RU2611347C1 - Personal hygiene agent with acaricidal activity on mite demodex - Google Patents

Abstract

FIELD: pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry and represents personal hygiene agent with acaricidal activity on mite Demodex, containing water as solvent, foaming agent sodium laureth sulphate, preservative, biologically active component – birch tar, flavoring agent, consistence amplifier and extracts, characterized by, that device additionally contains detergent Chegina K 40GLO, as amplifier of foam and thickener Emanon XLf, emulsifier, thickener and fatter Amidet N and Amidet B 112, as preserving agent – Mikroker DN, Apricot perfume as flavoring agent, as plant extracts – extract of Chamomile, tickseed herb extract, tansy herb extract, verbena herb extract, wherein ingredients in preparation are taken in certain proportions, wt%.

EFFECT: invention provides care of hair and human body, as well as high acaricide therapeutic effect on mites Demodex.

1 cl, 2 ex, 1 tbl

Description

The invention relates to pharmacy and can be used for the preparation of personal care products used both for hair, face and body care, and in the complex treatment of demodicosis

Demodecosis is a chronic parasitic disease of the skin of humans and mammals, widespread in all climatic zones of the globe, caused by the tick demodex folliculorum and demodex brevis. Parasitizing in the sebaceous, meibomian glands of the eyelids and eyelash follicles, the tick causes, in addition to blepharitis, symptoms such as blepharoconjunctivitis, episcleritis and even keratitis, eyelash loss. The penetration of a tick into the hair follicles of the skin is accompanied by the phenomena of dermatitis of various intensities and localizations.

Demodecosis of the eyelids is often combined with demodicosis of the skin of the face, demodecosis of the skin of the face with damage to the scalp. One of the characteristics of the physiology of ticks is the ability to migrate. Often, ticks from their main reservoir - the external auditory canal of the ears, earwax migrate to the eyelids, eyebrows and to adjacent areas of the skin of the face, neck and head. Such migration helps maintain local foci of demodicosis, and non-compliance with basic personal hygiene measures promotes repeated self-infection, as there is no immunity to demodicosis in humans.

Moreover, it is well known that treatment of demodicosis should be complex, including both local effects and effects on the patient’s body (see Sirmays N.S., Abesadze G.A., Ustinov M.V. “Demodecosis: pathogenetic aspects in various dermatoses faces. ”Moscow, 2013, pp. 17-22). According to this source of information, 3 groups of agents are used for the treatment of demodicosis: 1 - means of care and prevention (Demoten gel, soap, sulfur, cream, ointment); 2 - local therapy (antibacterial agents, antiprotozoal agents, glucocorticosteroids); 3 - systemic drugs - antibiotics, antiprotozoal drugs (metronidazole).

The choice of care and prevention is determined by the localization of the pathological process. For demodecosis of the skin of the face, Demoten gel is used, for blepharic demodecosis - Blefarogel gel, for demodecosis of the scalp - soaps, shampoos, gels.

There are many local therapies containing metronidazole, for example, Demalon ointment as a treatment for blepharitis (patent RU 2126668). This ointment has a significant drawback - a high concentration of metronidazole (up to 50%), which leads to side effects in the form of hyperemia and edema of the skin of the eyelids and conjunctival mucosa, itching or heaviness in the eyes of patients. The patent (RU 2192860) describes an ointment, including metronidazole (5.0-15.0%), proteoglycan aggregates (APGs), disaccharides, lanolin, vegetable oil, distilled water. However, these ointments based on metronidazole have weak acaricidal activity and cause irritation and toxic-allergic reactions. In addition, these ointments cannot be used to treat (for) demodecosis of the scalp. Good acaricidal efficacy was found in herbal formulations (see, for example, patents: RU 2313356, 2007; 2000; RU 2315614, 2006; RU 2227025, 2004). These agents are also recommended only for the treatment of demodicosis of the eyelids and face and cannot be used to treat scalp.

A large number of tar shampoos are known for the treatment of scalp “Tar Shampoo” for oily hair (http://www.dermosil.ru/ru/products/), Dermozil shampoo http://www.dermosil.ru/blog / = 3063, Shampoo "DEST" http://librederm.ru/shampun-degot/. These funds can also be used to care for the scalp with demodicosis of the scalp. However, none of these shampoos is recommended as a topical treatment for demodicosis.

It is known that the treatment of demodicosis should be comprehensive, including both local effects and effects on the patient’s body (see Sirmays N.S., Abesadze G.A., Ustinov M.V. “Demodecosis: pathogenetic aspects in various dermatoses of the face” Moscow, 2013, pp. 17-22). According to this source of information, 3 groups of agents are used for the treatment of demodicosis: 1 - means of care and prevention (Demoten gel, soap, sulfur, cream, ointment); 2 - local therapy (antibacterial agents, antiprotozoal agents, glucocorticosteroids); 3 - systemic drugs - antibiotics, antiprotozoal drugs (metronidazole). The choice of care and prevention is determined by the localization of the pathological process. For demodecosis of the skin of the face, Demoten gel is used, for blepharic demodecosis - Blefarogel gel, for demodecosis of the scalp - soaps, shampoos, gels.

Closest to the claimed technical solution is a shampoo described in RF patent No. 2259812, which includes water, a foaming agent, a thickener, citric acid as an acidity regulator, a preservative - methyl paraben, wood tar, flavoring and a consistency enhancer, additionally contains water-alcohol or water - alcohol-glycerin or propylene glycol extracts of birch buds and leaves, and as a biologically active substance - tar birch tar. Components are taken in a specific proportion. Shampoo has anti-inflammatory, antimicrobial, wound healing properties and can be used for eczema, dermatitis, seborrhea, psoriasis. The patent shows the effectiveness of treatment with the described means of acne, dermatitis of various etiologies, accompanied by itching of the skin of the body and head. Despite the fact that the patent does not contain information about the direct use of this agent for demodicosis, the presence of a therapeutic effect for dermatitis of various etiologies suggests that it can be used as a care agent for dermatitis caused by Demodex ticks, since this agent is the most common cause dermatitis (Demodex tick is found in almost every person). The disadvantage of this known tool is that it cannot provide an effective destructive effect on the Demodex tick, since it contains no substances that contribute to the expansion of pores of the skin and thereby increase the transport of active components deep into the skin to create increased concentrations of active substances, as well as for mechanical tick elimination. In addition, water-alcohol-glycerin or propylene glycol extracts of birch buds and leaves, which are part of the shampoo, have only a weak anti-inflammatory effect, but do not have a detrimental antiparasitic effect on the Demodex tick. Essentially, tar is the only component of a known acaricidal agent. Tar, as it was found when using it as part of various means without combining it with other therapeutic components, also does not provide a cure for a person from demodicosis.

The technical result of the claimed invention is the development of a tool used not only as a personal care product for hair and body care, but also as a local therapy with a higher acaricidal therapeutic effect due to its better penetration to the localization of Demodex mites - follicles and sebaceous glands of the skin, as well as due to a more effective destructive effect on the tick, in combination with an effective high degree of mechanical removal of ticks from the entire surface to Ms. person. A higher therapeutic acaricidal effect of the proposed agent is also ensured by the fact that it helps to break the vicious chain: it eliminates the ticks experience on large areas of the scalp, neck, chest and eliminates the possibility of re-infection of already cured skin areas. This technical result is achieved by the fact that in the well-known personal care product with acaricidal activity against the Demodex mite containing water as a solvent, the detergent in the form of a detergent is sodium laureth sulfate, a preservative, tar birch tar, flavor and consistency enhancer, the agent additionally contains Chegina detergent K 40GLO, as an amplifier for foam and thickener Emanon XLf, as an emulsifier, thickener and survivor Amidet N and Amidet B 112, as a preservative - Microker DN, as a flavoring agent - perfume apricot, chamomile herb extract, grass succession extract, birch tar, tansy extract, verbena extract with the following ratio of ingredients, wt. %:

sodium sulfate laureth 8.0-10 Chegina K 40GLO 1.5-2.0 Emanon XLf Surfactant 2.1-2.5 Amidet n 2.1-2.2 Amidet B 112 1.0-1.5 Microker DN 1.4-1.7 Sodium Chloride 2.0-2.5 perfume Apricot 2.4-2.6 chamomile herb extract 2.9-3.1 string herb extract 2.9-3.1 tar birch 0.28-0.32 tansy extract 0.28-0.32 verbena extract 0.28-0.32 water up to 100

It is known that verbena strengthens and cleans arterial and venous vessels, restores damaged capillaries, the drug improves blood microcirculation in tissues, restores blood circulation, normalizes metabolic processes at the cellular level (see instructions for dietary supplements Verbena Newman Nutrients AG, Russia http: / /medhall.ru/verbena/). In addition, it suppresses the phenomena of eczema, psoriasis, and upset.

The anti-inflammatory and anti-allergic properties of the series, which are used for dermatitis of various origins, diathesis, and others, are well known. Tansy has a very wide range of healing properties. It has antihelminthic, detoxifying, anti-inflammatory, diaphoretic and wound healing properties. In some countries, such as Belgium and France, tansy is officially recognized as an anthelmintic. It is used in everyday life due to its insecticidal effect: it saves from annoying insects (flies, bugs, moths, fleas). It is enough to sprinkle the powder of tansy with meat - and the flies will not even come close to it. And if you put a bunch of flowers in the room, then the annoying flies will leave him for a long time. These properties of tansy are due to the presence of thujone, a very toxic compound, in the composition of its essential oils. In addition, tansy contains essential oil, which includes camphor and other substances, as well as flavonoids, alkaloids, bitter substance tanacetin, organic acids, tannins, resins, sugar, gum, B vitamins, carotene, vitamin C. In the leaves and inflorescences contain flavonoids, alkaloids, tannins and bitter substances (see http://www.ourpmc.com/pizhma).

We believe that the action of the proposed personal care products with acaricidal activity is based on the combined use of components that have a multilateral combined synergistic effect.

- Birch tar has an antiparasitic effect, destroying adult individuals, larvae and eggs of the tick, showing an antibacterial effect. At the same time, skin turgor improves, the production of sebum, oiliness of the skin decreases, the effects of hyperkeratosis and inflammation are leveled.

- The extract of tansy ordinary has antiparasitic, antibacterial and insecticidal effects, eliminating pustular skin lesions, destroying mature mites and associated bacteria.

- The grass string and its extract are famous for their anti-allergic effect. Its pronounced dermatropia is known: it is effective for diathesis in children, psoriasis, various dermatoses, and promotes the healing of small wounds. The extract of the series cleanses the surface of the skin and promotes the healing of affected areas of the scalp.

- Verbena extract has therapeutic efficacy in dermatoses - scabies, psoriasis, eczema, as well as a wound healing effect due to the normalization of cell metabolism.

- Chamomile extract helps to subside inflammatory phenomena on the skin and at the same time has an insecticidal effect. Chamomile extract cleanses and softens the surface of the skin.

The tool is prepared as follows.

Preparation of the product is carried out in a stainless steel reaction apparatus with a rotational speed of 40-60 minutes.

The supply of components and their processing in the reaction apparatus is carried out in the following sequence.

The calculated amount of surfactants and the calculated amount of water are poured from the measuring device into the reaction apparatus. Include a stirrer mounted on the reaction apparatus. Further, all operations for the preparation of the agent are carried out with a constantly working stirrer until all components are fully incorporated.

After the introduction of surfactants, the contents of the reaction apparatus are mixed for 25-30 minutes until a homogeneous mass is formed.

Tar birch tar, tansy extract and verbena extract are mixed with a thickener emanon, mixed until a homogeneous mass and placed in the reaction apparatus.

The contents of the reaction apparatus are stirred for 15-20 minutes.

Thickeners are added to the reaction apparatus and mixed for 15-20 minutes.

After all the components are included in the composition, add the calculated amount of extracts and mix for another 10-15 minutes.

The last operation is the addition of sodium chloride to the desired viscosity and its complete dissolution.

The stirrer is stopped, a product sample is taken for analysis for compliance with technical specifications.

After receiving positive test results confirming the compliance of the product with the regulatory indicators of table 1, the finished product is sent to the packaging, capping and packaging department.

The above method was prepared composition No. 1, which contained the following number of ingredients:

sodium sulfate laureth 8.0 Chegina K 40GLO 1,5 Emanon XLf Surfactant 2.1 Amidet n 2.1 Amidet B 112 1,0 Microker DN 1.7 Sodium Chloride 2.5 perfume Apricot 2.6 chamomile herb extract 3,1 string herb extract 2.9 tar birch 0.28 tansy extract 0.28 verbena extract 0.28 water up to 100

The above method was prepared composition No. 2, which contained the following number of ingredients:

sodium sulfate laureth 10, Chegina K 40GLO 2.0 Emanon XLf Surfactant 2.5 Amidet n 2.2 Amidet B 112 1,5 Microker DN 1.4 Sodium Chloride 2.0 perfume Apricot 2,4 chamomile herb extract 2.9 string herb extract 3,1 tar birch 0.32 tansy extract 0.32 verbena extract 0.32 water up to 100

The above method was prepared composition No. 3, which contained the following number of ingredients:

sodium sulfate laureth 9.0 Chegina K 40GLO 1.75 Emanon XLf Surfactant 2.2 Amidet n 2.15 Amidet B 112 1.3 Microker DN 1,5 Sodium Chloride 2,3 perfume Apricot 2.5 chamomile herb extract 3.0 string herb extract 3,1 tar birch 0.30 tansy extract 0.30 verbena extract 0.30 water up to 100

In separate experiments, the effect of the constituents of the claimed composition on the acaricidal activity of the proposed drug was investigated.

It was found that the lack of content in the claimed tool of any of the ingredients: chamomile, string, tansy or verbena, even if tar is present in it, does not provide the therapeutic acaricidal effect that is associated with their combined use. The same acaricidal effect was expressed much weaker if the amount of tar, chamomile, string, tansy or verbena was taken less than the declared. The acaricidal effect can be explained by the fact that the listed components, having anti-inflammatory, antibacterial and anti-allergic effects, contribute to the reduction of exudative phenomena, thereby ensuring better penetration of the main acaricidal ingredients - tansy and tar to the place of mite localization. In addition, the best penetration of an agent containing acaricidal and detergents (detergents) to the place where ticks are located provides not only the best acaricidal action, but also the best mechanical removal of mature and immature individuals from the large surface of the skin with foaming agents. It is known that since ticks migrate over the entire surface of a person’s body, when applying only traditional local treatment, for example, with demodicosis of the eyelids, they easily re-enter the “treated” places and re-infect. The possibility of processing with the claimed means a large area of the body and head with one hygienic means allows you to break this vicious circle, which leads to a radical fracture in the treatment of this disease.

These formulations were tested for acaricidal activity.

Example 1

Patient B., 45 years old. Diagnosis: seborrheic demodicosis. Complaints of redness of the face, eyelids, scalp, itching. According to the patient, the duration of the disease is 2 years. Objectively: T-shaped hyperemia of the face, teleangectasia, combs. Around the mouth intense redness, isolated pustules. A scraping was taken from the surface of the skin of the forehead, cheeks, near-mouth, scalp, and ear passages. Microscopy of scraping the skin of the forehead, cheeks, near-mouth, scalp. Examined for the presence of Decomodex eyelashes. The study found a large number of mature individuals (from 3 to 12) in all samples, including those taken from the scalp and eyelids. Diagnosis: demodicosis.

Assigned to a prescription composition No. 2. The product was applied to all of these areas, rubbed into the skin, and then washed off with warm water. The edges of the eyelids were treated with an alcohol-containing solution of eucalyptus and cream "Demazol". Additionally, antibiotics and metronidazole were prescribed. The treatment was carried out for 45 days.

After the end of treatment it was stated: hyperemia of the skin of the face and scalp, eyelids disappeared. Under microscopy, the number of ticks in scrapings of the scalp ranged from 0 to 1, the forehead skin - 0-1.

It was concluded that a good clinical outcome was achieved.

The tool was used in patients suffering from various forms of demodicosis.

Example 2

Patient S., 55 years old. Complaints of dandruff and itching of the scalp, behind the ear, forehead, cheeks. Sick for more than 2 years. She was treated with sulfur talkers. Objectively: examined for the presence of the Demodex folliculorum tick and eyelashes. The study found a large number of mature individuals (from 3 to 5) in all samples, including those taken from the scalp of the eyelids, from the external auditory canals.

Assigned to a prescription composition No. 2. The product was applied to all of these areas, rubbed into the skin, and then washed off with warm water. The edges of the eyelids were treated with an alcohol-containing solution of eucalyptus and cream "Demazol". The treatment was carried out for 45 days. Additionally, the patient took metronidazole

The number of ticks after treatment in the scrapings of the scalp was 0-1, in the scrapings of the ear canals and behind the ear areas - 0, in the scrapings of the forehead and eyelids 0-1 and 0, respectively.

Comparative tests were carried out on the therapeutic effect of the claimed agent and the known Stop Demodex agent in 3 groups of patients with common demodecosis of the scalp, face and eyelids. Each group included 7-8 people.

The 1st group of patients was daily treated with shampoo on the basis of the claimed funds. For this, shampoo was applied daily to the hair and skin of the face, neck and décolleté, as well as to the external auditory canals. The tool is well rubbed into the treated areas. Maintained for 1-2 minutes and then washed off with warm water. The tool was used to obtain a persistent clinical cure for patients. The edges of the eyelids were treated with an alcohol-containing solution of eucalyptus and cream "Demazol".

The 2nd group of patients was daily treated with shampoo containing, in addition to a foaming agent, thickener, acidity regulator, preservative, extracts of birch buds and leaves, and birch tar in the form of a biologically active substance. This shampoo was prepared by the authors on the basis of the components of the claimed shampoo, however, instead of plant extracts according to the inventive tool, it used an extract of birch leaves and buds. Shampoo was applied daily to the hair and skin of the face, neck and décolleté, as well as to the external auditory canals. Well rubbed, kept for 1-2 minutes and then washed off with warm water. Shampoo was used to obtain a persistent clinical cure for patients. The edges of the eyelids were treated with an alcohol-containing solution of eucalyptus and cream "Demazol".

In the 3rd group of patients, Stop Demodex line products were used. Stop Demodex is a therapeutic cosmetic line, which is based on components traditionally used to treat demodicosis - metronidazole, sulfur, birch tar. It includes Shampoo Lotion Stop Demodex (skin care product), Shampoo Stop Demodex - for the care and local treatment of the scalp, Balm Stop Demodex and Gel Stop Demodex. Balm Stop Demodex (also called "cream" or "ointment") is a therapeutic drug against demodicosis (a local therapy drug), the action of which is based on a combination of birch tar, metronidazole and a number of plant components (chamomile, apple tree leaves, willow bark, rose petals, calendula). Gel Stop Demodex is used to treat demodecosis of the eyelids and to treat blepharitis that develops against the background of demodecosis (as a means of local therapy). Its main active ingredients are metronidazole, chamomile extract and hyaluronic acid, peppermint extract and glycerin. Stop Demodex lotion was used as a means of care and prevention for demodecosis in order to cleanse the skin, and also as a base before applying other means of the treatment line - balm or gel. They were daily rubbed on their face and other affected areas with a cotton pad.

Patients with advanced demodecosis of the scalp, face and eyelids were prescribed: daily shampooing with Stop Demodex shampoo, daily face skin rubbing with Stop Demodex Lotion and Balsam, and gel wiping with Stop Demodex Gel. Additionally, metronidazole was prescribed.

As follows from table 1, the duration of the preservation of clinical symptoms of the disease in patients of the 1st group was on average 45 days, while these periods in patients of the 2nd group were longer and amounted to an average of 70 days, and in patients 3 group I symptoms of the disease persisted 60 days. The number of Demodex ticks that we found in the scrapings taken on the 10th, 20th, and 30th day of use turned out to be that in patients of the 1st group who used the claimed tool, the number of ticks was lower compared to patients who used shampoo as based on birch extracts leaves and buds, and those who used the Stop Demodex complex.

The above observations clearly demonstrate the effectiveness of the use of the claimed funds for the treatment of demodicosis and its advantages over previously known drugs for a similar purpose.

Claims (2)

Personal hygiene product with acaricidal activity against Demodex mites, containing water as a solvent, a foaming agent in the form of a detergent, sodium laureth sulfate, a preservative, a biologically active component - tar birch, flavoring, consistency enhancer and plant extracts, characterized in that the product additionally contains detergent Chegina K 40GLO, as a foam enhancer and thickener Emanon XLf, as an emulsifier, thickener and cure agent Amidet N and Amidet B 112, as a preservative - Microker DN, as a flavor Ator - Apricot flavoring as extracts of plants - chamomile extract grass grass succession extract, tansy extract of herbs, grasses verbena extract with the following ratio of ingredients, wt. %: sodium sulfate laureth                                                             8.0-10 Chegina K 40GLO                                                                        1.5-2.0 Emanon XLf Surfactant                                                                         2.1-2.5 Amidet n                                                                                     2.1-2.2 Amidet B 112                                                                                     1.0-1.5 Microker DN                                                                        1.4-1.7 Sodium Chloride                                                                         2.0-2.5 perfume Apricot                                                                         2.4-2.6 chamomile herb extract                                                            2.9-3.1 string herb extract                                                             2.9-3.1 tar birch                                                                         0.28-0.32 tansy herb extract                                                             0.28-0.32 verbena herb extract                                                             0.28-0.32 water                                                                                                 up to 100