WO2014025290A1

WO2014025290A1 - External therapy remedy for patients with atopic dermatitis

Info

Publication number: WO2014025290A1
Application number: PCT/RU2013/000670
Authority: WO
Inventors: Николай Васильевич КУНГУРОВ; Екатерина Леонидовна ХАРСЕВИЧ; Наталья Владимировна ЗИЛЬБЕРБЕРГ; Муза Михайловна КОХАН; Андрей Станиславович ГАВРИЛОВ; Наталья Петровна ЕВСТИГНЕЕВА
Priority date: 2012-08-10
Filing date: 2013-08-02
Publication date: 2014-02-13
Also published as: RU2496476C1

Abstract

The invention relates to medicine, and specifically to dermatology, and can be used for treating patients with atopic dermatitis. The external therapy remedy for patients with atopic dermatitis comprises the following components: 0.20% by mass of zinc pyrithione, 1.50% by mass of urea, 3.00% by mass of glyceryl stearate, 3.00% by mass of emulsified wax, 0.50% by mass of triethanolamine, 3.00% by mass of cocoa butter, 1.00% by mass of corn oil, 5.00% by mass of mineral oil, 3.00% by mass of triglycerides of caprylic acid and capric acid, 2.00% by mass of cyclomethicone, 2.00% by mass of glycerin, 0.25% by mass of Carbopol, 0.10% by mass of peachy fragrance, with the remainder being drinking water. This external remedy is characterized by exceptional and effective tolerability (93.3%), high patient satisfaction from use of the preparation and general patient satisfaction with their skin properties after treatment (100% and 93.3%, respectively).

Description

OUTDOOR THERAPY FOR PATIENTS

ATOPIC DERMATITIS

The invention relates to medicine, namely to dermatology and can be used to treat patients with atopic dermatitis.

Currently, there are a large number of ointments and creams with absorbable and anti-inflammatory effects used in various clinical forms of atopic dermatitis.

One of such agents is an agent for atopic dermatitis, containing dry dropsy extract, a solution of 5% vitamin E oil, anhydrous lanolin, sunflower oil and distilled water at a certain ratio of components (RU, patent N ° 2028150, IPC A61K35 / 78, publ. 02/09/1995).

The disadvantage of this composition is the presence of anhydrous lanolin, which often causes allergic reactions, manifested in the form of redness and itching of the skin.

A known combination comprising pyrrolidone-5-carboxylic acid and at least one compound of citrulline, arginine and asparagine for the treatment of atopic dermatitis (RU, patent application N ° 2009147465/15, IPC A61KZ 1/198, publ. 27.06. 2011).

Since these components are only moisturizers that contribute to the preservation of moisture in the stratum corneum, therefore, they do not affect other layers of the skin. Therefore, the use of only moisturizing components as active substances calls into question the effectiveness of the treatment of atopic dermatitis.

Also known is an anti-inflammatory and antipruritic cream for the treatment of dermatological diseases, containing, as an active component, gamma-b-glutamylhistamine and a base comprising at least one of the oil components (olive oil, oil sunflower oil, vaseline oil), cosmetic stearin, emulsifier, emulsion wax, triethanolamine, vitamin A, distilled glycerin, antioxidant, preservative, tea tree oil and purified water at certain ratios (RU, patent N ° 2233152, IPC A61K7 / 48, A61K7 / 00, A61K9 / 06, A61K35 / 70, published on July 27, 2004).

This composition is not effective enough due to the use of stearin as a base. Stearin forms an impermeable film, thereby blocking the restoration of the skin’s own lipid balance, leaving a feeling of “greasy” skin, which reduces the compliance of the therapy.

The closest is a cream for external use - ZINOKAP (CINOCAP) 0.2%. As auxiliary substances, it includes macrogol cetostearate (emulsifier), cetostearyl alcohol (emulsifier), liquid paraffin (liquid paraffin) (propylene glycol (humectant), dexapanthenol (active substance), sodium dihydrogen phosphate dihydrate and sodium hydrogen phosphate) (Instructions for use of the drug TsINOKAP, Pharmstandard-Tomskkhimfarm OJSC, 201 1g., ATX code: D1 1AX12, registration JN LSR-010496/08, 12.24.08) - prototype.

This cream has anti-inflammatory, antibacterial and antifungal activity, however, the mechanism of anti-inflammatory action has not been studied, allergic reactions are possible.

The objective of the invention is to develop a cream for external use, providing a moisturizing, anti-inflammatory and softening effect on the skin of patients with atopic dermatitis in the inter-relapse period.

The technical result that will be achieved from the use of this invention is to eliminate side effects, restore the physiological properties of the skin and to ensure high patient satisfaction after treatment. The technical result is achieved by the fact that in an external therapy for patients with atopic dermatitis, including zinc pyrithione in an amount of 0.2%, the active substance, emulsifiers, emollients, moisturizer and water, urea is used as the active substance, glyceryl stearate is used as an emulsifier, emulsion wax and triethanolamine, as emollients - cocoa butter, corn oil, mineral oil, triglycerides of caprylic and capric acids and cyclomethicone, as a moisturizer - glycerin. In addition, carbopol and peach flavor are further added. The components are taken in the following ratio, wt.%:

Zinc pyrithione - 0.20

Urea - 1.50

Glyceryl stearate - 3.00

Emulsion Wax - 3.00

Triethanolamine - 0.50

Cocoa Butter - 3.00

Corn oil - 1, 00

Mineral oil - 5.00

Caprylic Triglycerides

and capric acid - 3.00

Cyclomethicone - 2.00

Glycerin - 2.00

Carbopol - 0.25

Peach Flavor - 0.10

Drinking water - the rest.

The invention consists in a combination of these components.

The use of urea as an active substance (along with zinc pyrithione) provides kerotolytic and penetrating effects, affecting keratin, improves the penetration of zinc pyrithione into the deeper layers of the skin, and since urea is part of the skin's NMF (Natural Moisturizing Factor), its small amounts help to retain its own moisture in the upper layers of the epidermis.

The use of glyceryl stearate, emulsion wax and triethanolamine as emulsifiers contributes to the activation of zinc pyrithione, since these emulsifiers are cationic.

The use of cocoa butter, corn oil, mineral oil, triglycerides of caprylic and capric acid and cyclomethicone as emollients not only creates a protective film on the skin, but also gives the skin a feeling of softness and silkiness.

Using glycerin as a moisturizer serves to moisturize the skin, does not cause complications from the liver and kidneys, and also does not cause allergies.

Introduction to the composition of the claimed funds carbopol, which is a gelling agent, is necessary for the formation of the optimal consistency.

Peach flavoring is necessary to create a gentle light fruity aroma to improve the organoleptic properties of the cream.

The qualitative and quantitative composition of the components of the drug are selected experimentally and provides a moisturizing, anti-inflammatory and softening effect on the skin of patients with atopic dermatitis and psoriasis in the inter-relapse period without side effects.

The invention is as follows.

On the scales set 3 chemical glasses. 151.2 g (75, 45 mass%) of water, 4.0 g (2.0 mass%) of glycerol and 0, 125 g are poured into the first glass (0.25 wt.%) Carbopol. 6.0 g of emulsion wax (3.0

mass%); glyceryl stearate 6.0 g (3.0 wt.%); mineral oil 10.0 g (5.0 wt.%); cocoa butter 6.0 g (3.0 May.%); corn oil 2.0 g (1.0 wt.%); caprylic and capric triglycerides 6.0 g (3.0 wt.%); cyclomethicone 4.0 g (2.0 wt.%) and urea 3.0 g (1.5 wt.%). Triethanoamine 0.6 g (0.5 wt.%) Is placed in a third glass.

The first and second glasses (with the aqueous and fat phase, respectively) are heated to a temperature of 80 ° C, then the fat phase is added to the water (in the first glass) and mixed. The resulting mass is homogenized and then cooled. In the process of cooling, triethnolamine is added and constantly stirred until thickened. After cooling the resulting mass, add 0.3 g (0.1 wt.%) Of peach flavor and 0.417 g of a 48% suspension of pyrithione zinc (which corresponds to 0.2 wt% in terms of pure zinc pyrithione) and mix.

Thus prepared external agent was used to treat patients with atopic dermatitis.

Example: Patient Ts-va, 19 years old, a student, suffers from blood pressure from 3 years of age, has been under the dispensary registration at UrNIIDViI for the past 5 years. Marks exacerbations of the disease of mild to moderate severity (SCORAD index from 6.9 to 7.5 points) after contact with household chemicals and in the autumn and winter, when rashes appear in the form of diffuse hyperemia and swelling, the formation of small cracks and erosion, severe itching in the area of the hands and arms, on the skin of the face and neck. When resolving inflammatory manifestations, dryness of the skin, tightness is significantly enhanced, and small-plate peeling appears. For many years, with an exacerbation of the process, she used topical corticosteroid drugs, but in the last year she refused to use them due to fear of possible topical complications (steroidophobia). From the designated in January 2012, the Tsinokap cream refused by the attending physician due to increased itching and dry skin after 7 days of using the drug.

The last typical exacerbation of blood pressure (SCORAD index 6.7 points) developed after contact with washing powder. The patient was prescribed a new external agent 2 times a day on the skin in the face and hands. The use of a new external agent was carried out for 20 days, after which all symptoms regressed (for a list of symptoms, see the Table). The patient noted the excellent tolerability of the drug, was satisfied with the properties of the skin after treatment, since dryness and tightness of the skin were completely absent; the use of the drug was continued in a maintenance mode (2 times a week), clinical remission of blood pressure remains.

This external agent was used to treat patients with mild atopic dermatitis (n = 15), while the standardized SCORAD disease severity index before treatment was 8.1 ± 1.3 points. The comparison group (according to the prototype) was composed of patients with mild atopic dermatitis, before the start of therapy, the average group index SCORAD was 8.3 ± 0.9 points, that is, it did not statistically differ from the index of the main group. For patients of the comparison group, Zinocap cream was used as an external agent. After a 4-week course of therapy in both groups, the residual symptoms of atopic dermatitis (BP) were evaluated by the attending physician and the subjective attitude of the patients to the external treatment was studied (therapy compliance factors).

A comparative assessment of the characteristics of the skin, side effects and tolerance when using the claimed external funds and cream Tsinokap (prototype) are shown in the table. Table

Comparative studies revealed a significant superiority of the new external agent, when used in patients with blood pressure 1.5 times less than peeling with Tsinokap cream, peeling of the skin was observed 2 times less, residual dryness of the skin and its redness were recorded, and constriction was observed about 4 times less skin, completely absent itching, burning and swelling of the skin.

According to patients, the new external agent was characterized by excellent and good tolerance (93.3%), high satisfaction with the use of the drug and overall satisfaction of the patient with skin properties after treatment (100% and 93.3%, respectively).

Claims

CLAIM

An external therapy agent for patients with atopic dermatitis, including zinc pyrithione in an amount of 0.2%, active substance, emulsifiers, emollients, moisturizer and water, characterized in that urea is used as the active substance, glyceryl stearate, emulsion wax are used as emulsifiers and triethanolamine, as emollients - cocoa butter, corn oil, mineral oil, triglycerides of caprylic acid and capric acid, cyclomethicone, glycerin as a humectant, and additionally contains carboprl, peach flavor p in the following ratio of components, wt.%: