Classifications

• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
  • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
  • A61K8/9783—Angiosperms [Magnoliophyta]
  • A61K8/9789—Magnoliopsida [dicotyledons]
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • 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
  • A61Q19/08—Anti-ageing preparations

Definitions

• the invention relates to the field of cosmetics and pharmaceuticals, in particular the field of dermatology.
• the main object of the present invention is the use of an effective amount of at least one extract of pear marc as active ingredient, in or for the preparation of a cosmetic and / or dermatological and / or pharmaceutical composition.
• the skin aging process is due to a gradual change in the structure and functions of the skin. These changes take place in the dermis and epidermis, they are caused, in part, by cell senescence.
• the main clinical signs are manifested, in particular, by the formation of wrinkles and fine lines, by the loss of elasticity of the skin but also by skin which becomes thinner and more sensitive to attack.
• Many products offer to fight against the manifestations of this aging and, in particular, to reduce wrinkles; but to date, few products have really significant results. It is therefore observed that there remains the need for a new product having an effective action on the manifestations of skin aging.
• One of the objectives of the present invention is therefore to be able to have a new product having an effective effect in order to combat the skin signs of aging.
• the pear is the fruit of the pear tree (Pirus communis), tree of the Rosaceae family, of the genus Pirus. It has been known since Antiquity and it is cultivated in all warm temperate climates. Pears come in many sizes, colors and flavors. There are several varieties: summer pears (Williams and Guyot varieties), autumn pears (buttery Hardy, Conf45, Comice) and winter pears (Passe-crassane). The pear has seeds, seeds, small, poor in albumen.
• the primary object of the invention is the use of an effective amount of at least one pear marc extract as active ingredient in or for the preparation of a cosmetic and / or dermatological and / or pharmaceutical composition.
• the active principle can be defined as being a molecule or a set of molecules capable of bringing modifications or modulations to the functioning of a biological system.
• pear marc designates the residue of the fruits (pears) that have been pressed to extract, in particular, the juice.
• extract relates to any isolated substance obtained from the raw material that constitutes pear marc.
• an extract of pear marc is understood to mean a crude mixture of the coarsely reduced parts of pears, in order to extract the juice from it, and of the extraction solvent, but also preparations of active principles which have were dissolved during extraction.
• the extract of pear marc must be understood as an extract of marc from at least one fruit from a plant belonging to the genus Pirus.
• the extract can be prepared from the marc of the fruits of at least any one of the many varieties and species belonging to the genus Pirus.
• the extract of "pear marc” is prepared from the fruits of at least one plant originating from the species Pirus communis.
• the pear marc consists, for the most part, of skins and pear seeds. It is thus possible to define the pear marc extract, according to the invention, as being an extract of skins and pear seeds.
• the pear marc that is to say the pear residue, consists essentially of pear seeds.
• the pear marc extract according to the invention is an extract of pear seed.
• the pear marc extract contains compounds such as phytosteroids, phytosterols or ursolic acid. Indeed, the presence of these compounds contributes to the exceptional qualities of the extract according to the invention. These compounds play an important role in the skin, they have, among other things, regenerating, antioxidant, firming or even soothing properties.
• Phytosteroids refer to steroids found in plants. They are polycyclic compounds of the terpene family.
• Phytosterols are steroids with an alcohol function. They have a chemical structure close to that of cholesterol, which gives them similar properties. They play, in particular, a major role in the stabilization of the lipid membrane structures thus strengthening the skin barrier and ensuring excellent protection of the skin against environmental stress. Phytosterols also have anti-inflammatory, antioxidant, cytoprotective and photoprotective properties. As an indication, phytosterols include, for example, stigmasterols, ⁇ and ⁇ sitosterols, campesterols, etc.
• the extract according to the invention contains between 5 and 30% phytosterol.
• the pear marc extract contains between 10 and 40% of ursolic acid.
• Ursolic acid a substance of a triterpenoid nature, is a compound well known for its beneficial activity in the skin, in particular by its action on the synthesis of fibers of the connective tissue, as well as for its anti-inflammatory activity (Price and al., 1987; Mahato et al., 1988).
• the marc extract according to the invention also contains tocopherols and tocotrienols which have an important anti-oxidation role; they protect polyunsaturated fatty acids and membrane proteins against oxidation by free radicals.
• the extract also contains waxes of essential fatty acids which improve the hydration and suppleness of the skin.
• the invention also relates to the use of an effective amount of at least one pear marc extract, as defined above, in or for the preparation of a composition; the extract or the composition being intended to treat curatively and / or preventively the cutaneous manifestations of aging.
• cutaneous manifestations of aging means any modification of the external appearance of the skin due to aging, for example, wrinkles and fine lines, withered skin, soft skin, thinned skin, lack of elasticity and / or skin tone, dull and dull skin but also all internal skin modifications which do not systematically result in a modified external appearance such as, for example, all internal degradations of the skin following exposure to ultra- purples.
• the extract, or the composition therefore have a positive effect on all the cutaneous manifestations of aging, they will thus be intended, in particular, to reduce wrinkles and / or fine lines and / or to smooth the skin.
• This extract will, in the same way, help fight against sagging and loss of skin tone.
• the skin After applying the pear extract according to the invention, the skin will be smoother, firmer and better hydrated. The skin will appear younger.
• This extract makes it possible to avoid the phenomena of withered skin, soft skin or even thinned skin. It makes it possible to prevent the lack of elasticity and / or tone of the skin, but also to fight against the internal degradations of the skin consecutive to an exposure to ultraviolet radiation.
• the extract of pear marc also has a positive effect on the extracellular matrix. Indeed, it has been demonstrated that the extract according to the invention increases the synthesis of proteins of the extracellular matrix, and in particular, that it increases the synthesis of collagen.
• the subject of the invention is also the use of an effective amount of at least one pear extract in or for the preparation of a composition; the extract or the composition being intended to hydrate the skin and / or to protect the skin against all types of external aggressions.
• a specialist in the extraction and purification of plants can be used in order to prepare the pear marc extract according to the invention.
• the pressing residue i.e. pear marc
• the pressing residue is treated in order to remove the residual components from the pulp, these components are then made soluble in water by the addition of a chemical agent and / or a mixture of one or more enzymes of the pectinase, cellulase or protease type.
• This operation is carried out at a temperature between 10 and 80 ° C.
• the medium is washed with water, for example, then a main residue composed mainly of seeds (seeds) and skins is recovered by filtration or centrifugation. This residue is subsequently washed and dried.
• solubilizers of the fruit flesh can be added before the pressing operation.
• the residue obtained after pressing can be dried directly.
• the residues are ground, then extracted with an organic solvent suitable for cosmetics, preferably an alcohol (ethanol, isopropanol) or a chlorinated solvent (chloroform, dichloromethane). Filtration and sterilization steps can be carried out thereafter.
• this extract can be redissolved in order to carry out a crystallization step with the aim of eliminating neutral lipids and / or enriching it with sterolic compounds and / or terpene acid.
• This step can advantageously be carried out before the total evaporation of the extraction solvent (ethanol or chloroform) if the latter authorizes it.
• the extract obtained can then contain between 5 and 90% of phytosterols and between 10 and 90% of ursolic acid.
• the evaporated extract is subsequently redissolved, or dispersed, in a solvent suitable for cosmetic use, preferably in a lipid solvent such as a fatty alcohol such as hydroxyldecanol, at a concentration of 3%. .
• the subject of the invention is a composition containing, as active principle, in a cosmetically or pharmaceutically acceptable medium, at least one extract of pear marc as defined above.
• the composition according to the invention can be a cosmetic and / or dermatological and / or pharmaceutical composition.
• the composition is a cosmetic composition, because it is intended to improve the appearance and the general cutaneous performance of the individual who uses it.
• the composition according to the invention is preferably a cosmetic and / or dermatological composition suitable for administration by the topical skin route comprising a cosmetically or dermatologically acceptable medium.
• the invention is intended for mammals in general and more particularly for human beings.
• the amount of extract usable according to the invention is, of course, a function of the desired effect and can therefore vary to a large extent.
• the abovementioned pear marc extract can be used, in the compositions of the invention, in an amount representing between 0.00001% and 20% approximately, of the total weight of the composition, and preferably , in an amount representing between 0.0001% and 5%, approximately, relative to the total weight of the final composition.
• the pear marc extract according to the invention can be used in pure form or in solution in one or more solvents suitable for cosmetics or pharmaceuticals.
• the above-mentioned extract is dissolved beforehand or dispersed in one or more cosmetically or pharmaceutically acceptable solvents such as ethanol, propanol or isopropanol, propylene glycol, butylene glycol, dipropylene glycol , ethoxylated or propoxylated diglycols or any mixture of these solvents.
• the pear marc extract is dissolved beforehand in a cosmetic or pharmaceutical carrier such as liposomes or adsorbed on powdery organic polymers, mineral supports such as talcs and bentonites, and more generally solubilized in, or attached to, any cosmetically or pharmaceutically acceptable carrier.
• a cosmetic or pharmaceutical carrier such as liposomes or adsorbed on powdery organic polymers, mineral supports such as talcs and bentonites, and more generally solubilized in, or attached to, any cosmetically or pharmaceutically acceptable carrier.
• the composition according to the invention can be ingested, injected or applied to the skin (on any cutaneous zone of the body), the hair, the nails or the mucous membranes.
• the composition according to the invention can be in all the galenical forms normally used.
• the compositions according to the present invention will be presented in a galenical form suitable for administration by the topical cutaneous route. They cover all cosmetic and dermatological forms. These compositions must therefore contain a cosmetically acceptable medium, that is to say compatible with the skin, hair or hair.
• compositions can in particular be in the form of an aqueous, hydroalcoholic or oily solution; an oil-in-water, water-in-oil or multiple emulsion; they can also be in the form of creams, suspensions or even powders, suitable for application to the skin, mucous membranes, lips and / or hair.
• compositions can be more or less fluid and have the appearance of a cream, a lotion, a milk, a serum, an ointment, a shampoo, a gel, a paste or foam. They can also be in solid form, such as a stick, or be applied to the skin in the form of an aerosol. They can be used as a care product and / or as a make-up product for the skin.
• the composition according to the invention can be in the form of an aqueous, oily lotion or in the form of serum.
• the composition can be in the form of drops and for ingestion, it can be in the form of capsules, granules, syrups or tablets.
• compositions also include any additive commonly used in the intended field of application as well as the adjuvants necessary for their formulation, such as solvents, thickeners, diluents, antioxidants, dyes, sunscreens, self-tanning agents, pigments, fillers, preservatives, perfumes, odor absorbers, cosmetic or pharmaceutical active ingredients, essential oils, vitamins, essential fatty acids, surfactants, film-forming polymers, etc. ....
• these adjuvants are chosen so as not to harm the desired advantageous properties of the composition according to the invention.
• These adjuvants can, for example, correspond from 0.01 to 20% of the total weight of the composition.
• the fatty phase may represent from 5 to 80% by weight and preferably from 5 to 50% by weight relative to the total weight of the composition.
• the emulsifiers and co-emulsifiers used in the composition will be chosen from those conventionally used in the field under consideration. For example, they can be used in a proportion ranging from 0.3 to 30% by weight, relative to the total weight of the composition.
• those skilled in the art will take care to choose any additional compounds, active or non-active, and / or their quantities, so that the advantageous properties of the mixture are not, or not substantially, altered by the addition considered.
• compositions according to the invention find application in particular as a cosmetic or pharmaceutical composition for the skin, mucous membranes and / or semi-mucous membranes, but also as a cosmetic composition for the hair and / or body hair.
• compositions which are the subject of the invention find their application in a large number of treatments, in particular cosmetic or dermatological treatments, and they can constitute a cosmetic composition, in particular for the treatment, protection, care, make-up removal and / or cleaning of the skin, lips and / or hair, and / or for making up the skin, lips, eyelashes and / or body.
• composition according to the invention may also consist of solid preparations also comprising soaps or cleaning bars.
• the composition can also be packaged in the form of an aerosol composition also comprising a propellant under pressure.
• composition can also be for oral use, for example a toothpaste paste.
• composition of the invention can also be a cosmetic composition intended for oral administration.
• the composition according to the invention can be in any suitable form, particularly in the form of an oral solution, a syrup, a tablet, a dragee, a capsule or still a food or nutritional supplement.
• the invention also relates to a cosmetic process intended to treat the cutaneous manifestations of aging, consisting in applying, to the skin, a composition, as defined above, comprising, at least, an extract of pear marc.
• the invention also relates to a cosmetic process intended to reduce wrinkles and / or fine lines on the skin, and / or to smooth the skin, consisting in applying the composition as defined above to the skin.
• the invention also relates to a cosmetic treatment method intended to fight against withered skin and / or to fight against thinned skin and / or to fight against soft skin and / or to fight against lack of elasticity and / or skin tone, consisting in applying, to the skin, a composition as defined above comprising at least one extract of pear marc.
• the invention also relates to a cosmetic treatment method intended to hydrate the skin and / or protect the skin against all types of external aggression, consisting in applying to the skin a composition as defined above comprising at least one marc extract. Pear.
• the cosmetic treatment process of the invention can be implemented in particular by applying the cosmetic compositions as defined above, according to the usual technique for using these compositions, for example: application of creams, gels, serums , lotions, milks, shampoos or sunscreen compositions, on the skin or on the hair, or else application of toothpaste on the gums.
• Example 1 Preparation of a pear marc extract.
• a kilogram of pear is sorted, washed vigorously with clean water and dried. These fruits are then pressed in a belt or belt press. We then recover between 100 and 300 g of residue from these fruits, called marc or drake.
• the pressing is progressive in order to avoid obstruction of the juice flow channels, its intensity depends on the maturity of the fruit.
• the marc is then suspended in 2 to 10 times its volume of water, in a tank with constant stirring.
• the medium is kept, with stirring, at a temperature between
• the medium is transferred to a 0.2 to 3 mm mesh sieve (or to a wringer with a similar mesh or, again, centrifuged) in order to separate the soluble elements present in the residue.
• This residue is then washed until an insoluble residue composed largely of seeds and fruit skins is obtained.
• This residue is then dried in an oven, and crushed using an appropriate plant grinder, preferably in a hammer mill.
• the powder is then extracted using an organic solvent (or a mixture of solvents).
• an organic solvent or a mixture of solvents.
• the solvent used will be an alcohol (ethanol or isopropanol).
• This extraction is carried out in a stirred extractor or, in a conventional manner, in a plant extractor, by circulation of the solvent.
• the temperature of the extraction varies from room temperature to the reflux temperature of the solvent.
• the extraction solvent is then filtered and then evaporated.
• a waxy extract of green color is then obtained which can be used as it is, titrating between 5 and 30% of phytosterol and between 10 and 30% of ursolic acid. Filtration and sterilization steps can be carried out thereafter.
• the extract is subsequently dispersed in a solvent suitable for cosmetic use, such as hydroxyldecanol, at a concentration of 3%.
• a solvent suitable for cosmetic use such as hydroxyldecanol
• Example 2 Effects of the extract of Example 1 on the skin and on the manifestations of skin aging
• Example 1 A clinical study was carried out, double blind, on a group of twenty volunteers, in order to highlight the effect of Example 1 on the improvement of the skin relief and, more particularly, its action on the condition of wrinkles.
• the volunteers applied the extract of Example 1, formulated at 2.5% in a cream, to the area around the eye, on one side of the face; the area around the eye on the other side of the face being used for the application of the placebo.
• the volunteers thus applied the product, dosed at 2 mg / cm 2 , twice a day, for 8 weeks.
• the evolution of the skin relief and the condition of wrinkles was evaluated after clinical observation (by the use of photos), as well as by an analysis of the surface of the skin using replicas of silicone.
• the study included nine follow-up visits: one visit before the start of treatment (T0), and one visit every week for 8 weeks. Photos were taken at T0 and T8 using a video camera (COHU High performance CDD camera) and negative impressions of silicone on the skin surface were made, using different markers, at the area around the eye. The photos of the prints were taken under oblique light, using the camera described above.
• the skin relief measurement was obtained by image analysis, after using a specific software (Quantirides, Monaderm) allowing to calculate the standard parameters of wrinkles such as the number, the complete surface (in mm 2 ) and the length total (in mm).
• Rejection region as far as the difference is predictable, the rejection region will be unilateral. The level of significance is at 5%.
• compositions were obtained by simple mixing of the various components.
• the quantities indicated are given as a percentage by weight.
• Aqueous phase Aqueous phase :

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