FR2680466A1 - PREPARATION FOR WHITENING THE SKIN. - Google Patents

Abstract

The present invention relates to a preparation for bleaching the skin. This composition may be in the form of a solution, creams, gels, sprays and the like, comprising a combination of an effective amount of a flavanoid and an effective amount of ascorbic acid or a suitable derivative thereof. here, if desired in combination with a sunscreen, an agent designed to suppress tyrosinase activity or a tocopheryl derivative.

Description

PREPARATION FOR WHITENING THE SKIN

  The present invention relates to novel cosmetic compositions for topical application. These compositions are bleaching preparations and may be of any conventional form for topical application, such as creams, gels, lotions, sprays and the like. like. Bleaching preparations result in bleaching of the user's skin and prevent

  also to a large extent the formation of new dark spots on the skin of the user.

  The melanocyte is the site of pigmentation in the skin Melanocytes produce melanosomes,

  organelles bound to membranes in the cytoplasm of the melanocyte, which are then transferred to neighboring keratinocytes.

  Melanin, which is formed in melanosomes, is responsible for the basic color of human skin. In the biosynthetic pathway of melanin, tyrosinase, a copper-containing enzyme, plays an important role in the degree of melanosome. The color of the skin is apparent only when melanosomes containing melanin are transferred into the keratinocytes. Several causes, including genetic control and environmental factors such as ultraviolet radiation, and hormones, regulate melanogenesis.

  Abnormal reactions of melanocytes with the above causes may result in increased accumulation of melanin in the skin in the form of brown spots.

  The present invention relates to novel cosmetic compositions for local application on the

  skin of a user, which result in bleaching of the skin and which largely prevent the formation of brown spots.

  The compositiows of the invention consist of

  combinations of flavonoids, which are effective in eliminating

  at least to greatly reduce the amount of pigments that have formed in the skin as a result of UV radiation, and ascorbic acid or a suitable derivative.

  of ascorbic acid (or its physio-

  logically tolerable) result in the reduction of DOPA-quinone to DOPA, and also convert the colored oxidized melanin to a reduced colorless form thereof. Advantageously, flavonoid derivatives of extracts are used.

  of plants, or extracts of plants as such which

  maintain an adequate concentration of such flavonoids Synthetic flavonoids can also be used.

  compositions of the present invention are also suitable

  required for the reduction of melanin formation in

  early stages of such training, and for the pre-

  The new bleaching compositions of this invention exert a pronounced whitening and brightening effect on the brown spots of the skin. Preferred plant extracts for use according to the invention are those obtained from yarrow , calendula, sage, witch hazel and blackberries.

  The preparations of the invention contain

  a suitable carrier or carrier, and also one or more additive components selected from the derivatives of toconterol, kojic acid, sunscreens chemical and physical UVA, UVB, IR and / or

  visible light; minerals such as titanium dioxide

  tane Suitable sunscreens are of the form

  readily available commercially, such as methoxy-

  octyl cinnamate, butyl methoxydibenzoylmethane,

  etc. A wide variety of formulations can be used

  and the following examples indicate some possible types of their formulations,

  In a general way, the formulations of the in-

  as ingredients from about 0.1%, by weight, of an extract of one or more of the following; yarrow, calendula, sage,

  witch hazel and mothers, Other herbal extracts

  The formulations generally contain from about 0.1% by weight to about 30% by weight of purified flavanoids, or a plant extract containing an equivalent amount of flavanoids. second ingredient is a physiologically tolerable derivative of ascorbic acid, such as ascorbyl palmitate, ascorbyl stearate,

  ascorbomagnesium phosphate and analogues The second

  It comprises from about 0.1% to about 5% by weight of the composition. Licorice extract from 0.01% by weight to about% by weight is a preferred component.

  The advantageous formulations also contain

  as an ingredient a suitable sunscreen, such as a filter UVA, UVB, IR and / or visible light; octyl methoxycinnamate, methoxydibenzoylmethane

  butyl Another additional substance of a similar effect

  In general, these ingredients constitute

  about 1% by weight to about 10% by weight of the formulation.

  An additional advantageous optional ingredient is a

  suitable tocopheryl derivative, such as tocopheryl linoleate

  pheryl Compounds of this type when used comprise from about 0.1% by weight to about 5% by weight

of the formulation.

  Another advantageous optional ingredient, designed

  to suppress the activity of tyrosinase, probably caused by

  chelation of copper is kojic acid. This ingredient is used at a concentration

  0.1% by weight to about 5% by weight of the formulation.

  The following examples which should be understood in a nonlimiting manner, represent the preparation of a number of effective formulations of the invention in the form of creams of lotions, sprays and gels: EXAMPLE 1; Cream Yarrow Extract 20% Ascorb Magnesium Palmitate 5% Cream Base to Complete to: 100 EXAMPLE 2; Cream Mothers extract 25% Ascorbic acid 0.1% Base cream to complete to: 100 EXAMPLE 3 Cream Yarrow extract 15% Ascorbyl stearate 5% Ti O 2 10% Cream base to complete to: 100 EXAMPLE 4 Lotion Yarrow Extract 10% Ascorbyl Palmitate 0.5% Octyl Methoxycinnamate 7.5% Methoxydibenzoylmethane Butyl 0.5% Ti O 2 10% Kojic Acid 3% Base Lotion to supplement; EXAMPLE 5 Lotion Yarrow extract 5% Ascorbyl palmitate 0.5% Benzophenone 5% Ti O 2 10% Tocopheryl linoleate 1% Lotion base to make up to: 100 EXAMPLE 6: 2% Ti kojic acid lotion O 2 5% Base lotion to supplement to; 100

EXAMPLE 7 Gel

  Kojic acid 0.1% UVA & UVB solar filters Gel base to complete at: 100 EXAMPLE 8; Ascorbyl palmitate lotion 0.1% Linoleate tocopheryl 3% Kojic acid 0.5% Lotion base to supplement to: 100 EXAMPLE 9: Cream Ingredients Ascorbyl palmitate 4 Water soluble extract from yarrow

  millefeuille (containing 3% of flavo-

  noides) 1 Tocopheryl linoleate 0.1 Octyl methoxycinnamate 2 Butyl methoxydibenzoylmethane 0.75 Ti O 2 1 Kojic acid 0.1 Panthenol 1 Chamomile extract 0.1

IPM 2

BHT 0.04

  Preservatives 0.5 Stearic Acid 4

NA 2 EDTA 0.1

  Cetyl phosphate DEA 3.5 Cetyl alcohol 2 Glycerin stearate 4 Water to make up to: 100 EXAMPLE 10: Cream Ingredients% ascorbyl palmitate 0.1 Water soluble extract of yarrow (containing 3% of flavonoid) 30 Linoleate tocopheryl 5 octyl methoxycinnamate 7 butyl methoxydibenzoylmethane 3 Ti O 2 10 kojic acid 5 panthenol, 1 chamomile extract 0.1

IPM 2

BHT 0.04

  Preservatives 0.5 Stearic acid 4 Na 2 EDTA 0, 1 Cetyl phosphate DEA 3.5 Cetyl alcohol 2 Glycerine stearate 4 Water to make up to: 100 EXAMPLE 11; Lotion Ingredients% Ascorbyl palmitate 0.1 Water soluble extract of yarrow (containing 3% flavonols) Tocopheryl linoleate 5 Methoxycinnamate octyl 7 Butyl methoxydibenzoylmethane 3 Ti O 2 10 Kohic acid 5 Panthenol 1 Chamomile extract 0.1

IPM 2

BHT 0.04

Conservatives 0.5

EXAMPLE 12

EXAMPLE 13

Stearic acid 2

NA 2 EDTA 0.1

  Cetyl phosphate DEA 3 P 5 Cetyl alcohol 0.2 Glycerine stearate 2 Water to make up to: 100 Lotion Ingredients% Pallmitate and ascorbyl 4 Water soluble extract of yarrow (containing 3% flavonoid) 1 Linoleate tocopheryl 0.1 Octyl methoxycinnamate 2 Butyl methoxydibenzoylmethane 0.75 Ti O 2 1 Kojic acid 0.1 Panthenol 1 Chamomile extract 0.1

IPM 2

BHT 0.04

  Preservatives 0.5 Stearic acid 2 Na 2 EDTA 0.1 Cetyl phosphate DEA 3.5 Glycerine stearate 2 Water to make up to: 100: Gel Ingredients'% Ascorbyl palmitate 0.5 Water soluble extract of Yarrow (containing 3% of flavonoids) 1 Polysorbate 6 Carbopol 1 Triethanolamine 4.2 Preservatives 1 Kojic acid 5 Ti O 2 1 Tocopheryl linoleate 2 Panthenol 1 Phenylbenzimidazole sulfonic acid 5 Water to make up to: 100 EXAMPLE 14; Gel Ingredients% Ascorbyl palmitate 3 Water soluble yarrow extract (containing 3% flavonoids) Tocopheryl linoleate 0.5 Polysorbate 6 Carbopol 1 Triethanolamine 1.6 Preservatives 1 Kojic acid 0.1 Sulfonic acid Phenylbenzimidazol-5 0.1 Ti O 2 1 Panthenol 1 Water to make up to: 100 EXAMPLE 15: Liquid Ingredients% Ascorbyl palmitate 3 Water soluble extract of yarrow (containing 3% flavonoid) Tocopheryl linoleate 0.5 Polysorbate 10 Triethanolamine 0.05 Preservatives I Kojic acid 0.1 Phenylbenzimridazol-5 sulfonic acid 0.1 Ti O 2 Panthenol 1 Water to make up to 100 EXAMPLE 16: Liquid Ingredients% ascorbyl palmitate 0.5 Soluble extract in yarrow water (containing 3% flavonoids) 1 Polysorbate 10 -15 Preservatives 1 Kojic acid 5 Ti O 2 1 Tocopheryl linoleate 2 Panthenol 1 Phenylbenzimidazol-5 sulfonic acid 6 Triethanolamine 3.1 Water to complete to: EXAMPLE 17: Gel Ingredients% Ascorbyl palmitate 3 Water soluble blackberry extract (sohakul) Tocopheryl linoleate 0.5 Polysorbate 6 Carbopol 1 Triethanolamine 4.2 Preservatives 1 Kojic acid 0.1 Acid sulfonic acid phenylbenzimidazol-5 0.1 Panthenol 1 Water to supplement to; EXAMPLE 18; Gel Ingredients% Ascorbyl palmitate 0.5 Water soluble blackberry extract (sohakul) 1 Polysorbate 6 Carbopol 1 Triethanolamine 4.2 Preservatives 1 Kojic acid 5 Ti O 2 10 Tocopheryl linoleate 1 Panthenol 1 Phenylbenzimidazole sulfonic acid 5 6 Water to complete to: 100

EXAMPLE 19

  Ingredients% Cetyl Alcohol 5 Glyceryl Stearate SE 3 Capryl Triglyceride / Caprylate 3 Distearate PEG 6000 1 Yarrow Extract 1 Licorice Extract 0.05 Ascorbyl Palmitate 0.5 Tocopheryl Linoleate 0.2 Titanium Dioxide 2 Acid Glycolic 5 Preservatives 9.5 xanthan gum 0.3 NH OH to obtain PH-4 Water to supplement to: 100

EXEMPIS 20

  Ingredients% Yarrow extract 2 Kojic acid 0.5 Ascorbyl palmitate 0.2 Hydroxylic acid (such as glycolic acid) 5 Lotion base to supplement to: 100 In the following examples the licorice extract used was TP licorice extract (Glycyrrhiza

  Glabra) produced by Nikko Chemicals, Japan The percentages

are by weight.

EXAMPLE 21

  Ingredients% Licorice Extract 0.05 Yarrow Extract 3.0 Palmitate Ascorbyl 0.5 Base Cream to Complete to: 100

EXAMPLE 22

  Ingredients% Licorice Extract 0.1 Ascorbyl Palmitate 1.0 Tocopheryl Linoleate 0.5 Base Lotion to Complement to: 100

EXAMPLE 23

  Ingredients% Licorice Extract 4.0 Yarrow Extract 3.0 Tocopheryl Linoleate 0.5 Butyl Methoxydibenzoylmethane 1.5 Titanium Dioxide 5.0 Chamomile Extract 0.1

I P M 2,0

BHT 0.04

  Preservatives 0.5 Stearic acid 2.0 Na EDTA 0.1 Cetyl phosphate DEA 3.5 Cetyl alcohol 0, 2 Glycerin stearate 2.0 Water to make up to: 100 Extensive experiments have been performed

  which led to the compositions of the present invention.

  The criteria used in the evaluations were arbitrary scales of values of 0, 1, 2 and 3 with regard to the number of spots, as far as

  stain color and contrast levels.

  of skin have been classified into four categories according to

  lift of sun burns and ease of tanning.

  The experiments were carried out with human subjects

  hands women and men who had accepted the tests The ages ranged from 50 to 92 years, and only were tested

  subjects who had bi-symmetrical age spots

  on the dorsal side of both hands, which had

  an adequate number of such stains of sufficient color

dark and contrasting.

  The tests were run with the main components, each by itself, and then, different

  combinations were tested, and assays (concentration

  different) were used.

  Ascorbic acid and its derivatives exerted a

  certain effect, but at relatively high doses

  the various flavonordes mentioned were testified

  in themselves, and they have a certain effect.

  It was surprisingly found that the combination of these two components increased the effect in a pronounced manner, even when lower doses than before were used. The addition to these, either

  of tocopheryl derivatives, ie kojic acid, has

  the bleaching effect, and this also in a way that can be explained by a synergistic effect,

  It is likely that the different compounds

  vitamins, especially ascorbic acid and its derivatives, as well as flavonoids exert their effect by different routes. This also applies to kojic acid which

  apparently inactivates an enzyme promoting the formation of

  Melanin The bleaching effect of

  the present invention is a very pronounced effect and requires

  site the application of a formulation of the invention during

about 2 to 3 months.

  As indicated above, it is very likely that

  that ascorbic acid and its derivatives together with the defined flavonoids exert a synergistic effect,

  which is further favored by components such as toco-

phérol or kojic acid.

Claims (11)

  1. Composition for bleaching skin and skin spots by topical application, in the form of   solution, lotion, gel, spray or cream,   taking a combination of an effective amount of a flavonoid and an effective amount of ascorbic acid or a suitable derivative thereof, if desired in combination   with a solar filter, an agent designed to suppress the   tyrosinase activity or a tocopheryl derivative.   2, Composition according to claim 1, in   which the flavonoid is in the form of a plant extract.   or in purified form, derived from yarrow, calendula sage, witch hazel, blackberries and licorice extract.   3 Composition according to claim 1 or 2,   wherein the sunscreen is comprised of one or more   UVA, UVB, IR and / or light filters   such as octyl methoxycinnamate, methoxy-   butyl dibenzoylmethane and titanium dioxide.   4, Composition according to any one of the   1 to 3, in which the reducing agent of DOPA-   quinone is ascorbic acid, ascorbyl palmitate, ascorbyl stearate, ascorbomagnesium phosphate or   another suitable derivative of physiological ascorbic acid acceptable.   5. Composition according to any one of the   dications 1 to 4 containing a tocopheryl derivative.   6. Composition according to any one of the   dications 1 to 5, containing kojic acid.   7, Composition according to any one of the   dications 1 to 6, containing from about 0.1% by weight to about   30% by weight of purified flavonoid, or an extract of   plants containing an equivalent amount of flavonoids.   8, Composition according to any one of the   dications 1 to 7, containing from about 0.1% by weight to about   5% by weight of ascorbic acid or a derivative thereof.   9, Composition according to any one of the   dications 1 to 8, containing from about 1% by weight to about % by weight of a sunscreen.   10 Composition according to any one of the   dications 1 to 9, containing from about 0.1% by weight to about 5% by weight of kojic acid.   11. Composition according to claim 2, in which the plant extract is a liquorice extract. (Glycyrrhiza Glabra).