FR2758724A1 - Controlling cellulite and fat deposition - Google Patents
Controlling cellulite and fat deposition Download PDFInfo
- Publication number
- FR2758724A1 FR2758724A1 FR9700777A FR9700777A FR2758724A1 FR 2758724 A1 FR2758724 A1 FR 2758724A1 FR 9700777 A FR9700777 A FR 9700777A FR 9700777 A FR9700777 A FR 9700777A FR 2758724 A1 FR2758724 A1 FR 2758724A1
- Authority
- FR
- France
- Prior art keywords
- protamine
- cellulite
- composition according
- esters
- salts
- 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.)
- Granted
Links
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- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- FDRQPMVGJOQVTL-UHFFFAOYSA-N quercetin rutinoside Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC=2C(C3=C(O)C=C(O)C=C3OC=2C=2C=C(O)C(O)=CC=2)=O)O1 FDRQPMVGJOQVTL-UHFFFAOYSA-N 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- IKGXIBQEEMLURG-BKUODXTLSA-N rutin Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](C)O[C@@H]1OC[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](OC=2C(C3=C(O)C=C(O)C=C3OC=2C=2C=C(O)C(O)=CC=2)=O)O1 IKGXIBQEEMLURG-BKUODXTLSA-N 0.000 description 1
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- 235000005493 rutin Nutrition 0.000 description 1
- 229960004555 rutoside Drugs 0.000 description 1
- 235000005713 safflower oil Nutrition 0.000 description 1
- 239000003813 safflower oil Substances 0.000 description 1
- 235000019515 salmon Nutrition 0.000 description 1
- 235000003441 saturated fatty acids Nutrition 0.000 description 1
- 150000004671 saturated fatty acids Chemical class 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 229920002545 silicone oil Polymers 0.000 description 1
- KZJWDPNRJALLNS-VJSFXXLFSA-N sitosterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CC[C@@H](CC)C(C)C)[C@@]1(C)CC2 KZJWDPNRJALLNS-VJSFXXLFSA-N 0.000 description 1
- 210000004927 skin cell Anatomy 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 229950006451 sorbitan laurate Drugs 0.000 description 1
- 235000011067 sorbitan monolaureate Nutrition 0.000 description 1
- 210000004003 subcutaneous fat Anatomy 0.000 description 1
- 239000002600 sunflower oil Substances 0.000 description 1
- 229960000278 theophylline Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000003944 tolyl group Chemical group 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 239000003053 toxin Substances 0.000 description 1
- 231100000765 toxin Toxicity 0.000 description 1
- 108700012359 toxins Proteins 0.000 description 1
- LINXHFKHZLOLEI-UHFFFAOYSA-N trimethyl-[phenyl-bis(trimethylsilyloxy)silyl]oxysilane Chemical compound C[Si](C)(C)O[Si](O[Si](C)(C)C)(O[Si](C)(C)C)C1=CC=CC=C1 LINXHFKHZLOLEI-UHFFFAOYSA-N 0.000 description 1
- BLGXFZZNTVWLAY-SCYLSFHTSA-N yohimbine Chemical compound C1=CC=C2C(CCN3C[C@@H]4CC[C@H](O)[C@@H]([C@H]4C[C@H]33)C(=O)OC)=C3NC2=C1 BLGXFZZNTVWLAY-SCYLSFHTSA-N 0.000 description 1
- 229960000317 yohimbine Drugs 0.000 description 1
- AADVZSXPNRLYLV-UHFFFAOYSA-N yohimbine carboxylic acid Natural products C1=CC=C2C(CCN3CC4CCC(C(C4CC33)C(O)=O)O)=C3NC2=C1 AADVZSXPNRLYLV-UHFFFAOYSA-N 0.000 description 1
Classifications
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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
- A61Q19/06—Preparations for care of the skin for countering cellulitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/1703—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- A61K38/1709—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/04—Dispersions; Emulsions
- A61K8/06—Emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/14—Liposomes; Vesicles
-
- 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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
- A61K8/4953—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom containing pyrimidine ring derivatives, e.g. minoxidil
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- 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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/60—Sugars; Derivatives thereof
- A61K8/602—Glycosides, e.g. rutin
-
- 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
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Birds (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pharmacology & Pharmacy (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Dermatology (AREA)
- Dispersion Chemistry (AREA)
- Marine Sciences & Fisheries (AREA)
- Zoology (AREA)
- Cosmetics (AREA)
Abstract
Description
La présente invention concerne une nouvelle application de la protamine, et plus particulièrement l'application de la protamine, ses sels ou esters, en cosmétique et en thérapeutique, ainsi que des compositions cosmétiques et pharmaceutiques en contenant. The present invention relates to a new application of protamine, and more particularly to the application of protamine, its salts or esters, in cosmetics and therapeutics, as well as cosmetic and pharmaceutical compositions containing it.
Les surcharges adipeuses et les accumulations de cellulite sont considérées selon les cas comme des défauts susceptibles de nuire à l'aspect esthétique ou comme des états physiologiques anormaux des individus, chez l'homme, mais surtout chez la femme. Ces états ne doivent cependant pas être confondus avec l'obésité, qui constitue une pathologie nécessitant un traitement systémique. Bien souvent il n'est pas utile de recourir à un traitement thérapeutique pour lutter contre les surcharges adipeuses, mais dans la plupart des cas leur présence est considérée comme disgracieuse, et un traitement cosmétique est alors souhaité pour en atténuer les effets. Adipose overloads and accumulations of cellulite are considered depending on the case as defects likely to harm the aesthetic appearance or as abnormal physiological states of individuals, in men, but especially in women. These states should not, however, be confused with obesity, which constitutes a pathology requiring systemic treatment. Very often it is not useful to resort to a therapeutic treatment to fight against adipose overloads, but in most cases their presence is considered unsightly, and a cosmetic treatment is then desired to mitigate the effects.
Des cellules de la peau, dénommées adipocytes, synthétisent des triglycérides par lipogénèse à partir d'acides gras libres et de glycérol provenant de la dégradation du glucose. Skin cells, called adipocytes, synthesize triglycerides by lipogenesis from free fatty acids and glycerol from the breakdown of glucose.
Les acides gras et le glucose sont apportés à l'organisme par les aliments. Inversement, les triglycérides contenus dans les adipocytes subissent une lipolyse sous l'action d'enzymes et libèrent du glycérol ou des esters de glycérol ainsi que des acides gras qui peuvent à leur tour circuler dans l'organisme et/ou être captés par des adipocytes où ils sont à nouveau transformés en triglycérides par lipogénèse. En cas de déséquilibre entre la lipogénèse et la lipolyse, il peut se produire une accumulation excessive de triglycérides qui se traduit pas des surcharges adipeuses.Fatty acids and glucose are brought to the body through food. Conversely, the triglycerides contained in adipocytes undergo lipolysis under the action of enzymes and release glycerol or glycerol esters as well as fatty acids which can in turn circulate in the organism and / or be taken up by adipocytes. where they are again transformed into triglycerides by lipogenesis. If there is an imbalance between lipogenesis and lipolysis, there can be an excessive accumulation of triglycerides which does not result in fat overloads.
Le brevet FR-A-2.712.811 propose un procédé de traitement in vivo utilisant des inhibiteurs de captation du glucose tels que la sérine et la rutine, qui évitent que le glucose puisse être utilisé par les adipocytes pour fixer, sous forme de triglycérides, les acides gras libres provenant des aliments ou libérés par lipolyse. L'intérêt de ces inhibiteurs est encore discuté en raison de leur action gênante pour les cellules nerveuses, très dépendantes de ces systèmes de transport en cas d'effet systémique. Patent FR-A-2,712,811 proposes an in vivo treatment method using glucose uptake inhibitors such as serine and rutin, which prevent glucose from being used by adipocytes to fix, in the form of triglycerides, free fatty acids from food or released by lipolysis. The interest of these inhibitors is still discussed because of their annoying action on the nerve cells, very dependent on these transport systems in the event of systemic effect.
Diverses compositions destinées à lutter contre la cellulite sont disponibles dans le commerce et notamment des compositions contenant des bases xanthiques telles que la théophylline et la caféine, en raison de son effet d'augmentation du taux intracellulaire d'AMPC par inhibition d'une phosphodiestérase et par un phénomène supposé d'interaction sur un récepteur membranaire ayant le même effet. Son action in vitro sur la lipolyse est clairement établie, ainsi que sa pénétration trans-épidermique. Cependant, aucune preuve n'a été apportée indiquant une quelconque action in vivo, particulièrement chez les individus consommant régulièrement des quantités importantes de café. Various compositions intended for combating cellulite are commercially available and in particular compositions containing xanthic bases such as theophylline and caffeine, because of its effect of increasing the intracellular level of AMPC by inhibiting a phosphodiesterase and by a supposed phenomenon of interaction on a membrane receptor having the same effect. Its in vitro action on lipolysis is clearly established, as well as its transepidermal penetration. However, no evidence has been provided indicating any action in vivo, particularly in individuals who regularly consume significant amounts of coffee.
On connaît aussi des alpha-2 inhibiteurs ou alpha-2 bloqueurs tels que ceux décrits au brevet FR-A-2.669.537 qui bloquent la fixation des catécholamines sur des alpha-2 récepteurs, inhibant fortement la lipolyse. Ces récepteurs sont plus nombreux chez les sujets de sexe féminin, en particulier chez les sujets présentant une surcharge pondérale. Also known are alpha-2 inhibitors or alpha-2 blockers such as those described in patent FR-A-2,669,537 which block the binding of catecholamines to alpha-2 receptors, strongly inhibiting lipolysis. These receptors are more numerous in female subjects, in particular in overweight subjects.
Pour lutter contre la cellulite, on a encore proposé d'utiliser des compositions à base de diverses substances d'origine végétale, supposées capables d'agir efficacement sur le drainage et l'élimination des toxines. To combat cellulite, it has also been proposed to use compositions based on various substances of plant origin, supposed capable of acting effectively on the drainage and elimination of toxins.
Cependant, aucune de ces substances ou compositions ne s'est avérée susceptible de procurer des effets permettant de les utiliser de manière avantageuse et efficace pour le traitement des surcharges adipeuses et de la cellulite. However, none of these substances or compositions has been found capable of providing effects making it possible to use them advantageously and effectively for the treatment of adipose overloads and cellulite.
La protamine est une protéine libérant par hydrolyse plusieurs amino-acides de base, et en particulier l'arginine qui est le composant principal, ainsi que l'alanine et la sérine. Plusieurs types de protamine existent et peuvent être extraits de substances d'origine animale, notamment de laitance de poissons tels que le saumon. Protamine is a protein which releases by hydrolysis several basic amino acids, in particular arginine which is the main component, as well as alanine and serine. Several types of protamine exist and can be extracted from substances of animal origin, especially milt from fish such as salmon.
La protamine et certains de ses sels, tels que le sulfate de protamine, sont utilisés comme conservateurs alimentaires, comme décrit par exemple dans le brevet EP 273.606, en raison de leur effet inhibiteur de multiplication de certaines bacté ries. Le sulfate de protamine est également utilisé dans certaines compositions pharmaceutiques en raison de ses effets hémostatiques, et il peut être utilisé pour neutraliser l'action anticoagulante de l'héparine. Enfin, le brevet FR 2.656.311 décrit des inhibiteurs d'enzymes lipolytiques comprenant des protéines ou des polypeptides de base tels que des purothionines, la protamine, une histone ou une polylysine, formulés dans des compositions pour administration orale pour la prévention de l'obésité. Protamine and some of its salts, such as protamine sulfate, are used as food preservatives, as described for example in patent EP 273,606, because of their inhibitory effect on the multiplication of certain bacteria. Protamine sulfate is also used in some pharmaceutical compositions due to its hemostatic effects, and it can be used to neutralize the anticoagulant action of heparin. Finally, patent FR 2,656,311 describes inhibitors of lipolytic enzymes comprising basic proteins or polypeptides such as purothionines, protamine, a histone or a polylysine, formulated in compositions for oral administration for the prevention of obesity.
Les travaux effectués par la demanderesse ont montré de manière tout à fait surprenante que la protamine, ainsi que ses sels et esters, peut être utilisée efficacement à des concentrations réduites dans des compositions cosmétiques et/ou pharmaceutiques topiques, destinées à lutter contre la cellulite et les surcharges adipeuses. The work carried out by the applicant has shown quite surprisingly that protamine, as well as its salts and esters, can be used effectively at reduced concentrations in topical cosmetic and / or pharmaceutical compositions, intended for combating cellulite and adipose overloads.
La présente invention a donc pour objet l'utilisation de la protamine, ses sels et esters, dans des compositions cosmétiques et/ou pharmaceutiques administrables par voie topique et destinées à lutter contre la cellulite et les surcharges pondérales et à en atténuer les effets. The present invention therefore relates to the use of protamine, its salts and esters, in cosmetic and / or pharmaceutical compositions which can be administered topically and which are intended to combat cellulite and overweight and to attenuate its effects.
L'invention a également pour objet l'utilisation de la protamine, ses sels et esters, pour la préparation d'un médicament pour le traitement de la cellulite et des surcharges pondérales. The invention also relates to the use of protamine, its salts and esters, for the preparation of a medicament for the treatment of cellulite and overweight.
Suivant la terminologie classique, l'administration par voie topique désigne toute méthode consistant à appliquer la substance ou la composition directement sur la peau. According to conventional terminology, topical administration means any method consisting in applying the substance or composition directly to the skin.
La protamine utilisable dans la présente invention peut être l'une quelconque des formes de protamines disponibles dans le commerce, dont la composition en amino-acides peut varier, ou un de ses sels ou esters compatibles sur le plan cosmétique ou pharmaceutique, tels que le sulfate, le chlorhydrate, le sorbate, le hyaluronate, l'héparinate, le gluconate et le lactate de protamine. The protamine which can be used in the present invention may be any of the commercially available forms of protamine, the amino acid composition of which may vary, or one of its cosmetically or pharmaceutically compatible salts or esters, such as sulfate, hydrochloride, sorbate, hyaluronate, heparinate, gluconate and protamine lactate.
Dans tout ce qui suit, l'expression "protamine" désignera tant la protamine elle-même que ses sels ou esters précités. In all that follows, the expression "protamine" will denote both the protamine itself and its salts or esters mentioned above.
Conformément à la présente invention, la composition administrable par voie topique peut avantageusement contenir, outre la protamine, ses sels ou esters, une ou plusieurs autres substances connues pour exercer des effets complémentaires, et plus particulièrement un composé favorisant la lipolyse, par exemple un inhibiteur de phosphodiestérase tel que la caféine, ainsi qu'un alpha-2 bloqueur, par exemple l'escine, des extraits de lierre, la yohimbine et des extraits de ginkgo biloba. In accordance with the present invention, the composition which can be administered topically may advantageously contain, in addition to protamine, its salts or esters, one or more other substances known to exert complementary effects, and more particularly a compound promoting lipolysis, for example an inhibitor phosphodiesterase such as caffeine, as well as an alpha-2 blocker, for example escin, ivy extracts, yohimbine and ginkgo biloba extracts.
Les compositions cosmétiques ou pharmaceutiques contenant la protamine, conformément à la présente invention, sont destinées à une administration topique, et contiennent des supports et excipients couramment utilisés dans des compositions de ce type, telles que des émulsions H/E ou E/H, des crèmes, des gels ou des lotions. Dans le cas des émulsions, la phase grasse peut représenter entre 10 et 60% environ du poids de la composition, la phase aqueuse entre 10 et 80% environ et l'agent émulsionnant entre 2 et 20%, le reste étant constitué par la protamine et les autres composants indiqués ci-après. Cosmetic or pharmaceutical compositions containing protamine, in accordance with the present invention, are intended for topical administration, and contain carriers and excipients commonly used in compositions of this type, such as O / W or W / O emulsions, creams, gels or lotions. In the case of emulsions, the fatty phase can represent between 10 and 60% approximately of the weight of the composition, the aqueous phase between 10 and 80% approximately and the emulsifying agent between 2 and 20%, the rest being constituted by protamine and the other components listed below.
Ainsi, les compositions peuvent contenir des agents émulsionnants, des agents hydratants, des agents viscosants, des conservateurs, des parfums, des huiles, des lipides, un solvant spécifique ainsi que de l'eau. Thus, the compositions can contain emulsifying agents, moisturizing agents, viscosifying agents, preservatives, perfumes, oils, lipids, a specific solvent as well as water.
On peut choisir l'agent émulsionnant parmi des polymères carboxyvinyliques à haut poids moléculaire (par exemple le Carbopol3), des polysorbates (par exemple le Tween 60 ou le
Tween 80 ), des esters de sorbitan et en particulier un monostéarate, un tristéarate, un monopalmitate, et un laurate de sorbitan (par exemple l'Arlacel . On peut encore utiliser d'autres agents émulsionnants tels que divers dérivés d'acide stéarique ou palmitique, et par exemple le stéarate de PEG 50, des mono- ou diglycérides d'acide stéarique ou palmitique, un stéarate de propylène glycol auto-émulsionnable, ou encore le polyglycéryl-2-sesquioléate, l'éther cétylique de polyoxyéthylène, un polyglucoside de siloxane, ou une silicone émulsionnable. On peut encore utiliser des mélanges émulsionnants non ioniques tels que le Protegin X. The emulsifier can be chosen from high molecular weight carboxyvinyl polymers (for example Carbopol3), polysorbates (for example Tween 60 or
Tween 80), sorbitan esters and in particular a monostearate, a tristearate, a monopalmitate, and a sorbitan laurate (for example Arlacel. It is also possible to use other emulsifying agents such as various derivatives of stearic acid or palmitic, and for example PEG 50 stearate, mono- or diglycerides of stearic or palmitic acid, a self-emulsifying propylene glycol stearate, or also polyglyceryl-2-sesquioleate, polyoxyethylene cetyl ether, a polyglucoside of siloxane, or an emulsifiable silicone. It is also possible to use nonionic emulsifying mixtures such as Protegin X.
Les agents viscosants utilisés dans les compositions de l'invention peuvent être choisis parmi divers polymères d'acide acrylique, une gomme cellulose, une silice, des poly mères carboxyvinyliques, un silicate d'aluminium et de magnésium, et on peut utiliser par exemple la silice colloïdale vendue sous la marque Aerosil 200 ou un acide polyacrylique réticulé tel que le Carbopol 940. The viscosifiers used in the compositions of the invention may be chosen from various polymers of acrylic acid, a cellulose gum, a silica, carboxyvinyl polymers, an aluminum and magnesium silicate, and it is possible, for example, to use the colloidal silica sold under the brand Aerosil 200 or a crosslinked polyacrylic acid such as Carbopol 940.
Les agents hydratants utilisés dans l'invention sont de préférence le glycérol ou des dérivés de glycérol. The hydrating agents used in the invention are preferably glycerol or glycerol derivatives.
Les constituants de la phase grasse, c'est-à-dire les huiles et lipides, peuvent être choisis parmi l'huile de jojoba, l'huile de maïs, l'huile de vaseline, l'huile de coco hydrogénée, l'huile de carthame, des glycérides d'acides gras saturés, l'acide stéarique, l'acide palmitique, le stéarate d'octyle, le palmitate de glycéryle, le 2-octyl-dodécanol, l'alcool de lanoline, le polyéthylène glycol, l'adipate d'éthyl-2 hexyle, ou encore des huiles de silicones telles que le méthyl phényl polysiloxane, la diméthicone, la cyclométhicone/diméthicone copolyol, la phényl triméthicone. The constituents of the fatty phase, that is to say the oils and lipids, can be chosen from jojoba oil, corn oil, petroleum jelly oil, hydrogenated coconut oil, safflower oil, glycerides of saturated fatty acids, stearic acid, palmitic acid, octyl stearate, glyceryl palmitate, 2-octyl-dodecanol, lanolin alcohol, polyethylene glycol, 2-ethylhexyl adipate, or alternatively silicone oils such as methyl phenyl polysiloxane, dimethicone, cyclomethicone / dimethicone copolyol, phenyl trimethicone.
La composition peut aussi contenir, outre l'eau (de préférence de l'eau déminéralisée), un solvant spécifique, tel qu'un alcool comme l'alcool éthylique, ou un éther de diéthylène glycol comme l'éthoxydiglycol ou l'éther monométhylique de diéthylène glycol (Transcutol
Tous les excipients et additifs couramment utilisés peuvent être employés dans l'invention pourvu qu'ils soient compatibles avec la protamine. L'un des avantages résultant de la présente invention est la possibilité de réduire la quantité de conservateur par comparaison avec les compositions classiques, en raison du pouvoir anti-bactérien de la protamine. Il est même possible de préparer des compositions à base protamine ne contenant aucun conservateur usuel.The composition can also contain, in addition to water (preferably demineralized water), a specific solvent, such as an alcohol such as ethyl alcohol, or a diethylene glycol ether such as ethoxydiglycol or monomethyl ether diethylene glycol (Transcutol
All the excipients and additives commonly used can be used in the invention provided that they are compatible with protamine. One of the advantages resulting from the present invention is the possibility of reducing the amount of preservative compared to conventional compositions, due to the anti-bacterial power of protamine. It is even possible to prepare protamine-based compositions containing no usual preservative.
La protamine est utilisée à raison de 0,001 à 10% en poids, et de préférence 0,05 à 1%, du poids total de la composition, dans le cas de formulations pour administration topique. Ce mode d'administration est particulièrement avantageux dans la présente invention car il permet une application très localisée sur les parties du corps à traiter. Cette application peut s'accompagner d'un massage de la zone à traiter. Protamine is used in an amount of 0.001 to 10% by weight, and preferably 0.05 to 1%, of the total weight of the composition, in the case of formulations for topical administration. This mode of administration is particularly advantageous in the present invention because it allows a very localized application on the parts of the body to be treated. This application can be accompanied by a massage of the area to be treated.
L'absence de toxicité bien connue de la protamine et de ses sels et esters disponibles permet de l'utiliser sans risque de complication tant dans les compositions cosmétiques que les compositions pharmaceutiques. En particulier, le risque athérogène est nul car la protamine est connue comme agent anti-athérogène par normalisation des indices lipidiques sanguins. The absence of well-known toxicity of protamine and of its available salts and esters makes it possible to use it without risk of complication in both cosmetic and pharmaceutical compositions. In particular, the atherogenic risk is zero because protamine is known as an anti-atherogenic agent by normalization of blood lipid indices.
Les essais réalisés avec les compositions conformes à la présente invention ont mis en évidence un effet de diminution des surcharges adipeuses et de la cellulite, en particulier dans le cas de l'application topique sous forme d'émulsion ou de gel, une ou plusieurs fois par jour pendant une durée pouvant aller de quelques jours à quelques semaines. The tests carried out with the compositions in accordance with the present invention have demonstrated an effect of reduction of adipose overloads and of cellulite, in particular in the case of topical application in the form of emulsion or gel, one or more times. per day for a period ranging from a few days to a few weeks.
Bien que le mode d'action de la protamine ne soit pas totalement élucidé, il apparaît que la captation des acides gras libres par l'adipocyte dans le tissu adipeux sous-cutané se trouve partiellement ou totalement inhibée par la protamine. En effet, l'adipocyte produit une lipoprotéine-lipase qui est normalement transportée jusqu'aux cellules endothéliales recouvrant la lumière des capillaires, et qui décroche les acides gras circulants des protéines qui les transportent. Although the mode of action of protamine is not fully understood, it appears that the uptake of free fatty acids by the adipocyte in the subcutaneous adipose tissue is partially or completely inhibited by the protamine. In fact, the adipocyte produces a lipoprotein lipase which is normally transported to the endothelial cells covering the lumen of the capillaries, and which detaches the circulating fatty acids from the proteins which transport them.
L'inhibition de cette fixation par la protamine a pour effet d'éviter l'entrée et l'accumulation des lipides dans l'adipocyte et est complémentaire de l'action des agents lipolytiques classiques.The inhibition of this fixation by protamine has the effect of preventing the entry and accumulation of lipids in the adipocyte and is complementary to the action of conventional lipolytic agents.
Les exemples suivants illustrent l'invention sans en limiter la portée. Ils décrivent des formulations topiques qui peuvent être préparées par les méthodes usuelles de la technique cosmétique. The following examples illustrate the invention without limiting its scope. They describe topical formulations which can be prepared by the usual methods of the cosmetic technique.
EXEMPLE 1
EMULSION E/H AMINCISSANTE
On prépare une émulsion eau-dans-huile par une méthode usuelle en utilisant les ingrédients suivants.EXAMPLE 1
SLIMMING W / O EMULSION
A water-in-oil emulsion is prepared by a usual method using the following ingredients.
Gluconate de protamine ....................... 0,5 g
Polyglycéryl-4 isostéarate et
cétyl diméthicone ............................ 5,0 g
Adipate d'éthyl-2 hexyle ..................... 5,0 g
Cyclométhicone ............................... 8,0 g
Huile de vaseline ............................ 5,0 g
Aérosil 200 .................................. 0,4 g
Stéarate d'octyle ............................ 14,0 g
Chlorure de sodium ........................... 0,5 g
Ethoxy diglycol .............................. 3,0 g
Extrait de ginkgo biloba ..................... 0,7 g
Caféine ...................................... 1,0 g
Conservateur ................................. 0,3 g
Eau déminéralisée ......... qsp ............... 100,0 g
Cette émulsion est appliquée directement sur la peau d'une patiente, au niveau d'une surcharge adipeuse, à raison de deux applications par jour complétées par un massage localisé, pendant une période de quatre semaines.Protamine gluconate ....................... 0.5 g
Polyglyceryl-4 isostearate and
cetyl dimethicone ............................ 5.0 g
2-ethylhexyl adipate ..................... 5.0 g
Cyclomethicone ............................... 8.0 g
Vaseline oil ............................ 5.0 g
Aerosil 200 .................................. 0.4 g
Octyl stearate ............................ 14.0 g
Sodium chloride ........................... 0.5 g
Ethoxy diglycol .............................. 3.0 g
Ginkgo biloba extract ..................... 0.7 g
Caffeine ...................................... 1.0 g
Preservative ................................. 0.3 g
Demineralized water ......... qs ............... 100.0 g
This emulsion is applied directly to the skin of a patient, at the level of an adipose overload, at the rate of two applications per day supplemented by a localized massage, for a period of four weeks.
On constate alors une diminution sensible de la surcharge adipeuse. There is then a significant reduction in adipose overload.
La même opération est répétée sur cinq autres patientes, avec la même émulsion, pendant une période comprise entre quatre et six semaines. Des résultats comparables sont obser vés. The same operation is repeated on five other patients, with the same emulsion, for a period of between four and six weeks. Comparable results are observed.
Exemple 2
EMULSION E/H AMINCISSANTE
Sulfate de protamine ......................... 0,5 g
Protegin X ................................... 20,0 g
Huile de vaseline ............................ 10,0 g
Composition aromatique ....................... 1,0 g
Huile de maïs ................................ 15,0 g
Conservateur ................................. 0,3 g
Glycérol ..................................... 5,0 g
Extrait de lierre ............................. 0,5 g
polyéthylène glycol (7) glycéryl monococoate . 4,0 g
Eau déminéralisée ......... qsp ............... 100,0 g
EXEMPLE 3
EMULSION H/E AMINCISSANTE SANS CONSERVATEUR
Sorbate de protamine ......................... 2,5 g
Cyclométhicone ............................... 10,0 g
Phytosqualane ................................ 18,0 g
Huile de vaseline ............................ 5,0 g
Lanoline liquide ............................. 4,0 g
Stéarate de glycéryle et PEG 100 stéarate . . . 6,0 g
Tween 60 ..................................... 2,0 g
Alcool cétylique ............................. 1,2 g
Acide stéarique .............................. 2,5 g
Triéthanolamine 99% .......................... 0,1 g
Antioxydants ................................. 0,3 g
Caféine ...................................... 1,0 g
Propylène glycol ............................. 5,0 g
Escine ....................................... 0,5 g
Eau déminéralisée ......... qsp............... 100,0 g
EXEMPLE 4
EMULSION H/E AMINCISSANTE
Protamine .................................... 0,01g
Polyéthylène glycol .......................... 2,0 g
PEG 8 ........................................ 3,0 g
Extrait de ginkgo biloba ..................... 0,3 g
Caféine ...................................... 3,0 g
Benzoate de sodium ........................... 3,0 g
Conservateur ................................. 0,3 g
Parfum ....................................... 0,5 g
Polymère caboxyvinylique 981 ................. 0,2 g
Adipate d'éthyl-2 hexyle ..................... 1,0 g
Alcool cétylique ............................. 3,0 g
Acide stéarique .............................. 3,0 g
Monostéarate de glycérol ..................... 3,0 g
Huile de tournesol ........................... 2,0 g
Triéthanolamine 99% .......................... 1,0 g
Eau déminéralisée ......... qsp............... 100,0 g
EXEMPLE 5
GEL AMINCISSANT HYDROALCOOLIQUE
Lactate de protamine ......................... 5,0 g
Polymère carboxyvinylique 980 ................ 0,9 g
Alcool éthylique ............................. 20,0 g
Triéthanolamine 99% .......................... 0,3 g
Parfum ....................................... 0,3 g
Conservateur ................................. 0,3 g
Ethoxydiglycol ............................... 5,0 g
Extrait de lierre ............................ 1,0 g
Eau déminéralisée ......... qsp............... 100,0 g
EXEMPLE 6
GEL EMULSIONNE H/E AMINCISSANT
Hyaluronate de protamine ..................... 1,0 g
Polymère carboxyvinylique 980 ................ 0,6 g
Cyclométhicone ............................... 3,0 g
Cétéaryl octanoate ........................... 7,0 g
PEG-6-32 stéarate ............................ 3,0 g
Conservateur ................................. 0,3 g
Parfum ....................................... 0,4 g
Alcool éthylique ............................. 10,0 g
Triéthanolamine .............................. 0,2 g
Caféine ...................................... 1,0 g
Polyéthylène glycol (7) glycéryl monococoate . 2,0 g
Eau déminéralisée ......... qsp............... 100,0 g
EXEMPLE 7
GEL AMINCISSANT
Chlorhydrate de protamine .................... 5,0 g
Polymère carboxyvinylique 940 ................ 0,6 g
Ethoxy diglycol .............................. 5,0 g
Triéthanolamine 99% .......................... 0,3 g
Conservateur ................................. 0,3 g
Propylène glycol ............................. 3,0 g
Extrait de lierre ............................ 1,0 g
Caféine ...................................... 1,0 g
Eau déminéralisée ......... qsp............... 100,0 g
EXEMPLE 8
LIQUIDE A IONISER
Sulfate de protamine ......................... 1,0 g
Benzoate de sodium ........................... 3,0 g
Conservateurs ................................ 0,2 g
Eau ....................... qsp............... 100,0 g
EXEMPLE 9
CREME AUX LIPOSOMES
Protamine .................................... 0,25 g
Alcool cétylique polyglycérolé ............... 3,8 g
B-sitostérol ................................. 3,8 g
Dicétyl phosphate ............................ 0,4 g
Conservateur ................................. 0,3 g
Huile de maïs ................................ 35,0 g
Parfum ....................................... 0,6 g
Polymère carboxyvinylique 980 ................ 0,2 g
Triéthanolamine 99% .......................... 0,2 g
Eau déminéralisée ......... qsp............... 100,0 g Example 2
SLIMMING W / O EMULSION
Protamine sulfate ......................... 0.5 g
Protegin X ................................... 20.0 g
Vaseline oil ............................ 10.0 g
Aromatic composition ....................... 1.0 g
Corn oil ................................ 15.0 g
Preservative ................................. 0.3 g
Glycerol ..................................... 5.0 g
Ivy extract ............................. 0.5 g
polyethylene glycol (7) glyceryl monococoate. 4.0g
Demineralized water ......... qs ............... 100.0 g
EXAMPLE 3
SLIMMING O / W EMULSION WITHOUT PRESERVATIVE
Protamine sorbate ......................... 2.5 g
Cyclomethicone ............................... 10.0 g
Phytosqualane ................................ 18.0 g
Vaseline oil ............................ 5.0 g
Liquid lanolin ............................. 4.0 g
Glyceryl stearate and PEG 100 stearate. . . 6.0 g
Tween 60 ..................................... 2.0 g
Cetyl alcohol ............................. 1.2 g
Stearic acid .............................. 2.5 g
Triethanolamine 99% .......................... 0.1 g
Antioxidants ................................. 0.3 g
Caffeine ...................................... 1.0 g
Propylene glycol ............................. 5.0 g
Escine ....................................... 0.5 g
Demineralized water ......... qs ............... 100.0 g
EXAMPLE 4
SLIMMING O / W EMULSION
Protamine .................................... 0.01g
Polyethylene glycol .......................... 2.0 g
PEG 8 ........................................ 3.0 g
Ginkgo biloba extract ..................... 0.3 g
Caffeine ...................................... 3.0 g
Sodium benzoate ........................... 3.0 g
Preservative ................................. 0.3 g
Perfume ....................................... 0.5 g
Caboxyvinyl polymer 981 ................. 0.2 g
2-ethylhexyl adipate ..................... 1.0 g
Cetyl alcohol ............................. 3.0 g
Stearic acid .............................. 3.0 g
Glycerol monostearate ..................... 3.0 g
Sunflower oil ........................... 2.0 g
Triethanolamine 99% .......................... 1.0 g
Demineralized water ......... qs ............... 100.0 g
EXAMPLE 5
HYDROALCOHOLIC SLIMMING GEL
Protamine lactate ......................... 5.0 g
Carboxyvinyl polymer 980 ................ 0.9 g
Ethyl alcohol ............................. 20.0 g
Triethanolamine 99% .......................... 0.3 g
Perfume ....................................... 0.3 g
Preservative ................................. 0.3 g
Ethoxydiglycol ............................... 5.0 g
Ivy extract ............................ 1.0 g
Demineralized water ......... qs ............... 100.0 g
EXAMPLE 6
SLIMMING M / W EMULSION GEL
Protamine hyaluronate ..................... 1.0 g
Carboxyvinyl polymer 980 ................ 0.6 g
Cyclomethicone ............................... 3.0 g
Cetaryl octanoate ........................... 7.0 g
PEG-6-32 stearate ............................ 3.0 g
Preservative ................................. 0.3 g
Perfume ....................................... 0.4 g
Ethyl alcohol ............................. 10.0 g
Triethanolamine .............................. 0.2 g
Caffeine ...................................... 1.0 g
Polyethylene glycol (7) glyceryl monococoate. 2.0 g
Demineralized water ......... qs ............... 100.0 g
EXAMPLE 7
SLIMMING GEL
Protamine hydrochloride .................... 5.0 g
Carboxyvinyl polymer 940 ................ 0.6 g
Ethoxy diglycol .............................. 5.0 g
Triethanolamine 99% .......................... 0.3 g
Preservative ................................. 0.3 g
Propylene glycol ............................. 3.0 g
Ivy extract ............................ 1.0 g
Caffeine ...................................... 1.0 g
Demineralized water ......... qs ............... 100.0 g
EXAMPLE 8
IONIZING LIQUID
Protamine sulfate ......................... 1.0 g
Sodium benzoate ........................... 3.0 g
Preservatives ................................ 0.2 g
Water ....................... qs ............... 100.0 g
EXAMPLE 9
LIPOSOME CREAM
Protamine .................................... 0.25 g
Cetyl alcohol polyglycerolated ............... 3.8 g
B-sitosterol ................................. 3.8 g
Diketyl phosphate ............................ 0.4 g
Preservative ................................. 0.3 g
Corn oil ................................ 35.0 g
Perfume ....................................... 0.6 g
Carboxyvinyl polymer 980 ................ 0.2 g
Triethanolamine 99% .......................... 0.2 g
Demineralized water ......... qs ............... 100.0 g
Claims (7)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9700777A FR2758724B1 (en) | 1997-01-24 | 1997-01-24 | TOPICAL COMPOSITION BASED ON PROTAMINE FOR THE TREATMENT OF CELLULITE AND PONDERAL OVERLOADS |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9700777A FR2758724B1 (en) | 1997-01-24 | 1997-01-24 | TOPICAL COMPOSITION BASED ON PROTAMINE FOR THE TREATMENT OF CELLULITE AND PONDERAL OVERLOADS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| FR2758724A1 true FR2758724A1 (en) | 1998-07-31 |
| FR2758724B1 FR2758724B1 (en) | 1999-04-23 |
Family
ID=9502951
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| FR9700777A Expired - Fee Related FR2758724B1 (en) | 1997-01-24 | 1997-01-24 | TOPICAL COMPOSITION BASED ON PROTAMINE FOR THE TREATMENT OF CELLULITE AND PONDERAL OVERLOADS |
Country Status (1)
| Country | Link |
|---|---|
| FR (1) | FR2758724B1 (en) |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2782453A1 (en) * | 1998-08-20 | 2000-02-25 | Rocher Yves Biolog Vegetale | Stable water-in-oil emulsions with a major proportion of dispersed phase give prolonged transcutaneous release of active material |
| EP1060739A1 (en) * | 1999-06-16 | 2000-12-20 | Exsymol S.A.M. | Slimming cosmetic composition containing L-arginine or a derivative thereof |
| WO2001032137A1 (en) * | 1999-11-05 | 2001-05-10 | Sanofi-Synthelabo | Slimming composition containing a substance inducing il-6 production |
| FR2804319A1 (en) * | 2000-01-28 | 2001-08-03 | Clarins Lab | SLIMMING COSMETIC COMPOSITION COMPRISING AS AN ACTIVE AGENT A PLANT EXTRACT CONTAINING ANP |
| EP1607083A1 (en) | 2004-06-16 | 2005-12-21 | L'oreal | Method to promote the penetration of a cosmetic active ingredient and the composition therefor |
| FR2883472A1 (en) * | 2005-03-23 | 2006-09-29 | Biolog Vegetale Yves Rocher Sa | USE OF A CHLOROGENIC ACID AS A SLIMMING ACTIVE INGREDIENT |
| WO2007006745A1 (en) | 2005-07-07 | 2007-01-18 | Beiersdorf Ag | Emulsifier combination for cosmetics |
| WO2012069902A1 (en) | 2010-11-23 | 2012-05-31 | Rhodia Poliamida E Especialidades Ltda | Cosmetic kit and use for improving the appearance of the skin |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB814491A (en) * | 1956-01-17 | 1959-06-03 | American Home Prod | Lipid mobiliser |
| JPS62209007A (en) * | 1986-03-10 | 1987-09-14 | Dasukin:Kk | Cosmetic |
| FR2656311A1 (en) * | 1989-12-25 | 1991-06-28 | Nisshin Flour Milling Co | INHIBITORS OF LIPOLYTIC ENZYMES. |
| JPH05339168A (en) * | 1992-06-08 | 1993-12-21 | Suisanchiyou Chokan | Pancreatic lipase inhibitor and cholesterol esterase inhibitor |
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1997
- 1997-01-24 FR FR9700777A patent/FR2758724B1/en not_active Expired - Fee Related
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB814491A (en) * | 1956-01-17 | 1959-06-03 | American Home Prod | Lipid mobiliser |
| JPS62209007A (en) * | 1986-03-10 | 1987-09-14 | Dasukin:Kk | Cosmetic |
| FR2656311A1 (en) * | 1989-12-25 | 1991-06-28 | Nisshin Flour Milling Co | INHIBITORS OF LIPOLYTIC ENZYMES. |
| JPH05339168A (en) * | 1992-06-08 | 1993-12-21 | Suisanchiyou Chokan | Pancreatic lipase inhibitor and cholesterol esterase inhibitor |
Non-Patent Citations (2)
| Title |
|---|
| DATABASE WPI Section Ch Week 8742, Derwent World Patents Index; Class D21, AN 87-296402, XP002043187 * |
| DATABASE WPI Section Ch Week 9404, Derwent World Patents Index; Class B04, AN 94-031737, XP002043188 * |
Cited By (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000010511A1 (en) * | 1998-08-20 | 2000-03-02 | Laboratoires De Biologie Vegetale Yves Rocher | Use of stable concentrated water-in-oil emulsions for controlled transcutaneous release of an active principle |
| FR2782453A1 (en) * | 1998-08-20 | 2000-02-25 | Rocher Yves Biolog Vegetale | Stable water-in-oil emulsions with a major proportion of dispersed phase give prolonged transcutaneous release of active material |
| US6716436B1 (en) | 1999-06-16 | 2004-04-06 | Exsymol S.A.M. | Cosmetic composition for slimming containing L-arginine, an L-arginine analogue, or one of their derivatives, for topical application |
| EP1060739A1 (en) * | 1999-06-16 | 2000-12-20 | Exsymol S.A.M. | Slimming cosmetic composition containing L-arginine or a derivative thereof |
| FR2794974A1 (en) * | 1999-06-16 | 2000-12-22 | Exsymol Sa | COSMETIC COMPOSITION FOR L-ARGININE-BASED SLIMMING OF AN ANALOGUE OF L-ARGININE OR ONE OF THEIR DERIVATIVES, WHICH CAN BE APPLIED TOPICLY |
| WO2001032137A1 (en) * | 1999-11-05 | 2001-05-10 | Sanofi-Synthelabo | Slimming composition containing a substance inducing il-6 production |
| FR2800610A1 (en) * | 1999-11-05 | 2001-05-11 | Sanofi Synthelabo | SLIMMING COSMETIC COMPOSITION COMPRISING A SUBSTANCE INDUCING THE PRODUCTION OF IL-6 |
| US8628770B2 (en) | 1999-11-05 | 2014-01-14 | Sanofi | Slimming cosmetic composition containing a substance inducing the production of IL-6 |
| FR2804319A1 (en) * | 2000-01-28 | 2001-08-03 | Clarins Lab | SLIMMING COSMETIC COMPOSITION COMPRISING AS AN ACTIVE AGENT A PLANT EXTRACT CONTAINING ANP |
| WO2001054659A3 (en) * | 2000-01-28 | 2002-03-14 | Clarins Lab | Slimming cosmetic composition comprising a plant extract containing a plant natriuretic peptide (pnp) |
| EP1607083A1 (en) | 2004-06-16 | 2005-12-21 | L'oreal | Method to promote the penetration of a cosmetic active ingredient and the composition therefor |
| FR2883472A1 (en) * | 2005-03-23 | 2006-09-29 | Biolog Vegetale Yves Rocher Sa | USE OF A CHLOROGENIC ACID AS A SLIMMING ACTIVE INGREDIENT |
| WO2007006745A1 (en) | 2005-07-07 | 2007-01-18 | Beiersdorf Ag | Emulsifier combination for cosmetics |
| WO2012069902A1 (en) | 2010-11-23 | 2012-05-31 | Rhodia Poliamida E Especialidades Ltda | Cosmetic kit and use for improving the appearance of the skin |
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| Publication number | Publication date |
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| FR2758724B1 (en) | 1999-04-23 |
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