Extract from aboveground parts of oat grown before ear formation

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical industry, in particular to a composition, possessing immunomodulating and anti-inflammatory properties. The dermatological composition, possessing immunomodulating and anti-inflammatory properties, as an active ingredient, contains an extract of the aboveground part/parts of oat, collected before ear formation. The cosmetic composition, possessing immunomodulating and anti-inflammatory properties. Application of the extract of the aboveground part/parts of oat, collected before ear formation, possessing immunomodulating and anti-inflammatory properties, as a medication.

EFFECT: composition and extract possess expressed immunomodulating and anti-inflammatory properties.

15 cl, 1 tbl, 3 ex

 

The present invention relates to an extract of the aerial parts of oats, mainly grown before heading, and to its use for the treatment of inflammatory dermatoses.

Oats or Avena sativa L., is a perennial plant that can reach heights of 1 m 50 cm When sprouting young plant grows as a lawn, and then gives a few stalks with special character growth. The stalk, or stubble, is hollow, with a diameter of several millimeters, interrupted in places where fitted sheet, solid diaphragms, called nodes. The intervals between the nodes, first very short at the base of the stem, becoming longer.

The leaves are alternate, double-row, matte blue-green color; they are mounted on the stem at the nodes through long separated the front of the vagina, which covers almost all of the upper space of the internode. Leaf blade is separated from it at right angles. It is wide, has a banded structure, covered with numerous parallel veins (pravilova); usually it is pubescent. On the leaf, where it is separated vagina, watching the lengthening of the thin film of the vagina, called the tongue, which is short and truncated, between stem and leaf lamina.

The stem ends with a large inflorescence is a panicle, RA is medistim in all directions, very loose pyramidal form, all the branches which end elementary inflorescence permanent structure in the entire family Roaseae and are called secondary spikelet. Secondary spikelets are hanging, relatively large and contain only two flowers. Secondary spikelet not laid in the bosom of the fallopian bract, and a short distance from his sitting, he carries two characteristic opposite bract called koloskovyy scales.

Glumes oats are large; they reach a length of 2 cm and fully embody the secondary spikelet; they are lanceolate, equipped with 7-9 veins and pubescent. Flowering scales are small; outer flowering glume carries a curved face, not planted on the top and back and longer secondary spikelets more than one centimeter.

Directly above the flowering scales the axis of the flower bears two small almost not visible parts, films and, finally, a real flower, which is reduced to three stamens and three carpels. Stamens first are essentially sedentary, then visible to their network, suddenly lengthening during flowering, so that the anthers become exposed and hanging with secondary spikelets. Anthers impaled on the network solely through their middle region, and therefore they are called medium-ol is fortified or swing anthers. Three carpel form a unilocular ovary with the stigma of the pistil, which is divided into very sprawling and Cirrus relave share. All these signs correspond to pollination by wind. There is only one ovule, which is anatropous and is right at the bottom of the cavity of the ovule.

The fruit is a one-seeded fruit of a certain type, where the outer base directly attached against pericardia. This fruit called a caryopsis. It is an oblong, narrow, pubescent grain with massive amyloid protein. The embryo has a very good sameday surrounding podsiadlo knee almost completely separating it from protein. Entire germ rejected him.

The fruit oats recognized as a medicinal plant raw material for oral use as a laxative agent due to its ballast effect, but also in the case of cholesterolemia or type 2 diabetes because it contains β-glucan. Local by the fruit oats, mainly used in the form of flour that is called extract colloids oats, has pharmacopoeial article in the U.S. Pharmacopoeia USP 22, 1990. This colloidal extract has softening and soothing properties and is defined as the powder obtained by grinding and other processing of whole grains, where the variety is so corresponds to the oat flour. In pharmacopoeial article sets out the standards of viscosity, microbiological purity, moisture loss during drying, particle size and ash content, lipid and nitrogen.

From the same part of the oats can also be extracted oil, used in cosmetics, and proteins. The latter, which are insoluble, cannot be used directly, but only after enzymatic or chemical hydrolysis. Get to a greater or lesser extent treated hydrolysate, from which you can get either peptides oats with different molecular weights, or amino acids depending on the strength of hydrolysis. Hydrolyzed proteins oats were evaluated for their properties in the fields of cosmetology and dermatology. So, demonstrated their properties for the hair, such as the ability possessed by these proteins, to form a film on the hair shaft, to penetrate into the cuticle and thus, due to the resulting sweetening effect, to ensure the conditioning effect.

In the work carried out in vitro on cell cultures, it was possible to evaluate anti-inflammatory activity of the extract of oat colloids. So, this extract showed inhibitory activity on skin metabolism of arachidonic acid and eicosanoids, on the expression of cytosolic phospholipase A2and the cycle is oxygenase on line human keratinocytes, as well as the induction of activity of anti-inflammatory cytokine TGFβ1. Cytokines of Th1 and Th2 immune cells, such as IL2IL4IL5IL13also subject to this colloidal extract. Finally, a clinical study demonstrates the usefulness of the extract of oat colloids on the model of cutaneous inflammation in the double-blind model of skin irritation and in 12 healthy volunteers.

The outer part of the grain provides glucan used in dietetics in the fiber of oats reduce cholesterol and the risk of cardiovascular diseases.

Glucan oats were also investigated for their giving to the viscosity and gelling properties for use as a food additive.

Glucan extracted from oat, also have immunostimulatory activity. Demonstrated other activity, adding value in the field of cosmetology: protection against the damaging effects of UV radiation, stimulation of cellular metabolism, stimulation of collagen synthesis and improve the strength of hair extension.

Apart from grain oats are used as fodder plants. Cut young, he provides valuable forage. Straw of oats to feed horses, cows and sheep, but not used in human nutrition. In traditional medicine oat straw is used for baths to facilitate the surveillance of rheumatic pain, sciatica and liver damage.

In India the usual concoction of oats used for getting rid of the addiction to the powder of opium. Alcohol extract prepared from fresh plants, used for getting rid of tobacco with statistically significant results.

Bath based on oat straw or commercial extracts have indications: rheumatism, neuralgia, chronic eczema, atopic dermatitis, peripheral vascular disorders, etc.

"Herbal medicines" oats are the subject of the article EALs (European Agency for the evaluation of medicinal products) (Ref: EMEA/NMRS/202966/2007), in which the said application or dried aerial parts of the plant collected before flowering, or liquid extract (1:5, 45% vol./about. ethanol), prepared from the fresh aerial parts of the plants collected during the flowering period.

Describes the traditional use of these aerial parts in the case of mild emotional stress and promote sleep.

Based on the bibliography of the aerial parts of oats contain:

Flavonoids:

- Glycosylamine apigenine type (vitexin, isovitexin...) or luteolin (orientin, isoorientin, sockopen...),

- O-glycosyl flavones technologo type

- Flavonolignan (alkaline a and b)

- Bisdesmosides steroid saponins: Avenacosides a and b (aglycone : NWT the Genin)

Proteins

- Other: Phenolic compounds (Avenanthramides, hydroxycotinine acid...), sterols, cerebrosides...

Atopic dermatitis (or atopic eczema) is a common dermatological condition that affects 10-15% of newborns in France, the frequency of which is increasing in recent decades.

Atopic dermatitis is a skin symptom of atopy, which is a chronic inflammatory dermatitis or eczema, occurs when a genetically determined condition, affecting 15-30% of children and 2-10% of adults, and its prevalence is growing in industrialized countries, it has doubled and even tripled in the past three decades, and is currently considered as a major public health problem. Atopic dermatitis is often associated with other atopic disorders such as allergic rhinitis and asthma. This lesion most often occurs in childhood and is characterized by periodic outbreaks for several years. It is manifested by rash, alternating with spontaneous remissions.

The quality of life of patients affected by atopic dermatitis, deeply disturbed. Approved therapies include corticosteroids and local immunomodulating agents, system agents, frequent secondary effects which limit long-term use, acytelene funds. Modern therapy is reactive - treatment flares - but it is now established that early intervention, focused on the fight against rash and skin inflammation, may be useful in relation to the struggle with the disease, and the possible emergence of asthma and/or rhinitis (BIEBER, T. 2008, Atopic dermatitis, The New England Journal of Medicine, Vol 358 (14) 1483-1494), and atopic dermatitis is considered as the initial phase of the so-called atopic development. In most cases, concomitant topical treatment provides Supplement to applied treatments and brings relief to the patient. There is a significant need for therapy, alternative therapy with corticosteroids.

Atopic dermatitis is the result of complex interactions between genetic predispositions, environmental factors such as allergens and microorganisms, dysfunction of the skin barrier, dysregulation of the immune system (SPERGEL, JM. 2008, Immunology and treatment ofatopic dermatitis, Am J Clin Dermatol, Vol 9(4) 233-244).

Psoriasis is also a skin inflammatory disease with chronic development; it only affects 2% of the population. Together with atopic dermatitis it is the most common chronic inflammatory skin disease. It is characterized by an abnormal growth of epidermal cells, associerad is authorized with inflammatory reaction. The Central mechanism of this inflammatory phenomenon associated with the action of T cells of the immune system, mainly cells of the Th1 type (WILSMANN-THEIS, D.; HAGEMANN, T.; JORDAN, J.; BIEBER, T.; NOVAK, N. 2008, Facing psoriasis and atopic dermatitis: are there more similarities or more differences? Eur J Dermatol, Vol 18 (2) 172-180)that initiate and maintain the inflammatory process and stimulate excessive proliferation of keratinocytes, which then undergo rapid and incomplete phase of differentiation. Keratinocytes Express receptors that make them sensitive to inflammatory signals, and release of proinflammatory mediators. Psoriatic inflammation, thus, supported by the mutual stimulation of T cells and keratinocytes.

Thus, this disease should be treated for a long time.

Therefore, there is a need and a strong need for therapeutic alternatives to these inflammatory dermatoses.

Unexpectedly and surprisingly, the inventors have shown new ways to add value extracts of the aerial parts of oats in therapy and cosmetology/dermatology. The advantage is that this extract has immunomodulatory and anti-inflammatory properties useful in the treatment of atopic dermatitis. The extract in accordance with the present invention also exhibits good capacity for treatment at the Rey and aging skin.

The object of the present invention, therefore, is the extract of the aerial parts/parts oats, excluding grain, characterized by a content of 2-15% of flavonoids and 0.2-2% of avenacosides a and B.

Under the aerial parts of oats, in the sense of the present invention, refers to any part of the plant oats, located above ground, except grain.

Preferably the aerial parts of oats include leaves and/or stems and/or secondary spikelets, and/or flowers.

Received oat extract is characterized by the content of interest flavonoids and saponins. The last analyzed by liquid chromatography high pressure in two different ways, suitable for each type of connection.

The content of these different molecules varies depending on the extraction conditions. The major flavonoids are isovitexin-2"-O-arabinopyranoside and isoorientin-2"-O-arabinopyranoside. Avenacosides a and b are the major saponins. They are bisdesmosides steroid saponins.

Preferably the extract in accordance with the invention contains a proportion of 5-10% of the main flavonoids: isovitexin-2"-O-arabinopyranoside and isoorientin-2"-O-arabinopyranoside.

Preferably the extract in accordance with the invention is an extract obtained in the organic solvent is.

Preferably the extract in accordance with the invention contains less than 1 million-1(ppm) protein, preferably less than 0.5 million-1and even more preferably less than 0.3 million-1protein.

Preferably the extract in accordance with the invention is an extract of the aerial parts of oats, collected before the start of the heading.

In the sense of the present invention "aerial parts of oats collected prior to the heading"mean aerial parts of oats collected after emergence (approximately from 2 weeks to 2 months after germination) during the stage of elongation just before heading, but does not include it.

In the sense of the present invention "elongation" means a stage of growth, which corresponds to the elongation of the stem and the beginning of formation of the ear, before flowering.

Another object of the present invention is a method of obtaining the extract of the aerial parts/parts oats, where this elevated part of/part does not contain any grains, comprising the following stages:

- drying and grinding above-ground parts/parts oats,

extraction in an organic solvent selected from the group consisting of ketones, esters, C1-C4alcohols and mixtures in any mixing ratio of these solvents, and

- centrifuging or filtering.

Preferably organization is systematic solvent in accordance with the invention is selected from the group consisting of acetone, methyl ethyl ketone, isobutyl ketone, ethyl acetate, C1-C4alcohol and the mixture in any mixing ratio of these solvents.

Preferably the above-ground part is collected after 2 months, at the end of the tube, but before heading, and then dried and milled.

The extraction was carried out with stirring or by static.

The extraction is carried out at boiling under reflux or at room temperature.

Preferably the extraction is carried out in a ratio plant/solvent, which can vary from 1/7 to 1/20, preferably from 1/8 to 1/12.

Preferably the extraction is carried out for a period of from 30 minutes to 48 hours, more preferably from 60 to 120 minutes.

The extraction can be resumed 2 or 3 times.

Then Marc, resulting from the extraction step, is separated from the extract by centrifugation or filtration, and the solution can be more or less concentrated to obtain a dry extract.

Processing the bleaching can be carried out either by skimming through concentration, precipitation and filtration, or by adding to a concentrated or non-concentrated extracted solution absorbent media, such as activated carbon or adsorber the maintenance resin.

Media can be added during the stage of drying in mass fractions relative to the extracted solids, which may vary from 1 to 75%. The media can be a sugar, such as maltodextrin, lactose, silica or any other kosmetologicheskii acceptable carrier.

Another object of the present invention is the extract of the aerial parts of oats, except seed, which can be obtained by the method in accordance with the invention.

Preferably the extract is obtained by extraction with acetone or a mixture of acetone/water containing up to 20% water.

The acetone extract or acetone-water type with 20% water consists of molecules of interest, flavonoids and saponins and very significantly depleted proteins. Indeed, ways of dispensing proteins described in the European Pharmacopoeia, did not give any results, and migration in the gel LTO-SDS page using electrophoresis after precipitation from acetone and the identification of Kumasi blue or silver nitrate shows the absence of any bands, indicating the presence of protein. By applying a control on the same electrophoresis it is possible to quantitatively determine the detection limit of protein to 1 ng, thus, this extract has a protein content of less than 1 million-1(reduced to the amount of extract, Nanase the nogo on the gel). Preferably the specified protein content is less than 0.5 million-1and even more preferably less than 0.3 million-1protein.

Another object of the present invention relates to a dermatological or cosmetic composition containing an extract in accordance with the invention and one or more than one or dermatologically or kosmetologicheskii acceptable excipient respectively.

The composition in accordance with the invention can, in particular, contain additives and excipients compositions, such as emulsifiers, thickeners, gelling agents, fixers water, lyophilizers agents, stabilizers, dyes, flavorings and preservatives.

Cosmetic or dermatological composition according to the invention additionally contains conventional dermatologically compatible excipients.

Preferably the composition in accordance with the invention contains an amount of the extract of the aerial parts/parts oats as an active ingredient comprising from 0.1 to 5 wt.% of the total weight of the composition.

Preferably the specified amount of the extract is from 0.1% to 0.5 wt.% of the total weight of the composition.

Dermatological or cosmetic composition in accordance with the present invention can be prepared in the form of emulsion, water-in-oil (V/M) or wt is about-in-water (M/V) in the form of a multiphase emulsion, such as, for example, emulsion water-in-oil-in-water (W/M/C) or oil-in-water-in-oil (M//M), microemulsions or even hydro-dispersion or optispray, gel or aerosol.

Dermatologically or kosmetologicheskii compatible excipients can represent any excipient among those known to experts in the art, with the purpose of obtaining a composition for topical application in the form of milk, cream, balm, oil, lotion, gel, foaming gel, ointment, spray, etc.

Another object of the present invention relates to the extract in accordance with the invention for use as a medicine.

Another object of the present invention relates to the extract in accordance with the invention for use in the treatment of inflammatory dermatoses.

Another object of the present invention relates to the extract in accordance with the invention for use in the treatment of atopic dermatitis, psoriasis or eczema, which are inflammatory dermatoses.

Another object of the present invention relates to the use of the extract in accordance with the invention for obtaining a medicinal product intended for the treatment of inflammatory dermatoses.

Another object of the present invention relates to the use of the extract in accordance with what Britanie to obtain medicines designed for treatment of atopic dermatitis, psoriasis or eczema, which are inflammatory dermatoses.

Another object of the present invention relates to the extract in accordance with the invention for use in the treatment of acne or aging skin.

Another object of the present invention relates to the use of the extract according to the invention in cosmetic and/or dermatological composition intended for the treatment of acne or aging skin.

Another object of the present invention relates to the extract in accordance with the invention for use in the treatment of rosacea.

Another object of the present invention relates to the use of the extract according to the invention in cosmetic and/or dermatological composition intended for the treatment of rosacea.

Rosacea are inflammatory and chronic disease of the skin. It is incurable, often benign skin disease, which is chronic red plaques on the nose, on the cheeks, and sometimes on the chin and on the forehead.

Another object of the present invention relates to the extract in accordance with the invention for use in the treatment of sensitive skin.

Another object of the present invention relates to the use of the structure of the extract in accordance with the invention in the cosmetic and/or dermatological composition, intended for the treatment of sensitive skin.

Under the sensitive skin in the sense of the present invention involve the skin with high sensitivity. Sensitive skin, or reactive skin, is a syndrome characterized by neurosensitivity signs, such as inflammation, itching, pain. Among the clinical signs resulting from the clinical evaluation by a dermatologist find: erythema, edema, dryness/scaling, papules/vesicles, acne lesions (L. Misery et al., JEADV 2009, 23, 376). Sensitive skin is a skin sensitivity, which requires the use of well-tolerated food hygiene and care. Sensitive individuals are people who, in particular, react to aggression faster than the skin of most people.

The following examples illustrate the invention without limiting its scope.

Example 1: obtaining an extract of the aerial parts of oats collected before earing, in accordance with the invention

A. by extraction with acetone

400 kg of dried aerial parts of oats collected before earing, grind, and then placed in a reactor with 10 volumes of a mixture of acetone/water with stirring for one hour at room temperature.

By separating the solid and liquid phases is possible is to teach the first extraction of the juice. Pomace is extracted a second time with 10 volumes of a mixture of acetone/water for one hour at room temperature with stirring. By separating the solid and liquid phases, it is possible to get a second extraction of the juice, which combine with the first. The resulting solution was concentrated on a water content of up to 1.33 volume/kg, and then filtered. The extract thus obtained, dried using microwave ovens after adding media maltodextrin (in the amount of 25% of the native extract).

Thus, received 36 kg light brown powder with a titer of 6% flavonoids (isovitexin-2"-O-arabinopyranoside and isoorientin-2"-O-arabinopyranoside) and 0.6% of avenacosides In, and the protein content of the extract thus obtained is less than 0.3 million-1.

b. by extraction with ethanol

Extraction of 100 g of dried and ground plants with a mixture of ethanol/water 50:50 for one hour at boiling under reflux, the separation of the solid and liquid phases and evaporation in vacuum at 50°C. Thus obtained 26 g of the extract in the form of a brown powder with a titer ranging from 1.5 to 3% flavonoids (isovitexin-2"-O-arabinopyranoside and isoorientin-2"-O-arabinopyranoside).

Example 2: a Biological study of the extract of the aerial parts of oats collected before earing, from example 1.a

Farmacologicas the e study of the extract of the aerial parts of oats refers to the immune-inflammatory component of atopic dermatitis. Change of epidermal barrier (namely mutation in the gene of filaggrin) promotes the penetration of allergens with a high molecular weight (from mites, pollen, ...), their capture by dendritic cells and their prezentowanie T cells; this interaction leads to T-cell response in the skin - first Th2 with the production group of proinflammatory cytokines and chemokines capable of maintaining inflammation: IL-4, IL-5, IL-13 associated with atopic dermatitis, with a significant appearance on the surface of IL-17 and IL-31 - but with a significant delay Th1 (INCORVAIA, C.; FRATI, F; VERNA N.; D ALO, S.; MOTOLESE, A.; PUCCI, S. 2008, Allergy and the skin, Clin Exp Immunol, Vol 153 (1) 27-29); (BIEBER, T. 2008, Atopic dermatitis, The New England Journal of Medicine, Vol 358 (14) 1483-1494). For the activation of T lymphocytes followed by the activation of other cell types, mainly keratinocytes and endothelial cells, which results in the production of inflammatory mediators (cytokines, prostaglandins) and the production of chemokines, enabling recruitment of inflammatory cells.

A. Obtaining fractions:

Extract of the aerial parts of oats you can fractionate to identify a class of molecules or molecules responsible for the activity.

This extract can be applied on a column of silica gel medium pressure and successively eluted with solvents of increasing polarity, for example, increasing the concentration is a function of methanol in water. Indeed, the fractionation obtained after application of the extract prepared according to example 1, on a column of silica gel and its first elution with a mixture of methanol/water from 25:75 to 50:50 and then to 100% methanol, gave the possibility to divide a fraction enriched in flavonoids (fraction of 50:50 methanol/water, 19% of flavonoids isovitexin-2-O-arabinopyranoside and isoorientin-2-O-arabinopyranoside, expressed as vitexin-2-arabinose) and the fraction enriched in saponins (fraction of 100% methanol, 15% of avenacosides In). Using prepreparation HPLC using a column of silica gel, reversed phase C-18, from the first fractions were isolated flavonoids isovitexin-2-O-arabinopyranoside and isoorientin-2-O-arabinopyranoside, including patterns, which were confirmed using mass spectrometry and nuclear magnetic resonance.

Using prepreparation HPLC of fraction enriched in saponins, were selected avenacosides and avenacosides, including patterns that have been identified using mass spectrometry and nuclear magnetic resonance.

b. Immunomodulating activity

Cytokines, which represent a vast group of regulatory proteins of the immune system responsible for the generation resident or infiltrated by skin cells that have been activated during the inflammatory and immune Pro is escow.

Interleukins, including II2II4II5and II13produced by lymphocytes are divided into two groups: cytokines of the Th1 type, including II2and cytokines of the Th2 type, including II4II5and II13. All of these interleukins excessively produced during inflammatory conditions such as atopy, contact eczema, or psoriasis.

Among them, interleukin 2 (IL-2) a person having origins of T cells capable of maintaining proliferation of activated T lymphocytes and induces the processes of differentiation and activation and NK (natural killer, Natural Killer) cells.

In vitro mononuclear cells can be stimulated and produce cytokines. The principle of this test is to study the influence of the extracts on the production of II2II4II5II13induced double stimulation forbesmarshall.com/ionomycin.

Results: the acetone extract of the aerial parts of oats collected before earing, according to example 1.a inhibited by 52% the number of CD4 lymphocytes expressing interleukin 2, and 21% of the intracellular level II-2 at a concentration of 30 μg/ml of the same extract at a concentration of 30 μg/ml inhibited the production of lymphocytes interleukin 4 by 51%, interleukin 5 by 31% and interleukin 13 to 78%.

This activity, int representing the RES for the treatment of atopic dermatitis, given saponin extract, including avenacosides a and B.

S. anti-Inflammatory activity

Principle: Keratinocyte, presents the most cell in the epidermis, plays a significant role in initiation and modulation of inflammatory reactions of the skin. Using this model it is possible to determine in vitro the ability of different molecules for modulating the production of mediators, derived from the metabolism of arachidonic acid. Prostaglandin PG6KF1a is a stable metabolite of prostacyclin PGI2, the main metabolite produced by stimulated keratinocytes person. The acetone extract of the aerial parts of oats collected before heading, and its fractions were evaluated for the production of this prostaglandin induced in keratinocyte calcium ionophores A (stimulating arachidonic acid cascade).

Results: the Acetone extract according to example 1.a has significant activity (40% inhibition at 0.1 µg/ml), and the fraction enriched in flavonoids, has significant activity for a maximum of 49% inhibition at 10 μg/ml.

This anti-inflammatory activity given the flavonoids present in the extract, and, in particular, isoorientin-2"-O-arabinoside (55% inhibition at 10 μg/ml).

The mechanism of action of this inhibition release simple is cyclina was partially clarified: we observed a direct inhibition of in vitro cyclooxygenase 2 acetone extract (68% inhibition at 100 µg/ml) and did not observe inhibition of phospholipase A2.

d. Antioxidant activity

Radical scavenging activity of the extract of the aerial parts of oats, obtained according to example 1.a, evaluated using the DPPH test(2,2'-diphenyl-1-picrylhydrazyl). This quick test, easy to use, is based on measuring the ability to capture a stable free radical DPPH. Free radical DPPHthat absorbs at 517 nm, is restored to the corresponding hydrazine when it interacts with donors proton:

R-OH+DPPHR-O+DPPH2

IC50concentration of the extract that causes 50% reduction in the absorption of methanolic solution of DPPH(=25 µg/ml).

Under these conditions, the vitamin E is IC506-10 mcg/ml, and the acetone extract of the aerial parts of oats collected before earing, has IC5070 µg/ml.

Thus, this extract has antioxidant activity, and therefore, it can be used in the composition of medical-cosmetic products for skin as an agent for preventing aging.

E. antimicrobial activity

The acetone extract obtained according to example 1.a, has a selective effect on the pathogen involved in the formation of acne, Propionibacterium acnes (see table 1).

Table 1
Minimum inhibitory concentrations, expressed in percent (wt./mass.) acetone extract of the aerial parts of oats according to example 1.a variety of pathogenic microorganisms, Gram+, Gram - bacteria, yeast and fungi.
PathogensMIC (minimum inhibitory concentration)
Staphylococcus aureus≥3,07%
Staphylococcus epidermidis≥3,07%
P. acnes0,096%
Pseudomonas aeruginosa≥3,07%
Escherichia coli≥3,07%
Candida albicans≥3,07%
Aspergillus niger>3,07%
M. furfur>3,07%

Example 3: Composition in accordance with the present invention

emollient CREAM ATOPIC SKIN

Extract of the aerial parts of oats (PRA)of 0.1-0.5%
The miner is the emotional butter 10-20%
Evening primrose oil2,5%
Cyclomethicone5-8%
Literallayout/PEG-100 stearate5%
Glycerin5%
Polyacrylamide &C13-14 isoparaffin & Laureth-73%
PEG-124%
EDTA0,2%
Triethanolamine0,1%
Preservativesqs (enough)
Waterup to 100%

moisturizing LOTION FOR ATOPIC SKIN

Extract of the aerial parts of oats (PRA)of 0.1-0.5%
Mineral oil3%
Vaseline6-12%
Dimethicone2%
Evening primrose oil2,5%
Sorbitan stearate/sucrose of cocoat5%
Xanthan gum0,4%
Carbomer0,2%
Triethanolamine0,1%
Glycerin3%
EDTA0,2%
Beganby alcohol1%
Preservativesqs (enough)
Waterup to 100%

1. Dermatological composition having immunomodulatory and anti-inflammatory properties, containing as active ingredient an extract of the aerial parts/parts oats collected before heading containing from 2 to 15% flavonoids and from 0.2 to 2% of avenacosides a and b, and one or more dermatologically acceptable excipients.

2. Dermatological composition according to claim 1, containing from 0.1 to 5 wt.% of the extract by weight of the total composition.

3. Dermatological composition according to claim 1, characterized in that the extract contains less than 1 million-1protein.

4. Dermatological composition according to the .3, characterized in that the extract obtained in acetone.

5. Cosmetic composition having immunomodulatory and anti-inflammatory properties, contains extract of the aerial parts/parts oats collected before heading containing from 2 to 15% flavonoids and from 0.2 to 2% of avenacosides a and b, and one or more cosmetically acceptable excipients.

6. Cosmetic composition according to claim 5, containing from 0.1 to 5 wt.% of the extract by weight of the total composition.

7. Cosmetic composition according to claim 5, characterized in that the extract contains less than 1 million-1protein.

8. Cosmetic composition according to claim 7, characterized in that the extract obtained in acetone.

9. Application of the extract of the aerial parts/parts oats collected before earing, have immunomodulatory and anti-inflammatory properties, containing from 2 to 15% flavonoids and from 0.2 to 2% of avenacosides and as a medicine.

10. The use according to claim 9 for the treatment of inflammatory dermatoses.

11. The use of claim 10, where the inflammatory dermatosis is a atopic dermatitis, psoriasis or eczema.

12. The use according to claim 9 for the treatment of acne.

13. The use according to claim 9 for the treatment of skin aging.

14. The use according to claim 9 for the treatment of rosacea.

15. The use according to claim 9 for the treatment of reactive skin.



 

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27 cl, 2 ex, 5 tbl, 6 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing N-substituted menthane carboxamides. The method is carried out via a coupling reaction between primary menthane carboxamides and aryl halides in the presence of a copper catalyst. The invention also relates to neoisomers having a 1S,2S,5R-configuration, menthane derivatives selected from menthyl esters, menthyl ethers, menthane carboxyl esters or menthane carboxamides, having cooling agent properties, as a product intended for oral application, containing an amount of a neoisomer sufficient to create a cooling sensation in the mouth, and a method of creating a cooling effect in the mouth.

EFFECT: improved method of producing menthane carboxamide derivatives with high output, neoisomers of menthane derivatives, having cooling agent properties.

18 cl, 4 ex

FIELD: chemistry.

SUBSTANCE: group of inventions relates to adhesive hydrogel compositions intended for oral application. The hydrophilic pressure-sensitive bioadhesive is a non-covalent complex of a film-forming polymer with at least one of the following complementary components: cross-linking polymer agent, cross-linking oligomer agent, low-molecular weight substance, or with a mixture of at least two of said components, where the film-forming polymer and the cross-linking polymer agent are selected from a class of hydrophilic polymers. Components of the bioadhesive are taken in an amount which enables to obtain a complex which is characterised by adhesion to the surface of teeth and the lack of adhesion towards other tissues in the oral cavity with particular values glass transition temperature, modulus of elasticity G′, loss tangent, swelling degree in aqueous medium and swell ratio. The film-forming hydrophilic polymer is preferably contained in a higher concentration than other components of the adhesive, wherein the latter have complementary reactive functional groups which are capable of forming non-covalent hydrogen, electrostatic or ionic bonds with functional groups of the hydrophilic film-forming polymer. In a swollen state, the "smart" hydrophilic pressure-sensitive adhesive is softer than the dental substrate but harder than the mucosal tissues in the oral cavity. Also disclosed is a dental care composition which contains the pressure-sensitive bioadhesive and one or more active agents, such as teeth whitening agents, fluoride sources, antibacterial agents etc. The preferred teeth whitening agent is a peroxide.

EFFECT: composition can be used as teeth whitening film-strips or gels.

56 cl, 3 tbl, 27 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to the field of individual hygiene and deals with a composition for teeth cleaning, which ensures a peeling effect with respect to soft tissues in the oral cavity, and its application. The peeling composition for teeth cleaning contains a multitude of granules, a carrier, acceptable for the oral cavity, and hydroxyacid, selected from lactic acid, glycolic acid and neutralised salicylic acid. The granules include: i) at least, one polymer binding substance; ii) a thickening agent, selected from hydroxypropylmethylcellulose, hydroxypropylcellulose (GPC), methylcellulose and corn starch; iii) plasticiser, selected from propylene glycol, glycerin and triacetin. At least, one component from the granules and acceptable for the oral cavity carrier additionally contains, at least, one abrasive substance, which includes silicon dioxide, which has an average particle diameter from 0.01 to 4 mm. Also claimed is a system for peeling of soft tissues in the oral cavity, which includes accessories for the oral cavity care and the said composition, as well as a method of peeling the oral cavity soft tissues with application of the said composition.

EFFECT: application of the claimed group of inventions ensures peeling or enhancement of desquamation of soft tissues in the oral cavity.

9 cl, 4 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of cosmetology, namely to a cosmetic composition for peroral introduction, which contains a combination of lycopene, vitamin C, vitamin E and at least one polyphenol compound, obtained from pine bark, in which the ratio of weight content of polyphenol compound to the sum of weight contents of lycopene, vitamin C and vitamin E constitutes from 0.3 to 0.7, as s single active ingredient.

EFFECT: invention is intended for prevention and/or treatment of wrinkles in the area of eyes and mouth angles, small wrinkles, eye bags and dark circles under eyes.

22 cl, 2 ex, 11 tbl

FIELD: chemistry.

SUBSTANCE: invention describes a skin and hand cleaner containing the following components: a) 5-70 wt % alkyl ester and/or diester, b) 0-40 wt % surfactant, selected from a group comprising ethoxylates of fatty alcohols, sulphoesters of fatty alcohols and salts of sulphated and/or sulphonated fatty acids, c) 0.5-10 wt % thixotropy agent, such as organic bentonite, and more than 0.1 wt % hydrophilic pyrogenic silicic acid, d) 0-30 wt % of one or more abrasive agents, e) 0-5 wt % physiologically compatible carbonic ester, f) 0 to less than 10 wt % water, g) optionally one or more viscosity stabilising agents, h) optionally other cosmetic auxiliary substances.

EFFECT: cleaner removes stubborn dirt from skin and hands, has a fluidity point which enables to prevent sedimentation if there is need to use abrasive particles, is easy to make, is homogeneous and stable and is easy to store.

16 cl, 29 ex, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetology and represents a complex cosmetic agent containing hyaluronic acid, colloidal silver, emulsion wax, water, carnosine, enfolin recovered from hydrogel of hyaluronic acid in the process of photochemical nanostructuring at wave length equal to 280 nm, while hyaluronic acid is nanostructured at a diameter of single chains up to 5 nm with the ingredients of the agent taken in certain ratio, wt %.

EFFECT: invention provides rejuvenating effect, anti-inflammatory action and lifting effect, besides it possess local immunostimulative action, extended storage period and high biological activity.

1 tbl, 3 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to dermatology and cosmetology, and represents a pharmaceutical composition that prevents or relieves a local dermal allergic reaction, and contains triethylene glycol, lanthanum or cerium nitrate or chloride, glycerol, polyethyl glycol-115, propylene glycol , ethanol, potassium hydroxide, cedar nut oil or milk thistle oil, vitamins A, E, C, F, analgin, glyciram, diazolin, hyaluronic acid and distilled water, wherein the ingredients are taken in a specific ratio, wt %.

EFFECT: invention provides an extended range of products improving the physiological skin condition and protecting the skin from the adverse environmental exposure.

1 tbl

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely therapeutic dentistry and may be used for treating destructive forms of chronic periodontitis. That is ensured by administering a therapeutic preparation into a root canal. A sonic phoresis of the therapeutic preparation Beresh plus drops is preceded by coating the skin surrounding a causative tooth with a therapeutic mixture containing the preparation Beresh plus drops, 10% calcium gluconate and Vaseline oil. Thereafter, an emitter is used to process the area. The sonic phoresis is followed by a root canal obturation with calcium hydroxide. That is combined with administering ascorbic acid in a daily dose of 50-100 mg and the preparation Beresh plus drops 1 drop per 2 kg of body weight a day orally. The therapeutic course is 5-8 procedures.

EFFECT: invention enables arresting the inflammatory process in the aggressive lesion, reducing the number of complications and aggravations ensured by accelerating the repair processes in the apical aggressive lesion.

2 dwg

FIELD: medicine.

SUBSTANCE: invention refers to cosmetic industry and represents a non-foaming cosmetic composition of an oil-in-water emulsion containing (i) retinol, (ii) at least one polar emollient specified in a group consisting of propylene glycol stearyl ester, propylene glycol isostearate and mixtures thereof (iii) at least one non-polar emollient specified in a group consisting of aromatic or linear esters, Gerbe ester, mineral oils, squalane, isohexadecane, squalene, liquid paraffin and mixtures thereof with the weight ratio of the above polar emollient and the above non-polar emollient is found within the range of approximately 95 to 5 to approximately 40 to 60.

EFFECT: provided considerable reduction of retinoid-caused skin irritation and higher efficacy or retinoid.

11 cl, 3 ex, 7 tbl, 3 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely a method of treating acne. The method of treating acne by prescribing line seed oil 10 ml 2 times a day, sodium selenite 90 mcg 1 time a day, tocopherol acetate 100 mg 2 times a day for 1 month.

EFFECT: method of treating acne is effective and enables reducing the length of treatment.

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetology and dermatology, and represents a water-based formulation for local application for treating acne, containing water, a water-miscible organic solvent and benzoyl peroxide, wherein the organic solvent concentration is 1-4 times higher than the benzoyl peroxide concentration in the formulation; the water and organic solvent concentrations are related as at least 7:1, preferentially at least 10:1, more preferentially at least 20:1; the benzoyl peroxide concentration in the formulation makes less than 5.0 wt %, but at least 1.0 wt %.

EFFECT: invention provides the clinical effectiveness with the reduced active agent concentration, as well as reduced irritant action.

27 cl, 4 ex, 3 tbl

FIELD: medicine.

SUBSTANCE: invention refers to cosmetology and represents a cosmetic composition containing: hydrolised yeast proteins as an active substance, and at least one acceptable carrier, differing by the fact that the above hydrolised yeast proteins are prepared by exogenic enzymatic hydrolysis and/or acid hydrolysis and/or alkaline hydrolysis of the yeast membranes.

EFFECT: invention provides improved cosmetic activity, excellent time stability.

17 cl, 6 ex, 3 tbl, 2 dwg

FIELD: medicine.

SUBSTANCE: invention refers to medicine, specifically to dermatology, and may be used for treating the patients suffering acne. That is ensured by local applications of a therapeutically effective amount of a fixed-dose combination containing adapalene and benzoyl peroxide. That is combined with oral administration of a therapeutically effective amount of an antibiotic for a particular period of time.

EFFECT: method provides the effective treatment of these patients, manifested as a significant decrease of all types of acne involvements, prevents the further development of these involvements, including after the withdrawal of oral antibiotics and the development of resistance, due to the synergistic effect of the above local combination and oral antibiotic.

11 cl, 11 tbl, 4 dwg, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and cosmetics, more specifically to a topical pharmaceutical composition possessing comedolytic and antibiotic action, comprising an effective amount of the antibiotic clindamycin, salicylic acid and excipients. The pharmaceutical composition is presented in the form of a gel. The excipients are as follows: acrylate copolymer emulsion Salcare SC80, allantoin, antioxidant dihydroquercetin preservative Sharomix MCI, propylene glycol, cyclomethicone DC 345, tocopherol phosphate, UV filter Escalol 567, emulsifier DC 5329, trometamol and thermal water.

EFFECT: stabilised composition has strong comedolytic and antibiotic action, comprises the protective SPF factor which protects inflamed skin against the negative effects of UV radiation and has a shelf life of at least 3 years.

3 ex, 4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of pharmaceutics and represents application of composition, including adapalene and benzoyl peroxide, in preparation of local medication, intended for application by patient who requires it to provide long-term treatment of acne vulgaris, where scheme of application of local medication includes application of therapeutically efficient quantity of composition for, at least, 9 months.

EFFECT: invention ensures achievement of stable positive effect in long-term treatment of acne with composition, including adapalene and benzoyl peroxide, as well as absence of side effects.

19 cl, 1 ex, 3 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of dermatology and represents application of 1-aminoalkylcyclohexane derivative, selected from neramexane and its pharmaceutically acceptable salts for treatment or prevention of inflammatory skin diseases, which represent acne, irritant dermatitis, impetigo and atopic dermatitis.

EFFECT: invention ensures extension of arsenal of medications for treatment of inflammatory skin diseases.

39 cl, 7 ex, 35 tbl, 5 dwg

FIELD: medicine.

SUBSTANCE: invention relates to medicine, particularly to dermatology, more specifically to methods of treating pyoinflammatory skin diseases, particularly furunculosis and acne. The method of treating the patients suffering pustular skin disorders, according to the invention, consists in the fact that the affected and surrounding skin areas are prepared with warm weak antiseptic, dried and further processed with an ointment prepared by thorough mixing on a water bath until smooth: zinc-salicylic paste, Lorinden C, gioxizone, streptocide liniment, synthomycin liniment and retinol acetate in the ratio of 3÷1÷1÷1÷0.8÷0.1 with skin treatment produced 2 times a day. The weak antiseptic is sodium bicarbonate or chamomile infusion at temperature 40-45°C. Besides, water bath temperature is to be 40-50°C, and the ointment is to be prepared is a glass or ceramic container. Face acne requires the affected area to be warmed with a vapour bath before finally applying the ointment. To prevent accidental wipe-out of ointment from the ointment treated skin, it is covered with the napkins attached to healthy skin. To enhance the effect of the ointment applications, the affected skin is exposed to UV lamp and/or sunlight for 10-30 minutes.

EFFECT: method enables faster treatment and prevented the recurrent disease, and also ensures the prevention of side effects and provides outpatient treatment.

6 cl, 7 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetology and dermatology and represents a composition for treating dermatological disorders containing in a physiologically acceptable medium, at least: (i) peroxide benzoyl, (ii) a naphthoic acid derivative specified in 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid, 6- [3-(1-adamantyl)-4-hydroxyphenyl]-2-naphthoic acid, 6-[3-(1-adamantyl)-4-decyloxyphenyl]-2-naphthoic acid and 6-[3-(1-adamantyl)-4-hexyloxyphenyl]-2-naphthoic acid and (iii) a compound of polyurethane polymer representing a polyol pre-polymer with said naphthoic acid derivative and said benzoyl peroxide being found in the dispersed form in said composition.

EFFECT: invention provides producing a non-irritant stable composition.

25 cl, 8 ex

FIELD: biotechnologies.

SUBSTANCE: invention refers to a compound of formula (I):

,

where R1 represents NR7C(O)R8 or NR9R10; R2 represents hydrogen; R3 represents halogen; R4 represents hydrogen, halogen, cyano, hydroxy, C1-4alkyl, C1-4alkoxy, CF3, OCF3, C1-4alkylthio, S(O)(C1-4alkyl), S(O)2(C1-4alkyl), CO2H or CO2(C1-4alkyl); R5 represents C1-6alkyl (replaced with NR11R12 or heterocyclyl that represents nonaromatic 5-7-membered ring containing 1 or 2 heteroatoms independently chosen from a group containing nitrogen, oxygen or sulphur); R6 represents hydrogen, halogen, hydroxy, C1-4alkoxy, CO2H or C1-6alkyl (possibly replaced with NR15R16 group, morpholinyl or thiomorpholinyl); R7 represents hydrogen; R8 represents C3-6cycloalkyl (possibly replaced with NR24R25 group), phenyl or heteroaryl, which represents aromatic 5- or 6-membered ring containing 1 to 3 heteroatoms independently chosen from the group containing nitrogen, oxygen and sulphur, and which is probably condensed with one 6-membered aromatic or nonaromatic carbocyclic ring or with one 6-membered aromatic heterocyclic ring, where the above 6-membered aromatic heterocyclic ring includes 1 to 3 heteroatoms independently chosen from a group containing nitrogen, oxygen and sulphur; R9 represents hydrogen or C1-6alkyl (possibly replaced with pyrazolyl); R10 represents C1-6alkyl (possibly replaced with phenyl or heteroaryl group, which represents aromatic 5- or 6-membered ring containing 1 or 2 heteroatoms independently chosen from the group containing nitrogen, oxygen or sulphur, and which is possibly condensed with one 6-membered heterocyclic ring, where the above 6-membered aromatic heterocyclic ring contains 1 or 2 heteroatoms independently chosen from the group containing nitrogen, oxygen or sulphur; where the above phenyl and heteroaryl groups in R8, R9 and R10 are possibly independently replaced with the following group: halogen, hydroxy, C(O)R42, C1-6alkyl, C1-6hydroxyalkyl, C1-6halogenoalkyl, C1-6alkoxy(C1-6)alkyl or C3-10cycloalkyl; unless otherwise stated, heterocyclyl is possibly replaced with group of C1-6alkyl, (C1-6alkyl)OH, (C1-6alkyl)C(O)NR51R52 or pyrrolidinyl; R42 represents C1-6alkyl; R12, R15 and R25 independently represent C1-6alkyl (possibly replaced with hydroxy or NR55R56 group); R11, R16, R24, R51, R52, R55 and R56 independently represent hydrogen or C1-6alkyl; or to its pharmaceutically acceptable salts.

EFFECT: new compounds are obtained, which can be used in medicine for treatment of PDE4-mediated disease state.

10 cl, 2 tbl, 202 ex

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