Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/465—Nicotine; Derivatives thereof
• • 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
  • A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
  • A61K8/4926—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P17/00—Drugs for dermatological disorders
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/06—Preparations for care of the skin for countering cellulitis

Definitions

• the subject of the invention is a composition based on free nicotine. It also relates to the use of said composition for reducing or eliminating any localized fatty overload of the cellulite type in particular. Finally, it relates to the cosmetic treatment of cellulite by local application of said cosmetic composition.
• LGL localized gynoid lipodystrophy
• LGL Localized gynoid lipodystrophy
• the classic treatment is based on local techniques based on massages and drainage, whose effectiveness is limited, or even liposuction or liposuction in difficult cases. But liposuction is especially interesting when the LGL is mainly adipose, not very organized.
• enzymes aimed at depolymerizing proteoglycans have been proposed, in particular hyaluronidase, thiomucase and Foc-mucase.
• Methods for stimulating lipolysis have also been proposed, the best known and most used being that which consists of inhibiting phosphodiesterase in order to limit the rate of degradation of cyclic AMP.
• the activation of cyclic AMP intervenes in the lipolytic activity of the adypocyte.
• phosphodiesterase inhibitors which have been recommended as weight loss agents, mention may in particular be made of xantics and more particularly theophyline, caffeine and theobromine.
• Document DE4461308 thus describes an anticellulitic composition associating a plant extract and an activator of the metabolism of the vitamin E type in the form of salt, in particular of nicotinate and with a draining active.
• Free nicotine has been used for many years in smoking cessation, since the nicotine contained in tobacco smoke leads to real physical dependence, the brutal withdrawal of which gives rise to serious mental and physical disorders. Consequently, free nicotine is incorporated into topical pharmaceutical compositions of the patch or oral type, of the chewing gum or oral lozenge type. Free nicotine can also be administered transmucosally using, for example, a nasal spray. Whatever the type of drugs used, the objective of smoking cessation is to deliver a sufficient amount of free nicotine in the brain and in the system as a whole for said withdrawal to be effective while being controlled. This is the reason why it is imperative to deliver a relatively large amount of nicotine continuously or at regular intervals, from 14 to 21 mg / 24 hours, or even more in certain cases of strong dependence on nicotine. These doses are then reduced to finalize weaning.
• the subject of the invention is therefore a topical cosmetic composition
• a topical cosmetic composition comprising nicotine in admixture with at least one cosmetically acceptable vehicle, which is characterized in that the nicotine is free nicotine.
• the free nicotine represents between 0.001 and 0.5% by weight of the composition.
• the topical composition of the invention is used in local application and can therefore be in various forms such as gel, oily gel, cream, ointment, milk, lotion, balm, spray, emulsion, patch, stick.
• the proportion of the fatty phase can range from 5% 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 0.3% to 30% by weight, and preferably from 0.5 to 20% by weight relative to the total weight of the composition.
• the cosmetic composition may also contain adjuvants customary in the cosmetic field, such as hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic additives, preservatives, antioxidants, solvents, perfumes, fillers, filters, odor absorbers and coloring matters.
• adjuvants customary in the cosmetic field such as hydrophilic or lipophilic gelling agents, 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.
• 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 (carbomer), acrylic copolymers such as acrylate / alkylacrylate 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
• the invention also relates to the use of the composition as described above, for reducing or limiting any localized fatty overload, of the cellulite type in particular.
• free nicotine is also planned for the manufacture of a composition intended to reduce or limit any localized fatty overload, of the cellulite type in particular.
• the invention also relates to the use of the cosmetic composition described above for increasing the firmness of the epidermis. This property is particularly advantageous for the treatment of wrinkles.
• composition described above for combating skin aging.
• the invention relates to the use of the composition described above to improve the smoothness of the epidermis.
• the invention also relates to a method of cosmetic treatment of local fatty overloads of the cellulite type in particular, according to which a locally effective amount of the composition described above is applied topically.
• the amount of nicotine released does not exceed 5 mg per application, it is advantageously between 0.3 and 3 mg.
• the Applicant has carried out a comparative trial intended to assess the effectiveness of the composition of the invention, in local topical application, in patients with gynoid lipodystrophy of the thighs and buttocks, in comparison with a placebo, considered as a control group. Concomitantly, the effects of the composition on the softness and firmness of the skin have been appreciated.
• the dose of nicotine delivered through the skin is from 0.5 mg per 'side (thigh and buttocks), facing areas of LGL, with two applications per day for 56 days.
• the formulas of the compositions applied are the following:
• Group 1 treatment with the composition of the invention (verum).
• Group 2 treatment with a percutaneous placebo topical
• This trial lasted 9 weeks and included a one-week inclusion phase, followed by an 8-week treatment phase. It has been performed in patients suffering from LGL.
• the total number of patients in this preliminary study is 40.
• the probe was placed on a tripod, at constant height from the ground for each subject. The measurement was made after acquisition of the last possible image by detaching the probe from the skin plane.
• the assessment of general tolerance was carried out during the final visit.
• a biological assessment was carried out during the selection visit and the final visit (blood count, platelet count, ALAT and ASAT transaminases).
• - Patient with a history of hypersensitivity to nicotine and to the other constituents of the studied product, - Patient using or having used a nicotinic product (transdermal device, chewing gum, spray etc.) for less than two years,
• Table 1 demographic criteria and characteristics at inclusion
• BMI body mass index (P / T2)
• Table 4 Questionnaires by visual analog scale on D56
• the daily leaves show an improvement in the smoothness of the skin, as well as its suppleness.
• Nicotine used in low doses, acts directly on localized gynoid lipodystrophy, more commonly called cellulite, by significantly reducing its thickness (by 8.9% on average).
• the entire study population lost weight (-1.37 Kg in the verum group, compared to -0.71 Kg in the placebo group).
• the free nicotine used in this study therefore does not show an overall weight loss effect.
• We therefore conclude that the effect of nicotine is localized and not systemic. The change in the thickness of cellulite is therefore not attributable to the weight loss noted in the two groups.
• nicotinic gel was effective overall to reduce the importance of their cellulite, reduce the number and depth of the dimples. This development is noticeable with the wearing of fitted clothing. Finally, the effect of nicotine gel on firmness, tone and smoothness of the skin is noted.
• Vaseline oil qs 100,000 Thermo-slimming body oil g% g
• Miglyol 812 (fatty acid triglycerides) from the company DYNAMIT NOBEL 15
• Vaseline oil qs 100,000
• composition is intended to be packaged in an aerosol in the presence of a propellant, butane for example.
• Oil-in-water emulsion prepared conventionally for those skilled in the art.
• Oil-in-water emulsion prepared in a conventional manner for a person skilled in the art.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Epidemiology (AREA)
• Pharmacology & Pharmacy (AREA)
• Medicinal Chemistry (AREA)
• Chemical & Material Sciences (AREA)
• Dermatology (AREA)
• Birds (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Bioinformatics & Cheminformatics (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Engineering & Computer Science (AREA)
• Medicinal Preparation (AREA)
• Cosmetics (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Applications Claiming Priority (3)

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• 2001
  • 2001-02-26 FR FR0102546A patent/FR2821270B1/fr not_active Expired - Fee Related
• 2002
  • 2002-02-19 WO PCT/FR2002/000625 patent/WO2002067891A1/fr not_active Application Discontinuation
  • 2002-02-19 EP EP02704862A patent/EP1363593A1/de not_active Withdrawn
• 2003
  • 2003-08-25 US US10/647,368 patent/US20040037860A1/en not_active Abandoned

Non-Patent Citations (1)

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