RU2843689C1 - Agent for treating skin diseases and damages and a method for preparing same - Google Patents

Abstract

FIELD: pharmaceutics.

SUBSTANCE: group of inventions refers to pharmaceutical industry, namely to a method for preparing an agent for treating skin diseases and damages specified in atopic dermatitis, diaper dermatitis, suture suppuration, shaving irritation, trophic ulcers, eczema, and to an agent. Method of producing an agent for treating diseases and skin lesions selected from atopic dermatitis, diaper dermatitis, suture suppuration, shaving field irritation, trophic ulcers, eczema, comprising grinding one part by weight of chamomile and one part by weight of calendula to particle size of 30-500 mcm, obtaining a powder, which is placed into ultrasonic extractor with distilled water in amount of four parts by weight, obtaining mixture of water and herbal powder, mixture is heated to temperature 30 °C and holding for ten minutes, wherein mixture is treated with ultrasonic waves in range of 80 kHz, then cooled to temperature of 18-20 °C, repeated mixture heating cycle to temperature 30 °C with treatment with said ultrasonic waves and cooling to temperature 18-20 °C five times, then obtained extract of chamomile and calendula is filtered through a filter with pore size 10 mcm, extract of chamomile and calendula in amount of 9.5-10 wt. % of agent is heated to temperature 31-40 °C, borax (sodium tetraborate) is placed therein in form of crystals in amount of 0.2-0.3 wt. % of agent, stirring until complete dissolution of borax in said extract, after which Vaseline is mixed and heated in amount of 70-71 wt. % of the agent and sperm whale hydrogenated fat in amount of 3-3.2 wt. % of the agent to temperature of 70-120 °C, to produce a mixture of Vaseline and sperm whale hydrogenated fat, wherein dynamic viscosity of said mix is controlled. When said dynamic viscosity reaches 0.8-1 cP, mix of Vaseline and hydrogenated fat is agitated by spatula at rate of 30-60 rpm and, at a time, temperature is decreased to 40-70 °C, then adding to mixture of Vaseline and hydrogenated fat tar in amount of 0.75-0.8 wt. % of agent and mometasone in amount of 0.002-0.003 wt. % of agent, obtained mixture is cooled to temperature 25-35 °C, then adding: concentrate of vitamin A in amount of 0.07-0.08 wt. % of agent, sanguinarine hydrosulphate in amount of 0.01875-0.02 wt. % of agent, chelerythrine hydrosulphate in amount of 0.01875-0.02 wt. % of agent, dexpanthenol in amount of 0.4-0.5 wt. % of agent, methyluracil in amount of 0.9-1 wt. % of agent, concentrate of sea-buckthorn oil in amount of 3.8-4 wt. % of agent, dry extract of Eucalyptus globulus leaves in amount of 0.125-0.15 wt. % of agent, aqueous extract of chamomile and calendula with diluted in it borax, olive oil in an amount supplementing required amount of agent to 100 wt. %, all said components are mixed, obtained composition is cooled to temperature 10-25 °C and stirring with frequency of 30-60 rpm until a dynamic viscosity of 3000-10000 cP is obtained, after which temperature of composition is lowered to 5-(-20) °C while continuing to mix and control the dynamic viscosity when the composition reaches a dynamic viscosity of 25000-30000 cP, mixing is stopped and composition is held at temperature 0-(-20) °C for 24 hours. Agent for treating skin diseases and damages specified in atopic dermatitis, diaper dermatitis, suture suppuration, shaving irritation, trophic ulcers, eczema produced by the above method and containing the following ingredients in the following proportions, wt. %: Vaseline 70-71; sperm whale hydrogenated fat 3-3.2; tar 0.75-0.8; borax 0.2-0.3; mometasone 0.002-0.003; vitamin A concentrate 0.07-0.08; sanguinarine hydrosulphate 0.01875-0.02; chelerythrine hydrosulphate 0.01875-0.02; dexpanthenol 0.4-0.5; methyluracil 0.9-1; concentrate of sea buckthorn oil 3.8-4; dry extract of Eucalyptus globulus leaves 0.125-0.15; water extract of chamomile and calendula 9.5-10, olive oil – the rest.

EFFECT: agent produced by the method described above is effective for treating the skin diseases and affections specified in atopic dermatitis, diaper dermatitis, suture suppuration, shaving irritation, trophic ulcers, eczema.

2 cl, 11 ex

Description

Scope of application

The invention relates to medicine, namely to medicinal products for the treatment of diaper dermatitis, bedsores, relief of exacerbation of atopic dermatitis, treatment of eczema, burns, long-term and poorly healing wounds, trophic ulcers, skin rejuvenation, improvement of skin condition during exacerbation of rosacea and psoriasis. In addition, the claimed invention can also be used in purulent surgery in the treatment of purulent wounds and trophic processes.

Prior art

The prior art discloses agents for treating various skin diseases and lesions, including diaper dermatitis, containing aqueous and oil phases, using natural or synthetic emulsifiers that stabilize the said agents, preventing them from separating into aqueous and oil phases. At the same time, emulsifiers that provide a stable connection between the fat base and aqueous components significantly reduce the absorption of active components into tissue cells and hinder or significantly slow down their action inside the cell, in the case of partial or complete penetration into it. In addition, it is known that emulsifiers reduce the transdermal delivery of active ingredients into cells (Nina Dragicevic, Howard I. Maibach. Percutaneous Penetration Enhancers. Chemical Methods in Penetration Enhancement. Springer-Verlag Berlin Heidelberg 2015). It is not advisable to use such products in the treatment of diaper dermatitis in children, since the speed of treatment is significantly reduced, and substances penetrate into healthy cells that impede the normal functioning of this cell, which can lead to the development of skin pathologies in children, turning into chronic skin diseases.

The prior art discloses a means for stimulating hair growth and skin regeneration (publication of Russian patent RU2097017 (C1), IPC class A61K7/06, published on 27.11.1997), which includes the following components in the following ratio, in may:

- mival (chloromethylsilatrane) 3-5;

- dimexide 2-5;

- ethyl alcohol 5-15;

- sunflower oil 10-20;

- sea buckthorn oil 5-10;

- lavender oil 2-3;

- anhydrous lanolin the rest.

This product is made in the following way. The calculated quantities of Mival, dimexide, sunflower, sea buckthorn, lavender oils and ethyl alcohol (ethanol) are loaded into a round-bottomed flask with a stirrer. The mixture is stirred until a uniform homogeneous light orange solution is obtained. In a fume hood in an enamel container, lanolin is heated to 45-50°C and the resulting alcohol-oil solution of Mival is added to it.

The disadvantages of this product are the use of lanolin and dimexide in its composition. Lanolin is quickly absorbed into the skin and penetrates into tissue cells, partially blocking the effect of active components on these cells, such as chloromethylsilatrane and sea buckthorn oil. Dimexide, also being an emulsifier, as is reported in the publication of the patent for utility model UA76971 (U) (IPC class A61K31/00, published on 25.01.2013), is quickly absorbed into the skin and penetrates into tissue cells, partially blocking the effect of active components on these cells, such as chloromethylsilatrane and sea buckthorn oil.

The method of manufacturing this product is simple and convenient due to the use of emulsifiers such as dimexide and lanolin. Due to the use of dimexide and lanolin, the treatment of diaper dermatitis and diaper dermatitis complicated by secondary fungal and / or bacterial infections, as well as the relief of exacerbation of atopic dermatitis, the treatment of eczema, burns, long-term and poorly healing wounds, bedsores, trophic ulcers, as well as the restoration of affected areas of the skin, using this product, significantly increases the time of exposure to tissue cells, which is unacceptable in the treatment of children, as well as in trophic processes, where there is a violation of tissue nutrition or there is thermal damage in which some of the cells died, and a large area of soft tissue can be saved by providing nutrition and stimulating the regeneration of damaged, but still living cells.

Also known from the prior art is a phytobalm for skin regeneration (publication of Russian patent RU2369377 (C1), class IPC A61K8/97, published 10.10.2009), containing dimexide (dimethyl sulfoxide), plant extracts: licorice root, small-flowered yarrow inflorescences, sandy helichrysum inflorescences; beeswax or paraffin; vitamins A and E, talc and vegetable oils selected from the series: olive, sea buckthorn, glycerin, petroleum jelly, petroleum jelly, castor, with the following component content, wt.%:

- dimexide (dimethyl sulfoxide) wt.% 0.5-2;

- extract of naked licorice root wt.% 0.5-2;

- extract of inflorescences of Yarrow small-flowered, wt.% 0.5-2;

- extract of Helichrysum arenarium inflorescences wt.% 0.5-2;

- beeswax or paraffin wt.% 9-11;

- retinol (vitamin A) wt.% 0.5-1;

- tocopherol (vitamin E) wt.% 0.5-1;

- zinc oxide (talc) wt.% 0.4-1.1;

- vegetable oils selected from the following range: olive, sea buckthorn, glycerin, petroleum jelly, Vaseline, castor - the rest.

The preparation of the phytobalm composition was carried out according to the following scheme:

Grinding wax or paraffin and weighing, feeding a portion of the crushed wax into the reactor and melting it, then adding vegetable oils, then dimexide. All this is stirred very slowly at a temperature of no more than 60 degrees. Then vitamins are added and then extracts emulsified with ammonia. After mixing, talc and fragrances are added.

The disadvantages of this phytobalm are the use of dimexide and ammonia as an emulsifier, which are quickly absorbed into the skin and penetrate into tissue cells, partially blocking the effect of active components on these cells, such as herbal extracts and vitamins.

The method of making this phyto-balm is simple and convenient due to the use of emulsifiers such as dimexide and ammonia; the water and oil phases do not separate.

Due to the use of demexide and ammonia, the treatment of diaper dermatitis and diaper dermatitis complicated by secondary fungal and/or bacterial infections, as well as the relief of exacerbation of atopic dermatitis, the treatment of eczema, burns, long-term and poorly healing wounds, bedsores, trophic ulcers, as well as the restoration of affected areas of the skin, with the use of this product, the time of exposure to tissue cells is significantly increased, which is unacceptable in the treatment of children, as well as in trophic processes where there is a violation of tissue nutrition or there is thermal damage in which some of the cells have died, and a large area of soft tissue can be saved by providing nutrition and stimulating the regeneration of damaged, but still living cells.

Also known from the prior art is a local skin-soothing composition aimed at treating diaper dermatitis in children (patent publication US8932656 (B1), IPC class A61K31/355, published on 13.01.2015), consisting mainly of an effective amount of a substantially anhydrous mixture of oils:

- about 38 vol.% unrefined virgin coconut oil (Cocos nucifera),

- about 19 vol.% extra virgin olive oil,

- about 19 vol.% jojoba oil (Simmondsia chinensis),

- about 19 vol.% calendula oil,

- about 1 vol.% tea tree oil (Melaleuca),

- about 0.1-1.0 vol.% of German chamomile extract (Matricaria chamomilla),

- about 0.1-1.0 vol.% mixed tocopherol oil,

wherein the mixed tocopherol oil does not contain soybean and corn oils, and the composition does not contain water-soluble active substances. The composition is produced by mixing the listed components. The publication states that when treating diaper dermatitis with this composition, the skin rash goes away in a few days.

The main disadvantage of this composition is (as stated in the patent description) that the treatment of diaper dermatitis in children takes several days, which can lead to various complications. In addition, this composition does not contain antiseptics that can suppress the action of various fungi and bacteria, especially those that get on the child's skin with feces from the intestines.

Also known from the prior art, selected as the closest analogue, is a universal ointment for young children (publication of application CN106389582 (A), IPC class A61K36/736, published on 15.02.2017), which includes the following raw materials by weight: 8-12 parts by weight of jojoba oil, 8-13 parts by weight of St. John's wort extract and 19-22 parts by weight of calendula and chamomile extract, 17-22 parts of olive oil, 26-31 parts of sweet almond oil, 7-11 parts of candelilla wax, 0.05-0.15 parts of peppermint essential oil, 0.7-1.0 parts of blue chamomile essential oil.

This ointment is made as follows. The necessary components are prepared in a given ratio, olive oil, sweet almond oil and candelilla wax are heated in a water bath to 30-50°C so that they melt, and jojoba oil and St. John's wort extract are added, chamomile and calendula extract, peppermint essential oil and blue chamomile essential oil are added to the melted oil in a water bath and mixed until completely dissolved.

This ointment works well to soften the skin and soothe itching.

The main disadvantages of this ointment include: the absence of plant antiseptic components, its components have a weak ability to regenerate skin cells, all components of the ointment are oils or oil extracts, they are well absorbed, moisturizing the skin and creating a fatty hydrophobic film that protects skin cells, but the active components of the ointment cannot fully perform their functions. In addition, the use of calendula and chamomile oil extract in the amount of 19-22 weight parts can oversaturate skin cells with carbohydrates and protein substances, slowing down the process of cell regeneration.

Brief description of the invention

The problem that the invention is aimed at solving is the creation of a means for treating diaper dermatitis in no more than six hours and diaper dermatitis complicated by secondary fungal and/or bacterial infections in no more than eleven hours in children, as well as a method for producing the means.

The technical result that can be obtained in the claimed invention is the creation of a method for producing a means for treating skin diseases and lesions with an antiseptic effect, with a balanced content of fatty and aqueous phases, in which there are no components that partially or completely penetrate into tissue cells, significantly reduce the absorption of active components into said cells and hinder or significantly slow down the action of active components inside the cell.

In addition, during clinical trials of the said product, an unexpected technical result was revealed, which is that the claimed product is capable of stopping exacerbations of atopic dermatitis and restoring areas of skin in children affected by atopic dermatitis and eczema, as well as stopping purulent processes in wounds within twelve hours.

The technical result, in relation to the method, is achieved in that in the method for producing a product for treating skin diseases and lesions, one part by weight of chamomile and one part by weight of calendula are ground to a particle size of 30-500 micrometers (μm), a powder is obtained, which is placed in an ultrasonic extractor with distilled water in an amount of four parts by weight, obtaining a mixture of water and herbal powder, the mixture is heated to a temperature of 30 ° C and held for ten minutes, while the mixture is treated with ultrasonic waves in the range of 80 kHz, then cooled to a temperature of 18-20 ° C, the cycle of heating the mixture to a temperature of 30 ° C with treatment with the said ultrasonic waves and cooling to a temperature of 18-20 ° C is repeated five times, then the resulting chamomile and calendula extract is filtered through a filter with a pore size of 10 μm, the chamomile and calendula extract in an amount of 9.5-10 wt. % of the product is heated to a temperature 31-40°C, add borax (sodium tetraborate) in the form of crystals in an amount of 0.2-0.3 wt.% of the product, stir until the borax is completely dissolved in the said extract, then mix and heat Vaseline in an amount of 70-71 wt.% of the product and sperm whale lard in an amount of 3-3.2 wt.% of the product to a temperature of 70-120°C, obtaining a mixture of Vaseline and sperm whale lard, while monitoring the dynamic viscosity of the said mixture, when the dynamic viscosity of the mixture reaches 0.8-1 centipoise (cP), begin to stir the mixture of Vaseline and lard with a spatula at a frequency of 30-60 rpm and simultaneously reduce the temperature to 40-70°C, then add tar to the mixture of Vaseline and lard in an amount of 0.75 - 0.8 wt.% of the product and mometasone in an amount of 0.002 - 0.003 wt.% of the product, the resulting mixture is cooled to a temperature of 25-35 °C, after which vitamin A concentrate is added to it in an amount of 0.07 - 0.08 wt.% of the product, sanguinarine hydrosulfate in an amount of 0.01875 - 0.02 wt.% of the product, chelerythrine hydrosulfate in an amount of 0.01875 - 0.02 wt.% of the product, dexpanthenol in an amount of 0.4 - 0.5 wt.% of the product, methyluracil in an amount of 0.9 - 1 wt.% of the product, sea buckthorn oil concentrate in an amount of 3.8 - 4 wt.% of the product, dry extract of eucalyptus globulus leaves in an amount of 0.125 - 0.15 wt.% of the product, aqueous extract of chamomile and calendula with borax diluted in it, olive oil in an amount supplementing the agent to 100 wt.%, all the specified components are mixed, the resulting composition is cooled to a temperature of 10-25°C and stirred at a frequency of 30-60 rpm until a dynamic viscosity of 3000-10000 cP is obtained, after which the temperature of the composition is lowered to 5 - (-20)°C, continuing to stir and monitoring the dynamic viscosity, when the composition reaches a dynamic viscosity of 25000-30000 cP, stirring is stopped and the composition is maintained at a temperature of 0 - (-20)°C for 24 hours.

The technical result in relation to the agent is achieved in that the agent for treating skin diseases and lesions is produced according to the method described above and contains the following components in the following content, wt.%:

- Vaseline - 70-71;

- sperm whale - 3-3.2;

- tar - 0.75-0.8;

- borax-0.2-0.3;

- mometasone - 0.002-0.003;

- vitamin A concentrate-0.07-0.08;

- sanguinarine hydrosulfate - 0.01875-0.02;

- chelerythrine hydrosulfate -0.01875-0.02;

- dexpanthenol - 0.4-0.5;

- methyluracil - 0.9-1;

- sea buckthorn oil concentrate - 3.8-4;

- dry extract of eucalyptus globulus leaves - 0.125-0.15;

- water extract of chamomile and calendula - 9.5-10;

- olive oil - the rest.

Disclosure of invention

The claimed method for producing a product for treating skin diseases and lesions allows for obtaining a homogeneous product with a stable combination of a fat base and aqueous components.

The method is based on thermal action on the components of the product and on their mixing at certain dynamic viscosities.

To prepare an aqueous extract of chamomile and calendula, grind one part by weight of chamomile (moisture content no more than 14%) and one part by weight of calendula (moisture content no more than 14%) to a particle size of 30-500 micrometers (μm), obtaining a powder. To control the particle size of the ground raw materials, sift the resulting powder through a sieve or any other suitable device (for example, through a filter bag) with a cell size of 500 μm. Grinding chamomile and calendula to 500 μm and filtering through a sieve with 500 μm cells allows you to subsequently dissolve more active substances and suspended active components in water.

After sifting, the chamomile and calendula powder are placed in an ultrasonic extractor with distilled water at a temperature of 15-25°C in an amount of four parts by weight, the powder is stirred in water to obtain a mixture of water and herbal powder, and the lid of the extractor is closed.

The mixture is heated to a temperature of 30°C and held for ten minutes, while the mixture is treated with ultrasonic waves in the range of 80 kHz. The temperature of 30°C is maintained and the said mixture is no longer treated with ultrasonic waves. After which the said mixture is cooled to a temperature of 18-20°C.

The cycle of heating the said mixture to 30°C, holding with ultrasonic wave treatment of the mixture, cooling to 18-20°C is repeated five times, i.e. five cycles are performed. Thus, chamomile and calendula extract is obtained. Then the obtained chamomile and calendula extract is filtered through a filter with a pore size of 10 μm, removing sediment from the chamomile and calendula powder.

It should be noted that the above five cycles are necessary to extract the required amount of active substances from the chamomile and calendula powder. The density of distilled water at 18-20°C is 1 g/ml, and the density of the saturated chamomile and calendula extract should be 1.05-1.08 g/ml. An extract with a density of 1.03 g/ml was obtained in four cycles, but an extract with such a density is not effective in the treatment of skin diseases. When the number of cycles was increased to eight, the increase in the extract density was insignificant - 1.06-1.1 g/ml. In addition, the above five ten-minute cycles cannot be replaced by one fifty-minute cycle, since exposure to ultrasonic waves in the 80 kHz range destroys most of the active components of chamomile and calendula in fifty minutes. In this regard, the five cycles mentioned above were chosen to prepare the required chamomile and calendula extract.

The obtained chamomile and calendula extract in the amount of 9.5-10 wt.% of the product is heated to a temperature of 31-40°C, borax (sodium tetraborate) is placed in it in the form of crystals in the amount of 0.2-0.3 wt.% of the product, and mixed, for example, with a stainless steel spatula until the borax is completely dissolved in the said extract.

Then prepare the fat base by heating a mixture of Vaseline in the amount of 70-71 wt.% of the product and sperm whale lard in the amount of 3-3.2 wt.% of the product to a temperature of 70-120°C. Heating is carried out in a ceramic or enamel container, less preferably in a stainless steel container, with any suitable device, for example, a steam generator. 70°C is the melting point of Vaseline; below this temperature, Vaseline cannot be mixed with molten sperm whale lard. It is important to control the dynamic viscosity of the said mixture of Vaseline and lard in order to begin mixing them to impart homogeneity to the mixture.

Dynamic viscosity is controlled using a rotational viscometer, such as the Elcometer 2250, using the Krebs method.

When the dynamic viscosity of the said mixture of Vaseline and lard reaches 0.8-1 centipoise (cP), begin to stir the said mixture, for example, with a stainless steel spatula at a frequency of 30-60 revolutions per minute (rpm. Here and further in the text, a revolution is understood as the passage of a spatula or other device for mixing a full revolution along the side walls inside the said container). A viscosity of 0.8 cP is sufficient to impart homogeneity to the mixture of Vaseline and lard by stirring. Viscosity above 1 cP hinders the complete dissolution of lard in Vaseline. In this case, the temperature of the mixture is reduced to 40-70°C.

Then, tar in the amount of 0.75-0.8 wt.% of the product and mometasone in the amount of 0.002-0.003 wt.% of the product are added to the mixture of Vaseline and salomas at the same temperature of 40-70°C. In this case, tar, being a liquid product, mixes well with Vaseline and salomas dissolved in it. Mometasone also dissolves well in Vaseline mixtures at a temperature of 40 to 70°C without losing its properties, so it is preferable to dissolve it in a mixture of Vaseline and salomas at this stage.

The resulting mixture of Vaseline, lard, tar and mometasone is cooled to a temperature of 25-35°C, preferably to a temperature of 25-30°C. This cooling is carried out so that the vitamins and biologically active substances in the plant components that need to be added to the mixture are not destroyed.

After which, vitamin A concentrate is added to the resulting mixture in an amount of 0.07-0.08 wt.% of the agent, sanguinarine hydrosulfate in an amount of 0.01875-0.02 wt.% of the agent, chelerythrine hydrosulfate in an amount of 0.01875-0.02 wt.% of the agent, dexpanthenol in an amount of 0.4-0.5 wt.% of the agent, methyluracil in an amount of 0.9-1 wt.% of the agent, sea buckthorn oil concentrate in an amount of 3.8-4 wt.% of the agent, dry extract of eucalyptus globulus leaves in an amount of 0.125-0.15 wt.% of the agent, an aqueous extract of chamomile and calendula with borax dissolved therein, previously obtained in the claimed method, olive oil in an amount supplementing the agent to 100 wt.%.

All of the above components are mixed in a mixture of Vaseline, lard, tar and mometasone, for example, with a stainless steel spatula, until a homogeneous mass is obtained.

The resulting composition is cooled to a temperature of 10-25°C, most preferably to a temperature of 10-15°C, and stirred, for example, with a stainless steel spatula at a frequency of 30-60 rpm until the first dynamic viscosity of 3000-10000 cP is obtained. After which the temperature of the composition is reduced to 5 - (-20)°C, while continuing to stir. The temperature must not be reduced before the composition reaches a dynamic viscosity of 3000 cP, otherwise the aqueous phase of the composition will separate from the oil phase. It is preferable to reduce the temperature after the composition reaches a dynamic viscosity of 10000 cP, since the thickened mass in it will have a uniform temperature. In this case, the dynamic viscosity is continued to be monitored.

When the composition reaches the second dynamic viscosity of 25,000-30,000 cP, stirring is stopped and the composition is maintained at a temperature of 0 to (-20)°C for 24 hours. In this case, it is not permissible to reduce the temperature to 0 to (-20)°C earlier than the composition reaches a dynamic viscosity of 25,000 cP, since the aqueous phase of the composition will separate from the oil phase. It is preferable to reduce the temperature after the composition reaches a dynamic viscosity of 30,000 cP, since the thickened mass in it will be homogeneous and will have a uniform temperature. The agent for the treatment of skin diseases and lesions obtained in the manner described above should be stored at a temperature of 2 to 10°C.

Thus, the method described above ensures the production of a means for treating diseases and lesions of the skin, while this method does not involve emulsification, which is provided by components that partially or completely penetrate into tissue cells, significantly reducing the absorption of active components into said cells and hindering or significantly slowing down the action of active components inside the cell.

The remedy for treating skin diseases and lesions obtained in the manner described above includes the following components in the following content, wt.%:

- Vaseline - 70 - 71;

- sperm whale - 3 - 3.2;

- tar - 0.75 - 0.8;

- borax-0.2-0.3;

- mometasone - 0.002 - 0.003;

- vitamin A concentrate - 0.07 - 0.08;

- sanguinarine hydrosulfate - 0.01875 - 0.02;

- chelerythrine hydrosulfate - 0.01875 - 0.02;

- dexpanthenol - 0.4 - 0.5;

- methyluracil - 0.9 - 1;

- sea buckthorn oil concentrate - 3.8 - 4;

- dry extract of eucalyptus leaves - 0.125 - 0.15;

- water extract of chamomile and calendula - 9.5 – 10;

- olive oil - the rest.

It should be noted that the content of each component in the composition of the declared product has a small range of values, calculated for errors in weighing, and in practice does not change the properties of the declared product.

In this product, Vaseline, sperm whale lard and olive oil form the fatty base.

Vaseline creates an occlusive layer on the skin, which holds the biologically active components of the product for treating skin diseases and lesions in the skin itself, preventing them from evaporating. Vaseline is a hypoallergenic substance and in practice does not cause allergic reactions. Therefore, Vaseline was chosen as the basis of the declared product, in which all active components dissolve.

Sperm whale lard is a product of sperm whale fat processing, it is rich in saturated fatty acids and has good penetrating ability. Sperm whale lard, due to natural fatty acids, can stimulate cell regeneration, restore damaged skin barriers and soften dry areas. This makes it more effective for the care of dry, irritated or damaged skin, as well as areas covered with rashes, crusts, dry scales. Due to its penetrating ability, lard penetrates the skin, nourishing skin cells with fatty acids. The content of sperm whale lard in the declared product is limited to 3 - 3.2 wt.%, since this amount is sufficient to fill the intercellular space with fatty acids perpendicular to the cell layers. If the amount of sperm whale fat in the declared product exceeds 3 - 3.2 wt.%, then the intercellular space will be excessively filled with fatty acids and the cells will be compressed by this excess amount of fatty acids.

Olive oil helps reduce inflammation due to the oleocanthal it contains. Olive oil contains omega-3 and omega-6 fatty acids necessary for cell regeneration. It should be noted that omega-6 fatty acid significantly narrows blood vessels and capillaries, so Vaseline was chosen as the main component of the fatty base for the stated product, olive oil makes up about 10 wt.% in the product.

Tar in the composition of the product has keratoplastic, antiseptic, anti-inflammatory, anesthetic effects, reduces erythema, soothes itching. In infiltrative processes in the skin, tar effectively has a resorptive effect. If the tar content in the product is less than 0.75 wt.%, this will lead to increased itching, especially in skin pathologies and trophic ulcers, while the tar content in the declared product of more than 0.8 wt.% does not improve the clinical effect, but causes organoleptic discomfort from the use of the ointment due to the pronounced tar smell.

Sea buckthorn oil concentrate contains carotenoids such as vitamin A and β-carotene, which protect cell membranes from the destructive action of free radicals, while β-carotene neutralizes dangerous types of free radicals: radicals of polyunsaturated acids and oxygen radicals, allowing cells to recover, and also increases the protective capabilities of the epidermis. A decrease in the proportion of sea buckthorn oil concentrate in the declared product below 3.8 wt.% leads to a slowdown in the restoration of damaged tissues. An increase in the content of sea buckthorn oil concentrate in the declared product above 4 wt.% does not lead to a significant effect.

It should be noted that without vitamin A concentrate in the first days of using the claimed product, tissues retain a tendency to necrosis and look non-viable, especially in the first 7-10 days. To eliminate necrosis at the initial stage of treatment, vitamin A concentrate in the amount of 0.07 - 0.08 wt.% is introduced into the claimed product. Introduction of vitamin A concentrate in the amount of less than 0.07 wt.% into the claimed product does not eliminate necrosis at the initial stage of treatment, and introduction of vitamin A concentrate in the amount of more than 0.08 wt.% into the claimed product is excessive and does not provide a significant effect. Vitamin A concentrate in the specified amount reduces the number of cells with terminal differentiation.

Mometasone is introduced into the declared product for the prevention and elimination of allergic reactions of patients to plant components. For this purpose, it is quite sufficient to introduce mometasone into the product in the amount of 0.002 - 0.003 wt.%.

Dexpanthenol is an organic alcohol, provitamin B5, a derivative of pantothenic acid. Dexpanthenol in the declared product in the amount of 0.4-0.5 wt.% moisturizes the skin, retains moisture in it, protects the lipid barrier of the skin, reduces skin irritation, reduces itching, accelerates wound healing. However, in an amount of over 0.5 wt.% dexpanthenol can cause contact dermatitis, allergic dermatitis, itching, redness and irritation of the skin.

Methyluracil in the declared product in the amount of 0.9 - 1 wt.% enhances the growth and reproduction of cells, improving the course of regeneration in damaged tissues, accelerates the healing of wounds, ulcers, burns, increases the body's resistance to infections. However, in an amount of more than 1 wt.% methyluracil can cause excess granulation in the wound or on the affected area of the skin.

The water extract of chamomile and calendula has a local anti-inflammatory, antiseptic, hemostatic effect, promotes the regeneration of damaged skin, saturating the cells with oleanolic acid, which improves the blood supply to cells and tissues, lupeol, which suppresses inflammatory processes in tissues, quercetin, which provides an antioxidant effect. In addition, the extract of chamomile and calendula nourishes skin cells with flavonoids, carbohydrates, protein substances, coumarins, carotene, vitamin C and essential oils. This water extract also helps restore the cell's water balance. For full saturation of cells with carbohydrates, protein substances, carotene, vitamin C and essential oils, it is enough to introduce 9.5-10 wt.% of chamomile and calendula extract into the declared product. If more than 10% by weight of chamomile and calendula extract is added to the declared product, the cells become oversaturated with carbohydrates and protein substances, which causes glycation, which is manifested by inhibition of the cell regeneration process.

It should be noted that the closest analogue ointment uses chamomile and calendula oil extract for better dissolution in other oil components. However, the oil extract penetrates the cell worse than the water extract, so in the claimed invention the chamomile and calendula oil extract is replaced by the water extract.

On damaged skin, in wounds and trophic ulcers, on burn surfaces, gram-positive bacteria and gram-negative bacteria, other bacteria and fungi, including intestinal flora, insensitive and weakly sensitive to antibiotics, actively develop; to suppress their activity, the declared product uses antiseptics with a broad spectrum of action against bacteria and fungi.

Borax is an effective component for fighting Candida fungi, staphylococci and streptococci.

Dry extract of eucalyptus globulus leaf is an effective component in combating Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumonia, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Haemophilus influenzae, Neisseria gonorrhoeae, Helicobacter pylori, Listeria monocytogenes (Listeria), Mycobacterium tuberculosis. (The causative agent of tuberculosis). In addition, the said extract of eucalyptus globulus leaves is effective in combating antibiotic-resistant strains, such as methicillin-resistant Staphylococcus aureus (MRSA) and nosocomial infections. Although eucalyptus globulus leaf extract is not a primary remedy against tuberculosis, some studies show its potential as an adjunct in therapy.

Sanguaritrin hydrosulfate is effective against bacteria such as: Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae, Corynebacterium diphtheriae, Neisseria gonorrhoeae, Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis and Proteus vulgaris, Klebsiella pneumoniae, Salmonella spp, Trichomonas vaginalis, Entamoeba histolytica. In addition, sanguaritrin hydrosulfate is effective against fungi such as: Candida albicans, Dermatophytes.

Cholerythrin hydrosulfate is effective in combating such bacteria as Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae, Corynebacterium diphtheriae, Neisseria gonorrhoeae, Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis and Proteus vulgaris, Klebsiella pneumoniae, Salmonella spp, Trichomonas vaginalis, Entamoeba histolytica. In addition, cholerythrin hydrosulfate is effective in combating such fungi as: Candida albicans, Dermatophytes.

Therefore, the composition of the claimed product includes such antiseptics as borax, dry extract of eucalyptus globulus leaves, sanguinarine hydrosulfate and cholerythrine hydrosulfate. At the same time, the said antiseptics cause a strong irritating and burning effect on the skin areas affected by dermatitis and in the wound, which complicates treatment and can lead to an unfavorable outcome of treatment. In this regard, a sufficient amount of antiseptics was found to suppress the above-mentioned microorganisms without causing an irritating and burning effect in wounds. Thus, the claimed product contains borax 0.2 - 0.3 wt.%, sanguinarine hydrosulfate 0.01875 - 0.02 wt.%, chelerythrine hydrosulfate 0.01875 - 0.02 wt.%, dry extract of eucalyptus globulus leaves 0.125-0.15 wt.%. It should also be noted that increasing the concentration of these antiseptics leads to increased bleeding of the wound surface and impregnation of tissues with capillary blood.

The influence of the essential features of the claimed remedy for the treatment of skin diseases and lesions on the achievement of the technical result is confirmed by the following examples.

Three batches of the product were prepared for use.

The first batch of the claimed agent was manufactured by the method described above with the first dynamic viscosity equal to 3000 cP and the second dynamic viscosity of 25000 cP, with the following content of components, wt.%: petroleum jelly - 70, sperm whale fat - 3, tar - 0.75, borax - 0.2, mometasone - 0.002, vitamin A concentrate - 0.07, sanguinarine hydrosulfate - 0.01875, chelerythrine hydrosulfate - 0.01875, dexpanthenol - 0.4, methyluracil - 0.9, sea buckthorn oil concentrate - 3.8, dry extract of eucalyptus globulus leaves - 0.125, aqueous extract of chamomile and calendula - 9.5, olive oil - the rest.

The second batch of the claimed agent was manufactured using the method described above with a first dynamic viscosity of 5000 cP ₃ and a second dynamic viscosity of 27500 cP, with the following component content, wt.%: petroleum jelly - 71, sperm whale fat - 3.2, tar - 0.8, borax - 0.3, mometasone - 0.003, vitamin A concentrate - 0.08, sanguinarine hydrosulfate - 0.02, chelerythrine hydrosulfate - 0.02, dexpanthenol - 0.5, methyluracil - 1, sea buckthorn oil concentrate - 4, dry extract of eucalyptus globulus leaves - 0.15, aqueous extract of chamomile and calendula - 10, olive oil - the rest.

The third batch of the claimed agent was manufactured by the method described above with the first dynamic viscosity equal to 10,000 cP and the second dynamic viscosity of 30,000 cP, with the following content of components, wt.%: petroleum jelly - 70, sperm whale fat - 3, tar - 0.75, borax - 0.2, mometasone - 0.002, vitamin A concentrate - 0.07, sanguinarine hydrosulfate - 0.02, chelerythrine hydrosulfate - 0.02, dexpanthenol - 0.5, methyluracil - 1, sea buckthorn oil concentrate - 4, dry extract of eucalyptus globulus leaves - 0.15, aqueous extract of chamomile and calendula - 10, olive oil - the rest.

Example 1

Patient 2 years old (boy), uncomplicated atopic dermatitis, exacerbation as a result of dietary violation, after application of the declared product of the first manufactured batch, after six hours, complete relief of exacerbation, skin without pathological changes.

Example 2

Patient 2.5 months (boy). Diaper dermatitis complicated by pyoderma against the background of Staphylococcus aureus in the intestine (complete resistance to antibiotics and bacteriophages). Stool is liquid, green, with an abundance of mucus and streaks of blood, receives therapy from a gastroenterologist. Buttocks, inguinal folds, scrotum, perianal area: the skin is edematous, sharply hyperemic, covered with pustular elements up to 1.5-2 mm in diameter. Four hours after using the declared product of the second manufactured batch, the pustules partially (up to 15%) opened, the rest decreased in size (no more than 1 mm in diameter). Hyperemia is practically absent, there is no swelling, pastosity or maceration. Eight hours and thirty minutes after the first application (four hours and thirty minutes after the second application of the declared product of the third manufactured batch), the skin is clean and of a natural color.

Example 3

Patient 4.5 months old (girl), diaper dermatitis complicated by candidiasis, with multiple punctate vesicular elements against the background of maceration of the skin of the buttocks, inguinal folds and perineum, alternating with erosions of the keratinized layer up to 0.5 cm in diameter. Five hours and thirty minutes after application of the declared product of the second manufactured batch: there is no maceration and hyperemia of the skin, erosions have decreased to 2-3 mm, vesicles are punctate, single. Eleven hours (five hours and thirty minutes after repeated application of the declared product of the first manufactured batch) the skin is of physiological color, there are no pathological elements and violation of the integrity of the skin.

Example 4

A 5-year-old patient with suppuration of sutures after primary surgical treatment - suturing of a linear bite wound (dog bite) of the right forearm. Upon examination, the wound edges are gaping, sharply hyperemic, edematous, there is abundant purulent discharge from the wound, the length of the wound is 5 cm, the width is 0.5 cm, the depth is 0.5 cm. After starting dressings twice a day, the first dressing with the declared product of the first manufactured batch, the second dressing with the declared product of the third manufactured batch, after twelve hours the purulent process is completely stopped, there is no inflammation of the wound edges. After twenty-four hours, active granulation in the wound. After ninety-six hours, the wound is completely closed by secondary intention.

Example 5

A 42-year-old patient with irritation after shaving complicated by pyoderma. After applying the claimed product of the second manufactured batch, after four hours, pustules with a diameter of 1.5 mm decreased to redness with a diameter of 0.5 mm, pustules are absent, redness zones with a diameter of up to 1.5 cm are completely removed, papules with a diameter of up to 2 mm are completely removed.

Example 6

Patient 4.5 months old, diaper dermatitis after night defecation with untimely hygiene of 52 ^cm2 in the anus and in the scrotal fold, four erosions of the skin of 1-1.5 ^cm2 . After applying the declared product of the third manufactured batch, after four hours the skin is clean, physiological color, there are no erosions or irritation.

Example 7

The patient is one year old, diagnosis - atopic dermatitis with secondary pyoderma. Multiple erosions of the skin in the area of large folds with abundant serous and purulent discharge, foci of atopic dermatitis with pronounced local inflammation, the head is hairless, covered with a bursting crust with purulent discharge from cracks.

At the time of initiation of therapy, the patient was discharged after in-patient treatment (6th hospitalization in six months), where he received systemic and local antibacterial and hormonal therapy, without effect. Against the background of local treatment with the declared product of the first manufactured batch, the second manufactured batch and the third manufactured batch of the skin and oral administration of probiotics for a week, the purulent-inflammatory process on the skin ceased, itching was completely relieved, sleep and appetite returned to normal. After one month of treatment with the declared product of the first manufactured batch, the second manufactured batch and the third manufactured batch, the skin is clean, without damage, the hair on the head has grown by 2.5 cm. The state of health is satisfactory. Appetite and sleep are good. Exacerbation of atopic dermatitis to a subacute course with damage to less than 3% of the skin against the background of tonsillitis at the age of two years was relieved by the declared product of the first manufactured batch in three days.

Example 8

A 54-year-old patient with a trophic ulcer (a consequence of trauma) on the anterior surface of the left shin, was treated in hospital, after which he was transferred to outpatient treatment by a surgeon. He received local dressings with stelaninum for three months without effect, which was replaced by iruksol for three months, against which the ulcer began to increase in depth and area. Further treatment was carried out in Israel and the USA, including Peruvian balsam and Berlin regenerating mesh were used, with negative dynamics. The size of the ulcer at the time of treatment was 3 × 12 cm in area and 1 cm deep into the skin. The ulcer is abundantly covered with fibrin with pronounced inflammation at the edges. During the first week of dressings with the declared agent alternately of the first manufactured batch and the second manufactured batch, the ulcer cleared up, single granulations of 2x2 mm appeared at the bottom and along the edges, the inflammatory process was stopped. After three weeks, the ulcer area began to decrease, the bottom of the ulcer was filled with granulation tissue. After four months, the ulcer completely closed flush with the surrounding tissues, the skin in its place was slightly pinkish, which was noticeably noticeable against the background of intense tanning.

Example 9

An 82-year-old patient with multiple trophic ulcers of the lower extremities (sixteen trophic ulcers) with abundant purulent discharge; the intestinal flora in the wound discharge culture was insensitive to antibiotics. Against the background of local dressings with the declared product of the third manufactured batch of both shins, the purulent process was completely stopped within two weeks, the ulcers began to clear of fibrin. The skin became more elastic and resilient, while above the dressings it remained "parchment". The healing process took a long time, which was due to age, severe atherosclerosis of the lower extremity vessels and difficulties with hygiene. Against the background of periodically occurring blunt injuries to the shins, new ulcers formed at the site of hematomas. Within a year and a half, all the ulcers closed without cosmetic defects flush with the surrounding tissues.

Example 10

The patient is 36 years old, works with aggressive chemicals, has a constant subacute course of eczema on his hands, with periodic exacerbations and cracks in the skin. In winter, the course of the pathological process is sharply exacerbated. Against the background of the use of the declared product of the first manufactured batch locally in winter, during the first week the pathological process was stopped to small foci of subacute course of eczema, during the second week the skin was completely restored. Later, the declared product was used periodically at night and during exacerbations.

Example 11

The patient is 34 years old. Atopic dermatitis since birth, in the last 20 years it has been occurring as neurodermatitis with severe itching. Skin lesions during exacerbations reach 92%. He used local antipruritic agents, systemic antihistamines and local mometasone. Remission occurred within two to three months during therapy. The first use of the declared product of the first manufactured batch gave remission in one week. Subsequently, during exacerbations, remission occurred in three to four days before the next severe stress. By the age of 38, exacerbations to a subacute course occur once or twice a year, and are stopped within two to three days.

From the above description it follows that by the described method, based on the thermal effect on the components of the product and on their mixing at given dynamic viscosities, it is possible to manufacture a product for the treatment of skin diseases and lesions with an antiseptic effect, with a balanced content of fatty and aqueous phases.

From the above description of the invention and examples it follows that the claimed agent is capable of treating diaper dermatitis in six hours, as well as diaper dermatitis complicated by secondary fungal and/or bacterial infections in no more than eleven hours in children, in addition, the claimed agent is capable of stopping exacerbations of atopic dermatitis and restoring skin areas affected by atopic dermatitis and eczema in children, as well as stopping purulent processes in wounds in twelve hours.

Claims (16)

1. A method for producing a remedy for treating skin diseases and lesions selected from atopic dermatitis, diaper dermatitis, suppuration of sutures, irritation after shaving, trophic ulcers, eczema, which consists in grinding one part by weight of chamomile and one part by weight of calendula to a particle size of 30-500 micrometers (μm), obtaining a powder that is placed in an ultrasonic extractor with distilled water in an amount of four parts by weight, obtaining a mixture of water and herbal powder, heating the mixture to a temperature of 30 ° C and holding for ten minutes, while treating the mixture with ultrasonic waves in the range of 80 kHz, then cooling to a temperature of 18-20 ° C, repeating the cycle of heating the mixture to a temperature of 30 ° C with treatment with the said ultrasonic waves and cooling to a temperature of 18-20 ° C five times, then the resulting extract of chamomile and calendula filtered through a filter with a pore size of 10 μm, chamomile and calendula extract in an amount of 9.5-10 wt.% of the product is heated to a temperature of 31-40 °C, borax (sodium tetraborate) is placed in it in the form of crystals in an amount of 0.2-0.3 wt.% of the product, stirred until the borax is completely dissolved in the said extract, after which petroleum jelly in an amount of 70-71 wt.% of the product and sperm whale lard in an amount of 3-3.2 wt.% of the product are mixed and heated to a temperature of 70-120 °C, obtaining a mixture of petroleum jelly and sperm whale lard, while monitoring the dynamic viscosity of the said mixture, when the dynamic viscosity of the mixture reaches 0.8-1 centipoise (cP), begin to stir the mixture of petroleum jelly and lard with a spatula at a frequency of 30-60 rpm and simultaneously reduce the temperature to 40-70°C, then tar in an amount of 0.75-0.8 wt.% of the product and mometasone in an amount of 0.002-0.003 wt.% of the product are added to the mixture of petroleum jelly and lard, the resulting mixture is cooled to a temperature of 25-35°C, after which vitamin A concentrate is added to it in an amount of 0.07-, 08 wt.% of the product, sanguinarine hydrosulfate in an amount of 0.01875-0.02 wt.% of the product, chelerythrine hydrosulfate in an amount of 0.01875-0.02 wt.% of the product, dexpanthenol in an amount of 0.4-0.5 wt.% of the product, methyluracil in an amount of 0.9-1 wt.% of the product, sea buckthorn oil concentrate in an amount of 3.8-4 wt.% of the product, dry extract of eucalyptus globulus leaves in an amount of 0.125-0.15 wt.% of the product, aqueous extract of chamomile and calendula with borax diluted in it, olive oil in an amount supplementing the required amount of the product to 100 wt.%, all of the specified components are mixed, the resulting composition is cooled to a temperature of 10-25°C and stirred at a frequency of 30-60 rpm until a dynamic viscosity of 3000-10000 cP is obtained, after which the temperature of the composition is lowered to 5-(-20)°C, continuing to stir and monitoring the dynamic viscosity, when the composition reaches a dynamic viscosity of 25000-30000 cP, stirring is stopped and the composition is maintained at a temperature of 0-(-20)°C for 24 hours. 2. A product for the treatment of skin diseases and lesions selected from atopic dermatitis, diaper dermatitis, suppuration of sutures, irritation after shaving, trophic ulcers, eczema, produced according to the method of item 1 and containing the following components in the following content, wt.%: Vaseline 70-71; sperm whale salomas 3-3.2; tar 0.75-0.8; borax 0.2-0.3; mometasone 0.002-0.003; vitamin A concentrate 0.07-0.08; sanguinarine hydrosulfate 0.01875-0.02; chelerythrine hydrogen sulfate 0.01875-0.02; dexpanthenol 0.4-0.5; methyluracil 0.9-1; sea buckthorn oil concentrate 3.8-4; dry extract of eucalyptus leaves 0.125-0.15; aqueous extract of chamomile and calendula 9.5-0; olive oil - the rest.