RU2293557C2 - Agent for topical using in treatment of skin and mucosa tissue disease - Google Patents

Abstract

FIELD: medicine, dermatology, pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to an agent used for topical using in treatment of skin and mucosa tissue diseases. Agent is made as a gel and contains 2-ethyl-6-methyl-3-oxypyridine succinate as an active component, hydroxyethylcellulose or carboxymethylcellulose sodium, or hydroxypropylcellulose as a gel-forming agent, and succinic acid and distilled water also taken in the definite ratio. Agent promotes to effective treatment of skin and mucosa tissue damages, among them complicated by suppurative-inflammatory processes, trophic ulcers, burns, wounds, hemorrhoid, anal fissure, mouth cavity inflammatory diseases, parodontium and parodontitis.

EFFECT: valuable medicinal properties of agent.

4 cl, 2 ex

Description

The invention relates to the pharmaceutical industry, in particular to the creation of a gel for topical application in the treatment of injuries of the skin and mucous membrane, trophic ulcers, wounds, burns, damage to the skin, complicated by purulent-inflammatory processes.

A large number of topical drugs are known in the form of various dosage forms: ointments, emulsions, applications, gels.

Ointments are known that contain substances that have an antimicrobial effect, for example, synthomycin, tetracycline, gentomycin and others (Kotelnikov V.P., Wounds and their treatment, M., Knowledge, 1991; Kuzin M.I. Wounds and wound infection, M. , Medicine, 1990).

The disadvantage of these ointments is the unidirectionality of their action - antimicrobial. They have limitations for use because of their individual intolerance, as well as the danger of developing side effects with prolonged use - reducing the sensitivity of microflora, impaired function of internal organs.

Multicomponent ointments on an osmotically active basis have a complex effect on the wound surface - Levomikol, Sulfamikol and Levosin (Mashkovsky MD Medicines, M., Medicine, 1995, v.2).

However, these ointments contain antibacterial and sulfamide preparations and have side effects.

Known wound healing agent - "Vitamustin-gel" (RF patent No. 2185149 from 2002), containing a gelling agent, purified mummy and distilled water.

As a gelling agent, in some cases polysaccharides (galactomannan or glucomannan or hyaluronic acid) can be selected, in other cases gelatin or pectin, or aerosil, or zeolites.

The disadvantages of the above gel composition include the manifestation of an allergic reaction due to mummies and therefore this gel can only be used in a limited number of patients in the treatment of damage to the skin and mucous membranes of various origins.

The objective of the present invention is to provide a highly effective wound healing agent with a pronounced wound healing effect in the 1st, 2nd and 3rd phases of the wound healing process.

The problem is achieved by the fact that the proposed tool for local use in the treatment of diseases of the skin and mucous membranes, made in the form of a gel and containing the active substance - 2-ethyl-6-methyl-3-hydroxypyridine succinate, the gelling agent - hydroxyethyl cellulose or sodium carboxymethyl cellulose, or hydroxypropyl cellulose , succinic acid and distilled water in the following ratio of ingredients, wt.%:

active substance 1-7 gelling agent 1-5 succinic acid 0.1-1.0 distilled water rest

The tool can be intended for the treatment of skin damage, including complicated by purulent-inflammatory processes, trophic ulcers, burns (including sun, radiation, etc.), wounds, as well as in the treatment of hemorrhoids, anal fissures and can be used for treatment of inflammatory diseases of the oral cavity, periodontitis, periodontal disease.

The tool is prepared as follows:

1. Dissolve in 445 g of distilled water at room temperature and stirring 50 g of the substance 2-ethyl-6-methyl-3-hydroxypyridine succinate and 5 g of succinic acid until the solution is completely transparent (about 15 minutes);

2. in 480 g of distilled water, heat to 70 degrees and with vigorous stirring, pour 20 g of hydroxyethyl cellulose into parts and mix for 2 hours until the system is completely transparent and uniform;

3. add to the solution prepared according to claim 2, a solution of the substance and succinic acid prepared according to claim 1 with vigorous stirring for 10 minutes;

4. Cool the resulting gel to room temperature.

pH of the resulting gel = 5.5-6.2.

As the gelling agent, either sodium carboxymethyl cellulose, or hydroxypropyl cellulose, or hydroxyethyl cellulose can be used.

Ways of application:

1. Dressing method: the gel was applied to burn wounds and an aseptic gauze dressing was applied on top (dressings every other day);

2. Open method: the gel was applied to burn wounds in the area of exposed skin (face, neck, hands) 2-3 times a day.

Clinical trials were conducted on volunteers:

1. in patients with superficial (II-IIIA) degree burns;

2. in patients with long-term non-healing (residual) burn wounds.

For the treatment of superficial burns with an area of 4 to 10% bp the gel was used in 11 patients aged 23 to 42 years; 4 of them used the dressing method, and 7 - the open one. All patients noted wound healing in a shorter time (6-8 days) from the moment of injury than when using standard procedures and drugs (8-14 days). Significantly reduced inflammation, swelling, accelerated reparative processes; Subjectively, a significant decrease or disappearance of pain was noted. The epithelization of the sites where the gel was applied occurred 2-3 days earlier than in the case of using standard methods and drugs. There were no complications when using the gel.

For the treatment of long-term non-healing wounds, the gel was used in 6 patients aged 27 to 64 years with burns of 10-50% bp, burn disease, wound depletion. The use of the gel began 12-14 days after the injury, after the staged surgical treatment of deep burns. Already by the 3rd day after the start of application of the gel, pronounced macrophage activation, proliferation of fibroblasts and angiogenesis, growth of granulation tissue, which by the 5th day matured and acquired a regular structure with all layers: fibrinous-leukocyte, vascular arches, vertical vessels, horizontal, were noted fibroblasts. Moreover, earlier than in patients for whom the gel was not used, marginal epithelium regeneration began, which actively continued by 7-10 days, ending by 15 days with complete epithelialization of wounds due to marginal epithelial regeneration, concentric scarring in a shorter time (on 3-4 days earlier) than in the group of patients who received standard therapy.

In all patients, the use of the gel was combined with hydrotherapy (washing wounds with antiseptics, detergents).

Purulent complications, bacterial proteolysis in this group of patients were not noted; at the same time, 2 cases of purulent complication were noted in the control group. Patients did not notice subjectively unpleasant sensations in the field of gel application.

In addition, the gel can be successfully used for infectious-inflammatory, ulcerative-necrotic, trophic diseases of the oral mucosa; stomatitis of various etiologies, gingivitis, periodontitis, damage to the mucous membrane when wearing dentures, injuries of the oral mucosa and surgical interventions.

Mode of application:

The gel composition is the same as for the treatment of wounds and burns, i.e. 5%.

Locally, 2-3 times a day after eating and before bedtime, the gel in an amount of about 1 g is squeezed onto a clean finger and rubbed with light massage movements into the affected area of the mucous membrane. For periodontal diseases, the gel is injected into the gingival pockets or applied in the form of compresses, or gently rubbed into the gums 3-4 times a day. The duration of treatment is 7-12 days, depending on the type and severity of the disease.

Clinical examples:

1. Patient B. And / b No. 64. Age 48 years old. Diagnosis: chronic generalized periodontitis of moderate severity. The treatment was carried out using 5% gel for 12 days by carefully rubbing it into the gums 3 times a day and 1 time using a compress with gel.

As a result of treatment, the depth of the periodontal pocket was significantly reduced until it was completely closed, the microcirculation of blood in the gums was restored, the bleeding of the gingival grooves stopped, and the gingival margin was marked. The mucous is pink. According to clinical data, there was a significant improvement in the condition of the mucosa and tissues of the oral cavity.

The biochemical parameters of mixed saliva have also changed. The concentration of MDA (malondialdehyde) after treatment decreased significantly: before treatment, it was 0.81 nmol / ml, after treatment - 0.24 nmol / ml; SOD (superoxide dismutase) activity increased: before treatment - 35.05 U / mg protein, after treatment - 63.1 U / mg protein.

Over the next 2 months of observation (remission period), exacerbation of periodontitis was not observed.

2. Patient K., 54 years old. Diagnosis: moderate gingivitis. The gel was treated for 10 days by gently rubbing it into the gums 2 times in the afternoon after eating and at night.

As a result of the treatment, the color and structure of the gums were restored, the bleeding and soreness of the gums stopped after eating and brushing, the gums inflammation and swelling, plaque completely disappeared.

In the next 2 months of observation, exacerbation of the disease was not noted.

During dental examinations, allergic manifestations in the oral cavity were not detected.

The technical result achieved by using the proposed tool is to quickly eliminate inflammatory processes. On the 2-3rd day of its use, a decrease in soreness, swelling is noted, the condition of the affected tissues is significantly improved, the time of epithelization is accelerated. At the same time, the gel has no contraindications, is harmless, does not cause allergic reactions, has no contraindications for age groups. In addition, it does not require additional use of other drugs, incl. antibacterial drugs, etc.

The gel has a wide spectrum of action and functionality, shows a pronounced therapeutic effect in the treatment of various injuries of the skin and mucous membrane - wounds, cracks, pressure sores, trophic ulcers of various origins, superficial burns of 1-3 degrees, radiation injuries, eliminates microdamages of the skin, which are cosmetic defects, improves the structure of the skin and can be used in medicine and cosmetology.

Claims (4)

1. The tool for local use in the treatment of skin and mucous membranes, characterized in that it is in the form of a gel and contains the active substance 2-ethyl-6-methyl-3-hydroxypyridine succinate, gelling agent-hydroxyethyl cellulose or sodium carboxymethyl cellulose, or hydroxypropyl cellulose, succinic acid and distilled water in the following ratio of ingredients, wt.%: Active substance 1-7 Gelling agent 1-5 succinic acid 0.1-1.0 Distilled water Rest 2. The tool according to claim 1, which is intended for the treatment of damage to the skin and mucous membranes, including complicated by purulent-inflammatory processes, trophic ulcers, burns, wounds. 3. The tool according to claim 1, which can be used in the treatment of hemorrhoids, anal fissures. 4. The tool according to claim 1, which can be used in the treatment of inflammatory diseases of the oral cavity, periodontitis, periodontal disease.