RU2407535C2 - Biologically-active agent for dermatoses treatment - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention refers to medicine, namely to balneology, and aims at dermatoses treatment. A biologically-active agent for dermatoses treatment containing an aqueous extract of peat mud extracted from peat mud in sodium hydrocarbonate mineral water, the emulsifying agent 'Blanoze™ Cellulose TaM - (7HF)', arabinogalactan in the certain ratio.

EFFECT: agent exhibits the improved therapeutic effect.

1 tbl, 3 ex

Description

The invention relates to medicine, namely to balneology, and can be used for the treatment and prophylaxis of various forms of dermatoses as an immunocorrective agent both in medical institutions and at home.

The prior art means of immunostimulating therapy for the treatment of dermatoses based on biologically active peat fractions in the form of mud bath preparations (www.binorm-spa.ru). The disadvantage of these funds is the creation of special conditions for performing medical procedures, significant economic costs, certain difficulties for the nursing staff, the inability to perform procedures at home, as well as the insufficiently high efficiency of medical procedures.

It is known a tool with a wide spectrum of action (antiviral, bactericidal anti-inflammatory, immunomodulatory and antitumor effects) for the treatment of various diseases in the form of 40% alcohol tincture containing peat, coal, garlic, rose hips and honey bee, while the ratio of water-alcohol mixtures to the composition of the active components 10: 1. The tool can be used both orally and for external use (RU, p.2149637, A61K 35/10, A61K 35/64). The disadvantage of this tool is the large number of components that complicate the cooking technology, as well as the presence of alcohol, which limits the range of users

In addition, it is known that it has an anti-inflammatory and wound healing effect for the treatment of ultraviolet dermatitis, which is an ointment containing sodium humate powder from lowland wood-grass peat of the Tomsk Region, polyethylene glycol with a molecular weight of 400 and 1500, dimexide and drinking water (RU, p. 2316331, A61K 35/10, A61P 17/00).

The ointment does not cause allergic reactions, however, a significant disadvantage of this tool is the low permeability of the ointment through the skin and, in addition, the structure of the drug in the form of an ointment is inconvenient for use, since it takes considerable effort to evenly distribute it on the skin when applied to a diseased skin surface patient bring additional pain. The disadvantage is the limited raw materials for the main active component, the powder of sodium humate, which increases economic costs.

The closest technical solution to the claimed is a tool for the treatment of patients with chronic dermatoses using peat oxidate in common heat baths and applications (RU, p.2187315, A61K 35/10, A61P 37/04) Since peat oxidate was originally intended for use in crop production in order to increase productivity, the technology for its preparation does not provide sufficient purity in its use for treating people and, as a result, the low efficiency of the drug. The disadvantages include the possibility of using it only in medical institutions

The technical result of the claimed technical solution is to expand the range of effective therapeutic agents based on peat preparations and the possibility of using them both in medical institutions and at home).

The technical result is achieved by the fact that the biologically active agent for treating dermatoses contains a biologically active peat fraction in the form of an aqueous extract of peat mud obtained by extraction of peat mud with hydrocarbonate sodium mineral water, and additionally contains the Blanose ™ Cellulose Gam- (7НР) emulsifier and arabinogalactan filler, in the following ratio, wt.%

Blanose ™ Cellulose Gam- (7HP) 1.95-2.0.5 Arabinogalactan, 2.90-3.10 Peat Mud Water Extract rest

The aqueous extract of peat mud used in the inventive product is an environmentally friendly product of natural origin, containing humic and fulvic acids, nitrogen-containing and protein substances, cellulose derivatives and a large number of trace elements and minerals. The main biological value of the extract is humic acids, which have high biological activity, antimicrobial, biostimulating, anti-inflammatory properties, suppress the vital activity of pathogenic microflora, activate metabolism, carbohydrate and protein metabolism. The presence of a large number of organic substances with preservative properties allows you to get a fairly highly stable gel-like structure without the presence of an additional preservative.

The therapeutic effect in the treatment of dermatoses is associated with the amphiphilic features of the applied concentrated aqueous extract of peat mud obtained by extracting peat mud with mineral hydrocarbonate sodium water, which inhibits the vital processes of pathogenic microorganisms and nourishes the affected skin with essential amino acids, vitamins, enzymes, etc. It is such an extract of peat mud, transformed into a gel form, by diluting in it an emulsifier of the Blanose ™ brand of cellulose GAM (7 HF) that allows you to deposit enzymes, amino acids, vitamins and hormones into the patient’s body through the pore openings of the skin, which are part of the extract. The hydrophilic system of the drug with signs of polyelectrolytes and micromosaic heterogeneity in the human body provides the restructuring of the immune-biological processes through complex "two-part" neural-humoral reactions and leads to the formation in the patient with dermatosis of a persistent and long-term state of non-specific increased resistance to negative external influences.

In addition, cellulose derivatives of an aqueous extract of peat mud enhance the stability of the gel structure of the claimed composition, that is, the aqueous extract enhances to some extent the role of an emulsifier.

The arabinogalactan introduced into the composition of the drug basically contains macromolecules, which are formed by units of galactose and arabinose monosaccharides. In the claimed amount during mixing, in combination with amino acids and vitamins of the peat mud water extract, arabinogalactan not only enhances the exchange potential of a homogeneous mass, but also leads to a state of critical micelle formation concentration (CMC). At concentrations below CMC, the active substance of the drug is in a molecularly dissolved state and exhibits the properties of ordinary electrolytes; with increasing concentration, aggregation occurs in micelles, while a small part of the surface active substances of the drug (carboxylic acids, as well as citric, acetic, oxalic and alcohols) continue to remain in the solution of the drug in the liquid phase, which allows maintaining the acidity of the skin surface in the pH range from 4 up to 6. The “acid mantle" of the skin is to a certain extent regarded as a protective mechanism against invasive microorganisms. The acid gradient in the stratum corneum of the skin contributes to the process of exfoliating horn plates and replacing them with new ones. This is due to the controlled destruction of desmosomes in the stratum corneum. With slightly alkaline values of the surface of the skin, diseases associated with violation of the skin barrier, such as atopic dermatitis and some others, usually begin to manifest.

The presence of micelles - supramolecular structures in the patented preparation provides human skin integument with the solution of physiological problems in the separation of the aqueous phase of the body and the air environment. The microscopically thin and specifically organized stack of lipid biolayers of the stratum corneum of the human skin with high immune status is successfully coping with this problem of efficient separation of the two media. Under other conditions, when the keratinocyte membranes involved in the formation of the lipid barrier at the stage of the basal skin cells are not suitable for organizing extended lipid layers of the stratum corneum, a person is forced to use emulsifiers. The bulk of the emulsifiers on the market today is made from lipids dispersed in the aquatic environment through the formation of micellar structures, often leading to negative consequences. The least harm to the skin is caused by emulsifiers, whose structure is similar to that of the lipid barrier itself. The basis of such emulsifiers are mainly bilayer (lamellar) micelle structures. For the most part, the formation of a lamellar liquid crystal phase, consisting of parallel biolayers of surfactant lamellas alternating with layers of water, is most typical for preparations of a humic nature when they reach CMC. Moreover, the sugar-containing substances of arabinogalactan are structurally related to biological membranes of the stratum corneum of the skin and can participate in the activation of the process of their regeneration.

Thus, by dissolving cellulose and arabinogalactan in an aqueous extract of peat mud, it was possible to activate the galactose and arabinose arabinogalactan macromolecules by substances of a humic nature by imparting a significant degree of branching to them, since only in their branched region localization of immunodeterminant groups occurs. formulations of the purified cellulose preparation allowed to stimulate the immune response through deposition into the cellular structures of the muscle mass of a patient with dermatosis the body to neutralize and suppress such manifestations as lichenoid papule - a kind of dermatosis ..

The drug is prepared as follows.

Example 1

Arabinogalactan 30 g, Blanose ™ Cellulose Gam- (7НР) 20 g and an aqueous extract in the amount of 950 g are placed in a homogenizer and stirred at room temperature until a homogeneous composition is obtained. A dark brown gel-like preparation was obtained with sanitary-microbiological indicators that comply with sanitary rules and norms (SanPiN 1.2681-97).

Example 2

The preparation is prepared according to example 1 with the addition of arabinogalactan 29 g, Blanose ™ Cellulose Gam- (7HP) -19.5 g and an aqueous extract up to 1 kg of the total mass.

Example 3

The preparation is prepared according to example 1 with the addition of arabinogalactan 31 g, Blanose ™ Cellulose Gam- (7НР) -20.5 g and an aqueous extract up to 1 kg of the total mass.

All the obtained compositions in examples 1-3 have a uniform gel structure, have storage stability and biological activity.

The inventive tool has passed clinical trials at the Department of Dermatovenereology and Physiotherapy, Khabarovsk State Medical University. Given positive feedback on the test results.

Examples of the use of the drug

The drug was used in the form of lotions and compresses in 24 patients with eczema and exudative neurodermatitis in the phase of increasing phenomena and weeping. The temperature of the compress and exposure were determined by the nature of the inflammatory reaction. With applications, the skin warms up, causing the expansion of capillaries, blood and lymph vessels, not only at the site of application of the drug, but throughout the body. Biologically active substances (histamine, acetylcholine, serotonin, etc.) are formed in the skin, which enter the bloodstream and are delivered to their destination. At the same time, external heat leads to irritation of the receptors of the skin and mucous membranes. Information about such irritation is transmitted to the central and vegetative parts of the nervous system. After processing the information, a neurohumoral response of the body is formed with the participation of the endocrine, immune and other systems. After 3-4 applications, a regression appeared in the foci, the scales departed. By the 8-10th session, the plaques were flattened, and by 20-25 they either resolved, or a small infiltration remained in their place. Side effects and allergic reactions during drug treatment have not been recorded. Other examples are given in the table.

Table of comparative results of the treatment of dermatoses using the claimed composition and prototype. Patient diagnosis Treatment result prototype The claimed composition 1. Torpid form of psoriasis Shared baths. Recovery and significant improvement in 51%. patients and an improvement in the skin process of 48.3% of individuals on average within 29.03 days. The reduction in the length of hospital stay was 10-12 days. Applications. Recovery and significant improvement in 53%. patients and improvement of the skin process of 49% of individuals on average within 25.5 days. The reduction in the length of hospital stay was 12–13 days. Normalization of the proliferative activity of the epidermis was noted. Thus, the index of labeled nuclei in the biopsy of patients decreased from 15.02 ± 0.55% to 5.9 ± 0.42% (control - 3.9 ± 0.43%) 2. Atopic dermatitis Shared baths. Duration of treatment is 3 weeks. 92% of the children were discharged in a state of marked improvement in the clinical skin process (an obvious decrease in lichenification infiltration in the lesion foci) and general condition (disappearance of irritability, normalization of sleep). Applications. The duration of treatment is 2.5 weeks. 95% of patients were discharged with positive dynamics of functional parameters. The capacitive resistance of the epidermis increased from 39.6 ± 9.7 to 51.4 ± 10.2 srvc. (control 61.5 ± 14.2). pH decreased from 6.9 ± 0.4 to 6.3 ± 0.3 3. Subacute allergic dermatitis Shared baths. The phenomenon of dermatitis disappeared or decreased in 12 patients after taking 10 daily baths, in 5 patients there was a noticeable improvement in the skin process Local applications. The phenomenon of allergic dermatitis disappeared or decreased after administration in 14 patients after taking 6-8 daily procedures. 4. Soaking eczema Local applications. Of 18 patients, 14 patients received a quick antiexudative effect within 3-4 days with the need for further anti-inflammatory therapy Local applications. After 3-4 applications, regression appeared in the foci, by the 8th session they were flattened, and by 20 they resolved. No further anti-inflammatory therapy needed

Claims (1)

A biologically active agent for treating dermatoses, including a biologically active peat fraction, characterized in that it additionally contains the Blanose ™ Cellulose Gam- (7HF) emulsifier and arabinogalactan filler, and as a biologically active peat fraction, an aqueous extract of peat mud obtained by extraction of peat mud with hydrocarbonate sodium mineral water in the following ratio of components, wt.%:
Blanose ™ Cellulose Gam- (7HF) 1.95-2.05 Arabinogalactan 2.90-3.10 Peat Mud Water Extract Rest