Hair growth reduction

FIELD: cosmetic medicine.

SUBSTANCE: invention proposes a method for reducing growth of human hair by way of applying dermatologically acceptable topical-administration composition onto skin in amount sufficient to reduce hair growth, which composition contains α-difluoromethylornitin (DFMO) and dermatologically acceptable carrier including at least 4% polyoxyethylene ether to provide percutaneous effects.

EFFECT: enhanced percutaneous power of active ingredient (DFMO).

38 cl, 2 tbl, 6 ex

 

Background of the invention

The present invention relates to the reduction of hair growth in mammals, especially for cosmetic purposes.

The main function of hair in mammals is ensuring protection from exposure to the environment. However, this feature is largely lost in people who retain or remove the hair in different parts of the body, mainly for cosmetic purposes. For example, generally prefer to have the hair on the scalp, but not on the face.

Removal of unwanted hair using a variety of treatments, including shaving, hair removal using electrolysis, creams or lotions-depilatory, waxing, plucking and therapeutic antiandrogens. Data standard procedures usually have associated disadvantages. Shaving, for example, can lead to abrasions and cuts, and can also leave a sense of increasing the speed of hair re-growth. Shaving can leave unwanted stubble. Hair removal using electrolysis, on the other hand, can leave treated areas without hair for long periods of time, but can be expensive, painful and can leave scars. Creams-depilatories, although very effective, are generally not recommended for frequent use because of their high annoying when osobnosti. Waxing and plucking can cause pain, discomfort and ill remove short hairs. And finally, antiandrogens used to treat hirsutism in women, can have unwanted side effects.

Previously it was found that the rate and character of hair growth can be changed by application to the skin of inhibitors of certain enzymes. These inhibitors include inhibitors of 5-alpha-reductase, interdiscursivity, S-adenosylmethionine, gamma glutamyltranspeptidase and transglutaminase. See, for example, Breuer et al., U.S. patent No. 4885289; Shander, U.S. patent No. 4720489; Ahluwalia, U.S. patent No. 5095007; Ahluwalia et al., U.S. patent No. 5096911 and Shander et al., U.S. patent No. 5132293.

α-Deformational (DFMO) is an irreversible inhibitor of interdiscursivity (ODC), an enzyme that limits the rate of biosynthesis of putrescine, spermidine and spermine de novo. The role of the polyamines in cell proliferation are not yet fully understood. However, it appears that they play a role in the synthesis and/or regulation of DNA, RNA and proteins. High levels of ODC and polyamines are found in malignant tumors and other types of cells that have a high rate of cell proliferation.

DFMO binds the active site of ODC as a substrate. Associated DFMO then decarboxylated and converted into reactive intermediate substance which forms a covalent bond with the enzyme, preventing, thus, the binding of the natural substrate ornithine by the enzyme. Cellular inhibition of ODC by DFMO causes a noticeable decrease in the number of putrescine and spermidine, and a variable decrease in the number of spermine depending on the duration of exposure and the type of cells. Usually to DFMO caused a significant antiproliferative effect, inhibition of the synthesis of polyamines should be supported by sustained any abscopal levels DFMO, because the half-period of the existence of ODC is approximately 30 minutes, one of the shortest of all known enzymes.

The preparation for skin containing DFMO (sold under the brand name Vaniqa®company Bristol Myers Squibb), was recently approved for use by the Management of the food and drug administration (FDA) for the treatment of unwanted hair growth on the face in women. Its local application in a creamy medium has been shown to reduce the rate of growth of facial hair in women. Cream Vaniqa® includes racemic mixture of D-and L-DFMO enantiomers (i.e. D, L-DFMO) in the form of monohydrochloride at a concentration of 13.9 wt.% active agent (15% in the case of monohydrate monohydrochloride). The recommended treatment regimen for Vaniqa® - twice a day. Creamy medium Vaniqa®described in example 1, PA is enta USA no 5648394, which is included in the present description by reference. Creamy medium includes 2.5 wt.% ceteareth-20. Ceteareth-20 is a mixture of two polyoxyethylenated esters alilovic alcohols having the chemical formula CH3(CH2)15(OCH2CH2)bOH and CH3(CH2)17(OCH2CH2)bOH, where b has an average value of 20.

Usually for inhibiting hair growth efficacy of Vaniqa cream®it became apparent that it takes about eight weeks of continuous treatment. Cream Vaniqa®as shown, reduces hair growth on average by 47%. In one study, clinical success was observed in 35% of women who were treated with Vaniqa cream®. These women in their condition, there was a noticeable improvement or complete purification, the results of scoring the doctors reduce the visibility of facial hair and reduce darkening of the skin caused by hair. Another 35% of women who participated in the trials, there was a slight improvement. However, several women had been poor treatment response or lack of response.

Accordingly, although the cream Vaniqa®is an effective product, it would be even more effective if provided earlier onset of inhibition of hair growth (i.e. demonstrated its efficiency is of earlier than eight weeks) and/or showed a higher degree of clinical success rate (i.e demonstrated its efficacy in a larger percentage of users). These improved results can not be obtained by simply increasing the concentration of D,L-DFMO in creamy media. First, increasing the concentration of D,L-DFMO above about 14% may cause increased burning of the skin and/or may leave a residue, making it aesthetically unacceptable. Secondly, it is difficult to produce a composition with active concentrations above about 15%, because much higher concentrations of D,L-DFMO are not sufficiently soluble in the carrier or destabilize the emulsion.

Molecules that are identical to each other by chemical structural formula and still not overlap each other, represent enantiomers. From the point of view of their physico-chemical properties of enantiomers differ from each other only in their ability to rotate the plane of plane-polarized light, and this ability is often used in their designation. The enantiomer that rotates the plane of plane-polarized light to the right, called Pervouralsky and denote the (+)or d-, or D - in front of the title compound; those that rotate the plane of plane-polarized light to the left, called levogyrate and about the mean (-), or a prefix of l-or L-. Racemic mixture stand for (±), or a prefix of d,l-or D,L-. According to another Convention (or item) to distinguish between enantiomers on the basis of their absolute configuration, you can use R,S or rule sequence. When using this system, L-DFMO corresponds to R-DFMO and D-DFMO corresponds to S-DFMO. Enantiomers are physico-chemically similar in that they have similar melting point, boiling point, relative solubility and chemical reactivity in an achiral environment. A racemate is a composition of equimolar amounts of the two enantiomers, often called DL-form. Single enantiomers of chiral molecules can have different pharmacological profiles, i.e. differences in the pharmacokinetics, toxicity, effectiveness, etc.

A brief description of the nature of the inventions

The present invention relates to a method (typically a cosmetic method) of reducing hair growth in humans by application to the skin in a quantity effective to reduce hair growth, dermatologically acceptable composition for topical application, containing α-deformational (DFMO) and a dermatologically acceptable carrier. The carrier includes at least 4, preferably at least 5 wt.%, more preferably, at least Mas.% polyoxyethylene ether, having the chemical formula R(OCH2CH2)bOH, where R represents a saturated or unsaturated alkyl group containing from 6 to 22 carbon atoms, and b is a number from 2 to 200. Preferably the alkyl group contains from 8 to 20, more preferably from 10 to 18 carbon atoms, and b represents the average value from 2 to 100, more preferably from 2 to 50, most preferably from 2 to 30. Unwanted hair growth may be undesirable from a cosmetic point of view, or may result, for example, diseases or pathological conditions (e.g., hirsutism).

For the purposes of this application, the media includes all the components of the composition, in addition to DFMO. DFMO, as used in this application includes the actual DFMO and its pharmaceutically acceptable salts.

Preferably DFMO will include at least about 70%, or 80%, more preferably at least about 90%, most preferably at least 95%, L-DFMO. Ideally, DFMO will be an essentially optically pure L-DFMO. "Essentially optically pure" means that DFMO includes at least 98% L-DFMO. "Optically pure" L-DFMO means that DFMO includes essentially 100% L-DFMO.

The present invention also relates to compositions for topical application containing DFMO in number, f is an objective to reduce hair growth, and dermatologically acceptable medium containing at least 4%, preferably at least 5 wt.% polyoxyethylenated ester having a chemical formula described above.

The above compositions have a high efficiency as compared with similar compositions with media not containing or containing, for example, smaller amounts (e.g., 2.5 wt.%) polyoxyethylene ether. This increased efficiency can manifest itself, for example, in the earlier beginning of inhibiting hair growth activity, the greater the reduction in the rate of hair growth and/or in a greater number of persons who have reduced hair growth. Not limited to any theory, it is assumed that polyoxyethylene ether breaks, solubilities and/or emuleret lipid component of the skin, which leads to increased absorption of skin DFMO.

Preferred compositions contain from about 0.1% to about 30%, preferably from about 1% to about 20%, more preferably from about 5% to about 15 wt.% DFMO.

Other characteristics and advantages of the present invention will be apparent from the description and claims.

Detailed description

Preferred compositions contain essentially optically pure L-DFMO in kosmetologicheskii and/liedermaching acceptable carrier, comprising at least 5 wt.% polyoxyethylene ether having the chemical formula R(och2CH2)bHE, where R is a saturated or unsaturated alkyl group containing from 8 to 20 carbon atoms, and b represents the average value from 2 to 100. The composition may be solid, semi-solid, cream or liquid. The composition may represent, for example, cosmetic and dermatological product in the form of, for example, ointment, lotion, foam, cream, gel or solution. The composition may also be in the form of the preparation for shaving or after shaving. The media itself may be inert or may have cosmetic, physiological and/or pharmaceutical benefits.

Preferred polyoxyethylene esters include polyoxyethylene (2) ether of stearyl alcohol (steareth-2) (R=CH3(CH2)17, b=2), polyoxyethylene (2) ether olejowego alcohol (oleth-2) (R=CH3(CH2)7SNSN(CH2)8, b=2), polyoxyethylene (4) ester of lauric alcohol (laureth-4) (R=CH3(CH2)11, b=4), polyoxyethylene (23) ester of lauric alcohol (laureth-23) (R=CH3(CH2)11, b=23), polyoxyethylene (20) ether of cetyl alcohol and polyoxyethylene (20) ether of stearyl alcohol ceteareth-20) (R=CH3(CH2)15and (R=CH3(CH2)173(CH2)17, b=20).

The composition may contain one or more other types of agents that reduce hair growth, such as those described in U.S. patent No. 5364885 or in U.S. patent No. 5652273.

The concentration of DFMO in the composition can be varied in a wide range up to a saturated solution, preferably from 0.1 to 30 wt.%; reduction of hair growth increases with the number of DFMO caused per unit area of skin. Maximum effective damage number is limited only by the speed with which DFMO penetrates the skin. Effective amounts can be in the range of, for example, from 10 to 3000 micrograms or more per square centimeter of skin.

The media may be liquid or solid softening products, solvents, thickeners, moisturizers and/or powders. Softening means include, for example, stearyl alcohol, mink oil, cetyl alcohol, alerby alcohol, isopropylene, polyethylene glycol, olive oil, vaseline, palmitic acid, oleic acid and myristoleate. The solvents include, for example, water, ethanol, isopropanol, acetone, diethylene glycol, ethylene glycol, dimethylsulfoxide and dimethylformamide.

Optically pure L-DFMO, you can get known the different ways. See, for example, U.S. patent No. 4309442; Gao et al., Ann. Pharm. Fr. 52(4):184-203 (1994); Gao et al., Ann. Pharm. Fr. 52(5):248-59 (1994); and Jacques et al., Tetrahedron Letters, 48:4617 (1971), which are included in the present description as a reference.

The following are examples of compositions.

Example 1

The composition contains up to 15 wt.% DFMO in media containing water 64,6%, ethanol 15,2%, propylene glycol at 4.75%, dipropyleneglycol of 4.75%, polyoxyethylene ether 5%, benzyl alcohol 3.8% propylene carbonate and 1.9%. Polyoxyethylene ether may represent, for example, oleth-2, steareth-2, laureth-23 and laureth-4.

Examples 2-5

Examples of compositions with DFMO polyoxyethylene ether with an additional amplifier penetration or without it.

IngredientExample 2Example 3Example 4Example 5
Percent (wt./wt.)Percent (wt./wt.)Percent (wt./wt.)Percent (wt./wt.)
Waterq.s.q.s.q.s.q.s.
Glicerinstearat14,034,243,844,24
PEG-100 stearate13,894.09 to3,714.09 to
Cetearyl alcohol22,90 3,05was 2.763,05
Ceteareth-2022,372,502,252,50
Mineral oil2,112,222,012,22
Stearyl alcohol1,591,671,511,67
Dimethicone0,530,560,50,56
Preservative30,4-0,780,4-0,780,4-0,780,4-0,78
Polyoxyethylene ether45555
Urea--55
All media100%100%100%100%
DFMO52-15%52-15%52-15%52-15%5
1Available in the form of a mixture, for example, Cithrol GMS A/S ES0743 from the company Croda Chemical Company (UK).
2Available in the form of a mixture, for example, Cosmowax EM5483 from the company Croda Chemical Company (UK).
3Preservative: a combination of Phenoxyethanol and methyl-, ethyl-, propyl - and butyl is Kabanov. The preservative is available as a premixed mixture or as separate ingredients.
4Polyoxyethylene ether you can choose from: ceteareth-20, ceteth-20, steareth-20, oleth-2, steareth-2, laureth-23 and laureth-4.
5Active medicinal component DFMO add at end levels 2-15% or emulsified media of examples 2-5, or first dissolved in the water component, and then add the remaining ingredients to the formation of stable emulsions. After addition of DFMO concentration of other ingredients in the medium is reduced accordingly. Preferably DFMO is an essentially optically pure L-DFMO.

Example 6

Any one or more of the previous examples in combination with one or more of the following amplifiers penetration: terpenes (3-hydroxy-3,7,11-trimethyl-1,6,10-dodecatrien or nerolidol), CIS-9-octadecanoic acid (oleic acid), propane-2-I, terpenes, CIS-fatty acids (oleic acid, palmitoleate acid), acetone, laurocapram, dimethylsulfoxide, 2-pyrrolidone, aerowyn alcohol, glyceryl-3-stearate, cholesterol, isopropyl ester of myristic acid and propylene glycol. Power penetration can be added at a concentration of, for example, from 0.10 to 20 wt.% or from 0.5 to 12 wt.%.

The composition should be applied topically on the selected area of the body where it is desirable to reduce hair growth. For example, the composition can be applied on the face, especially on the part of the beard, on the cheeks, neck, upper lip or chin. The composition can also be used as an adjunct to other methods of hair removal, including shaving, waxing, mechanical epilation, chemical depilation, hair removal using electrolysis and laser hair removal.

The composition can also be used on legs, arms, torso or armpit. The composition is particularly suitable for reducing unwanted hair growth in women, especially unwanted hair on the face, such as the upper lip or the chin. The composition should be applied once or twice a day or even more often to achieve a tangible reduction of hair growth. The feeling of reduced hair growth can be observed already after 24 or 48 hours (for example, between normal intervals shaving) after applying or may require, for example, three months. The reduction in hair growth is demonstrated, for example, when the rate of hair growth slows, the need for hair removal is reduced, the subject feels less hair in the treated area, or quantitatively, when the weight remote hair (i.e. the mass of hair) decreases (quantitatively), the subjects felt the t reduction, for example, facial hair, or actors are less concerned or less annoying unwanted hair (e.g., facial hair).

Analysis of skin penetration

Analysis of in vitro diffusion media was carried out on the basis of the analysis described Franz, Curr. Probl. Dermal. 7:58-68 (1978). The skin of the back of Golden Syrian hamsters pinched electrical terminals, cut to a suitable size and placed in a diffusion chamber. The receptor fluid consisted of saline phosphate buffer, isotonic to maintain the viability of the cells, and 0.1% of sodium azide, preservative, and it was placed in the lower chamber of the diffuser so that the liquid level was fixed parallel to the sample skin. After equilibration at 37°C for at least 30 minutes, 10 μl or 20 μl of14With DFMO (0.5 to 1.0 TCI on diffusion chamber) in the test or control composition was added to the surface of the skin and gently distributed over the entire surface with a glass rod. The DFMO penetration was evaluated through periodic sampling aliquot (400 THB) during the experiment and quantification using liquid scintillation.

This analysis was carried out with the composition described in example 1 using each of polyoxyethylenated esters listed in example 1. The nose is tel, not included polyoxyethylene ether, was used as control. It was found that the media, including laureth-4, increased the DFMO penetration into the skin in 2,5-3 times; the media, including oleth-2 1.5-2 times; the media, including laureth-23, approximately 1.5 times, and the media, including steareth-20, approximately 1.5-2 times.

Other embodiments of the present invention are included in the scope of the claims.

Analysis of penetration through the skin

The skin of the back hamsters (Charles River Labs, Worcester, MA) cut electric scissors and mounted in glass diffusion cells Franz to the epidermal side of the skin was exposed to the ambient air through the donor chamber. The underside of the skin was in contact with 8.5 ml of receptor fluid (saline solution buffered with phosphate and 0.1% of sodium azide), so that the fluid layer is flush with the surface of the skin. Camera Franz was placed in a heating block and the experiments were conducted at 37°under stirring. For testing received two composition of the medium (without active agent): control carrier according to WO 9421216, exp, with 2.5% ceteareth-20, and is almost identical to the tested media received in accordance with WO 9421216, exp, but modified to include 4% ceteareth-20 in accordance with the present invention. a 25 μl aliquot of control is about the media (without active agent) or the test media (without active agent) was applied to the surface of the skin and distributed with a glass rod. For each composition was doing nine replicates. Twenty hours 25 μl aliquot of the control or the test media containing 1%3H-DFMO, was applied to the skin surface with a pipette and distributed evenly over the entire surface with a glass rod. At different time points (2, 6 and 24 hours after application) 400 ál aliquots of the receptor fluid was removed through the upper surface and placed in vials for analysis by liquid scintillation. Deleted volumes immediately resumed with fresh receptor fluid. Penetration3H-DFMO through the skin was assessed by determining the level of radioactivity using liquid scintillation. The test media containing 4% ceteareth-20, showed a substantial increase in penetration into the skin active agent compared with the control media with 2.5% ceteareth-20. The increased penetration occurred at 2.3-times higher at 2 hours, 2.1-fold at 6 hours, and about 1.5-fold at 24 hours. The results are shown in the table below:

MediaThe DFMO penetration (% of applied dose) (Mean + STD. error of the mean)
2 hours6 hours24 hour
CTR. media (prior art)2,49�B1; 0,474,56±0,6816,48±1,44
The test media (Nast. an invention.)of 5.84±1,509,67±2,1024,14±3,63

The results clearly demonstrate the unexpected increase in the absorption of the active agent (DFMO) with the use of the preparation according to the present invention in comparison with the product of the prior art. This unexpected result could not be predicted based on the level of technology.

1. A method of reducing hair growth in humans, including the selection of an area of skin on which it is desirable to reduce the growth of hair, and apply to skin in a quantity effective to reduce hair growth, a composition containing α-deformational and dermatologically acceptable medium containing at least 4 wt.% polyoxyethylene ether having the chemical formula R(och2CH2)bHE, where R is a saturated or unsaturated alkyl group containing from 6 to 22 carbon atoms, and b is a number from 2 to 200.

2. The method according to claim 1, wherein the carrier includes at least 5 wt.% polyoxyethylene ether.

3. The method according to claim 1, wherein the carrier comprises at least 6 wt.% polyoxyethylene ether.

4. The method according to claim 1 in which R contains from 10 to 18 carbon atoms.

5. JV the property according to claim 1, in which b is a number from 2 to 50.

6. The method according to claim 1, in which polyoxyethylene ether is polyoxyethylene (2) ether of stearyl alcohol.

7. The method according to claim 1, in which polyoxyethylene ether is polyoxyethylene (2) ether olejowego alcohol.

8. The method according to claim 1, in which polyoxyethylene ether is polyoxyethylene (4) ester of lauric alcohol.

9. The method according to claim 1, in which polyoxyethylene ether is polyoxyethylene (23) ester of lauric alcohol.

10. The method according to claim 1, in which polyoxyethylene ether is polyoxyethylene (20) ether of cetyl alcohol.

11. The method according to claim 1, in which polyoxyethylene ether is polyoxyethylene (20) ether of stearyl alcohol.

12. The method according to claim 1, in which polyoxyethylene ether is polyoxyethylene (20) ether of cetyl alcohol and polyoxyethylene (20) ether of stearyl alcohol.

13. The method according to claim 1, in which α-deformational contains at least about 80% L-α-deformationand.

14. The method according to claim 1, in which α-deformational is an optically pure L-α-deformational.

15. The method according to 14, in which the composition contains from 5 to 15 wt.% optically pure α-deformationand, wear the ü includes, at least 5 wt.% polyoxyethylene ether, and polyoxyethylene ether is polyoxyethylene (20) ether of cetyl alcohol and polyoxyethylene (20) ether of stearyl alcohol.

16. The method according to claim 1, wherein the composition comprises from 1 to 20 wt.% α-deformationand.

17. The method according to claim 2, in which the composition contains from 5 to 15 wt.% α-deformationand.

18. The method according to claim 1, in which the skin is on the face.

19. Composition for topical application on the skin, containing from 0.1 to 30 wt.% α-deformationand, and a dermatologically acceptable carrier, which includes, from 4 to 6 wt.% polyoxyethylene ether having the chemical formula R(OCH2CH2)bOH, where R represents a saturated or unsaturated alkyl group containing from 6 to 22 carbon atoms, and b is a number from 2 to 200.

20. The composition according to claim 19, in which the carrier includes at least 5 wt.% polyoxyethylene ether.

21. The composition according to claim 19, in which the carrier comprises at least 6 wt.% polyoxyethylene ether.

22. The composition according to claim 19, in which R contains from 10 to 18 carbon atoms, and b is a number from 2 to 50.

23. The composition according to claim 19, in which polyoxyethylene ether is polyoxyethylene (2) ether of stearyl alcohol.

24. The composition according to claim 19, the cat is Roy polyoxyethylene ether is polyoxyethylene (2) ether olejowego alcohol.

25. The composition according to claim 19, in which polyoxyethylene ether is polyoxyethylene (4) ester of lauric alcohol.

26. The composition according to claim 19, in which polyoxyethylene ether is polyoxyethylene (23) ester of lauric alcohol.

27. The composition according to claim 19, in which polyoxyethylene ether is polyoxyethylene (20) ether of cetyl alcohol.

28. The composition according to claim 19, in which polyoxyethylene ether is polyoxyethylene (20) ether of stearyl alcohol.

29. The composition according to claim 19, in which polyoxyethylene ether is polyoxyethylene (20) ether of cetyl alcohol and polyoxyethylene (20) ether of stearyl alcohol.

30. The composition according to claim 19, in which α-deformational is an essentially optically pure L-α-deformational.

31. The composition according to claim 19, in which the composition contains from 5 to 15 wt.% optically pure α-deformationand, the carrier includes at least 5 wt.% polyoxyethylene ether, and polyoxyethylene ether is polyoxyethylene (20) ether of cetyl alcohol and polyoxyethylene (20) ether of stearyl alcohol.

32. The method according to any one of claims 1 to 18, in which the specified application in the specified composition has a cosmetic effect.

33. Composition according to any one of p-31, which was before the hat is a cosmetic composition.

34. Application polyoxyethylene ether having the chemical formula R(OCH2CH2)bOH, where R represents a saturated or unsaturated alkyl group containing from 6 to 22 carbon atoms, and b is a number from 2 to 200, as a carrier for the manufacture of a medicinal product containing at least 4 wt.% specified polyoxyethylene ether and α-deformational to reduce hair growth in humans.

35. The application 34, where polyoxyethylene ether is as defined in any of claims 4 to 12.

36. A method of obtaining a composition for reducing hair growth in humans, including mixing α-deformationand and a dermatologically acceptable carrier, including at least 4 wt.% polyoxyethylene ether having the chemical formula R(och2CH2)bHE, where R is a saturated or unsaturated alkyl group containing from 6 to 22 carbon atoms, and b is a number from 2 to 200.

37. The method according to p, which produces cosmetic composition.

38. The method according to p, wherein said polyoxyethylene ether is as defined in any of claims 4 to 12.



 

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8 cl, 5 ex

FIELD: organic chemistry, pharmaceuticals.

SUBSTANCE: invention relates to new solid form of 4-cyclipentyl resorcine, namely 4-cyclipentyl resorcine monohydrate and crystalline polymorph thereof, namely Form I, as well as pharmaceutical composition for skin depigmentation and uses thereof for drug preparation. Polymorph of Form I has powder X-rays diffraction pattern obtained with CuKα-irradiation with characteristic peaks (2Θ) at approximately 8.1, 16.2, and 23.8.

EFFECT: new depigmentation agent.

8 cl, 4 tbl, 4 dwg, 5 ex

FIELD: method and composition for oral cavity care.

SUBSTANCE: claimed form contains a) 1-40 % of retaining agent, Selected from group containing water soluble hydrophilic resins, water soluble hydrophilic polymers or mixtures thereof, wherein retaining agent is capable of hydration under water or saliva action to produce retention coefficient of 1-4; and b) 60-90 % of local carrier. Moreover composition contains 65 wt.% of water-insoluble particles. Further disclosed is dental paste composition containing a) 30-65 % of water-insoluble particles as retaining agent, wherein solubility of retaining agent in water is less then 1 g/30 g at 25°C; b) 0.01-40 % of active agent for oral cavity care; c) 0.1-25 % of buffer agent. Claimed composition has retention coefficient of 1-4.

EFFECT: improved compositions for oral cavity care.

9 cl, 3 dwg, 5 ex

FIELD: cosmetic products.

SUBSTANCE: invention relates to antiperspirant compositions for human skin application methods for production and uses thereof. Transparent anhydrous antiperspirant compositions contain from 1 to 30 mass % of quick antiperspirant salt dispersed in water immiscible liquid carrier, which is cured with effective amount of structuring agent.

EFFECT: compositions with improved transparency.

32 cl, 4 ex, 5 tbl

FIELD: cosmetic products.

SUBSTANCE: invention relates to antiperspirant compositions for human skin application methods for production and uses thereof. Transparent anhydrous antiperspirant compositions contain from 1 to 30 mass % of quick antiperspirant salt dispersed in water immiscible liquid carrier, which is cured with effective amount of structuring agent.

EFFECT: compositions with improved transparency.

32 cl, 4 ex, 5 tbl

FIELD: technique for producing of biologically active substances based on water-containing substances such as solution, syrup, saccharine, cream, paraffin, homeopathic balls, nosodes and other substances capable of structuring.

SUBSTANCE: apparatus has signal source 1 for emitting signal at a frequency f1, signal source 2 for emitting signal at a frequency f2, emitter 3, and amplifier 4. Emitter may be made in the form of metal plate, inductance coil, or it may be made of acoustic type.

EFFECT: provision for producing of biologically active substances with various predetermined activity.

5 cl, 5 dwg

FIELD: medicine, endocrinology.

SUBSTANCE: invention relates to a method for treatment diabetes mellitus of type 2. Method involves using a birch bark extract in addition to usually used preparations. Method provides enhancing the effectiveness of treatment based on sugar-decreasing, antioxidant and hypolipidemic properties of biologically active components of birch extract.

EFFECT: improved and enhanced method of treatment.

14 tbl

FIELD: cosmetic industry.

SUBSTANCE: it is necessary to carry out immobilization of native casein of goat milk at 50°C obtained as a result of flocculation onto methyl cellulose followed by introducing fucoidane hydrolyzate, silver nitrate and glycoproteins of mucus of animal origin at the ratio of components that provide the following ratios of cream's components, weight%: glycoproteins of mucus of animal origin 13.0-15.0; native casein of goat milk 30.0-35.0; methyl cellulose 30.0-35.0; silver nitrate 2.0-2.5; fucoidane hydrolyzate 15.0-22.5.

EFFECT: higher efficiency.

7 cl, 2 ex, 1 tbl

FIELD: medicine.

SUBSTANCE: method involves carrying out immobilization of protein on methylcellulose used as a high-molecular compound and modification of its surface. Goat native milk casein prepared by flocculation is immobilized on its surface at temperature 50°C. Then silver nitrate and fucoidan are added in the ratio of components providing the following ratio of components in the agent, wt.-%: goat native casein, 40-45; methylcellulose, 40-45; silver nitrate, 0.5-2.5, and fucoidan, 9.5-17.5. Invention provides expanding antibacterial and wound-healing agents.

EFFECT: improved preparing method of agent.

7 cl, 1 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: method involves administering immune correction therapy, vitamin C and group B vitamins, local treatment with antivirus ointments, antiseptics and analgesic remedies, as well as phytotherapy with helium-neon laser treatment. Fentaline, Thianeptine, Bioparox, oral rinsing with 0.1% aqueous Levamisol solution prepared immediately before being applied. Gltoxime is administered at the tenth day beginning from the exacerbation onset. 20% Levocarnitine solution and oral rinsing with 10% aqueous ASD-2F solution prepared immediately before being applied. Ajurvedic preparation Chavanprash is additionally prescribed for 108 days and then daily from full moon to full moon 1 year long. Tooth pastes like Cloves and Sweet Basil are to be alternatively applied during the whole treatment period.

EFFECT: enhanced effectiveness of treatment; prevented relapses; normalized mental and emotional state of patients.

3 cl, 1 dwg, 2 tbl

FIELD: medicine.

SUBSTANCE: method involves administering immune correction therapy, vitamin C and group B vitamins, local treatment with antivirus ointments, antiseptics and analgesic remedies, as well as phytotherapy with helium-neon laser treatment. Fentaline, Thianeptine, Bioparox, oral rinsing with 0.1% aqueous Levamisol solution prepared immediately before being applied. Gltoxime is administered at the tenth day beginning from the exacerbation onset. 20% Levocarnitine solution and oral rinsing with 10% aqueous ASD-2F solution prepared immediately before being applied. Ajurvedic preparation Chavanprash is additionally prescribed for 108 days and then daily from full moon to full moon 1 year long. Tooth pastes like Cloves and Sweet Basil are to be alternatively applied during the whole treatment period.

EFFECT: enhanced effectiveness of treatment; prevented relapses; normalized mental and emotional state of patients.

3 cl, 1 dwg, 2 tbl

FIELD: medicine, gynecology.

SUBSTANCE: at the first stage it is necessary to introduce a protein-vitamin complex "Kedrovaya sila" ("Cedar power") per 1 table spoon thrice daily for 1 mo, moreover, for about 5-7 d one should inject antibiotic under vaginal musosa at ¼ daily dosage, and a suppository with trypsin rectally. Then, in 15 min it is important to carry out physiotherapy with sinusoidal modulated currents. At the second stage a woman should be inspected by otorhinolaringologist and gastroenterologist and according to indications specialized testing and therapy should be carried out. At the third stage during 3 mo it is necessary to follow cyclic vitaminotherapy. In the first half of menstrual-ovarian cycle one should prescribe vitamin B6 per 0.015 g daily; folic acid 0.03 g. During the second half of the cycle one should introduce vitamin C 0.3-0.5 g thrice daily and capsulated cedar oil with vitamin E per 2 capsules thrice daily. Moreover, during 6 mo one should prescribe adaptogens: eleutherococcus, or leusea, golden root, or ginseng tincture under standard dosages. The innovation provides normalization of biochemical, immune and hormonal indices, reconstruction of reproductive function and the absence of relapses during 3 yr.

EFFECT: higher efficiency of prophylaxis and therapy.

1 ex

FIELD: medicine, gynecology.

SUBSTANCE: at the first stage it is necessary to introduce a protein-vitamin complex "Kedrovaya sila" ("Cedar power") per 1 table spoon thrice daily for 1 mo, moreover, for about 5-7 d one should inject antibiotic under vaginal musosa at ¼ daily dosage, and a suppository with trypsin rectally. Then, in 15 min it is important to carry out physiotherapy with sinusoidal modulated currents. At the second stage a woman should be inspected by otorhinolaringologist and gastroenterologist and according to indications specialized testing and therapy should be carried out. At the third stage during 3 mo it is necessary to follow cyclic vitaminotherapy. In the first half of menstrual-ovarian cycle one should prescribe vitamin B6 per 0.015 g daily; folic acid 0.03 g. During the second half of the cycle one should introduce vitamin C 0.3-0.5 g thrice daily and capsulated cedar oil with vitamin E per 2 capsules thrice daily. Moreover, during 6 mo one should prescribe adaptogens: eleutherococcus, or leusea, golden root, or ginseng tincture under standard dosages. The innovation provides normalization of biochemical, immune and hormonal indices, reconstruction of reproductive function and the absence of relapses during 3 yr.

EFFECT: higher efficiency of prophylaxis and therapy.

1 ex

FIELD: medicine, oncology, amino acids.

SUBSTANCE: invention relates, in particular, to the development of an antitumor preparation based on natural substances. Invention relates to an amino acid preparation comprising at least one modified essential amino acid obtained by treatment of amino acid by ultraviolet radiation (UV) at wavelength 250-350 nm for 12-80 h at temperature 15-30oC or with ozone at temperature 15-25oC. The modified amino acid has no toxicity for health cells. Also, invention relates to a method for preparing such preparation. Invention provides the development of an antitumor preparation based on modified amino acids and expanded assortment of antitumor preparations being without cytotoxicity for normal cells.

EFFECT: valuable medicinal antitumor properties of preparation.

8 cl, 4 tbl, 2 dwg, 4 ex

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