WO2003024418A2

WO2003024418A2 - Use of birch sap in cosmetic and dermopharmaceutical compositions

Info

Publication number: WO2003024418A2
Application number: PCT/FR2002/003112
Authority: WO
Inventors: Karl Lintner
Original assignee: Sederma
Priority date: 2001-09-14
Filing date: 2002-09-12
Publication date: 2003-03-27
Also published as: FR2829695B1; FR2829695A1; AU2002339046A1; WO2003024418A3

Abstract

The invention relates to the use of birch sap in cosmetic and dermopharmaceutical compositions, either alone or together with other active agents, in order to provide care for the skin, mucous membranes and epithelial appendages (nails, bristles and hair). The invention is intended specifically to soothe razor burn, to moisturise and soften the skin, to produce an anti-fatigue sensation and to detoxify and vitalise tissues.

Description

TITLE Use of birch sap in cosmetic and dermopharmaceutical compositions.

To fully ensure its physiological barrier function against external aggressions, the skin, and more particularly the stratum corneum, must have perfect integrity and a good state of hydration.

Skin hygroscopy is linked to a mixture of different hygroscopic substances contained in horny cells, the Natural Moisturizing Factor or NMF, consisting of inorganic ions, organic acids, urea and amino acids. The NMF seems to be protected by a semi-permeable lipid membrane which allows it to attract water by osmosis but which prevents it from leaving the cells. In addition, sebum constitutes with sweat a water-in-oil emulsion which exerts a regulating role in the evaporation of insensible perspiration, which maintains the hydration of the horny cells at its best level. Any dysregulation, physiological or artificial of these factors results in skin dehydration or skin dryness which results in a feeling of discomfort with tightness of the skin, then roughness and skin peeling with most often, signs of inflammation. The causes of skin dryness are multiple. For example, with regard to natural causes, we can cite: aging, diabetes, ichthyosis, hormonal imbalances, abuse of certain drugs (laxatives, diuretics ...).

Our way of life adds other sources of disruption such as, for example: more or less excessive exposure to ultraviolet radiation, atmospheric pollution (factories, cars ...), hot, firoid, wind, overheated housing, various skin reactions to synthetic fibers, consumption of tobacco and / or alcohol, untimely use of detergents, prolonged baths, mechanical friction exerted on the skin (clothing, shaving) this list is not exhaustive. Dry skin is not only a discomfort for the person affected but it makes the skin lose its mechanical barrier properties, between the internal environment which is the organism and the external world. Indeed, the skin then loses its elasticity, becomes dry, rough, brittle, which promotes excessive flaking. The cosmetic industry is therefore fully in its role when it is constantly looking for new concepts and products capable of preventing or reducing skin dryness of all origins.

The object of this patent application lies in the discovery, and in the demonstration, that a new solution, which is the subject of this patent application, can be proposed in the situations described above.

Indeed, surprisingly, by its properties, properly prepared and used, birch sap is able to rehydrate the skin at an optimal level, to calm the feelings of discomfort produced by mechanical irritation, in particular by shaving. daily well known to start the razor fire, to provide an anti-fatigue feeling and to vitalize the tissues.

Man has been using birch for a long time. The Nalmont-Bomare Universal Raised Dictionary (1791) mentions that baskets, baskets & hoops for barrels & for tanks, abots, wheels are made of them (page 423). The sap was also used to make an empyreumatic oil, a slightly acidic Hqueur, to treat kidney and bladder stones, as well as to remove facial spots (page 425).

As the birch sap is remarkably stable over time and that its composition differs little according to the species and the origins, the birch sap usable within the framework of this patent application can be collected by any process on any what birch, from any country.

Currently, birch sap is mainly used as a food supplement providing trace elements (silicon, selenium, lithium, chromium, manganese, zinc, gold, cobalt, copper) and minerals (calcium, potassium magnesium). During the development of the project that led to this patent application, we We have found that the beneficial activities of birch sap on the applications mentioned above can be explained by its composition.

Calcium, in its mineralized phosphate form and strengthens the extracellular matrix and magnesium intervenes as an enzyme cofactor in tissue energy metabolism.

Silicon strengthens the elastic connective tissues where the concentration of this trace element is very high in the inter fibrillar proteoglycans, zinc intervenes in the healing processes as a co-factor of many enzymes and selenium has a strong antioxidant power and plays a powerful detoxification role by activating glutathione peroxidase.

The following two examples will illustrate the use of birch sap in effective cosmetic preparations. Example 1: Gel

Phenova 0.60

Ultrez 10 0.30

Natrosol 250 M 0.05

Sorbate 0.10

NaOH 30% 0.30

Birch sap 5.00

Perfume & Demineralized water qs 100

Example No. 2: After Shave Balm

NaOH 30% 0.40

Sorbate 0.10

DC 200 2.00

PemulenTR2 0.20

Cithrol GMS 1.00

Covio T70 0.20

Crodamol IPP 4.00 Nipastat 0.20

Glycerin 5.00

Ultrez 10 0.20

Birch sap 5.00

Perfume & Demineralized water qs 100

The following four examples demonstrate the effectiveness of our invention through in vivo testing. Example 3: Skin irritation - Razor burn - sensory test - In vivo

The test consisted of being evaluated by 30 volunteers, male, aged 25 to

50 years, the shaving balm of example n ° 2 following a shaving carried out according to their daily habits. The balm was applied immediately after shaving on the right hemi-face (arbitrarily defined before the test) while the other hemi-face received nothing.

Thus, 16 volunteers used an electric razor while the other 14 shaved with a mechanical razor of the same model and the same shaving cream, the balm being applied immediately after shaving.

The sensory test consisted in defining and quantifying the duration as well as the intensity of the sensations felt by each panelist on the parts of the face having received or not having received the application of the balm containing birch sap.

The following table indicates, for each criterion identified, the percentages of variation (positive or negative) between the treated hemi-face compared to the untreated hemi-face.

Electric shaving Mechanical shaving

Intensity Duration Intensity Duration

Heating - 25.4% - 21.3% - 17.3% - 26.2%

Irritation - 19.7% - 25.5% - 26.9% - 31.1%

Hydration + 22.7% - 26.9% - 11.2% - 10.3%

Freshness + 27.2% - 29.2% - 21.7% - 24.6%

Thus, the balm of Example 2 which contains 5% birch sap provides clearly soothing sensations on the razor burn, and this, as well for panelists using electric shaving as mechanical shaving.

Example No. 4: In Vivo Skin Hydration

This example demonstrates the skin moisturizing effect obtained, in vivo, on the legs of 15 adult female volunteers. The hydrating power of the birch sap which is the subject of this patent application, incorporated in concentrations of 0.3,

3.0 and 7.0% in the preparation of Example No. 1 (where the only concentration of 5% was mentioned), was compared with that of a placebo (ie the same preparation but without birch sap ) and no treatment. This test can be briefly described as follows. The skin's hydration level is measured by the skin's electrical capacity using a corneometer (Courage and Khazaka, model CM 820), a technique conventionally used in cosmetology.

Indeed, the electrical properties of the surface layers of the skin are strongly linked to its water content. Five independent sites are identified using adhesives and pen markings, then, after a period of 20 minutes of rest in a seated position, the same measurements as those made at T0 are carried out in triplicate, at each site.

Each cream studied (placebo and birch sap extract at different concentrations) is then applied until complete penetration, on an independent site, at a rate of 20 μl per site.

The fifth site previously identified does not receive any product.

The volunteers remain at rest.

Three measurements per site are carried out every hour, and this, for 6 hours.

The temperature and humidity of the room where the test is carried out are kept constant throughout the test.

The following table shows the results obtained during the realization of this example, (Read birch sap for Birch).

T 0 T + 1H T + 2H T + 3H T + 4H T + 5H T + 6H ien 0 - 0.6 - 0.4 - 0.5 ± 0.1 + 0.4 + 0.2 lacebo 0 + 0 , 1 0.0 + 0.8 + 1.1 + 0.9 + 1.3 Birch 0.3% 0 + 7.5 + 11.0 + 13.2 + 13.6 + 11.8 + 10.2 Birch 3.0% 0 + 15.6 + 23.1 + 24.9 + 26 , 7 + 26.5 + 20.9 Birch 7.0% 0 + 25.5 + 32.2 + 33.8 + 36.8 + 35.2 + 32.2 This example clearly demonstrates a strong hydrating power since no only, depending on the type of extract tested, skin hydration is increased by 30% to 35% compared to the start of the test but, moreover, it is sustained since the effect is particularly evident during at least the six hours of the test. In addition, the observed effect is clearly concentration-dependent, which proves that it is indeed the birch sap tested that we owe the measured effect. A final argument which confirms the role of birch sap in the observed effect lies in the fact that, under the same conditions, the placebo cream (without birch sap), has no hydrating effect, just as it is possible to see it when no product is applied. Example n ° 5: Energizing effect in vitro At the intra-cellular level, energy is supplied by adenosine triphosphate (ATP). Its specific measurement is therefore equivalent to establishing the cellular energy level and thereby that of the tissue itself.

The intracellular quantity of ATP is measured by luminescence, a well-established technique (Doctor & al., (1994) Am. J. Physiol, 266, C1803-C1811; DeLuca & MacElroy (1978) Methods Enzymol. 57, 3 -15).

It is based on the dependence on ATP of the luciferase / luciferase reaction, a reaction which emits light. Photonic measurement also makes it possible to highlight very small amounts of ATP (of the order of 10E-10M). In the protocol used, the cells used, normal human fibroblasts in culture, are purged of their intracellular ATP stock using a DMEM medium (*) deficient in glucose and pyruvate (metabolite of the Krebs cycle) but containing glutamine and 2-deoxy-D-glucose which is a non-ATP glucose producing analogue. Washing the culture removes 2-deoxyglucose, the cultures then receive different media whose capacity to increase ATP synthesis compared to the control is evaluated

The following table indicates the cellular ATP concentrations (pM.10 ⁶ cells) obtained after 6 independent tests of each other, during which the birch sap was tested at different concentrations (indicated as [c]): 0.1, 0.3

1.0, 3.0 and 5%.

The values given correspond to the means and standard deviations.

Birch | c | 0 0J 0.3 1.0 3.0 5.0]

Average 4.9 6.1 7.4 10.3 13.1 15.0 Standard deviation 0.5 0.9 1.1 2.1 1.5 1.9

It should be noted that, under our conditions, when these same cells are incubated in the presence of glucose, the normal ATP level is 19.0 + 1.0 pM.10 ⁶ cells. These results clearly demonstrate that the birch sap, at the concentrations tested, has a powerful effect of restoring the intracellular energy level since the ATP levels approach the normal value.

In addition, it should be noted that this effect is concentration dependent, which demonstrates the specificity of the results.

Finally, this effect is only observed in the presence of birch sap, which demonstrates that the energy deprivation conditions were correctly achieved, which validates the test and therefore confirms the results.

Example No. 6: Effect on the viscoelastic properties of the skin - in vivo The study was carried out to evaluate the effect of birch sap, in comparison with a control without application, on the viscoelastic properties of the skin, by successive Cutometry measurements, at T0 and 28 days after the start of twice daily application of the T481 cream, in 15 adult female volunteers.

Relevance of the measurement: The measurement of the viscoelastic skin parameters using a Cutometer makes it possible to objectively judge the effect of the cosmetic product on the biomechanical properties of the skin during repeated applications. This device measures the deformation of a stressed skin area mechanical (six successive sucks, repeated three times) and its recovery power (Barel et al., (1995), in Handbook of non-invasive methods and the skin, Serup and Jemec (eds.), CRC Press, pp 335- 340).

It is a classic method of study, the viscoelastic properties of the skin are indeed correlated to the notions of flexibility, elasticity and firmness of the seed coat.

The product tested was the gel of Example 1 (containing 5% birch sap).

The test was carried out on 15 people, female, (38 to 44 years old), selected according to classic criteria: being of legal age, voluntary for this study etc. The panéUstes are installed in a sitting position at least 10 minutes before the start of the test. The room temperature and humidity are constant throughout the duration of the test.

The site of application of the cream is located on the right or left neck according to a randomized distribution. The mechanical properties of the skin are determined using a cutometer

SEM474 (Courage + Khazaka, Germany). In each case, 5 successive measurements are made at T0 on the site. The Cutometer measurement probe is carefully repositioned between each measurement. The values obtained at T0 serve as reference values for the rest of the test. Each of the gels of Example No. 1 is applied, under normal conditions of use, to the measurement site by the volunteer until complete penetration, this twice a day for 28 days from the delivery of the cream. . Each volunteer is expressly asked not to apply another cream with a similar aim on the neck. Five measurements are made 28 days (T +28) after the start of applications in the same way as at T0. The average values of the measurements made at T +28 are compared with those obtained at T0.

The parameters determined after 6 constraints are:

• Ue: immediate elongation (purely elastic component) • Uv: delayed elongation (viscoelastic component) • Ur: immediate retraction (elastic return)

• Ua: elongation recovered after stress

• Uf: final elongation (total deformation: elastic and plastic)

• Residue: residual deformation after a stress • Residu2: residual deformation after six stresses

For our study, we took into account:

• Ur / Ue: (ratio of elastic deformations = tone)

• Ur: immediate retraction (elastic return)

• Résidu2 -Résidul (cutaneous fatigue) The viscoelastic properties of the skin are evaluated in vivo with the SEM 474 Cutometer (Courage and Khazaka, Germany). This device measures the deformation of a skin area subjected to mechanical suction stress and its recovery power. The Cutometer includes three elements and a computer to control the measuring device and view the graphs obtained. For each parameter and for each site, a statistical analysis was carried out (Student test) to compare the changes between TO and T 28 days as well as the comparison between the sites treated by applying the gel of Example No. 1 with the site without application. The following table indicates the results obtained on the viscoelastic parameters of the skin at TO and T +28 with the gel of Example No. 1.

Ur / Ue Ur Residue 2 - Residue 1

Deformation report Immediate retraction Skin fatigue Elastics (tone) or Elastic return

Avg. T Ô 0.744 0.383 0.107 Avg. T +28 0.743 0.452 0.087

The following table indicates the values of the viscoelastic parameters of the skin at T0 and T +28 obtained without application: Ur / Ue Ur Residue 2 - Residue 1

Avg. T 0 0.808 0.420 0.078

Avg. T +28 0.693 0.425 0.107

The following table indicates the results of the statistical analyzes between T0 and Tl, for each site and those of the statistical analyzes between treated site and control site for the parameter Ur / Ue which translates the report of the elastic deformations "tone".

Application site Site without gel comparison (ex n ° 1) application of the 2 sites

% change * - 0.2% - 14.2% -

Analysis of variance Identical ** Identical ** Identical **

T test 0.06 2.96 2.53

Judgment Dns Ds p <0.05 Ds p <0.05

The following table indicates the results of the statistical analyzes between T0 and T +28, for each site and those of the statistical analyzes between treated site and control site for the Ur parameter or Immediate retraction or elastic return. Application site Site without gel comparison (ex n ° 1) application of the 2 sites

% change * + 18.2% + 1.3% -

Analysis of variance Identical ** Identical ** Identical **

T test 2.86 0.01 2.53

Judgment Ds p <0.05 Dns Ds p <0.05

The following table indicates the results of the statistical analyzes between T0 and T +28, for each site and those of the statistical analyzes between treated site and control site for the parameter residue2 - residue, skin fatigue.

Application site Site without Comparison gel (ex n ° 1) application of the 2 sites

% change * - 18.2% + 37.3% -

Analysis of variance Identical ** Identical ** Identical **

T test 1.17 2.39 4.31

Judgment Dns Ds P <0.05 Ds P <0.01

(*):% variation between Tl and TO: 100 x (Average T +28 - Average T0) /

Average T0.

(**): Variance (TO compared to T +28 or site treated compared to control site) identical to the 5% risk. (***): Significance is obtained if t above is greater than 2.26 (p <0.05) or greater than 3.25 (p <0.01).

Ds: significant difference between (between T0 and T +28 or treated site and control site).

Dns: non-significant difference between (between T0 and T +28 or treated site and control site). In conclusion, it is clear that the gel of Example No. 1 containing 5% birch sap caused the parameters studied to vary between TO and T +28 as follows

• Very small non-significant 0.2% variation in the Ur / Ue ratio (this ratio reflects the "tone").

• 18.2% increase in the Ur parameter (immediate retraction or elastic return). This increase is statistically significant (p <0.05).

• 18.2% decrease in the Residue2-Residul parameter (skin fatigue). However, this decrease is not significant (p = 0.27).

In addition, the parameters studied between T0 and Tl on the site without application varied as follows: • Decrease of 14.2% in the Ur / Ue ratio (this ratio reflects the "tone").

This decrease is statistically significant (p <0.05).

• Very small non-significant variation of 1.3% of the Ur parameter (immediate retraction or elastic return).

• Significant increase of 37.3% in the Residue2-Residul parameter (skin fatigue). This increase is statistically significant (p <0.05). Finally, the statistical analysis of the difference LogTl - LogTO between the treated site and the site without application shows that whatever the parameter studied, the difference in effect observed between a treatment with the gel of example n ° 1 containing 5% birch sap and no treatment, is statistically significant (p <0.05 or p <0.01).

Due to the activities demonstrated above, birch sap can be used as it is or in cosmetic or dermopharmaceutical preparations for all skin care, mucous membranes and dander (nails, hair and hair), especially to soothe fire razor, to hydrate and soften the skin, provide an anti-fatigue feeling, as well as to detoxify and vitalize the tissues. In addition, its obtaining, its ease of incorporation into all preparations conventionally used in cosmetics or dermopharmacy as well as its cost price, makes it an elegant solution and perfectly usable at the industrial level to solve the skin problems exposed above. In the cosmetic or dermopharmaceutical composition, it may be advantageous to combine birch sap with other active agents, and in particular with sea buckthorn juice, in order to reinforce its effect by additivity or synergy between the effects of these different products. , or in order to associate the effect described in this patent application with another beneficial physiological effect on the skin, mucous membranes, integuments (nails, hair and hair).

In the finished cosmetic or dermopharmaceutical composition, the concentration of birch sap can vary between 0.001% and 50% (w / w), preferably between 0.1% and 10% (w / w). Birch sap, alone or in combination with other active ingredients, and in particular with sea buckthorn juice, is used in any dosage form used in cosmetics or dermopharmacy: O / W and W / O emulsions, milks, lotions, ointments, hair lotions, shampoos, soaps, sticks and pencils, sprays, body oils, without this list being exhaustive. Birch sap, alone or in combination with other active ingredients, and in particular with sea buckthorn juice, is used in the form of a solution, dispersion, emulsion, or encapsulated in vectors such as macro-, micro- or nanocapsules, liposomes or chylomicrons, or included in macro-, micro- or nanoparticles, or in micro-sponges, or adsorbed on powdery organic polymers, talcs, bentonites and other mineral supports. Birch sap, alone or in combination with other active ingredients, and in particular with sea buckthorn juice, is incorporated into any other ingredient usually used: extraction and / or synthetic lipids, gelling and viscosifying polymers, surfactants and emulsifiers, water- or fat-soluble active ingredients, plant extracts, tissue extracts, marine extracts, sun filters, antioxidants. Birch sap, alone or in combination with other active ingredients, and in particular with sea buckthorn juice, is used in cosmetic or dermopharmaceutical compositions; used for all skin care, mucous membranes and dander (nails, hair and hair), especially to soothe razor burn, to moisturize and soften the skin, provide an anti-fatigue sensation, as well as to detoxify and vitalize tissue.

Birch sap, alone or in combination with other active ingredients, and in particular with sea buckthorn juice, is incorporated into cosmetic or dermopharmaceutical compositions for the preparation of a medicament used for all skin care, mucous membranes and integuments (nails, hair and hair), especially to soothe the razor burn, to moisturize and soften the skin, to provide an anti-fatigue sensation, as well as to detoxify and vitalize the tissues. Birch sap, alone or in combination with other active ingredients, and in particular with sea buckthorn juice, is incorporated into cosmetic or dermopharmaceutical compositions, linked or incorporated or absorbed or adsorbed in the form of macro-, micro- and nanoparticles or in macro-, micro- and nanocapsules, in textiles, synthetic or natural fibers, wool and all materials likely to be used to make clothes and underwear for day or night, directly in contact with the skin or hair to allow continuous topical delivery.

Claims

1. Use of birch sap in cosmetic and dermopharmaceutical compositions for all skin care, mucous membranes and dander (nails, hair and hair), especially to soothe razor burn, to moisturize and soften the skin, provide an anti-fatigue sensation, as well as to detoxify and vitalize the tissues.

2. Use of birch sap according to claim 1 characterized in that the birch sap is used alone or in combination with other active ingredients, and in particular with sea buckthorn juice.

3. Cosmetic and dermopharmaceutical compositions according to claims 1 or 2, for all skin care, mucous membranes and dander (nails, hair and hair), especially to soothe razor burn, to hydrate, to provide an anti-fatigue sensation and to vitalize the tissues characterized in that they contain birch sap obtained by any process from all varieties of birch of any origin whatsoever.

4. Cosmetic and dermopharmaceutical compositions according to claim 3, characterized in that the content of birch sap can vary between 0.001% and 50% (w / w), preferably between 0.1% and 10% (w / w).

5. Cosmetic and dermopharmaceutical compositions according to any one of claims 3 to 4, characterized in that they are in any galenic form used in cosmetics or dermopharmacy: HE and W / O emulsions, milks, lotions, ointments, hair lotions, shampoos, soaps, sticks and pencils, sprays, body oils.

6. Cosmetic and dermopharmaceutical compositions according to any one of claims 3 to 5, characterized in that birch sap is incorporated in cosmetic vectors such as liposomes, chylomicrons, macro-, micro- and nanoparticles as well as macro- , micro- and nanocapsules, to absorb them on powdery organic polymers, talcs, bentonites and other mineral supports.

7. Cosmetic and dermopharmaceutical compositions according to any one of claims 3 to 6, characterized in that birch sap is used with any other ingredient usually used in cosmetics: extraction and / or synthetic lipids, gelling and viscosifying polymers, surfactants and

5 emulsifiers, water- or fat-soluble active ingredients, in particular caffeine, extracts from other plants, tissue extracts, marine extracts.

8. Use of the birch sap according to any one of claims 1 to 2, or compositions according to any one of claims 3 to 7 for the preparation of medicaments for all care of the skin, mucous membranes and skin appendages (nails, hair and hair), especially to soothe the razor burn, to hydrate and soften the skin, provide an anti-fatigue sensation, as well as to detoxify and vitalize the tissues.

9. Use of birch sap according to any one of claims 1 to 2, or compositions according to any one of claims 3 to 7 5 characterized in that they are bonded or incorporated or absorbed or adsorbed in the form of macro-, micro- and nanoparticles or in macro-, micro- and nanocapsules, in textiles, synthetic or natural fibers, wool and all materials capable of being used to make clothes and underwear for day or night, directly in contact with the skin or hair to allow continuous topical delivery.