Composition and method of treating pathological skin conditions

FIELD: medicine.

SUBSTANCE: invention refers to cosmetic industry and represents a non-foaming cosmetic composition of an oil-in-water emulsion containing (i) retinol, (ii) at least one polar emollient specified in a group consisting of propylene glycol stearyl ester, propylene glycol isostearate and mixtures thereof (iii) at least one non-polar emollient specified in a group consisting of aromatic or linear esters, Gerbe ester, mineral oils, squalane, isohexadecane, squalene, liquid paraffin and mixtures thereof with the weight ratio of the above polar emollient and the above non-polar emollient is found within the range of approximately 95 to 5 to approximately 40 to 60.

EFFECT: provided considerable reduction of retinoid-caused skin irritation and higher efficacy or retinoid.

11 cl, 3 ex, 7 tbl, 3 dwg

 

The scope of the invention

The present invention relates to containing retinoid compositions and to the use of such compositions for the treatment of pathological conditions of the skin.

Background of invention

Human skin undergoes a series of processes of aging, some of which are driven by internal processes (e.g., age ageing), and some are caused by external factors (e.g., photoaging). In addition, the possible short-term or chronic changes in the skin, such as acne, oily or dry skin, keratosis, rosacea, sensitivity, inflammation, erythema, and allergic or autoimmune reactions such as dermatitis and photodermatosis.

These factors can cause thinning of the skin, weakening the strength of adhesion of the epidermis and dermis, as well as reduce the number of skin cells and feeding them blood vessels. This often leads to the formation of wrinkles and pigmented defects.

Retinoids are used to treat pathological conditions of the skin caused by age ageing, external factors and skin diseases. More specifically, retinol is widely used for the treatment of acne and reduce the severity of wrinkles, stretch marks and cellulite.

However, despite the positive results of the use of retinoids, they can vyzyvaet the irritation. This side effect limits the application of retinoids.

Therefore, the aim of the present invention is the creation of new containing retinoids compositions and methods of treatment of the above pathological conditions of the skin, which avoids the adverse effects of retinoids. In particular, it was found that control of the speed of release of the retinoid of cosmetic compositions, for example, by adjusting the polarity of the components of the composition, to enhance the activity of retinoid and caused them to reduce irritation. The inventors have unexpectedly discovered that the combination of non-polar softener and polar softener within the desired weight ratios of these two components containing the retinoid composition leads to a significant reduction caused by retinoid irritation of the skin and increases the efficiency of the retinoid.

Brief description of the invention

The present invention relates to nebenabreden cosmetic compositions of the type emulsion oil-in-water containing (i) at least one retinoid selected from the group consisting of retinol, retinal and esters of retinol, (ii) at least one polar softener with a relative index polarity to the retinoid in the range from approximately 0.5 to 2, and (iii) IU is greater least one nonpolar softener with a relative index polarity to the retinoid in the range of from about 7 to about 10. The weight ratio mentioned polar softener and the above-mentioned non-polar softener is in the range from about 95 : 5 to about 40 to 60.

The present invention also relates to nebenabreden cosmetic compositions of the type emulsion oil-in-water containing at least one unencapsulated public retinoid selected from the group consisting of retinal and esters of retinol, and the rate of release of the above-mentioned retinoid of these compositions is in the range from about 1 mg/cm2/h to approximately 2.6 mg/cm2/hour.

In addition, the present invention relates to methods for treating acne and reducing the severity of wrinkles, stretch marks and cellulite by local administration of a cosmetically effective amount of the compositions that are the subject of the present invention, on the skin, requiring such treatment.

Other distinctive features and advantages of the present invention will become clear from the text of the detailed description of the invention and of its formula.

Brief description of drawings

Figure 1 shows the relationship between the polarity of the softener and the rate of release of the retinoid of cosmetic compositions.

On figa (the level of expression of HB-EGF in the Explant human skin) and 2B (the level of expression of CRABPII in the Explant is human skin) shows the relationship between the activity of retinol and content of isohexadecane in the Explant model of human skin.

Figure 3 shows the relationship between a called retinol irritation (level of IL8 expression after 24 hours of therapy) and the content of isohexadecane in the Explant model of human skin.

Detailed description of preferred embodiments of the invention

Unless otherwise noted, all materials used in this application of technical and scientific terms have a common value that is familiar to the expert in the field of the present invention. Everything mentioned in this application publications, patent applications, patents, and other references to external documents incorporated into it by reference. Unless otherwise stated, all of these descriptions percentages are given in weight percent (i.e.% wt.).

Used in this application, the term "local administration" means direct application to the skin or distribution on the skin, for example, by hand or using an appropriate applicator, such as a napkin.

Used in this application, the term "cosmetically effective amount" means an amount of a physiologically active compound or composition sufficient to treat acne or to reduce the severity of wrinkles, stretch marks or cellulite, but low enough to avoid any serious side effects. Cosmetically effective amount of the compound or composition is smenyaetsya depending on the specific condition, the treatment is carried out, age, and physical condition of the end user, the severity of the condition, the treatment is carried out, the duration of treatment, the nature of other treatment modalities, specific applicable connection, or a product (composition), and other such factors.

Used in this application, the term "acne" means an inflammatory disease of the hair follicles and sebaceous glands accompanied by the appearance on the skin black or whiteheads, pimples, nodules or, in more severe forms, cysts and scars. Such damage can occur on the face, neck, back, chest and arms.

Used in this application, the term "wrinkles" includes fine lines and wrinkles. Examples of wrinkles, among other things, include fine lines around the eyes (e.g., crows feet), wrinkles on the forehead and cheeks, brow wrinkles and wrinkles around the mouth.

Used in this application, the term "stretching" means shallow scars pink, reddish or purple colours often appear on the skin of the abdomen, Breasts, upper arms, buttocks and thighs.

Used in this application, the term "cellulite" means localized fat deposits, leading to bumpy skin. Caused by cellulite roughness does not have a uniform distribution or the government who enoi form, and affected by cellulite skin associated with orange peel or rind of the cheese.

It is assumed that the specialist based on this description, will be able to use the present invention in its maximum volume. Below, specific embodiments of the invention should be considered only as examples, which in no way limit disclose the essence of the present invention application.

Cosmetic compositions.

In one embodiment of the present invention disclose cosmetic compositions related to nebenabreden cosmetic compositions of the type emulsion oil-in-water, contain at least one retinoid selected from the group consisting of retinol, retinal and esters of retinol, at least one polar softener and at least one nonpolar softener.

In another embodiment, the disclosed cosmetic compositions related to nebenabreden cosmetic compositions of the type emulsion oil-in-water, containing at least one unencapsulated public retinoid selected from the group consisting of retinol, retinal and esters of retinol, and the rate of release of the above-mentioned retinoid of these compositions is in the range from about 1 mg/cm2/h to approximately the nutrient 2.6 mg/cm 2/hour.

In the following embodiment, the disclosed cosmetic composition contains a fatty phase in which is dissolved at least one retinoid selected from the group consisting of retinol, retinal and esters of retinol, and mentioned fatty phase preferably has a relative index polarity to the retinoid in the range of from about 0.5 to about 5.

Retinoid

Used in this application, the term "retinoid" refers to a class of compounds with the skin biological activity of vitamin A.

Relevant to the purposes of the present invention retinoid selected from the group consisting of retinol, retinal and esters of retinol. Preferred retinoids include retinol, retinilpalmitat, reinjected, retailpoint, retinal, or a mixture thereof. Preferred retinoids include retinol, retinal, or a mixture thereof. The most preferred retinoid is retinol. These compounds are well known to specialists in this field and are supplied by a number of companies, for example, Sigma Chemical Company, St. Louis, PCs Missouri, USA) and Boerhinger Mannheim (, Indianapolis, PCs Indiana, USA).

Forming the subject of the present invention the compositions contain a safe and effective amount of a retinoid. The described compositions preferably will gain from about 0,001% to about 2% of a retinoid, more preferably from about 0.01% to about 1% of a retinoid, and most preferably from about 0.05% to about 0.5% of a retinoid.

In one embodiment, the retinoid is used in the unencapsulated public form. This means that the retinoid is not contained in and not deposited on the surface of another material. One of the advantages of the present invention is the ability to use retinol is not in the form supplied by the company BASF ingredient RetiSTAR®, as for use in the compositions that are the subject of the present invention does not require stabilization of retinol.

Softeners

Disclosed cosmetic compositions contain at least one polar softener and at least one nonpolar softener. Relevant to the purposes of the present invention the polar softener preferably has a relative index polarity to the retinoid in the range from approximately 0.5 to 2. Relevant to the purposes of the present invention nonpolar softener preferably has a relative index polarity to the retinoid in the range of from about 7 to about 10. The composition forming the subject of the present invention, preferably have a relative index polarity to the retinoid range from about 0.5 to about 5. Moreover, used retinoid has sufficient speed of the release described cosmetic composition to the skin while maintaining reduced irritation and increased activity.

The concept of relative index polarity (RPI) of the softener is well known to specialists in this field. The methodology of its calculation is described in the article Wiesher et al. 2004 Int J. Cosmetic Science. 26, 173-182). The RPI can be calculated from the distribution coefficient octanol/water (K) as follows:

RPI=log K.

Calculated distribution coefficient K, for example, in the following works:

- Leo A, Hansch C, and D Elkins (1971). "Partition coefficients and their uses". Chem Rev 71 (6): 525-616.

Wilkinson, Andrew M.; McNaught, Alan D. (1997). "Partition Coefficient". Compendium of Chemical Terminology: IUPAC Recommendations. Oxford: Blackwell Science. doi:10.1351/goldbook. ISBN 0-86542-684-8. http://goldbook.iupac.org/P04437.html" _ and

- Sangster, James (1997). Octanol-Water Partition Coefficients: Fundamentals and Physical Chemistry, Vol. 2 of Wiley Series in Solution Chemistry. Chichester: John Wiley & Sons Ltd. pp. 178 pages.

The RPI value for retinol is approximately 1.

Rpis for retinal and esters of retinol is well known to specialists in this area and is close to the value of the RPI for retinol.

The net value of the RPI for the softener to the retinoid equal to the difference between the values of RPI for the softener and the values of RPI for retinoid.

The net value of the RPI for the composition to the retinoid is equal to RA the particular values of RPI for the composition and values of RPI for retinoid.

The net value of the RPI for oily phase to the retinoid equal to the difference between the values of RPI for oily phase and the values of RPI for retinoid.

The purpose of the present invention in the role of nonpolar softener correspond to aromatic or linear esters, ether Emblem, mineral oil, squalane, isohexadecane, squalene, liquid paraffin, etc.

Preferred non-polar softeners for the purposes of the present invention include isohexadecane, squalane, and mixtures thereof.

The purpose of the present invention in the role of the polar softener correspond stearyl ether, propylene glycol, isostearic propylene glycol, etc.

Preferred polar softeners include stearyl ether GPR-15, isostearic propylene glycol and mixtures thereof.

In accordance with the disclosed invention, the weight ratio of the used polar softener used to the nonpolar softener depends on a number of factors, including the molecular weight of water softeners, the relative index polarity of softeners to the selected retinoid and solubility of retinoids. In one embodiment, the weight ratio mentioned polar softener to the mentioned non-polar the softener is in the range from about 95 : 5 to about 40 to 60. The weight ratio mentioned polar softener to the mentioned non-polar is the softener is preferably in the range from about 90 to 10 to about 45 to 55, and most preferably is in the range of from about 85 to 15 to approximately 50 to 50.

In another embodiment, the weight ratio of the used polar softener used to nonpolar the softener can be adjusted so that the rate of release of the above-mentioned retinoid described cosmetic composition was in the range of from about 1 mg/cm2/h to approximately 2.6 mg/cm2/hour.

Nonpolar and polar softeners together comprise from about 0.1% to about 50% weight. the described compositions preferably comprise from about 1% to about 40% weight. the described composition, and most preferably comprise from about 2% to about 25% weight. the described composition.

Cosmetically acceptable carriers

Cosmetic compositions forming the subject of the present invention may also contain one or more cosmetically acceptable carriers.

Used in this application, the term "cosmetically acceptable" means use in contact with tissues (e.g., the skin) without showing nonspecific toxicity, incompatibility, instability, irritation, allergic reactions, etc. commensurate with a reasonable ratio of the olza/risk.

The objectives of the present invention, the media, inter alia, include water, ethanol, isopropanol, 1,2-propandiol, glycerol, benzyl alcohol, dimetridazole, triacetin, glycol ethers, propylene glycol and polyethylene glycol (PEG). Especially preferred solvents include PEG with an average molecular weight in the range from about 200 to about 400, castor oil, triacetin, dimetridazole, ethanol and water, and combinations thereof. Mentioned cosmetically acceptable carrier comprises from about 50% to about 99.99% of the weight. the described composition, more preferably is from about 80% to about 95% weight. the described composition.

For adjusting the osmolarity and / or pH to an acceptable level in the composition can optionally enter a different connection. The latter, inter alia, include mannitol, sucrose, calcium chloride, sodium chloride, monobasic sodium phosphate, dibasic sodium phosphate, sodium hydroxide and hydrochloric acid.

The described compositions can be made in the form of a wide range of cosmetics, which, among other things, includes lotions, creams, gels, sticks, sprays, ointments, cleansing liquid funds and solid Soaps, shampoos and hair conditioners, pastes, foams, powders, mousses, shaving creams, CA is petki, strips, patches, electroplater, bandages and band-AIDS, hydrogels, film-forming products, masks for skin and face, means for makeup such as concealer, pencil eye liner, eye shadow, etc.

These kinds of products can contain several types of cosmetically acceptable carriers, including, without limitation, solutions, suspensions, emulsions, such as micro-emulsions and nano-emulsion, gels, solid carriers, and liposomes. A specialist in this area has to offer and other media.

Emulsifying system

To obtain the corresponding purposes of the present invention emulsions of the type oil-in-water may be any cosmetically acceptable emulsifying system. Used emulsifying system has only a minor influence on the rate of release of the retinoid.

Used emulsifying system may be preferably selected from the group consisting of:

a) stearates, in particular, steareth 21, steareth 2 and mixtures thereof (such as 3% Brij 72/2% Brij 721);

b) glyceraldehyde, cetyl alcohol, stearyl alcohol, BeginInvoke alcohol, palmitic acid, stearic acid, hydroxyethylidenediphosphonic chloride and mixtures thereof, in particular, 4% Prolipid 151; and

c) Cetearyl alcohol/ceteareth-20, ceteareth-20/stearyl sleep the TA and / or their mixtures, in particular, Promulgen G and Promulgen d

More preferably used emulsifying system is a mixture of Cetearyl alcohol/ceteareth-20, ceteareth-20/stearyl alcohol.

Additional cosmetically active substances

In one embodiment, the composition forming the subject of the present invention may also contain one or more cosmetically active substances in addition to the above components. "Cosmetically active agent" is a compound, which may be a synthetic compound or a compound extracted, isolated, purified, or concentrated from a natural source, or a natural extract containing a mixture of compounds that has a cosmetic or therapeutic effect on the tissue of the body, including, but not limited to: antimicrobial agents, such as protivogryazevye, antifungal and antibacterial agents, anti-inflammatory substances that slow the aging agents, antiparasitic agents, antioxidants, keratolytic substances, nutrients, vitamins, minerals, energy supplements, pH correctors, etc.

Examples of vitamins that may be included in the compositions that are the subject of the present invention, inter alia, include vitamins is A, the B vitamins, such as vitamin B3, vitamin B5, vitamin B7, and vitamin B12, vitamin C, vitamin K, vitamin E, for example, alpha-, gamma - or Delta-tocopherol, and derivatives thereof (such as salts and esters) and mixtures.

Examples of antioxidants, among other things, include water soluble antioxidants such as sulfhydryl compounds and their derivatives (e.g., sodium metabisulfite and N-acetyl cysteine), lipoic acid and dihydrolipoic acid, resveratrol, lactoferrin, as well as ascorbic acid and derivatives of ascorbic acid (e.g., ascorbyl palmitate and askorbinovoyj polypeptide). The objectives of the present invention the fat-soluble antioxidants, among other things, include bottled hydroxytoluene (OSH), different types of Tocopherols (e.g., alpha-, gamma - and deltatheta and their esters, such as acetates and mixtures thereof, the tocotrienols. The objectives of the present invention contains natural extracts containing antioxidants, among other things, include extracts containing flavonoids, isoflavones and their derivatives, such as genistein and diacetin (for example, extracts of soybean and clover containing resveratrol extracts and so on).

Preferably the composition forming the subject of the present invention, do not contain ubiquinone.

More preferably, compositions, SOS is alaysia object of the present invention, not contain any of the b group vitamins, particularly vitamin D3.

In a preferred embodiment, the composition constituting the object of the present invention, does not contain any additional cosmetically active substances.

Other substances

The composition can also include various other substances. These include proteins and polypeptides, preservatives and alkaline substances. Examples of such substances are disclosed in the Handbook 2008 International Cosmetic Ingredient Dictionary and Handbook, 12thEdition, published by the Council by means of personal hygiene.

In one embodiment, the retinoid is dissolved in the fatty phase of the composition, and mentioned fatty phase has a relative index polarity to the retinoid in the range of from about 0.5 to about 5. The components mentioned fatty phase of the compositions described selected and combined in their respective weight or molar ratios to achieve the desired relative index polarity of the fatty phase.

In another embodiment, the retinoid is used in the unencapsulated public, and the rate of release of the above-mentioned retinoid of these compositions is in the range from about 1 mg/cm2/h to approximately 2.6 mg/cm2/hour. This can be achieved, for example, through the skin is of polar and nonpolar softeners with relative index polarity to the retinoid in the range from approximately 0.5 to 2 and 7 to 10, accordingly, as described in this application.

The present invention further defined in the following examples. It should be understood that these examples, while the preferred embodiments of the present invention, given solely for the purpose of illustration. From the above description and the following examples, the person skilled in the art can understand the main characteristics of the present invention and, without departing from its essence and scope, to perform various changes and modifications of the invention to adapt it to various purposes and conditions of use.

Unless otherwise specified, all of these percentages are given in weight percent.

EXAMPLES

Example 1. Cosmetic compositions.

In Tables 1 and 2 shows examples of compositions in accordance with the present invention.

Dost. Qty
Table 1
ComponentThe softener
7%
(wt%)
The softener
7%
(wt%)
The softener
20%
(wt%)
The softener
20%
(wt%)
WaterDost. QtyDost. QtyDost. Qty
Carbomer0,40,40,40,4
Disodium add0,10,10,10,1
Methylparaben0,20,20,20,2
Propylparaben0,150,150,150,15
Phenoxyethanol0,50,50,50,5
Sodium hydroxide1111
Literallayout; PEG-100 stearate2222
OSH0,1 0,10,10,1
Cetyl alcohol1111
Isohexadecane3,50,5100,5
BCP-15 stearyl ether3,571020
Retinol0,1150,1150,1150,115
Polysorbate 20is 0.135is 0.135is 0.135is 0.135
Ascorbic acid0,050,050,050,05

/tr>
Table 2
Component% the weight.
Water Dost. Qty
The copolymer of acryloyldimethyltaurate ammonium/vinylpyrrolidone0,50
Disodium add0,10
Allantoin0,10
Glycerin5,0
Butyleneglycol2,0
Carisolrodol0,50
Methylparaben0,250
PEG-85,0
Dihydroxyethane0,10
Cetearyl alcohol; ceteareth-203,0
Stearyl alcohol; ceteareth-203,0
Ethylhexylacrylate2,0
Isohexadecane1,5
BCP-15 stearyl ether4,5
Pentaerythritoltetranitrate7,0
Oil karite (Shea butter)1,0
Tocopherylacetate0,25
OSH0,1
Dimethicone2,0
Cyclohexasiloxane; Cyclopentasiloxane2,0
Glycerides of coconut oil; DISTEARYL ether; literallayout; literallayout (self emulsifiable); ministerului alcohol; stearyl alcohol1,5
Phenoxyethanol0,6
Ethylparaben0,15
Propylparaben0,15
Polyacrylamide, C13-14 isoparaffin; Laureth-7; water2,0
Hydroxyphenylpropionic acid; butyleneglycol; pentilenglikol1,0
Nylon-123,0
Hyaluronic acid; water0,1
Ascorbic acid0,05
Retinol0,115
Polysorbate 20is 0.135
Sodium hydroxide0,0277

The composition specified in Table 2, were prepared as follows.

Aqueous phase: mixed water, disodium etc and a copolymer of acryloyldimethyltaurate ammonia/methanol. Then added glycerin and butyleneglycol.

A mixture of 1: mixed dihydroxyethane with PEG-8, the resulting mixture was heated to 80°C and kept for 10 minutes and then allowed to cool.

Fatty phase: mixed Cetearyl alcohol, ceteareth-20, stearyl alcohol, ceteareth-20, ethylhexylacrylate, GPR-15 stearyl ether, isohexadecane, pentaerythritoltetranitrate, oil karite (Shea butter), tocopherylacetate, OSH, Dimethicone, glycerides of coconut oil, DISTEARYL ether, literallayout, self emulsifiable literallayout, ministerului alcohol, stearyl alcohol, Phenoxyethanol, ethylparaben, propylparaben, and hyaluronic acid.

Emulsion: the aqueous phase is added to the fatty phase. At a temperature of 75°C was added polyacrylamide, C13-14 isoparaffin, Laureth-7, cyclohexasiloxane and Cyclopentasiloxane. The resulting mixture was cooled to 30°C, then added the powder components: Nylon-12, hydrox phenylpropiophenone acid, ascorbic acid, retinol and odorant and adjusted the pH of the mixture with sodium hydroxide. Then added a previously prepared Mixture of 1.

Example 2. The impact of water softeners on the rate of release of retinol

Compositions with different rates of release of retinol in vitro prepared by changing the weight ratio of polar and non-polar softener in the composition. This was achieved by solubilization of retinol in a mixture of two softeners different polarity: BCP-15 stearyl ether having a relative index polarity to retinol, is equal to 1 (i.e. which has the same polarity as retinol), and isohexadecane having a relative index polarity to retinol, equal 9,11. Total concentration of softeners in each composition was 7%; however, their ratio varied depending on the composition. The composition of the prepared compositions (compositions A-E) are shown in Table 4.

td align="justify"> 1
Table 4
Composition (wt%, ROL 0,1%)
ComponentABCDE
In the Yes Dost. QtyDost. QtyDost. QtyDost. QtyDost. Qty
Carbomer0,40,40,40,40,4
Disodium add0,10,10,10,10,1
Methylparaben0,20,20,20,20,2
Propylparaben0,150,150,150,150,15
Phenoxyethanol0,50,50,50,50,5
Sodium hydroxide1111
Literallayout; PEG-100 stearate22222
OSH0,10,10,10,10,1
Cetyl alcohol11111
Isohexadecane01,753,5the 5.257
BCP-15 stearyl ether7the 5.253,51,750
Retinol0,1150,1150,1150,1150,115
Polysorbate 20is 0.1350,13 is 0.135is 0.135is 0.135
Ascorbic acid0,050,050,050,050,05

In vitro rate of release of retinol from compositions A-E are given in Table 5. Speed was determined by measuring the diffusion of retinol through soaked maritimerelated porous membrane of cellulose acetate, mounted in the diffusion cell Franz. The diffusion of retinol through the membrane into the receiving fluid was observed within 24 hours. The rate of release of retinol from the composition was calculated in units of μg/cm2/hour.

Table 5
The rate of release of retinol
(μg/cm2/hour)
Composition A1,395
Composition Bto 1.767
Composition C2,502
Composition Dof 2.514
Composition E 3,802

Example 3. The effect of the rate of release of retinol to retinol activity

Prepared additional composition (composition F-H). Amount of retinol in each composition was chosen so that each of the composition for 24 hours did the same amount of retinol, but with different speeds. The compositions F-H are shown in Table 6.

Table 6
Retinol
(wt%)
BCP-15 stearyl ether
(wt%)
Isohexadecane
(wt%)
The ratio of softeners
(non-polar/polar)
Composition F0,115%0%7%7/0
Composition G0,226%3,5%3,5%1/1
Composition H0,306%7%0%0/7

The activity of retinol was measured by determining the level of expression of the two meters is kernich genes associated with the activity of retinol in the epidermis: heparin-binding epidermal growth factor (HB-EGF) and cellular protein that binds retinoic acid, type 2 (CRABP2). Inflammatory effects of retinol was measured by determining the level of expression of the marker sub-chronic skin inflammation, interleukin 8 (IL8). Composition F-H were applied to the explants of human skin for 24 hours, and then measured the levels of expression of these genes in the epidermis by way of quantitative PCR.

As shown in figa and 2B, measured in the Explant model of human skin activity of retinol was higher for compositions with a lower rate of release of retinol. The highest activity of retinol was observed for the composition H.

As shown in figure 3, the potential caused by retinol irritation was higher than for a product with a higher rate of release of retinol. The highest potential caused by retinol irritation was observed for the composition F.

The tolerability profiles for compositions F-H were determined from the results of the multiple allergic skin samples from 60 volunteers. Conducted the test was repeated application of the investigated compositions under semi-hermetic patch three times a week during a three-week study. After removal of the patch was determined by the degree of redness of the skin (the index mRIPT). After three weeks all the indexes redness summarized, getting the final index redness.

The results are shown in Table 7. Compositions with lower rate of release of retinol showed better tolerability profiles.

Table 7
Index redness (MRIPT)
Composition F443
Composition G70,5
Composition H69,5

1. Natoora cosmetic composition type emulsion oil-in-water containing (i) retinol, (ii) at least one polar softener selected from the group consisting of stearyl ether of propylene glycol, isostearate propylene glycol and mixtures thereof and (iii) at least one non-polar softener selected from the group consisting of aromatic or linear esters, ether Emblem, mineral oil, squalane, isohexadecane, squalene, liquid paraffin and mixtures thereof, and the weight ratio mentioned polar softener and the above-mentioned non-polar softener is in the range from about 95 to 5 to arr is siteline 40 to 60.

2. The composition according to claim 1 where the above-mentioned non-polar softener selected from the group consisting of isohexadecane, squalane, and mixtures thereof.

3. The composition according to claim 1 where the above-mentioned polar softener selected from the group consisting of BCP-15 stearyl ether, isostearate propylene glycol and mixtures thereof.

4. The composition according to claim 1, where the weight ratio mentioned polar softener to the mentioned non-polar the softener is in the range of from about 85 to 15 to approximately 50 to 50.

5. The composition according to claim 1, where said composition comprises from about 0.001 wt.% to about 2 wt.% mentioned retinol.

6. The composition according to claim 1, where said composition comprises from about 0.1 wt.% to about 50 wt.% mentioned non-polar and polar softeners or from about 1 wt.% to about 40 wt.% mentioned non-polar and polar softeners.

7. The composition according to claim 1, where said composition contains from about 0.02 wt.% up to about 0.5 wt.% mentioned retinol and from about 2 wt.% to about 25 wt.% mentioned non-polar and polar softeners.

8. The composition according to claim 1, additionally containing from about 0.001 wt.% to about 10 wt.% one or more cosmetically active substances, selected from the group consisting of proteomically the substances, anti-inflammatory substances that slow down the aging agents, antioxidants, keratolytic agents, vitamins, minerals, energy supplements, pH correctors, and mixtures thereof.

9. Composition according to any one of claims 1 to 8 for use in the treatment of acne by topical application on the skin, in need of such treatment.

10. The use of a composition according to any one of the preceding paragraphs for a local cosmetic use on skin.

11. The use of claim 10 to reduce the severity of wrinkles, fine mesh, stretch marks or cellulite.



 

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EFFECT: group of inventions enables applying the composition for non-therapeutic disinfection, in treating skin infections.

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to dentistry and may be used for making hygienic and therapeutic products for daily dental and oral care, namely to mouth rinses. A mouth rinse formulation contains troxerutin 0.1-0.3 wt % in a combination with ectoin 0.01-1.0 wt %, nicotinamide 0.05-0.1 wt % and a complex of bisabolol and ginger extract 0.01-0.03 wt %, as well as a cosmetically acceptable base containing a water-retaining additive, a structure-forming agent, a filming agent, an anti-caries additive, a flavouring agent and a target additive in the amounts to provide performing the above functions, a biologically active additive consisting of Aloe Vera and herbal infusion, while a medium is water.

EFFECT: formulation provides the effective repair action on the periodontal tissues and high cleansing properties when using the mouth rinse.

14 cl, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetology and represents a sun-protection cream consisting of aqueous-alcohol extract of grape skins, CO2-extract of grape skins, olive oil, isopropyl myristate, higher synthetic primary fatty alcohols C16-C20 fraction, polyethylene glycol-400 stearate, bee wax, glycerol, stearine, triethanolamine, benzyl alcohol, a preserving agent, a flavouring agent and water with the ingredients of the cream are found in certain proportions, wt %.

EFFECT: invention provides a higher rate of sun-protective action of the sun-protection cream.

4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetic industry and represents an oil-in-water emulsion composition for UV protection, containing: (a) octocrylene, (b) bis- ethylhexyloxyphenol methoxyphenyl triazine, (c) hexyldiethylamino-hydroxybenzoyl benzoate, (d) 4-tert-butyl-4'-methoxybenzoyl methane, wherein the amount of the ingredients (a), (b), (c) and (d) makes 1 - 40 wt/wt %, (e) a water-soluble polymer in the amount of 0.01-5 wt/wt %, (f) a water-swellable clay mineral in the amount of 0.01-4 wt/wt %, (g) an oil ingredient having NOB 0.05 or more in the amount of 1 - 70 wt/wt %, (h) a higher fatty acid in the amount of 0.1-10 wt/wt %, (i) a surfactant in the amount of 0.1-10 wt/wt %, (j) water - the rest, wherein all the amounts are presented as a percentage of the total amount in the oil-in-water emulsion composition.

EFFECT: invention provides developing the composition having the good UV protection effect, exhibiting the emulsion stability and pleasant sensation.

6 cl, 8 ex, 4 tbl, 1 dwg

FIELD: medicine.

SUBSTANCE: invention refers to cosmetology and represents a cosmetic product for face and body skin care containing a basic component presented by dry feed rye spent wash with syrup, as well as at least one paste-forming component specified in a group: water, liquid soap and optionally at least one component specified in a group of: sugar-free cultured milk product, rye flour, vegetable oil, honey.

EFFECT: invention provides preparing the high efficacy natural dry cosmetic product for face, hand and body skin cleansing, nourishment and regulation.

7 cl, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: claim describes a cosmetic or dermatological composition in the form of cream, foam, spray, gel, gel spray, lotion, oil, oil gel or mousse. The composition contains at least one active substance, at least one molecular imprinted polymer in the presence of the same active substance, and at least one oil phase. The polymer contains a) a monoethylene-saturated mono- or dicarboxylic acid or α,β-ethylene-unsaturated mono- or dicarboxylic acid esters with diols and b) methacrylic acid esters of at least dihydric alcohols. The molar ratio of the compounds a) and b) makes 1:2 to 1:4, and the polymer is prepared in the medium of a solvent wherein monomers, but not the polymer to be prepared is dissolved in the presence of the active substance.

EFFECT: combination of the molecular imprinted polymer prepared by precipitative polymerization, and the oil phase provides the release of the active substance both in the water phase, and in the oil phase which ensures the best contact with a lipophilic surface, such as skin.

3 cl, 3 dwg, 7 tbl, 37 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a polyphenol derivative formulation and is used in cosmetics, nutrition science and therapy. The polyphenol derivative formulation possessing antioxidant and antiradical activity and having an effect on carbonyl stress. A method for preparing the formulation. The cosmetic formulation possessing antioxidant and antiradical activity and having an effect on carbonyl stress. Using the formulation in nutrition science. The formulation to be used as a therapeutic agent possessing antioxidant and antiradical activity and having an effect on carbonyl stress. The pharmaceutical formulation possessing antioxidant and antiradical activity and having an effect on carbonyl stress.

EFFECT: formulation has an effect on carbonyl stress.

23 cl, 11 dwg, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetology and represents an oil-in-water emulsion sun-protection cosmetic composition containing: (A) 1 to 7.5 wt % of octyl methoxycinnamate; (B) 1 to 4 wt % of tret-butyl methoxydibenzoyl methane and/or 2-hydroxy-4-methoxybenzophenone; (C) 0.5 to 3 wt % of a polyoxyethylene/polyoxyalkylene alkyl ester block copolymer; (D) 10 wt % or more of a nonpolar oil relative to the total amount of the oil component; wherein an average emulsion particle diameter makes not more than 700 nm.

EFFECT: invention provides developing the stable sun-protection composition having improved ultraviolet blocking capability and good usability.

4 ex, 4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely a method of treating acne. The method of treating acne by prescribing line seed oil 10 ml 2 times a day, sodium selenite 90 mcg 1 time a day, tocopherol acetate 100 mg 2 times a day for 1 month.

EFFECT: method of treating acne is effective and enables reducing the length of treatment.

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetology and dermatology, and represents a water-based formulation for local application for treating acne, containing water, a water-miscible organic solvent and benzoyl peroxide, wherein the organic solvent concentration is 1-4 times higher than the benzoyl peroxide concentration in the formulation; the water and organic solvent concentrations are related as at least 7:1, preferentially at least 10:1, more preferentially at least 20:1; the benzoyl peroxide concentration in the formulation makes less than 5.0 wt %, but at least 1.0 wt %.

EFFECT: invention provides the clinical effectiveness with the reduced active agent concentration, as well as reduced irritant action.

27 cl, 4 ex, 3 tbl

FIELD: medicine.

SUBSTANCE: invention refers to cosmetology and represents a cosmetic composition containing: hydrolised yeast proteins as an active substance, and at least one acceptable carrier, differing by the fact that the above hydrolised yeast proteins are prepared by exogenic enzymatic hydrolysis and/or acid hydrolysis and/or alkaline hydrolysis of the yeast membranes.

EFFECT: invention provides improved cosmetic activity, excellent time stability.

17 cl, 6 ex, 3 tbl, 2 dwg

FIELD: medicine.

SUBSTANCE: invention refers to medicine, specifically to dermatology, and may be used for treating the patients suffering acne. That is ensured by local applications of a therapeutically effective amount of a fixed-dose combination containing adapalene and benzoyl peroxide. That is combined with oral administration of a therapeutically effective amount of an antibiotic for a particular period of time.

EFFECT: method provides the effective treatment of these patients, manifested as a significant decrease of all types of acne involvements, prevents the further development of these involvements, including after the withdrawal of oral antibiotics and the development of resistance, due to the synergistic effect of the above local combination and oral antibiotic.

11 cl, 11 tbl, 4 dwg, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and cosmetics, more specifically to a topical pharmaceutical composition possessing comedolytic and antibiotic action, comprising an effective amount of the antibiotic clindamycin, salicylic acid and excipients. The pharmaceutical composition is presented in the form of a gel. The excipients are as follows: acrylate copolymer emulsion Salcare SC80, allantoin, antioxidant dihydroquercetin preservative Sharomix MCI, propylene glycol, cyclomethicone DC 345, tocopherol phosphate, UV filter Escalol 567, emulsifier DC 5329, trometamol and thermal water.

EFFECT: stabilised composition has strong comedolytic and antibiotic action, comprises the protective SPF factor which protects inflamed skin against the negative effects of UV radiation and has a shelf life of at least 3 years.

3 ex, 4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of pharmaceutics and represents application of composition, including adapalene and benzoyl peroxide, in preparation of local medication, intended for application by patient who requires it to provide long-term treatment of acne vulgaris, where scheme of application of local medication includes application of therapeutically efficient quantity of composition for, at least, 9 months.

EFFECT: invention ensures achievement of stable positive effect in long-term treatment of acne with composition, including adapalene and benzoyl peroxide, as well as absence of side effects.

19 cl, 1 ex, 3 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of dermatology and represents application of 1-aminoalkylcyclohexane derivative, selected from neramexane and its pharmaceutically acceptable salts for treatment or prevention of inflammatory skin diseases, which represent acne, irritant dermatitis, impetigo and atopic dermatitis.

EFFECT: invention ensures extension of arsenal of medications for treatment of inflammatory skin diseases.

39 cl, 7 ex, 35 tbl, 5 dwg

FIELD: medicine.

SUBSTANCE: invention relates to medicine, particularly to dermatology, more specifically to methods of treating pyoinflammatory skin diseases, particularly furunculosis and acne. The method of treating the patients suffering pustular skin disorders, according to the invention, consists in the fact that the affected and surrounding skin areas are prepared with warm weak antiseptic, dried and further processed with an ointment prepared by thorough mixing on a water bath until smooth: zinc-salicylic paste, Lorinden C, gioxizone, streptocide liniment, synthomycin liniment and retinol acetate in the ratio of 3÷1÷1÷1÷0.8÷0.1 with skin treatment produced 2 times a day. The weak antiseptic is sodium bicarbonate or chamomile infusion at temperature 40-45°C. Besides, water bath temperature is to be 40-50°C, and the ointment is to be prepared is a glass or ceramic container. Face acne requires the affected area to be warmed with a vapour bath before finally applying the ointment. To prevent accidental wipe-out of ointment from the ointment treated skin, it is covered with the napkins attached to healthy skin. To enhance the effect of the ointment applications, the affected skin is exposed to UV lamp and/or sunlight for 10-30 minutes.

EFFECT: method enables faster treatment and prevented the recurrent disease, and also ensures the prevention of side effects and provides outpatient treatment.

6 cl, 7 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetology and dermatology and represents a composition for treating dermatological disorders containing in a physiologically acceptable medium, at least: (i) peroxide benzoyl, (ii) a naphthoic acid derivative specified in 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid, 6- [3-(1-adamantyl)-4-hydroxyphenyl]-2-naphthoic acid, 6-[3-(1-adamantyl)-4-decyloxyphenyl]-2-naphthoic acid and 6-[3-(1-adamantyl)-4-hexyloxyphenyl]-2-naphthoic acid and (iii) a compound of polyurethane polymer representing a polyol pre-polymer with said naphthoic acid derivative and said benzoyl peroxide being found in the dispersed form in said composition.

EFFECT: invention provides producing a non-irritant stable composition.

25 cl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to chemical-pharmaceutical industry, and concerns preparing an agent for treating various dermatopathies: psoriasis, eczema, atopic dermatitis, ulcers incl. trophic and other diseases accompanied by inflammation or skin flaking. According to the first version, the composition contains ethoxylated alcohol, glycerol monostearate, higher fatty alcohols C16-C18 and cocoglycerides, as well as glycerol, olive oil and water. According to the other versions, it contains naphthalan oil or pentoxifylline or urea. All the versions provide a liposomal form of the composition improving healing, soothing and trophic effects.

EFFECT: composition is hypoallergic, easy-to-use.

12 cl, 8 ex

FIELD: chemistry.

SUBSTANCE: surface lustre enhancing composition contains a pigment particle which is pre-coated with a cationic substance in amount of 0.1-10 wt % and isopropyl titanium triisostearate. The cationic substance is a substance selected from a group comprising quaternium, polyquaternium and a cationic polymer.

EFFECT: invention increases lustre of a surface on which a cleaning composition is deposited owing to retention, on the surface, of a pigment capable of increasing lustre.

16 cl

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