RU2778503C1 - Composition for hygienic treatment of the eyelids - Google Patents

Abstract

FIELD: ophthalmology, hygiene and cosmetology.

SUBSTANCE: invention relates to ophthalmology, hygiene and cosmetology. The composition for hygienic treatment of the eyelids contains the following ratio of components, wt.%: sodium salt of hyaluronic acid 0.50–3.00, silver glycinate 0.25–1.00 or natural calendula flower water 100% hydrolat 1.00–10 .00, dexpanthenol 0.50–6.00 or sulfoconcentrol 0.60–1.00, purified water and functional additives up to 100.

EFFECT: invention provides effective cleansing and moisturizing of the eyelid surface in various pathological conditions of the eyelids.

2 cl, 6 ex

Description

The invention relates to ophthalmology, hygiene and cosmetology and is intended for hygienic treatment of the eyelids. The composition can be used in the prevention and treatment of blepharitis, dysfunction of the meibomian glands, styes and chalazions, as well as dry eye syndrome.

Diseases of the ocular surface, which include blepharitis, dysfunction of the meibomian glands, and dry eye syndrome, are a social problem, since the incidence of this pathology is, according to various sources, from 50 to 85% of the population (TFOS DEWS II Pathophysiology report / AJ. Bron [et al.] // Ocul Surf. - 2017. - V. 15. - P. 438-510). The number of such diseases is increasing every year, and this is due to several reasons, such as the influence of urban factors (working in an air-conditioned office environment, environmental degradation, daily use of chlorinated water), intensive use of gadgets. An increase in the number of patients suffering from diseases of the ocular surface is also caused by the widespread use of cosmetic procedures in the periorbital region (botulinum toxin for aesthetic purposes, eyelash extensions, eyelid tattooing), as well as ophthalmic surgical interventions, including

blepharoplasty operations (Trubilin V.N., Polunina E.G., Kurenkov V.V., Angelova D.V., Kapkova S.G., Chinenova K.V. Effect of cosmetic procedures in the periorbital region on the organ of vision: a review. Ophthalmology, 2018;15(3):233-241 https://doi.org/10.18008/1816-5095-2018-3-233-241) Brzhesky V.V., Prozornaya L.P., Efimova E. L., Brzheskaya I.V. New possibilities of antibiotic therapy in pediatric and adult ophthalmology. Ophthalmology. 2019;16(1):56-62.https://doi.org/10.18008/1816-5095-2019-l-56-62.

All of the above factors directly or indirectly affect the functional activity of the meibomian glands located in the thickness of the eyelid and producing the lipid component of the tear film, which protects the ocular surface. Increased visual load when working with gadgets reduces the number of blinks, during which the lipid secretion is evacuated from the meibomian glands and distributed over the ocular surface. A decrease in the number of blinks leads to the development of secretion stagnation in the mouths of the ducts of the meibomian glands with the development of a subsequent inflammatory process - blepharitis, meibomitis, barley and chalazions. The use of chlorinated water dries out the skin, including the most sensitive area - the skin of the eyelids. It should be noted that moisturizing this area requires a specialized approach, since the skin of the eyelids in the area of the costal edge of the eyelid passes into the mucous membrane of the eye. The use of cosmetic procedures such as eyelid tattooing and eyelash extensions can directly affect the condition of the eyelids and the functional activity of the meibomian glands, causing inflammation, toxic-allergic reactions, as well as atrophic processes of the meibomian glands. The use of botulinum toxin in the periorbital zone for aesthetic purposes, as well as the use of gadgets, leads to a decrease in the frequency and strength of blinking, and therefore to the development of dysfunction of the meibomian glands.

The basis for the prevention and treatment of meibomian gland dysfunction, which accompanies inflammatory diseases of the eyelids - blepharitis, styes and chalazions, and is also the main factor causing dry eye syndrome, is therapeutic hygiene of the eyelids. This procedure is aimed at restoring the patency of the meibomian glands by eliminating plugs in the mouths of their ducts. This reduces the risk of inflammation of the eyelids, and also promotes the entry of the lipid component of the tear film, which is released from the meibomian glands to the surface of the eye and protects it from drying out. Therapeutic hygiene of the eyelids consists of two stages - warm compresses and self-massage of the eyelids with gel. When performing self-massage of the eyelids, it is necessary to use gels that should moisturize the surface of the eyelids, reduce the risk of microtraumatization of the skin of the eyelid due to the sliding effect, and also help reduce the risk of developing an inflammatory process on the eyelids due to cleansing their surface from scales, crusts, mucus. Hygiene gels are effective for daily use, so a low concentration of preservative is an important factor, which reduces the risk of allergic reactions.

Current skin care products for the face and eyelids often contain hyaluronic acid, which has moisturizing properties by retaining (binding) water molecules, which increases skin firmness and improves its elasticity.

Known cosmetic compositions based on hyaluronic acid that contain Aloe Vera, they are used to obtain moisturizing gels for face and eyelid skin care (US 6007796, 12/28/1999. RU 2114602 C1, 07/10/1998. RU 2174985 C1, 10/20/2001. ).

However, these cosmetics contain the preservative propylparaben, which is toxic and can cause allergic reactions, especially with long-term daily use.

For the treatment of inflammation and infections of the eyelids and eyes, including blepharitis, numerous compositions have been developed containing various drugs as an active ingredient (US 5556848, 1996), (US 5614545, 1997), (US 6174859, 2001). These compositions contain various synthetic and natural ophthalmologically acceptable carriers, including Carbopol and Aloe Vera gel, the latter component often playing an important role in allergic reactions.

Known composition for the care of the skin of the face and eyelids, containing the sodium salt of hyaluronic acid, Aloe Vera, polyvinylpyrrolidone in the following ratio, wt. %.:

Sodium salt of hyaluronic acid 0.01-2.5

Aloe Vera gel or juice 0.1-10.0

Polyvinylpyrrolidone 0.01-2.0

Water up to 100.

(RU 2218907. 12/20/2003) The use of Aloe Vera in this composition may cause undesirable side effects, especially with prolonged use.

The objective of the invention is to create a hypoallergenic composition for hygienic treatment of the eyelids.

The technical result of the proposed composition is the effective cleansing and moisturizing of the eyelid surface in various pathological conditions of the eyelids in the form of blepharitis, meibomitis, barley, chalazion.

The technical result is achieved due to the sodium hyaluronate included in the composition in combination with silver glycinate or calendula hydrolate, dexpanthenol or sulfoconcentrol in certain proportions.

The composition contains sodium hyaluronate, silver glycinate or natural calendula flower water 100% hydrolate, dexpanthenol or sulfoconcentrol in the following ratio of components in wt%:

sodium salt of hyaluronic acid - 0.50-3.00

silver glycinate - 0.25-1.00 or

natural calendula flower water 100% hydrolat - 1.00-10.00

dexpanthenol - 0.50-6.00

or

sulfoconcentrol - 0.60-1.00

purified water and functional additives up to 100

Additionally, the composition contains vitamin B3.

Hyaluronic acid is a non-sulfonated glycosaminoglycan, which is part of the connective, epithelial and nervous tissue, is one of the main components of the extracellular matrix. Due to its high content in the extracellular matrix, hyaluronic acid plays an important role in tissue hydrodynamics, cell migration and proliferation processes, and also participates in a number of interactions with cell surface receptors, in particular with its primary CD44 receptor. The effectiveness of hyaluronic acid is based on the ability to bind moisture - 1 molecule holds up to 1000 water molecules - and to ensure the correct arrangement of the chains of the main skin proteins - elastin and collagen. The list of beneficial effects that hyaluronic acid has on the skin is not limited to moisturizing, there are many more functions - this is skin softening; healing of microcracks, wounds, scars; reduction of inflammation, delivery of nutrients to the deep layers of the skin, creation of a protective barrier against external negative effects.

The sodium salt of hyaluronic acid is able to penetrate the epidermis and form a wider range of positive effects. In addition to moisturizing and all the functions that hyaluronic acid performs, sodium hyaluronate is able to stimulate the production of collagen and elastin, as well as hyaluronic acid itself.

Silver glycinate - obtaining silver compounds to create medicinal and disinfectants against pathogens (bacteria, viruses, etc.) led to their use. Solutions of nitrate and other silver compounds obtained chemically from nitrate or hydroxide, in which silver is in the form of a cation, their properties are well studied and described many times [Scherbakov A.B. Silver preparations yesterday, today and tomorrow. Pharmaceutical Journal, No. 5, 2006, p. 45-57]. Silver compounds with amino acids are of particular interest, since the presence of an amino acid reduces the toxicity of silver already in the chemical compound itself. Such complexes with various amino acids were synthesized from silver nitrate by chemical transformations followed by isolation, purification from impurities, etc. [Kenji Nomiya and Hironari Yokoyama. Syntheses, crystal structures and antimicrobial activities of polymeric silver(I) complexes with three amino-acids [aspartic acid (H2asp), glycine (Hgly) and asparagine (Hasn)] J. Chem. Soc, Dalton Trans., 2002, 2483-2490.] Silver glycinate is used in antiviral and antibacterial compositions as having antiseptic properties (RU 2281107, 04.08.2004, RU 2281107,.20.09.2012).

In the claimed composition, silver glycinate is used for its intended purpose as an antiseptic.

For the same purpose, instead of silver glycinate, you can use natural calendula flower water 100% hydrolate, obtained in the process of water-steam distillation of calendula officinalis flowers. 100% calendula hydrolate does not contain artificial additives, dyes and preservatives, is saturated with valuable water-soluble components contained in plants: essential oils, organic acids, vitamins, etc., contains about 0.2-0.5%) of water-soluble plant components, distributed in water in ionized form. It has antibacterial properties, and also additionally has a moisturizing effect; promotes regeneration.

Dexpanthenol - a drug, a provitamin of group B ₅ - a derivative of pantothenic acid, passes in the body into pantothenic acid, which is an integral part of coenzyme A and is involved in the processes of acetylation, carbohydrate and fat metabolism, in the synthesis of acetylcholine, corticosteroids, porphyrins; stimulates the regeneration of the skin, mucous membranes, normalizes cellular metabolism, accelerates mitosis and increases the strength of collagen fibers. It has an anti-inflammatory effect with the normalization of the sebaceous glands, a regenerating effect.

Sulfoconcentrol - organically bound sulfur (Organically bound sulfur with neutralized fatty acid - Sulfated TEA-ricinoleate, PEG-35 castor oil, propylene glycol. (http://www.balticgreen.ru/catalog/belava-kosmetika/aktivnvie-veshhestva/deodoriruyushhie, antibacterialnyie-ingredientyi/) helps to eliminate the inflammatory process on the eyelids and normalizes the functioning of the glands located in their thickness - the sebaceous glands, has a regenerating effect - restores the protective barrier of the epidermis. blepharitis.

Vitamin B3 - includes two main forms - nicotinamide and nicotinic acid. During metabolic processes in the body, they are converted into nicotinamide adenine dinucleotide (NAD, nicotinamide adenine dinucleotide - NAD) and nicotinamide adenine dinucleotide phosphate (NADP, nicotinamide adenine dinucleotide phosphate - NADP) - coenzymes of many redox reactions that are vital for cellular metabolism. In these molecular structures, nicotinamide acts as an electron donor and acceptor and participates in vital redox reactions catalyzed by dozens of different enzymes. Nicotinamide dilates small blood vessels and improves microcirculation.

The complex effect of the above components allows you to achieve the desired effect - cleansing, moisturizing the surface of the eyelids, restoring the functional activity of the meibomian glands, reducing inflammatory manifestations, and additionally destroying the Demodex mite. The composition may include functional additives: polyvinylpyrrolidone, glycerin, hydroxyethylcellulose gelling agent, carboxymethylcellulose, Iodopropynyl Butylcarbamate, Butylene Glycol, Sodium Hydroxide, Sodium Benzoate, DMDM Hydantoin.

The composition is prepared as follows:

Example 1. Mix 0.50-1.00 wt. % sodium salt of hyaluronic acid in 10.0 wt. % water, add 0.25-0.50 silver glycinate and 1.00-2.00 wt. % dexpanthenol, functional additives are added - polyvinylpyrrolidone, glycerin, carboxymethylcellulose, Iodopropynyl Butylcarbamate, DMDM Hydantoin.

The mixture is adjusted to 100 wt. % water and mix. Get the gel.

Example 2. Mix 0.50-1.00 wt. % sodium salt of hyaluronic acid in 10.0 wt. % water, add 0.25-0.50 silver glycinate and 0.50-1.00 wt. % sulfoconcentrol. add functional additives. The mixture is adjusted to 100 wt. % water and mix. Get the gel.

Example 3. Mix (0.50-1.00 wt.%) sodium salt of hyaluronic acid in 10.0 wt. % of water, add (1.00-5.00 wt.%) natural calendula flower water 100% hydrolate, (1.00-2.00 wt.%) vitamin B ₃ , and (1.00-2.00 wt. .%) dexpanthenol. add functional additives. The mixture is adjusted to 100 wt. % water and mix. Get the gel.

Example 3. Mix (0.50-1.00 wt.%) sodium salt of hyaluronic acid in 10.0 wt. % water, add (1.00-5.00 wt.%) natural flower water of calendula 100% hydrolat and (0.50-1.00 wt.%) sulfoconcentrol. add functional additives. The mixture is adjusted to 100 wt. % water and mix. Get the gel.

Clinical and toxicological tests of cosmetic compositions were carried out on the basis of Dr. Kurenkov's Clinic.

When using this composition, an improvement was noted in both the subjective state of patients - there were no complaints about the feeling of dryness, discomfort in the eyes, itching in the eyelids, and an improvement in objective indicators, and objective indicators - there was no hyperemia and thickening of the edges of the eyelids, an improvement in tear production was noted. The improvement in clinical parameters is due to the restoration of the outflow of lipid secretion from the mouths of the ducts of the meibomian glands, which occurs due to self-massage of the edges of the eyelids with a gel that has an anti-inflammatory, moisturizing effect, and also mechanically cleans the surface of the eyelid. The ingress of lipid secretion from the meibomian glands, in the process of blinking, onto the ocular surface protects the surface of the eye, including the cornea and conjunctiva, from drying out. It should be noted that dynamic monitoring of patients (up to 6 months) who perform eyelid hygiene with the above compositions showed a subsequent increase in tear production tests and a decrease in complaints of dryness and discomfort in the eyelids and eyes.

The gels were used daily, self-massaging the eyelids with it. Self-massage of the eyelids was carried out for 1-2 minutes. The gel is applied to a cotton swab, cotton pad or fingertips. Using soft circular movements with a stick with gel, with slight pressure, self-massage the edge of the eyelid. Eyelid hygiene is recommended to be carried out 2 times a day - in the morning and in the evening for 1 month.

Clinical example 1.

Visit 1. Patient N., 47 years old. She complained of redness of the eyelids of both eyes, discomfort, dryness in the eyes.

Anamnesis morbi: According to the patient, moderate myopia since childhood. Uses contact correction - more than 8 hours a day.

Status about cuius OU: Eyelids - hyperemic, edematous, multiple cysts of the excretory ducts of the meibomian glands. Conjunctiva - slightly hyperemic, mucous discharge. The cornea is transparent, spherical, shiny. The anterior chamber is of medium depth, the moisture is transparent. The iris is structural. Pupil with a diameter of 3.0 mm, round shape, reaction to light is alive. The lens is transparent. The vitreous body is transparent. Additional studies have been carried out to assess the function of the meibomian glands: Schirmer test 7 mm (normal 15 mm); Meiboscopy - 4 points (with a norm of 8); Meibography - prolapse of meibomian glands 25%. Compression test - 1 point (norm 3 points).

Diagnosis: OU Meibomian gland dysfunction. Dry eye syndrome, moderate myopia.

Recommended:

OS - hygienic eyelid hygiene with a gel containing sodium hyaluronate, dexpanthenol, silver glycinate, 2 times a day - morning, evening.

Visit 2 in 1 month. No active complaints. Status oculus OU: Eyelids are calm. The conjunctiva is pale pink, there is no discharge. The cornea is transparent, spherical, shiny. The anterior chamber is of medium depth, the moisture is transparent. The iris is structural. Pupil with a diameter of 3.0 mm, round shape, reaction to light is alive. The lens is transparent. The vitreous body is transparent.

Additional studies have been carried out to assess the function of the meibomian glands: Schirmer test 13 mm (normal 15 mm); Meiboscopy - 6 points (at a rate of 8); Meibography - prolapse of meibomian glands 25%. Compression test - 2 points (norm 3 points).

As a result of the treatment, the inflammatory process on the eyelids was stopped.

Clinical example 2.

Visit 1. Patient D., 35 years old. She complained of a feeling of dryness and discomfort in the eyes, accumulation of secretion in the corners of the eyes after sleep. Anamnesis morbi: According to the patient, he works in an office environment, uses a computer for more than 6 hours a day.

Status oculus OU: Eyelids - slightly hyperemic, edematous, obstruction of the ducts of the meibomian glands, crusts on the eyelids, mucus. The conjunctiva is slightly hyperemic. The cornea is transparent, spherical, shiny. The anterior chamber is of medium depth, the moisture is transparent. The iris is structural. Pupil with a diameter of 3.0 mm, round shape, reaction to light is alive. The lens is transparent. The vitreous body is transparent.

Additional studies have been carried out to assess the function of the meibomian glands: Schirmer test 10 mm (normal 15 mm); Meiboscopy - 6 points (with a norm of 8); Meibography - meibomian gland prolapse 0%. Compression test - 2 points (norm 3 points).

Diagnosis: OU Chronic blepharitis. Dry eye syndrome.

Recommended:

OS - hygienic eyelid hygiene with a gel containing sodium hyaluronate, natural calendula flower water 100% hydrolat, sulfoconcentrol, vit. B3, 2 times a day - morning, evening.

Visit 2 in 2 months. No active complaints.

Status oculus OU: Eyelids are calm. The conjunctiva is pale pink, there is no discharge. The cornea is transparent, spherical, shiny. The anterior chamber is of medium depth, the moisture is transparent. The iris is structural. Pupil with a diameter of 3.0 mm, round shape, reaction to light is alive. The lens is transparent. The vitreous body is transparent.

Additional studies have been carried out to assess the function of the meibomian glands: Schirmer test 15 mm (normal 15 mm); Meiboscopy - 8 points (at a rate of 8); Meibography - meibomian gland prolapse 0%. Compression test - 3 points (norm 3 points).

As a result of the treatment, the inflammatory process on the eyelids was stopped, the functions of the tear-producing system were restored.

Claims (3)

1. Composition for hygienic treatment of the eyelids, characterized in that it contains sodium hyaluronate, silver glycinate or natural calendula flower water 100% hydrolate, dexpanthenol or sulfoconcentrol in the following ratio of components, wt.%: sodium salt of hyaluronic acid 0.50–3.00 silver glycinate 0.25–1.00 or natural flower water calendula 100% hydrolat 1.00–10.00 dexpanthenol 0.50–6.00 or sulfoconcentrol 0.60–1.00 purified water and functional additives up to 100 2. Composition according to claim 1, characterized in that it additionally contains vitamin B3.