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
  • A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
  • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated 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
  • A61Q19/08—Anti-ageing preparations
• • 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
  • A61K8/67—Vitamins
  • A61K8/671—Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal

Definitions

• the present invention relates to the treatment of the skin using compositions containing retmoids, in order to combat skin ageing and the formation of wrinkles More particularly, the invention relates to a method for the cosmetic treatment of the skin, m particular the face, the neck or the hands, with retinoid compositions, which is less irritant than the known methods and allows the individual to use higher and more effective doses during the treatment, and at an earlier stage than previously
• patent US-5,401,517 suggests using a lower dose of retmoids for several days and then increasing the dose of retmoids in the composition on the following days, when the sk has become accustomed to the compounds.
• this method has drawbacks since it requires a change in the application regime to use a different formulation containing a higher dose of retinoid. This places the onus on the user to remember to change product and to buy an additional product before the first one has been used up.
• compositions containing low doses of retmoids are used during the day but allow the individual to apply formulations containing a higher, more effective dose in the evening before going to bed. All of each tube of product will be used during the treatment, thus avoiding any loss of product and excessive costs.
• the application procedure will remain similar from the initial day of the treatment, which will thereby encourage the individual to acquire suitable habits and to maintain these habits from the first day of use.
• the individual applies high doses of retinoids from the start of the treatment and thus obtains the benefits of high doses immediately.
• one of the subjects of the inven ⁇ tion is to provide a method for treating the skin by applying an effective amount of retinoid onto the skin during the day, in order to combat the ageing process.
• Another of the subjects of the invention is to provide a method for treating the skin with retinoids and for attenuating the irritation produced by retinoids.
• Another of the subjects of the invention is to provide a method for treating the skin which allows a high dose of retinoids to be applied from the first day of use .
• Another subject of the invention is to provide a method for treating the skin which allows the individual to use the retinoid-based product on a daily basis from the start of the treatment.
• the invention relates to a method for treating the skin according to the following procedure : a) application of a composition containing a weak dose of retinoids, comprising a compound of retinoid type which is effective for combating skin ageing, at a sub-irritant dose, once a day; and b) application of a composition containing a higher dose of retinoids approximately 10 to 16 hours, advantageously 12 hours, after the first dose.
• composition formulated specifi- cally for a part of the face for example the eyes, may be applied once or twice a day at a low, sub-irritant dose.
• the formulations serving as vehicle for each of the applications of the product in the method according to the invention may be identical or may be different, depending upon the particular requirements of the regime and of the user.
• a base or a lighter formulation may be used during the day whilst a richer emulsion of firmer consistency may be used at night for greater skin comfort while the individual is resting.
• the aim pursued in developing the invention is to allow the individual using retinoid-based compositions to become more tolerant to retinoids more quickly. Often, individuals react by developing red ⁇ ness, itchiness, stinging, a burning sensation and desquamation when retinoids are applied. However, by using retinoids in an application procedure according to the present invention, the individuals may tolerate the application of retinoids at an effective dose more quickly then if an amount which produces the irritation had to be applied immediately on a daily basis.
• retinoids should be understood to include retinoic acid or tretinoin, retinol, retinaldehydes and salts and esters thereof.
• Typical salts are alkali metal, ammonium and C 2 -C 30 ammonium salts.
• the sodium, potassium, triethanolammonium and ammonium salts are particularly preferred. Combinations of all the above compounds may be present in the compositions.
• retinol and retinoic acid should be understood to include hydrogenated and non-hydrogenated isomers such as 9-cis-retinol, didehydroretinol, 13-cis- retinoic acid, 13-trans-retinoic acid and didehydro- retinoic acid.
• Other retinoids which are effective in treating skin ageing, wrinkles and other anomalies are present in US patents Nos. 4,603,146, 4,887,805 and 4,888,342, the contents of which are incorporated herein by way of reference . They may be present in the compositions used according to the invention at concen ⁇ trations from about 0.0001 % to about 5 %.
• they will be present in amounts of between 0.0001 % and about 0.3 %. Even more preferably, they must be present in amounts of between about 0.01 % and about 0.075 %. Even more preferably, they are present in amounts of between about 0.015 % and about 0.04 %.
• the concentrations will be determined by those skilled in the art according to the nature of the retinoids specifically present in the composition. They will also be adapted as a function of the excipients and of the ability of the formulation to release active retinoid molecules which can be used by the skin. A large variety of pharmaceutically and/or cosmetologically acceptable supports may be used for the present invention.
• the amounts of vehicles may be from about 1 to 99.9 % and preferably from about 80 to 98 %, advantageously between about 95 and about 99.950 % of the composition by weight.
• compositions used in the products according to the invention as vehicles or bases may be in the form of emulsions, such as oil-in-water or water-in-oil emulsions. They may also be in the form of liposomal emulsions or any other emulsion known to those skilled in the art, which are physically and chemically stable.
• the compositions which may be used in the method according to the invention comprise water-in-oil emulsions as described in EP 91 9137059 which is incorporated herein by way of reference.
• Oil-in-water formulations which may be used in the method according to the invention are presented in WO/US 95/11750 which is incorporated herein by way of reference .
• Liposomal compositions wnich may be used as vehicles for the retinoid compositions in the method according to the invention are described in WO/US 96/04557 which is incorporated herein by way of reference.
• compositions may also be formulated in gel or lotion form with cosmetologically acceptable excipients known to those skilled in the art.
• compositions according to the invention may also be included in the compositions according to the invention.
• ingredients may include, in parti- cular, sunscreens and screening agents, tanning agents, antiacne agents, in particular salicylic acid, antiinflammatories (in particular panthenol, Gingko biloba, glycyrrhetinic acid, etc.) , depigmenting agents, hydrating agents, plant extracts and other anti-wrinkle agents.
• the sunscreens comprise, in particular, 4-aminobenzoic acid and derivatives thereof, dibenzoyl- methane, camphor derivatives, homosalate, oxybenzone, cinnamic esters, 3-imidazol-4-ylacrylic acid and benz- imidazole derivatives such as 2-phenylbenzimidazole- 5-sulphonic acid and its sodium and TEA salts.
• the first application of the day should be made in the morning, after cleansing the skin, on waking up.
• the first application should contain a sub-irritant dose of retinoids, for example from about 0.0001 % to about 0.04 % and preferably less than 0.04 %, advantageously from 0.01 % to 0.02 %.
• a particularly suitable concentration is 0.015 % by weight.
• the first application may preferably be made in an oil-in-water emulsion which is relatively light and easy to apply and to wear.
• the second application should preferably be made in the evening, just before going to bed and approximately 10 to 16 hours after the first applica ⁇ tion.
• the second application should contain a relatively large amount of retinoids, which will allow the administration of a larger amount of retinoids onto the skin.
• This higher-concentration formulation will be more effective as a remedy for skin anomalies, since it contains a higher dose of active principles.
• This second application may be made in an oil-in-water emulsion. However, it may also be placed in a water-in- oil emulsion. Water-in-oil emulsions have a tendency to be slightly more nourishing and "greasy" than oil-in- water compositions. However, such formulations may be well tolerated at night and provide the skin with complementary moisturization.
• the retinoid content in the second application should preferably be from about 0.04 % to 0.3 %, although it may be higher if the patient is capable of tolerating this dosage.
• compositions specially formulated for particular areas of the upper part of the body such as the neck and around the eyes or the mouth, may be used in lower retinoid doses along with other formulations in order to provide additional assistance to these areas without causing any further irritation.
• the examples which follow are intended to illustrate the present invention without limiting its scope in any way.
• EXAMPLE 1 A composition containing retinol, having the formulation A and containing 0.015 % by weight of retinol, is applied daily to the face and the neck in the morning after cleansing the appropriate areas. In the evening, the neck and the face are again cleansed and a retinol formulation, having the composition B and containing 0.075 % by weight of retinol, is applied to the same area. The irritation symptoms are expected to be less than if a formulation containing about 0.04 % retinol was applied twice a day.
• the tolerance results are compared after treat ⁇ ment for 15 days and 1 month in 2 groups of users, according to two different administration procedures.
• the 1st group applies formulation A in the morning and formulation B in the evening as indicated above.
• a second group applies formulation C in the morning and formulation D in the evening under the same conditions.
• the tolerance is better in the 1st group, where less than 4 % of the individuals stop the application after 15 days.
• formulation A in the morning thus entails virtually no additional irritation but allows the skin to be prepared to receive the dose present in formulation B and to adjust the total daily dose administered.
• formulation E in the morning may thus be combined with that of a stronger-dosed formulation, such as formulation B, in the evening, onto the entire face.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Birds (AREA)
• Epidemiology (AREA)
• Gerontology & Geriatric Medicine (AREA)
• Dermatology (AREA)
• Cosmetics (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Priority Applications (5)

Applications Claiming Priority (2)

Publications (1)

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Family Applications (1)

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Cited By (4)

Families Citing this family (5)

Citations (2)

• 1996
  • 1996-06-07 FR FR9607110A patent/FR2749511B1/fr not_active Expired - Fee Related
• 1997
  • 1997-06-05 CZ CZ98317A patent/CZ31798A3/cs unknown
  • 1997-06-05 HU HU9802916A patent/HUP9802916A3/hu unknown
  • 1997-06-05 EP EP97922001A patent/EP0845979A1/en not_active Withdrawn
  • 1997-06-05 WO PCT/IB1997/000642 patent/WO1997046221A1/en not_active Application Discontinuation
  • 1997-06-05 AU AU27861/97A patent/AU2786197A/en not_active Abandoned
  • 1997-06-05 BR BR9702284-5A patent/BR9702284A/pt not_active Application Discontinuation
  • 1997-06-05 CN CN97190973A patent/CN1198092A/zh active Pending
  • 1997-06-05 EA EA199800194A patent/EA199800194A1/ru unknown
  • 1997-06-05 PL PL97324929A patent/PL324929A1/xx unknown
  • 1997-06-05 CA CA002228750A patent/CA2228750A1/en not_active Abandoned
  • 1997-06-05 JP JP10500379A patent/JPH11510824A/ja active Pending
  • 1997-06-05 KR KR1019980700901A patent/KR19990036233A/ko not_active Application Discontinuation

Patent Citations (2)

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