BG2764U1 - Cosmetic composition containing benzoyl peroxide - Google Patents

Abstract

So far, there have not been known cosmetic compositions containing Benzoyl peroxide with a concentration below 0.7%. The present utility model relates to a stable cosmetic composition comprising Benzoyl peroxide, at least one gel-forming agent of the group of acid-dependent, acid-independent or a mixture thereof; at least one solvent which is water and/or at least one organic solvent of the glycol group; at least one wetting agent; at least one chelating agent and at least one supplement. The cosmetic product, subject to this utility model, is intended for daily use by adolescents and adults with oily, sensitive and acne-prone skin or mild acne, as well as after treatment of severe forms of acne. The product has antibacterial and anti-inflammatory action. It can prevent the formation and progress of inflammatory processes and reduce comedones.

Description

(54) COSMETIC COMPOSITION CONTAINING BENZOYL PEROXIDE (57) To date, no cosmetic compositions containing Benzoyl peroxide with a concentration below 0.7% are known. The present utility model relates to a stable cosmetic composition comprising Benzoyl peroxide, at least one gel-forming agent from the group of acid-dependent, acid-independent or a mixture thereof; at least one solvent which is water and / or at least one organic solvent from the group of glycols; at least one wetting agent; at least one chelating ingredient and at least one additive. The cosmetic product subject to this utility model is intended for daily use by adolescents and adults with oily, sensitive and prone to acne skin or mild forms of acne, as well as after treatment of severe forms of acne. The product has antibacterial and anti-inflammatory action. It can prevent the occurrence and development of inflammatory processes and reduce comedones.

claims

2764 UI (54) COSMETIC COMPOSITION CONTAINING BENZOIL PEROXIDE

Field of technology

The present utility model relates to a stable cosmetic composition containing benzoyl peroxide.

The composition is intended for application on oily, sensitive and acne-prone skin, for mild forms and / or after treatment of severe forms of acne.

BACKGROUND OF THE INVENTION

Acne is a skin disease caused by the bacterium Propionibacterium acnes, which manifests itself in the appearance of clogged pores, blackheads - comedones, red pimples with purulent tips, impaired skin integrity, hyperpigmentation.

The treatment of this unpleasant disease is difficult and long depending on the depth of the disease. In addition to oral therapy, the most commonly used therapy is the superficial treatment of the affected areas of the skin on the face and body with topical medications. Medicinal products containing benzoyl peroxide with an active substance concentration of 2.5 to 10.0% are known. It is present in them alone or in combination with another active substance, which is most often an antibiotic or retinoid. Combination preparations with antibiotics include: Erythromycin, Clindamycin, Lincomycin, and those with Retinoids-Tretinoin and Adapalene.

The effectiveness of benzoyl peroxide is related to its decomposition on contact with the skin and in particular to the oxidizing properties of the free radicals that are released during its decomposition. It is important to maintain the high efficiency of the active substance and its stability during storage.

Benzoyl peroxide is one of the most powerful means of combating acne, but its high concentration and long-term use often leads to unwanted side effects such as: irritation, redness, flaking, burning.

A stable composition containing benzoyl peroxide can be obtained if the following are overcome:

- the highly irritating effect of benzoyl peroxide on the skin, which is directly dependent on its concentration and particle size (Mills et all '' International Journal of Dermatology, 25 (10): 664-667 (1986); Lassus' Current Medical Research and Opinion, 7 (6): 370373 (1981);

- its instability in the dissolved state.

Schwarz (US 7153888) and De Villez (US 4923900) found that benzoyl peroxide in dissolved state causes little or no skin irritation. It is dissolved with organic solvents, which are mixed with water by adding antioxidants to improve its stability. The disadvantage of this formulation is the use of a large amount of solvent, which is 10-15 times more than benzoyl peroxide and, in addition to irritating the skin, dries it due to the dissolution of skin lipids.

Chang and Dow by DowPharm. Sciences Inc (US 2014 0134252) reduced the amount of solvent used and micronized benzoyl peroxide to 2.5 to 30 μ. Their clinically tested formulations contain 1.2% clindamycin phosphate, and the best formula contains 3.75% benzoyl peroxide. The results of the studies showed side effects from 22 to about 27% such as: redness, burning, burning.

Benzoyl peroxide solubility studies have been published by Chellquist EM and Gorman W. G (Chellquist EM and Gorman WG, Pharm. Res., 1992, Vol. 9, 1341-1346), according to which benzoyl the peroxide is dissolved only in polyethylene glycol 400, ethanol and propylene glycol. However, the stability of these solutions at a concentration of 0.5 mg / g at 40 ° C lasts 1.4 respectively; 29 and 53 days.

All attempts to obtain stable benzoyl peroxide solutions have failed. Many years of experimentation have led to the conclusion that the best, stable composition is obtained if the active substance is in the form of a suspension.

However, obtaining a stable suspension has faced new challenges for researchers due to the possibility of unwanted sedimentation, stratification, uneven distribution or oxidative processes associated with premature oxygen release.

2764 IU of benzoyl peroxide.

Particle size is one of the important characteristics for its good tolerability by the skin due to the possibility of its irritation due to a local high concentration of the active substance.

Chris Gerlach and Mike Davis of Essential Ingradients Inc (US 20140161853) reduce the irritability of benzoyl peroxide by grinding it with water to a size <25 microns without the use of an organic solvent. Studies of their products show stability under accelerated aging at 40 ° C / 75% RH.

From the above it can be concluded that side effects are most often associated with high concentrations of benzoyl peroxide.

The cosmetic composition presented by us contains a low concentration of the active substance, in accordance with the requirements of the European regulatory system for cosmetic products.

The cosmetic product, subject to this utility model, is intended for daily use by adolescents and adults with oily, sensitive and prone to acne skin or mild forms of acne, as well as after treatment of severe forms of acne. The product has antibacterial and anti-inflammatory action. It can prevent the occurrence and development of inflammatory processes and reduce comedones.

Technical essence of the utility model

The technological processes for obtaining the cosmetic composition, subject of the present utility model are the following:

Step 1: In a 50 ml container, measure the required amounts of Water, Propylene Glycol, Sodium docusate. The mixture is stirred with a mechanical or magnetic stirrer until the sodium docusate is completely dissolved.

Step 2: To the resulting clear solution from step 1 was added the sieved and weighed Benzoyl peroxide. Stirring is continued for 0.5 to 1.0 h.

Step 3: Place the required amount of Water in a 150 ml vessel and add Ethylenediamine Tetraacetate Disodium Salt and Panthenol in succession with stirring with a mechanical stirrer.

Step 4: Gelling and thickening agents are added to the clear solution of step 3.

Step 5: The resulting viscous mass from step 4 is mixed with the suspension from step 1 and the mixture is stirred until it is completely homogenous.

General description of the utility model

The aim of the present utility model is to obtain a cosmetic composition with a low content of Benzoyl peroxide, having high stability.

No cosmetic products containing Benzoyl peroxide are known in the amount provided for in Regulation 1223/2007 of the European Community, which according to the Annex to the same Regulation is not more than 0.70%.

The active component of the cosmetic composition is Benzoyl peroxide with a concentration in the range of 0.10 to 0.70% by weight of the total composition. It is good to be in the range: from 0.20 to 0.60% and preferably from 0.50 to 0.65%.

Granular or powdered Benzoyl peroxide was used, which was ground and sieved before use through a sieve measuring 0.025 mm to 0.100 mm to ensure approximately uniform particle size and uniform distribution in the suspension.

The main solvent in the cosmetic composition is Water, and Benzoyl peroxide is insoluble in it.

An important part of obtaining a stable suspension is finding a suitable wetting agent to aid in the absorption of the solid component from the liquid phase. The role of wetting agents is to reduce the surface tension and to ensure the placement of liquid over a wide area of the surface of the solid particles.

The wetting agents in our composition may be at least one representative of the glycol groups such as: propylene glycol, dipropylene glycol, lauro glycol, ethoxydiglycol, anionic wetting agents such as sodium docusate or nonionic wetting agents such as polyoxyethyl / polyoxypropyl.

Our preferred wetting agents, without limitation, are a mixture of Propylene Glycol and Sodium docusate.

The total amount of wetting agents

2764 UI is in the range of 0.10 to 15.0%, preferably 1.0 to 10.0%, and most preferably 3.0 to 7.0%.

The gel-forming component in the cosmetic composition may be a polymer whose viscosity is dependent on or independent of the acidity of the medium.

Acid-independent polymers do not change their viscosity when the pH of the medium changes and retain their viscosity. Such agents may be among Acrylic Acrylate cross-linked polymers; Polysaccharides; Cellulose; Aluminum magnesium silicates.

Some of the representatives of cellulose derivatives are: Carboxymethyl cellulose; Hydroxyethyl cellulose; Hydroxypropyl methyl cellulose, anapolysaccharides: Xanthan gum, Guar gum, Pectin. Each of these gelling agents may be used in our composition alone or in admixture with a member of the same group or another group of compounds.

Environmentally dependent polymers such as Carbomer 940 (polyvinyl carboxy polymer cross-linked to pentaerythritol ethers) usually achieve the desired viscosity after neutralization with alkaline agents, which may be inorganic or organic bases such as metal hydroxides, ammonium hydroxide and alkyl alkyl. - primary, secondary and tertiary as well as amino acids.

The amount of gelling agent is in the range of 0.1 to 10.0%, preferably 0.5 to 8.0, and most preferably 1.0 to 5.0%, and the amount of the thickener from the group of polysaccharides of 0.01 to 1.00, preferably 0.05 to 0.50 and most preferably 0.10 to 0.30% of the composition of the whole mixture.

The chelating ingredient may be Ethylenediamine tetraacetic acid or its Disodium salt. The amount of the ingredient is in the range of 0.01 to 0.50, preferably 0.05 to 0.10% of the total composition of the mixture.

The additives in our cosmetic composition are emollient, moisturizing ingredients such as Panthenol and Glycerin.

The healing effect of Panthenol on the skin is known. Its presence in the cosmetic composition developed by us together with Glycerin contributes to the rapid healing of damaged skin, its softening and moisturizing. For the purposes of the utility model, Panthenol or Dexpanthenol can be used alone or in a mixture with Glycerin in amounts sufficient to achieve the desired effect, which in total are from 1.0 to 20.0%, it is good to be from 2.0 to 15 , 0 or preferably from 3.0 to 10.0%.

Detailed description of the utility model

The main achievement of the present utility model is the creation of a stable cosmetic composition containing not more than 0.70% Benzoyl peroxide.

The amount of active ingredient in the cosmetic product is defined in Regulation (EC) No 1223/2007 of the European Communities.

The cosmetic composition we offer is a suspension of solid particles evenly distributed in the mixture of the other components. For this purpose, it is important to find suitable wetting agents in the necessary, sufficient amount to obtain a smooth, soft and pleasant to use mixture containing the active substance. From the wetting agents we have chosen a representative from the group of glycols and in particular: propylene glycol, as well as an anionic wetting agent such as: sodium docusate. We found the best ratio between them and Benzoyl peroxide after a series of experiments with different ratios.

We achieved the best total amount of wetting agents in the range of 3.0 to 7.0%.

To obtain a stable composition, we used gelling agents from different groups of compounds.

One of the groups of gel-forming compounds are acid-dependent compounds whose viscosity and stability strongly depend on the pH of the medium. Representative of this group of compounds is: Carbomer 940 (polyvinyl carboxy polymer cross-linked to pentaerythritol ethers).

One of the claims of our utility model is to obtain a stable composition with a representative of this group of compounds, the viscosity of which we controlled by neutralization with dilute solutions of inorganic bases such as: Sodium hydroxide, Potassium hydroxide, Calcium hydroxide and organic bases such as: Triethanol amine, triethyl amine, diethyl amine, ethyl amine Trimethyl amine, dimethyl amine, methyl amine, benzyl methyl amine.

2764 UI

Our preferred neutralizing component is triethanolamine, due to the absence of metal ions and its ability to neutralize the polymer without the need for large amounts of it.

The dissolution of the gelling agent was carried out in the temperature range from 25 to 80 ° C and in particular in the range from 25 to 60 ° C depending on the solubility of the particular polymer.

Another achievement of the present utility model is the preparation of a stable cosmetic composition with acid-independent gelling agents such as: Acrylic Acrylate cross-polymers, Polysaccharides, Celluloses, Aluminum-magnesium silicates.

Representatives of the Cellulose group are: Hydroxy propyl methyl cellulose, Ethyl cellulose, Hydroxy ethyl cellulose, and those of the polysaccharides are: Xanthan gum, Guar gum, Pectin.

Our preferred combination of gel-forming and thickening component is Hydroxy propyl methyl cellulose and Xanthan gum.

Satisfactory consistency density was achieved with amounts of the gel-forming ingredient from 0.1 to 5.0% of the total composition and thickeners from 0.1 to 3.0%.

One of the advantages of the cosmetic composition created by us with acid-independent gel-forming component is that all components involved in it provide a pH of about 5.5-6.5 and it does not require the introduction of inorganic or organic bases to correct the acidity of the environment. .

An important component of the cosmetic composition is the supplement that promotes rapid healing of damaged skin, representatives of which are: Panthenol, Dexpanthenol and Natural herbal extracts.

The moisturizing, softening and soothing effect of the skin was achieved with the combination of Panthenol and Glycerin, the total amount of which is from 1.0 to 20.0%, preferably from 2.0 to 15.0%, most preferably from 3.0 to 10 , 0% of the total composition of the mixture.

The chelating ingredient was selected from Ethylenediaminetetraacetic acid, Ethylenediamine dihydroxyacetic acid, Hydroxyethyldiamino trioacetic acid, Ethylenediamine (o-hydroxy-p-methyl) phenyl acetic acid and their salts. Its amount varies from 0.01 to 0.50, preferably from 0.05 to 0.10% of the total composition of the mixture.

We achieved high microbiological stability due to the antimicrobial properties of Benzoyl peroxide and Hydroxypropylmethyl cellulose. Microbiological analysis for the content of: molds, yeasts, Escherichia coli, Staphylococcus aureus, Candida albicans, Psedomonas aeroginosis, shows their complete absence in batches, stayed 3 months in conditions of long-term stability.

No additional introduction of any preservatives is required to obtain high microbiological quality.

Examples of implementation of the utility model

Example 1. Cosmetic composition with acid-dependent gelling agent Carbomer 940.

Composition % y / y Water up to 100 Panthenol 5.0 Propylene glycol 3.0 Glycerin 7.0 Carbomer 940 1.5 Benzoyl peroxide 0.7 Disodium edetate 0.05 Sodium is added 0.01 Sodium hydroxide -pH - 5.5-6.5

2764 UI

Physical and chemical stability at 25 ° C / 60% RH

Indicators and norms Storage time (month) 0 1 2 Appearance White, soft, gel-like mass Answer Answer Answer pH 5.5-6.5 5.56 5.00 5.45 Related substances -benzoic acid <1.5% -any other impurity ^ 0.25% - total impurities <2.0% 0 0 0.01 0.01 0 Quantitative content of benzoyl peroxide - 0.665% - 0.700% 0.693 0.690 0.689

Example 2. Cosmetic composition with mixed gel-forming agents - acid-dependent and acid-independent

Composition % y / y % y / y % y / y % y / y % y / y Water up to 100 up to 100 up to 100 up to 100 up to 100 Panthenol 5.0 5.0 5.0 5.0 5.0 Propylene glycol 4.0 4.0 4.0 4.0 4.0 Glycerin 4.0 4.0 4.0 4.0 4.0 Carbomer 940 0.5 0.2 0.1 0.3 0.3 Hydroxypropylmethyl cellulose 0.5 0.8 0.7 0.7 1.2 Benzoyl peroxide 0.7 0.7 0.7 0.7 0.7 Disodium edetate 0.1 0.1 0.1 0.1 0.1 Sodium is added 0.05 0.05 0.05 0.05 0.05 Sodium hydroxide 5.5-6.5 5.5-6.5 5.5-6.5 5.5-6.5 5.5-6.5

2764 UI

Physical and chemical stability at 25 ° C / 60% RH

Indicators and norms Storage time (month) 0 1 2 Appearance White, soft, gel-like mass Answer Answer Answer pH 5,, 5-6.5 5.46 5.40 5.45 Related substances -Benzoic acid <1.5% -every other impurity 0.25% - total impurities ^ 2.0% 0 0 0 0.01 Quantitative content of Benzoyl peroxide (C14H10O4) - 0.665% - 0.700% 0.687 th most common 0.685 0.685

Example 3. Cosmetic composition with an acid-independent gelling agent

j Composition % y / y Water up to 100 Panthenol 5.0 Propylene glycol 4.0 Glycerin 4.0 Hydroxypropylmethyl cellulose 2.5 Benzoyl peroxide 0.7 Sodium edetate 0.1 Sodium is added 0.05 Sodium hydroxide - pH - 5.5-6.5

2764 UI

Physical and chemical stability at 25 ° C / 60% RH

Indicators and norms Storage time (month) 0 1 2 Appearance White, soft, gel-like mass Answer Answer Answer pH 5.5-6.5 5.56 5.50 5.45 Related substances -benzoic acid ^ 1.5% -every other impurity <0.25% - total impurities <2.0% 0 0 - ' 0 0 Quantitative content of Benzoyl peroxide (C14H10O4) - 0.665% - 0.700% 0.689 0.685 0.680

Example 4. Cosmetic composition with a mixture of acid-independent gelling agent and thickener of the mixture from the group of polysaccharides.

Composition % y / y Water up to 100 Panthenol 5.0 Propylene glycol 4.0 Glycerin 4.0 Hydroxypropylmethyl 2.0 cellulose Xanthan gum 0.2 Benzoyl peroxide 0.7 Disodium edetate 0.1 Sodium docusate - 0.05 Sodium hydroxide - pH - 5.5-6.5

2764 UI

Physical and chemical stability at 25 ° C / 60% R.H

Indicators and norms Storage time (month) 0 1 2 3 6 Appearance White, soft, gel-like mass Answer Answer Answer Answer Answer pH 5.5-6.5 5.56 5.60 5.40 5.30 5.50 Related substances -benzoic acid <1.5% -every other impurity £ 0.25% - total impurities <2.0% 0 0 0 0 0 0 0 0 0 0 Quantitative content of Benzoyl peroxide (C14H10O4) - 0.665% - 0.700% 0.698 0.675 0.680 0.685 0.688

Application of the utility model

The present utility model presents an industrially applicable method and composition for the preparation of a stable cosmetic composition for topical application in children and adults. The low content of the active substance Benzoyl peroxide greatly reduces the appearance of unwanted side effects and allows to maintain clean and healthy skin. The combination of the antibacterial action of the active ingredient with the healing, emollient and moisturizing action of Panthenol provides the expected positive result from its application.

Claims (5)

Cosmetic composition containing benzoyl peroxide, characterized in that it contains the following components in concentrations expressed as a percentage by weight (g / g): water - with a concentration of 45.0 to 80.0%; benzoyl peroxide with a concentration of 0.1 to 0.7%; at least one wetting agent with a concentration of 0.1 to 15.0%; at least one gelling agent with a concentration of 0.1 to 10.0% at least one chelating ingredient with a concentration of 0.1 to 0.5% at least one additive with a concentration of 1.0 to 20.0% . Cosmetic composition according to claim 1, in which at least one of the wetting agents is from the group of glycols and / or anionic or nonionic surfactants. 5 A cosmetic composition according to claim 1, wherein the gel-forming component in the composition may be both pH dependent and pH independent, a combination of both or one of them and a thickener from the group of polysaccharides. A cosmetic composition according to claim 1, wherein the chelating ingredient is at least one of ethylenediamine derivatives and acetic acid. Cosmetic composition according to claim 1, in which panthenol is used as an additive.