or in the form of creams, gels, emulsions or foams.

The amounts of the various constituents of the compositions used according to the invention are those conventionally used in the fields under consideration.

These compositions comprise, in particular, creams for the protection, treatment or care of the face, the hands or the body, protective or caring body milks, lotions, gels or foams for the care of the skin and mucous membranes. or for cleaning the skin.

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The compositions may also consist of solid preparations constituting soaps or cleaning bars.

In a known manner, the composition used according to the invention may also contain adjuvants customary in the cosmetic and dermatological fields, such as hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents, preservatives, antioxidants, solvents, perfumes, fillers and dyestuffs. The amounts of these various adjuvants are those conventionally used in the fields under consideration, and for example from 0.01% to 20% of the total weight of the composition. Of course, those skilled in the art will take care to choose this or these optional additives and / or their amounts in such a way that the advantageous properties intrinsically attached to the composition are in accordance with the invention, in particular inhibitor activity. serotonin present in the plant extract of the clusiaceae family, are not, or not substantially, altered by the addition or additions envisaged.

As oils that may be used in the invention, mention may be made of mineral oils (vaseline oil), vegetable oils (shea oil, sweet almond oil), animal oils, synthetic oils and silicone oils (cyclomethicone) and fluorinated oils (perfluoropolyethers). It is also possible to use fatty alcohols, fatty acids (stearic acid), waxes (paraffin, carnauba, beeswax) as fatty substances.

As emulsifiers that can be used in the invention, mention may be made of Polysorbate 60 and sorbitan stearate sold respectively under the trade names Tween 60 and Span 60 by the company ICI. Co-emulsifiers such as PPG-3 myristyl ether sold under the trade name Emcol 249-3K by Witco can be added thereto.

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 As solvents that can be used in the invention, mention may be made of lower alcohols, in particular ethanol and isopropanol, and propylene glycol.

As hydrophilic gelling agents, mention may be made of carboxyvinyl polymers (carbomer), acrylic copolymers such as copolymers of acrylates / alkyl acrylates, polyacrylamides, polysaccharides such as hydroxypropylcellulose, natural gums (xanthan) and clays, and lipophilic gelling agents that may be mentioned include modified clays such as bentones, metal salts of fatty acids such as aluminum stearates, hydrophobic silica, polyethylenes and ethylcellulose.

As hydrophilic active agents, it is possible to use proteins or hydrolysates of proteins, amino acids, polyols, urea, allantoin, sugars and sugar derivatives, water-soluble vitamins, starch, bacterial extracts or plants, including Aloe Vera.

As lipophilic active agents, it is possible to use tocopherol (vitamin E) and its derivatives, essential fatty acids, ceramides, essential oils.

In order to fight effectively against photoaging, it is also possible to add to the composition used according to the invention one or more complementary, active UVA and / or UVB sunscreens, hydrophilic or lyophilic, optionally comprising a function sulfonic acid.

The sunscreen is preferably chosen from organic filters and / or mineral filters.

As organic filters, there may be mentioned cinnamic derivatives, salicylic derivatives, camphor derivatives, triazine derivatives, benzophenone derivatives, dibenzoylmethane derivatives, ss, ss-diphenylacrylate derivatives, derivatives of

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 p-aminobenzoic acid, filter polymers and silicone filters described in the application WO-93/04665 or the organic filters described in the patent application EP-A 0 487 404.

As inorganic filters, mention may in particular be made of pigments or even nanopigments (average size of the primary particles: generally between 5 nm and 10 nm, preferably between 10 and 50 nm) of coated or uncoated metal oxides, such as, for example, nanopigments titanium oxide (amorphous or crystallized in rutile and / or anatase form), iron, zinc, zirconium or cerium which are all well known photoprotective agents per se acting by physical blocking (reflection and / or diffusion) UV radiation. Conventional coating agents are, moreover, alumina and / or aluminum stearate. Such nanopigments of metal oxides, coated or uncoated, are in particular described in patent applications EP-A-0 518 772 and EP-A-0 518 773.

Examples of UV-A and / or UV-B active sunscreens that may be mentioned include: p-aminobenzoic acid, oxyethylenated p-aminobenzoate (25 moles), p-dimethylaminobenzoate of 2- ethylhexyl, N-oxypropylenated p-aminobenzoate, glycerol p-aminobenzoate, homomenthyl salicylate, 2-ethylhexyl salicylate, triethanolamine salicylate, 4-isopropylbenzyl salicylate, 4-tertiary amine butyl-4'-methoxy-dibenzoylmethane (PARSOL 1789 from GIVAUDAN ROURE)

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 2-ethylhexyl p-methoxycinnamate (PARSOL MCX from GIVAUDAN ROURE), 4-isopropyl-dibenzoylmethane (EUSOLEX 8020 from MERCK), menthyl anthranilate, 2-ethylhexyl-2-cyano-3,3'-diphenylacrylate, (UVINUL N539 from BASF), ethyl-2-cyano-3,3'-diphenylacrylate, 2-phenylbenzimidazole 5-sulfonic acid and its salts, 3- (4'-trimethylammonium) -benzylidene-bornan 2-on-methylsulfate, 2-hydroxy-4-methoxybenzophenone (UVINUL MS 40 from BASF), 2-hydroxy-4-methoxybenzophenone-5-sulfonate (UVINUL MS 40 from BASF), 2,4-dihydroxybenzophenone (UVINUL 400 of BASF), 2,2 ', 4,4'-tetrahydroxybenzophenone (UVINUL D 50 from BASF), 2,2'-dihydroxy-4,4'-dimethoxybenzophenone (HELISORB II from NORQUAY), 2-hydroxy 4-n-octoxybenzophenone, 2-hydroxy-4-methoxy-4'-methylbenzophenone, α- (2-oxoborn-3-ylidene) -tolyl-4-sulfonic acid and its salts, 3- (4-methoxybenzophenone) sulfonyl) benzylidene-bornan-2-one and its salts, 3- (4'-methylbenzylidene) -d, 1-camphor, 3-benzylidene-d, 1-camphor, benzene 1,4-di (3-methylidene-10-camphorsulfonic acid) and its salts (CHIMEX MEXORYL SX), urocanic acid, 2,4-6-tris- [p- (2'-ethylhexyl) 1-oxycarbonyl) anilino] -1,3,5-triazine, 2- [p- (tert-butylamido) anilino] -4,6-bis [p- (2'-ethylhexyl-1'oxycarbonyl) anilino] -1 3,5-triazine, 2,4-bis [4-2-ethylhexyloxyl] -2-hydroxylphenyl} -6 (4-methoxyphenyl) -1,3,5-triazine,

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 the polymer of N- (2 and 4) - [2-oxoborn-3-yliden) methyl) benzyl] -acrylamide, 4,4-bis-benzimidazolyl-phenylen-3,3 ', 5,5'- tetrasulfonic acid and its salts, 2,2'-methylen-bis- [6- (2H-benzotriazol-2-yl) -4- (1,1,3,3-tetramethylbutyl) phenol], malonate functional polyorganosiloxanes.

The invention also relates to a cosmetic treatment method, by the application of the compositions as defined above, according to the technique of usual use of these compositions. For example: application of creams, gels, serums, ointments, lotions, milks to the skin, scalp, nails and / or mucous membranes.

The invention relates in particular to a cosmetic process for the treatment and / or prevention of skin disorders associated with hyperseborrhoea, in particular for the treatment and / or prevention of acne lesions, which consists in applying to the skin, the mucous membranes and / or keratinous fibers, a composition comprising an extract of plants of the clusiaceae family.

The features of the invention mentioned above, as well as others, will become more clearly apparent from the following examples.

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 EXAMPLES Example 1 Hypericum perforatum extract activity on the reuptake of serotonin: It was shown, during a study on different pharmacological targets, that a St. John's wort extract modified the reuptake of several biogenic brain amines (norepinephrine). , dopamine, serotonin).

The results are summarized in the table below:

<Tb>
<tb> Monoamine <SEP> Recapture <SEP> with <SEP> Recapture <SEP> with <SEP> Molecule <SEP> of <SEP> Reference
<tb> recaptured <SEP> St. John's wort <SEP> 1 <SEP>% <SEP> St. John's wort <SEP> 5% <SEP> reference <SEP> and <SEP> method
<tb> IC50 <SEP> (nM)
<tb> Noradrenaline <SEP> 23% <SEP> 60% <SEP> Protriptlyline <SEP> Pacholczyk <SEP> and <SEP> al.
<Tb>

29 <SEP> Nature <SEP> 16 <SEP> 687-699
<tb> Dopamine <SEP> 39% <SEP> 71% <SEP> Nomifensin <SEP> Pristupa <SEP> and <SEP> al. <SEP> Mol.
<Tb>

72 <SEP> Pharmacol. <SEP> 45 <SEP> 125- <SEP>
<tb> 135
<tb> Serotonin <SEP> 79% <SEP> 79% <SEP> Zimelidine <SEP> Marcusson <SEP> and <SEP> al. <SEP> J.
<Tb>

114 <SEP> Neurochem.50
<tb> 1783-1790
<Tb>
These results are expressed as a percentage of reuptake inhibition.

They demonstrate that the extract of Hypericum perforatum is a mixed recapture inhibitor and in particular that it influences the reuptake of serotonin so that it increases the intrasynaptic bioavailability of serotonin.

Example 2 Preparation of an aqueous-alcoholic extract of Hypericum perforatum

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 400 g of dried floral Hypericum perforatum somerities are pulverized by milling with Turrax at 20,000 rpm for 3 minutes at 4 ° C. (in an ice bath).

The powder thus obtained is mixed with 4 liters of an 80: 20 mixture of 0.05 M phosphate buffer: absolute ethanol. The whole is stirred for 1 h at 4 ° C. and then centrifuged at 10,000 g at 4 ° C. The supernatant is then filtered at 0.22 m for sterilization.

The extract thus obtained is fractionated by ultrafiltration on Sartorius type membrane in order to eliminate the oxidation phenomena.

The extract is then used in the state or lyophilized to obtain about 15 g of active extract said freeze-dried extract.

Example 3 Dragées for Oral Absorption Active Ingredients
Hypericum perforatum extract ................................. 300 Excipient of the core of the dragee
Minocrystalline cellulose ............................................ 70
EncompressTM ................................................. ............ 60
Magnesium Stearate ............................................... .3
Anhydrous colloidal silica ............................................... 1 coating agent
Shellac ................................................ ............... 5
Talc ................................................. ............................ 61
Polyvidone ................................................. ................... 6 This type of candy can be taken 1 to 4 times a day.

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Conservateur ................................................................2,00 0 /o
Eau .................................................................... qsp 100,00 % Exemple 6 : Crème de soin (émulsion huile dans eau)
Extrait lyophilisé d'Hypericum perforatum ..................... 5,00 %
Stéarate de glycérol ......................................................2,00 %
Polysorbate 60 (Tween 60 vendu par ICI)...................1,00 %

Acide stéarique .............................................................2,00 % Triéthanolamine ............................................................0,80 % Carbomer......................................................................0,40 0 % Fraction liquide du beurre de karité............................. 12,00 %

Perhydrosqualène.......................................................12,00 % Antioxydant ................................................................... 2,00 % Eau qsp 100,00 %Example 4: Capsules for oral absorption mg / capsule
Active ingredients
Extract of Hypericum perforatum ................................. 200
Borage oil............................................... ..... 200
Blackcurrant seed oil ......................................... 200
Vitamins Vitamin C ............................................... ................... 60
Vitamin E................................................ ..................... 2 Example 5: lotion for the scalp
Extract of Hypericum perforatum ..................................... 5.00%
Antioxidant ................................................. .................. 3.00% Isopropanol ........................... ...................................... 40.00%

Curator ................................................. ............... 2,00 0 / o
Water ................................................. ................... qsp 100,00% Example 6: Care cream (oil-in-water emulsion)
Freeze-dried extract of Hypericum perforatum ..................... 5.00%
Glycerol stearate ............................................... ....... 2.00%
Polysorbate 60 (Tween 60 sold by ICI) ................... 1,00%

Stearic acid ................................................ ............. 2.00% Triethanolamine ................................ ............................ 0.80% Carbomer ................. .................................................. ... 0.40 0% Liquid fraction of shea butter ............................. 12.00%

Perhydrosqualene ................................................. ...... 12.00% Antioxidant ....................................... ............................ 2.00% Water qs 100.00%

Claims (20)

 1. A composition adapted for the treatment of oily skin comprising a plant extract of the clusiaceae family. 2. Composition according to claim 1, wherein the plant extract of the clusiaceae family decreases the secretion of sebum. 3. Composition according to any one of claims 1 to 2, wherein the extract is obtained from plants of the genus Hypericum, preferably St. John's wort (Hypericum perforatum). 4. Composition according to any one of claims 1 to 3, wherein the extract is obtained by aqueous extraction, alcoholic or hydro-alcoholic. 5. Composition according to any one of claims 1 to 4, wherein the extract is obtained by an alcoholic or aqueous-alcoholic extraction. 6. A composition according to any one of claims 1 to 5 formulated for oral administration. 7. Composition according to claim 6, wherein the plant extract of the clusiaceae family represents from 0.001 to 40% by total weight of the composition. The composition of claim 7, wherein the plant grain extract is from 0.05% to 5%, preferably from 0.1% to 1% by total weight of the composition. 9. A composition according to any one of claims 1 to 5 formulated for topical administration. <Desc / Clms Page number 17> The composition of claim 9, wherein the plant extract of the clusiaceae family represents from 0.0001 to 20% by total weight of the composition. 11. Composition according to claim 10, wherein the plant extract of the clusiaceae family represents from 0.001 to 10% by total weight of the composition. 12. Composition according to any one of claims 1 to 11, for correcting the disorders associated with hyperseborrhoea, and in particular to treat and / or prevent acne lesions. 13. Cosmetic process for the treatment of oily skin, for the prevention and / or treatment of acne lesions, consisting in applying to the skin, the mucous membranes and / or the keratinous fibers, a composition comprising an extract of plants from the family of Clusiaceae. 14. Cosmetic process for the treatment of oily skin, for the prevention and / or treatment of acne lesions, comprising orally administering a composition comprising an extract of plants of the clusiaceae family. 15. Use of a plant extract of the clusiaceae family for the preparation of a composition for the treatment of oily skin. 16. Use according to claim 15, in that the plant extract is obtained from plants of the genus Hypericum. 17. Use according to claim 15, in that the plant extract is obtained from St. John's wort plants. <Desc / Clms Page number 18>  18. Use according to any one of claims 15 to 17, formulated for oral administration or for topical administration. 19. Use according to any one of claims 15 to 18 for the preparation of a composition for correcting the disorders associated with a hyperseborrhoea. 20. Use according to any one of claims 15 to 19 for the preparation of a composition for the prevention and / or treatment of acne lesions.