WO1997017056A1

WO1997017056A1 - Cosmetic composition containing a viburnum extract

Info

Publication number: WO1997017056A1
Application number: PCT/FR1996/001741
Authority: WO
Inventors: Bernard Fabre; Marie-Thérèse Trebosc
Original assignee: Pierre Fabre Dermo-Cosmetique
Priority date: 1995-11-07
Filing date: 1996-11-06
Publication date: 1997-05-15
Also published as: FR2740681A1; FR2740681B1

Abstract

A cosmetic composition having anti-free radical and/or draining activity is disclosed. The composition contains a viburnum bark and/or leaf extract.

Description

COSMETIC COMPOSITION BASED ON A VIBURNUM EXTRACT

The present invention relates to a cosmetic composition with anti-free radical and / or draining activity.

The main function of adipose tissue is the storage of lipid reserves. In humans only 300 to 400 g of glycogen can be stored by the liver and muscles. They are barely sufficient to meet the body's energy needs for twelve hours. On the other hand, the reserves of adipose tissue (triglycerides) of a 75 kg man are 15 kg, which is enough for energy needs for two months.

The adipose tissue is localized at the level of the hypodermis more particularly in certain zones. These vary by gender. In humans, it is mainly axillary and abdominal and corresponds to 20% of the weight.

Subcutaneous adipose tissue is a connective tissue composed of multiple fatty lobules, separated by conjunctivovascular spans. Lobules are clumps of adipocytes, large vacuolated cells, almost completely filled with triglycerides. These adipocytes are derived from particular fibroblasts which undergo differentiation into pre-adipocytes.

The conjunctivovascular spans are organized differently according to sex. In women, they form vertical partitions perpendicular to the fascial planes. pinching accentuates the profusion of nodules in the deep dermis, explaining the irregularity of the skin surface hence the "orange peel". In humans, the conjunctivovascular spans form oblique partitions with aponeurotic planes, moreover the lobules are smaller, which allows them to slide over each other when pinching without causing "orange peels".

These partitions are made up of collagen fibers, reticulin and reticuloendothelial cells. Vascularization is very important. Numerous capillaries surround each adipocyte and flow into the small vessels of the interlobular partitions. Each lobule is vascularized by an artery and two veins. A rich lymphatic network is also present in the adipose tissue.

What is called cellulite is the result of various genetic, hormonal, stress, dietary, etc. factors. In women, female hormones (estrogens, progesterone) will intervene cyclically in the dermal tissues. The first signs of cellulite therefore appear from adolescence. A woman's hormonal rhythm is a 28-day cyclical rhythm: the first half is under the influence of estrogen, it leads to ovulation. The second half is under progestogen dependence, it is the expectation of a possible implantation.

These hormones are responsible at the level of the walls of the blood vessels which irrigate the dermis and the adipose tissue, of a relaxation promoting the leakage of the serum towards the surrounding tissues. At the same time, there is a general tendency for water-sodium retention. Hence the feeling of swelling experienced during the second half of the cycle. Finally, we observe at the level of adipocytes, a storage of fatty substances, of energy stored by the body.

At the end of the cycle, everything comes back in order: the water permeating the dermis is taken up by the general and lymphatic circulation, the fats are destocked as and when the body's energy needs, and all the better that we have an adequate lifestyle. We find a state of equilibrium, precarious, it is true, since the new cycle involves the same phenomena. This cellulite is that of the young woman: reversible, manifested by regular and rhythmic pushes. It is important to act on it as soon as it appears, so as to accompany this physiological rhythm and ensure that its reversibility is as complete as possible. The period from 15 to 35 years is the most favorable.

Then comes an intermediate period: over time, the repeated exercise of these phenomena will alter the subcutaneous tissues. Water ebb and flow, fat storage and destocking, with years, fatigue, stress and small excesses, everything slows down, the return to normal is less good. Part of the cellulite remains reversible, the other settles in chronicity, between 35 and 55 years of age.

The vascular walls deteriorate, becoming less flexible, the volume of water passing increases and the lymphatic circulation itself slows down, no longer allowing good drainage of water and its associated substances. In the long run, substances accumulate in the tissues, denature them, the fibers stiffen and the whole gene cell exchanges. In addition, the fat cells store more and more fats, and the sedentary life helping, these fats are less and less destocked. The surrounding tissue stiffens, trapping the fatty lobules, vascular and nerve endings as in the cracks of a net.

Increasingly deep, these changes will soon reveal real nodules, a padded appearance of the skin. If you have not taken care of your cellulite, the evolution will be towards a definitive and anchored stage.

An effective way to fight against cellulite is to maintain and restore the drainage of water and its associated substances. This drainage can be done by playing on the vascular walls, so as to restore its flexibility but also on the lymphatic network. The extracts of Vibumum prunifolium and Vibumum lantana fulfill this function and thus preserve an activity towards cellulite. The present invention consisted in developing an anti-radical, draining and / or slimming composition which makes it possible to ensure effective treatment of cellulite by the topical route.

The cosmetic composition according to the invention is characterized in that it contains an extract of bark and / or leaves of Vibumum in combination with caffeine.

According to another characteristic of the invention, the cosmetic composition is characterized in that it contains an extract of barks of Vibumum prunifolium.

According to the present invention, the cosmetic composition is characterized in that it contains an extract of leaves of Vibumum lantana.

According to another characteristic of the invention, the cosmetic composition is characterized in that the extract of Vibumum has a titer in amentoflavone of between 0, 10 and 5.0% by weight relative to the dry matter.

According to another characteristic of the invention, the cosmetic composition is characterized in that it contains 0.5 to 10% by weight of a Vibumum extract.

According to the present invention, the cosmetic composition is characterized in that it contains 0.5 to 5% by weight of an extract of Viburnum in combination with 0.5 to 5% by weight of caffeine.

According to another characteristic of the invention, the cosmetic composition is characterized in that its use is made as a product with anti-radical and / or draining activity, useful in particular in the treatment of cellulite. We briefly recall the botanical description of the plant used in the context of the present invention. The vibumum, viburnums for the vernacular name, belong to the botanical family of Caprifoliaceae. This small family is close to the Rubiaceae. It includes shrubs with generally simple leaves, without stipulations or with deciduous stipules. The flowers are type 5 with 5 sepals, 5 petals, 5 stamens and 3 carpels.

Three species of vibumum are particularly important among the 125 enumerated = Vibumum prunifolium, Vibumum opulus and Vibumum lantana.

Vibumum prunifolium is a shrub or small tree 3 to 8 meters high. The trunk is short and often tortuous, the spreading branches with hairy twigs bear obovate glabrous leaves, short petiolate, finely toothed and taking a scarlet red hue in autumn. The flowers are white, small and grouped in umbelliform cymes. The fruit is a small ovoid drupe, dark blue at maturity and containing one or two albuminous seeds.

The Vibumum opulus is smaller. It is a shrub 2 to 4 meters high. The branches, fragile, glabrous and whitish gray, also bear glabrous leaves, opposite, petiolate. The flowers are white, arranged in corymbs with 6 to 7 main branches. The flowers around the edge are sterile, without stamen and without pistil. The central flowers are fertile and much smaller. This arrangement earned Viburnum opulus, the vernacular name of Snowball and to be a highly used ornamental plant. The fruit is a bright red drupe at maturity.

The Viburnum lantana is the smallest of the 3 since it is only 1 to 2 meters high. The branches are felted, with gray hairs and stars. The leaves are thick, almost whitish on their underside. Their ribs are protruding. They are petiolate, opposite, oval in shape and denticulate around the edges. They are also covered with much more abundant gray hairs on the young leaves and buds. The flowers are quite small white and organized in tight false umbrellas. The fruits are green drupes, then red and black when ripe.

Viburnums are different in their chemical composition. Viburnum opulus is particularly rich in tannins condensed in the bark and in less proportion in the leaves. The bark also contains coumarins, saponin leaves and triterpene acids.

Viburnum prunifolium and lantana contain less abundant condensed tannins than V. opulus in the bark and leaves. Coumarins are also found in the bark, triterpene acids and saponins in the leaves. However, the peculiarity of these two plants is the presence of aamentoflavone in the bark of V. prunifolium and in the leaves of V. l antana; V. opulus does not contain any.

The aamentoflavone is a biflavonoid = biapigenin = bis hydroxy 5, 7, 4 'flavone. The asymmetric carbon-carbon bond between the two flavonoids is between the 3 'and 8 "carbons. The amentoflavone content naturally varies according to the species, the parts harvested and the harvest periods. Only the bark of V. prunifolium in contain in proportions varying from 0.1 to 0.3%. Traces are found in the bark of V. lantana. The leaves contain 0.3 to 0.7% depending on whether they are harvested in summer or in spring.

We already know a certain number of traditional uses of Viburnum. V. opulus is widely used because of its inflorescences in "Snowball" as an ornamental plant in parks. In addition, the bark has been listed in the Pharmacopoeia of the United States of America because of its antispasmodic properties.

V. prunifolium is the Viburnum most used in therapy; it also bears the name of V. officinal. The bark has been listed in the Pharmacopoeia American from 1882 and to the French Codex in 1908, for its antispasmodic properties and in particular with respect to the uterus. It is therefore used in the form of a tincture or fluid extract in dysmenorrhea, threats of abortion, nervous disorders of pregnancy. It is also used in combination with witch hazel, brown turkey as a venous tonic.

Viburnum lantana is the least known for its therapeutic properties. Only a few applications exist as astringents and refreshing in the case of angina, for example.

Some examples of bark and / or leaves of Viburnum are indicated below.

The barks of Viburnum prunifolium and the leaves of Viburnum lantana are dried and then ground. The drugs thus prepared are extracted with a C 1 to C 4 alcohol or with a water-alcohol mixture in proportions varying from 100-0 to 0-100. The extraction can also be done with pure acetone or a water-acetone mixture in proportions of 100-0 to 0-100. The plant / solvent ratio varies from 1/3 to 1/30. The extraction is carried out at temperatures varying from room temperature to boiling, with stirring or statically. The durations of the extraction range from 1 hour to 48 hours.

Once the extraction has been carried out, the extracted drug is separated from the solution by filtration or by spinning. The drug can be re-extracted under the same conditions described above, a third extraction can be carried out if necessary.

The filtrates of the different extractions are combined. They can be used as is or concentrated. To do this, the solutions are concentrated under reduced pressure at temperatures between 40 ° C and 100 ° C until a concentrated fluid extract or a powder is obtained. It is also possible during the concentration operation to add a solvent to high boiling point like glycerin, propylene glycol, butylene glycol or transcutol pure or mixed with water. In this case, the extraction solvent evaporates completely.

The different extracts of Viburnum are dosed for their amentoflavone content. The assay is done by high performance liquid chromatography on a C 18 type column with a mobile phase water-acetic acid 2% = methanol-acetic acid 2% = -40/60. Detection is done at 350 nm. The assay is carried out in relation to a standard range of aamentoflavone. The amentoflavone contents vary between 2% and 0.1% compared to the dry matter.

Example 1

100 kg of dry bark of Viburnum prunifolium is ground using a hammer mill. The crushed bark is extracted using 1,000 kg of 95% ethanol under reflux for 1 hour. The drug is filtered, then re-extracted with 1000 kg of 95% ethanol under the same conditions. After filtration, the drug is washed with 500 kg of 95% ethanol at room temperature. The two extraction solutions and that from the washing are combined, re-filtered if necessary. The extract is in clear form, light yellow-brown in color. Its dry matter content is between 0.25 and 0.45%. The aamentoflavone is dosed by HPLC between 0.3 and 1.5 96.

Example 2

10 kg of dried leaves of Viburnum lantana are ground and then extracted with 100 kg of 95% ethanol. The extraction is carried out under reflux, with stirring for 1 hour. After returning to room temperature, the drug is filtered, discarded. The extracted solution is concentrated until an extract is obtained, the dry matter content of which is 10%. The concentration is carried out under reduced pressure at 50 ° C. Theamentoflavone is dosed by HPLC, its content varies from 0.3% to 1.5% compared to the dry matter. Example 3

1 kg of dried leaves of Viburnum lantana is ground and then extracted with 7 kg of a water / acetone mixture = 30/70. The extraction is a static leaching, carried out at room temperature for 48 hours. The leachate is filtered and then concentrated after adding 5 kg of propylene glycol. The concentration is carried out at 60 ° C. under reduced pressure until complete evaporation of the water and the acetone. The propylene glycol solution is filtered, its dry matter content is between 7 and 3%, its amentoflavone content between 0.3% and 1.5% compared to the dry matter.

Example 4

1 kg of Viburnum prunifolium bark is extracted after grinding with 10 kg of 60% ethanol. The extraction is carried out under reflux, with stirring, for 4 hours. The drug is drained and then discarded, the extracted solution is filtered, then concentrated until a powder is obtained. 80 to 150 g of a dry extract are thus obtained titrating between 0.3 and 1.5% of aamentoflavone.

The anti-radical activity of the Viburnum extract as well as its draining activity alone or in synergy with caffeine have been studied in the context of the present invention.

Anti-radical activity

The stiffening of adipose tissue is largely due to crosslinking of the collagen. This crosslinking comes from the oxidation phenomena of proteins initiated by free radicals. Fighting these free radicals will contribute to anti-cellulite activity.

We evaluated the free radical scavenger activity of the alcoholic extract of Viburnum prunifolium titrating 0.65% in amentoflavone on a stable free radical of diphenyl hydrazine hydrate (DPPH). The IC50, the concentration necessary to trap 50% of DPPH, is 0.64 mg / ml.

Draining activity

This activity is evaluated by applying topically to rats, an 8% solution of a fluid Vibumum extract alone or associated with 3% caffeine and by measuring the diuretic activity caused by these treatments by comparison with a control.

The topical treatment is carried out for 3 consecutive days, the last treatment taking place before diuresis.

The quantity of 1.1 ml of preparation is applied to the skin of the back and flanks of the shorn animal with massage using the gloved finger until the product is completely absorbed.

The control animals receive the solvent, ie 95 ° ethanolic alcohol diluted to 10% in distilled water, under the same conditions.

The weight of excreted urine is increased to + 1 hour, + 3 hours, + 6 hours and + 24 hours.

On urine collected for 24 hours, it is determined:

by reading with a Labstix strip: pH, ketonuria, the presence of blood, glucose and proteins, the level of Na +, according to the direct potentiometric technique developed by Eisenmann. - the rate of K +, according to the direct potentiometric technique developed by Pioda et Coll. the urea level according to the method described by 'Talke and Schubeπ, modified by Tiffany et al. the level of creatine according to the technique of Jaffe. The weights of excreted urine are recorded 1 h, 3 h, 6 h and 24 hours after the diuresis.

During the readings 1 h, 3 h and 6 hours after diuresis, we did not note any favorable difference in the treated animals.

During the 24-hour reading, an increase in urine excretion appears in animals treated with the viburnum + caffeine combination.

Statistical analysis carried out by analysis of variance, Bonferroni test, comparing the 4 batches of animals, indicates that the amount of urine excreted by animals treated with caffeine + viburnum is statistically greater than the control (+ 115%) and the viburnum alone.

The amount of urine emitted in 24 hours corresponds to the amount of water consumed during the 24 hours of diuresis.

Determination by the Labstix strip, on the urine collected for 24 hours of the pH, of the presence of blood, acetone, glucose and proteins.

There is no noticeable difference in the parameters indicated above between treated animals and control animals.

On urine collected for 24 hours, we determined the main biochemical parameters in urine and in particular the contents of sodium, potassium, creatinine and urea.

The concentrations of sodium, potassium, urea and creatinine are lower in animals treated with caffeine and even more by the combination viburnum + caffeine where the differences with control and / or viburnum alone are statistically significant (except for the sodium concentration ). When we consider these parameters in quantity excreted for 24 hours, we observe a stability of urea and creatinine excreted over 24 hours, on the other hand for the association viburnum + caffeine, an increase in sodium (+ 30 96) and at the same time a significant decrease in potassium (- 30 96) compared to the control treatment and viburnum alone.

The diuretic study clearly shows the draining activity of a viburnum-caffeine association. This activity is particularly interesting; to be implemented in the case of topical cellulite in a cosmetic product.

Some examples of particular compositions falling within the scope of the present invention will be indicated below.

EXAMPLE 5 Draining Slimming Fluid Gel

Fluid viburnum extract 0.5 to 5%

Caffeine base 0.5 to 5%

Hydroalcoholic extract of ruscus 1 to 3%

Ethoxylated oleic alcohol 10 moles o, ι at 2%

Oleic acid 0'1 to 1%

Xanthan gum 0.05 to 0.2%

Hydroxypropylcellulose O'I at 0.3 96

Denatured 95 ° alcohol 20 to 50%

Perfume qs

Anti-oxidant qs

Demineralized water qs lOO g EXAMPLE 6 Slimming Massage Gel

Fluid viburnum extract 0.5 to 5%

Caffeine base 0.5 to 5%

Caffeic acid, carboxylic 0.5 to 3%

Triethanolamine 0.5 to 1.5%

Cyclomethicone / dimethicone copolyol 1 to 6%

PEG 200 3 to 6 96

Hectorite 1 to 3%

Vitamin E acetate 0.5 to%

Perfume qs

95 'alcohol denatured 20 to 50%

Demineralized water qs 100 g

EXAMPLE 7 Microparticles with a Long-Lasting Effect, Dispersible in an Alcohol-Medium

Ethyl cellulose micronized 4 to 8%

Dry extract of viburnum 0.5 to 2%

Caffeine 0.5 to 5 96

Vitamin E acetate 10 to 15%

Caπhame oil 1 to 6% Corn starch qs 100 g

The mixture previously wetted with 95 ° alcohol is then granulated and then sieved into microparticles <0.5 mm. Example 8: draining spray, decongestant, tonic against heaviness of the legs

Viburnum fluid extract 1 to 10 96 Caffeine base 0.5 to 2%

Hydralcoholic extract of ruscus 1 to 3%

Menthyl pyrrolidone 0.1 to 1%

95 'alcohol denatured 10 to 2%

Perfume, coloring qs Demineralized water qs 100 g

This solution is sprayed using a multidirectional jet pump.

Example 9: firming cream (for distended areas such as the belly, internal surface of the thighs and knees)

Fluid viburnum extract 0.5 to 5

Wheat protein 1 to 5

Vitamin E acetate 0.2 to 1%

D Panthenol 0.5 to 2%

Ethoxylated sorbitan monostearate

(40 moles) 1 to 3%

Sorbitan monostearate 1 to 3%

Safflower oil 5 to 10%

Isopropyl palmitate 1 to 5%

Glycerin 1 to 5 96

0.1 to 0.5% carboxyvinyl polymer

Triethanolamine 0.1 to 0.5%

Perfume qs

Preservatives qs

Demineralized water qs 100 g

Claims

1. Cosmetic composition characterized in that it contains an extract of bark and / or leaves of Viburnum in combination with caffeine.

2. Cosmetic composition according to claim 1, characterized in that it contains a bark extract of Viburnum prunifolium.

3. Cosmetic composition according to claim 1, characterized in that it contains an extract of leaves of Viburnum lantana.

4. Cosmetic composition according to one of claims 1 to 3, characterized in that the Viburnum extract has an amentoflavone content of between 0.10 and 5.00% by weight relative to the dry matter.

5. Cosmetic composition according to one of claims 1 to 4, characterized in that it contains 0.5 to 10% by weight of an extract of

Viburnum.

6. Cosmetic composition according to one of claims 1 to 5, characterized in that it contains 0.5 to 5% by weight of an extract of Viburnum in combination with 0.5 to 5% by weight of caffeine.

7. Use of a cosmetic composition according to one of claims 1 to 6 as a product with anti-radical and / or draining activity, useful in particular in the treatment of cellulite.