RU2517520C1 - External therapeutic agent for patients suffering from atopic dermatitis - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: agent contains 0.2% Pyriton, an emulsifier, an emollient - isopropyl myristate, and a solvent. The emulsifier is presented by glycerol cocoate PEG-7; the emollient is presented by triglycerides of caprylic and capric acids; the solvent is water. Besides, the agent additionally contains glycerol, cyclomethicone, urea, allantoin and a flavouring agent. All the ingredients of the agent are taken in certain mass ratio.

EFFECT: invention enables eliminating side effects, recovering physiological properties of skin and providing high patient's satisfaction upon completion of the treatment.

1 tbl, 1 ex

Description

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

Known means for external use in the treatment of atopic dermatitis in the form of aerosols.

One of these preparations is Skin-cap aerosol (trade name SKIN-KAP) for external use in the form of an oily solution from white with a yellow tint to light yellow with a characteristic odor. 100 g of the composition includes: the active substance - zinc pyrithione activated 0.2% and auxiliary substances - sodium lauryl sulfate, isopril myristate, ethanol and propellants (isobutane, propane and butane) (Instructions for medical use of the drug Skin-cap aerosol, “Kheminova Internacional S.A. Macarena, 14, 28016 Madrid, Spain, General Representative - INVAR LLC, Moscow, Russia, ATX code: D11AX12, registration number P N012231 / 03, 03/10/2005, INVAR 2006-2012 website - WebProvision )

However, this drug can cause allergic reactions in people with hypersensitivity to certain components of the drug, in patients with atopic dermatitis - hyperemia and burning (hypersensitivity to Skin-cap aerosol) (Kulagin V.A., Shekrota A.G., Pavlova O .V., Nikiforova GD, Arutyunova ES Nonsteroidal external therapy with activated zinc pyrithione of atopic dermatitis and psoriasis in children. Pediatrics named after GN Speransky, 2005; 6: 57-61).

Another external agent in the form of an aerosol and the closest composition to the claimed is an aerosol for external use of TsINOKAP in the form of an oily liquid from white to light yellow in color with a specific odor, including 2 mg (0.2%) zinc pyrithone and excipients: sodium lauryl sulfate , isopropyl myristate is an element, silicon dioxide colloidal (aerosil) is an emulsifier, dexpanthenol (D-pathenol), polysorbate 80 (tween 80) is an emulsifier, ethanol (rectified ethyl alcohol) is a solvent and tetrafluoroethane (freon 134) (Instructions for p the use of the drug TsINOKAP, Pharmstandard-LEXREDSTVA OJSC, Russia, ATX code: D11AX12, registration number LSR-010497/08, 12/24/2008 - Medical reference book. Drug catalog. site: medicalhandbook.ru | catalog-lekarstv / 03/12/12 ) is a prototype.

This drug is used in the treatment of psoriasis, atopic dermatitis, seborrheic dermatitis, however, it can also cause allergic reactions and is not well tolerated by patients. So, according to A.A. Tikhomirov and N.G. Short (2011) when using Tsinokap aerosol in patients with atopic dermatitis, the drug intolerance phenomena were observed, which led to the cessation of treatment; some patients had a burning sensation of the skin after applying the drug, its “satisfactory” tolerance was revealed in 15.8% of patients, and in 10.5% the tolerance was assessed as “bad” (Tikhomirov A.A., Korotky N.G. Atopic dermatitis in children - the strategy and tactics of rational pharmacotherapy. -Questions of practical pediatrics. 2011; 6 (2); 58-62).

With a high probability, the cause of the formation of adverse events and poor tolerance of Tsinokap aerosol is the presence of HFC 134a and ethanol (rectified ethyl alcohol) in its composition, which actively evaporate when exposed to atopic dermatitis on the patient’s inflamed skin, causing additional irritation and dryness.

The objective of the invention is to develop a composition for external therapy for patients with atopic dermatitis in the inter-relapse period, providing anti-inflammatory and at the same time moisturizing, protective and softening effect on the skin of patients with atopic dermatitis.

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 pyrithone 0.2%, an emulsifier, an isopropyl myristate emulsifier and a solvent, glyceryl cocoate PEG 7 is used as an emulsifier, caprylic and capric acid triglycerides are additionally used as an emulsifier, water is used as a solvent, and glycerin, bee-methicone, urea, allantoin and flavor are additionally added in the following ratio of components, wt.%:

Zinc pyrithione - 0.2 PEG glyceryl cocoate - 7-9.0 Glycerol - 2.0 Cyclomethicone - 2.0 Urea - 1.5 Isopropyl myristate - 1.0 Caprylic and triglycerides capric acid - 1.0 Allantoin - 0.5 Flavoring - 0.08 Water - the rest

The invention consists in a combination of these components.

The use of glyceryl cocoate PEG-7 as an emulsifier provides the mixing of aqueous and fatty components of an external therapy.

The use of caprylic and capric acid triglycerides, along with isopropyl myristate, not only creates a protective film on the skin, but also gives the skin a feeling of softness and silkiness.

The use of glycerin in the composition is used to moisturize the skin, does not cause complications from the liver and kidneys, and also does not cause allergies.

The use of cytoclomethine provides skin nutrition, and allantoin has a softening effect on the skin.

Urea in the composition of external therapy is used as an additional active substance - keratolytic.

Fragrance is introduced into the composition to give a pleasant smell.

The use of water as a solvent is necessary for the formation of an optimal consistency.

The qualitative and quantitative composition of the components of the funds are selected experimentally.

From the analysis of scientific, technical and patent literature, the claimed combination of components that provide anti-inflammatory moisturizing, protective and softening effects on the skin of patients with atopic dermatitis in the inter-relapse period without side effects, we have not revealed that allows us to draw conclusions about the compliance of the proposed solution with the criteria of "novelty" and "Inventive step". The invention is as follows. On the scales set 2 chemical glasses. 165.0 g (82.72 wt.%) Of water, 4.0 g (2.0 wt.%) Of glycerol, and 1.0 g (0.5 wt.%) Of allantoin are poured into the first glass. PEG-7 glyceryl cocoate 18.0 g (9.0 wt.%) Was added to the second glass; cyclomethicone 4.0 g (2.0 wt.%); isopropyl myristate 2.0 g (1.0 wt.%); caprylic and capric acid triglycerides 2.0 g (1.0 wt.%) and urea 3.0 g (1.5 wt.%).

To the contents of 1 glass (with the aqueous phase) add the contents of the second glass (with the fat phase) and mix them. After the emulsion is prepared, 0.16 g (0.08 wt.%) Of flavoring and 0.84 g of a 48% suspension of zinc pyrithione are added (which corresponds to 0.2 wt% of pure zinc pyrithione) and mixed. Thus prepared external product is placed in polymer bottles with a dispenser and used to treat patients with atopic dermatitis.

To determine the characteristics of the therapeutic effect of the new external agent and its tolerance parameters, the “Clinical trial participant questionnaire of the new agent for patients with atopic dermatitis in the inter-relapse period” was used, which provides an assessment of skin characteristics and the severity of possible side effects when using the new external agent, for a total of 12 signs with objective clinical data using visual analogue scales (VAS) from 0 to 10 points (Danilycheva I.V., Ilyina N.I. Quality of life in patients urticaria and atopic dermatitis. Consilium Medicum. 2001; v. 3 (No. 4); p. 184-186).

The claimed external therapy agent (in the form of a spray) was used to treat patients with mild atopic dermatitis in the inter-relapse period (n = 13), while the standardized SCORAD disease severity index before treatment was 7.4 ± 1.8 points. The comparison group consisted of patients with mild atopic dermatitis, before the start of therapy, the average group index SCORAD was 7.7 ± 1.3 points, that is, it did not statistically differ from the index of the main group. Patients of the comparison group as an external agent used Tsinokap aerosol (prototype). After completing a 4-week course of therapy, the residual symptoms of atopic dermatitis were evaluated by the attending physician in both groups and the subjective assessment of patients underwent external treatment was studied, with an assessment of the compliance factors of therapy.

Clinical example

Patient K-s, 23 years old, a system administrator, suffers from blood pressure from a year of age, when he began to appear and often (2-4 times a year) to recur manifestations of blood pressure in the face, neck, and upper extremities. He was treated at the pediatrician's place of residence, hormonal creams and ointments (usually alklomethasone) were used externally for long courses with a moderate effect. From the age of 15, a diagnosis of bronchial asthma has been established, with which the patient is observed by a specialist allergist. Skin manifestations from adolescence recur 1-2 times a year in the form of acute eczema of the hands, which is a typical manifestation of the adult phase of blood pressure.

The process with a small lesion area (2.0% of the body surface), mild, with the registration of the SCORAD index from 6.2 to 8.0 points). During an exacerbation, the clinical picture is dominated by the phenomena of hyperemia, swelling, focal wetness, and itching of the skin. The patient categorically refuses treatment with hormonal agents (corticosteroid creams and ointments), uses only herbal remedies in the form of lotions and baths, after which he notes a decrease in itching and hyperemia, however, he complains of dry skin and a feeling of tightness.

Another exacerbation - in August 2012, the treatment undertaken - without effect. The patient was prescribed the claimed external agent in the form of a spray 2-3 times a day on the rear skin of the hands. On the 3rd day, there was a decrease in hyperemia and swelling in the foci, areas of weeping regressed. The use of local irrigation with a new external agent in the form of a spray was continued for up to 4 weeks. Clinical observations and the results of a patient survey (see table) showed that the use of a new external agent contributed to a complete regression of the symptoms of the disease, was characterized by the absence of undesirable consequences in the form of dryness, peeling, and skin tightening. The patient actively expressed his opinion about the good tolerability of the new agent, about the convenience of its use (the absence of an excessive fat film on the skin surface), as a result of which the use of the new agent was continued in a single application regimen once a day). Currently, the clinical remission of dermatosis in the patient persists for 3 months.

The results of comparative studies to evaluate the characteristics of the skin, side effects and tolerance when using the claimed external funds in the form of a spray and aerosol Tsinokap (prototype) are shown in the Table.

Table Symptoms (% of patients) The inventive tool (spray)
N = 13 Aerosol Tsinokap N = 13 According to time estimates Dryness 7.7% 23.1% Skin tightness 7.7% 30.8% Itching - 7.7% Skin burning - 15.4% Skin redness - 15.4% Skin swelling - 7.7% Skin peeling 7.7% 23.1% Small abscesses - - A patient General discomfort - 23.1% Drug tolerance is excellent, good 92.3% 69.2% Satisfaction with the use of the drug 100.0% 73.3% Overall patient satisfaction with skin properties after treatment 100.0% 69.2%

Comparative studies revealed a significant superiority of the new external agent, when using it in patients with blood pressure 4.0 times less than with Tsinokap aerosol treatment, a feeling of skin tightening was recorded; 3.0 times less often - dryness and peeling of the skin. The new tool did not lead to the appearance of itching, burning, redness and swelling of the skin, while Tsinokap aerosol caused the indicated phenomena. According to patients, the use of a new external agent (in the form of a spray) did not cause discomfort, while the means of comparison caused this condition in 23.1% of patients. The new external agent is characterized by excellent and good tolerance (92.3%), high satisfaction with the use of the drug and overall satisfaction of the patient with skin properties after treatment (100%).

Claims (1)

An external therapy for patients with atopic dermatitis, including 0.2% pyrithone zinc, an emulsifier, isopropyl myristate emollient and a solvent, characterized in that it contains PEG 7 glyceryl cocoate as an emulsifier, additionally contains caprylic and capric triglycerides as an emulsifier, as a solvent - water and additionally contains glycerin, cyclomethicone, urea, allantoin and flavor in the following ratio, wt.%:
Zinc pyrithione - 0.2 Glyceryl cocoate PEG-7 - 9.0 Glycerol - 2.0 Cyclomethicone - 2.0 Urea - 1.5 Isopropyl myristate - 1.0 Caprylic and triglycerides capric acid - 1.0 Allantoin - 0.5 Flavoring - 0.08 Water - the rest