WO2001039740A1 - Novel topical compositions based on idazoxan and caffeine or soluble derivatives thereof and their use for slimming and/or for treating cellulitis - Google Patents
Novel topical compositions based on idazoxan and caffeine or soluble derivatives thereof and their use for slimming and/or for treating cellulitis Download PDFInfo
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- WO2001039740A1 WO2001039740A1 PCT/FR2000/003346 FR0003346W WO0139740A1 WO 2001039740 A1 WO2001039740 A1 WO 2001039740A1 FR 0003346 W FR0003346 W FR 0003346W WO 0139740 A1 WO0139740 A1 WO 0139740A1
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- idazoxan
- caffeine
- composition according
- soluble derivatives
- slimming
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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
- A61K8/49—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
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
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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
Definitions
- the present invention relates to new topical compositions based on Idazoxan and caffeine or its soluble derivatives and their use as a slimming agent and / or in the treatment of cellulite Idazoxan, the chemical structure of which is:
- 300427.2 describes the production of these derivatives and their pharmacological properties as inhibitors of the adrenergic ⁇ .2 receptors; these components are useful for treating depression, migraine and obesity.
- FR n ° 92 14694 and FR n ° 97 01 670 more particularly for the treatment of Parkinson's disease. More recently, the Applicant has sought applications topically and more particularly in the treatment of cellulite and adipose overloads located at the waist and thighs.
- new formulations are proposed making it possible to solve the problems of compatibility between several active agents, their stability as a function of physicochemical parameters such as the pH, in addition the Referenced formulations are those for which, surprisingly, a potentiation of the slimming activity is observed.
- caffeine and its soluble derivatives more particularly the carboxylic caffeines which have been the subject of patent FR 2 639 541, have been studied for the present invention.
- the present invention relates to a topical composition, useful as a slimming agent and / or in the treatment of cellulite comprising, as active principle and per 100 g of final formulation:
- the pH of the topical composition is from 3 to 6, preferably from 4 to 5.
- the cosmetic composition according to the present invention in addition to Idazoxan and the caffeine derivatives, can comprise other active principles leading to a complementary or possibly synergistic effect.
- composition according to the invention is generally an aqueous composition consisting of water or a mixture of water.
- the cosmetic composition may also contain at least one adjuvant usually used in topical compositions intended for the care of the skin.
- the cosmetic composition may be in the form of cream, milk, lotion, serum, transdermal device, gel, oil in water emulsion, water in oil emulsion, optionally two- or three-phase.
- the present invention also relates to a method of cosmetic treatment of the human or animal body, in particular for the treatment of cellulite, consisting in applying to the human or animal body a composition according to the present invention.
- Figure 1 represents the UV spectrum of Idazoxan hydrochloride
- Figure 6 represents the reaction kinetics profile at 3 wavelengths (240, 274 and 294 nm) at pH 7.5
- FIG. 7 represents the reaction kinetics profile at 3 wavelengths
- Figure 8 shows the diffusion flow of a gel containing 0.5% Idazoxan alone and a gel containing 0.5% Idazoxan and 1.5% caffeine.
- Figure 9 shows the distribution (dermis / epidermis) after 24 hours of diffusion expressed as a percentage of the quantity deposited
- Idazoxan may degrade by hydrolysis depending on the reaction
- the degradation products are monitored by spectrography in ultra violet at characteristic wavelengths (240, 274 and 294 nm)
- the optimal pH is acidic, but thanks to the excipients used in the formulation, this pH is compatible with good tolerance Idazoxan stability measurement techniques
- Table IV percentage change in the thickness of adipose tissue on the treated side
- Glycerol qs Example 5 Liquid biphasic single dose. Liquid with extemporaneous dilution or for alternate use to be used in two-compartment single doses.
- Phase 1 PEG 200 80 g
Abstract
The invention concerns topical compositions, useful for slimming and/or for treating cellulitis, comprising as active principle and for 100 g of final formulation: 10 to 400 mg of Idazoxan (structure I) in free form or its salts acceptable in dermatology; and 1 to 10 g of caffeine or its soluble derivatives and having a pH of 3 to 6. The invention also concerns a cosmetic method for treating the human or animal body, in particular for treating cellulitis using said compositions.
Description
Titre : NOUVELLES COMPOSITIONS TOPIQUES A BASE D'IDAZOXAN ET DE CAFEINE OU DE SES DERIVES SOLUBLES ET LEUR UTILISATION COMME AMINCISSANT ET/OU DANS LE TRAITEMENT DE LA CELLULITETitle: NEW TOPICAL COMPOSITIONS BASED ON IDAZOXAN AND CAFFEINE OR ITS SOLUBLE DERIVATIVES AND THEIR USE AS SLIMMERS AND / OR IN THE TREATMENT OF CELLULITE
La présente invention concerne de nouvelles compositions topiques à base d'Idazoxan et de caféine ou de ses dérivés solubles et leur utilisation comme amincissant et/ou dans le traitement de la cellulite L'Idazoxan dont la structure chimique est :The present invention relates to new topical compositions based on Idazoxan and caffeine or its soluble derivatives and their use as a slimming agent and / or in the treatment of cellulite Idazoxan, the chemical structure of which is:
a été développé avec une série de dérivés imidazoliniques par RECKITT etwas developed with a series of imidazolinic derivatives by RECKITT and
COLMAN ; le brevet européen déposé le 2 février 1981 sous le numéro 81COLMAN; the European patent filed on February 2, 1981 under number 81
300427.2 décrit l'obtention de ces dérivés et les propriétés pharmacologiques en tant qu'inhibiteurs des récepteurs α.2 adrenergiques; ces composants sont utiles pour traiter la dépression, la migraine et l'obésité.300427.2 describes the production of these derivatives and their pharmacological properties as inhibitors of the adrenergic α.2 receptors; these components are useful for treating depression, migraine and obesity.
Des travaux ont été entrepris qui ont conduit au dépôt de nouveaux brevetsWork was undertaken which led to the filing of new patents
(FR n°92 14694 et FR n°97 01670) plus particulièrement pour le traitement de la maladie de Parkinson. Plus récemment, la demanderesse a recherché des applications par voie topique et plus particulièrement dans le traitement de la cellulite et des surcharges adipeuses situées au niveau de la taille et des cuisses.(FR n ° 92 14694 and FR n ° 97 01 670) more particularly for the treatment of Parkinson's disease. More recently, the Applicant has sought applications topically and more particularly in the treatment of cellulite and adipose overloads located at the waist and thighs.
Selon la présente invention de nouvelles formulations sont proposées permettant de résoudre les problèmes de compatibilité entre plusieurs actifs, leur stabilité en fonction de paramètres physico-chimiques tels que le pH, en outre les
formulations référées sont celles pour lesquelles, de façon surprenante, on observe une potentialisation de l'activité amincissante.According to the present invention, new formulations are proposed making it possible to solve the problems of compatibility between several active agents, their stability as a function of physicochemical parameters such as the pH, in addition the Referenced formulations are those for which, surprisingly, a potentiation of the slimming activity is observed.
Parmi les actifs associés à l'Idazoxan, la caféine et ses dérivés solubles, plus particulièrement les caféines carboxyliques ayant fait l'objet du brevet FR 2 639 541, ont été étudiés pour la présente invention.Among the active agents associated with Idazoxan, caffeine and its soluble derivatives, more particularly the carboxylic caffeines which have been the subject of patent FR 2 639 541, have been studied for the present invention.
La présente invention concerne une composition topique, utile comme amincissant et/ou dans le traitement de la cellulite comportant à titre de principe actif et pour 100 g de formulation finale :The present invention relates to a topical composition, useful as a slimming agent and / or in the treatment of cellulite comprising, as active principle and per 100 g of final formulation:
10 à 400 mg, de préférence 10 à 100 mg, d 'Idazoxan sous forme libre ou de ses sels dermatologiquement acceptables, de préférence sous forme de sels de chlorhydrate, et10 to 400 mg, preferably 10 to 100 mg, of Idazoxan in free form or its dermatologically acceptable salts, preferably in the form of hydrochloride salts, and
1 à 10 g, de préférence 1,5 à 5g, de caféine ou de ses dérivés solubles, de préférence les caféines carboxyliques. Selon la présente invention, le pH de la composition topique est de 3 à 6, de préférence de 4 à 5.1 to 10 g, preferably 1.5 to 5 g, of caffeine or its soluble derivatives, preferably carboxylic caffeines. According to the present invention, the pH of the topical composition is from 3 to 6, preferably from 4 to 5.
La composition cosmétique selon la présente invention, outre l'Idazoxan et les dérivés de caféines, peut comprendre d'autres principes actifs conduisant à un effet complémentaire ou éventuellement synergique.The cosmetic composition according to the present invention, in addition to Idazoxan and the caffeine derivatives, can comprise other active principles leading to a complementary or possibly synergistic effect.
On citera notamment les vitamines, les oligo-éléments, les dérivés protéiques, les huiles essentielles. Bien entendu cette liste n'est pas limitative et l'homme du métier pourra avec ses connaissances choisir d'autres matières actives qui en complément de la composition cosmétique selon l'invention produiront l'effet souhaité.These include vitamins, trace elements, protein derivatives, essential oils. Of course this list is not exhaustive and the person skilled in the art can, with his knowledge, choose other active materials which, in addition to the cosmetic composition according to the invention, will produce the desired effect.
La composition selon l'invention est généralement une composition aqueuse constituée par de l'eau ou un mélange d'eau.The composition according to the invention is generally an aqueous composition consisting of water or a mixture of water.
La composition cosmétique peut en outre renfermer au moins un adjuvant utilisé habituellement dans les compositions topiques destinées au soin de la peau.The cosmetic composition may also contain at least one adjuvant usually used in topical compositions intended for the care of the skin.
Parmi ces adjuvants, on peut citer les épaississants, les agents conservateurs, les agents antioxydants, les filtres solaires, les parfums, les colorants, les agents hydratants, les eaux thermales, les pigments minéraux, les émollients, les tensioactifs, les polymères, les huiles de silicone etc.
La composition cosmétique peut se présenter sous la forme de crème, lait, lotion, sérum, dispositif transdermique, gel, émulsion huile dans l'eau, émulsion eau dans l'huile, éventuellement bi- ou tri-phasique.Among these adjuvants, mention may be made of thickeners, preservatives, antioxidants, sunscreens, perfumes, dyes, hydrating agents, thermal waters, mineral pigments, emollients, surfactants, polymers, silicone oils etc. The cosmetic composition may be in the form of cream, milk, lotion, serum, transdermal device, gel, oil in water emulsion, water in oil emulsion, optionally two- or three-phase.
La présente invention concerne également une méthode de traitement cosmétique du corps humain ou animal, notamment pour le traitement de la cellulite consistant à appliquer sur le corps humain ou animal une composition selon la présente invention.The present invention also relates to a method of cosmetic treatment of the human or animal body, in particular for the treatment of cellulite, consisting in applying to the human or animal body a composition according to the present invention.
Les figures présentées en annexe sont explicitées ci après La figure 1 représente le spectre UV du chlorhydrate d'Idazoxan La figure 2 représente le spectre UV du chlorhydrate d'Idazoxan à pH = 6The figures presented in the appendix are explained below. Figure 1 represents the UV spectrum of Idazoxan hydrochloride Figure 2 represents the UV spectrum of Idazoxan hydrochloride at pH = 6
La figure 3 représente le spectre UV du chlorhydrate d'Idazoxan à pH = 7,5 La figure 4 représente le spectre UV du chlorhydrate d'Idazoxan à pH = 8,9 La figure 5 représente le spectre UV du chlorhydrate d'Idazoxan à pH = 13 La figure 6 représente le profil de cinétique de réaction à 3 longueurs d'onde (240, 274 et 294 nm) au pH de 7,5Figure 3 shows the UV spectrum of Idazoxan hydrochloride at pH = 7.5 Figure 4 shows the UV spectrum of Idazoxan hydrochloride at pH = 8.9 Figure 5 shows the UV spectrum of Idazoxan hydrochloride at pH = 13 Figure 6 represents the reaction kinetics profile at 3 wavelengths (240, 274 and 294 nm) at pH 7.5
La figure 7 représente le profil de cinétique de réaction à 3 longueurs d'ondeFIG. 7 represents the reaction kinetics profile at 3 wavelengths
(240, 274 et 294 nm) au pH de 9,8(240, 274 and 294 nm) at pH 9.8
La figure 8 représente le flux de diffusion d'un gel contenant 0,5% d'Idazoxan seul et d'un gel contenant 0,5% d'Idazoxan et 1,5% de caféine La figure 9 représente la répartition (derme/épiderme) au bout de 24h de diffusion exprimée en pourcentage de la quantité déposéeFigure 8 shows the diffusion flow of a gel containing 0.5% Idazoxan alone and a gel containing 0.5% Idazoxan and 1.5% caffeine. Figure 9 shows the distribution (dermis / epidermis) after 24 hours of diffusion expressed as a percentage of the quantity deposited
STABILITESTABILITY
L'étude a été conduite à partir de solution d'Idazoxan en faisant varier le pH pour déterminer les conditions optimalesThe study was conducted using Idazoxan solution by varying the pH to determine the optimal conditions
L'Idazoxan peut se dégrader par hydrolyse selon la réaction
Idazoxan may degrade by hydrolysis depending on the reaction
Le suivi des produits de dégradation est réalisé par spectrographie dans l'ultra violet aux longueurs d'ondes caractéristiques (240, 274 et 294 nm)The degradation products are monitored by spectrography in ultra violet at characteristic wavelengths (240, 274 and 294 nm)
Tableau I : stabilité de l'exemple 1 à différents pHTable I: stability of Example 1 at different pHs
Le pH optimal est acide, mais grâce aux excipients utilises dans la formulation, ce pH est compatible avec une bonne tolérance
Techniques de mesure de la stabilité de l'IdazoxanThe optimal pH is acidic, but thanks to the excipients used in the formulation, this pH is compatible with good tolerance Idazoxan stability measurement techniques
La stabilité du chlorhydrate d'Idazoxan (CnHι2N202, HC1 = 240,69 g/mol CAS Number 79944-56-2) est suivie par spectrophotométπe UV en solution aqueuse à différents pH (figure 1 à 5)The stability of Idazoxan hydrochloride (C n Hι 2 N 2 0 2 , HC1 = 240.69 g / mol CAS Number 79944-56-2) is followed by UV spectrophotometry in aqueous solution at different pH (Figure 1 to 5)
La structure du chlorhydrate d'Idazoxan a été déterminée par RMN du proton à 250MHzThe structure of Idazoxan hydrochloride was determined by proton NMR at 250 MHz
Déplacement (ppm) 6,95 - 7,06 (m, 4 H) protons aromatiques , 5,42 - 5,45 (t, 1 H) CH sur dioxanne, 4,41 - 4,43 (qd, 2 H) CH2 sur dioxanne , 3,93 (s, 4H) CH2-CH2 sur le noyau imidazorineDisplacement (ppm) 6.95 - 7.06 (m, 4 H) aromatic protons, 5.42 - 5.45 (t, 1 H) CH on dioxane, 4.41 - 4.43 (qd, 2 H) CH 2 on dioxane, 3.93 (s, 4H) CH 2 -CH 2 on the imidazorine nucleus
(m massif , s singulet , t triplet , qd quadruplet dédoublé)(m massive, s singlet, t triplet, qd quadruplet split)
Tableau II : solutions tampons réaliséesTable II: buffer solutions produced
L'étude de la décomposition de l'Idazoxan par spectroscope UV multi- longueur d'onde montre que le spectre obtenu au cours de l'hydrolyse dépend du pH (figure 1 à 5)The study of the decomposition of Idazoxan by multi-wavelength UV spectroscope shows that the spectrum obtained during hydrolysis depends on the pH (Figure 1 to 5)
3 longueurs d'onde ont été choisies pour suivre la cinétique de la reaction 240, 274 et 294 nm Les cinétiques des reactions sont suivies à différents pH (figure 6 et 7)
Il a été ainsi démontré que dans les conditions de l'expérience l'Idazoxan est stable pour des pH acides (tl/2 = 2,1 j à pH = 7, 1 , tl/2 = 200 j à pH = 5,0)3 wavelengths were chosen to follow the kinetics of the reaction 240, 274 and 294 nm The kinetics of the reactions are followed at different pH (Figure 6 and 7) It has thus been demonstrated that under the conditions of the experiment Idazoxan is stable for acid pHs (tl / 2 = 2.1 d at pH = 7.1, tl / 2 = 200 d at pH = 5.0 )
PROPRIETES PHARMACOCLNETIQUESPHARMACOCLNETIC PROPERTIES
Une étude de pharmacocinétique réalisée en laboratoire a permis d'apprécier le passage transcutané de l'Idazoxan, appliqué seul ou en association avec de la caféine afin de mettre en évidence l'intensité du passage de l'Idazoxan Le dosage est réalisé par scintillation liquide en double comptage dans le liquide récepteur et dans les différents compartiments cutanésA pharmacokinetic study carried out in the laboratory made it possible to assess the transcutaneous passage of Idazoxan, applied alone or in combination with caffeine in order to highlight the intensity of the passage of Idazoxan The assay is carried out by liquid scintillation double counting in the receiving liquid and in the various skin compartments
L'étude montre que la cinétique de diffusion de l'Idazoxan est comparable en présence ou non de caféine (figure 8) L'étude porte sur l'application de deux gelsThe study shows that the kinetics of diffusion of Idazoxan is comparable in the presence or not of caffeine (Figure 8) The study relates to the application of two gels
- un gel contenant 0,5% d'Idazoxan seul- a gel containing 0.5% Idazoxan alone
- un gel contenant 0,5% d'Idazoxan et 1,5% de caféine Par ailleurs, l'étude met en évidence la répartition épidermique au bout de- a gel containing 0.5% Idazoxan and 1.5% caffeine In addition, the study highlights the epidermal distribution after
24 heures de diffusion (figure 9) exprimée en pourcentage de la quantité déposée On conclut à un bon passage de l'Idazoxan, comparable à celui de la caféine24 hours of diffusion (Figure 9) expressed as a percentage of the quantity deposited We conclude that Idazoxan passes well, comparable to that of caffeine
PROPRIETES PHARMACOLOGIQUESPHARMACOLOGICAL PROPERTIES
L'évaluation de l'efficacité des produits est réalisée grâce à une méthode échographique (RICHARD B , Echographie Principes et Techniques, J Med Nucl Biophy, 1991, 15, 123-131 et PERLN F , PITTET J C , PERRIER P , SCHNEBERT S , BEAU P , Ultrasound Imaging assessment of adipose tissue thickness varriations during the menstrual cycle, Skin Research and Technology, 1997, 3, 204), laquelle permet d'évaluer l'épaisseur du tissu adipeux au niveau de la cuisse L'évaluation est réalisée pendant 14 jours, sur 20 volontaires sains, répondant strictement aux critères d'inclusion et d'exclusion du protocole d'étude Les résultats sont reportés dans les tableaux III et IV ci-après
Tableau Hl : mesure de l'épaisseur de tissu adipeux côté traité (en mm)The effectiveness of the products is assessed using an ultrasound method (RICHARD B, Principles and Techniques Echography, J Med Nucl Biophy, 1991, 15, 123-131 and PERLN F, PITTET JC, PERRIER P, SCHNEBERT S, BEAU P, Ultrasound Imaging assessment of adipose tissue thickness varriations during the menstrual cycle, Skin Research and Technology, 1997, 3, 204), which makes it possible to assess the thickness of adipose tissue in the thigh The assessment is carried out during 14 days, out of 20 healthy volunteers, strictly meeting the inclusion and exclusion criteria of the study protocol The results are reported in Tables III and IV below Table Hl: measurement of the thickness of adipose tissue on the treated side (in mm)
Tableau IV : pourcentage d'évolution de l'épaisseur de tissu adipeux côté traitéTable IV: percentage change in the thickness of adipose tissue on the treated side
Un effet synergique de l'action de la caféine et de celle de l'Idazoxan est donc observé de façon surprenante.A synergistic effect of the action of caffeine and that of Idazoxan is therefore surprisingly observed.
A titre d'exemples non limitatifs, nous décrivons quelques formulations qui illustrent l'invention sans en limiter la portée :By way of nonlimiting examples, we describe some formulations which illustrate the invention without limiting its scope:
Exemple 1 :Example 1:
Idazoxan 10-400 mgIdazoxan 10-400 mg
Stéarate de sorbitane 3 gSorbitan stearate 3 g
Stéarate de sorbitane polyoxyéthylénée 3 gPolyoxyethylenated sorbitan stearate 3 g
Alcool oléique polyoxyéthylénée 2 gPolyoxyethylene oleic alcohol 2 g
Huile minérale et animale 30 gMineral and animal oil 30 g
Huiles de silicones 20 gSilicone oils 20 g
Caféine dispersée 5-10 gDispersed caffeine 5-10 g
Conservateur, parfum, colorant qs pour une formule émulsionnée
Exemple 2 : monodose biphasiquePreservative, perfume, coloring qs for an emulsified formula Example 2: biphasic single dose
Phase poudre :Powder phase:
Idazoxan chlorhydrate 10-100 mgIdazoxan hydrochloride 10-100 mg
Béhénate de glycérol 5 g Phase liquide :Glycerol behenate 5 g Liquid phase:
Caféine anhydre 1,5 gAnhydrous caffeine 1.5 g
Acide caféine carboxylique 7,0 gCaffeine carboxylic acid 7.0 g
Triethanolamine 2 gTriethanolamine 2 g
Carbonate de guanidine 2,2 g Excipient qsGuanidine carbonate 2.2 g Excipient qs
Exemple 3Example 3
Caféine anhydre 1,5 gAnhydrous caffeine 1.5 g
Caféine carboxylate de 3-nicotinol 7,0 g Gomme xanthane 0,5 gCaffeine 3-nicotinol carboxylate 7.0 g Xanthan gum 0.5 g
Gel de polyacrylate 0,3 gPolyacrylate gel 0.3 g
Acide salicylique 1,0 gSalicylic acid 1.0 g
Idazoxan chlorhydrate 10-400 mg Système acide pH < 4Idazoxan hydrochloride 10-400 mg Acid system pH <4
Exemple 4 : Composition é ulsionnée sur base siliconeEXAMPLE 4 Composition E ulsioned on Silicone Base
Idazoxan chlorhydrate 10-400 mgIdazoxan hydrochloride 10-400 mg
Diméthicone copohyol 5 gDimethicone copohyol 5 g
Cyclométhicone 10 gCyclomethicone 10 g
Hexaméthyldisiloxane 10 gHexamethyldisiloxane 10 g
Alcanediol 25 gAlcanediol 25 g
Propylène glycol 5 gPropylene glycol 5 g
Acide Caféine carboxylique 5 gCaffeine carboxylic acid 5 g
Glycérol qs
Exemple 5 : Monodose biphasique liquide. Liquide à dilution extemporanee ou à usage alterné à utiliser dans des unidoses bicompartimentales.Glycerol qs Example 5: Liquid biphasic single dose. Liquid with extemporaneous dilution or for alternate use to be used in two-compartment single doses.
Phase 1 : PEG 200 80 gPhase 1: PEG 200 80 g
Alcool cétostéarylique ethoxylé 20 gEthoxylated cetostearyl alcohol 20 g
Idazoxan 20 à 1 OOmgIdazoxan 20 to 1 OOmg
Phase 2 :Phase 2:
Caféine anhydre 1,5 g Acide caféine carboxylique 7,0 gAnhydrous caffeine 1.5 g Caffeine carboxylic acid 7.0 g
Alcool oléique polyoxyéthyléné 1,0 gPolyoxyethylene oleic alcohol 1.0 g
Gomme xanthane 0,4 gXanthan gum 0.4 g
Gel de polyacrylate 0,5 gPolyacrylate gel 0.5 g
Créatinol 4,3 g Conservateur, parfum, colorant qs
Creatinol 4.3 g Preservative, fragrance, color qs
Claims
1. Composition topique, utile comme amincissant et/ou dans le traitement de la cellulite, caractérisée en ce qu'elle comporte à titre de principe actif et pour 100 g de formulation finale :1. Topical composition, useful as a slimming agent and / or in the treatment of cellulite, characterized in that it comprises, as active principle and per 100 g of final formulation:
10 à 400 mg d'Idazoxan sous forme libre ou de ses sels dermatologiquement acceptables, et 1 à 10 g de caféine ou de ses dérivés solubles et que son pH est de 3 à 6. 10 to 400 mg of Idazoxan in free form or its dermatologically acceptable salts, and 1 to 10 g of caffeine or its soluble derivatives and that its pH is 3 to 6.
2. Composition selon la revendication 1, caractérisé en ce que l'Idazoxan est sous forme de sels de chlorhydrate.2. Composition according to claim 1, characterized in that Idazoxan is in the form of hydrochloride salts.
3. Composition selon les revendications 1 ou 2, caractérisée en ce que les dérivés de caféine sont des caféines carboxyliques.3. Composition according to claims 1 or 2, characterized in that the caffeine derivatives are carboxylic caffeines.
4. Composition selon l'une quelconque des revendications précédentes, caractérisée en ce qu'elle comporte 10 à 100 mg d'Idazoxan.4. Composition according to any one of the preceding claims, characterized in that it comprises 10 to 100 mg of Idazoxan.
5. Composition selon l'une quelconque des revendications précédentes, caractérisée en ce qu'elle comporte 1,5 à 5 g de caféine ou de ses dérivés solubles.5. Composition according to any one of the preceding claims, characterized in that it comprises 1.5 to 5 g of caffeine or of its soluble derivatives.
6. Composition selon l'une quelconque des revendications précédentes, caractérisée en ce que son pH est de 4 à 5. 6. Composition according to any one of the preceding claims, characterized in that its pH is from 4 to 5.
7. Composition selon l'une quelconque des revendications précédentes, caractérisée en ce qu'elle se trouve sous forme de crème, lait, lotion, sérum, dispositif transdermique, gel, émulsion huile dans l'eau, émulsion eau dans l'huile, éventuellement bi- ou tri-phasique.7. Composition according to any one of the preceding claims, characterized in that it is in the form of a cream, milk, lotion, serum, transdermal device, gel, oil in water emulsion, water in oil emulsion, possibly bi- or tri-phasic.
8. Méthode de traitement cosmétique du corps humain ou animal, notamment pour le traitement de la cellulite caractérisée en ce qu'elle consiste à appliquer sur le corps humain ou animal une composition selon l'une quelconque des revendications précédentes. 8. A method of cosmetic treatment of the human or animal body, in particular for the treatment of cellulite, characterized in that it consists in applying to the human or animal body a composition according to any one of the preceding claims.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9915141A FR2801786B1 (en) | 1999-12-01 | 1999-12-01 | NOVEL TOPICAL COMPOSITIONS BASED ON IDAZOXAN AND CAFFEINE OR ITS SOLUBLE DERIVATIVES AND THEIR USE AS SLIMMERS AND / OR IN THE TREATMENT OF CELLULITE |
| FR99/15141 | 1999-12-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2001039740A1 true WO2001039740A1 (en) | 2001-06-07 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/FR2000/003346 WO2001039740A1 (en) | 1999-12-01 | 2000-11-30 | Novel topical compositions based on idazoxan and caffeine or soluble derivatives thereof and their use for slimming and/or for treating cellulitis |
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| Country | Link |
|---|---|
| FR (1) | FR2801786B1 (en) |
| WO (1) | WO2001039740A1 (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002026216A1 (en) * | 2000-09-26 | 2002-04-04 | Pierre Fabre Medicament | Pharmaceutical oxan preparation |
| FR2861299A1 (en) * | 2003-10-28 | 2005-04-29 | Pf Medicament | Pharmaceutical composition for prevention or treatment of e.g. depression, Parkinson's disease comprises idazoxan salt or idazoxan hydrate, microcrystalline cellulose, lubricant, colloidal silica and lactose |
| US7595335B2 (en) | 2003-10-28 | 2009-09-29 | Pierre Fabre Medicament | Pharmaceutical composition based on idazoxan, salts, hydrates or polymorphs thereof |
| US8476307B2 (en) | 2003-10-28 | 2013-07-02 | Pierre Fabre Medicament | Pharmaceutical composition based on idazoxan, salts, hydrates or polymorphs thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0033655A2 (en) * | 1980-02-04 | 1981-08-12 | Reckitt And Colman Products Limited | Imidazoline derivative, its salts, process for preparation and pharmaceutical compositions thereof |
| US4288433A (en) * | 1976-11-08 | 1981-09-08 | L'oreal | Cosmetic compositions having a slimming action |
| US4938962A (en) * | 1987-12-07 | 1990-07-03 | Pierre Fabre Cosmetique | Heterogeneous topical compositions having a base of microgranules of caffeine and/or its derivatives, which can be used as slenderizer and/or in the treatment of cellulitis, as well as their preparation |
| FR2733149A1 (en) * | 1995-04-21 | 1996-10-25 | Sederma Sa | Stable slimming cosmetic contg. cyclic adenosine mono:phosphate, caffeine |
-
1999
- 1999-12-01 FR FR9915141A patent/FR2801786B1/en not_active Expired - Fee Related
-
2000
- 2000-11-30 WO PCT/FR2000/003346 patent/WO2001039740A1/en active Application Filing
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4288433A (en) * | 1976-11-08 | 1981-09-08 | L'oreal | Cosmetic compositions having a slimming action |
| EP0033655A2 (en) * | 1980-02-04 | 1981-08-12 | Reckitt And Colman Products Limited | Imidazoline derivative, its salts, process for preparation and pharmaceutical compositions thereof |
| US4938962A (en) * | 1987-12-07 | 1990-07-03 | Pierre Fabre Cosmetique | Heterogeneous topical compositions having a base of microgranules of caffeine and/or its derivatives, which can be used as slenderizer and/or in the treatment of cellulitis, as well as their preparation |
| FR2733149A1 (en) * | 1995-04-21 | 1996-10-25 | Sederma Sa | Stable slimming cosmetic contg. cyclic adenosine mono:phosphate, caffeine |
Non-Patent Citations (1)
| Title |
|---|
| S. K. NORDEEN ET AL: "Modulation of Glucocorticoid-regulated transcription by purines: novel characteristics and implications for tissue specificity of steroid responses", ENDOCRINOLOGY, vol. 136, no. 3, March 1995 (1995-03-01), pages 1120 - 1127, XP002146319 * |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002026216A1 (en) * | 2000-09-26 | 2002-04-04 | Pierre Fabre Medicament | Pharmaceutical oxan preparation |
| FR2861299A1 (en) * | 2003-10-28 | 2005-04-29 | Pf Medicament | Pharmaceutical composition for prevention or treatment of e.g. depression, Parkinson's disease comprises idazoxan salt or idazoxan hydrate, microcrystalline cellulose, lubricant, colloidal silica and lactose |
| WO2005041956A1 (en) * | 2003-10-28 | 2005-05-12 | Pierre Fabre Medicament | Pharmaceutical compositions based on idazoxan salt or one of the polymorphs thereof |
| US7338970B2 (en) | 2003-10-28 | 2008-03-04 | Pierre Fabre Medicament | Pharmaceutical composition based on a polymorphic form I of idazoxan |
| US7595335B2 (en) | 2003-10-28 | 2009-09-29 | Pierre Fabre Medicament | Pharmaceutical composition based on idazoxan, salts, hydrates or polymorphs thereof |
| US8124640B2 (en) | 2003-10-28 | 2012-02-28 | Pierre Fabre Medicament | Pharmaceutical composition based on idazoxan, salts, hydrates or polymorphs thereof |
| US8476307B2 (en) | 2003-10-28 | 2013-07-02 | Pierre Fabre Medicament | Pharmaceutical composition based on idazoxan, salts, hydrates or polymorphs thereof |
| CN102349873B (en) * | 2003-10-28 | 2013-09-25 | 皮埃尔法布雷医药公司 | Pharmaceutical compositions based on idazoxan salt or one of polymorphs thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| FR2801786A1 (en) | 2001-06-08 |
| FR2801786B1 (en) | 2002-03-01 |
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