RU2851422C1 - Pastille for treating skin diseases and lesions - Google Patents

Abstract

FIELD: pharmaceutical industry.

SUBSTANCE: invention relates to the pharmaceutical industry, namely to a remedy for treating skin diseases and lesions selected from atopic dermatitis, nappy rash, and wounds. A lozenge for treating skin diseases and lesions selected from atopic dermatitis, nappy rash, wounds, made in the form of a plate from the following components, with the following content, mas.%: Vaseline 55-56; laurel oil (butter) 15-15.5; spermaceti 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; sanguinaria hydrosulphate 0.01875-0.02; chelerythrine hydrosulphate 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; aqueous extract of chamomile and calendula flowers 9.5-10, olive oil remainder.

EFFECT: above-described lozenge is effective for treating skin diseases and lesions selected from atopic dermatitis, nappy rash, and wounds.

6 cl, 6 dwg, 6 ex

Description

Scope of application

The invention relates to medicine, specifically to agents for the treatment of diaper rash, bedsores, atopic dermatitis flare-ups, eczema, burns, slow-healing wounds, trophic ulcers, skin rejuvenation, and improvement of skin condition during flare-ups of rosacea and psoriasis. Furthermore, the invention can also be used in purulent surgery for the treatment of purulent wounds and trophic processes.

Prior art

The prior art includes treatments for various skin conditions and lesions, including diaper dermatitis, containing aqueous and oil phases. These treatments utilize natural or synthetic emulsifiers to stabilize the formulations, preventing them from separating into aqueous and oil phases. Emulsifiers, which provide a stable bond between the fat base and aqueous components, significantly reduce the absorption of active ingredients into tissue cells and hinder or significantly slow their action within the cell, even if they partially or completely penetrate. Furthermore, emulsifiers are known to reduce the transdermal delivery of active ingredients to cells (Nina Dragicevic, Howard I. Maibach. Percutaneous Penetration Enhancers. Chemical Methods in Penetration Enhancement. Springer-Verlag Berlin Heidelberg 2015). Such agents are not recommended for use in the treatment of diaper dermatitis in children, as the healing rate is significantly reduced, and substances penetrate healthy cells, impeding the normal functioning of these cells, which can lead to the development of skin pathologies in children, developing into chronic skin diseases.

For example, a phytobalm for skin regeneration is known from the prior art (publication of Russian patent RU2369377 (C1), IPC class A61K 8/97, published on 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) 0.5-2;

- licorice root extract 0.5-2;

- extract of Yarrow inflorescences 0.5-2;

- extract of Helichrysum arenarium inflorescences 0.5-2;

- beeswax or paraffin 9-11;

- retinol (vitamin A) 0.5-1;

- tocopherol (vitamin E) 0.5-1;

- zinc oxide (talc) 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:

The wax or paraffin is ground and weighed, a portion of the ground wax is added to the reactor and melted, followed by the addition of vegetable oils and then dimethyl sulfoxide. Everything is stirred very slowly at a temperature no higher than 60 degrees Celsius. Vitamins are then added, followed by extracts emulsified with ammonia. After mixing, talc and fragrances are added.

The disadvantages of this phytobalm include the use of dimethyl sulfoxide and ammonia as emulsifiers, which are quickly absorbed into the skin and penetrate tissue cells, partially blocking the effect of active ingredients, such as herbal extracts and vitamins, on these cells. Furthermore, the fat base and aqueous phase in the emulsion quickly separate (1 to 6 months), and the ointment loses its healing properties.

A universal ointment for young children is known from the prior art and was selected as the closest analogue (publication of application CN106389582 (A), IPC class A61K 36/736, 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 works well to soften the skin and soothe itching.

The main drawback of this ointment is that it cannot be used to create a solid substance that melts at body temperature and is absorbed into the skin. Furthermore, its components have weak skin cell regeneration properties. All components of this ointment are oils or oil extracts. While they are readily absorbed, moisturizing the skin and creating a hydrophobic fatty film, protecting skin cells, the active ingredients cannot fully perform their functions. Furthermore, the use of calendula and chamomile oil extracts in quantities of 19-22 parts by weight can oversaturate skin cells with carbohydrates and proteins, slowing down the cell regeneration process.

Brief description of the invention

The objective of the invention is to create a medicinal product 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, improvement of skin condition during exacerbation of rosacea and psoriasis, and can also be used in purulent surgery for the treatment of purulent wounds and trophic processes, wherein the claimed product has a solid aggregate state and is dosedly distributed over an area.

The technical result that can be obtained in the claimed invention is the creation of a lozenge capable of treating diseases and skin lesions, primarily diaper dermatitis and deep wounds, into which the lozenge can be immersed without instruments, made in the form of a solid dose distributed over an area, capable of fitting the surface of the patient's body and melting at the temperature of his body.

The technical result is achieved in that the lozenge for the treatment of skin diseases and lesions is made in the form of a plate from the following components in the following content, wt%:

- Vaseline - 55 - 56;

- laurel oil (butter) - 15 - 15.5;

- 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;

- aqueous extract of calendula and chamomile - 9.5 - 10,

- olive oil - the rest.

The plate may be rectangular or oval and 1-5 mm thick. Rectangular plates have rounded corners. Furthermore, the plate may have at least one through hole.

Description of drawings

The claimed invention is explained with the help of the drawings presented in Figs. 1 - 6.

In this case, Fig. 1 shows the claimed rectangular-shaped lozenge.

Fig. 2 shows a side view of the lozenge of Fig. 1.

Fig. 3 shows the claimed oval-shaped lozenge.

Fig. 4 shows a side view of the lozenge of Fig. 3.

Fig. 5 shows the claimed rectangular lozenge with a hole made in it.

Fig. 6 shows a section along line A-A in Fig. 5, passing through the center of the hole made in the plate.

Disclosure of invention

A lozenge for the treatment of skin diseases and lesions, made in the form of a plate (medical plate).

Moreover, its components are selected so that they not only perform therapeutic functions (as in the ointment), but also, when combined, create a solid substance that can be molded into any shape upon hardening. These components and their content in the lozenge were selected empirically, through experimentation.

The declared lozenge is made from the following components in the following content, wt%: Vaseline - 55-56, laurel oil (butter) - 15-15.5, sperm whale lard - 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 calendula and chamomile - 9.5 - 10, olive oil - the rest.

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

In the stated lozenge, Vaseline, sperm whale fat, and bay oil (butter) form the fatty base of the medicinal substance. Vaseline, sperm whale fat, and butter also form the solid base of the stated lozenge, as their melting point is at least 25°C.

Petroleum jelly creates an occlusive layer on the skin, which retains the biologically active ingredients of the treatment for skin diseases and lesions within the skin itself, preventing them from evaporating. Petroleum jelly is hypoallergenic and does not cause allergic reactions. Therefore, petroleum jelly was chosen as the base for the formulation of the claimed lozenge, in which all the active ingredients are dissolved. However, petroleum jelly is not hard enough to make a lozenge, so to give the lozenge sufficient hardness to maintain its shape, butter and sperm whale fat are added to the petroleum jelly. Their fatty acids maintain the lozenge's firmness, while also allowing it to maintain its shape.

Bay leaf oil (butter) contains lauric acid, which has an antiseptic effect, as well as myristic and palmitic acids, which improve the absorption of nutrients by the skin. Additionally, the butter contains phytosterols, which stimulate collagen synthesis and suppress inflammation, chlorophyll, which clears pores and suppresses acne, and tannins, which have an anti-inflammatory effect on affected areas of the skin. The butter content in the stated lozenge is limited to 15.5% by weight, as a higher butter content causes the lozenge to lose its elasticity, become too hard, and contact with the skin surface will be difficult. If the butter content in the stated lozenge is less than 15% by weight, collagen molecules will be synthesized in insufficient quantities to intensively restore connective tissue in the skin. If the butter content in the declared lozenge is less than 15% by weight, the lozenge's hardness will be low and it will bend freely under the force of gravity on one side, which is very inconvenient to use. If the butter content in the declared lozenge is higher than 15% by weight, cracks will form in the lozenge, and fungi and bacteria will penetrate the cracks and multiply in the voids, rendering the lozenge unsuitable for use.

Sperm whale fat is essential in this lozenge to increase the hardness and melting point of the entire lozenge. Furthermore, sperm whale fat, a byproduct of sperm whale fat processing, is rich in saturated fatty acids and has excellent penetrating properties. Thanks to its natural fatty acids, sperm whale fat can stimulate cell regeneration, restore damaged skin barriers, and soften dry areas. This makes it more effective for treating dry, irritated, or damaged skin, as well as areas covered with rashes, crusts, and dry scales. Due to its penetrating properties, sperm whale fat penetrates the skin, nourishing skin cells with fatty acids. The sperm whale fat content in this lozenge is limited to 3-3.2% by weight, as 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 lozenge exceeds 3-3.2% by weight, the intercellular space will be excessively filled with fatty acids, and the cells will be compressed by this excess fatty acid content. A sperm whale fat content of 3-3.2% by weight allows the declared lozenge to melt at approximately 30°C. If the sperm whale fat content is less than 3% by weight, the lozenge will begin to melt at temperatures below 30°C. This is unacceptable for lozenge storage at room temperature, as the lozenge will transform into a semi-liquid (gelatinous) state and become unsuitable for use as a solid. Furthermore, sperm whale fat increases the hardness of the lozenge, but its content in the lozenge above 3.2% by weight significantly reduces its plasticity.

To ensure that the solid ingredients of the lozenge (Vaseline, sperm whale fat, and butter) do not prevent the lozenge from bending and maintaining its curved shape for application to the patient's skin, the lozenge contains plasticizers such as olive oil, tar, sea buckthorn oil concentrate, and dexpanthenol. Additionally, to impart flexibility, the lozenge contains an aqueous extract of chamomile and calendula.

Since the dynamic viscosity and impact on the treatment process of these components are different, their content in the lozenge was selected empirically.

Olive oil helps reduce inflammation thanks to its oleocanthal content. Olive oil contains omega-3 and omega-6 fatty acids, essential for cell regeneration. It's important to note that omega-6 fatty acids significantly constrict blood vessels and capillaries, so petroleum jelly is chosen as the main component of the fatty base for this product. Olive oil makes up approximately 10% by weight of the lozenge (added to the formulation to reach 100% by weight). If the olive oil content in the lozenge is increased, it will no longer retain its shape and will not be malleable.

Tar in the lozenge has keratoplastic, antiseptic, anti-inflammatory, and anesthetic effects, reduces erythema, and soothes itching. Tar effectively acts as a resorptive agent for infiltrative skin conditions. Tar content less than 0.75% by weight in the lozenge will increase itching, especially in cases of skin conditions and trophic ulcers. Tar content greater than 0.8% by weight does not improve the clinical effect but causes organoleptic discomfort due to a strong tar odor. Tar content less than 0.75% by weight will result in insufficient flexibility, while tar content greater than 0.8% by weight will result in greater flexibility than is necessary for insertion into deep wounds, making insertion difficult.

Sea buckthorn oil concentrate contains carotenoids such as vitamin A and β-carotene, which protect cell membranes from the destructive effects of free radicals. β-carotene neutralizes dangerous free radicals, such as polyunsaturated fatty acid radicals and oxygen radicals, allowing cells to recover and enhancing the protective capabilities of the epidermis. Reducing the sea buckthorn oil concentrate content in the stated lozenge below 3.8% by weight results in a slower recovery of damaged tissue. Increasing the sea buckthorn oil concentrate content in the stated lozenge above 4% by weight does not produce a significant effect.

An aqueous extract of chamomile and calendula provides local anti-inflammatory, antiseptic, and hemostatic effects, promoting the regeneration of damaged skin by saturating cells with oleanolic acid, which improves blood flow to cells and tissues; lupeol, which suppresses inflammation in tissues; and quercetin, which provides antioxidant properties. Furthermore, chamomile and calendula extract nourishes skin cells with flavonoids, carbohydrates, proteins, coumarins, carotene, vitamin C, and essential oils. To fully saturate cells with carbohydrates, proteins, carotene, vitamin C, and essential oils, it is sufficient to add 9.5-10% by weight of chamomile and calendula extract to the stated lozenge. If more than 10% by weight of chamomile and calendula extract is added to the stated lozenge, the cells become oversaturated with carbohydrates and protein substances, which causes glycation, which is manifested by inhibition of the cell regeneration process.

If the sea buckthorn oil concentrate content in the lozenge is below 3.8% by weight, and the aqueous chamomile and calendula extract content is below 9.5% by weight, the lozenge will not be flexible enough to adhere tightly to the patient's skin. If the sea buckthorn oil concentrate content in the lozenge is above 4% by weight, and the aqueous chamomile and calendula extract content is below 10% by weight, the lozenge will lose approximately 5% of its hardness, resulting in a deterioration in its strength properties, making it difficult to place the lozenge over overlapping postoperative sutures and inserting the lozenge into open wounds. This means the lozenge will become softer, requiring insertion into the open wound only with instruments such as tweezers. When applied to postoperative sutures, the lozenge may occupy a larger area than necessary.

Dexpanthenol is also included in the lozenge formulation to increase its flexibility, at a concentration of 0.4–0.5% by weight. Dexpanthenol promotes the mobility of protein molecular components, so its content in the lozenge exceeding 0.5% by weight may cause protein breakdown, resulting in the loss of its therapeutic properties. Dexpanthenol is an organic alcohol, provitamin B5, and a derivative of pantothenic acid. Dexpanthenol in the stated lozenge, at a concentration of 0.4–0.5% by weight, moisturizes the skin, retains moisture, protects the skin's lipid barrier, reduces skin irritation, reduces itching, and accelerates wound healing. However, in quantities exceeding 0.5% by weight, dexpanthenol may cause contact dermatitis, allergic dermatitis, itching, redness, and skin irritation.

To prevent lipid peroxidation in the lozenge, which leads to its destruction by disrupting the structure of fatty acids, a concentrate of vitamin A and methyluracil were added to the lozenge.

It should be noted that without vitamin A concentrate, during the first days of using the stated lozenge, tissues remain prone to necrosis and appear non-viable, especially during the first 7-10 days. To prevent necrosis at the initial stage of treatment, vitamin A concentrate was added to the stated lozenge in an amount of 0.07 - 0.08 wt%. The addition of vitamin A concentrate in an amount of less than 0.07 wt% to the stated lozenge does not eliminate necrosis at the initial stage of treatment, and the addition of vitamin A concentrate in an amount of more than 0.08 wt% to the stated lozenge is excessive and does not provide a significant effect. Vitamin A concentrate in the specified amount reduces the number of cells with terminal differentiation. It was determined experimentally that the addition of vitamin A concentrate in an amount of less than 0.07 wt% to the stated lozenge provides insufficient resistance to lipid peroxidation, and oxidation occurs partially. However, the introduction of vitamin A concentrate in the amount of 0.08 wt% into the declared lozenge provides complete resistance to lipid peroxidation in the lozenge composition and there is no need to increase its content.

Methyluracil in the stated lozenge, at a concentration of 0.9-1% by weight, enhances cell growth and proliferation, improving regeneration in damaged tissues, accelerating the healing of wounds, ulcers, and burns, and increasing the body's resistance to infections. However, in concentrations exceeding 1% by weight, methyluracil may cause excessive granulation in the wound or affected area of skin.

It was also experimentally determined that the addition of methyluracil in an amount less than 0.9% by weight to the claimed lozenge weakly prevents lipid peroxidation, with oxidation occurring gradually. However, the addition of methyluracil in an amount greater than 1% by weight provides complete resistance to lipid peroxidation within the lozenge, and there is no need to increase this level.

Since the molecules of the aqueous extract of chamomile and calendula in the stated lozenge are in a liquid state, their carbons have a tendency to degenerate into fatty molecules. Mometasone has been added to the lozenge composition, preventing the transformation of carbon atoms into fat molecules, which can form hard conglomerates, reducing the plasticity and therapeutic properties of the lozenge.

Borax is added to increase the lozenge's resistance to cracking and cracking. Furthermore, borax is an effective ingredient against Candida fungi, staphylococci, and streptococci, which can attack the herbal ingredients.

It should be noted that gram-positive and gram-negative bacteria, as well as other bacteria and fungi, including intestinal flora that is resistant or weakly sensitive to antibiotics, actively develop within the lozenge itself, as well as on damaged skin, wounds, trophic ulcers, and burn surfaces. To suppress their activity, the lozenge contains antiseptics with a broad spectrum of activity against bacteria and fungi. These antiseptics prevent the penetration of these microorganisms into the lozenge and prevent the destruction of the active medicinal ingredients. Increasing their concentration will not result in a significant effect, as the amount specified below was sufficient to prevent the penetration and development of these microorganisms. Conversely, decreasing their concentration resulted in the development of Streptococcus pyogenes and Salmonella spp., rendering the lozenge unsuitable for use.

Dry extract of eucalyptus globulus leaf is effective against Staphylococcus aureus, Streptococcus pneumoniae, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Haemophilus influenzae, Neisseria gonorrhoeae, Helicobacter pylori, Listeria monocytogenes (Listeria), and Mycobacterium tuberculosis (the causative agent of tuberculosis). Furthermore, this eucalyptus globulus leaf extract is effective against antibiotic-resistant strains, such as methicillin-resistant Staphylococcus aureus (MRSA), and hospital-acquired infections. Although eucalyptus globulus leaf extract is not a primary treatment for 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, and Entamoeba histolytica. Sanguaritrin hydrosulfate is also effective against fungi such as Candida albicans and Dermatophytes.

Cholerythrin 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, and Entamoeba histolytica. Cholerythrin hydrosulfate is also effective against fungi such as Candida albicans and Dermatophytes.

Therefore, the composition of the claimed lozenge includes such antiseptic agents as borax, dry extract of eucalyptus globulus leaves, sanguinarine hydrosulfate and cholerythrine hydrosulfate. However, the said antiseptic agents 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. In this regard, an amount of antiseptics sufficient to suppress the above-mentioned microorganisms without causing an irritating and burning effect in wounds was identified experimentally. Thus, the claimed lozenge 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.

From the above, it can be seen that the composition of the declared lozenge does not contain components that partially or completely penetrate tissue cells, significantly reduce the absorption of active components into these cells and hinder or significantly slow down the action of active components inside the cell.

The stated lozenge is made as follows.

One part chamomile flowers by weight and one part calendula flowers by weight are ground. The resulting powder is placed in an ultrasonic extractor with four parts by weight distilled water at a temperature of 15-25°C, and the mixture is heated to 30°C. The mixture is then held for ten minutes while being exposed to ultrasonic waves in the 80 kHz range. The temperature is maintained at 30°C, and the ultrasonic treatment is stopped. The mixture is then cooled to 18-20°C. The cycle of heating the mixture to 30°C, holding with ultrasonic treatment, and cooling to 18-20°C is repeated at least five times, for a total of five cycles. Thus, chamomile and calendula extract are obtained. Chamomile and calendula extract in the amount of 9.5-10% by weight of the required amount for the production of a batch of lozenges is heated to a temperature of 30 - 40°C, borax (sodium tetraborate) is added to it in the form of crystals in the amount of 0.2 - 0.3% by weight of the required amount for the production of a batch of lozenges, and mixed until the borax is completely dissolved.

Next, prepare the fat base by heating the butter in an amount of 15-15.5% by weight of the amount required to produce a batch of lozenges to a temperature of 70-120°C. Heating is carried out in a ceramic or enamel container, less preferably in a stainless steel container. Vaseline is added to the butter in an amount of 55-56% by weight of the amount required to produce a batch of lozenges, and sperm whale lard in an amount of 3-3.2% by weight of the amount required to produce a batch of lozenges.

When the dynamic viscosity of the said mixture of butter, petroleum jelly and lard reaches 0.8-1 centipoise (cP), begin to stir the said mixture, for example, with a stainless steel spatula, and reduce the temperature to 40-65°C.

Then, tar in an amount of 0.75 - 0.8 wt% of the required amount for the production of a batch of lozenges and mometasone in an amount of 0.002 - 0.003 wt% of the required amount for the production of a batch of lozenges are added to the mixture of butter, petroleum jelly and lard at a temperature of 40-65°C.

The resulting mixture of butter, petroleum jelly, lard, tar and mometasone is cooled to a temperature of 25-35°C.

After which, vitamin A concentrate is added to the resulting mixture in an amount of 0.07 - 0.08 wt% of the required amount for the manufacture of a batch of lozenges, sanguinarine hydrogen sulfate in an amount of 0.01875 - 0.02 wt% of the required amount for the manufacture of a batch of lozenges, chelerythrine hydrogen sulfate in an amount of 0.01875 - 0.02 wt% of the required amount for the manufacture of a batch of lozenges, dexpanthenol in an amount of 0.4 - 0.5 wt% of the required amount for the manufacture of a batch of lozenges, methyluracil in an amount of 0.9 - 1 wt% of the required amount for the manufacture of a batch of lozenges, sea buckthorn oil concentrate in an amount of 3.8-4 wt% of the required amount for the manufacture of a batch of lozenges, dry extract of eucalyptus globulus leaves in an amount of 0.125-0.15 wt% of the required amount for the manufacture of a batch of lozenges, an aqueous extract previously obtained in the described method chamomile and calendula with borax dissolved in it, olive oil in an amount that supplements the required amount for the production of a batch of lozenges up to 100% by weight.

All the above ingredients are mixed into a mixture of butter, petroleum jelly, lard, tar, and mometasone, using a stainless steel spatula, for example, until a homogeneous mass is obtained. The resulting mixture is then poured into a flat tray to obtain a layer of the desired thickness, gradually cooled to 0 to -20°C, and maintained at this temperature for 24 hours. The resulting flat sheet, which hardens in the tray, is then removed and cut into lozenges of the desired shape and size.

Thus, the declared lozenge is produced with a balanced content of fatty and water phases.

The lozenges obtained in this manner can be stored outdoors at a temperature not exceeding 25°C. However, to ensure the sterility of the lozenges, it is preferable to store them in sealed packaging, such as blister packs. The plastic strength of the lozenges obtained in this manner, measured using a Vicat apparatus, ranges from 25 to 40 kPa, depending on the rate of temperature reduction.

The most preferred lozenge shapes are the rectangular lozenge shown in Fig. 1, for application to long, narrow affected areas of skin, and the oval lozenge shown in Fig. 2, for application to oval or round (essentially tablet-shaped) affected areas of varying sizes. The rectangular lozenges have rounded corners (R) to prevent damage to the skin when the still-solid lozenge is applied to the affected area. The radius of the rounding (R) is essentially irrelevant, but it should not limit the lozenge's area and may be equal to 0.1 times the length of the shorter side of the rectangle. It is important that the lozenge completely covers the affected area and that the sharp corner does not injure the skin when applied to it.

The lozenges can have a thickness h from 1 mm to 5 mm, as shown in Figures 2 and 4. Lozenges with a thickness of 1 mm are suitable for the treatment of uncomplicated diaper dermatitis and the relief of exacerbations of atopic dermatitis. Lozenges with a thickness of 2-4 mm are suitable for the treatment of complicated diaper dermatitis, eczema, and burns. Lozenges with a thickness of 5 mm are suitable for the treatment of purulent processes in poorly healing wounds, animal bites, and deep wounds.

If rapid melting of the lozenge is required, through cylindrical holes (D) should be drilled in the plates, as shown in Figs. 5 and 6. The axis of each hole (D) is perpendicular to the plate surface. Heat from the patient's body penetrates through the hole (D) into the central layers of the lozenge, warming them and accelerating melting. The diameter of the hole (D) can vary from 3 mm to 5 mm. A hole (D) diameter of less than 3 mm will not ensure sufficient heat exchange between the patient's body and the inner layers of the plate to heat them to the melting temperature within 5 seconds, and a hole (D) diameter greater than 5 mm will not significantly accelerate melting of these layers compared to a diameter of 5 mm. The larger the plate surface, the more holes (D) should be drilled.

The claimed lozenge works as follows.

The lozenge is applied to the affected area of skin. The lozenge melts under the influence of body temperature (the melting point of a lozenge is 32-33°C), and its active ingredients penetrate the skin and cells. The lozenges are highly flexible and easily adhere to curved surfaces, especially the buttocks and anal area, and the groin folds in children. The lozenges can also be placed directly into deep wounds.

The influence of the essential properties of the declared lozenge for the treatment of skin diseases and lesions on the achievement of the technical result is confirmed by the following examples.

Three batches of lozenges were prepared for use. Each batch included rectangular and oval-shaped lozenges with varying surface areas from 0.5 ^cm² to 10 ^cm² , with area increments of 0.5 ^cm² .

The first batch of the declared lozenges, 1 mm thick, was manufactured using the method described above with the following content of components, wt%: vaseline - 70, butter - 15, sperm whale lard - 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 plastic strength of the lozenges in this batch was 25 kPa. The lozenges were made in rectangular and oval shapes.

The second batch of the declared lozenges, 2 mm thick, was manufactured using the method described above with the following component contents, wt%: petroleum jelly - 71, butter - 15.5, sperm whale lard - 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 plastic strength of the lozenges in this batch was 30 kPa. The lozenges were made in the shape of rectangles and ovals.

The third batch of the declared lozenges, 5 mm thick, was manufactured using the method described above with the following content of components, wt %: Vaseline - 70, butter - 15, sperm whale lard - 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. The plastic strength of the lozenges in this batch was 40 kPa. The lozenges were made in the shape of rectangles and ovals.

Example 1

A 2-month-old male patient presented with diaper dermatitis manifesting locally: hyperemic, edematous skin, hot to the touch, without disruption of the epidermal integrity, in the groin area, lower half of the buttocks, scrotum, and base of the penis. All of the skin lesions were roughly circular, oval, or elliptical in shape. Five hours after application of the first batch of oval-shaped lozenges of varying sizes, covering the lesions by 1-5 mm, which melted within 1.5 minutes, the swelling and hyperemia in the affected areas had completely subsided, the skin integrity was intact, and there was no localized increase in temperature.

Example 2

A 6-month-old female patient presented with the following local manifestations: skin markedly hyperemic with spots up to 3-3.5 cm in diameter in the perianal area, inguinal folds, and labia majora, with isolated papular elements up to 2 mm in diameter, raspberry-colored, covered with a white, cheesy coating. All of these skin lesions were roughly circular, oval, or elliptical in shape. Six hours after the first application of the second batch of oval-shaped lozenges of varying area, reaching 10-12 ^cm2 , which melted within 1 minute 56 seconds, the papular elements faded, decreased in diameter to 1 mm, hyperemia subsided, and swelling disappeared. After 6 hours of repeated use of the first batch of oval-shaped lozenges of varying area, reaching 10-12 ^cm2 , which melted in 1.6 minutes, the skin was clean and of physiological color.

Example 3

A 34-year-old male patient recovered from surgery for a herniated disc at the L1-L2 level. The wound was covered with a clean surgical dressing. Four sutures were closed, with swelling and moderate hyperemia in the area of one suture. The sutures were straight and roughly rectangular in shape. Twelve hours after topical application of the third batch of rectangular lozenges, which overlapped each suture longitudinally and transversely by approximately 1-3 mm and melted within 3 minutes, there was no hyperemia, no swelling, no hyperemia, no detectable fluctuation, no local skin temperature increase, and a moderate amount of bloody discharge was found on the napkin. Another 12 hours after the dressing with repeated use of the third batch of rectangular lozenges, overlapping each seam in the longitudinal and transverse direction by 1-3 mm, which melted in 3 minutes, the skin in the area of surgical intervention was without pathological changes.

Example 4

A 1.5-year-old patient with atopic dermatitis, exacerbation. Localized areas of hyperemia up to 3.5 cm in diameter with moderate scaling in the center are present in the elbow and popliteal folds. All of these skin lesions are roughly circular, oval, or elliptical in shape. 5.5 hours after using the first batch of oval-shaped lozenges of varying area up to 10 ^cm2 , overlapping the said lesions by 3-7 mm, which melted in 1.6 minutes, there was no peeling, the edges of the hyperemia foci became smoothed and indistinct, 8 hours after using the first batch of oval-shaped lozenges of varying area up to 10 ^cm2 , overlapping the said lesions by 5-8 mm, which melted in 1.7 minutes, the skin had a physiological color, there was no peeling or itching, the skin was smooth and moderately moist to the touch.

Example 5

A 9.5-month-old patient presented with diaper dermatitis complicated by pyoderma. The perianal, infragluteal, and inguinal folds presented with moderate hyperemia and edematous skin, a pustular rash up to 2-2.5 mm in diameter, and isolated papules up to 3 mm in diameter. All of these lesions were roughly circular, oval, or elliptical in shape. After the first application of the second batch of oval-shaped lozenges, varying in size up to 7-8 ^cm2 and overlapping the lesions by 5-8 mm, the lozenges melted within 2.3 minutes. After 3.5 hours, the papules had decreased to 1 mm in size, partially ruptured, and subsided. There was no hyperemia or swelling. Four hours after application of the first batch of oval-shaped lozenges of varying area, reaching 7-8 ^cm2 , overlapping the aforementioned lesions by 6-10 mm, which melted within 1.6 minutes, the remaining pustules had decreased to 1 mm, and there were no papular elements. Six hours after application of the first batch of oval-shaped lozenges of varying area, reaching 7-8 ^cm2 , overlapping the aforementioned lesions by 3-4 mm, which melted within 1.5 minutes, the skin was clean, had a physiological color, and there were no pathological changes in the skin.

Example 6

A 14-year-old patient, following primary surgical debridement (PSD) of a penetrating soft tissue wound on the posterior surface of the leg. A 1.5 cm gaping canal is locally observed. × 0.5 cm, 2.5 cm deep, approximately rectangular in shape. A glass fragment was removed during primary surgical treatment, the wound was flushed with octenisept, there was no bleeding, and tetanus vaccinations were administered according to schedule. Using sterile tweezers, under local anesthesia with lidocaine spray, four rectangular lozenges from the first batch, measuring 1 x 0.5 cm (with a surface area of 0.5 cm), were inserted into the wound.²) one on top of the other along the entire length of the wound, allowing the wound to be treated without leaving pockets, and the upper lozenge melted in 2.5 minutes, after which the edges of the wound were pulled together with surgical tape. After 12 hours, when re-dressing, there were no local signs of inflammation, the wound depth was about 1.5 cm, when squeezing the soft tissues, the remains of melted lozenges with a few drops of ichor were released from the wound, the wound was treated with octinecept, one rectangular lozenge of the third batch measuring 1 × 0.5 cm (with a surface area of 0.5 cm) was immersed in the wound²), which melted within 3 minutes, the edges were pulled together with surgical tape. After 12 hours, there were no signs of inflammation on the re-dressing, the wound remained 0.5 cm deep and 1.5 cm x 0.3 cm in area. One rectangular lozenge from the third batch, measuring 1 x 0.5 cm (with a surface area of 0.5 cm), was applied over the wound.²), after the lozenge had partially melted after 1.7 minutes under the influence of body temperature and the molten mass had penetrated the wound, the edges were pulled together with surgical tape. After 12 hours, the locally damaged skin measuring 1.0 cm x 0.2 cm and 0.2 cm in depth was present on the dressing, with no signs of inflammation or pathological separation. One rectangular lozenge from the second batch measuring 1 x 0.5 cm (with a surface area of 0.5 cm) was placed on the brought together edges of the wound.²) and secured with surgical tape (the time it took for complete melting was not recorded). After 12 hours, a delicate, pale pink scar measuring 1.5 x 0.1 cm was observed, with no signs of soft tissue inflammation. A follow-up soft tissue ultrasound was performed, which revealed no pathological changes.

Thus, thanks to the selected composition of components that form a homogeneous mass, and their content in the claimed lozenge, the claimed lozenge is capable of treating diseases and skin lesions, including diaper dermatitis and deep wounds, into which the lozenge can be dipped without any instruments. In addition, the lozenge is made in a form distributed over the area of a solid dose, capable of clinging to the surface of the patient's body and melting at his body temperature.

Claims (7)

1. A lozenge for the treatment of skin diseases and lesions selected from atopic dermatitis, diaper dermatitis, wounds, made in the form of a plate from the following components, in the following content, wt.%: Vaseline 55-56 bay oil (butter) 15-15.5 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 hydrogen sulfate 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 globulus leaves 0.125-0.15 aqueous extract of chamomile and calendula flowers 9.5-10 olive oil the rest 2. A lozenge according to item 1, characterized in that the plate has a rectangular shape. 3. A lozenge according to item 1, characterized in that the plate has an oval shape. 4. A lozenge according to item 1, characterized in that the plate has a thickness of 1-5 mm. 5. A lozenge according to item 2, characterized in that the corners of the plates are rounded. 6. A lozenge according to claim 1, characterized in that at least one through hole is made in the plate.