LV14788B - Cream for prevention and treatment of facial skin xerosis - Google Patents

Abstract

Invention relates to compositions for taking care of the facial skin. The cream composition contains perhydrosqualene, alpha-tocopherol (vitamin E), selenomethionine, aloe vera extract, triglycerides of caprylic and capric acid, apricot oil, glycerol stearate, stearic acid, glycerol, cetyl alcohol, carbomer and distilled water. The cream prevents early occurence of xerosis, skin photoaging and improves its smoothness.

Description

DESCRIPTION OF THE INVENTION

The invention relates to cosmetology, in particular to therapeutic preventive skin care products.

TECHNICAL LEVEL

Irritable facial skin syndrome is known and occurs very commonly and is characterized by erythematous, erythematous-scaly and papular foci. One of the first signs of irritated facial skin is cutaneous xerosis. Skin xerosis is characterized by the following stages:

1) In the first stage, the skin of the face becomes dry and tight, these signs appear rapidly under the influence of ultraviolet (UV) radiation - photon aging of the skin,

2) in the second stage, epidermis exfoliation, formation of fine wrinkles,

3) in the third stage, changes in the dermis layer, facial skin appear stretched, bran scales appear, seborrheic signs and deep wrinkles in the eye area, on the nose, on the forehead (mimic activity zones), onset of pigmentation, inflammatory and vascular disorders.

Failure to prevent and treat facial xerosis results in signs of mature and aging facial skin: loss of turgor, deep wrinkles, skin loosening and flaking, increased pigmentation - dark / light spots, seborrheic manifestations - keratosis and dyskeratosis (severe peeling of the skin) , inflammatory and vascular disorders.

Known cosmetic compositions for the treatment of the first stage of xerosis - dry, contracted and photo-aging skin [1-3]. Known compositions contain extracts and herbal components in combination with various oils.

Known cosmetic compositions for treating the second stage of xerosis, epidermis exfoliation and fine wrinkle formation. The composition of the cream is known for the prevention and treatment of peeling of the epidermis of the skin and for the treatment of fine wrinkles [4]. V, propolis, vitamin B ₂ and fragrances.

Known cream composition for the prevention and treatment of fine facial wrinkles [5]. The cream contains DNM + cream base with eftiderm, calendula, kalanchoe, chamomile, ele-rococo, sage, copper and zinc ions, propolis, jojoba oil, wheat germ oil and avocado, aloe, bisabolol, collagen, horse chestnut and fragrance.

Known creams for the prevention and treatment of second-stage xerosis, which normalize and restore the skin, delay the aging process. However, the known compositions of the creams and the technology for their preparation are complex. Known creams require the MZUTS 300 mixer model.

Known cream composition for treating wrinkles. This composition contains a complex of selenium and vitamin E in nanoparticulate form [6]. The formulation of such a cream is difficult because the components of the cream are not compatible: selenium is a hydrophilic substance and vitamin E is a hydrophobic substance. The preparation of such an incompatible complex of nanoparticulate components requires special technology and special equipment.

Known cosmetic compositions for the prophylaxis and treatment of the third stage of xerosis, for the prevention and treatment of signs of seborrhea, deep wrinkles, changes in pigmentation, inflammation and vascular disorders. Known compositions contain plant alcohol extracts as whitening and exfoliating agents to smooth out wrinkles and whiten skin [7-101. Alcohol extracts of known compositions require sophisticated high temperature technology, filtration of mixtures and condensation of filtrates.

Known cosmetic compositions for the treatment of skin inflammation and vascular disorders [11, 12], Known compositions contain non-steroidal anti-inflammatory drugs, indomethacin in combination with copper and zinc complexes [11], or calendula extracts in combination with placenta [12].

In view of the widespread nature of facial xerosis, the development of an effective cream composition for the prevention and treatment of facial xerosis has become a pressing issue. In order to obtain an effective composition of the cream, it was desirable to include components that could penetrate (penetrate) into the deeper layers of the skin, which could promote the transfer of biologically active substances, the regeneration of epidermis structures and the lipid barrier. Based on these requirements, it became necessary to include both hydrophilic and hydrophobic components in the cream.

It is known that. during mixing, hydrophilic and hydrophobic substances are segregated. Under experimental conditions, it was necessary to find the composition of the components and their relationship, which would maintain the stability and biological activity of the components in the process of the process by obtaining a common mixture of hydrophilic and hydrophobic substances.

Disclosure of Invention

Objective and technical result of the invention:

• development of a composition capable of preventing the appearance of xerosis, premature aging of the skin, improving the micro-relief of the skin, • searching for new composition components and their relationship, • development of a simple cream preparation technology, • development of the optimal form of the cream.

The aim is achieved by the formulation of a cream containing perhydrosqualene, αΖ / α-tocopherol (vitamin E), selenomethionine, aloe, capric acid and caprylic triglycerides, apricot oil, glycerol stearate, stearic acid, glycerol, cetyl alcohol, carbomer g):

perhydrosqualene 10.0-15.0 a // h-tocopherol (vitamin E) 1.0-3.0 selenomethionine 0.05 - 0.5 aloe 23.0-25.0 triglycerides of capric acid and caprylic acid 12.2-13.4 apricot oil 5.7-6.3 glycerol stearate 4.0-4.4 stearic acid 0.8-0.9 glycerol 1,2-1,3 cetyl alcohol 1.6-1.8 carbomer 0.4-0.5 distilled water the rest of.

The composition of the cream consists of a homogeneous, white or white-yellow mass with a slight, pleasant smell corresponding to apricot oil. All components of the cream are authorized for pharmaceutical use.

The cream is intended to prevent the clinical manifestations and development of xerosis and irritated facial skin syndrome.

The cream contains the following components:

Perhydroqualene (Perhydro squalus) - a naturally occurring hydrocarbon belonging to the carotenoid group. Squalene - A colorless, viscous solution, freely soluble in ethers and in ethanol, but insoluble in water. Squalene is a hydrophobic substance that is actively involved in metabolism, biological synthesis of steroids, and contains shark liver and vegetable oils. Known use of squalene in dietary supplementation (UB) [13-16], Squalene is easily absorbed into the skin. This is due to the fact that squalene has a close biochemical relationship with the sebaceous gland secretion of the skin. The sebaceous gland secretion is a mixture of lipids that form the lipid mantle of the skin with its bactericidal properties [17-19]. By allowing oxygen to escape from water, squalene provides oxygen to cells and activates immune responses. Deep penetration of the skin promotes the transfer of biologically active substances, restores the structure of the epidermis, protects the skin from UV radiation and ensures the skin's resistance to photon aging.

The optimum effect of the perhydrosqualene content in the cream was observed at 10.0 - 15.0 g. If its content was less than 10 g, the effect was significantly reduced. If the Perhidrosqualene content was greater than 15.0 g, the consistency of the cream changed, the cream became much more fluid, and a layer formed which made it difficult to use.

/ i // a-Tocopherol (alpha-Tocopherolum) or Vitamin E - Light yellow viscous solution with a slight odor. It oxidizes in the light and becomes dark. Tocopherol is a hydrophobic substance, it contains green parts of young plants, vegetable oils. Vitamin E is a natural antioxidant (antioxidant) that engages in the inactivation of free radicals and protects cell membranes from collapse, including the effects of UV radiation. Vitamin E engages in protein biosynthesis, gives the skin suppleness and elasticity, promotes the prevention of inflammation, reduces seborrheic manifestations, activates skin regenerative processes [20-22].

The optimum effect of ΑΖ / ΰ-tocopherol (vitamin E) content in the cream was observed at 1.0 - 3.0 g. If its content was less than 1.0 g, the effect was significantly reduced, but if its content was greater than 3.0 g, the consistency of the cream changed, it became thinner, and a layer formed which made it difficult to use.

Capric acid and caprylic triglycerides (Caprylic / Capric triglycerida) an oily liquid obtained from coconut oil. Insoluble in water, miscible with oils. Due to its long shelf life, it does not require special storage and handling conditions. It should be stored in a dry, cool place. Triglycerides, as structuring agents, promote the emulsification of hydrophobic substances in the cream. Triglycerides, like plasticizers, in combination with aloe, provide a high degree of skin compatibility, which gives the cream a high degree of coverage and promotes the formation of a thin, elastic layer that is quickly absorbed into the skin. The triglyceride content is in the range 12.2-13.4 g. Reducing the triglyceride content to less than 12.2 g made the cream denser, less elastic. Increasing the amount of triglycerides by more than 13.4 g reduced the density of the cream and worsened its structuring properties.

Apricot oil (Prunus armeniaca) - a product obtained from apricot kernels by cold pressing. Apricot oil has a low acidity and low viscosity, and is homologous in composition to skin fat and epidermis lipids. In the composition of the new cream, it is a structuring component that allows to obtain a low viscosity cream. The amount of apricot oil is set within the range of 5.7 - 6.3 g. Reducing the amount of apricot oil by less than 5.7 g increased the density of the cream and reduced its elasticity. Increasing the amount of apricot oil by more than 6.3 g made the cream liquid, reducing its density, which made it difficult to use.

Glycerol stearate (Glyceroli stearas) - It is used as a stabilizing and structuring component in 4.0 to 4.4 grams to emulsify the hydrophobic components of the new cream. Reducing the amount of glycerol stearate by less than 4.0 g impaired the emulsification of the hydrophobic components of the cream. Increasing the amount of glycerol stearate by more than 4.4 g caused a change in the base state of the cream and reduced its elasticity, which made it difficult to use.

Stearic acid (Acidum stearicum, CjJhiOz) - It is used as a plastic thickener. The acid structuring properties make the cream more dense and absorbs into the stratum corneum, leaving the skin smooth and soft. The amount of stearic acid was determined in the range 0.8 - 0.9 g. Decreasing the amount of stearic acid by less than 0.8 g impaired its structuring properties and the emulsification of the composition. Increasing the amount of stearic acid by more than 0.9 g changed the cream base and increased its density.

Carbomer (Sodium carbomer) - a synthetic polymer used to thicken and stabilize the composition of the cream. It is used as a thickener. Carbomer promotes the formation of a lipid barrier that protects the skin from dehydration. The amount of carbomer was determined in the range 0.4 - 0.5 g. Reducing the amount of carbomer to less than 0.4 g made the cream more fluid, which worsened the skin's lipid barrier. Increasing the amount of carbomer would not be desirable as the density of the cream changed, which made it difficult to use.

Selenomethionine (Selenium methioninum) is an antioxidant that neutralizes oxides and peroxides (acids), stimulates collagen biosynthesis, prevents cell membrane collapse, gives skin firmness and elasticity, reduces seborrheic manifestations, activates regenerative processes in the skin, restores the epidermis. Selenium (Selenium) is a trace element contained in active centers in the form of an amino acid: selenomethionine, selenocysteine. Selenomethionine is a hydrophilic substance. Selenium in the body interacts with vitamins, enzymes, biological membranes and participates in oxidation-regeneration processes [23]. Selenium disulphide is used to treat seborrheic scalp [24]. Selenomethionine is a hydrophilic substance.

Optimum effect of selenomethionine content in the cream: 0.05-0.5 g. If its content was less than 0.05 g, the effect of restoring the structure of the epidermis was significantly reduced, but if its content was greater than 0.5 g, it was difficult to make the cream, the consistency of the cream changed, it became significantly thicker, use.

Aloe (Aloe barbadensis) - a jelly-like substance found in the leaves of the aloe plant. It promotes the delivery of biologically active substances to the deeper layers of the skin, and its recommended use is 23.0 - 25.0 g. If its content was less than 23.0 g, the curative effect of the cream was reduced, if its content was greater than 25.0 g, there were difficulties in the preparation of the cream, its consistency changed, the cream became thinner, and the exfoliation made it more difficult. and worsened formation of the lipid barrier on the skin, which protects against dehydration.

Glycerol (Glycerolum), a Trisatomic alcohol, a viscous, transparent substance which acts as a solvent. The glycerol content is determined in the range of 1.2 - 1.3 g. Reducing the amount of glycerol to less than 1.2 g impaired the dissolution of the hydrophobic constituents of the cream (perhydrosqualene, αΖ / α-tocopherol), resulted in delamination and altered activity. Increasing the amount of glycerin by more than 1.3 g made the cream more liquid and its density decreased.

Cetyl alcohol (Cetyl alcohol, CH / C ^ juCHCHOH), used as a cream emulsifier. The emulsifier reduces the surface tension at the phase boundary of the dispersed system. The amount of cetyl alcohol is determined in the range 1.6 - 1.8 g. Reduction of the amount of cetyl alcohol by less than 1.6 g reduced the stability of the hydrophobic components of the cream and resulted in delamination. Increasing the amount of cetyl alcohol by more than 1.8 g reduced the density of the cream, making it more liquid, which made it more difficult to use.

Distilled water (Aqua destillata) is included in the base as a part of the "water in oil" emulsion (where water is the hydrophilic part of the emulsion, oil and squalene is the hydrophobic part). Water - a clear, colorless liquid, odorless and tasteless. The addition of water to the new cream provides a cooling and softening effect, as well as allowing the cream to maintain its optimum consistency. The amount of water is within the limits of the rest (32.0 - 36.0 g).

The new cream composition was successfully used to obtain a dosage form of 100.0-200.0 g.

Each component included in the cream has only its specific and useful properties. The experimentally found composition of the components, their interrelationship and the technology of their application, made it possible to obtain a biologically active cream composition that maintains stability, restores the structure of the epidermis and the lipid barrier of the skin.

All components of the new cream composition, as separate preparations, are authorized for use in dermatology within the scope of the invention.

I.- II. Examples of cream composition

perhydrosqualene 10.0-15.0 αΖ / α-tocopherol (Vitamin E) 1.0-3.0 selenomethionine 0.05 - 0.5 aloe 23.0-25.0 triglycerides of capric acid and caprylic acid 12.2-13.4 apricot oil 5.7-6.3 glycerol stearate 4.0-4.4 stearic acid 0.8-0.9 glycerol 1,2-1,3 cetyl alcohol 1.6-1.8 carbomer 0.4-0.5 distilled water the rest of.

The method of obtaining the cream

The complexity of the preparation of the new cream is due to the fact that perhydrosqualene and ezZ / h-tocopherol are hydrophobic substances and selenomethionine is a hydrophilic substance.

Experimentally derived components and their ratio: hydrophilic components (water, aloe, glycerol), structurizers and plasticizers (capric and caprylic triglycerides, glycerol stearate, stearic acid, carbomer), emulsifier (cetyl alcohol), diluent (cetyl alcohol), glycerol the ability to maintain the activity and stability of the hydrophilic (selenomethionine) and hydrophobic (squalene, αΖ / ά-tocopherol) substances contained in the cream composition.

During the preparation of the cream, the hydrophobic components are first mixed. The first mixture of hydrophobic components contains perhydrosqualene (10.0 - 15.0 g), placed in a laboratory glass, heated in a water bath to 45-50 ° C. Weigh individually, 1.0 to 3.0 g of alpha-tocopherol (vitamin E) and introduce into the heated perhydrosqualene, mix thoroughly for 15 to 20 minutes, periodically (2 to 3 times) turning the homogenizer on for 2 to 3 minutes until homogeneous mass. A second mixture of hydrophobic components and stabilizers is then prepared; weigh separately triglycerides (12.2 - 13.4 g), apricot oil (5.7 - 6.3 g), glycerol stearate (4.0 - 4.4 g), steanic acid (0.8 - 0.9 g) ) and carbomer (0.4-0.5 g). All components of the second mixture are heated in a water bath to 45-50 ° C, mixed together and added to the first mixture. The two mixtures are mixed together for 15-20 minutes, periodically (2-3 times) turning on the homogenizer for 2-3 minutes until a common, homogeneous, hydrophobic mass is formed.

The mixture is then prepared from solvents which are individually weighed and heated in a water bath to 45-50 ° C: aloe (23.0-25.0 g), glycerol (1.2-1.3 g), cetyl alcohol (1.6 1.8 g), water (32.0 - 36.0 g). Stir the heated solvents together for 15-20 minutes.

Weigh separately the selenomethionine (0.05 - 0.5 g) as the solvent is introduced into the heated mixture. The heated mixture of selenomethionine and solvents is thoroughly mixed for 15-20 minutes. The heated selenomethionine mixture is mixed with the total heated hydrophobic mixture over a period of 15-20 minutes, periodically (2-3 times) turning on the homogenizer for 2-3 minutes until a homogeneous white or white-yellowish mass with a slight apricot oil aroma is obtained. Cool to 30-32 ° C. The resulting cream is packaged in 100.0 and 200.0 g light-tight containers.

The incorporation of natural solvents and oils, structurizers and plasticizers in the cream, in the amount obtained experimentally, allows the activity of the biologically active hydrophilic (selenomethionine) and hydrophobic (squalene, αΖ / α-tocopherol) components to be preserved, as well as their properties and composition.

The new cream composition provides an effective nourishing and softening effect.

Clinical trials were conducted with 15 volunteers, women aged 35-45 at the Health Center 4 Aesthetic Dermatology and Surgery Clinic. Clinical trials included:

1. Visual examination of the skin, during which the skin's dermatological status was determined, its general condition (color, turgor, exfoliation), skin micro-relief, wrinkles, pigmentation.

2. Skin examination with a dermatoscope. The skin relief and morphology was determined with a dermatoscope HEINE alpha +, Heine Optotechnic, Germany. As a non-invasive method of skin examination, dermatoscopy allows assessment of skin relief, pores, capillary and pigmentation. As the skin ages, it is necessary to detect signs of pigmentation disorders: lentigo and / or dishromia (light or dark spots).

In the process of dermatoscopic examination:

1) assessed the degree of skin turgor and skin looseness in the décolleté and cheek areas by measuring the height of the small area of skin using the suction method,

(2) assessed the degree of flaking and dry skin,

3) determined the amount of wrinkles and their characteristics (total amount, depth, width, length),

4) assessed for signs of skin pigmentation disorders: lentigo or / and dishromia (dark / light spots).

All women (15) had a mixed facial skin type, predominantly dry facial skin, typical of the first stage of xerosis (7 women); 3 women had a second stage of xerosis: dry skin, peeling of the epidermis, fine lines in the mimic activity zones; Five women were diagnosed with the third stage of xerosis: scaly face on face, deep wrinkles in the eye area, upper nose, changes in pigmentation (dark / light spots).

Clinical trials were conducted both before, 3, 7 and 14 days after, 30, 40 and 60 days after the start of the application. Apply a thin layer of cream twice a day (morning and evening) to the cleansed face and neck skin. The pH of the facial skin was measured during the study. During the first days the skin pH was 7.3 - 7.4.

The study determined the following: all 15 women on day 3-4 improved their complexion, skin turgor, and dry and tight skin; On day 14, the depth and amount of wrinkles decreased, the scaly scales disappeared, the pH of the skin normalized (6.5); On day 30, the pigmentation spots decreased in size, disappeared, or became lighter. All the women surveyed admitted that the skin had become significantly softer, younger and cleaner. The composition of the cream did not cause inflammation and comedones.

Studies have shown that the new composition of the cream has cosmetic and curative-preventive properties. It restores the structure of the epidermis and the lipid barrier of the skin, enables the prevention and effective treatment of facial xerosis, restores the condition of the skin after photon aging caused by UV damage: improves turgidity and moisturizing, relieves tightness and exfoliation of the epidermis and smooth relief, reduces pigmentation, inflammation and vascular disorders.

The complexity of the invention is due to the fact that the components of the new composition and their relationship when the new composition has an effective preventive and curative effect on the manifestations of facial xerosis and on the skin were unknown. photo-aging. The problem of cream development was exacerbated by the fact that the components of the new composition are both hydrophilic (selenomethionine) and hydrophobic (vitamin E, squalene) substances. The conditions under which the hydrophilic and hydrophobic components can be combined in a cream were unknown. The experimentally found components, their relationship and technological conditions for obtaining the new cream composition, made it possible to prepare a stable, homogeneous cream composition which maintains its effectiveness and stability at room temperature for 6-8 months.

The composition of the new cream was not found in scientific and patent sources. Experimental tm clinical studies performed indicate that the criterion of "invention level" is met.

INDUSTRIAL USE

There are 2 industrial forms of cream developed: 100.0 g tm 200.0 g in light-proof containers. The stability and technological properties of both formulations of the new cream remain at room temperature for 6-8 months.

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Claims (1)

THE CLAIM Cream for prevention and treatment of facial xerosis is characterized by containing perhydrosqualene, α-α-tocopherol (vitamin E), selenomethionine, aloe, capric acid and caprylic triglycerides, apricot oil, glycerol stearate, stearic acid, glycerol, cetyl water in the following quantities (g): perhydrosqualene 10.0-15.0 chz // b-tocopherol (vitamin E) 1.0-3.0 selenomethionine 0.05 - 0.5 aloe 23.0-25.0 triglycerides of capric acid and caprylic acid 12.2-13.4 apricot oil 5.7-6.3 glycerol stearate 4.0 - 4.4 stearic acid 0.8-0.9 glycerol 1,2-1,3 cetyl alcohol 1.6-1.8 carbomer 0.4-0.5 distilled water the rest of.