New dermatological cream prepared with use of sodium fusidate

FIELD: medicine.

SUBSTANCE: invention represents cream for skin infections, containing fusidic acid formed in situ in an oxygen-free medium with the use of sodium fusidate. The above cream contains fusidic acid prepared in situ by the conversion of sodium fusidate with adding acid slowly, with a particle size of the active substance of 2.33 mcm to 16.3 mcm, and the cream base containing at least one ingredient of each type: primary and secondary emulsifying agents specified in a group containing ketostearyl alcohol, ketomacrogol-1000, Polysorbate-80 and Span-80, paraffin as wax, a combined dissolving agent specified in a group including propylene glycol, hexylene glycol, polyethylene glycol 400, nitric acid or lactic acid and water.

EFFECT: invention provides high stability of the active ingredient throughout the whole shelf life.

10 cl, 16 tbl

 

The technical field

This invention relates to primary and secondary bacterial skin infections, and, in particular, it relates to the treatment of these infections with the use of a cream containing fuseboy acid, which was manufactured using fusidate of sodium as the source of pharmaceutically active ingredient (AI).

Background of invention

Currently, there are many types of treatment, both local and systemic, primary and secondary skin infections caused by gram-positive organisms such as Staphylococcus aureus, Staphylococcus spp, etc., In compositions for topical and systemic treatment of bacterial infections is usually used at least one active pharmaceutical ingredient (AI) in combination with the component framework. When using the cream, the AI usually include antibiotic/antibacterial such as positiva acid, etc.,

In the present creams containing fuseboy acid, positiva acid in the form of a fine powder is used as AI. The small particle size increases its contact with skin and penetration due to the formation of large specific surface area, and provides a sensation when applied to the skin. However, a serious disadvantage arising from the small size of h is CI fuseboy acid, is that this forms a huge surface area for contact and reaction with molecular oxygen during manufacturing and processing of this cream. This has serious implications for its chemical stability and can lead to a rapid decrease in the efficiency of AI (fuseboy acid) in the final cream.

Degradation due to oxidation is the main cause of instability currently available creams. Table 1 shows that the degradation in the samples AI (fuseboy acid) when exposed to oxygen ranged from 7.7% to 11% in conditions varying from room temperature to 45°C, in the analysis three months, during which they were exposed to these conditions.

You know, the longer the time during which positiva acid as the source of AI is exposed to oxygen, the more there will be restrictions on the stabilization of fuseboy acid in the recipe. However, no published data on the stability of fuseboy acid within a certain period of time.

Alternatively, fuseboy acid known use of fusidate sodium in the manufacture of a dermatological medicines for local use. However, they are presented in the form of ointments and creams not. Disadvantages ointments compared to credit the AMI is well known, and for local use, in General, preferable to use lotions, not creams.

Well there are several aspects of the use of fuseboy acid as AI:

it is thermolabile;

- it is available in the formulation of the cream;

is it possible to get out of fusidate sodium by dissolving the latter in the aqueous phase and add to this acid solution, while positiva acid precipitates. However, besieged fuseboy acid is difficult to enter into the cream, firstly, due to the large and uneven size of its particles and, secondly, removing fuseboy acid from a crude sediment layer assumes its drying and further processing, which cause deterioration in the quality of fuseboy acid due to exposure to oxygen;

- stability of the AI in the cream containing fuseboy acid, is unreliable due to thermolability fuseboy acid.

Stabilization of medicines containing fuseboy acid against oxidation includes compliance with the many precautions during its production and storage. They include the following:

- substitution of oxygen in the pharmaceutical containers inert gases such as nitrogen, carbon dioxide, helium, etc.;

- excluding contact of the drug with ions of heavy metals, which are the catalysts for the oxidation;

- keeping the AI at a lower temperature throughout its period of storage before processing.

In practice, this means strict control during manufacture and storage of such AI (usually stored at temperatures between 2° to 8°C in airtight containers during the entire storage period).

Therefore, there is a need to create a cream containing fuseboy acid, which positiva acid would have greater stability during manufacture of cream and which would retain its stability at an acceptable level throughout the storage period.

The objects and advantages of the invention

Thus, one object of this invention is to provide a cream containing fuseboy acid as active pharmaceutical ingredient, but which would have greater stability AI throughout the period.

Summary of the invention

In the invention disclosed dermatological cream containing fuseboy acid, which is formed in situ from fusidate sodium, used as starting material, while fusidate sodium becomes fuseboy acid, in an environment that does not contain oxygen. The cream is proposed in this invention has high storage stability, and particle AI have smaller is d size compared to traditional creams, containing fuseboy acid. Cream, proposed in the present invention contains fuseboy acid as AI, which is formed in situ from fusidate sodium cream base containing acid, a co-solvent, an emulsifier and a waxy product with water, preferably purified water.

Detailed description of the invention

Earlier we discussed the known aspects of the compositions for topical application which contain fuseboy acid and fusidate sodium as the active ingredients. It is now known that:

- Creams containing fuseboy acid, which are manufactured using fusidate of sodium as the source of AI, are not available.

- There are no published data on the stability of fusidate sodium as AI.

- It is believed that fusidate sodium has no more stability as an AI than positiva acid.

With this in mind, it has been unexpectedly discovered that fusidate sodium as the AI is much more stable than positiva acid, and that positiva acid breaks down much faster than fusidate sodium.

There are no published data on the stability of fusidate sodium as AI. The applicant conducted a series of experiments with fusidate sodium in order to assess its stability. From Table 2 we can see that degrades what I fusidate sodium in the temperature range from room temperature up to 45°C ranged from 2.45 per cent to 6 per cent.

In Table 1 and 2 also shows a comparison between the stability of fuseboy acid and fusidate sodium used as the source of AI. The study was conducted using the method of liquid chromatography high pressure developed by the applicant, which, according to the applicant, is an accurate method of determining stability compared with the titration method proposed in British Pharmacopea (BP). This occurs in consequence of the fact that BP method does not distinguish between intact AI and its degraded form.

Stability studies fuseboy acid:

Table 2
The results of stability studies of fusidate sodium (AI) after three months storage by liquid chromatography high pressure and titration method.
No.conditions* initial (%)samples of fusidate sodium (%)reduction (%)comments
titrationliquid chromatography high on the compliance titrationliquid chromatography high pressureAI was analyzed after 3 months
1room temperature (open)98,797,7196,250,992,45
2room temperature (closed)98,8597,67-0,151,03
345°C (open)97,0792,651,636,05
445°C (closed)97,1692,961,545,74
Sample name: fusidate sodium BP
Container: open and closed Petri dish.

In both studies, * denotes the Initial results related to the samples subjected to anal the memory during retrieval of the AI from the provider.

From Tables 1 and 2 we can draw the following conclusions:

- In case for fuseboy acid, there is a loss of about 7.7% for the 3 months of storage at room temperature (open container) and about 11% for 3 months at 45°C (open container).

- In the case of fusidate sodium, there is a loss of about 2.5% for the 3 months of storage at room temperature (open container) and about 6% for 3 months at 45°C (open container).

Thus, these data show that fusidate sodium used as the active ingredient, is more stable than positiva acid.

Applicants investigated the possibility of making the cream rather than the ointment) using fusidate sodium (and not fuseboy acid). Although fusidate sodium is used in dermatological practice, it was impossible to produce creams that use fusidate sodium. This is due to the inherent fusidate sodium alkalinity (pH from 7.5 to 9), which means that it cannot be used in cream form, so all the products are manufactured using fusidate of sodium as the source of the product are ointments. Dermatological cream, which uses fusidate sodium, has the advantage consisting in the fact that fusidate sodium bladiebla stability, than positiva acid, and it allows you to create a recipe of cream, which is much higher than the ointment on quality when applying. Thus, it will fill an existing need in the cream, which would have had better stability than currently available creams containing fuseboy acid.

Thus, the applicant has unexpectedly found that, in order to achieve greater stability of the AI in dermatological cream, as the source of AI at the time of manufacture of the cream is preferable to use fusidate sodium, and not fuseboy acid. The use of fusidate of sodium as the source of the product eliminates the disadvantages associated with the manufacture and storage of existing creams containing fuseboy acid.

The applicant has also found that a cream containing fuseboy acid, manufactured using fusidate of sodium as the source of AI, showed good chemical stability, efficiency and antibacterial activity.

This application discloses a cream containing fuseboy acid (AI), which was manufactured using fusidate of sodium as the source of AI and in which positiva acid is formed in situ in completely devoid of oxygen environment by slow addition of any acid in molecular variance (due to the presence of SOR is storytale) at an intermediate stage, and fucicola acid is recovered in the form of extremely fine dispersion when added to the final cream base, which leads to the formation of fine and homogeneous dispersion of fuseboy acid in the final cream. All these operations are performed in an environment free of atmospheric oxygen. Cream, proposed in the present invention contains fuseboy acid as the AI, which was formed in situ from fusidate sodium cream base containing acid, a co-solvent, an emulsifier and a waxy product with water, preferably purified water.

The active ingredients which can be used in this invention as the source of AI are either acid active substances or their salts, are well known in the field of treatment of primary and secondary bacterial infections. Examples of suitable acid active substances or their salts that may be used is, but not limited by, fusidate sodium.

These acidic active compounds or their salts require component basis to ensure that they can be used in pharmaceutical compositions which include these compounds, since these compounds cannot by themselves be applied directly to human skin due to their krupnodernytsi.

Cream Foundation, according to data from the WMD to the invention, may, in addition, contain an ingredient selected from the group comprising a preservative, a buffering agent, antioxidant, chelating additive and hygroscopic means or any combination of them.

The present invention proposes a new cream that was made with the use of fusidate of sodium as the source material, this cream contains fuseboy acid, which has a high therapeutic efficacy and chemical stability, which is usually greater than the industrial manufactured creams containing fuseboy acid.

Cream containing fuseboy acid, according to this invention, was made in an environment completely devoid of oxygen, injecting an inert gas and vacuum use. Under these conditions, fusidate sodium is converted in situ in fuseboy acid. Cream, proposed in the present invention, is used in the treatment of bacterial skin infections.

The product offered in this invention has a pH of about 3 to 6. On the other hand, industrial manufactured ointments that contain fusidate sodium, are greasy and cosmetically unappealing.

It is important that the active substance has penetrated into the skin for optimal bioeffectives in the skin. Here the important role played by the particle size of the active substance. It is necessary that the active substances the STV was available in fine form for to the product was effective. It also should be achieved in an environment that is safe compatible pH of the skin (pH 4.0 to 6.0). In order to meet these requirements, it is important to choose a suitable transporting substances or co-solvents for dissolving or dispersing the drug.

Analysis of particle size was carried out for the product offered in this invention (product Apex) and for the few examples of industrial manufactured products (samples a, C, D, F, G, and K). Were estimated maximum and minimum particle size and standard deviation, and coefficient of variation. Table 3 shows comparative data.

Table 3
the minimum particle size (µm)the maximum particle size (microns)the average particle size (µm)the standard deviationthe coefficient of variation
this invention (Apex)2,3316,3010,013,9820,397
Andof 7.23 39,5818,099,2510,511
6,0732,6914,116,6920,474

D9,827,5218,48to 4.980,269
Fto 7.9319,9014,824,0330,272
G7,2929,48of 14.256,0650,398
Kof 5.7532,63Ls 16.808,1120,483

The analysis of the distribution of particle size definitely indicates the presence of fuseboy acid in the form of fine particles in the product as proposed in the present invention, the size of which is significantly less than traditional products. Uh what about the can be attributed to the fact that that the immediate product is manufactured using fusidate sodium, using the reaction conversion in situ of fusidate sodium fuseboy acid in fine form. All measured parameters were better than the industrial manufacture of creams containing fuseboy acid. This is another obvious benefit of the product, unveiled here, compared to industrially produced products.

The product offered by the present invention, is effective through the apparent antibacterial activity restored fuseboy acid, which is available in the form of smaller particles than traditional products, and in fine form.

The inventor has selected different co-solvents such as propylene glycol, hexyleneglycol, polyethylene glycol-400 and so on, and dissolved fusidate sodium in one of the above joint solvents, the content of which varied from approximately 5% (in weight ratio) to 40% (in weight ratio), injecting an inert gas in the vacuum and turned it into fuseboy acid in situ by adding an acid such as HCl, H2SO4, HNO3, lactic acid, etc. in respect of approximately 0.005% (in weight ratio) to about 0.5%(in weight ratio) with stirring and received fusicology is islote in a more stable and soluble form, that allowed us to make our final product on cream base, which easily penetrates the skin and makes it highly efficient and highly compatible with the skin due to the fact that it has a pH from about 3.0 to about 6,0.

The stability of the product is confirmed by the stability studies that were performed within 6 months according to the ICH guidelines, and comparison studies of adverse factors, conducted for manufactured at the place of product and samples of industrially produced comparable products.

Experimental data

Experiments to determine the stability of the active ingredients was conducted (see Table 4-14) using the product proposed in this invention, and products, industrial currently produced. The tests were carried out to observe (or measure, respectively) the appearance of the product, the pH value and the quantitative analysis of the active ingredient within a certain period of time. Trials were also conducted to assess the stability when exposed to the product of adverse factors, such as tests in an autoclave and test for oxidative degradation. In addition, a study was carried out in vitro antimicrobial zone of suppression during the period of time. Every gram of product, the proposal is built in this invention and used in the test contained fusidate sodium in an amount necessary for the formation of 2% (in weight ratio) of fuseboy acid in the final product.

The product used in the stability studies and trials in the autoclave and the test for oxidative degradation, contained approximately 10% excess of the AI. The product of this invention, used for research, contained the cream with fuseboy acid, produced using fusidate of sodium as the source material. He was Packed in soft aluminum tube, and each gram of the product contained 20,8 mg of fusidate sodium (according to BP), which is equivalent to 20 mg of fuseboy acid (according to BP). The details of this analysis are comparable industrial products (creams containing fuseboy acid) are presented in Tables 13A and 14, respectively).

Table 5
Measurement of pH, Batch No. ASF-09
Measured parameter: pH
The limits of measured parameter: 3-6
Method of measurement: Digital pH meter
conditions the initial valuethe first monththe second monththe third monthsixth month
40°C 75% relative humidity4,224,214,224,204,19
30°C, 65% relative humidity4,204,214,214,20
25°C 60% relative humidity4,214,214,204,19
thermal Cycling4,22---
freeze-thaw4,21---

Table 6
Quantitative analysis (%), Batch No. ASF-09
Measured parameter: Quantitative analysis (%)
The limits of measured parameter: 90-110%
Method of measurement: the method of liquid chromatography high pressure
conditionsthe initial valuethe first monththe second monththe third monthsixth month
40°C 75% relative humidity108,60108,56108,26108,11108,05
30°C, 65% relative humidity108,53108,36108,26108,11
25°C 60% relative humidity108,59108,45108,39108,26
thermal Cycling107,53---
freeze-thaw108,01---

Table 8
measurement of pH, Batch No. ASF-10
The limits of measured parameter: 3-6
Method of measurement: Digital pH meter
conditionsthe initial valuethe first monththe second monththe third monthsixth month
40°C 75% relative humidity4,234,224,214,204,20
30°C, 65% relative humidity4,214,204,214,21
25°C 60% relative humidity4,20 4,214,214,20
thermal Cycling4,21---
freeze-thaw4,20---

Table 10
Descriptive test, Batch No. ASF-12
Measured parameter: appearance
The best possible values of measured parameter: Homogeneous white to cream-colored viscous cream.
Method of measurement: Observation by naked eyes
conditionsthe initial valuethe first monththe second monththe third monthsixth month
40°C 75% relative humidityg is moeny viscous cream white to cream-coloured homogeneous viscous cream white to cream-colouredhomogeneous viscous cream white to cream-colouredhomogeneous viscous cream white to cream-colouredhomogeneous viscous cream white to cream-coloured
30°C, 65% relative humiditythe same thingthe same thingthe same thingthe same thing
25°C 60% relative humiditythe same thingthe same thingthe same thingthe same thing
thermal Cyclingthe same thing---
freeze-thawthe same thing---

Table 12
The number is n analysis (%), Party No. ASF-12
Measured parameter: Quantitative analysis (%)
The limits of measured parameter: 90-110%
Method of measurement: the method of liquid chromatography high pressure
conditionsthe initial valuethe first monththe second monththe third monthsixth month
40°C 75% relative humidity108,59108,44average 108.41108,36108,10
30°C, 65% relative humidityaverage 108.41108,40108,32108,15
25°C 60% relative humidity108,42108,36108,31108,28
thermal Cycling107,64-- -
freeze-thaw108,11---

When considering Table 4-12 becomes obvious that all items: pH, appearance, and stability, the product offered by the present invention has a high quality.

In table 13 are the key dates for samples A-I, which was taken for analysis from a number of industrial manufactured creams containing fuseboy acid.

Table 13
sample numberdate of manufacturedate of expiration
this invention (apex)Oct 09Sep 11
a sample AndAug 09Jul 11
sampleAug 09Jul 11
sampleJul 09Jun 11
sample Dthe Oia is 09 Jun 11
sample EAug 09Jul 11
sample FAug 09Jul 11
sample GAug 09Jul 11
sample NJul 09Jun 11
the sample IDec 09Nov 11

Table 13-
Reference analysis (%) when tested in the autoclave.
Measured parameter: Quantitative analysis (%)
The limits of measured parameter: 90-110%
Measurement method: Method of liquid chromatography high pressure.
No.product name and detailsAnalysis I (%)Analysis II (%) the average value in the Analysis I and Analysis II (%)
the initial valueAfter the autoclavereduction (%)the initial valueAfter the autoclavereduction (%)
1the invention (Apex)110,47104,615,86110,62104,865,76of 5.81
2A sample And101,8191,7910,02100,9391,659.28 are9,65
3Sample92,69at 83.549,1591,1383,088,058,6

4Sample 110,4798,5611,91110,299,2110,99of 11.45
5Sample D101,394,846,46102,1394,65of 7.486,97
6Sample E100,9994,516,48100,2193,516,706,59
7Sample F96,3384,1512,1895,8885,1210,7611,47
8Sample G104,7593,19to 11.56103,2593,1210,13 10,84
9Sample N101,2688,3512,91100,8687,9812,8812,89
10The sample I101,5887,0614,52100,6188,0112,613.56MHz

Table 14
Quantitative analysis in the test for oxidative degradation.
Measured parameter: Quantitative analysis (%)
The limits of measured parameter: None
Measurement method: Method of liquid chromatography high pressure.
No.product name and detailsAnalysis (%)
the initial value after oxidationdegradation (%)
1the invention (Apex)110,47106,753,72
2A sample And101,8195,636,18
3Sample92,6983,159,54
4Sample110,47101,938,54
5Sample D101,393,258,05
6Sample E100,9995,475,52
7Sample F96,3390,705,63
8Sample G104,75 96,468,29
9Sample N101,2694,53of 6.73
10The sample I101,5888,9212,66

The conclusion from Table 13A. The results of quantitative analysis when tested in an autoclave (121°C, heated for 15 minutes) show that samples of industrially produced cream containing fuseboy acid (№ p/p 2-10) show a more significant decrease in the percentage content of active ingredient compared with the product proposed in the present invention (№ p/p 1).

Conclusions from Table 14. The above results of the quantitative analysis when tested in oxidative degradation (30% solution of hydrogen peroxide was affected in 12 hours) show that different samples present on the market creams containing fuseboy acid (№ p/p 2-10) show significantly greater degradation of the active ingredient (shown as a reduction of AI per cent) compared with the product proposed in the present invention (№ p/p 1).

From the above data it is obvious that the product proposed in this izaberete the AI, is quite stable when stored in ambient conditions and in conditions of high temperature and humidity. Research in the autoclave and studies of oxidative degradation is even more confirmed the stability of this product. This is its main advantage compared to currently available creams with fuseboy acid. The stability of the product, in addition, confirmed the prediction of the shelf life of this recipe by using curve degradation Arrhenius equation using the software Nova-LIMS.

Antimicrobial/antibacterial activity of this product is confirmed by studies of antimicrobial zone of suppression for a given product against Staphylococcus aureus, performed in vitro. Details of these studies are provided below in Table 15.

From the above data it is obvious that this product has an appropriate antimicrobial/antibacterial activity for the treatment of primary and secondary bacterial infections.

In accordance with the preferred implementation of the present invention features a composition for the local treatment of bacterial infections on the skin, this composition contains fuseboy acid formed in situ due to the conversion is usedata sodium, a cream base containing primary and secondary emulsifiers, waxy products, joint solvents, acids and water.

We offer the following proportions of the various components in the preferred embodiment, the:

A. Positiva acid from about 0.1% to 25% in weight ratio, preferably from about 0.5% to 5% in weight ratio, and more preferably about 2% in weight ratio, which was formed in situ from fusidate sodium, the content of which is approximately from 0.1% to 25% in weight ratio, preferably from about 0.5% to 5% in weight ratio, and more preferably about 2,08% in weight ratio, and

C. a cream base containing primary and secondary emulsifiers, waxy products, joint solvents, acids and water, while

- primary and secondary emulsifiers are selected from the group consisting of cetostearyl alcohol, cetomacrogol-1000, Polysorbate-80, Span-80 and the like, in amounts from about 1% to 15% in weight ratio, preferably 15% in terms of weight, even more preferably 14.5% in weight ratio;

- waxy products are selected from the group consisting of white soft paraffin, liquid paraffin, hard paraffin and the like, in amounts from about 5% to 20% in weight from what Oseni, preferably 15% in terms of weight, more than approximately 12.5% in weight ratio;

- joint solvents are selected from the group consisting of propylene glycol, hexyleneglycol, polyethylene glycol-400 and the like, in amounts from about 5% to 40% in weight ratio, preferably 30% in terms of weight, more preferably 25% in weight ratio;

- acids are selected from the group consisting of HCl, H2SO4, HNO3, lactic acid and the like, in amounts of about 0.005% to 0.5% in weight ratio, preferably 0.3% in terms of weight, more preferably 0.25% in weight ratio, and

- water is taken in an amount of from 20% to 75% in weight ratio, preferably from 35% in weight ratio to 50% in weight ratio, more preferably from 40% to 43% in weight ratio, preferably purified water.

In another embodiment of this invention, the product corresponding to the preferred option of perform, in addition, incorporates preservatives, and the preservatives are selected from the group consisting of methylparaben, propylparaben, chlorocresol, potassium sorbate, benzoic acid and the like, in amounts from about 0.05% to 0.5% in weight ratio, preferably 0.3% in terms of weight, more preferably 0.2% in weight relationship is.

In another embodiment of this invention, the product corresponding to the preferred option of perform, in addition, comprises a buffering agent selected from the group consisting of dvuhkamernyi orthophosphoric acid sodium, phosphoric acid, sodium and the like, in amounts from about 0.01% to 1% in weight ratio, preferably 0.5% in terms of weight, more preferably 0.05% in terms of weight.

In another embodiment of this invention, the product corresponding to the preferred option of perform, in addition, incorporates antioxidants selected from the group containing butylhydroxyanisole, butylhydroxytoluene and the like, in the amount of approximately from 0.001% to 5% in weight ratio, preferably 0.1% in terms of weight, more preferably 0.01% in terms of weight.

In another embodiment of this invention, the product corresponding to the preferred option of perform, in addition, incorporates a chelating additive selected from the group consisting of the disodium salt of EDTA and the like, in amounts from about 0.01% to 1% in weight ratio, preferably 0.5% in terms of weight, more preferably 0.1%) weight ratio.

In yet another embodiment, the present invention product is t, the corresponding preferred variant implementation, moreover, is composed of a hygroscopic agent selected from the group consisting of glycerin, sorbitol, propylene glycol and the like, in amounts from about 5% to 40% in weight ratio, preferably 30% in terms of weight, more preferably 25% in terms of weight.

In another embodiment of this invention, the product corresponding to the preferred option of perform, in addition, comprises at least one component selected from the group consisting of buffer additives, preservatives, antioxidants, chelating additives, hygroscopic agent, or any combination of them in appropriate proportions disclosed in the previously described variants of execution.

In yet another embodiment, the present invention discloses a new dermatological cream, in which fusidate sodium is converted in situ in completely devoid of oxygen environment at slow addition of acid in fuseboy acid in the form of a molecular dispersion (due to the joint presence of the solvent) at an intermediate stage, and this positiva acid is recovered in an extremely fine form when adding it to the final cream base, resulting in the final cream is positiva acid in the Orme small homogeneous dispersion; all processes of transformation of fusidate sodium fuseboy acid is carried out preferably in an environment devoid of oxygen.

From the above description should be pretty obvious that this invention includes the following options:

1. A new dermatological cream containing fuseboy acid, which is formed in situ in not containing oxygen environment using fusidate sodium, this cream contains the specified fuseboy acid formed in situ by conversion of fusidate sodium, and a cream base containing at least one ingredient each type: primary and secondary emulsifiers, waxy product, joint solvent, an acid and water, preferably purified water.

2. A new dermatological cream, as described in paragraph 1, which stated positiva acid is present in amount from about 0.1% to 25% in weight ratio, preferably from about 0.5% to 5% in weight ratio, and more preferably about 2% in weight ratio, and in which the number of fusidate sodium used for formation of the in situ fuseboy acid is in the range of from about 0.1% to 25% in weight ratio, preferably from about 0.5% to 5% in terms of weight and the school more preferably approximately 2,08% in weight ratio, and

the specified primary and secondary emulsifier is selected from the group consisting of cetostearyl alcohol, cetomacrogol-1000, Polysorbate-80, Span-80 and the like, either one by one or in any combination, therefore, to form a proportion from about 1% to 15% in weight ratio, preferably 15% in terms of weight and even more preferably 14.5% in terms of weight,

specified waxy product is selected from the group consisting of white soft paraffin, liquid paraffin, hard paraffin and the like, either alone or in any combination, therefore, to form a proportion from about 5% to 20% in weight ratio, preferably 5% in weight ratio, more preferably 12.5% in terms of weight,

this collaborative solvent is selected from a group comprising propylene glycol, hexyleneglycol, polyethylene glycol-400 and the like, either alone or in any combination, therefore, to form a proportion from about 5% to 40% in weight ratio, preferably 30% in terms of weight, and even more preferably 25% in weight ratio,

this acid is selected from the group consisting of acids such as HCl, H2SO4, HNO3, lactic acid and the like, either alone or in any combin, is of so to form a proportion from about 0,005% in weight ratio to 0.5% in weight ratio, preferably 0.3% in terms of weight and even more preferably 0.25% in weight ratio, and

water is taken in an amount of from 20% to 75% in weight ratio, of approximately from 35% in weight ratio to 50%, even more preferably from 40% to 43% in weight ratio, preferably purified water.

3. A new dermatological cream, as it is described in paragraph 2, which further contains a preservative, with the specified preservative is selected from the group consisting of methylparaben, propylparaben, chlorocresol, potassium sorbate, benzoic acid and the like, either alone or in any combination, therefore, to form a proportion from about 0.05% to 0.5% in weight ratio, preferably 0.3% in terms of weight and even more preferably 0.2% in terms of weight.

4. A new dermatological cream, as it is described in paras.2-3, which further contains a buffering agent, such as a buffering agent selected from the group comprising dvuhkamernyi orthophosphoric acid sodium, phosphoric acid, sodium and the like, one or any combination of them in such a way as to form a proportion from about 0.01% to 1% in weight ratio, preferably 0.5% in terms of weight, and even more PR is doctitle - 0.05% in terms of weight.

5. A new dermatological cream, as it is described in paragraph (2 to 4, which further contains an antioxidant, with the specified antioxidant is selected from the group including butylhydroxyanisole, butylhydroxytoluene and the like, either alone or in any combination, therefore, to form a proportion of approximately from 0.001% to 5% in weight ratio, preferably 0.1% in terms of weight, and even more preferably 0.01% in terms of weight.

6. A new dermatological cream, as it is described in paragraph 2-5, which further contains chelating additive, with the specified chelating additive is selected from a group comprising disodium salt of EDTA and the like, either alone or in any combination, therefore, to form a proportion from about 0.01% to 1% in weight ratio, preferably 0.5% in terms of weight, and even more preferably 0.1% in terms of weight.

7. A new dermatological cream, as it is described in paras.2-6 which, in addition, contains a hygroscopic agent, such hygroscopic agent is selected from a group comprising glycerin, sorbitol, propylene glycol and the like, one or any combination of them, therefore, to form a proportion from about 5% to 40% in weight ratio, preferably 30% in weight relationship is, and even more preferably 25% in terms of weight.

8. A new dermatological cream, as it is described in paras.1-7, in which fusidate sodium is converted in situ in completely devoid of oxygen environment at slow addition of acid in fuseboy acid in the form of a molecular dispersion (due to the joint presence of the solvent) at an intermediate stage, and this positiva acid is recovered in an extremely fine form when adding it to the final cream base, resulting in the final cream is positiva acid in the form of a fine and homogeneous dispersion, the operation of turning fusidate sodium fuseboy acid is carried out preferably in an environment devoid of oxygen.

9. A new dermatological cream, as it is described on p. 3, in which the indicated transformation of fusidate sodium fuseboy acid and the subsequent formation of fuseboy acid in fine form in the final cream base is in an environment devoid of oxygen.

10. A new dermatological cream, as it is described on p. 9, which is devoid of oxygen environment contains gaseous environment, formed from an inert gas selected from the group comprising carbon dioxide, nitrogen, helium and the like.

11. A method of treating primary and secondary infections of the skin, while pointed to by the second method involves applying the cream, containing fuseboy acid, which is formed in situ without oxygen environment using fusidate sodium, this cream contains the specified fuseboy acid formed using fusidate sodium and creamy Foundation contains a primary and secondary emulsifiers, waxy products, joint solvents, acids and water.

12. A method of treating primary and secondary infections of the skin, thus this method involves applying the cream, as it is described in paragraph 11, with the specified cream, in addition, contains any substance from the group comprising a buffering agent, preservative, antioxidant, chelating additive and hygroscopic agent, or any combination thereof.

13. A method of treating primary and secondary infections of the skin, thus this method involves applying the cream, as it is described in paragraph 12, in which positiva acid is present in amount from about 0.1% to 25% in weight ratio, preferably from about 0.5% to 5% in weight ratio, and more preferably about 2% in weight ratio, and in which the number of fusidate sodium used for formation of the in situ fuseboy acid is in the range of about from 0.1% to 25% in weight ratio, preferably about 0.5% up to 5% in weight ratio, and in the preferred embodiment, OK the lo of 2.08% in weight ratio,

these primary and secondary emulsifiers are selected from the group comprising cetostearyl alcohol, cetomacrogol-1000, Polysorbate-80, Span-80 and the like, either one by one or in any combination, therefore, to form a proportion from about 1% to 15% in weight ratio, preferably 15% in terms of weight and even more preferably 14.5% in terms of weight,

specified waxy product is selected from the group consisting of white soft paraffin, liquid paraffin, hard paraffin and the like, either alone or in any combination, therefore, to form a proportion from about 5% to 20% in weight ratio, preferably 15% in weight ratio, more preferably 12.5% in terms of weight,

this collaborative solvent is selected from a group comprising propylene glycol, hexyleneglycol, polyethylene glycol-400 and the like, either alone or in any combination, therefore, to form a proportion from about 5% to 40% in weight ratio, preferably 30% in terms of weight, and even more preferably 25% in weight ratio,

this acid is selected from the group consisting of acids such as HCl, H2SO4, HNO3, lactic acid and the like, either alone or in any combination, thereby to form the PCC is a resource center approximately 0.005% in weight ratio to 0.5% in weight ratio, preferably - 0.3% in terms of weight and even more preferably 0.25% in weight ratio,

the specified preservative is selected from the group consisting of methylparaben, propylparaben, chlorocresol, potassium sorbate, benzoic acid and the like, either alone or in any combination, therefore, to form a proportion from about 0.05% to 0.5% in weight ratio, preferably 0.3% in terms of weight and even more preferably 0.2% in weight ratio,

the specified buffer substance is selected from the group comprising dvuhkamernyi orthophosphoric acid sodium, phosphoric acid, sodium and the like, one or any combination of them in such a way as to form a proportion from about 0.01% to 1% in weight ratio, preferably 0.5% in terms of weight, and even more preferably 0.05% in weight ratio,

specified the antioxidant is selected from the group including butylhydroxyanisole, butylhydroxytoluene and the like, either alone or in any combination, therefore, to form a proportion of approximately from 0.001% to 5% in weight ratio, preferably 0.1% in terms of weight, and even more preferably 0.01% in weight ratio,

specified chelating additive is selected from a group comprising disodium salt of EDTA and the like, either alone or in any com is inali thus, to form a proportion from about 0.01% to 1% in weight ratio, preferably 0.5% in terms of weight, and even more preferably 0.1% in weight ratio, and

specified hygroscopic agent is selected from a group comprising glycerin, sorbitol, propylene glycol and the like, one or any combination of them, therefore, to form a proportion from about 5% to 40% in weight ratio, preferably 30% in terms of weight, and even more preferably 25% in weight ratio, and

water is taken in an amount of from 20% to 75% in weight ratio, of approximately from 35% in weight ratio to 50%, even more preferably from 40% to 43% in weight ratio, preferably purified water.

From the above description should be pretty obvious that this invention has the following differences and advantages compared to industrially produced similar products:

- Offer the product was manufactured using fusidate sodium, which is more stable than positiva acid.

He contains as an active ingredient fuseboy acid with a higher quality and stability.

- Positiva acid in this invention degrades slower than traditional products.

- The level of stability of fusedav the th acid in this invention remains within acceptable boundaries for the entire retention period.- The particle size of fuseboy acid smaller and the overall distribution of particles in the cream are better than traditional products, which provides greater dermatological efficiency.

Although the above description contains much specificity, this should not be construed as limiting the scope of the invention, but only as an illustrated example of the preferred option it is running. You need to understand that based on the above disclosure, it is possible to make various modifications and variations which will not go beyond the nature and scope of this invention. Therefore, the scope of this invention should be determined not illustrated variants of execution, but the accompanying paragraphs patent claims and their legal equivalents.

1. Cream for the treatment of infections of the skin, containing fuseboy acid, which is formed in situ in not containing oxygen environment using fusidate sodium, this cream contains the specified fuseboy acid formed in situ by conversion of fusidate sodium slow addition of acid, the particle size of the active substance from 2,33 μm to 16.3 microns and a cream base containing at least one ingredient each type: primary and secondary emulsifiers are selected from the group consisting of cetostearyl alcohol, cetomacrogol-1000, Polysorbate-80, Span-80; paraffin as boskoop the testing of the product; joint solvent selected from the group comprising propylene glycol, hexyleneglycol and polyethylene glycol-400; nitric acid or lactic acid and water.

2. Cream under item 1, in which the specified positiva acid is present in an amount of from 0.1% to 25% in weight ratio, preferably from 0.5% to 5% in terms of weight, and still more preferably 2% in weight ratio, and in which the number of fusidate sodium used for formation of the in situ fuseboy acid is in the range from 0.1% to 25% in weight ratio, preferably from 0.5% to 5% in terms of weight and even more preferably of 2.08% in weight ratio, and
the specified primary and secondary emulsifier is selected in such a way as to form a proportion from about 1% to 15% in weight ratio, preferably 15% in terms of weight and even more preferably 14.5% in terms of weight,
specified waxy product is selected from the group consisting of white soft paraffin, liquid paraffin, solid paraffin thus, to form a proportion from 5% to 20% in weight ratio, preferably 15% in weight ratio, more preferably 12.5% in terms of weight,
this collaborative solvent is selected in such a way as to form a proportion from 5% to 40% in weight ratio, preferably 30% in weight against the AI, and even more preferably 25% in terms of weight,
this acid is chosen in such a way as to form a proportion of 0.005% in weight ratio to 0.5% in weight ratio, preferably 0.3% in terms of weight and even more preferably 0.25% in weight ratio, and
water is taken in an amount of from 20% to 75% in weight ratio, preferably from 35% in weight ratio to 50%, even more preferably from 40% to 43% in weight ratio, preferably purified water.

3. Cream under item 1, which further contains a preservative, selected from the group consisting of methylparaben, propylparaben, chlorocresol, potassium sorbate, benzoic acid, either alone or in combination in such a way as to form a proportion from 0.05% to 0.5% in weight ratio, preferably 0.3% in terms of weight and even more preferably 0.2% in terms of weight.

4. Cream under item 1, which further contains a buffering agent, such as a buffering agent selected from the group comprising dvuhkamernyi orthophosphoric acid sodium, phosphoric acid sodium, either one or in combination in such a way as to form a proportion from 0.01% to 1% in weight ratio, preferably 0.5% in terms of weight and even more preferably 0.05% in terms of weight.

5. Cream under item 1, which further contains an antioxidant, with specified anti oxidant is selected from the group includes butylhydroxyanisole, butylhydroxytoluene, either alone, or in combination in such a way as to form a proportion from about 0.001% to 5% in weight ratio, preferably 0.1% in terms of weight and even more preferably 0.01% in terms of weight.

6. Cream under item 1, which further contains chelating additive disodium salt EDTA thus, to form a proportion from 0.01% to 1% in weight ratio, preferably 0.5% in terms of weight and even more preferably 0.1% in terms of weight.

7. Cream under item 1, which further contains hygroscopic agent, such hygroscopic agent is selected from a group comprising glycerin, sorbitol, propylene glycol, one or in combination, thus, to form a proportion from 5% to 40% in weight ratio, preferably 30% in terms of weight and even more preferably 25% in terms of weight.

8. Cream on PP.1-7, in which fusidate sodium becomes fuseboy acid in the form of a molecular dispersion in the intermediate stage, and this positiva acid is recovered in fine form when adding it to the final cream base, resulting in the final cream is positiva acid in the form of a fine and homogeneous dispersion.

9. Cream under item 1, which is devoid of oxygen environment will win a gaseous environment, formed from an inert gas selected from the group comprising carbon dioxide, nitrogen and helium.

10. A method of treating primary and secondary infections of the skin, which comprises applying cream on p. 1.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine and concerns a pneumococcal vaccine containing saccharide of 4, 6B, 9V, 14, 18C, 19F and 23F serotypes, separately conjugated with CRM197, and at least one Toll-like receptor-9 (TLR-9) agonist as an adjuvant, wherein the above Toll-like receptor-9 agonist represents CpG-oligonucleotide. Also, the group of inventions concerns using the pneumococcal vaccine for preparing the therapeutic agent for preventing or treating diseases caused by S.pneumoniae; a method for individual's immunisation against the diseases caused by S.pneumoniae infection, involving administering the immunoprotective dose of the vaccine into the above individual.

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45 cl, 9 dwg, 4 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: invention represents an antimicrobial agent for preventing an implant-associated infection containing gentamicin sulphate 0.96 g, dioxidine 1.0 g, medium-molecular-weight medical collidone (molecular weight 30000D) 10.0 g, distilled water up to 100.0 ml.

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2 cl, 1 ex, 3 tbl

FIELD: medicine.

SUBSTANCE: agent possessing the anti-inflammatory, antipyretic and antimicrobial action representing a dry extract of drug hedge hyssop leaves and blossom by grinding them, extracting in 96% alcohol on a water bath to a boil, and boiling, evaporating, diluting the evaporated residue by distilled water first, adding chloroform then, cooling to a room temperature and centrifuging, separating a water fraction and drying it in the certain environment.

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5 dwg, 5 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and represents a composition possessing the antioxidant and antibacterial activity and containing lithium ascorbate, differing by the fact that it additionally contains lithium benzoate in the following proportions, wt %: lithium ascorbate - 50; lithium benzoate - 50.

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1 ex, 2 tbl

FIELD: medicine.

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1 dwg, 2 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the pharmaceutical industry, namely to a method of obtaining a preparation, possessing an antimicrobial activity. The method of obtaining the preparation, possessing he antimicrobial activity, where an aboveground part of freshly harvested bear leek (Allium ursinum L.) or victory onion (Allium victoriale L.) is crushed to a paste-like state, poured with ethyl alcohol, infused tree times, under certain conditions, after each extraction the extracts are poured off, the obtained extracts are combined.

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2 cl, 1 tbl, 6 ex

FIELD: medicine.

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4 cl, 2 tbl, 11 ex

Antimicrobial gels // 2535013

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to medicine, particularly to aspects covering antimicrobial compositions, and described antimicrobial compositions, antimicrobial silicone gel based on the above antimicrobial composition, a wound dressing and methods for preparing them. Among other things, the antimicrobial compositions contain at least one alkenyl- and/or alkynyl-substituted polysiloxane, at least one polysiloxane containing silicone-linked hydrogen atoms, and at least one hydroxylation catalyst, at least one hydrophilic ingredient, at least one silver salt.

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19 cl, 5 dwg, 8 ex, 6 tbl

FIELD: veterinary science.

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1 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: group of inventions refers to veterinary science and aims at treating subclinical mastitis in cows. A preparation and a method for using it are declared. The preparation contains silver nanoparticles stabilised by submicrone titanium dioxide particles, poly-N-vinylpyrrolidone-2, and water in the following proportions, wt %: silver nanoparticles having a size of 200-300 nm 2.0×10-3, titanium dioxide particles having a size of 2-4 mcm 60.0×10-3, poly-N-vinylpyrrolidone-2 10.0, water - the rest up to 100.0. The method involves intracisternal introduction of the declared drug preparation in a dose of 10.0 ml twice a day for 2-4 days.

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2 cl, 4 dwg, 7 tbl, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and represents a gel biologically active composition for topical application containing chitosan hydrochloride in an amount of 10-20 wt %, an organic acid in an amount of 1-10 wt %, distilled water - the rest. The above organic acid is specified in acetic, ascorbic, glycolic, lactic, citric or succinic acids.

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11 ex, 11 tbl, 2 dwg

FIELD: veterinary science.

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1 ex

FIELD: chemistry.

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4 cl, 5 dwg, 31 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the pharmaceutical industry and represents a local pharmaceutical composition for treating rosacea containing at least 0.02% berberine or a biologically equivalent berberine analogue, such as palmatine, and an ingredient specified in a group consisting of water, methanol, ethanol and dimethylsulphoxide, wherein berberine or the biologically equivalent berberine analogue represents the major pharmaceutically active ingredient.

EFFECT: invention provides extending the range of products for treating rosacea.

4 cl, 6 ex, 2 dwg

FIELD: medicine.

SUBSTANCE: group of inventions refers to medicine, namely to dermatology, and can be used for treating such diseases, as rosacea, psoriasis, topic dermatitis or acne. That is ensured by a local application on an individual's skin area of a topical composition, which can be an ingredient of a kit and contains a therapeutically effective amount of an α2-adrenergic receptor agonist, wherein the α2-adrenergic receptor agonist is specified in a group consisting of: a compound of formula (Ia) wherein each of R1, R2 and R3 independently means hydrogen, halogen, (C1-C8)alkyl or alkoxy; each of R4 and R5 independently means hydrogen, (C1-C8)alkyl or alkoxy; each of R6 and R7 independently means hydrogen, nitro, (C1-C8)alkyl or alkoxy; alkoxy is specified in methoxy, ethoxy, n-propoxy, sec-butoxy, tret-butoxy, n-hexyloxy; and a therapeutically effective amount of the non-steroid anti-inflammatory agent diclofenac and a pharmaceutically acceptable carrier, wherein the skin area is subject to or can be injured by an inflammatory skin disease or a symptom related to the above disease. The α2-adrenergic receptor agonist can be presented by, e.g. brimonidine.

EFFECT: ensuring the synergetic effect when using the declared combination which shows the synergetic effect by improving the anti-inflammatory action of diclofenac that leads to the complete relief of any symptoms of the inflammatory disease.

21 cl, 3 ex, 6 tbl, 2 dwg

FIELD: medicine.

SUBSTANCE: topical cosmetic composition effective for stimulating each of SIRT1, Gadd45b and SOD2, which contains a senna alata leaves extract, a great morinda leaves extract and a melon flesh extract taken in certain proportions. A method for the protection against or recovery of an oxidative injury involving administering the topical composition containing the senna alata leaves extract, the great morinda leaves extract and the melon flesh extract taken in certain proportions. The topical cosmetic or dermatological composition for stimulating each of SIRT1, Gadd45b and SOD2. Using the above composition for producing a drug preparation for treating the oxidative injury.

EFFECT: composition is effective for stimulating each of SIRT1, Gadd45b and SOD2.

8 cl, 1 dwg, 1 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of obtaining a polymer conjugate of an indolocarbazole compound of formula (I), where R1, R2, R3, W1 and W2 represent hydrogen, X represents methoxy-polyethyleneglycol. The method includes the interaction of a polymer compound of formula (II) with an indolocarbazole compound of formula (III), where Y stands for a methoxygroup. The nvention also relates to a polymer conjugate of formula (I), a pharmaceutical composition, containing the conjugate of formula (I) as an active ingredient, and to the application of the polymer conjugate of formula (I).

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48 cl, 7 dwg, 7 tbl, 15 ex

FIELD: pharmacology.

SUBSTANCE: method involves preparing a liquid composition containing a pharmaceutical active ingredient, a mixture of solvents containing water, isopropanol in an amount of 5 wt % to 20 wt % and propylene glycol in an amount of 2 wt % to 25 wt %, and a phospholipid foaming agent in an amount of 2 wt % to 25 wt %, foaming the liquid composition mechanically with no propellant used, and measuring the foam volume and stability. That is followed by transforming the nature and/or changing the concentration of the pharmaceutically active ingredient and/or the phospholipid foaming agent and/or changing the concentration of one of the solvents to produce 250 ml of the liquid composition. The above liquid composition is expected to produce foam in the volume of 400 ml and with the stability so that 50% of an initial foam volume is observed so far after the 10-minute hold-up and measured by the standard SITA procedure. The invention also relates to a composition applicable for topical use and prepared by the method described above.

EFFECT: preparing the composition presented by the stable foam.

22 cl, 18 dwg, 1 tbl, 18 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula I: cis-COOR-XCH-(CH2)a-CH=CH-(CH2)b-CH3, wherein (a) and (b) can take any value from 0 to 14, (X) is specified in: OH, NH2, CH3, F, F3C, HS, O-CH3, PO4(CH2-CH3)2 and CH3COO, and (R) represents sodium (Na) applicable for preventing and/or treating obesity, hypertension and/or cancer. Also, the invention refers to using the compounds of formula I for preparing a pharmaceutical and/or nutrient composition, to the pharmaceutical and/or nutrient composition based on the compounds of formula I, to a cosmetic, non-therapeutic method for improving skin manifestations and to a method for preventing and/or treating the diseases in humans and animals with using the compounds of formula I.

EFFECT: preparing the new compounds.

18 cl, 22 dwg, 5 tbl, 9 ex

FIELD: medicine, pharmaceutics.

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EFFECT: what is shown is the synergetic effect of the combination in treating rosacea and eliminating the withdrawal effect usually observed at the end of treatment with alpha-2 adrenergic receptor agonists.

20 cl, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to medicine. Described is a composition for the transdermal introduction of medications (M) into a human and animal organism, including cases of urgent drug treatment and prevention of acute pathological conditions. The composition consists of a solution of one or several M in a mixture of at least two solvents: dialkylamide of lower carboxylic acid and (or) alkylpyrrolidone and monoterpenes and (or) monoterpenoids. The total volume concentration of N,N-dialkylamides of lower carboxylic acids or N-alkylpyrrolidones constitutes from 1% to 99% of the mixture volume.

EFFECT: composition makes it possible to realise urgent drug treatment and prevention of acute pathological conditions of a human and animal organism by a simple in implementation, safe and cheap method.

12 cl, 6 dwg, 4 ex

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