Foam formulation of immune response modifier, method for preparing based drug preparation (version) and therapeutic kit containing said formulation

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, particularly to a foam formulation of an immune response modifier. The foam formulation of the immune response modifier, which contains: imiquimod; isostearic acid; a propellant; a mixture of preserving agents; sorbitan monostearate; a viscosifying agent taken in a specific ratio. A kit containing a drug preparation and an aerosol bottle. The use of the foam formulation for treating senile keratosis, basal cell skin cancer, anogenital warts, photodamaged skin, or for improving skin characteristics, cervical dysplasia, viral diseases, particularly herpes, skin metastases, skin damages caused by bites, self-healing epithelioma, for inducing interferon biosynthesis (versions).

EFFECT: above-described foam formulation of the immune response modifier is stable.

24 cl, 8 tbl, 1 ex

 

The technical field to which the invention relates.

The present invention relates to a foam composition that includes an effective amount of modifier in the immune response, which can be represented by imiquimod, sotiriadou, resiquimod or their mixture, as well as fatty acid and auxiliary agents. The present invention also relates to a pharmaceutical kit containing the specified foam composition, and to the use of this foam composition for the treatment of skin diseases and disorders.

The level of technology

In recent years, considerable efforts have been made for the discovery of new drugs that act through stimulation of some of the key processes of the immune system, as well as by suppressing some other processes (see, for example, U.S. Patent Nos 6,039,969 and 6,200,592). These compounds, sometimes referred to as modifiers of the immune response (IRM), seems to act through the basic mechanisms of the immune system, known as toll-like receptors inducyruya biosynthesis of certain cytokines, and can be used to treat a wide range of diseases and conditions. For example, some modulators of the immune response can be used for the treatment of viral diseases (for example, human papilloma virus, hepatitis virus, herpes virus), neoplasms (e.g., basal cell carcinoma flat cell carcinoma, senile keratosis) and T2-mediated diseases (e.g. asthma, allergic rhinitis, atopic dermatitis), and can be used as an auxiliary medicinal components in vaccines. Unlike many conventional antiviral and antitumor compounds, the primary mechanism of action of modulators of the immune response is not direct, but is to stimulate the immune system to recognize and take appropriate action against the pathogen.

Many of IRM compounds are derivatives of imidazoquinolines (see, for example, U.S. Pat. No. 4,689,338), but it is also known by several other classes of compounds (see, for example, U.S. Pat. Nos. 5,446,153; 6,194,425; and 6,110,929).

Pharmaceutical compositions containing the IRM compounds described in U.S. Patent Nos. 5,238,944; 5,939,090 and 6,425,776; European Patent 0394026: and U.S. Patent Publication 2003/0199538. IRM-junction 1-(2-methylpropyl)-1H-imidazo[4,5-C]quinoline-4-amine, also known as imiquimod, was put into production in the composition for external use ALDARA for the treatment of senile keratosis, basal cell carcinoma or anogenital warts associated with human papilloma virus.

IRM-connection 2-methyl-1-(2-methylpropyl)-1H-imidazo[4,5-C][1,5]naphthiridine-4-amine, also known kakatamad, described in EP 1512685 for the treatment of viral infections and the induction of the biosynthesis of cytokines.

Resiquimod (4-amino-α,α-dimethyl-2-ethoxymethyl-1H-imidazo[4,5-C]quinoline-1-ethanol), as described in EP 582581, is another member of imidazoquinolines family modifiers of the immune response.

However, therapeutic effects when applied externally IRM compounds for the treatment of certain conditions in a certain place or certain fabrics can prevent a variety of factors, such as, for example, chemical degradation IRM connection and/or other ingredients, and physical instability of the composition (for example, separation of components, salustiana, the precipitation or agglomeration of active particles, and the like).

There is therefore a need for constant development of new and/or improved formulations based on IRM connections.

Disclosure of inventions

Found that imiquimod, satirist or resiquimod can be prepared in the form of foams.

Accordingly, the present invention is a foam composition. In General, the composition contains a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid.

In another aspect, the present invention also provides a method of treating senile keratosis. In General, the method includes applying a composition that contains a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid on the skin of a subject in need of such treatment.

the other aspect of the present invention also provides a method of treating basal cell carcinoma. In General, the method includes applying a composition that contains a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid on the skin of a subject in need of such treatment.

In another aspect, the present invention also provides a method of treatment of anogenital warts. In General, the method includes applying a composition that contains a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid on the skin of a subject in need of such treatment.

In another aspect, the present invention also provides a method of treatment fotopovrezhdeniyu skin or to improve the characteristics of the skin. In General, the method includes applying a composition that contains a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid on the skin of a subject in need of such treatment.

In another aspect, the present invention also provides a method of treatment of cervical dysplasia. In General, the method includes applying a composition that contains a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid on the skin of a subject in need of such treatment.

In another aspect, the present invention also provides a method of treatment of viral diseases, particularly what of ERISA. In General, the method includes applying a composition that contains a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid on the skin of a subject in need of such treatment.

In another aspect, the present invention also provides a method of removing tattoos. In General, the method includes applying a composition that contains a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid on the skin of a subject in need of such treatment.

In another aspect, the present invention also provides a method of treatment of skin metastases. In General, the method includes applying a composition that contains a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid on the skin of a subject in need of such treatment.

In another aspect, the present invention also provides a method of treating skin damage caused by the bites. In General, the method includes applying a composition that contains a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid on the skin of a subject in need of such treatment.

In another aspect, the present invention also provides a method of treatment of keratoacanthoma. In General, the method includes applying the composition to the St contains a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid on the skin of a subject in need of such treatment.

In another aspect, the present invention also provides a method of induction of the biosynthesis of interferon. In General, the method includes applying a composition that contains a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid on the skin of a subject in need of the biosynthesis of interferon.

Other characteristics and advantages of the present invention will become clear from the following detailed description, examples, claims and accompanying figures. In some places in the text description of the invention, explanations are outlined through lists of examples. In each case, the following list is only a representative group and should not be interpreted as an exhaustive list.

The implementation of the invention

Found that imiquimod, satirist or resiquimod can be used in compositions in the form of a pen-based emulsion for use in the pharmaceutical and medical purposes. In General, the foam composition includes a therapeutically effective amount of imiquimod, satirised or resiquimod and fatty acid.

In this text the terms "any", "some", "at least one" and "one or more" are used interchangeably. So, e.g. the measures a composition comprising "any" fatty acid, can be interpreted in the sense that the composition includes at least one fatty acid.

Also in this text transfer numeric intervals at points includes all numbers limited to this interval (for example "1 to 5" includes 1; 1,5; 2; 2,75; 3; 3,80; 4; 5 and so on).

Unless otherwise stated, reference to any connection can include this compound in any pharmaceutically acceptable form, including any isomer (for example, a diastereoisomer or enantiomer), salt, MES, polymorph and the like. In particular, if a compound is optically active, the mention of this connection may include any of the enantiomers of this compound, as well as racemic and enriched mixture of its enantiomers.

The composition includes imidazoquinolines 1-(2-methylpropyl)-1H-imidazo-[4,5-C]quinoline-4-amine, also known as imiquimod, the synthesis of which is described, for example, in U.S. Patent No.4,689,338, Example 99; or the composition includes imidazolidin 2-methyl-1-(2-methylpropyl)-1H-imidazo[4,5-C]-[1,5]naphthiridine-4-amine, also known as satirist, the synthesis of which is described, for example, in WO 2006/074046; or the composition includes imidazoquinolines 4-amino-α,α-dimethyl-2-ethoxymethyl-1H-imidazo[4,5-C]quinoline-1-ethanol, also known as resiquimod, the synthesis of which is described, for example, in EP 582581.

The number of imiquimod, hundred who rimada or resiquimod in the compositions of this invention is a number, effective to treat, prevent recurrence or to activate the immune system to target painful condition or to improve the characteristics of the skin. The total number of imiquimod may be at least 0.1 wt.%, but not more than 9 wt.%. In some aspects, the total amount of imiquimod may be at least 0.5 wt.%, but not more than 9 wt.%, based on the total weight of the composition (if not stated otherwise, all percentages in this text represent the ratio weight/weight relative to the total weight of the composition), although in some embodiments, the composition may contain imiquimod in amounts outside this interval. For example, the composition may contain imiquimod concentration in 0,1%, 0,5%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8% or 9%.

The total number of satirised or resiquimod may be at least about 0.001 wt.%, but not more than 9 wt.%. In some aspects, the total number of satirised or resiquimod may be at least 0.1 wt.%, but not more than 9 wt.%, preferably, at least 0.5 wt.%, but not more than 9 wt.% based on the total weight of the composition (if not stated otherwise, all percentages in this text represent the ratio weight/weight relative to the total weight of the composition), although in some embodiments, the implementation of the composition may contain satirised or resiquimod quantities outside this interval. For example, the composition may contain satirised or resiquimod concentration 0,001%, 0,01%, 0,1%, 05%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8% or 9%.

The foam compositions of the present invention can include one or more additional fillers, such as, for example, fatty acid, preservative, thickener, emulsifier, solvent, softener or humidifier.

The compositions of the present invention include at least one fatty acid. In this context, the term "fatty acid" means a carboxylic acid, saturated or unsaturated, having from 6 to 28 carbon atoms, for example from 10 to 22 carbon atoms. Fatty acids suitable for use in the compositions described herein include, which may contribute to the dissolution of imiquimod, satirised or resiquimod. Suitable fatty acids include, for example, isostearoyl acid, oleic acid, myristic acid, palmitic acid, palmitoleic acid, heptadecanoic acid, stearic acid, linoleic acid, linolenic acid or mixtures thereof. In some embodiments, the implementation of the composition contains, for example, isostearoyl acid, oleic acid or their mixture. In a particular embodiment, the composition contains isostearoyl acid.

Fatty acid present in the composition in which Alceste, sufficient for dissolution of imiquimod, satirised or resiquimod. In some embodiments, the implementation of the total amount of fatty acid is at least of 0.05 wt.%, at least 1 wt.%, at least 3 wt.%, at least 5 wt.%, at least 10 wt.%, at least 15 wt.% or at least 25 wt.%, with respect to the total weight of the composition. In some embodiments, the implementation of the total amount of fatty acid is not more than 40 wt.%, a maximum of 30 wt.%, a maximum of 15 wt.% or a maximum of 10 wt.% with respect to the total weight of the composition.

For some embodiments of the present invention the composition also includes a propellant. In some embodiments, the implementation of the propellant is a hydrocarbon propellant. Suitable hydrocarbon propellants include, for example lower alkanes, such as propane, isobutane and butane. The composition may contain any combination of suitable propellants. For example, the composition may contain a mixture of propane and butane. One of the embodiments includes a mixture of propane and butane 50:50. Another variant implementation includes a mixture of propane and butane 10:90. Another variant implementation includes a mixture of propane and butane 15:85.

The total amount of propellant can be from about 2% to about 25%, although in some embodiments, the composition can sod is neigh total number of propellant outside these limits. In one embodiment, the total amount of the propellant is about 5%. In another embodiment, the total amount of the propellant is about 10%. In another embodiment, the total amount of the propellant is about 15%.

For some embodiments of the present invention the composition includes a mixture of preservatives. It includes one or more compounds that inhibit the growth of microbes (for example, the growth of bacteria and fungi) within the composition (e.g., during production and use). The mixture of preservatives in General includes at least one preservative, such as methylparaben, ethylparaben, propylparaben, butylparaben, benzyl alcohol, Phenoxyethanol, and sorbic acid, or derivatives of sorbic acid, such as esters and salts. The mixture of preservatives may include various combinations of these compounds. In some embodiments, implementation of the present invention the mixture of preservatives include methylparaben, propylparaben and benzyl alcohol. In other embodiments, implementation of the present invention the mixture of preservatives include methyl paraben and benzyl alcohol.

In some embodiments, implementation of the present invention the mixture of preservatives contained in an amount of at least 0.01 wt.%, for example, at least 0.02 wt.%, for less than the least 0.03 wt.%, at least 0,04 wt.% and at least to 0.05 wt.%, with respect to the total weight of the composition. In other embodiments, implementation of the present invention the mixture of preservatives contained in the maximum number of 10 wt.%, preferably up to 3 wt.%, for example, a maximum of 7 wt.%, a maximum of 5 wt.%, maximum of 2.5 wt.%, a maximum of 2.0 wt.%, maximum of 1.0 wt.%, maximum of 0.5 wt.%, most 0.4 wt.%, most 0.3 wt.% and most 0.2 wt.%, with respect to the total weight of the composition.

For some embodiments of the present invention the composition also contains an emulsifier. Suitable emulsifiers include nonionic surfactants, such as Polysorbate 60, servicemonitor, polyglyceryl-4-oleate, polyoxyethylene(4)lauric ether, poloxamer and sarbatorile. In some embodiments, the implementation of the emulsifier is selected from Polysorbate 60 and servicemonitoring, and mixtures thereof.

If the emulsifier is included in the composition, usually in an amount of from 0.1 wt.% up to 10 wt.% of the total weight of the composition, such as from 0.5 wt.% up to 5 wt.%, and from 0.75 wt.% to 4.0 wt.%. In some embodiments, the exercise quantity of the emulsifier, if it is included in the composition is at least 0.1 wt.%, at least 0.5 wt.%, at least 0.75 wt.%, at least 1.0 wt.%, at least 2.5 wt.%, at least 3.5 wt.%, at least 4.0 wt.% or minority is her least 5.0 wt.%, with respect to the total weight of the composition. In some embodiments, the exercise quantity of the emulsifier, if it is included in the composition is a maximum of 10 wt.%, or, at most 5.0 wt.%, or a maximum of 3.5 wt.%, with respect to the total weight of the composition.

For some embodiments of the present invention the composition also contains a magnifier viscosity. Examples of suitable enlargers viscosity include long-chain alcohols, for example cetyl alcohol, stearyl alcohol, Cetearyl alcohol; cellulose ethers, such as hypromellose, hydroxyethylcellulose, hydroxypropylcellulose and carboxymethylcellulose; polysaccharide gums, such as xanthan gum; and homopolymers and copolymers of acrylic acid crosslinked with allilohreos or allinterracial, such as polymers, designated as carbomer in the US Pharmacopoeia. In some embodiments, the implementation of the enlarger viscosity is a xanthan resin.

In some embodiments, the implementation of a number of magnifier viscosity, if it is included in the composition is at least 0.1 wt.%, at least 0.2 wt.%, at least 0.5 wt.%, at least 0.6 wt.%, at least 0.7 wt.%, at least 0.9 wt.% or at least 1.0 wt.%, with respect to the total weight of the composition. In some embodiments, the implementation of a number of zoom is the determinant of viscosity, if it is included in the composition is a maximum of 10 wt.%, most 5.0 wt.%, maximum of 3.0 wt.%, a maximum of 2.0 wt.% or a maximum of 1.5 wt.%, with respect to the total weight of the composition.

In some embodiments, implementation of the present invention the composition also contains at least one softening agent. Examples of suitable softeners include, but are not limited to, long-chain alcohols, for example cetyl alcohol, stearyl alcohol, Cetearyl alcohol; esters of fatty acids, such as isopropylmyristate, isopropyl, diisopropyl dimer of delineat; medium-chain (for example, from 8 to 14 carbon atoms) triglycerides such as Caprylic/capric triglycerides; citylove esters; hydrocarbons having 8 or more carbon atoms, such as light mineral oil, white petrolatum; waxes, such as beeswax. Various combinations of these softeners may be used as desired. In some embodiments, the implementation of the softening agent is selected from cetyl alcohol, stearyl alcohol, petrolatum and mixtures thereof.

In some embodiments, the implementation of a number softener is at least 1.0 wt.%, at least 3.0 wt.%, at least 5.0 wt.% or at least 10 wt.%, with respect to the total weight of the composition. In some embodiments, the implementation of a number softener is Maxim is Ino 30 wt.%, a maximum of 15 wt.% or a maximum of 10 wt.%, with respect to the total weight of the composition.

In some embodiments, the implementation of the compositions of the present invention are emulsions of the type oil-in-water". Used in such compositions, the water is usually purified.

The compositions of the present invention may include additional pharmaceutically acceptable excipients, such as humectants, such as glycerol: chelating agents such as ethylenediaminetetraacetic acid; acidity regulators, such as, for example, potassium hydroxide or sodium hydroxide. In some embodiments, the implementation of the composition comprises glycerin.

In some cases, one ingredient can perform more than one function in the composition. For example, cetyl alcohol can act as a softening agent, and as a magnifier viscosity.

Conditions that can be treated by the introduction of imiquimod, satirised or resiquimod in the form of a foam composition of the present invention include, but are not limited to:

(a) viral diseases such as, for example, diseases resulting from infection by adenovirus, herpes virus (e.g., HSV-1, HSV-II, CMV, or VZV), a poxvirus (e.g., an orthopoxvirus such as variola virus, cowpox or molluscum contagiosum), picornaviruses (for example, rhinoviruses or enterovirus is), orthomyxoviruses (e.g., influenza virus), paramyxoviruses (e.g., parainfluenza virus, mumps virus, measles virus and virus acute respiratory infections (ARI)), a coronavirus (e.g., SARS), papovaviruses (for example, human papilloma virus, such as, for example, the virus that causes genital warts, plain warts or plantar warts), hepadnaviruses (e.g. hepatitis b virus), flaviviruses (for example, hepatitis C virus or virus, dengue fever), or a retrovirus (e.g., lentiviruses such as HIV);

(b) bacterial diseases, such as, for example, diseases resulting from infection by bacteria, for example, the genus Escherichia, Enterobacter, Salmonella, Staphylococcus, Shigella, Usteria, Aerobacter, Helicobacter, Klebsiella, Proteus, Pseudomonas, Streptococcus, Chlamydia, Mycoplasma, Pneumococcus, Neisseria, Clostridium, Bacillus, Corynebacterium, Mycobacterium, Campylobacter, Vibrio, Serratia, Providencia, Chromobacterium, Brucella, Yersinia, Haemophilus, or Bordetella;

(C) other infectious diseases, such as chlamydia, fungal diseases, including (but not limited to them alone) candidiasis, aspergillosis, histoplasmosis, cryptococcal meningitis, or parasitic diseases, including (but not limited to them alone) malaria ploskokletochnyi pneumonia, leishmaniasis, cryptosporidiosis, toxoplasmosis and Trypanosomosis infection;

(d) neoplastic diseases, such as in reepithelialize neoplasia, cervical dysplasia, senile keratosis, keratoakantoma, basal cell carcinoma, flat-cell carcinoma, cutaneous metastases, renal cell carcinoma, sarcoma Kaposi, melanoma, leukemia, including (but not limited to them alone) myeloma leukemia, chronic lymphocytic leukemia, multiple myeloma, non-Hodgkins lymphoma, lymphoma T-cell skin lymphoma b-cells and hairy cell leukemia, and other cancers;

(d) TN2-mediated atopy, such as atopic dermatitis or eczema, eosinophilia, asthma, Allergy, allergic rhinitis or syndrome Ommen;

(e) some autoimmune diseases such as systemic lupus erythematosus, primary thrombocythemia, multiple sclerosis, discoid lupus erythematosus, alopecia areata:

(g) diseases associated with wound healing, such as, for example, inhibition of the formation of keloid zone and other types of scars (for example, improving the healing of wounds, including chronic wounds);

(C) skin conditions, such as, for example, votuporanga skin, improve skin characteristics, the removal of tattoos or skin damage caused by the bites.

The characteristics of the skin are a constant depending on various factors, including, for example, humidity, UV radiation, cosmetics, aging, illness, stress, Smoking and eating habits.

To the MS, which can be treated by the present invention, may include a facial skin, neck skin, arms, forearms, legs or torso and other body parts.

The improved characteristics of the skin includes rejuvenation, growth retardation or prevention of skin changes associated with natural or innate aging. In this context, the term "prevention" and its variants refer to any stage of the delay skin changes. For example, the improved characteristics of the skin includes rejuvenation, growth retardation or prevention of skin changes associated with damage to sunlight or photoaging, i.e. with skin changes associated with exposure to sunlight or other forms of actinic radiation (such as UV light and camera fake tan). As another example, the improved characteristics of the skin may also include rejuvenation, growth retardation or prevention of skin changes that occur due to external factors, including (but not limited to, radiation, air pollution, wind, cold, humidity, heat, chemicals, smoke, Smoking, and combinations thereof.

Improve skin characteristics may also include rejuvenation, prevention or reduction of scarring that can occur, for example due to certain skin conditions (e.g., PRA and), infections (e.g., leishmaniasis) or injury (e.g., abrasions, punctures, cuts or surgical incisions).

Changes in the skin that can be treated using the present invention include, for example, wrinkles (including, but not limited to, human facial wrinkles), deepening of skin lines, thinning of the skin, small scars, yellowing of the skin, mesoscutal, hyperpigmentation, pigmentation and/or non-pigmented age spots, rough skin, loss of elasticity, loss of collagen fibers, abnormal changes in elastic fibers, deterioration of small blood vessels of the skin, the formation of spider veins and their combinations.

Additionally, the foam composition may be used for delivery of imiquimod, satirised or resiquimod as AIDS vaccines for local use with any material that enhances humoral and/or cell-mediated immune response, such as, for example, live viral, bacterial or parasitic immunogen; inactivated viral immunogen, immunogen derived from tumors, using protozoa, bacteria, fungi or bacteria, toxoid, toxins; autoimmune antigens; polysaccharides; proteins; glycoproteins; peptides; cellular vaccines; DNA vaccines; autovaccine; recombinant Proteus is s, glycoproteins, peptides, and the like, for use, for example, vaccines BCG, cholera, plague, typhoid, hepatitis a, hepatitis b, hepatitis C, influenza A, influenza b, parainfluenza, polio, rabies, measles, mumps, rubella, yellow fever, tetanus, diphtheria, Haemophilus influenza b, tuberculosis, meningococcal and pneumococcal vaccines, vaccines, adenovirus, HIV, chicken pox, cytomegaly virus, dengue fever, feline leukemia, avian influenza, HSV-1 and HSV-2, swine fever, Japanese encephalitis, respiratory syncytial virus, rotavirus, human papilloma virus, yellow fever and Alzheimer's disease.

The methods of the present invention can be implemented on any suitable subject. Suitable subjects include, but are not limited to) animal organisms, such as man, other primates, poultry, rodents, dogs, cats, horses, pigs, sheep, goats or cows.

Examples

The following examples were selected only to further illustrate the properties, advantages and other aspects of the present invention. However, it should be clearly understood that while the examples serve this purpose, used specific materials and quantities, as well as other conditions and details should not be construed as any limitation of the present and the gain.

The compositions shown in the following tables 1 to 4 were prepared following General method.

Preliminary preparation of a mixture of the imiquimod/ezoterikova acid/benzyl alcohol: imiquimod is mixed with ezoterikovou acid and stirred under heating (about 55°C) to dissolve the bulk of imiquimod. Add benzyl alcohol and continue mixing until until the entire imiquimod does not go into solution.

Preparation of oil phase: cetyl alcohol, stearyl alcohol, white petrolatum, Polysorbate 60 and servicemonitor added to the previously prepared mixture imiquimod/ezoterikova acid/benzyl alcohol and stirred with heating (about 55°C.) until complete dissolution of all components.

Preparation of aqueous phase: methylparaben and propylparaben is mixed with water and a portion (about 50%) of glycerin and stirred under heating (about 55°C) to dissolve the parabens. Separately prepare a dispersion of xanthan resin mixing xanthan resin with the remaining portion of glycerin and mixing to disperse xanthan resin. The dispersion of xanthan resin is added slowly with stirring to a solution of parabens, holding a temperature of about 55°C. the Stirring continued until until all xanthan gum is not fully dispersed

The mixing of the phases, the aqueous phase is added to the oil phase at about 55°C. the Mixture is homogenized for at least 15 minutes. The resulting emulsion is cooled to room temperature and then placed in a glass vessel. The following tables 1 and 2 show the composition (wt.%) compounds before the addition of the propellant.

Adding propellant: the emulsion is placed in a plastic-covered glass container. The vessel steamed up aerosol valve (or valve DC or dosing valve). The vessel is filled with propellant gas burette pressure with nitrogen. The vessel is then shaken to disperse the emulsion in the propellant. The following tables 3 and 4 show the composition (wt.%) compositions after the addition of the propellant.

Table 1
Trains to add propellant
IngredientNo. 1No. 2No. 3No. 4No. 5No. 6
The imiquimod5,885,885,565,26 55
Ezoterikova acid29,4129,4127,7826,322525
Benzyl alcohol : 2,352,352,222,1122
Polysorbat 604,004,003,78to 3.583,43,4
Servicemonitor0,710,710,670,630,60,6
Xanthan gum0,590,590,560,530,50,5
Methylparaben0,240,240,22 0,210,20,2
Propylparaben0,020,020,020,020,020,02
Cetyl alcohol2,592,592,442,322,22,2
Stearyl alcoholthe 3.65the 3.653,443,263,13,1
Vaseline3,533,533,333,1633
Glycerin2,352,352,222,1122
Water44,6844,6847,7652,9852,98

1,80
Table 2
Trains to add propellant
IngredientNo. 7No. 8No. 9No. 10No. 11No. 12
The imiquimod5,565,565,565,565,565,56
Esterina acid13,9513,9513,9513,9513,9513,95
Benzyl alcohol : 2,222,222,222,222,222,22
Polysorbate 601,901,901,90 1,901,901,90
Sorbitan-monostearate2,002,002,002,002,002,00
Xanthan gum0,150,150,150,150,150,15
Methylparaben0,330,330,330,220,220,22
Propylparaben0,030,030,030,020,020,02
Cetyl alcohol1,301,301,301,301,301,30
Stearyl alcohol1,801,801,801,801,80
Vaseline1,751,751,751,751,751,75
Glycerin3,103,103,103,103,103,10
Water65,9165,9165,9166,0366,0366,03

Table 3
The composition after addition of the propellant
IngredientNo. 1No. 2No. 3No. 4No. 5No. 6
The imiquimod555 54,254,75
Ezoterikova acid25252525each holding 21.2523,75
Benzyl alcohol : 22221,71,9
Polysorbate 603,43,43,43,42,893,23
Sorbitan-monostearate0,60,60,60,60,510,57
Xanthan gum0,50,50,50,50,430,48
Methylparaben0,20,2 0,20,20,170,19
Propylparaben0,020,020,020,020,020,02
Cetyl alcohol2,22,22,22,21,872,09
Stearyl alcohol3,13,13,13,12,642,95
Vaseline33332,552,85
Glycerin22221,71,9
Water37,9837,98 42,9847,9845,0250,32
Propane:butane (50:50)150105155
Propane:butane (10:90)0150000

Table 4
The composition after addition of the propellant
IngredientNo. 7No. 8No. 9No. 10No. 11No. 12
The imiquimod5,005,005,005,005,005,00
Esterina acid12,5612,562,56 12,5612,5612,56
Benzyl alcohol : 2,002,002,002,002,002,00
Polysorbate 601,711,711,711,711,711,71
Sorbitan-monostearate1,801,801,801,801,801,80
Xanthan gum0,140,140,140,140,140,14
Methylparaben0,300,300,300,200,200,20
Propylparaben0,03 0,030,030,020,020,02
Cetyl alcohol1,171,171,171,171,171,17
Stearyl alcohol1,621,621,621,621,621,62
Vaseline1,581,581,581,581,581,58
Glycerin2,792,792,792,792,792,79
Water59,3059,3059,3059,4159,4159,41
Propane:butane (50:50)1 001000
Propane:butane (10:90)01000100
Isobutane00100010

The compositions shown in the following tables 5 and 6 were prepared following General method.

Preliminary preparation of a mixture of the imiquimod/ezoterikova acid: imiquimod is mixed with ezoterikovou acid and stirred under heating (about 55°C) to dissolve the bulk of imiquimod and up until the whole imiquimod does not go into solution.

Preparation of oil phase: cetyl alcohol, stearyl alcohol, medical petrolatum, Polysorbate 60 and servicemonitor added to the previously prepared mixture imiquimod/ezoterikova acid and stirred under heating (about 55°C.) until complete dissolution of all components.

Preparation of aqueous phase: methylparaben and propylparaben are mixed in with the water and a portion (about 50%) of glycerin and stirred under heating (about 55°C) to dissolve the parabens. Separately prepare a dispersion of xanthan resin mixing xanthan resin with the remaining portion of glycerin and mixing to disperse xanthan resin. The dispersion of xanthan resin is added slowly with stirring to a solution of parabens, holding a temperature of about 55°C. the Stirring continued until until all xanthan gum is not fully dispersed.

The mixing of the phases, the aqueous phase is added to the oil phase at about 55°C. the Mixture is homogenized for at least 15 minutes. The resulting emulsion is cooled to room temperature and then placed in a glass vessel. The following table 5 shows the composition (in wt.%) compounds before the addition of the propellant.

Adding propellant: the emulsion is placed in a plastic-covered glass container. The vessel steamed up aerosol valve (or valve DC or dosing valve). The vessel is filled with propellant gas burette pressure with nitrogen. The vessel is then shaken to disperse the emulsion in the propellant. The following table 6 shows the composition (in wt.%) compositions after the addition of the propellant.

Table 5
Trains to add propellant
IngredientNo. 13No. 14No. 15
The imiquimod5.565.565.56
Ezoterikova acid13.9513.9513.95
Polysorbate 601.901.901.90
Servicemonitor2.002.002.00
Xanthan gum0.150.150.15
Methylparaben0.330.330.33
Propylparaben0.030.030.03
Cetyl alcohol1.301.301.30
Stearyl alcohol1.80 1.801.80
Vaseline1.751.751.75
Glycerin3.103.103.10
Water68.1368.1368.13

Table 6
The composition after addition of the propellant
IngredientNo. 13No. 14No. 15
The imiquimod5.005.005.00
Ezoterikova acid12,5625,0025.00
Polysorbate 601,713.403.40
Servicemonitor1.800.600.60
Xanthan gum0.140.500.50
Methylparaben0.300.200.20
Propylparaben0.030.020.02
Cetyl alcohol1.172.202.20
Stearyl alcohol1,623.103.10
Vaseline1.583.003.00
Glycerin2.792.002.00
Water61,3037,9842,98
Propane:butane (50:50)1000
Propane:butane (10:90)0 0
Isobutane0010

The compositions shown in the following tables 7 and 8, were prepared following General method.

Preliminary preparation of a mixture of the imiquimod/ezoterikova acid/benzyl alcohol: imiquimod is mixed with ezoterikovou acid and stirred under heating (about 55°C) to dissolve the bulk of imiquimod. Add benzyl alcohol and continue mixing until until the entire imiquimod does not go into solution.

Preparation of oil phase: Polysorbate 60 and servicemonitor added to the previously prepared mixture imiquimod/ezoterikova acid/benzyl alcohol and stirred with heating (about 55°C.) until complete dissolution of all components.

Preparation of aqueous phase: methylparaben and propylparaben, if they enter the composition is mixed with water and stirred with heating (about 55°C) to dissolve the parabens. Add xanthan resin and pereshivayut the aqueous phase at about 55°C to until all xanthan gum is not fully dispersed.

The mixing of the phases, the aqueous phase is added to the oil phase at about 55°C. the Mixture is homogenized for at least 15 minutes. The obtained emulsion of ohla who give to room temperature and then placed in a glass vessel. The following table 7 shows the composition (in wt.%) compounds before the addition of the propellant.

Adding propellant: the emulsion was placed in a plastic-covered glass container. The vessel steamed up aerosol valve (or valve DC or dosing valve). The vessel is filled with propellant gas burette pressure with nitrogen. The vessel is then shaken to disperse the emulsion in the propellant. The following table 8 shows the composition (in wt.%) compositions after the addition of the propellant.

Table 7
Trains to add propellant
IngredientNo. 16No. 17No. 18No. 19No. 20No. 21
The imiquimod5,885,885,565,265,261,05
Ezoterikova acid29,4129,4127,7826,32 26,325,26
Benzyl alcohol : 2,352,352,222,112,110,42
Polysorbate 604,004,003,78to 3.58to 3.580,72
Servicemonitor0,710,710,670,630,630,13
Xanthan gum0,590,590,560,531,051,05
Methylparaben0,240,240,220,210,110,11
Propylparaben0,020,02 0.020,0200
Water56,8056,8059,2061,3560,9591,26

Table 8
The composition after addition of the propellant
IngredientNo. 16No. 17No. 18No. 10No. 20No. 21
The imiquimod255551
Ezoterikova acid25252525255
Benzyl alcohol : 222 220,4
Polysorbate 603,43,43,43,43,40,68
Servicemonitor0,60,60,60,60,60,12
Xanthan gum0,50,50,50,511
Methylparaben0,20,20,20,20,10,1
Propylparaben0,020,020,020,0200
Water48,2848,2853,28 58,2857,986,7
Propane:butane (50:50)15010500
Propane:butane (10:90)0150055

Example 1

Male naked CD rats (Charles Rivers Laboratories, Wilmington, MA) weighing 220-250 grams (approximate age 8-10 weeks) taught by a neck collar for two days prior to the introduction of the drug on the day of the experiment the rats wore collars to prevent oral penetration of the composition, and then were treated topically 45-47 milligrams of the composition of table 3 or 8 on an area of about 6 cm, in the right lower back. The composition is rubbed into the skin with your finger in a nitrile glove for about 1-3 minutes. Rats were placed in individual cages and were unable to take the collars within 6 hours.

After 6 hours took the blood by heart puncture under anesthesia with carbon dioxide. The blood was left to collapse at room temperature for about 20 minutes, then serum was separated from the clot center is fugiranje (Beckman Coulter Allegra 21R, 4180 horizontal rotor, Beckman Coulter, Inc. Fullerton, CA) at 2000 rpm for 10 minutes while cooling. The resulting serum was stored at

-20°C until analysis on the concentration of TNF-alpha and MCP-1.

Animals were scored, spent three puncture biopsy 8 mm from each of the two sides of each animal: the treated side and the opposite side (lower left side back). Tissue biopsies were weighed and placed in a sealed 1,8 ml cryoprobes and quickly frozen in liquid nitrogen. Frozen skin tissue suspended in 1.0 ml of RPMI medium (Protide Pharmaceuticals, St. Paul, MN) and 10% fetal bovine serum, 2 mm L-glutamine, 1% penicillin/streptomycin, 5×10-5M 2-mercaptoethanol and 1% protease-inhibition of complex III (Calbiochem/EMD Biosciences, San Diego, CA). Skin tissue homogenized on ice using a TISSUE TEAROR (Biospec Products, Inc. Bartlesville, OK) for about 1 minute. Supernatant skin tissue was centrifuged (Beckman Coulter Allegra 21R, 4180 horizontal rotor) at 4800 rpm for 10 minutes while cooling to precipitate cellular residues. Supernatant was collected and stored at -20°C until analysis on the concentration of TNF-alpha and MCR-1.

The concentration of TNF-alpha and MCR-1 was determined by ELISA method (TNF-alpha, BD Pharmingen, San Diego, CA; IVICP-1, Biosource International, Camarillo, CA) according to manufacturer's instructions. The ELISA plate was displayed on the device SpectraMax reader plates microanalysis of the (Molecular Devices Corp., Sunnyvale, CA) and used the software package SOFTMAX PRO for smoothing the curves of absorption. The results of measurements of concentrations of TNF-alpha and MCR-1 in serum is expressed in pilgrammage per milliliter (PG/ml) serum. The measurement results of concentrations for dermal tissue are expressed in PG 200 mg of tissue.

Full disclosure of the patents, patent documents, and publications cited herein are incorporated as references in their entirety as if each was incorporated individually. In case of conflict, the present description, including definitions, is fundamental.

Various modifications and variations of the present invention is obvious to a qualified employee without violating the boundaries and substance of the present invention. Illustrative embodiments of, and examples are given only as examples and are not intended to limit the scope of the present invention. The borders of the present invention is limited only by the claims set forth below.

1. The foam composition of the modifier of the immune response, including the ingredients in the following ratio, wt.%:

the imiquimod2.0 to 3.0,
ezoterikova acid0,05-40,0
p is opulent 2,0-25,0
the mixture of preservativesof 0.01 to 3.0
servicemonitor1,0-3,5
enlarger viscosity0,1-10,0
waterrest

2. The composition according to claim 1, in which the propellant is a hydrocarbon.

3. The composition according to claim 2, in which the hydrocarbon is selected from the group comprising propane, butane, isobutane or mixtures thereof.

4. The composition according to claim 1, in which the mixture of preservatives include ethylparaben, butylparaben, Phenoxyethanol, sorbic acid, derivatives of sorbic acid, such as esters or salts, methylparaben, propylparaben, benzyl alcohol, or a mixture thereof.

5. The composition according to claim 1, in which the magnifier viscosity selected from the group including cetyl alcohol, stearyl alcohol, Cetearyl alcohol, hypromellose, hydroxyethyl cellulose, hydroxypropylcellulose, carboxymethylcellulose, xanthan resins, and homopolymers and copolymers of acrylic acid, crosslinked with allilohreos or allinterracial, or mixtures thereof.

6. The composition according to claim 1, which further comprises a softening agent.

7. The composition according to claim 6, in which the softening agent is present in an amount of 1-30 wt.%.

8. The composition is .6, in which the softening agent selected from the group including cetyl alcohol, stearyl alcohol, Cetearyl alcohol, isopropylmyristate, isopropyl, Diisopropylamine dimer of delineat, Caprylic/capric triglyceride, citylove esters, light mineral oil, white petrolatum and beeswax, or a mixture thereof.

9. The composition according to claim 1, which further comprises a humectant.

10. The composition according to claim 9, in which the humidifier is a glycerin.

11. The composition according to claims 1-10, which is an emulsion of the type oil-in-water".

12. Set comprising drug-containing composition according to claims 1-11, and the aerosol container, in which the tool is placed.

13. Set indicated in paragraph 12, in which the aerosol container equipped with a metering valve.

14. Set indicated in paragraph 12, in which the aerosol container equipped with a valve continuous current.

15. Applying a composition according to any one of claims 1 to 11 for the treatment of senile keratosis.

16. Applying a composition according to any one of claims 1 to 11 for the treatment of basal cell carcinoma.

17. Applying a composition according to any one of claims 1 to 11 for the treatment of anogenital warts.

18. Applying a composition according to any one of claims 1 to 11 for the treatment fotopovrezhdeniyu skin or improvements of the skin.

19. Applying a composition according to any one of claims 1 to 11 for the treatment of cervical dysplasia.

20. Applying a composition according to any one of claims 1 to 11 for the treatment of a virus who's diseases, especially herpes.

21. Applying a composition according to any one of claims 1 to 11 for the treatment of skin metastases.

22. Applying a composition according to any one of claims 1 to 11 for the treatment of skin damage caused by the bite.

23. Applying a composition according to any one of claims 1 to 11 for the treatment of keratoacanthoma.

24. Applying a composition according to any one of claims 1 to 11 for the induction of the biosynthesis of interferon.



 

Same patents:

FIELD: medicine.

SUBSTANCE: group of inventions relates to cosmetology. Method includes stages at which processing of skin image is performed, which includes cross conversion to binary form and/or processing by comparison of short linear segments to obtain 10 or more types of physical parameters, related to dermal furrow; then physical parameters, obtained at previous stage are substituted into prediction formula. Prediction formula is determined by multi-variant analysis of 10 or more types of physical parameters, related to dermal furrow, and visual assessment values, distributes by categories from third to tenth degree, related to skin and/or wrinkle, obtained from a number of samples in order to obtain assessment value by categories from 3 to 10 degree and assessment of obtained assessment value as assessment result with respect to skin and/or wrinkle texture. Described are device for assessment of skin texture and method of selecting medication for external application on skin, which uses assessment method or device.

EFFECT: providing assessment of epidermal tissues.

7 cl, 11 dwg, 10 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to new benzimidazole derivatives of general formula (I) or to its pharmacologically acceptable salts wherein R1 represents a C6-aryl group which can be substituted by 1-3 groups optionally specified in a group of substitutes (a), or a heterocyclic group which represents pyridyl, dihydrobenzofuranyl, 1,3-benzodioxolyl, tetrahydropyranyl, tetrahydrofuranyl which can be substituted by 1-3 groups optionally specified in a group of substitutes (a), R2 represents a C1-C6 alkyl group, R3 represents a C6-aryl group which can be substituted by 1-2 groups optionally specified in a group of substitutes (a), Q represents a group represented by formula =CH-, or a nitrogen atom and a group of substitutes (a) represents a group consisting of a halogen atom, a C1-C6 alkyl group, a C1-C6 halogenated alkyl group, a carboxyl group, a C2-C7 alkylcarbonyl group, a C2-C7 alkoxycarbonyl group, a C1-C6 alkoxy group, a C1-C6 halogenated alkoxy group, an amino group, a 4-morpholinyl group and a di-C1-C6 alkyl)amino group. Also, the invention refers to a pharmaceutical composition based on a compound of formula (I), to a PPARγ activator/modulator based on the compound of formula (I), to using the compound of formula (I), to a method of reducing blood glucose, to a method of activating PPARγ, a method of treating and/or preventing said pathological conditions.

EFFECT: there are produced new benzimidazole derivatives showing PPARγ modulatory activity.

41 cl, 2 dwg, 6 tbl, 76 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical and cosmetic industry, particularly an agent applied to skin. A vesicle applied to skin containing α,ε-bis(γ-N-(C10-30)acylglutamyl)lysine and/or its salt; ceramide and/or its derivative; and one or more ethers selected from glycerin ether of fatty acid, polyglycerin ether of fatty acid and glycerin ether of pyroglutamic acid taken in certain proportions. The therapeutic agent for external application to skin containing a certain amount of the vesicle.

EFFECT: vesicle and based therapeutic agent are stable, effectively encapsulates an active ingredient that allows it reaching true skin, effectively suppress transepidernal dehydration.

6 cl, 13 tbl, 8 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of medicine, namely to pharmaceutics. Essence of method lies in obtaining preparation which inhibits apoptosis of cells containing DNA directly or indirectly damaged by ultraviolet irradiation or something similar. Apoptosis-inhibiting preparation for epidermal cell contains as an active ingredient water- and ethanol-soluble liquorice extract. Apoptosis-inhibiting preparation contains anti-apoptosis factor resulting from BCL-2 protein expression and possesses ability to prevent damage to DNA, caused by ultraviolet irradiation.

EFFECT: application of claimed preparations will make it possible to enhance ability of cells to restore tissue, can be added into various medications, as well as reduces damage to epidermal cell DNA, caused by impact of ultraviolet irradiation, moreover, it does not produce abnormal or negative effect on normal skin cells.

5 cl, 6 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine, cosmetology, and may be used for treating or preventing light exposure on a human or an animal. That is ensured by a photoprotective composition, including in the form of a cosmetic preparation containing the carotenoid compound diadinoxantine or its pharmaceutically acceptable prodrug or salt. There are also offered a method for diadinoxantine recovery from algae, as well as a method for producing a photoprotective or photoprotected product involving application or impregnation of said product with photoprotective composition containing diadinoxantine.

EFFECT: composition is effective in protection against light of wave length 350 to 500 nm.

21 cl, 4 tbl, 3 ex, 4 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is offered is application of allopurinol or its pharmaceutically acceptable salt for treating or preventing palmoplantar erythrodysesthesia (PPE) induced by fluoropyrimidine chemotherapy, a related method of treating and a pharmaceutical composition for skin application of the same purpose, and the composition does not contain methyl sulphonyl methane or cetomacrogol.

EFFECT: relief, and in 66% of patients - delitescence of PPE symptoms in the absence of toxic effects on allopurinol and compliance of the patients is shown.

12 cl, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to agent for skin bleaching, representing pyrimidyl pyrazole compound of formula (1), where R1, R3, R4 and R6 each independently represents C1-3alkyl and R2 and R5 each independently represents hydrogen atom or C1-3alkyl, or its pharmacologically acceptable salt. Said agent inhibits production of melanin, possesses low cytotoxicity and can be used as bleaching agent for improvement or prevention of pigment spots, freckles, skin darkening, etc. Invention also relates to composition for skin bleaching for external application, which contains effective amount of said pyrimidyl pyrazole compound of formula (1), described in any of items 1-3, or its pharmacologically acceptable salt. Preferable composition represents cosmetic preparation.

EFFECT: obtaining agent for skin bleaching.

6 cl, 3 tbl, 17 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel carbostyril compounds of general formula (1) or salts thereof with common pharmaceutically acceptable acids or pharmaceutically acceptable basic compounds, having activity on promotion of TFF2 production, a pharmaceutical composition based on said compounds, an agent based on disclosed compounds used in case of a disorder where up-regulation of TFF has a prophylactic and/or therapeutic effect, use of disclosed compounds to prepare said agent and a method of producing disclosed compounds. The invention also relates to novel specific carbostyril compounds or salts thereof with common pharmaceutically acceptable acids or pharmaceutically acceptable basic compounds. In structural formula (1), A is a direct bond, a lower alkylene group or lower alkylidene group, X is an oxygen or sulphur atom, the bond between positions 3 and 4 of the carbostyril backbone is a single bond or a double bond, R4 and R5 each denotes a hydrogen atom provided that, when the bond between positions 3 and 4 of the carbostyril backbone is a double bond, R4 and R5 can instead be bonded to each other in form of a -CH=CH-CH=CH- group, and R1, R2 and R3 assume values given in the claims.

EFFECT: high efficiency of compositions based on said compounds.

32 cl, 23 dwg, 184 tbl, 1535 ex

FIELD: medicine.

SUBSTANCE: there are described phosphorylated triterpenic acids and/or their salts including ursolic acid phosphate, oleanolic acid phosphate, betulinic acid phosphate and asiatic acid phosphate used as ingredients of topical drugs and cosmetic preparations as those exhibiting anti-inflammatory action and inhibiting melanin production. A topical skin preparation is preferentially a beauty preparation, particularly preferentially - a quasi-drug.

EFFECT: intensified anti-inflammatory action of the preparation.

8 cl, 6 ex

FIELD: medicine.

SUBSTANCE: benzylursolate of formula I is prepared: of ursolic acid by adding an alkaline agent, alkylation with benzyl halogen in dimethyl formamide and following purification of an end product. As a source of ursolic acid, cowberry extraction cake in ethyl alcohol is used; extracts are transferred in salts by boiling with potassium hydroxide added; benzyl chloride is used as benzyl halogen, and purification involves rinsing with petroleum ester and crystallisation of acetone.

EFFECT: invention enables simplifying the process and reducing its price.

1 ex

FIELD: medicine.

SUBSTANCE: for pigmentation removal, there is offered a device for pigmentation elimination from a skin area and a method of applying the same. The given device comprises a handle section accommodating a motor and a gear assembly employed for the provision of reciprocation of a rod coupled with the gear assembly, a body section enclosing such rod with a first end of the body being attached to the handle and a second end of the body having a tip tightly jointed with a skin area, a kit of needles attached to the end of a rod near the tip, a cylindrical valve which is attached to the rod above the kit of needles and has an inlet and an outlet connected through a liquid with a bottom of the cylindrical valve. When using the device, a skin pigmentation elimination solution is placed in a solution container. The latter and a suction mechanism are attached to said device, and then the tip of the specified device is positioned over the skin area. After the motor is actuated, the kit of needles is alternately projected from the specified tip and pulled from the skin area back to the specified tip.

EFFECT: complete skin pigmentation elimination, including due to destruction of the cells containing a pigment by means of moving the needles in a skin surface and back and maintaining synchronised needle movement and solution flow.

7 cl, 5 dwg, 3 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, in particular to dermatovenerology and gynaecology and to treatment of anogenital warts. For this purpose 30% glicifon ointment is applied onto lesion foci. Ointment is applied daisy in a thin layer for 6-8 hours. Course of treatment is 5-14 days.

EFFECT: method provides for efficient destruction of warts without systematic side effects.

3 ex

FIELD: medicine.

SUBSTANCE: declared invention concerns chemical-pharmaceutical industry, and covers a medicinal agent for treating benign, virus, premalignant and malignant non-metastasing skin affections, dysplastic (pretumour) and inflammatory affections of visible mucous membranes, virus, mycosis of skin and nails, as well as correction of wrinkles and senile pigment spots by lifetime devitalisation, containing alpha-haloidcarboxylic acid and its zinc salt of general formula R-(CH2)m-CXY-COOH and [R- (CH2)m-CXY-COO]2Zn where Y = CI, Br or J, X=H or Y, m=1-10, R = H, aryl, cycloalkyl, alkyl of general formula CnH2n+1, n=1-5, in the ratio 500:1 to 10:1 and water in amount 1.5 to 70.0 wt %.

EFFECT: agent is characterised with high efficiency; it is not toxic in small dosage and does not have by-effects.

4 cl, 77 ex, 1 tbl

FIELD: medicine.

SUBSTANCE: tablets Iodantirypine are taken in dose 100 mg twice a day within 30 days. Simultaneously suppositories genferon are used in dosage 250000 ME vaginally for women and in dosage 500000 ME through rectum for men. Suppositories are introduced twice a day within 10 days. In case condyloma sizes within 0,1 to 1 cm, specified pharmacotherapy is simultaneously combined with chemical destruction thereof.

EFFECT: provides complex antiviral, antiinflammatory, regenerating, anti-oxidant, membrane stabilising action, reduced recurrence rate without by-effects.

2 ex

FIELD: medicine.

SUBSTANCE: invention concerns application of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid (adapalene) or its salts in obtaining of pharmaceutical gel composition intended for treatment of dermatological diseases of inflammatory of proliferate nature, including common, comedonal, polymorphous, nodulocystic acne, acne conglobata, secondary acne, such as sun, drug or occupational acne, extensive and/or severe psoriasis, ichtyosis and ichtyosiform states, Darier disease, palmar-plantar keratoderma, comedo nevus and post-inflammatory pigmentation. The pharmaceutical composition is a gel of the following formula:

Adapalene3 mgCarbomer 940 (BF Goodrich Carbopol 980)11 mgDisodium edetate1 mgMethylparaben2 mgPoloxamer 1242 mgPropyleneglycol40 mgSodium hydroxide: quantity required for obtaining рН 5.0+0.3

Distilled water sufficient quantity up to 1 g.

EFFECT: good tolerance at reduced concentration of active substance.

5 cl, 3 dwg, 3 ex

Compound // 2323940

FIELD: chemistry.

SUBSTANCE: photosensitising agents obtained by reducing a double bond in porphyrinic macrocycle of sulphonated mesotetraphenylporphyrine, preferably disulphonated mesotetraphenylporphyrine, such as TPPS2a. Resulting sulphonated mesotetraphenylchlorines are compounds of formula (I) , (where X stands for -SO3Н; each of n, p, q and r independently stands for 0 or 1; and sum of n, p, q and r is an integer from 1 to 4, preferably at least 2, in particular, 2 or 4), isomers or isomeric mixture. Compounds in accordance with the said invention and pharmaceutically suitable salts thereof have a high extinction coefficient in the region of 630 to 680 nm.

EFFECT: compounds are widely used as photosensitising agents for photochemical internalisation of molecules and photodynamic therapy.

25 cl, 8 ex, 8 dwg

FIELD: medicine.

SUBSTANCE: method involves administering combined medical preparation composed of 0.2 g of nisoral and 0.5 g of aspirin. Finger- or toe-nails are heat treated in hot water containing sodium chloride solved in 10:1 proportion during 20-30 min. Injured nail surface is erased and the preparation is applied. The mixture is covered with gauze napkin matching nail bed in size. Air-tight bandage with adhesive plaster is applied covering also 0.5-1 cm large healthy tissue zone above eponychium. The bandage is taken off 4-5 days later. The procedure is repeated 4 times or less, depending on injury depth.

EFFECT: enhanced effectiveness of treatment; reduced risk of complications and disease recurrence.

2 cl, 2 dwg

FIELD: medicine, in particular composition for chemical piling.

SUBSTANCE: claimed composition contains component (A) of general formula B-[-(CH2CH2O)m(AO)n-H]a, wherein B is alcohol residue, AO is alkyleneoxy group having from 3 to 18 carbon atoms; a = 1 or more, integer number; m = 4 or more, integer number; n = 0 or 1 or more, integer number; with the proviso that ethylene oxide molar amount (m) is 40 % or more based on total molecular weight of ethylene oxide chain; and phenol compound (B). Composition of present invention has no side effects after treatment such as red spots, pigmentation or cicatrices and is useful in skin regeneration, spot elimination, pimple treatment, fat skin improvement, etc.

EFFECT: composition for chemical piling of improved effect.

3 cl, 5 ex

FIELD: medicine.

SUBSTANCE: the present innovation deals with a self-gluing matrix system that contains crystalline aminolevulinic acid. The latter is in ready-to-use form being resistant at storage at minimal decomposition.

EFFECT: higher efficiency of application.

12 cl, 9 dwg, 6 ex, 2 tbl

FIELD: medicine.

SUBSTANCE: remedy has alkaline metal hydroxide selected from group comprising potassium hydroxide, and/or sodium hydroxide, and/or calcium hydroxide and distilled water. Zinc compounds are additionally introduced under ingredients proportion, in % by mass: alkaline metal hydroxide 2-34; zinc compounds 0.01-1.2; distilled water the rest. Zinc oxide and/or zinc salt like ZnSO4 are selected as the zinc compounds. Stain solution is introduced into remedy composition, like 1-5% brilliant ethyl solution in alcohol in the amount of 0.1-0.5% by mass.

EFFECT: enhanced effectiveness of treatment; accelerated wound healing.

2 cl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to medicine and describes a solution for producing an inhalation preparation containing fenoterol hydrobromide as an active agent, purified water and excipients with the excipients presented by sodium benzoate, an acidity regulator representing an organic acid in the following proportions, mg/ml: fenoterol hydrobromide 1.0-1.1; sodium benzoate 0.2-2.0; organic acid 1.4-1.7; purified water the rest provided pH makes 3.2-3.5.

EFFECT: solution has the high value of respirable fractions and high stability.

6 cl, 3 ex

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