WO2003009826A1 - Use of steroids as slimming agents - Google Patents
Use of steroids as slimming agents Download PDFInfo
- Publication number
- WO2003009826A1 WO2003009826A1 PCT/FR2002/002387 FR0202387W WO03009826A1 WO 2003009826 A1 WO2003009826 A1 WO 2003009826A1 FR 0202387 W FR0202387 W FR 0202387W WO 03009826 A1 WO03009826 A1 WO 03009826A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- chosen
- dhea
- steroid
- composition according
- group
- Prior art date
Links
- 0 C[C@](CC1)(C(CC2)C(C(*)C3)C1[C@@](C)(CC1)C3C[C@]1O*)C2=O Chemical compound C[C@](CC1)(C(CC2)C(C(*)C3)C1[C@@](C)(CC1)C3C[C@]1O*)C2=O 0.000 description 1
Classifications
-
- 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
- A61K8/63—Steroids; Derivatives thereof
-
- 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
Definitions
- the present invention relates to the cosmetic use, by topical application to the skin, of at least one steroid chosen from: 7OH DHEA and its chemical derivatives, as a slimming agent, in particular for preventing and / or combating cellulite or orange peel and / or to refine facial contours.
- composition containing, in a physiologically acceptable medium, at least one steroid as defined above and at least one lipolytic agent other than said steroid.
- adipocytes which contain variable amounts of fat stored in the form of triglycerides.
- triglycerides are synthesized in vivo by the adipocytes themselves, according to reactions of the enzymatic type (lipogenesis), from the free fatty acids contained in the blood in the form of lipoproteins and the glucose provided in particular by means of certain foods.
- lipoproteins into fatty acids is done using an enzyme, lipoprotein lipase, contained in adipocytes or via cellular receptors for HDL, LDL or VLDL lipoproteins.
- the transformation of glucose leads either to the formation of glycerol or to the formation of free fatty acids via a specific enzyme, acetylCoA-carboxylase which transforms glucose into acetyl-CoA and then into fatty acids.
- the triglycerides thus formed, then stored, in the cells of the adipocytes can also degrade (lipolysis), always under the action of specific enzymes, the triglycerides lipases, contained in these same cells, and which are susceptible to '' be activated by cyclic AMP.
- Cyclic AMP is regulated by adenyl cyclase and capable of being hydrolyzed to 5'AMP by phosphodiesterase. This lipolysis mechanism leads to the release of fatty acids on the one hand and glycerol and / or mono- and or di-esters of glycerol on the other hand.
- the fatty acids thus released can then either diffuse in the organism to be consumed or transformed in different ways, or be re-captured (immediately or a little later) by the adipocytes to generate triglycerides again by lipogenesis.
- triglyceride lipase or hormone-sensitive lipase
- stimulating cyclic AMP generally by activation of adenyl cyclase, or by causing its accumulation by inhibition of phosphodiesterase.
- NPY neuropeptide Y receptor antagonists
- the cosmetic compositions hitherto proposed for the treatment of adiposity therefore contain so-called slimming compounds which act on one or more of the mechanisms mentioned above.
- xanthine bases ie xanthine derivatives
- theophylline caffeine, theobromine and 1-hydroxyalkylxanthines and their compatible salts
- nicotinic acid derivatives such as more particularly alpha-tocopherol nicotinate and hexyl nicotinate
- the so-called alpha-2 blocking substances capable of blocking the alpha-2 receptors on the surface of adipocytes such as, for example, ginkgo biloba (see in particular on this subject the document FR-A-2 669 537), and ⁇ 3-adrenergic receptor agonists such as alverine and
- DHEA has the capacity to inhibit the differentiation of adipocytes in vitro and in vivo, allowing to consider its use as slimming. It was further proposed in application ES-2 098 193 to use topically a composition containing DHEA and a xanthic base for the treatment of obesity. Topical anti-cellulite compositions based on DHEA are also disclosed in documents US-5,869,090 and US-6, 120,779.
- the invention relates to the cosmetic use, by topical application to the skin, of at least one steroid chosen from: 7OH DHEA and its chemical derivatives, as a slimming agent.
- the subject of the invention is the cosmetic use, by topical application to the skin, of at least one steroid chosen from: 7OH DHEA and its chemical derivatives, to prevent and / or fight against cellulite or the skin orange and / or to refine the contours of the face.
- 7-OH DHEA is meant, according to the present invention, both 7 ⁇ -OH DHEA and 7 ⁇ -OH DHEA. This term will therefore be used subsequently to identify either of these compounds. 7 ⁇ -OH DHEA is however preferred for use in the present invention. Its method of preparation is notably described in patent applications FR-2,771,105, WO 94/08588 and FR 01/01998.
- R1 and R2 are independently chosen from:
- heterocycle can advantageously be chosen from an indole, a pyrimidine, a piperidine, a morpholine, a pyran , furan, piperazine, pyridine;
- an alkylcarbonyl group the C1-C24 alkyl part of which is saturated or unsaturated, linear, branched or cyclic, and optionally substituted by one or more groups chosen from -OR 'and / or -SR' and / or -COOR 'and / or -NR'R 'and / or halogen and / or sulfate and / or phosphate and / or aryl and / or heterocycle
- said heterocycle can advantageously be chosen from an indole, a pyrimidine, a piperidine, a morpholine, a pyran, a furan, piperazine, pyridine;
- an arylcarbonyl group preferably a phenylcarbonyl, or an arylalkylcarbonyl group, preferably a benzylcarbonyl, optionally substituted by one or more groups -OR 'and / or -SR' and / or -COOR 'and / or -NR'R' and / or halogen and / or aryl and / or heterocycle;
- R ' is chosen from a hydrogen atom, a C1-C12, preferably C1-C6, saturated or unsaturated, linear, branched or cyclic alkyl group which may optionally contain one or more heteroatoms, optionally functionalized with one or more several groups -OR ", -COOR", halogen, -NR “R”; or by an aryl group, preferably a phenyl, optionally functionalized by one or more groups -OR ", -COOR", halogen or -NR “R”;
- R represents a hydrogen atom, an alkyl chain, preferably C1-C6, saturated or unsaturated, linear, branched or cyclic, it being understood that in each of the groups -NR'R 'and -NR" R ", the substituents R ', respectively R ", are the same or different.
- GATTEFOSSE under the trade name 3-acetoxy 7-benzoate DHEA.
- the steroid according to the invention is advantageously used in a composition containing a physiologically acceptable medium.
- physiologically acceptable medium is meant a medium compatible with the skin, the mucous membranes and / or the integuments.
- composition according to the invention can be applied locally to the areas of the face or of the body to be refined, in particular on the hips, the buttocks, the thighs, the belly, and the oval of the face.
- One of the great advantages of the present invention lies in the possibility of being able to carry out, whenever necessary or - desirable, very localized and selective "mild" treatments thanks to the mode of application by topical route.
- the amount of steroid which can be used according to the invention obviously depends on the desired effect and must be in an amount effective to promote thinning.
- the steroid can represent from 0.001% to 10% of the total weight of the composition and preferably from 0.001% to 5% of the total weight of the composition.
- this composition can be in all the galenical forms normally used.
- the composition can thus have the form in particular of an aqueous, alcoholic or hydroalcoholic solution or suspension or of an oily suspension or of a solution or dispersion of the lotion or serum type, of an emulsion of liquid or semi consistency -liquid of the milk type, obtained by dispersion of a fatty phase in an aqueous phase (O / W) or vice versa (W / O), or of a suspension or emulsion of soft consistency of the O / W or E / cream type H or an aqueous or anhydrous gel, an ointment, a free or compacted powder to be used as it is or to be incorporated in an excipient, or else microcapsules or microparticles, or vesicular dispersions of ionic type and / or non-ionic.
- These compositions are prepared according to the usual methods.
- compositions in the form of a foam or also in the form of aerosol compositions also comprising a propellant under pressure it is also possible to envisage a composition in the form of a foam or also in the form of aerosol compositions also comprising a propellant under pressure.
- the proportion of the fatty phase can range from 2% to 80% by weight, and preferably from 5% to 50% by weight relative to the total weight of the composition.
- the oils, waxes, emulsifiers and coemulsifiers used in the composition in the form of an emulsion are chosen from those conventionally used in the cosmetic field.
- the emulsifier and the coemulsifier are present in the composition in a proportion ranging from 0.1% to 30% by weight, and preferably from 0.5 to 20% by weight relative to the total weight of the composition.
- the emulsion may, in addition, contain lipid vesicles.
- the fatty phase can represent more than 90% of the total weight of the composition.
- the cosmetic composition may also contain adjuvants customary in the cosmetic field, such as hydrophilic gelling agents or lipophilic, hydrophilic or lipophilic additives, preservatives, antioxidants, solvents, perfumes, fillers, filters, odor absorbers and coloring matters.
- adjuvants customary in the cosmetic field such as hydrophilic gelling agents or lipophilic, hydrophilic or lipophilic additives, preservatives, antioxidants, solvents, perfumes, fillers, filters, odor absorbers and coloring matters.
- the amounts of these various adjuvants are those conventionally used in the cosmetic field, and for example from 0.01% to 10% of the total weight of the composition.
- These adjuvants depending on their nature, can be introduced into the fatty phase, into the aqueous phase and / or into the lipid spherules.
- emulsifiers which can be used in the invention, there may be mentioned for example stearate, glycerol, polysorbate 60 and the mixture of PEG-6 / PEG-32 / Glycol Stearate sold under the name Tefose R 63 by the company Gattefosse.
- solvents which can be used in the invention mention may be made of lower alcohols, in particular ethanol and isopropanol, propylene glycol.
- hydrophilic gelling agents which can be used in the invention, mention may be made of carboxyvinyl polymers (carbomers), acrylic copolymers such as acrylate / alkyl acrylate copolymers, polyacrylamides, polysaccharides such as hydroxypropylcellulose, natural gums and clays, and, as lipophilic gelling agents, mention may be made of modified clays such as bentones, metal salts of fatty acids such as aluminum stearates and hydrophobic silica, ethylcellulose, polyethylene.
- carboxyvinyl polymers carboxyvinyl polymers
- acrylic copolymers such as acrylate / alkyl acrylate copolymers
- polyacrylamides polysaccharides
- polysaccharides such as hydroxypropylcellulose
- natural gums and clays and, as lipophilic gelling agents
- modified clays such as bentones, metal salts of fatty acids such as aluminum stearates and hydrophobic silica
- the composition containing the steroid in a physiologically acceptable medium also contains at least one lipolytic agent and / or inhibitor of lipogenesis, other than said steroid.
- the composition is preferably, but not necessarily, suitable for topical application to the skin.
- the lipolytic agent can in particular be chosen from: phosphodiesterase inhibitors, ⁇ -2 blocking compounds capable of blocking ⁇ -2 receptors on the surface of adipocytes, ⁇ -adrenergic agonists, compounds inhibiting the synthesis of LDL receptors or VLDL, compounds stimulating ⁇ receptors and / or G proteins, glucose transport blockers, neuropeptide Y antagonists (NPY) capable of blocking NPY receptors on the surface of adipocytes, agents modifying acid transport fatty, lipolytic peptides and lipolytic proteins.
- phosphodiesterase inhibitors phosphodiesterase inhibitors
- ⁇ -2 blocking compounds capable of blocking ⁇ -2 receptors on the surface of adipocytes
- ⁇ -adrenergic agonists compounds inhibiting the synthesis of LDL receptors or VLDL
- compounds stimulating ⁇ receptors and / or G proteins glucose transport blockers
- NPY neuropeptide Y antagonists
- phosphodiesterase inhibitors As phosphodiesterase inhibitors, mention may in particular be made of xanthic bases and natural extracts containing them. Examples are constituted by cefine and its derivatives, in particular the 1-hydroxyalkylxanthines described in document FR-A-2 617 401, caffeine citrate, theophylline and its derivatives, theobromine, acefylline, aminophylline, chloroethyltheophylline, diprophylline, diniprophylline, etamiphylline and its derivatives, etofylline and proxyphylline.
- cefine and its derivatives in particular the 1-hydroxyalkylxanthines described in document FR-A-2 617 401, caffeine citrate, theophylline and its derivatives, theobromine, acefylline, aminophylline, chloroethyltheophylline, diprophylline, diniprophylline, etamiphylline and its derivatives,
- xanthic bases can be used alone or in commercial mixtures such as the combination of caffeine and alginate and caffeinate of methylsilanetriol sold by the company EXSYMOL under the trade name Caféisilane C.
- natural extracts containing xanthic bases mention may be made extracts of tea, coffee, guarana, mate, cola (Cola Nitida) and in particular the dry extract of guarana fruit (Paulina sorbilis) containing 8 to 10% caffeine.
- alverine As ⁇ -adrenergic agonist, mention may in particular be made of alverine or an organic or inorganic salt of alverine such as alverine citrate.
- lipolytic agents which can be used in the present invention are certain plant extracts not containing caffeine and certain extracts of marine origin. Among these, we can mention in particular:
- John's wort Boperycum perforatum
- fragon Ruscus acul ⁇ at ⁇ s L
- ulmaire Filipendula ulmaria L
- orthisiphon Orthosiphon stamincus benth
- birch Bertula alba
- cecropia argan, Ginkgo biloba, horsetail, escin, cangzhu, Chrysanthellum indicum, diosgenes rich in diosgenin including Dioscorea opposita or mexicana or villosa, plants of the genus Armeniacea, Atractylodis platicodon, sinom-menum, Pharbitidis or Flemingia, Coleus such as Coleus fors Moscowii or blumei or esquirolii or esquirolii or or barbatus, of ballote, of Gu / oa, of Davallia, of Terminalia, of Bar ⁇
- algae or phytoplankton extracts such as an extract of Laminaria digitata sold under the name PHYCOX75 by the company SECMA, the skeletonema alga as described in particular in patent FR-2,782 921 or diatoms such as those described in patent FR-2774292.
- lipolytic agent peptides or proteins such as the peptides derived from parathyroid hormone, described in particular in patents FR-2 788 058 and FR-2 781 231 or the peptides described in document FR-2 786 693, without this list being exhaustive. Mention may also be made of protamines and their derivatives such as those described in document FR-2758724.
- any compound acting on the metabolic pathways leading to the synthesis of triglycerides can be used.
- lipoprotein receptors LDL or others
- DDL lipoprotein receptors
- inhibitors of the synthesis of lipoprotein receptors such as extracts of Dioscorea opposita
- inhibitors of glucose uptake such as serine or rutin
- inhibitors enzymes of fatty acid synthesis such as acetyl CoA carboxylase or fatty acid synthetase and in particular cerulenine.
- the amount of lipolytic active agent or inhibitor of lipogenesis, other than the steroid, present in the composition according to the invention can vary to a large extent and will preferably be between 0.001 and 20% by weight, better still, between 0.1 and 10% by weight, relative to the total weight of the composition.
- the slimming composition according to the invention also contains at least one additional active agent chosen from: - the active ingredients acting on the microcirculation (vasculoprotectors or vasodilators) such as flavonoids, ruscogenins, natural or synthetic esculosides (including Permethol sold by the company SOCHIBO), escin extracted from horse chestnut, nicotinates, heperidin methyl chalcone, small holly, essential oils of lavender or rosemary, extracts of Ammi visnaga;
- the active ingredients acting on the microcirculation such as flavonoids, ruscogenins, natural or synthetic esculosides (including Permethol sold by the company SOCHIBO), escin extracted from horse chestnut, nicotinates, heperidin methyl chalcone, small holly, essential oils of lavender or rosemary, extracts of Ammi visnaga
- the active ingredients acting on the microcirculation such as flavonoids, ruscogenins, natural or synthetic esculosides (including Per
- the firming and / or anti-glycant active ingredients preventing the fixing of sugar on the collagen fibers
- active ingredients such as the extracts of Centella asiatica and Siegesbeckia, silicon, amadorine, ergothioneine and its derivatives, hydroxystilbenes and their derivatives, in particular resveratrol, plant extracts of the Ericaceae family, in particular extracts of bilberry (Vaccinium angustifollium), vitamin C and its derivatives and retinol and its derivatives.
- these complementary assets can vary to a large extent.
- these active agents will be present in the composition according to the invention in an amount representing from 0.01 to 15% and, better still, from 0.05 to 10% by weight, relative to the total weight of the composition.
- the present invention further relates to a cosmetic treatment process with a view to preventing and / or combating cellulite and / or orange peel and / or refining or thinning the silhouette or the contours of the face, comprising topical application to the skin of a composition comprising, in a physiologically acceptable medium, at least one steroid chosen from: 7OH DHEA, 7-oxo DHEA and their chemical derivatives.
- the present invention also relates to the use of at least one steroid chosen from: 7OH DHEA and its chemical derivatives for the preparation of a composition intended for the treatment of obesity.
- the steroid according to the invention can be administered orally.
- the steroid according to the invention can be administered at a rate of 1 to 200 mg / day, preferably from 25 to 75 mg / day.
- This composition can be in any dosage form suitable for this mode of administration, for example in the form of breakable tablets or not, granules, capsules, capsules, solutes, suspensions or solutions comprising an appropriate excipient.
- compositions illustrate the invention without limiting it no.
- proportions indicated are percentages by weight, unless otherwise indicated.
- phase A The polymer of phase A is dispersed in water at 40 ° C.
- the constituents of phase B are heated to 70 ° C until complete dissolution and then the temperature is reduced to 40 ° C.
- the constituents of phase C are mixed at 50 ° C.
- Phase B is introduced into phase A at 40 ° C with stirring and then phase C is added to them.
- Phases D then E are introduced into the mixture previously obtained.
- This cream is particularly well suited to the treatment of cellulite.
- This gel-cream can be prepared in the same way as the composition of Example 1.
- This cream can be applied morning and evening to the localized curves on the belly, buttocks and thighs to reduce them.
- a lotion having the following composition is prepared, conventionally for a person skilled in the art, intended to be introduced into an aerosol device.
- This lotion can be applied morning and / or evening by spraying on the parts of the body to be refined, where it forms a patch in situ which allows good penetration and prolonged diffusion of the active ingredients in the skin.
- This gel can be administered at the rate of 100 to 200 ml per day to treat overweight.
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Abstract
Description
Claims
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
FR0109854 | 2001-07-24 | ||
FR0109854A FR2827762A1 (en) | 2001-07-24 | 2001-07-24 | USE OF STEROIDS AS SLIMMERS |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2003009826A1 true WO2003009826A1 (en) | 2003-02-06 |
Family
ID=8865835
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/FR2002/002387 WO2003009826A1 (en) | 2001-07-24 | 2002-07-08 | Use of steroids as slimming agents |
Country Status (2)
Country | Link |
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FR (1) | FR2827762A1 (en) |
WO (1) | WO2003009826A1 (en) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2830015A1 (en) * | 2001-09-27 | 2003-03-28 | Berkem Sa | New air- and light-stable esters of hydroxylated pregnane and androstane series steroids, useful in phamaceutical, cosmetic or food compositions, e.g. skin creams |
JP2022106792A (en) * | 2021-01-08 | 2022-07-20 | 小林製薬株式会社 | Phosphodiesterase 5 activity inhibiting composition |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2862533B1 (en) * | 2003-11-21 | 2006-04-28 | Oreal | COSMETIC USE OF AT LEAST ONE ACTIVATOR IN THE PRODUCTION OF AN INTERLEUKIN 11 AS A TOPICAL SLIMMING AGENT |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1998040074A1 (en) * | 1997-03-10 | 1998-09-17 | Vitasterol (S.A.R.L.) | Cosmetic or dermatological use of 7-hydroxylated steroids |
US5869090A (en) * | 1998-01-20 | 1999-02-09 | Rosenbaum; Jerry | Transdermal delivery of dehydroepiandrosterone |
US6120779A (en) * | 1998-01-29 | 2000-09-19 | Soma Technologies | Use of partial and complete salts of choline and carboxylic acids for the treatment of skin disorders |
FR2803514A1 (en) * | 1999-10-13 | 2001-07-13 | Oreal | Composition used for treating chronological and actinic skin ageing contains dehydroepiandrosterone and desquamative agent |
-
2001
- 2001-07-24 FR FR0109854A patent/FR2827762A1/en not_active Withdrawn
-
2002
- 2002-07-08 WO PCT/FR2002/002387 patent/WO2003009826A1/en not_active Application Discontinuation
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1998040074A1 (en) * | 1997-03-10 | 1998-09-17 | Vitasterol (S.A.R.L.) | Cosmetic or dermatological use of 7-hydroxylated steroids |
US5869090A (en) * | 1998-01-20 | 1999-02-09 | Rosenbaum; Jerry | Transdermal delivery of dehydroepiandrosterone |
US6120779A (en) * | 1998-01-29 | 2000-09-19 | Soma Technologies | Use of partial and complete salts of choline and carboxylic acids for the treatment of skin disorders |
FR2803514A1 (en) * | 1999-10-13 | 2001-07-13 | Oreal | Composition used for treating chronological and actinic skin ageing contains dehydroepiandrosterone and desquamative agent |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2830015A1 (en) * | 2001-09-27 | 2003-03-28 | Berkem Sa | New air- and light-stable esters of hydroxylated pregnane and androstane series steroids, useful in phamaceutical, cosmetic or food compositions, e.g. skin creams |
JP2022106792A (en) * | 2021-01-08 | 2022-07-20 | 小林製薬株式会社 | Phosphodiesterase 5 activity inhibiting composition |
JP7331190B2 (en) | 2021-01-08 | 2023-08-22 | 小林製薬株式会社 | Composition for inhibiting phosphodiesterase 5 activity |
Also Published As
Publication number | Publication date |
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FR2827762A1 (en) | 2003-01-31 |
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