EP2139459A1

EP2139459A1 - Dermatological composition for the prevention and/or treatment of rosacea, of couperose or of skin which exhibits diffuse redness or small dilated vessels

Info

Publication number: EP2139459A1
Application number: EP08749681A
Authority: EP
Inventors: Valérie PERIER; Stéphanie RINALDIN
Original assignee: Pierre Fabre Dermo Cosmetique SA
Current assignee: Pierre Fabre Dermo Cosmetique SA
Priority date: 2007-04-23
Filing date: 2008-04-23
Publication date: 2010-01-06
Also published as: FR2915101A1; WO2008129066A1; JP2010525021A; FR2915101B1; JP5749006B2; US20100136068A1; CA2684835A1; US20140030299A1

Abstract

The invention relates to a dermatological composition for the prevention and/or treatment of rosacea, of couperose or of skin which exhibits diffuse redness or small dilated vessels, characterized in that it contains: -at least one interference pigment comprising titanium dioxide-coated mica, transmitting a colour complementary to red; -at least one sunscreen that is active in the UVA and UVB ranges; -one or more soothing and/or moisturizing active ingredients; and -the rest as dermatologically acceptable excipient(s) necessary for formulating said composition.

Description

Dermatological composition for the prevention and / or treatment of rosacea, rosacea or skin with diffuse redness or small dilated vessels

The present invention relates to a dermatological composition for the prevention and / or treatment of rosacea, rosacea or skin with diffuse redness or small dilated vessels.

The rosacea is a permanent red state of the convex areas of the face (nose, cheeks, forehead, chin ...), sometimes with small vessels visible to the naked eye. Rosacea is all manifestations (pimples, plaques, tingling and redness of eyes ...) that complicate rosacea.

The pathophysiology of rosacea is still poorly understood even if a primitive vascular abnormality of the face is suspected. The cold climate, the heat work and the sun exposure are incriminated in the triggering of the initial forms of rosacea.

Most dermatological anti-redness formulations use high-masking pigments that work mechanically by covering the abnormally red areas of the skin. However, these formulations are unsatisfactory because they leave an unsightly opaque film on the skin. Other formulations employ colored pigments that complement red. However, these formulations have the disadvantage of coloring the areas of the face that are not affected by redness.

The inventors of the present patent application have developed a formulation which on the one hand makes it possible to obtain an immediate effect of masking the redness of the skin without presenting the disadvantages mentioned above, and which on the other hand allows the prevention and treatment of rosacea in the short, medium and long term.

The present invention relates to a dermatological composition for the prevention and / or treatment of rosacea, rosacea or skin that has diffuse redness or small dilated vessels, characterized in that it contains: at least one interference pigment comprising mica coated with titanium dioxide, transmitting a color complementary to that of red; at least one active sun filter in UVA and UVB; one or more soothing and / or moisturizing active ingredients; and the complement of dermatologically acceptable excipient (s) necessary to formulate said composition. The dermatological composition according to the present invention is endowed with a triple action staged over time, namely: an immediate action of optical masking of redness; a soothing effect and / or protection against UVA and UVB radiation in the short and medium term; - a long-lasting moisturizing effect.

The interference pigment allows instant optical masking of redness of the skin. It is chosen so as to transmit a complementary color to that of red, which will make it possible to make the flesh color natural to the areas of the skin affected by redness. The effect of the composition on the redness of the skin is immediate.

Thanks to the titanium dioxide which coats each particle of mica, the interference pigment also makes it possible to provide the composition with a protective effect against infrared radiation which, via warming of the skin, promotes the manifestations of rosacea. The interference pigment therefore also prevents the appearance or aggravation of rosacea or redness of the skin.

The interference pigment preferably represents between 0.5% and 10%, preferably between 0.5% and 3% by weight of the composition. The optimal amount of interfering pigment which allows the composition a good instant masking of redness, a good protection against infrared radiation and a quality of consistency and satisfactory rendering, is between 1% and 3% by weight of the composition.

The interference pigment is preferably composed of titanium dioxide coated mica particles, whose particle size at 80% is between 10 microns and 60 microns and whose ED50 is between 18 microns and 25 microns. The Timiron ® Super Green marketed by

Merck. The dermatological composition according to the present invention is advantageously devoid of any other white or colored pigment.

The broad-spectrum sunscreen active in UVA and UVB provides the composition with a preventive effect in the short and medium term against the appearance or aggravation of redness of the skin and other manifestations of rosacea. It is indeed known that solar damage in the dermis and dermal vessels, which are mainly due to UVA, are undeniably involved in the pathogenesis of rosacea. A mixture of UVA-active filters and UVB-active filters, whose anti-UVA activity is predominant or of broad-spectrum filters in sufficient quantity so as to obtain a consequent UVA protection, will preferably be used. Preferably, the amounts of anti-UVA filter and anti-UVB filter in the composition are determined so that the ratio between the protection factor measured by the in vivo test method of the Sun Protection Factor ^ι (SPF ) (mainly UVB rays) of the composition and the protective factor measured in vivo by persistent pigmentation test ² (mainly UVA rays) of the composition is much lower than 3. 1 method of calculation described in the International Method of sun protection factor test (2006).

Japan Cosmetic Industry Association (JCIA) Measurement standards for UVA protection efficacy. Nov 21, 1995.

The photoprotective system preferably represents between 15% and 30% by weight of composition. It may be chosen from the following organic screening agents: ethylhexyl salicylate, ethylhexylmethoxycinnamate, octocrylene, butylmethoxydibenzoylmethane, phenylbenzimidazole sulfonic acid, n-hexyl 2- (4-diethylamino-2-hydroxybenzoyl) benzoate, 4-methylbenzylidene camphor, terephthalylidene dicamphoric acid sulfonic acid, disodium phenyl dibenzimidazole tetrasulfonate, 2,4,6-tris- (diisobutyl 4'-amino benzalmalonate) -s-triazine anisotriazine, ethylhexyl triazone, diethylhexyl butamido triazone, methylene bis-benzotriazolyl tetramethylbutylphenol, drometrazole trisiloxane, polysilicone-15, 1,1-dicarboxy- (2 ', 2'-dimethyl-propyl) -4,4-diphenylbutadiene, B-ethylhexyloxyphenol methoxyphenyl triazine

The broad spectrum sunscreen active in UVA is preferably selected from Tinosorb® M (methylene bis-benzotriazolyl-tetramethylbutylphenol) and Tinosorb®

S (bis-ethylhexyloxyphenolmethoxyphenyl triazine), as well as mixtures thereof. Preferably, Tinosorb® M represents between 1% and 14% by weight of the composition and Tinosorb® S represents between 1% and 7% by weight of the composition.

The active sun filter in the UVB is preferably between 1 and 10% by weight of the composition. Preferably, 2-ethylhexyl A-methoxycinnamate, or Tinosorb® M (methylenebis-benzotriazolyltetramethylbutylphenol) broad spectrum filters or Tinosorb® S (bis (ethylhexyloxyphenolmethoxyphenyltriazine) filters for their UVB protection flap are used. The dermatological composition according to the present invention also comprises one or more soothing and / or moisturizing active ingredients, for a soothing action in the short and medium term and a long-term moisturizing action. The soothing active ingredient may be hamamelis water, bisabolol, allantoin, aloe vera, batyl alcohol and beta-glycerrhetinic acid, preferably water of hamamelis. The moisturizing active ingredient may be glycerine, d-panthenol, sodium hyaluronate, butylene glycol, propylene glycol, sorbitol, hyaluronic acid or chondroitin sulfate acid; glycerol is preferably used. The composition may also contain other active ingredients, such as antioxidants, such as, for example, α-tocopheryl acetate, ascorbic acid or ascorbyl palmitate. It may further contain a stabilizing agent, a sequestering agent and / or an anti-radical agent.

The dermatological composition according to the present invention may be prepared in the form of a water-in-oil (W / O) or oil-in-water (O / W) emulsion, a multiple emulsion such as, for example, a water-in-oil emulsion. water (W / O / W) or an oil-in-oil (W / O / W) emulsion, or in the form of a hydrodispersion or a lipodispersion, a gel, a stick or an aerosol. It is preferably in the form of an emulsion comprising an oily phase and an aqueous phase, said oily phase containing the sunscreen or sunscreens, and said aqueous phase containing the hydrating and soothing active ingredient (s).

The present invention is illustrated by the following examples. 1) Example of composition

Cream for the face, against diffuse redness and visible vessels.

¹ Mica coated with titanium oxide, marketed by Merck under the name ® Timiron Super Green

² Methylene bis-benzotriazolyl-tetramethylbutylphenol, marketed by Ciba under the name Tinosorb M

³ Bi-éthylhexyloxyphénolméthoxyphényl triazine sold by Ciba under the name Tinosorb S

The cream given as an example is an oil-in-water emulsion, the aqueous phase of which contains witch hazel water, glycerin, EDTA, xanthan gum, magnesium aluminum silicate, chlorphesin and water, and the oily phase contains tocopheryl acetate, ethylhexyloxyphenol, methoxycinnamate, behenate diglyceryl, benzoate, ethylhexyl palmitate, glyceryl stearate, potassium cetyl phosphate and siloxane.

2) Efficiency tests

2.1) Evaluation of the immediate soothing effect of the cream according to Example 1 on a thermal simulation model

The test is conducted on 12 women aged 20 to 42, on average 30.25 years.

The experimental plan is as follows: - taking the marks in grease pencil of an area of 3cm x 3cm at the cheekbone, basal measure of temperature and redness, performing the thermal stimulation at 38 ⁰ C for βminutes, temperature and redness measurements immediately after stimulation (TO), - triggering the stopwatch, according to the randomization, for the treated area only:

. application of 20 μl of the cream according to Example 1,

. Temperature and redness measurements at:

* Tl = 3 minutes after thermal stimulation * T2 = 5 minutes after thermal stimulation

* T3 = 7 minutes after thermal stimulation * T4 = 10 minutes after thermal stimulation

* T5 = 15 minutes after thermal stimulation

Evaluation of the tolerance of the product, - Realization of the same operations on the other cheek,

Evaluation of the tolerance of the product.

Efficacy results:

Cutaneous temperature: After thermal stimulation, the cutaneous temperature is immediately lowered and maintained at the basal level with the cream according to Example 1, unlike the untreated side for which it is necessary to wait 10 minutes.

Skin redness: After thermal stimulation, skin redness is significantly improved with the cream of Example 1 compared to the untreated side. Immediately after application of the product, the redness decreases by 13% against 3.6% untreated side. A quarter of an hour after application of the product, the redness decreased by 14.3% side treated with the cream according to Example 1, against 5% untreated side.

Conclusion: the cream according to Example 1 has a significant effect on the lowering of the temperature and the redness of the skin after thermal stimulation.

2.2) Consumer test carried out under confidentiality

70 women evaluated the cream according to Example 1 over a period of 21 days. After application, the vast majority of interviewees declare a supple and comfortable skin and for more than half, this comfort lasts all day.

Three quarters of them perceive a calming in the epidermis and two thirds the protective effect of the treatment.

The result obtained is considered natural by the very large majority. At the end of the 5 days of use, three quarters of the women questioned evoke less visible redness (clearly for a quarter) and a unified complexion (almost half of them).

At the end of the 21 days of use, the results observed at the end of the first 5 days are significantly improved. The redness is reduced for the vast majority and clearly for half of women. The complexions are more even (84%) and lighter (81%).

2.3) Immediate action of optical masking of redness obtained following the application of the cream according to Example 1

The test is performed on 2 women with blotchy skin and diffuse redness on the cheeks.

TO is the starting point of the study (before application of the cream according to Example 1).

This test is based on the measurement of changes in skin color.

Two series of colorimetric measurements are made with two different devices:

- on the one hand using a MINOLTA CR 300 ^® chromameter; - on the other hand using a CM508i ^® spectrocolorimeter.

These are devices intended to perform a three-dimensional analysis of the skin color (hue, saturation, clarity) according to the sensitivity curve of the eye. They indicate the

3 following parameters in arbitrary units (u. A.):

• L *: luminance that corresponds to brightness or brightness; "A *: represents the hue and saturation of the color on a green-red axis;

• b *: represents the hue and saturation of the color on a blue-yellow axis.

Thus, in the case of a color change: - if the color of the skin is lighter: the parameter L * increases; - if the skin is less red: the parameter a * decreases; - if the skin is less "yellow" (less bronzed appearance): the parameter b * decreases.

PROTOCOL:

• Measuring area: skin discoloration is measured at the cheek level on a previously defined area and marked with a marker mask. The diameter of the measuring surface is 1 cm.

• Application of the cream to be tested: the cream according to Example 1 is applied at a level of 2 mg / cm ² over a wider surface (approximately 5 cm * 5 cm) than the actual measurement zone (probe dimer).

• Measuring time: the values were recorded at TO (before application of the cream) and at T10 (after 10 minutes of exposure). Each measurement is repeated 3 times.

RESULTS:

The results of the measurements performed on each subject are presented in Tables 1 and 2 below:

Table 1: Chromameter measurements of parameters L *, a * and b * before and just after application of the cream according to Example 1 on skins with redness

Table 2: Spectrocolorimeter measurements of parameters L *, a * and b * before and just after application of the cream according to Example 1 on skins with redness

We observe that:

• L * increases: meaning that there is globally a lightening of the skin.

• a * decreases: which reasonably indicates that there is globally a decrease in redness.

• b * decreases: there is also a tendency to decrease the tanned appearance of the skin.

The Applicant has demonstrated the immediate action of a composition according to the present invention on redness. Indeed, after only 10 minutes of application, the skin is visually clearer, and less red.

Claims

1. Dermatological composition for the prevention and / or treatment of rosacea, rosacea or skin with diffuse redness or small dilated vessels, characterized in that it contains:

at least one interference pigment comprising mica in the form of particles coated with titanium dioxide, transmitting a color complementary to that of red and whose particle size at 80% is between 10 μm and 60 μm and whose ED50 is between 18 μm and 25 μm

at least one broad-spectrum sunscreen active in UVA and UVB;

one or more soothing and / or moisturizing active ingredients; and

- The complement dermatologically acceptable excipient (s) necessary (s) to formulate said composition.

2. dermatological composition according to claim 1, characterized in that it is provided with a triple step action over time.

3. Dermatological composition according to claim 2, characterized in that said triple step staged over time is broken down into:

an immediate action of optical masking of the redness;

- a soothing effect and / or protection against UVA and UVB radiation, in the short and medium term; - a long-lasting moisturizing effect.

4. Dermatological composition according to any one of claims 1 to 3, characterized in that it contains approximately between 0.5% and 10%, preferably between 0.5% and 3% by weight of said interference pigment .

5. Dermatological composition according to any one of claims 1 to 4, characterized in that the ratio between the protection factor measured by the in vivo test method of the Sun Protection Factor of the composition and the measured protection factor in vivo by persistent pigmentation test of the composition is less than 3.

6. Dermatological composition according to any one of claims 1 to 5, characterized in that said active filter in UVA is selected from Tinosorb® M and Tinosorb® S, and mixtures thereof.

7. Dermatological composition according to any one of claims 1 to 6, characterized in that it contains about 1% to 10% by weight of a UV active sun filter.

8. Dermatological composition according to claim 7, characterized in that said UV active solar filter is 2-ethylhexyl 4-methoxycinnamate.

9. Dermatological composition according to any one of claims 1 to 8, characterized in that the active ingredients are selected from water witch hazel, glycerin and α-tocopheryl acetate.

10. Dermatological composition according to any one of claims 1 to 9, characterized in that it further contains a stabilizing agent, a sequestering agent and / or an anti-radical agent.

11. Dermatological composition according to any one of claims 1 to 10, characterized in that it contains an emulsion comprising an oily phase and an aqueous phase, said oily phase containing the sunscreen, and said aqueous phase containing the principle or principles (s) active.

12. Composition according to claim 11 characterized in that the emulsion is an oil-in-water emulsion.

13. Dermatological composition according to any one of claims 1 to 12, characterized in that it corresponds at least substantially to the following composition: