FR3126870A1 - Pharmaceutical or cosmetic composition intended to improve cellulite and varicose veins, characterized in that it comprises a combination of theanine and polysaccharides derived from matcha. - Google Patents
Pharmaceutical or cosmetic composition intended to improve cellulite and varicose veins, characterized in that it comprises a combination of theanine and polysaccharides derived from matcha. Download PDFInfo
- Publication number
- FR3126870A1 FR3126870A1 FR2109754A FR2109754A FR3126870A1 FR 3126870 A1 FR3126870 A1 FR 3126870A1 FR 2109754 A FR2109754 A FR 2109754A FR 2109754 A FR2109754 A FR 2109754A FR 3126870 A1 FR3126870 A1 FR 3126870A1
- Authority
- FR
- France
- Prior art keywords
- pharmaceutical
- emulsion
- cosmetic composition
- skin
- composition according
- 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.)
- Pending
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- 239000000203 mixture Substances 0.000 title claims abstract description 19
- 239000002537 cosmetic Substances 0.000 title claims abstract description 14
- DATAGRPVKZEWHA-YFKPBYRVSA-N N(5)-ethyl-L-glutamine Chemical compound CCNC(=O)CC[C@H]([NH3+])C([O-])=O DATAGRPVKZEWHA-YFKPBYRVSA-N 0.000 title claims abstract description 12
- 208000035484 Cellulite Diseases 0.000 title claims abstract description 11
- 206010049752 Peau d'orange Diseases 0.000 title claims abstract description 11
- 206010046996 Varicose vein Diseases 0.000 title claims abstract description 11
- 230000036232 cellulite Effects 0.000 title claims abstract description 11
- 208000027185 varicose disease Diseases 0.000 title claims abstract description 11
- 150000004676 glycans Chemical class 0.000 title claims abstract description 8
- 229920001282 polysaccharide Polymers 0.000 title claims abstract description 8
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Classifications
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- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
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Abstract
Composition pharmaceutique ou cosmétique destinée à améliorer l’apparence de la cellulite et à diminuer les varices, caractérisée en ce qu’elle comprend une association de théanine et des polysaccharides extraits de Camellia sinensis, et d’au moins 2 métabolites produits par une bactérie Bacillus subtilis tel que Bacillus subtilis Gozen GZN-08 .Pharmaceutical or cosmetic composition intended to improve the appearance of cellulite and to reduce varicose veins, characterized in that it comprises a combination of theanine and polysaccharides extracted from Camellia sinensis, and at least 2 metabolites produced by a Bacillus bacterium subtilis such as Bacillus subtilis Gozen GZN-08.
Description
La présente invention a pour objet une composition pharmaceutique ou cosmétique destinée à améliorer l’apparence de la cellulite et à diminuer les varices caractérisée en ce que ladite composition comprend une association de théanine et des polysaccharides extraits des feuilles de matchaCamellia sinensis, et d’au moins 2 métabolites produits par la bactérieBacillus subtilis Gozen GZN-08parmi le groupe : acide gallique, lobéline, biotine, catéchine, pyridoxine, acide syringique, butyrate, propionate, zinc, acide linoléique, saikosaponine, acacétine, saponarine, acide butyrique.The subject of the present invention is a pharmaceutical or cosmetic composition intended to improve the appearance of cellulite and to reduce varicose veins, characterized in that the said composition comprises a combination of theanine and polysaccharides extracted from the leaves of matcha Camellia sinensis , and at least 2 metabolites produced by the bacterium Bacillus subtilis Gozen GZN-08 from the group: gallic acid, lobeline, biotin, catechin, pyridoxine, syringic acid, butyrate, propionate, zinc, linoleic acid, saikosaponin, acacetin, saponarin, butyric acid.
On sait que la cellulite est un problème esthétique appelé « lipodystrophie gynoïde (GLD) » touchant 85 à 98% des femmes post-pubertaires. La cellulite est une altération de la topographie de la peau qui survient au niveau de la région pelvienne, des membres inférieurs et de l'abdomen. Elle se caractérise par un aspect capitonné ou « peau d'orange ». C'est un problème complexe mettant en jeu le système micro circulatoire et lymphatique, ainsi que la matrice extracellulaire et la présence d'un excès de graisse sous‐cutanée dans le derme. En effet, il est caractérisé par une altération des adipocytes associée à une stase lymphatique, une diminution du flux sanguin et une augmentation de protéines dans le liquide interstitiel provoquant une altération de la microcirculation, une diminution de la collagenèse associée à une hyperkératose folliculaire qui provoque l’apparence de peau d’orange et une altération du tissu sous-cutané du derme profond donnant une texture granulaire à la peau. Certains facteurs prédisposent les femmes à une GLD : génétiques (sexe, race, distribution des tissus adipeux), hormonal (insuline, œstrogène, prolactine), vasculaire, mauvaise hygiène de vie (sédentarité, alimentation). Une altération de la microcirculation peut induire également des varices. Les varices sont une dilatation anormale d'une veine et sont visibles sous la peau au niveau des membres inférieurs de manière disgracieuse. Pour réduire la cellulite, c’est-à-dire diminuer les tensions générées sur les fibres conjonctives, il faut diminuer le volume des adipocytes, ce qui revient à diminuer leur contenu en triglycérides et donc stimuler la lipolyse ou réduire la lipogenèse. La lipogenèse est une voie métabolique qui permet d’estérifier les acides gras sous forme de triglycérides où ils seront stockés dans les adipocytes. Les triglycérides sont fabriqués dans le foie, dans les cellules adipeuses ainsi que dans les cellules intestinales. La lipolyse correspond au catabolisme des triglycérides stockés dans les adipocytes c’est-à-dire leur dégradation en acides gras non estérifiés et en glycérol. Les molécules ainsi libérées dans le flux sanguin peuvent être utilisées par d’autres tissus comme substrat énergétique (acides gras) ou servir de précurseurs néoglucogéniques (glycérol). Un des traitements actuels contre la cellulite utilise des essences de plantes (EP2813207) mais a besoin de plusieurs essences pour que cela fonctionne. Un autre traitement (W02011152692) utilisant un actif naturel, la fucoxanthine est utilisé contre la cellulite. Ce traitement permet d’activer l’expression UCP-1 dans la masse grasse blanche, ce qui provoque l’apoptose des cellules adipeuses donc une réduction de la cellulite. Cependant, il existe d’autres mécanismes permettant de réduire la taille des adipocytes comme une augmentation intracellulaire d’AMPc, une réduction de la lipogenèse ou une augmentation de la lipolyse. Ce traitement n’est donc efficace que partiellement dans l’augmentation de la lipolyse. De plus, il ne prend pas en compte la réduction des varices ou l’amélioration de la microcirculation.It is known that cellulite is an aesthetic problem called "gynoid lipodystrophy (GLD)" affecting 85 to 98% of post-pubertal women. Cellulite is an alteration in the topography of the skin that occurs in the pelvic region, lower limbs and abdomen. It is characterized by a padded or "orange peel" appearance. It is a complex problem involving the microcirculatory and lymphatic system, as well as the extracellular matrix and the presence of excess subcutaneous fat in the dermis. Indeed, it is characterized by an alteration of adipocytes associated with lymphatic stasis, a decrease in blood flow and an increase in proteins in the interstitial fluid causing an alteration in microcirculation, a decrease in collagenosis associated with follicular hyperkeratosis which causes the appearance of orange peel and an alteration of the subcutaneous tissue of the deep dermis giving a granular texture to the skin. Certain factors predispose women to GLD: genetic (sex, race, distribution of adipose tissue), hormonal (insulin, estrogen, prolactin), vascular, poor lifestyle (sedentary lifestyle, diet). An alteration of the microcirculation can also induce varicose veins. Varicose veins are an abnormal dilation of a vein and are visible under the skin in the lower limbs in an unsightly way. To reduce cellulite, i.e. to reduce the tensions generated on the connective fibers, it is necessary to reduce the volume of the adipocytes, which amounts to reducing their triglyceride content and therefore stimulating lipolysis or reducing lipogenesis. Lipogenesis is a metabolic pathway that allows fatty acids to be esterified in the form of triglycerides where they will be stored in adipocytes. Triglycerides are made in the liver, in fat cells and in intestinal cells. Lipolysis corresponds to the catabolism of triglycerides stored in adipocytes, i.e. their degradation into non-esterified fatty acids and glycerol. The molecules thus released into the blood stream can be used by other tissues as an energy substrate (fatty acids) or serve as neoglucogenic precursors (glycerol). One of the current cellulite treatments uses herbal essences (EP2813207) but needs multiple essences for it to work. Another treatment (W02011152692) using a natural active ingredient, fucoxanthin is used against cellulite. This treatment activates UCP-1 expression in the white fat mass, which causes apoptosis of fat cells and therefore a reduction in cellulite. However, there are other mechanisms that can reduce the size of adipocytes such as an intracellular increase in cAMP, a reduction in lipogenesis or an increase in lipolysis. This treatment is therefore only partially effective in increasing lipolysis. In addition, it does not take into account the reduction of varicose veins or the improvement of microcirculation.
C’est en étudiant les propriétés des métabolites du thé vert que la demanderesse a mis en évidence que les problèmes liés à une augmentation de la taille des adipocytes, une altération de la microcirculation ainsi que l’apparence des varices et une altération de la matrice extracellulaire peuvent être améliorés par un traitement composé de ces métabolites.It was by studying the properties of green tea metabolites that the applicant demonstrated that the problems linked to an increase in the size of adipocytes, an alteration of microcirculation as well as the appearance of varicose veins and an alteration of the matrix extracellular can be improved by a treatment composed of these metabolites.
Pour ce faire, la demanderesse a développé une composition pharmaceutique ou cosmétique destinée à être utilisée par voie topique ou orale comprenant une association de théanine et des polysaccharides extraits des feuilles de matchaCamellia sinensis, associée à au moins 2 métabolites, tyiquement produits par la bactérieBacillus subtilis Gozen GZN-08. Ces métabolites peuvent être préparés par la fermentation deBacillus subtilis Gozen GZN-08.To do this, the Applicant has developed a pharmaceutical or cosmetic composition intended for topical or oral use comprising a combination of theanine and polysaccharides extracted from Camellia sinensis matcha leaves, combined with at least 2 metabolites, typically produced by the bacterium Bacillus subtilis Gozen GZN-08 . These metabolites can be prepared by fermentation of Bacillus subtilis Gozen GZN-08 .
RESUMÉSUMMARY
Dans un premier aspect l’invention a trait à une composition pharmaceutique ou cosmétique destinée à améliorer l’apparence de la cellulite et à diminuer les varices caractérisée en ce qu’elle comprend une association de bioactifs comprenant de la théanine et des polysaccharides extraits des feuilles de matcha Camellia sinensis, et au moins 2 métabolites produits par une bactérie Bacillus subtilis choisis dans le groupe : acide gallique, lobéline, biotine, catéchine, pyridoxine, acide syringique, butyrate, propionate, zinc, acide linoléique, saikosaponine, acacétine, saponarine.In a first aspect, the invention relates to a pharmaceutical or cosmetic composition intended to improve the appearance of cellulite and to reduce varicose veins, characterized in that it comprises a combination of bioactive agents comprising theanine and polysaccharides extracted from the leaves matcha Camellia sinensis, and at least 2 metabolites produced by Bacillus subtilis bacteria selected from the group: gallic acid, lobeline, biotin, catechin, pyridoxine, syringic acid, butyrate, propionate, zinc, linoleic acid, saikosaponin, acacetin, saponarin.
Dans un mode de réalisation la composition pharmaceutique selon l’invention comprend du zinc à une concentration d’au moins 0,5% et de préférence d’au moins 2% en poids par rapport au poids total des bioactifs dans ladite composition et des polysaccharides à une concentration d’au moins 0,5% et de préférence d’au moins 5% en poids par rapport au poids total des bioactifs dans ladite composition.In one embodiment, the pharmaceutical composition according to the invention comprises zinc at a concentration of at least 0.5% and preferably at least 2% by weight relative to the total weight of the bioactives in said composition and of the polysaccharides at a concentration of at least 0.5% and preferably at least 5% by weight relative to the total weight of the bioactives in said composition.
Dans un deuxième aspect, l’invention porte sur un procédé de fabrication pour la réalisation de la composition pharmaceutique ou cosmétique selon l’invention. Le procédé comprend une étape de fermentation naturelle des feuilles de matchaCamellia sinensisà l’air libre, suivie d’une fermentation contrôlée en présence deBacillus subtilis ,typiquementBacillus subtilis Gozen GZN-08 ,à une température comprise entre 25 et 30°C.In a second aspect, the invention relates to a manufacturing process for producing the pharmaceutical or cosmetic composition according to the invention. The process includes a step of natural fermentation of Camellia sinensis matcha leaves in the open air, followed by controlled fermentation in the presence of Bacillus subtilis , typically Bacillus subtilis Gozen GZN-08 , at a temperature between 25 and 30°C .
L’invention se réfère également à une composition pharmaceutique ou cosmétique susceptible d’être obtenue par le procédé de l’invention.The invention also refers to a pharmaceutical or cosmetic composition capable of being obtained by the process of the invention.
La composition pharmaceutique ou cosmétique selon l’un quelconque aspects et modes de réalisation susmentionnés peut être sous la forme d’une émulsion huile dans eau (H/E) ou eau dans huile (E/H), d’émulsion multiple (H/E/H, E/H/E), de microémulsion, d’émulsion à phase gémellaires, d’émulsion PIT, de nano-émulsion, de pseudo-émulsion, de gel aqueux, de gel gras, de gel hydro-alcoolique, de phase grasse, de suspension, de savon liquide ou solide, de solution moussante ou non, de poudre, de gel ou d’émulsion lyophilisée, de préférence sous la forme de crèmes, liquides, pâtes, lotions, émulsions, huiles, gels, sirops, solides, poudres, masques, stick, comprimés, sprays, aérosol, gélules, ou de sirop.The pharmaceutical or cosmetic composition according to any of the aforementioned aspects and embodiments may be in the form of an oil-in-water (O/W) or water-in-oil (W/O) emulsion, of a multiple emulsion (O/ W/O, W/O/W), microemulsion, twin phase emulsion, PIT emulsion, nano-emulsion, pseudo-emulsion, aqueous gel, fatty gel, hydro-alcoholic gel, fatty phase, suspension, liquid or solid soap, foaming or non-foaming solution, powder, gel or freeze-dried emulsion, preferably in the form of creams, liquids, pastes, lotions, emulsions, oils, gels, syrups, solids, powders, masks, sticks, tablets, sprays, aerosol, capsules, or syrup.
Dans un troisième aspect, l’invention porte sur la composition pharmaceutique de l’invention, pour son utilisation dansIn a third aspect, the invention relates to the pharmaceutical composition of the invention, for its use in
- la réduction de l’accumulation de graisse dans le tissu adipeux et intestinal en inhibant l’enzyme intestinale lipase et l’enzyme phosphodiestérase ; et/ou- the reduction of fat accumulation in adipose and intestinal tissue by inhibiting the intestinal enzyme lipase and the enzyme phosphodiesterase; and or
- pour diminuer le risque d’apparition de varices, pour fluidifier la circulation sanguine et/ou pour et améliorer la micro-circulation dans les jambes.- to reduce the risk of appearance of varicose veins, to improve blood circulation and/or to improve micro-circulation in the legs.
Dans un quatrième aspect, l’invention porte sur l’utilisation non-thérapeutique d’une composition cosmétique selon l’invention pour tonifier la peau des cuisses et des bras, pour épaissir la peau des cuisses et des bras, pour moduler la production d’acide hyaluronique par les cellules de la peau, pour améliorer l’apparence de la peau et augmenter l’élasticité de la peau, ou pour moduler l’épaississement des fibres de collagène de la peau.In a fourth aspect, the invention relates to the non-therapeutic use of a cosmetic composition according to the invention for toning the skin of the thighs and arms, for thickening the skin of the thighs and arms, for modulating the production of hyaluronic acid by skin cells, to improve skin appearance and increase skin elasticity, or to modulate the thickening of skin collagen fibers.
Claims (8)
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FR2109754A FR3126870A1 (en) | 2021-09-16 | 2021-09-16 | Pharmaceutical or cosmetic composition intended to improve cellulite and varicose veins, characterized in that it comprises a combination of theanine and polysaccharides derived from matcha. |
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FR2109754A FR3126870A1 (en) | 2021-09-16 | 2021-09-16 | Pharmaceutical or cosmetic composition intended to improve cellulite and varicose veins, characterized in that it comprises a combination of theanine and polysaccharides derived from matcha. |
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