Compositions for hair growth enhancement and/or recovery

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetology, namely represents a composition containing minoxidil and/or minoxidil sulphate combined with additives containing at least one antioxidant, at least one organic acid and selected fatty acids mixture. Besides, the invention refers to using the compounds for hair growth enhancement/recovery and/or hair loss prevention in mammals, particularly in a human.

EFFECT: using the invention provides faster anagen phase in mammalian hair growth and/or enhanced terminal hair above the skin surface by local application the declared compositions.

19 cl, 9 tbl

 

AREA of TECHNOLOGY

The present application relates to compositions containing certain pyrimidine compounds such as Minoxidil, and certain compounds of the pyrimidine sulfate, for example, Minoxidil sulfate and especially compounds containing a pyrimidine, in combination with mixtures containing at least one antioxidant, at least one organic acid and a selected mixture of fatty acids. The present application also relates to the use of compounds for hair growth and/or to prevent their loss in mammals, particularly in humans.

Background of the INVENTION

I believe that the various pyrimidine compounds contribute to the growth and/or regrowth in mammals, including humans. For example, see U.S. patent No. 4139619 Chidsey, III, the subject of which is incorporated in this application by reference. In particular, Minoxidil (6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinylidene currently used as a drug to promote hair growth, as well as for the treatment of baldness in males.

Recently it was proposed to use the sulfates of certain pyrimidines, such as Minoxidil sulfate, as a means for hair growth in mammals. In particular, see U.S. patent No. 4287338. It is reported that the effect of sulphate on the growth of hair occurs fast�her and more pronounced than the action of Minoxidil.

In certain situations, and/or segments of the market more rapid and/or intense growth or regrowth is subject to ongoing requests or purpose, so research on the development of improved drugs for hair growth does not cease.

Accordingly, an object of the present invention is compositions for the growth and/or recurrence of hair growth, which can be used to treat or prevent hair loss, or for a more dense growth.

Another object of the present invention is the use of compositions pertaining to the present invention, which accelerate the onset of the anagen phase in hair growth cycle in mammals.

Another aspect of the present application is the use of the compositions of the present invention to accelerate the development of terminal hair on a certain area of the skin.

Another object of the present invention relates to compositions containing at least one pyrimidine compound and a mixture comprising at least one antioxidant, at least one organic acid and a selected mixture of fatty acids or fatty acid sources, and represents an advanced tool for elimination or prevention of hair loss.

To�WAY description of the INVENTION

The present invention relates to preparations containing at least one of the pyrimidine compounds described in U.S. patent No. 4139619 and/or at least one compound of the pyrimidine sulfate as described in U.S. patent No. 4287338; both patents incorporated herein by reference.

More specifically, one embodiment of the present invention relates to compositions for the growth or recurrence of hair growth, containing;

a. at least one compound selected from the following group of compounds represented by the formulas:

The formula I

and

Formula II,

and mixtures thereof,

where R1represents a functional group selected from the following functional groups with the formula-N(R3)(R4), where R3and R4selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower aralkyl and lower cycloalkyl, and R3and R4may represent a heterocyclic functional group selected from the group comprising: aziridinyl, azetidin, pyrrolidine, the piperidine hexahydroazepin, heptamethylnonane, octamethylene, morpholine and lower 4-alkylpiperazine, each of the heterocyclic functional groups has 0-3 Deputy in the form NISS�th alkyl, hydroxyl or alkoxylic one group of carbon atoms; and where R2is selected from the following group comprising: hydrogen, lower alkyl, lower alkenyl, lower alkoxyalkyl, low cycloalkyl, lower aryl, lower aralkyl, low alkaryl, low alcalali, low alkoxyalkyl, and halogen-substituted lower alkyl, and pharmaceutically acceptable salts of these compounds, obtained by attaching acid; and

b. from about 0.1% to about 99%, from about 5% to about 50%, and possibly from about 10% to about 40%, may be from about 15% to about 30% (mass.) additives containing:

i. perhaps from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or from 30% to 40%, or perhaps approximately 33% (mass.) acid selected from the group including intermediates of the Krebs cycle intermediate alpha-keto-acids that are not related to the Krebs cycle, their derivatives and mixtures;

ii. perhaps from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) antioxidant; and

iii. from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) �IRNA acids or fatty acid sources, containing at least 7, at least 14, and possibly at least 22, unsaturated or saturated fatty acids selected from the group including, without limitation, butyric acid, caproiu acid, Caprylic acid, capric acid, lauryl acid, myristic acid, myristoleate acid, palmitic acid, palmitoleate acid, stearic acid, oleic acid, linoleic acid, linolenic acid, arachidonoyl acid, gadolinium acid, pentadecanoic acid, margaric acid, margarino acid, behenic acid, digabriele acid, arachidonic acid and lignoceric acid.

In another embodiment of the present invention relates to compositions for the growth or recurrence of hair growth, including;

a. at least one compound selected from the following group of compounds represented by the formulas:

The formula I

and

Formula II,

and mixtures thereof,

where R1represents a functional group selected from the following functional groups with the formula-N(R3)(R4), where R3and R4selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower aralkyl and lower cycloalkyl, and g�PI R 3and R4may represent a heterocyclic functional group selected from the group comprising: aziridinyl, azetidin, pyrrolidine, the piperidine hexahydroazepin, heptamethylnonane, octamethylene, morpholine and lower 4-alkylpiperazine, each of the heterocyclic functional groups has 0-3 Deputy in the form of lower alkyl, hydroxyl or alkoxylic one group of carbon atoms; and where R2is selected from the following group comprising: hydrogen, lower alkyl, lower alkenyl, lower alkoxyalkyl, low cycloalkyl, lower aryl, lower aralkyl, low alkaryl, low alcalali, low alkoxyalkyl, and halogen-substituted lower alkyl, and pharmaceutically acceptable salts of these compounds, obtained by attaching acid; and

b. from about 0.1% to about 99%, from about 5% to about 50%, and possibly from about 10% to about 40%, from about 15% to about 30% (mass.) additives containing:

i. from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) alpha-ketoacids;

ii. from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or maybe about�olo 33% (mass.) antioxidant; and

iii. from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33%, from approximately 2.0% to approximately 33.3 per cent, and possibly from about 2.0% to about 7.0% (mass.) a mixture of fatty acids or sources of fatty acids containing at least 7, at least 14, and possibly at least 22, unsaturated or saturated fatty acids selected from the group including, without limitation, butyric acid, caproiu acid, Caprylic acid, capric acid, lauryl acid, myristic acid, myristoleate acid, palmitic acid, palmitoleate acid, stearic acid, oleic acid, linoleic acid, linolenic acid, arachidonoyl acid, gadolinium acid, pentadecanoic acid, margaric acid, margarosanite acid, behenic acid, digabriele acid, arachidonic acid and lignoceric acid.

In the following embodiment of the present invention relates to compositions for acceleration and/or the resumption of hair growth, containing;

a. at least one compound selected from the following group of compounds represented by the formulas:

The formula I

and

/p>

Formula II,

and mixtures thereof,

where R1represents a functional group selected from the following functional groups with the formula-N(R3)(R4), where R3and R4selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower aralkyl and lower cycloalkyl, and R3and R4may represent a heterocyclic functional group selected from the group comprising: aziridinyl, azetidin, pyrrolidine, the piperidine hexahydroazepin, heptamethylnonane, octamethylene, morpholine and lower 4-alkylpiperazine, each of the heterocyclic functional groups has 0-3 Deputy in the form of lower alkyl, hydroxyl or alkoxylic one group of carbon atoms; and where R2is selected from the following group comprising: hydrogen, lower alkyl, lower alkenyl, lower alkoxyalkyl, low cycloalkyl, lower aryl, lower aralkyl, low alkaryl, low alcalali, low alkoxyalkyl and halogen-substituted lower alkyl, and pharmaceutically acceptable salts of these compounds, obtained by attaching acid; and

b. from about 0.1% to about 99%, from about 5% to about 50%, and possibly from about 10% to about 40%, from about 15% to about 30% (mass.)supplements containing:

i) from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) acid selected from the group, consisting of pyruvic acid, its salts and mixtures thereof:

ii) from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) tocopherol or its ester; and

iii) from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) a mixture of fatty acids or their sources, a mixture of sources of fatty acids is an oil mixture that contains:

i) from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) olive oil;

ii) from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) coconut oil; and

iii) from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) cottonseed oil.

In the following embodiment of the present invention relates to compositions for accelerating and/or in�pack of hair growth, contains;

a. at least one compound selected from the following group of compounds represented by the formulas:

The formula I

and

Formula II,

and mixtures thereof,

where R1represents a functional group selected from the following functional groups with the formula-N(R3)(R4), where R3and R4selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower aralkyl and lower cycloalkyl, and R3and R4may represent a heterocyclic functional group selected from the group comprising: aziridinyl, azetidin, pyrrolidine, piperidine, hexahydroazepin, heptamethylnonane, octamethylene, morpholine and lower 4-alkylpiperazine, each of the heterocyclic functional groups has 0-3 Deputy in the form of lower alkyl, hydroxyl or alkoxylic one group of carbon atoms; and where R2is selected from the following group comprising: hydrogen, lower alkyl, lower alkenyl, lower alkoxyalkyl, low cycloalkyl, lower aryl, lower aralkyl, low alkaryl, low alcalali, low alkoxyalkyl, and halogen-substituted lower alkyl, and pharmaceutically acceptable salts of these compounds, obtained by attaching acid; and

i. from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) acid selected from the group consisting of pyruvic acid, its salts and mixtures;

ii. from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) antioxidant; and

iii. from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) a mixture of fatty acids or of fatty acids,

in which the ratio of the pyruvic acid is from 0.01:1 (or about 0.01:1 to 1:0.01 to about 1:0,01); the ratio of pyruvic acid to the antioxidant from 0.01:1 (or about 0.01:1 to 1:0.01 (or about 1:1,01); and the ratio of the mixture of fatty acids and antioxidant from 0.01:1 (or about 0.01:1 to 1:0.01 (or about 1:0,01), or perhaps the ratio of pyruvic acid or mixture of fatty acids to antioxidant is from 1:1 (or about 11) to 1:0.01 (or about 1:0,01).

In one of the embodiments of the present invention relates to compositions containing:

a. from approximately 0.1% to approximately 20% (mass.), at least one compound selected from the group consisting of compounds represented by the formulas:

The formula I

and

Formula II,

and mixtures thereof,

where R1represents a functional group selected from the following functional groups with the formula-N(R3)(R4), where R3and R4selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower aralkyl and lower cycloalkyl, and R3and R4may represent a heterocyclic functional group selected from the group comprising: aziridinyl, azetidin, pyrrolidine, the piperidine hexahydroazepin, heptamethylnonane, octamethylene, morpholine and lower 4-alkylpiperazine, each of the heterocyclic functional groups has 0-3 Deputy in the form of lower alkyl, hydroxyl or alkoxylic one group of carbon atoms; and where R2is selected from the following group comprising: hydrogen, lower alkyl, lower alkenyl, lower alkoxyalkyl, low cycloalkyl, lower aryl, lower aralkyl, low alkaryl, low alcalali, lower alkoxyalkyl�, and halogen-substituted lower alkyl, and pharmaceutically acceptable salts of these compounds, obtained by attaching acid; and

b. 5% (or approximately 5%) to 10% (or approximately 10%), possibly from 6% (or approximately 6%) to approximately 8% (or approximately 8%) (mass.) acid;

c. 5% (or approximately 5%) to 10% (or approximately 10%), possibly from 6% (or approximately 6%) to approximately 8% (or approximately 8%) (mass.) antioxidant; and

d. 5% (or approximately 5%) to 10% (or approximately 10%), possibly from 6% (or approximately 6%) to approximately 8% (or approximately 8%) (mass.) a mixture of fatty acids or of fatty acids, wherein the mixture of fatty acids or of fatty acids contains:

i) from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) first oil;

ii) from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) the second oil; and

iii) from 0.01% up to 99.98% or possibly 10% to 90% or perhaps 20% to 70%, or maybe 25% to 50% or perhaps 30% to 40%, or perhaps approximately 33% (mass.) acids third of the oil.

The present invention is applicable to all mammalian species, including� animals and humans. In humans the composition of the present invention can be applied, for example, on the scalp, groin area, upper lip, eyebrows and eyelids. In fur-bearing animals such as mink, the compositions can be applied to the entire surface of the body to improve the quality of furs for commercial purposes. The compositions can also be applied to animals such as dogs and cats, for cosmetic purposes, in the presence of foci of alopecia due to the infestation of scabies or other reasons.

Other objects of the present invention will become apparent to experts in this field from the following detailed description, which shows and describes only the preferred embodiments of the invention that illustrate the best way. It should be understood that the invention may have other options of implementation, and its several details can be modified in various obvious reasons, without deviation from the spirit of the invention. Accordingly, the present description should be considered as illustrating the invention and in no way limiting.

DETAILED description of the INVENTION

The compositions according to the present invention can include, consist of, or consist primarily of essential elements and features of the invention described in this document and any additional or used for choosing �of ngredients, components or features of the invention described herein.

In the context of this publication, the term "containing" (and its grammatical variants) is used in the meaning including the concept of "comprising" or "comprising" and not preclude the sense of "consisting only of". In the context of this publication, it is considered that the terms apply both to the singular and the plural.

All documents are fully incorporated herein by reference, is included only to the extent that they are inconsistent with this specification.

All percentage concentrations, parts and ratios are based on the total mass of the composition according to the present invention, if not specified. All such mass relating to listed ingredients are based on the content of active substance and, therefore, do not include carriers or by-products that may be included in commercially available materials, unless otherwise indicated.

The term "safe and effective dose" as used herein means that dose of a compound or composition of local or systemic action, sufficient to bring significant benefits, for example, to cause the growth or regrowth, but low enough to avoid serious side-effect�projects, i.e., to ensure a reasonable ratio of benefit/risk within the sound judgment of a specialist in this field.

The pyrimidine compound

The compositions of the present invention contain at least one compound represented by the formula:

The formula I

and/or

Formula II

R1represents a functional group selected from groups of the formula-N(R3)(R4).

Each R3and R4individually selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower aralkyl and low cycloalkyl, and the groups R3 and R4 may be a heterocyclic functional group selected from the following: aziridinyl, azetidin, pyrrolidine, piperidine, hexahydroazepin, heptamethylnonane, octamethylene, formalin and 4-low alkylpiperazine, wherein each of the heterocyclic functional groups has 0-3 Deputy in the form of lower alkyl, hydroxyl or alkoxylic one group of carbon atoms, and where R2is selected from the group including hydrogen, lower alkyl, lower alkenyl, lower alkoxyalkyl, low cycloalkyl, lower aryl, lower aralkyl, low alkaryl, low alcalali, low alkoxyalkyl and halogen-substituted lower alkyl, and pharmaceutically acceptable salts obtained p�Saedinenie acid.

The content of compounds of the above formulas I and/or II is a safe and effective amount, contributing to the acceleration and/or regrowth. In certain embodiments, compounds of formulas I and/or II are present in a concentration from 0.1% (or 0.1%) to 20% (or approximately 20.0 percent) of the drug, or possibly from about 0.5% to about 10% (mass.).

Listed below are the various terms used to describe the present invention. These definitions only apply to the terms used in this application, unless specifically stated otherwise, individually or as part of a larger group.

The term “lower alkyl” means a hydrocarbon straight or branched chain, usually consisting of 1-6 carbon atoms or, more common, from 1 to 3 carbon atoms.

Examples of suitable lower alkyl groups include methyl, ethyl and propyl. Examples of branched alkyl groups include isopropyl and t-butyl. Examples of suitable alkoxylic one of the groups include methoxy-, ethoxy - and propoxylate.

Group “lower cycloalkyl” usually contain 3-6 carbon atoms and include cyclopropyl, cyclobutyl and cyclopentyl.

The term “lower alkenyl” means a group, which usually contains 2-6 carbon atoms and includes ethenyl, propenyl and butenyl

Group “lower cycloalkenyl” usually contain 3-6 carbon atoms and include cyclopropyl, cyclobutenyl, cyclopentenyl and cyclohexenyl.

The term “lower aryl” means a monocyclic or containing multiple aromatic hydrocarbon rings, generally containing from 6 to 14 carbon atoms in the ring, e.g., phenyl, 2-naphthyl, 1-naphthyl, 4-biphenyl, 3-biphenyl 2-biphenyl and diphenyl.

Examples of Halogens include Cl, F, Br and I.

Compounds of Formulas I and/or II may also be dissolved in organic solvents, e.g., dimethylsulfoxide (DMSO), acetonitrile, dimethylformamide (DMF), dimethylacetamide (DMA), propylene glycol/ethanol/water and their mixtures.

In addition, the compositions can be dissolved in or contain auxiliary substances, such as acids (in particular lactic acid) or alcohol additives to improve solubility. For example, the compositions of the present invention may additionally include a solubilizer for compounds of formulas I and/or II, as described in U.S. patent No. 5652274, incorporated herein by reference. In other embodiments, suitable soljubilizatory include propylene glycol and alcohol. The solubilizer, if present, may be contained in an amount of from about 1% to about 60%, or possibly from approx�flax 20% to about 50%.

Lactic acid or lactate, if used, can be selected from the group consisting of lactic acid, precursors of lactic acid and mixtures thereof. Salt of lactic acid may include, without limitation, salts of alkali and alkaline earth metals. In certain embodiments, the lactate is selected from the group comprising lactic acid, lithium lactate, sodium lactate, potassium lactate, magnesium lactate, calcium lactate, zinc lactate, manganese lactate, etc., and also mixtures. In other embodiments, the lactate is selected from the group comprising lactic acid, lithium lactate, sodium lactate, potassium lactate, magnesium lactate, calcium lactate, zinc lactate, manganese lactate, etc., and also mixtures. In another embodiment, lactate is a lactic acid.

Lactate if present in the composition of the present invention is contained in an amount sufficient to dissolve the compound of formula I or formula II. In certain embodiments, the lactate is contained in an amount of from about 0.05% to about 50%, from about 1.0% to about 45%, or perhaps from about 1.0% to about 5.0 percent, by weight of the composition.

Supplement

The compositions of the present invention further includes�Ute additive containing: 1) an acid selected from the group consisting of intermediates of the Krebs cycle, the intermediate keto acid, not related to the Krebs cycle, their derivatives and mixtures; and/or an antioxidant and 2) a mixture of saturated and unsaturated fatty acids.

In certain embodiments, the additive is present in the composition in a concentration from 0.1% (or 0.1%) to 99% (or approximately 99%), possibly 3% (or approximately 3%) to 75% (or approximately 75%) of perhaps 5% (or approximately 5%) to 50% (or approximately 50%), perhaps 10% (or approximately 10%) to 40% (or approximately 40%), possibly from 15% (or approximately 15%) to 30% (or approximately 30%), or possibly from 19% (or approximately 19%) to 23% (or approximately 23%) (masses).

Acid

In certain embodiments, the acid included in the composition of the additive of the present invention, is selected from the group consisting of derivatives of the Krebs cycle, alpha-keto acids that are not related to the Krebs cycle, their derivatives and mixtures.

Derivatives of the Krebs cycle (or citric acid cycle) used in the present invention include, without limitation, 2-oxoglutarate, fumarate, succinate, oxaloacetate, citrate, CIS-aconitate, isocitrate, oxalosuccinic, alpha-Ketoglutarate, L-malate, complex and simple esters or salts, as well as their �MESI.

In other embodiments, the acid is an intermediate ketokislot not related to the Krebs cycle (or 2-oxanilate). Alpha-keto acid (or 2-oxanilate) has a ketone group adjacent to the carboxylic acid group. Under "intermediate product, not related to the Krebs cycle" herein refers to a chemical compound or an intermediate product is not formed in the Krebs cycle or the citric acid cycle. In certain embodiments, alpha-ketoacids, not related to the products of the Krebs cycle include, without limitation, pyruvic acid (alpha-ketopropane acid), alpha-ketoisovaleric acid alpha-ketoisocaproic acid, their salts and mixtures. However, it should be understood that, in addition to these alpha-keto acids, the term "alpha-keto acid" further includes, without limitation, alpha-ketoglutaric acid.

In certain embodiments, as an alpha-keto acid pyruvic acid is used. Pyruvic acid, suitable for use in the present invention, can be selected from the group consisting of pyruvic acid, its prodrug, or their mixtures. In certain embodiments, salts of pyruvic acid can be a Sol� alkali and alkaline earth metals. In certain embodiments, pyruvic acid is selected from the group consisting of pyruvic acid, lithium pyruvate, sodium pyruvate, potassium pyruvate, magnesium pyruvate, calcium pyruvate, zinc pyruvate, manganese pyruvate, methyl ester of pyruvic acid, and mixtures thereof.

In other embodiments, pyruvic acid is selected from the group consisting of sodium pyruvate, potassium pyruvate, magnesium pyruvate, calcium pyruvate, zinc pyruvate, manganese pyruvate, etc. and mixtures thereof. In other embodiments, pyruvic acid is a sodium pyruvate.

Not limited to a specific theory, it is believed that the acid in the additive serves as a source of energy. In certain embodiments, the acid is present in an amount of from 0.01% (or about 0.01%) up to 99.98% (or approximately 99,98%), or perhaps 10% (or approximately 10%) to 90% (or approximately 90%), or perhaps 20% (or approximately 20%) to 70% (or approximately 70%), or, perhaps, from 25% (or approximately 25%) to 50% (or approximately 50%), or perhaps 30% (or approximately 30%) to 40% (or approximately 40%), or perhaps approximately 33% of the mass

Antioxidant

Antioxidants, as mentioned above, are also present in cm�C of the present invention. In General, antioxidants are substances that inhibit oxidation or reactions, accelerating under the action of oxygen or peroxides. Not limited to a specific theory, it is believed that antioxidants, or perhaps fat-soluble antioxidants that can be absorbed by the cell membrane and neutralize oxygen radicals, thereby protecting the hair follicles from oxidative damage. In certain embodiments, the antioxidant can be selected from the group that includes all forms of vitamin A, including lycopene, lutein, retinal and 3,4-delegitimating, all forms of carotene such as alpha-carotene, beta-carotene, gamma-carotene, Delta-carotene, all forms of vitamin C (D-ascorbic acid, L-ascorbic acid), all forms of tocopherol, such as vitamin E (alpha-tocopherol), 3,4-dihydro-2,5,7,8-tetramethyl-2-(4,8,12-trimethylacetyl)-2H-1-benzopyran-6-ol), beta-tocopherol, gamma-tocopherol, Delta-tocopherol, takkinen, tocotrienol and esters of vitamin E, rapidly undergo hydrolysis to vitamin E, for example, acetate and succinate vitamin E, salts of vitamin E, for example, phosphate, prodrugs of vitamin A, carotene, vitamin C and vitamin E, salts of vitamin A, carotene, vitamin C and vitamin E, etc., flavonoids, and mixtures thereof. Flavonoids used in the present invention, described� in U.S. patent No. 6051602 Bissett, which is incorporated herein by reference. In another embodiment, the antioxidant is selected from the group of fat-soluble antioxidants, including vitamin a, beta-carotene, tocopherol, and mixtures thereof. In other embodiments, the antioxidant is a tocopherol, vitamin E acetate vitamin E. In other embodiments, the antioxidant is a polyphenol, for example, resveratrol or epigallocatechin gallate.

In certain embodiments, the antioxidant is present in the composition in an amount of from 0.01% (or about 0.01%) up to 99.98% (or approximately 99,98%), or perhaps 10% (or approximately 10%) to 90% (or approximately 90%), or perhaps 20% (or approximately 20%) to 70% (or approximately 70%), or, perhaps, from 25% (or approximately 25%) to 50% (or approximately 50%), or perhaps 30% (or approximately 30%) to 40% (or approximately 40%), or perhaps approximately 33% (mass.).

In certain embodiments, the ratio of the acid content and antioxidant (mass.) is from about 0.01:1 (or about 0.01:1 to 1:0.01 (or about 1:0.01), and perhaps from 1:1 (or about 1:1 to 1:0.1 (or about 1:0,1), perhaps from 1:1 (or about 1:1 to 1:0.5 (or approaching�Uo 1:0.5).

The mixture of fatty acids or fatty acid sources

Supplement relating to the present invention, also contains a mixture of saturated or unsaturated fatty acids, free or bound, or source of such saturated or unsaturated fatty acids, which can serve as a readily available source of nutrients for the hair follicles.

Suitable mixtures of saturated or unsaturated fatty acids can be derived from animal or vegetable fats and waxes, mammals or fish eggs, predecessors of saturated or unsaturated fatty acids used in the present invention, or their mixtures. Fatty acids in the mixture of fatty acids may be present in the form of mono-, di - or triglycerides, free fatty acids or their mixtures.

In one of the embodiments of the invention a mixture of saturated or unsaturated fatty acids has a composition similar to the composition of adipose tissue of man, and includes the following fatty acids: butyric acid, Capraia acid, Caprylic acid, capric acid, laurinova acid, myristic acid, myristoleate acid, palmitic acid, palmitoleate acid, stearic acid, oleic acid, linoleic acid, linolenic acid, orhideea acid, chomolangma acid, arachidonic acid, running�OIC acid, lignocellulose acid and gadolinia acid. Usually, butyric acid, Capraia acid, Caprylic acid, capric acid, laurinova acid, maistrova acid, myristoleate acid, palmitic acid, palmitoleate acid, stearic acid, oleic acid, linoleic acid, linolenic acid, orhideea acid and gadolinia acid present in the mixture in the following weight percent proportions, respectively: approximately 0.2-0.4% of butyric acid, approximately 0.1% of Chapaevo acid, approximately 0.3 to 0.8% Caprylic acid, about 2.2 to 3.5% capric acid, about 0.9 5.5% of laurinova acid, approximately 2,8-8,5% myristic acid, about 0.1 to 0.6% myristoleate acid, approximately 23,2-24,6% palmitic acid, about 1.8 to 3.0% by palmitoleic acid, approximately 6,9-9,9% stearic acid, about 36,0-36.5% of oleic acid, approximately 20-20,6% linoleic acid, about 7.5-7.8% of linolenic acid, approximately 1.1 to 4.9% arachinovo acid, approximately 2-3% digomolinolenovoy acid, approximately 7-9% of arachidonic acid, approximately 3-4% of beganovi acid, approximately 11-13% of lignoceric acid and approximately 3,3-6,4% gadolinia acid.

In another embodiment of the invention the mixture on�imennyh and unsaturated fatty acids has a composition, similar to the composition of chicken fat, and contains the following fatty acids: laurinova acid, myristic acid, myristoleate acid, pentadecanoic acid, palmitic acid, palmitoleate acid, heptadecanoic acid, margarina acid, stearic acid, oleic acid, linoleic acid, linolenic acid, orhideea acid and gadolinia acid. Perhaps laurinova acid, maistrova acid, myristoleate acid, pentadecanoic acid, palmitic acid, palmitoleate acid, heptadecanoic acid, margarina acid, stearic acid, oleic acid, linoleic acid, linolenic acid orhideea acid and gadolinia acid present in the mixture in about the following weight percent proportions, respectively: approximately 0.1% of laurinova acid, approximately 0.8% ministerului acid, about 0.2% myristoleate acid, approximately 0.1% pentadecanoic acid, approximately 25.3% of palmitic acid, approximately 7.2% of palmitoleate acid, approximately 0.1% margaric acid, approximately 0.1% heptadecanoic acid, approximately 6.5% of stearic acid, approximately 37.7% of oleic acid, approximately 20.6 percent linoleic acid, about 0.8% of linolenic acid, approximately�about 0.2% arachinovo acid and approximately 0.3% gadolinia acid.

In certain other embodiments, the mixture of saturated and unsaturated fatty acids has a composition similar to the composition of lecithin. Lecithin (phosphatidylcholine) is phosphated contained in all living organisms (plants and animals) and is an important component of nervous tissue and brain tissue. Lecithin is a mixture of diglycerides of stearic acid, palmitic acid and oleic acids linked to the choline ester of phosphoric acid. A product designed for commercial applications, is a predominantly soy lecithin, obtained as a by-product in the production of soybean oil. Soy lecithin contains palmitinovuyu acid in the amount of 11.7% (mass.), stearic acid in the amount of 4.0% (mass.), politologue acid in the amount of 8.6% (mass.), oleic acid in the amount of 9.8% (mass.), linoleic acid in the amount 55,0% (mass.), linolenic acid in the amount of 4.0% (mass.), acid, C20-C22(including arachidonic acid) in an amount of 5.5% (mass.). Lecithin can be represented by the formula: C8H17O5NR9R10in which each group R9and R10independently selected from the group consisting of stearic acid, palmitic acid and oleic acid.

In defined�s other embodiments, the mixture of saturated and unsaturated fatty acids has a composition, similar to the composition of egg yolk. Composition of the most prevalent mixture of fatty acids in egg yolk has the following mass composition:

A. unsaturated fatty acids, e.g. oleic acid (about 47%), linoleic acid (approximately 16%), palmitoleate acid (approximately 5%) and linolenic acid (about 2%); and

B. saturated fatty acids: for example, palmitic acid (approximately 23%), stearic acid (approximately 4%) and myristic acid (approximately 1%).

Egg yolk is also a source of lecithin.

The above mixture of fatty acids (or fatty acid sources) and the percentages of fatty acids (or sources) in various mixtures are given as examples. The exact type of fatty acids present in the mixture of fatty acid (or mixture of sources) and the exact amount of fatty acids in the mixture of fatty acid (or mixture of sources) can be varied to produce the desired end-product results, and such variations are known to specialists in this field and do not require further experiments.

In certain embodiments of the present invention, the mixture of fatty acids or fatty acid sources contains at least 7, at least 14, and possibly at least 22, unsaturated or n�over-enriched fatty acids, selected from the group including, without limitation, butyric acid, caproiu acid, Caprylic acid, capric acid, lauryl acid, myristic acid, myristoleate acid, palmitic acid, palmitoleate acid, stearic acid, oleic acid, linoleic acid, linolenic acid, arachidonoyl acid, gadolinium acid, pentadecanoic acid, margaric acid, margarino acid, behenic acid, digabriele acid, arachidonic acid, lignoceric acid. Other potential fatty acids described in U.S. patent No. 4874794 Adachi et al., which is incorporated herein by reference.

In certain embodiments, the mixture of fatty acids derived from oily mixtures or oil mixtures are its source. For example, the ratio of the concentration of polyunsaturated and saturated fatty acids in cottonseed oil is 2:1. It generally consists of 70% unsaturated fatty acids including 18% monounsaturated (oleic), 52% polyunsaturated (linoleic) and 26% saturated (mainly palmitic and stearic). More specifically, the fatty acid composition of cottonseed oil in the mixture in percent by weight is as follows: about 0.5 to 2.0% myristic acid, about 17,0-29,0% palmitic acid, less than approximately 5% palmitoleate acid, approximately 1.0 to 4.0% stearic acid, approximately 13.0-44.0 per cent of oleic acid, approximately 40,0-63,0% linoleic acid and about 0.1 to 2.1% of linolenic acid.

Mass fatty acid composition of cocoa butter in the mixture about the following: at least about 0.1% myristic acid, about 0.5-26.3% of palmitic acid, at least about 0.4% palmitoleate acid, about 0.5 to 33.8% stearic acid, about 0.5-34,4% oleic acid and about 0.5-3.1% of linolenic acid.

According to one study, olive oil has the following mass composition of fatty acids: approximately 0,5-9,0% palmitic acid, at least about 0.4% palmitoleate acid, about 0.5 to 2.7% stearic acid, about 0.5-80.3% of oleic acid, about 0.5 to 6.3% linoleic acid and about 0.5 to 0.7% linolenic acid.

Oils that can be used as a source of a mixture of fatty acids include, without limitation, oil of adansonia digitata; apricot kernel oil (Prunus armeniaca); oil agrani barbed; oil of agramon Mexican; avocado oil (Persea gratissima) oil the Bubba (Orbignya olelfera); peppermint oil (Melissa officinalis); oil of bitter almonds (Prunus amygdalus amara) oil cherry (Prunus cerasus); black currant oil (Ribes nigrum); �aslo borage (Borago officinalis); oil Brazil nut (Bertholletia excelsa); the seed oil of burdock (Arctium lappa); butter; oil calophylla (Calophyllum tacamahaca); Camellia oil (Camellia kissi); seed oil Camellia (Camellia oleiferal); canola oil seed oil of caraway (Carum carvi); carrot oil (Daucus carota sativa); oil of cashew (Anacardium occidentale); castor oil benzoate; castor oil (Ricinus communis); zevalin; almograve oil (Taraktogenos kurzii), Chia oil (Salvia hispanica); cocoa butter (Theobrama cocao); coconut oil (Cocos nucifera); fish oil; oil coffee (Coffea arabica); oil, corn germ (Zea mays); corn oil (Zea mays); Cottonseed oil (Gossypium); borage oil (Cucumis sativus ); rosehip oil(Rosa canina); egg fat; EMU oil; epoxidized soybean oil; oil biennial four-o'clock (Oenothera biennis); fish oil; oil genuine avalanche; goat fat, grapeseed oil (Vitis vinifera); hazelnut oil (Croylus americana); hazelnut oil (Corylus aveilana); lipids human placenta; hybrid sunflower oil (Carthamus tinctorius); oil seeds, hybrid sunflower (Helianthus annuus); Arctic Fox fat; oil plants cockoos tears (Coix lacryma-jobi); jojoba; seed oil, kiwi (Actinidia chinensis); Kukui nut oil (Aleurites moluccana); lard; oil of linseed (Linum usitatissiumum); butter lupine (Lupinus albus); oil for macadamia nuts; oil seeds macadamia (Macadamia ternifolia); oil seeds macadamia (Macadamia integrifolia); maledizione soybean oil; seed oil mango (Mangifera indic); surovy fat; seed oil, meadow foam (Limnanthes fragraalba); Menhaden oil; lipids milk fat; mink oil; Moringa oil cryptomelane; mortierella oil; seed oil, musk rose (Rosa moschata); bone fat, derived from tibial bones of cattle; seed oil Azadirachta indica (Melia azadirachta); oil seeds of oats (Avena sativa); the oil membranes of the olive tree (Olea europaea), olive oil (Olea europaea); omental fat; oil holostea; fat South American ostrich oxidized corn oil; stone fruit, palm oil (Elaeis guineensis); palm oil (Elaeis guineensis); oil of passion fruit (Passiflora edulis) oil; peach stone fruit oil (Prunus persica); peanut oil (Arachis hypogaea); nut oil-pecan (Caiya illinoensis); Oil cibotium (Cibotium barometz); pistachio oil (Pistacia vera); lipids placenta; poppy seed oil (Papaver orientale); pumpkin seed oil (Cucurbita pepo); oil of quinoa (Chenopodium quinoa); rapeseed oil (Brassica campestris); rice bran oil (Oryza sativa); the oil from rice bran (Oryza sativa); sunflower oil Carthamus tinctorius; salmon oil; seed oil sandalwood (Santalum album); sea buckthorn oil (Hippophae rhamnoides); sesame oil (Sesamum indicum); shark liver oil; Shea butter (Shea butter) lipids of the silkworm; skin lipids; soybean oil (Glycine soja; soybean lipids; sphingolipids; seed oil sunflower (Helianthus annuus); sweet almond oil (Prunus amygdalus dulcis) oil; mA�lo of sweet cherry (Prunus avium); tall oil; fat; tea tree oil (Melaleuca alternifolia); oil telfairia stopvideo; oil of tomato (Solanum lycopersicum); oil Trichodesma zeylanicum; fat tuna; vegetable oil; walnut oil (Juglans regia); the lipids of wheat bran; and wheat germ oil (Triticum vulgare), and mixtures thereof.

In certain embodiments, the oil is present in the compositions of the present invention in an amount of from about 0.01% (or about 0.01%) up to 99.98% (or approximately 99,98%), or perhaps 10% (or approximately 10%) to 90% (or approximately 90%), or perhaps 20% (or approximately 20%) to 70% (or approximately 70%), or, perhaps, from 25% (or approximately 25%) to 50% (or approximately 50%), or perhaps 30% (or approximately 30%) to 40% (or approximately 40%), or perhaps approximately 33% (mass.).

In certain embodiments, the oil mixture used as a source of fatty acids, produced from selected oils to obtain the following composition of fatty acids is 0.3% (or about 0.3%) myristic acid, 19% (or approximately 19%) palmitic acid, and 0.5% (or about 0.5%) palmitoleate acid, 13% (or approximately 13%) of stearic acid, 44.4 per cent (or approximately 44.4 per cent) of oleic acid, 21.3 per cent (or approximately 21.3 per cent) of linoleic acid and 0.5% (or appr� 0,5%) linolenic acid. In certain embodiments, the oil mixture used as a source of a mixture of fatty acids obtained from the group including coconut oil, olive oil, cottonseed oil, or mixtures thereof.

In certain embodiments, the mixture of fatty acids or fatty acid sources is present in the compositions of the present invention in an amount of from about 0.01% (or about 0.01%) up to 99.98% (or approximately 99,98%), or perhaps 10% (or approximately 10%) to 90% (or approximately 90%), or perhaps 20% (or approximately 20%) to 70% (or approximately 70%), or, perhaps, from 25% (or approximately 25% to 50% (or approximately 50%), or perhaps 30% (or approximately 30%) to 40% (or approximately 40%), or perhaps approximately 33% (mass.).

In certain embodiments, the ratio of the content of the acid and a mixture of fatty acids (mass.) is from about 0.01:1 (or about 0.01:1 to 1:0.01 (or about 1:0.01), and perhaps from 1:1 (or about 1:1 to 1:0.1 (or about 1:0,1), perhaps from 1:1 (or about 1:1 to 1:0,5 (or approximately 1:0,5), or possibly 1:1 (or approximately 1:1).

In certain embodiments, the ratio of the content of a mixture of fatty acids and antioxidant by weight of sostavljae� from about 0.01:1 (or about 0.01:1 to 1:0.01 (or about 1:0.01), and perhaps from 1:1 (or about 1:1 to 1:0.1 (or about 1:0,1), perhaps from 1:1 (or about 1:1 to 1:0,5 (or approximately 1:0,5).

In certain embodiments, the ratio of pyruvic acid or mixture of fatty acids to the antioxidant by weight is from about 1:1 (or approximately 1:1) to 1:0.01 (or about 1:0,01).

Not limited to a specific theory, it is believed that the compositions and methods of the present invention contribute to the improvement or regrowth; provide growth more dense or rich hairline; and/or allow you to treat or prevent hair loss, accelerating the onset of the anagen phase in mammals, and/or reduce the appearance of hair on the skin of a mammal.

Based on the studies of hair growth, it was concluded that the histological characteristics of the hair follicle significantly vary during the cycle of its growth. Hair can be classified as: 1. terminal hair, pigmented, long and thick, or 2. vellus hair, very thin and light colored. In balding men, terminal hair is replaced by fine vellus hair.

All hair, terminal and vellus go through a growth phase (anagen) phase of regression or transitional (catagen) and phase poko� (telogen).

During the anagen phase of growing stands in nosochkah dermis easily share and form the hair shaft, and squamous emerges from the follicle via the pore. Hair follicles in the anagen phase are located in the deeper layer of subcutaneous fat in the skin. Follicles in the catagen state are located in the dermis, and the telogen in the middle or upper layers of the dermis. Anagen phase lanugo hair is usually much shorter than terminal hair.

Additional active ingredients that are acceptable from a cosmetic point of view

In one embodiment of the compositions forming the subject of the present invention may also contain one or more cosmetically active substances in addition to the above components. The term "active substance acceptable from a cosmetic point of view," understand the connection, which can be obtained synthetically or isolated by purification and concentration from natural sources, or natural extract containing a mixture of compounds that have a cosmetic effect on the tissue, including, without limitation: substance that prevents aging, sunscreens, photoprotectors, antioxidants, keratolytic substances, surfactants/detergents, moisturizers, nutrients, vitamins, minerals, energy-intensive prophetic�PTS hair colouring, pigments, means for stiffening, tools for improve skin and odour control, for example, the means for masking an unpleasant smell, means for changing the pH and buffering agents.

In certain embodiments, may be additional acceptable from cosmetically active substances, for example, for hair growth selected from the group of compounds able to accelerate the growth of hair produced as medicines, for example, diazoxide, pinacidil, bimatoprost, finasteride, an inhibitor of 5-alpha-reductase type 2 and dutasteride, an inhibitor of 5-alpha-reductase type 1 and 2, as well as flutamide, bikalutamid, pregnane derivatives, derivatives of progesterone, experimental drugs, such as FCE 28260, etc. Perhaps the use of spironolactone and other diuretics, which shows women in some cases (also known as aldactone: the antagonist of the aldosterone receptor).

In other embodiments, in the compositions of the present invention may include synthetic or natural inhibitors of 5-alpha-reductase or other components that reduce the formation of sebum, including, without limitation, epicanthal (capilarity, sarcosin and tanning extract, cinnamon tree, Cu, etc.�IU, to obtain the compositions of the present invention can be used MC5 receptor antagonists. Examples of antagonists MC5-R can be found in U.S. patent No. 7,049,331, which is incorporated herein by reference.

In addition, in certain embodiments, can be used herbal remedies possessing inhibitory effect on 5-alpha-reductase or otherwise inducing hair growth, which may include: the palm of Serenoa and Pygeum bark. Other substances that may possess such action include beta sisterol, epicanthal and liquorice, gamma-linolenic acid and other unsaturated fatty acids, zinc and zinc salts, smoke tree extract ordinary, green tea catechin (-)-epigallocatechin gallate (EGCG) and other polyphenols, etc., Extracts of grape seed, apples, Apple juice and barley also have potential properties of the agents, accelerating hair growth, although I believe that these funds will not receive wide distribution and will not achieve satisfactory results.

Carriers for the manufacture of compositions for topical use

Compositions for topical use, applicable in the present invention contain compounds that are suitable for application to the skin and scalp. The term "topical application" nowadays�hydrology and hydrogeology refers to the use of the composition in combination with pharmaceutically acceptable carrier, applied, in accordance with the method in the present invention, on the site of hair loss, slow hair growth or baldness for the purpose of local impact on these areas. Accordingly, such compositions are topical applications used in the methods of the present invention include dosage forms, in which the compound is applied to the external surfaces of the body and in direct contact with the skin requiring treatment.

In one embodiment, the compositions contain the above components in the carrier for the manufacture of means of the local application is acceptable from a cosmetic point of view. To suitable carriers include ointments, pastes, gels, jellies, serum, aerosol and non-aerosol sprays, foams, creams, lotions, solutions, suspensions, etc., the Term "ointment" refers to formulations (including creams) for oily, absorbed, water-soluble and emulsion-based, for example, petrolatum, lanolin, polyethylene glycol, or mixtures thereof. A more detailed discussion of specific media and additional compounds in the compositions of the present invention can be found in the publication of U.S. patent 2008/0145331 Bruning et al., which is incorporated in this application by reference. In one of the embodiments of the invention the media to produce a local �karstenii forms, acceptable from a cosmetic point of view, is from about 50% to about 99.99 percent (mass.), or, possibly, from about 80% to about 95% (wt.).

Other materials

The drugs that can be used in the present invention may also contain various other materials. These include moisturizers, proteins and polypeptides, preservatives, alkalinizing supplements and mixtures thereof. The drugs that are the subject of the present invention may also contain chelating agents (e.g., EDTA) and preservatives (e.g., parabens). In addition, the local use drugs that can be used in the present invention may contain traditional cosmetic additives such as dyes, sunscreens (e.g., titanium dioxide), pigments and flavors. A more detailed discussion of these and other materials can be found in an earlier patent publication U.S. 2008/0145331 Bruning et al., and also in U.S. patent No. 5658956 Martin et al., which are incorporated herein by reference.

In addition, there can be used mixtures of the above preservatives.

Methods of application

The possibility of applying the compositions of the present invention to accelerate the onset of the anagen phase in the hair growth of a mammal and/or acceleration of appearance�the access terminal hair above the surface of the skin by topical application of these compositions was investigated in experiments on mice as described below.

In certain embodiments, the compositions of the present invention should be applied topically to the desired area of the body of a mammal or human, at least once a day for at least 11 weeks, probably at least 9 weeks, or possibly at least 7 weeks. Hair growth under the action of the compositions of the present invention can be maintained indefinitely through regular application of the compositions of the present invention.

Examples

The compositions of the present invention described in following examples illustrate specific examples of application in practice of the compositions of the present invention, but are not limited to these examples. Other modifications can be made by a person skilled in the art without departing from the scope of the present invention and a retreat from its essence.

The definition of accelerated onset of anagen phase

To establish the possibility of accelerating the onset of the anagen phase in mice C3H, prepared following local formulations using conventional mixing technology.

Composition for treatment of 1Composition for treatment 2Composition for treatment 3a Composition for the treatment of 4 Composition for treatment 5Composition for treatment of 6
IngredientThe percentage (mass%)
Water Farm. USA52,4058,4658,4058,4057,4062,94
Lactic acid NF3,153,153,153,153,153,15
Methylparaben NF0,200,200,200,200,200,20
Minoxidil Pharm. USA5,005,005,005,00---5,00
Sodium pyruvate7,007,001,007,007,00 3,50
Polyoxyethylene (2) stearyl ether6,006,006,006,006,006,00
Polyoxyethylene (20) stearyl ether6,006,006,006,006,006,00
Cetearyl alcohol (and) cetearate-206,006,006,006,006,006,00
Propylparaben NF0,200,200,200,200,200,20
Vitamin A acetate NF7,007,007,001,007,003,50
Cocoa butter NFOf 2.350,33 Of 2.35Of 2.35Of 2.351,17
Olive oil NFOf 2.350,33Of 2.35Of 2.35Of 2.351,17
Cottonseed oil NFOf 2.350,33Of 2.35Of 2.35Of 2.351,17
Citric acid or sodium hydroxide---how much is requiredhow much is requiredhow much is requiredhow much is requiredhow much is required
pH4,54,44,44,54,44,4

The percentage (mass%)
Composition for treatment of 7
(solution Actavis Minoxidil for topical application of 5%)1
IngredientspH
Water Farm. USANo dataThe apparent pH=8,1
Propylene glycolNo data
AlcoholNo data
Minoxidil Pharm. USA5,00
1Comes Actavis MidAtlantic LLC, Baltimore, Maryland

Female C3H mice aged 6-7 weeks, were purchased in the company Taconic Farms (Germantown, NY). The cycle of hair growth in mice C3H consists of similar phases anagen, catagen and telogen. (Table I) (I. Miyamoto; K. Hamada, he is considered to be Journal of Science, Volume 10, Number 1, July 1995, pp. 99-99(1)).

Table I
Weeks after birthWeeks. 0Weeks. 2Weeks. 3Weeks. 4Weeks. 6Weeks. 7Weeks. 15
Stage of hair growthMorphogenesisCatagenTelogen AnagenCatagenTelogenAnagen

Each phase is significantly shorter than the corresponding phase in the cycle of hair growth in humans, and occurs synchronously in all hair follicles. Therefore, C3H mice are convenient to use as a model for studying induction of growth or recurrence of hair growth under the action of active substances. Telogen phase in mice C3H long and lasts from 7 to 15 a week. Therefore, usually study on the resumption of hair growth begins in week 7 and end on 15 week, i.e. last about 8 weeks.

Mice kept in cages of suitable size in a room with controlled environmental conditions with a 12-hour light cycle, and given food and water indefinitely. Care of animals was based on the recommendations of the “Guidelines for care of laboratory animals and their use”, No. NIH publication 85-23. After the occurrence of a long phase of telogen/resting from all the animals on the back was shaved an area of about 1.5×5 cm (using clippers Wahl Clippers 8900, blade No. 1086). Five female mice in each group, the skin area was shaved under sedation 2% for induction of anesthesia and for maintenance of anesthesia used isoflurane and 0.5 l of oxygen. The actual number of mice indicated in the data that may improves�to face because of accidental death in the course of the study.

The experimental group and compositions for the treatment were selected as follows:

GroupA composition for the treatment
AStudy part 1
(additive [7:7:7] with 5% Minoxidil)
BThe study part 2
(additive [7:7:1] with 5% Minoxidil)
CStudied composition 3
(additive [1:7:7] with 5% Minoxidil)
DStudied composition 4
(additive [7:1:7] with 5% Minoxidil)
EThe study consists of 5
(additive [7:7:7] without Minoxidil)
FThe investigated compound 6
(additive [3,5:3,5:3,5] with 5% Minoxidil)
GStudied composition 7
(5% Minoxidil without additives)
HWithout treatment
(in brackets “[ ]” shows the % of the ratio (mass.) alpha-keto acid, an antioxidant and a mixture of fatty acids in the composition to be processed)

200 mg of each tested composition was applied �and the investigated area of the skin daily 5 days a week. On day 5 of each week of treatment and every 7 days subsequently took the pictures for visual observation of the first signs of anagen/active phase of hair growth and determining the rate of development of terminal hair coat to the skin area. During the study conducted (the journal of the anagen phase), in which we celebrate daily monitoring of mice, in which began the anagen phase (i.e., the observation of changes in color of skin to gray, the first visual sign of hair growth). Treatment continued for 9 weeks. Unexpectedly, it was observed that the anagen phase in the group of mice SN, which was treated with 5% Minoxidil and the additive of the present invention, it was faster than in mice, which were treated only with 5% Minoxidil.

Table II shows the time of onset of the anagen phase in groups a-N a log of observations of the anagen phase.

Table II
GroupA composition for the treatmentThe onset of the anagen phase (day treatment)
AStudied composition 1 (additive [7:7:7] Minoxidil)15
BExplore�th part 2 (additive [7:7:1] Minoxidil) 15
CStudied composition 3 (additive [1:7:7] Minoxidil)15
DStudied composition 4 (additive [7:1:7] Minoxidil)11
EThe study consists of 5 (additive [7:7:7] without Minoxidil)19
FThe investigated compound 6 (Supplement [3,5:3,5:3,5] with 5% Minoxidil)14
GStudied composition 7 (5% Minoxidil without additives)24
HWithout treatment42
(in brackets “[ ]” shows the % of the ratio (mass.) alpha-keto acid, an antioxidant and a mixture of fatty acids in the composition to be processed)

The data in table II show the next time of onset of the anagen phase in each of the groups treated with the mixture:

I. In groups a, b and C for 9 days earlier than in group G, and 27 days earlier than in group H;

II. In group D on 13 days earlier than in group G, and 31 days earlier than in group H

III. In group E �and 5 days earlier than in group G, and 23 days earlier than in group H.

IV. In group F to 10 days earlier than in group G, and 18 days earlier than in group H.

The average degree of development of terminal hair coat in mice in each group was determined visually by the images taken at 0, 4 and 5 week. The phrase "degree of development of terminal hair coat" means the average percentage of the treated area covered with terminal hairs. The phrase "a greater degree of development of terminal hair coat" means that the average coat in one group of mice a. on average, thicker or darker; and/or b. covers a large average size of the treated area than in the other group. The phrase "lower degree of development of terminal hair coat" means that the average coat in one group of mice a. on average, less or lighter; and/or b. covers the lower average size of the treated area than in the other group. The phrase "more rapid development of terminal hair coat" means that the terminal cover develops earlier. The term "average" means the average value of mice in each group. The term "observation" or "visual supervision" means a visual assessment of the images with the naked eye.

Then the groups arranged from most to least degree of development of hair. Ratio�their acid, an antioxidant and a mixture of fatty acids in the description of the specified component mixture is shown in brackets [] after the term "additive".

Visual assessment of images taken at 0 week (on the day of the shaving wool) showed the removal of all terminal hair in mice in groups a-N.

Differences in the degree of development of terminal hair coat between groups A-H were first evident in the images obtained at the end of 4 weeks. Based on the evaluation of images obtained at week 4, the group arranged according to the degree of development of terminal hair coat, as shown in table III.

Table III
GroupAssessment at week 4: the Degree of development of terminal hair coat (the lowest number having the greatest degree of development of coat)
D1
A, B, C, F2
E, H, G3

Classification groups in table III shows that in group D, which used the composition 4 (5% Minoxidil with the admixture [7:1:7]), the degree of development of terminal hair coat was higher and the increase was the least�trim. Animals in groups A, B, C and F, which were treated with Compound 1 (5% Minoxidil with the admixture [7:7:7]); Compound 2 (5% Minoxidil with the admixture [7:7:1]); Compound 3 (5% Minoxidil with the admixture [1:7:7]); And compound 6 (5% Minoxidil with the admixture [3,5:3,5:3,5]), respectively, were second in growth rate and development of terminal hair coat among all groups. Group E was treated with compound 5 (compound [7:7:7] without Minoxidil)); In the untreated group G and group H, chemically treated, 7 (5% Minoxidil without mixture) development of terminal hair coat at this stage of research was the smallest.

Table IV presents the distribution of groups according to the degree of development of terminal hair coat according to the evaluation of images obtained at week 5.

Table IV
GroupAssessment week 5: the Degree of development of terminal hair coat (the lowest number having the greatest degree of development of coat)
A, B, C, D, F1
E2
G, H3

Distribution of groups in table IV shows that in groups A, B,C, D and F, treated with composition 1 (5% Minoxidil with the admixture [7:7:7]); Compound 2 (5% Minoxidil with the admixture [7:7:1]); Compound 3 (5% Minoxidil with the admixture [1:7:7]); Composition 4 (5% Minoxidil with the admixture [7:1:7]); and compound 6 (5% Minoxidil with the admixture [3,5:3,5:3,5]), respectively, observed the fastest growth of wool and the greatest degree of development of terminal hair coat at this stage of research. Group E, treated with composition 5 (additive [7:7:7] without Minoxidil) was second in growth rate and development of terminal hair coat. Untreated group G and group H, chemically treated, 7 (5% Minoxidil) remained in last place, that is, the degree of development of terminal hair coat in animals in this group was the smallest.

A summary of data classification groups are presented in tables III and IV shows that:

a. in mice, the skin treated with compositions containing Minoxidil and an additive of the present invention, the development of terminal hair coat was faster than:

i. in mice, the skin treated with compositions containing the same amount of Minoxidil without the additive;

ii. in mice, the skin which was treated by the compositions with the same amount of additive without Minoxidil, and

iii. untreated mice;

b. in mice, the skin which was treated with composition�s, containing additives of the present invention without Minoxidil, development of terminal hair coat was faster than untreated mice.

c. in mice whose skin had been treated with compositions containing additive with a ratio of alpha-keto-acids and mixtures of fatty acids of 1:1, but proportionally smaller content of antioxidant, the rate of development of terminal hair was higher than in mice, which were treated composition with a relatively low content of alpha-keto-acids or mixtures of fatty acids (i.e., the ratio of antioxidant to the keto acid or an antioxidant for fatty acids 1:1).

The present invention is further illustrated by the following examples, which should not be construed as limiting it. The components in each example are prepared by mixing the listed ingredients and traditional techniques.

Ointment to accelerate/resume hair growth
The name according to INCITrade nameExample 1 (lotion)
(% wt.)
Example 2 (lotion)
(% wt.)
Example 3 (cream) (% wt.)Example 4
(serum) (% (mass.)
Example 5 (lotion)
(% wt.)
Manufacturer
MinoxidilMinoxidil5,05,05,05,020,0Pfizer
WaterWater Farm. USA24,65Of 6.6542,1564,518,15
FinasterideFinasteride-5,0---WuHan GuangGu Pharm Ltd.
BimatoprostBimatoprost---0,05-LGM Pharmaceu-ticals Inc.
DiazoxideDiazoxide--2,0- -Parchem Trading, Ltd.
EthanolEthanol20,020,0--15,0Parchem Trading, Ltd.
Propylene glycolPropylene glycol10,030,015,0-10,0Parchem Trading, Ltd.
Lactic acidPurac PF 901,0-3,03,153,5PURAC, Inc.
Sodium pyruvateSodium pyruvate NF7,01,07,01,07,0Torary Industries, Inc.
Coconut oilCoconut oilOf 2.35Of 2.35Of 2.35Of 2.35Newtown Foods USA
Olive oilOlive oilOf 2.35Of 2.35Of 2.350,33Of 1.35Ventura Food, LLC
Cottonseed oilCottonseed oilOf 2.35Of 2.35Of 1.350,33Of 2.35Ventura Food, LLC
Vitamin E acetateVitamin E acetate7,007,001,007,007,00BASF
MethylparabenMethylparaben NF0,20,20,20,20,2ISP
PropylparabenPropylparaben NF0,10,1 0,10,10,1Tri-K Industries
Polyoxyethylene (2) stearyl etherBrij 7266666ICI
Polyoxyethylene (20) stearyl etherBrij 7866666ICI
Cetyl alcoholCetyl alcohol6666---Henkel Co.
Xanthan gumXanthan gum--0,5-1,0CPKelco
pH3-73-73-7 3-73-7

/table>

1. Composition to accelerate/resume hair growth, containing;
a. at least one compound selected from Minoxidil or Minoxidil sulfate; and
b. from about 0.1% to about 99% (wt.) supplements:
i) from about 0.01% to about 99,98% (mass.) acid selected from the group including intermediates of the Krebs cycle, their salts and mixtures, and pyruvic acid or its salt, in particular, such as sodium pyruvate;
ii) from about 0.01% to about 99,98% (mass.) antioxidant; and
iii) from about 0.01% to about 99,98% (mass.) a mixture of fatty acids comprising at least 7 unsaturated or saturated fatty acids selected from the group comprising butyric acid, caproiu acid, Caprylic acid, capric acid, lauryl acid, myristic acid, myristoleate acid, palmitic acid, palmitoleate acid, stearic acid, oleic acid, linoleic acid, linolenic acid, arachidonoyl acid, gadolinium acid, pentadecanoic acid, margaric acid, margarino acid, behenic acid, digabriele acid, arachidonic acid and lignoceric acid, or a mixture of sources of fatty acids comprising a mixture of olive oil, coconut oil and cotton�wow oil.

2. A composition according to claim 1, further comprising finasteride.

3. A composition according to claim 1 in which the antioxidant is selected from the group consisting of: vitamin A; vitamin C; tocopherol; precursors of vitamin A, vitamin C and vitamin E; salts of vitamin A, vitamin C and vitamin E; flavonoids; polyphenols and their mixtures.

4. A composition according to claim 3, in which the antioxidant is a vitamin E is selected from the group consisting of: alpha-tocopherol, beta-tocopherol, gamma-tocopherol, Delta-tocopherol, takkinen, tocotrienols and their esters and mixtures.

5. A composition according to claim 4, in which the vitamin E is selected from the group consisting of: esters of tocopherol, esters of beta-tocopherol, an ester of gamma-tocopherol, an ester of Delta-tocopherol, esters of takkinen, esters tocotrienol and mixtures thereof.

6. A composition according to claim 5, in which the vitamin E is selected from the group consisting of: acetic acid ester of tocopherol, the acetate ester of beta-tocopherol, acetic-acid ester of gamma-tocopherol, acetate ester of Delta-tocopherol, acetate ester of takkinen, acetate ester tocotrienol and mixtures thereof.

7. A composition according to claim 1, further comprising lactic acid, sodium lactate, or mixtures thereof.

8. A composition according to claim 1 in the form of a suitable carrier for local drug forms.

9. The compositing�tion according to claim 8, in which a carrier for topical application is prepared in the form of an ointment, paste, gel, jelly, serum, aerosol, non-aerosol means for spray, foam, cream, lotion, or suspension.

10. Composition for acceleration or recurrence of hair growth that contains:
a. at least one compound selected from Minoxidil or Minoxidil sulfate; and
b. from about 5% to about 50% Supplement that contains:
i) from about 0.01% to about 99,98% (mass.) pyruvic acid or its salts, in particular, such as sodium pyruvate;
ii) from about 0.01% to about 99,98% (mass.) antioxidant; and
iii) from about 0.01% to about 99,98% (mass.) a mixture of fatty acids or mixtures of fatty acid sources defined in claim 1;
in which the ratio of pyruvic acid and a mixture of fatty acids is from 0.01:1 (or about 0.01:1 to 1:0.01 to about 1:0,01); the ratio of the pyruvic acid and the antioxidant is from 0.01:1 (or about 0.01:1 to 1:0.01 (or about 1:1,01); the ratio of the mixture of fatty acids and the antioxidant is from 0.01:1 (or about 0.01:1 to 1:0.01 (or about 1:0,01).

11. A composition according to claim 10, in which the ratio of pyruvic acid or mixture of fatty acids and the antioxidant is from 1:1 to 1:0.5 in.

12. Composition for speed�tion/resume hair growth, contains:
a. at least one compound selected from Minoxidil or Minoxidil sulfate; and
b. from about 0.1% to about 99% supplements:
i) from about 0.01% to about 99,98% (mass.) pyruvic acid, its salts, in particular, such as pyruvate sodium, or mixtures thereof;
ii) from about 0.01% to about 99,98% (mass.) tocopherol or its ester; and
iii) from about 0.01% to about 99,98% (mass.) mixture of fatty acid sources, predstavljajushej an oil mixture that contains:
1) from about 0.01% to about 99,98% (mass.) olive oil;
2) from about 0.01% to about 99,98% (mass.) coconut oil; and
3) from about 0.01% to about 99,98% (mass.) cottonseed oil.

13. Composition for enhancing or resumption of growth of hair that contain:
a. at least one compound selected from Minoxidil or Minoxidil sulfate; and
b. from about 0.1% to about 99% (wt.) supplements:
i) optionally from about 0.01% to about 99,98% (mass.) pyruvic acid;
ii) optionally, from about 0.01% to about 99,98% (mass.) antioxidant; and
iii) from about 0.01% to about 99,98% (mass.) a mixture of fatty acids comprising at least 7 unsaturated or cargoes or long goods.�enny fatty acids, selected from the group comprising butyric acid, caproiu acid, Caprylic acid, capric acid, lauryl acid, myristic acid, myristoleate acid, palmitic acid, palmitoleate acid, stearic acid, oleic acid, linoleic acid, linolenic acid, arachidonoyl acid, gadolinium acid, pentadecanoic acid, margaric acid, margarino acid, behenic acid, digabriele acid, arachidonic acid and lignoceric acid, or a mixture of sources of fatty acids comprising a mixture of olive oil, coconut oil and cottonseed oil.

14. A composition according to claim 13 in which each of the fatty acids present in the mixture of fatty acids in the following amounts: approximately 0.2-0.4% of butyric acid, approximately 0.1% of Chapaevo acid, approximately 0.3 to 0.8% Caprylic acid, about 2.2 to 3.5% capric acid, about 0.9 5.5% of laurinova acid, approximately 2,8-8,5% myristic acid, about 0.1 to 0.6% myristoleate acid, approximately 23,2-24,6% palmitic acid, about 1.8 to 3.0% by palmitoleic acid, approximately 6,9-9,9% stearic acid, approximately 36,0-36.5% of oleic acid, approximately 20-20,6% linoleic acid, about 7.5-7.8% of linolenic acid, approximately�about 1.1 to 4.9 per cent arachinovo acid and approximately 3,3-6,4% gadolinia acid.

15. A composition according to claim 14 in which each of the fatty acids present in the mixture of fatty acids in the following mass proportions: approximately 0.3% myristic acid, about 19% palmitic acid, about 0.5% palmitoleate acid, about 13% of stearic acid, approximately 44.4% of oleic acid, approximately 21.3% of linoleic acid and about 0.5% linolenic acid.

16. Composition for enhancing or resumption of growth of hair that contain:
a. at least one compound selected from Minoxidil or Minoxidil sulfate; and
b. from 5% to 10% pyruvic acid based on the weight of the composition;
c. from 5% to 10% of an antioxidant based on the weight of the composition; and
d. from 5% to 10% (mass.) in the calculation of the weight of the mixture of fatty acid sources, representing an oil mixture that contains:
i) from 0.01% up to 99.98% (mass.) olive oil;
ii) from 0.01% up to 99.98% (mass.) coke oil; and
iii) from 0.01% up to 99.98% (mass.) cottonseed oil.

17. Method for accelerating the onset of the anagen phase in the cycle of hair growth in a mammal, comprising applying an effective amount of a composition according to claim 1, which stimulate hair growth.

18. Method of accelerating the occurrence of terminal hair on the skin of a mammal, comprising applying an effective amount of a composition according to claim 1, providing steam�the stimulation of hair growth.

19. A method according to claim 17, wherein the mammal is a human, and the site of application is a scalp.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine, namely to dermatology, and can be used for preventing and/or treating skin itching. It involves using L-serine as a therapeutic agent, a pharmaceutical composition containing L-serine, as well as a dermato-cosmetic composition containing L-serine as a single active agent, Avene Thermal Spring Water, glycerine and a cosmetically acceptable carrier. The L-serine concentration in the composition makes from 0.01 wt % to 10 wt % in relation to the total weight of the composition. More preferentially, the concentration makes 0.5 wt % to 3 wt % in relation to the total weight of the composition.

EFFECT: group of inventions provides the effectiveness of application.

8 cl, 2 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to medicine, namely to dermatology and mycology, and can be applied in the treatment of skin and its appendages. A pharmaceutical composition for external application contains nanoparticles for the laser thermotherapy of infectious affections of the skin and its appendages. The nanoparticles are characterised by, at least, one localised surface Plasmon resonance in the range of a wavelength from 400 to 1100 nm. The nanoparticles are dispersed in a physiologically acceptable carrier, which is characterised by the absence of the absorption or weak absorption and/or weak dispersion of light radiation in the said range of wavelengths and possessing biocidal properties. The pharmaceutical composition is applied on an affected area and irradiated by laser radiation with a wavelength close to the wavelength of the localised surface Plasmon resonance of the nanoparticles, contained in the composition, or equal to it. The irradiation is continued until the desirable temperature of heating of the said area is achieved.

EFFECT: group of inventions ensures an increased treatment efficiency, reduction of a risk of development of side effects, reduction of the number of recurrences due to the application of the pharmaceutical composition, capable of absorbing energy of the light radiation and transforming it into heat energy with the achievement of the specified temperature with laser irradiation at the specified wavelength with the lower intensity of laser radiation and possessing biocidal properties.

63 cl, 3 dwg, 1 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry and represents a pharmaceutical composition for the external application for the treatment of skin diseases in the form of a cream, which includes as an active substance methylprednisolone aceponate in a therapeutically effective amount and a lipophilic base, characterised by the fact that as the lipophilic base it contains petrolatum, liquid paraffin and oil of castor oil plant seeds and additionally white bee wax, with the components of the composition being in a specified ratio in g/100 g of the composition.

EFFECT: invention provides the creation of the stable composition, improved pharmacological properties and absence of an irritating effect.

1 tbl

Antiallergic agent // 2553354

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents an anti-allergic agent containing polysaccharide containing galactose, glucose and rhamnose as ingredients, wherein polysaccharide contains galactose, glucose and rhamnose in molar ratio 3-5:1-3:1, and polysaccharide has certain structure.

EFFECT: invention provides extending the range of antiallergic agents.

12 cl, 6 ex, 6 dwg, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: pharmaceutical composition in the form of a tablet with an erodible matrix, which contains one or more fumaric acid ethers, as well as a rate-controlling agent, representing hydroxypropylcellulose and a binding agent, representing lactose, with the decomposition of the said degradable matrix providing the controlled release of the said fumaric acid ether (ethers).

EFFECT: provision of the controlled release of fumaric acid ether (ethers).

19 cl, 43 ex, 2 tbl, 2 dwg

FIELD: chemistry.

SUBSTANCE: invention relates to the beauty industry, representing a gel-like composition for topical application, containing salicylic acid with the concentration of ca. 17 wt %, elastic collodion in the amount of 5 to 10 wt % and ethyl lactate in the amount of 20 to 25 wt %, where the elastic collodion contains 65.8 wt % diethyl ether, 24.3 wt % ethanol, 2 wt % camphor, 3 wt % castor oil and 4.9 wt % nitro-cellulose.

EFFECT: invention provides excellent stability, even drying and the formation of a uniform film.

5 cl, 1 tbl, 4 dwg

FIELD: medicine.

SUBSTANCE: melanin having water-solubility of at least 80% and an paramagnetic centre concentration of at least 8·1017 spin/g is administered orally into the animals having been exposed to the radiation in a dose high enough to cause a spinal radiation injury; melanin is administered after dissolved in distilled water in the effective concentration. Melanin water is used as drinking water for the mice having been exposed to single and fractionated acute radiation, which is able to cause acute radiation disease. Melanin water is taken from the 1st to 30th day following the single radiation, or from the 1st day of the fractionated radiation to the 30th day on completion of the radiation.

EFFECT: higher survival rate, faster recovered haemopoiesis, body weight and orientation and motion activity.

7 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine, more specifically to clinical dentistry. The invention represents a composition for treating erosive ulcerative and exudative hyperaemic forms of oral lichen planus.

EFFECT: implementing the invention provides high oral adhesion of the preparation, increases the therapeutic concentration of the preparation in the area of involvement (inflammation), accelerates the length of treatment (reduces the size of erosion, the length of epithelisation of erosions).

2 dwg

FIELD: medicine.

SUBSTANCE: pharmaceutical composition possessing a therapeutic action on various skin pathologies contains triptantrin, chitosan and distilled water, a lanoline and Vaseline mixture and protein-nucleic hydrolyzate of the salmonid fishes milt in a certain mixture ratio.

EFFECT: composition enables increasing the clinical effectiveness in the skin pathologies of various origins and extending the range of pharmaceutical compositions having the therapeutic effect on the various skin pathologies.

3 tbl, 4 dwg, 7 ex

Elastase inhibitor // 2548794

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical and cosmetic industries, namely to an elastase inhibitor. The elastase inhibitor containing active ingredients presented by raspberry (Rubus idaeus L.) extract and hydroxyproline in the dry state in a certain amount, wherein the raspberry extract is prepared by using an extraction solvent specified in a group consisting as follows: water, methanol, ethanol, hydroethanol, 1,3-butylene glycol, acetone and/or ethyl acetate. The composition for external skin application containing the elastase inhibitor.

EFFECT: agent is the effective elastase inhibitor.

6 cl, 2 dwg, 6 ex

FIELD: medicine.

SUBSTANCE: invention represents an agent for treating septic wounds, pus pockets and trophic ulcers containing betaine hydrochloride, methyluracil, trimecaine, pepsin powder and polyethylene oxide 400 with the ingredients taken in certain proportions, wt %, and polyethylene oxide 400 is taken in an amount of 87.0-84.0 ml.

EFFECT: invention provides fastening necrolysis, intensifies bactericidal action, stimulates regeneration, prevents secondary infection.

4 ex

FIELD: medicine.

SUBSTANCE: invention represents an anti-inflammatory antibacterial wound-healing agent containing a polyethylene oxide base with molecular weight 400 (PEO-400) as a forming agent, as well as polyethylene oxide with molecular weight 1,500 (PEO-1500); an active substance is chloramphenicol and methyluracil; the agent is characterised by the fact that it additionally contains rifampicin and/or cycloserine; the cycloserine content in the rifampicin mixture is specified within the range of 18 to 82 wt %, whereas the ingredients are taken in certain ratio, wt %.

EFFECT: invention provides more effective healing of open wounds, ulcers, bedsores, as well as increased necrolytic effect, reduced exudation, and also a lower risk of allergic reactions.

3 cl, 9 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to oncology, and can be applied for the treatment of adenogenous locally advanced cancer of the rectum. For this purpose chemotherapy with 5-fluorouracil, medical therapy, gamma-therapy are realised by a method of dynamic fractioning of a dose. 5-fluorouracil is introduced into the pararectal cellular tissue, adjacent to a tumour, in a volume of 5-15 ml 5-15 min before an irradiation session of before the first three large fractions. As the drug therapy realised is infusion introduction of Mabthera in a dose of 50-70 70 mg/m2 50-60 minutes before radiotherapy on the 1, 7 and 14 days of treatment. From the 1 to 12 days from the treatment beginning radiotherapy is performed on the tumour zone and the zone of regional metastases from 2-4 fields in a mode of dynamic fractioning with SFD=3.6 Gy 3 times and further with SFD=2.2-2.4 Gy 9 times to TFD=32.4-34.8 Gy.

EFFECT: method ensures the reduction of the volume and size of the initial tumour, transfer of non-operable and conditionally operable stages of the disease into the operable state and a possibility of carrying out radical operations with an increase of therapy tolerance as a result of reduction of toxic and cytotoxic effects of the treatment, increase of protective powers of the organism and a possibility of carrying of radiotherapy in the total volume.

2 ex

FIELD: medicine.

SUBSTANCE: invention provides a solid hypolipidemic dosage form containing rosuvastatin or its pharmaceutically acceptable salt in an amount of 3 to 15%, processing additives and a pharmaceutically acceptable excipient containing microcrystalline cellulose, lactose monohydrate, polyvinylpyrrolidone and croscarmellose sodium. The above excipient represents granulate in an amount of 79 to 95 wt % of the dosage form containing absorbed moisture within the range of 0.5% to 1.5%. What is also described is a method for preparing the dosage form.

EFFECT: uniform distribution of the active substance and storage stability of the dosage form of rosuvastatin.

11 cl, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine, more specifically to an implanted device comprising a biologically compatible, biologically degradable polymer mixed with TMC278 (rilpivirine) and with one or more release-enhancing agents specified in a group consisting of poloxamers, polysorbates and a combination of dimethylsulphoxide (DMSO) and poly(vinylpyrrolidone) (PVP).

EFFECT: device provides the extended release of the active ingredient for long periods of time.

17 cl, 3 dwg, 5 tbl, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine and concerns a stable composition of nanostructured Sildenafil inhibiting cyclic guanosine monophosphate (cGMP) specific phosphodiesterase type 5 (PDEV) containing a nanostructured Sildenafil base or its pharmaceutically acceptable salts having an average particle size of less than approximately 500nm, a stabilising agent, wherein the composition is prepared in a microfluidics-based continuous-flow tank reactor, and the composition possesses a semi-amorphous structure. The group of inventions also concerns a method for preparing the composition of nanostructured Sildenafil; using the above composition for preparing the pharmaceutical composition for treating male or female sexual dysfunction and pulmonary arterial hypertension.

EFFECT: group of inventions provides the improved solubility of the composition.

8 cl, 11 ex, 14 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to experimental pharmacology and represents a method for correction of bone tissue microcirculation in experimental osteoporosis and associated fractures, involving administering a combination of pharmacological agents into a laboratory animals after simulating osteoporosis by a bilateral ovariectomy and osteoporotic femoral fractures in Wistar rats, differing by the fact that the above agents are presented by a combination of recombinant erythropoietin in a single sub-erythrostimulating dose of 50 international units/kg administered into the laboratory animal subcutaneously once a day every week, and rosuvastatin in a dose of 0.86 mg/kg, which is administered intragastrically daily into the laboratory animal once a day with underlying simulating osteoporosis for eight weeks, and in associated fractures - for twelve weeks.

EFFECT: invention provides the synergism on the positive effect on the bone tissue microcirculation.

1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of structural formula (I), which can be used for treating diseases mediated by an androgen receptor. In formula (I), R1 means (C2-6)alkyl, (C1-6)alkyloxy, -S(O)m-(C1-6)alkyl, (C1-6)fluoroalkyl, CN or halogen, R2 and R3 are identical or different and mean a hydrogen atom or (C1-9)alkyl, R4, R5, R6, R7 are identical or different and mean a hydrogen or halogen, X means CH or N, Y means either a nitrogen atom, or a carbon atom substituted by (C1-6)alkyl, (C1-6)alkyloxy, (C1-6)fluoroalkyl, a hydrogen atom or halogen; m is equal to 0, 1 or 2.

EFFECT: invention refers to using the compounds for preparing a therapeutic agent for preventing and/or treating hirsutism, androgenetic alopecia, hypertrichosis, atopic dermatitis, disordered sebaceous gland, such as hyperseborrhea, acne, greasy skin or seborrheic dermatitis.

8 cl, 2 tbl, 26 ex

FIELD: veterinary medicine.

SUBSTANCE: preparation for treatment of infected wounds in the toe region of animals, containing dimethyl sulphoxide, methyl cellulose, additionally comprises tylosin tartrate, sulphadimine, trimethoprim in the following ratio of components, wt %: tylosin tartrate - 2-3, sulphadimine - 4-5, trimethoprim - 1-1.5, dimethyl sulphoxide - 10-15, methylcellulose - 3.0-3.5, water - the rest. The claimed method comprises applying the claimed preparation without preliminary wound cleaning. The preparation is applied to the wound with the layer thickness of 2-3 mm, without application of soft dressing. The treated animals are kept for 2-3 hours on the dry surface.

EFFECT: use of claimed group of inventions increases the efficiency of treatment.

4 cl, 7 tbl, 2 ex

FIELD: medicine.

SUBSTANCE: invention represents an agent for preventing and treating prostatitis and prostate adenoma in the form of a capsule, which contains doxazosin, diisopropylammonium dichroloacetate, afobazol, copper glycinate, vitamin E (d-alpha tocopherol acetate), zinc glycinate; L-Glutamine; L-Alanine; L-Arginine and excipients: corn starch and talc.

EFFECT: extended range of products for treating and preventing prostatitis and prostate adenoma.

4 ex, 3 tbl

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to an intermediate compound, i. e. tert.-butyl-(E)-(6-{2-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-pyrimidine-5-yl}-(4R,6S)-2,2-dimethyl[1,3]dioxane-4-yl]acetate that can be used in synthesis of compound of the formula (IV)

eliciting inhibitory effect on activity of HMG-CoA-reductase and, therefore, can be used for preparing pharmaceutical agents for treatment, for example, hypercholesterolemia, hyperproteinemia and atherosclerosis. Also, invention relates to a method for preparing indicated intermediate compound by reaction of the new parent compound - diphenyl-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidine-5-ylmethyl]phosphine oxide with tert.-butyl-2-[(4R,6S)-6-formyl-2,2-dimethyl-1,3-dioxane-4-yl]acetate in the presence of a strong base in simple ether or aromatic solvents or their mixtures at temperature in the range from -200C to -900C. Also, invention relates to a method for preparing of compound of the formula (IV) wherein R1 means hydrogen atom or pharmaceutically acceptable cation and to a method for preparing intermediate compounds of the formula (VI):

wherein each P1 and P2 represents independently (C1-C4)-alkyl or group:

and wherein P3 represents (C1-C8)-alkyl. Applying new intermediate compounds and proposed methods provide enhancing quality and yield of compounds.

EFFECT: improved preparing methods.

9 cl, 1 tbl, 8 ex

Up!
Ointment to accelerate/resume hair growth
The name according to INCITrade nameExample 6 (ointment) (% wt.)Example 7 (ointment) (% wt.)Manufacturer
MinoxidilMinoxidil Pharm. USA5,0Pfizer
FinasterideFinasteride5,0WuHan GuangGu Pharm Ltd.
VaselineWhite vaseline Pharm. USA52,2555,0Dow Chemicals
Lactic acidPurac PF 901,507,0PURAC, Inc.
Sodium pyruvateSodium pyruvate NF7,0 Of 2.35Torary Industries, Inc.
Coconut oilCoconut oilOf 2.35Of 2.35Newtown Foods USA
Olive oilOlive oilOf 2.35Of 2.35Ventura Food, LLC
Cottonseed oilCottonseed oilOf 2.351,00Ventura Food, LLC
Vitamin E acetateVitamin E acetate7,00,2BASF
PropylparabenPropylparaben NF0,21,50Tri-K Industries
Propylene glycolPropylene glycol20,023,25Parchem Trading, Ltd.
pH3-73-7