Antimicrobial composition

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine. An antimicrobial composition contains chlorhexidine and pentane-1,5-diol, wherein the amount of chlorhexidine makes 0.000001 to 5 wt %, while the amount of pentane-1,5-diol makes 1 to 75 wt %. The composition is applicable for local administration; it contains a carrier and a gelling material.

EFFECT: group of inventions enables applying the composition for non-therapeutic disinfection, in treating skin infections.

 

The SCOPE of the INVENTION

Embodiments of the present invention relates to antimicrobial compositions containing chlorhexidine and pentane-1,5-diol and, optionally, to the use of such compositions for combating microorganisms.

PRIOR art

With microorganisms can be treated in different ways depending on the reasons against them. The approach differs depending on whether the purpose of preventing the growth of microorganisms, inhibition of further growth or reduction and elimination of the microorganism. In addition, the approach differs depending on where the microorganism, such as, for example, in a liquid, on the surface, inside the body of a mammal, etc.

In the US 2004/0191274 A1 discloses compositions for topical application, which can be used as an antiseptic and/or disinfectant. The disclosed composition for topical application comprises at least one C1-C4 alcohol; at least one antimicrobial agent such as chlorhexidine; and at least one emollient substance, such as polyethylene glycol.

CN 1130020, Tawil, G.G. et al Alexandria Journal of Pharmaceutical Sciences, 1988, 2 (1), 58-60 and Frank M. von et al Pharmaceutische Industrie, 1991, 53 (5) 512-516, all reveal the combination of chlorhexidine and propylene glycol. Frank M. von et al concluded that cannot be detected sinner the AI between chlorhexidine and propylene glycol in combination. On the other hand, previous data obtained Tawil, G.G. et al suggest that propylene glycol should enhance the bactericidal effect of chlorhexidine. However, Tawil, G.G. et al do not provide data on propylene glycol, tested separately. In JP 2003267862 disclosed the combination of chlorhexidine and 1,3-butanediol.

In WO 07/063065 disclosed the use of a composition containing pentane-1,5-diol, to reduce and/or eliminate odor from a mammal, such as the smell of urine, menses, feces, fluids of feet ulcers, bedsores, blood and sweat. In addition, in WO 07/063065 disclosed absorbent product containing pentane-1,5-diol, to reduce and/or eliminate odor from a mammal, such as the smell of urine, menses, feces, fluids of feet ulcers, bedsores, blood and sweat.

There are different compositions and compounds are known to have antibacterial properties.

One example of compounds, which is known that it has antibacterial properties, is propane-1,2-diol (propylene glycol), which is a diol, are widely used to control microorganisms in dermatology. Pentane-1,5-diol was also used in dermatology to combat microorganisms, although not as widely as propylene glycol.

According to WO 04/112765 antibacterial action pentane-1,5-diol, as I believe, sec which enables and other low molecular weight aliphatic diols. In addition, it is disclosed that the use of pentane-1,5-diol has activity against multidrug-resistant strains of bacteria.

Chlorhexidine is a chemical antiseptic. He is as bactericidal against gram-positive, and gram-negative microorganisms. In addition, it is bacteriostatic. It is assumed that the mechanism of action is the destruction of the membrane, but not inactivation of the ATPase, as previously thought. Chlorhexidine is used for General cleansing of the skin, such as surgical scrubs for preoperative skin preparation. He has a greater duration of action and low toxicity. Reported skin sensitivity to chlorhexidine. Also Chlorhexidine can be neurotoxic in high concentrations, which is why it would be useful to reduce the level of chlorhexidine, along with the fact that continued to be its effect.

The MDR bacteria to antibiotics is becoming more and more common. Today in the health sector around the world is growing concern about the future use of traditional antimicrobial agents. For the manufacture of effective antimicrobial agents should be used alternative methods and approaches.

Accordingly, there is a growing m the medical need to identify new antimicrobial compositions which can be effectively used for inactivation of microorganisms. Specifically, there is a growing list of microorganisms, such as bacteria, viruses and fungi that become resistant to antibiotics. In addition, there is a growing population of individuals becoming allegehny against a number of antibiotics or preservative components used in the preparations of antibiotics, which leads to the need for new compositions that can be used as alternatives to traditional technologies.

In addition to the search for new antibiotics, it would also be highly desirable to identify novel synergistic mixture of known antimicrobial compounds. Some known antibiotics used doses may cause unwanted side effects when introduced separately.

SUMMARY of the INVENTION

Accordingly, the present invention seeks to mitigate, reduce, avoid or eliminate one or more than one defined above disadvantages by providing a composition containing from 0.000001 to 5% by mass. chlorhexidine and 1 to 75% of the mass. pentane-1,5-diol. In addition, different embodiments of the present invention relate to the use of a composition containing chlorhexidine and diol for inactivation of microorganisms selected from the group consisting of g is polozhitelnyh and gram-negative bacteria, fungi, including yeast, fungi and dermatophytes, and viruses, especially Staphylococcus aureus and P. acnes.

Useful features of the invention are defined in dependent claims.

Detailed description of illustrative embodiments of the

In the context of the present description and the attached formula assumes that the "C3-Salkantay" means an organic compound containing a linear or branched saturated hydrocarbon with 3-8 carbon atoms, which has two hydroxyl groups attached to different carbon atoms. Examples of such C3-Calendarof include, but are not limited to, propane-1,2-diol, propane-1,3-diol, butane-1,2-diol, butane - 1,3-diol, butane-1,4-diol, butane-2,3-diol, 2-methylpropane-1,2-diol, 2-methylpropane-1,3-diol, 2-hydroxymethyl-1-propanol, pentane-1,2-diol, pentane-2,3-diol, 2-hydroxymethyl-1-butanol, 2-methylbutane-1,2-diol, 3-methylbutane-1,2-diol, 2-methylbutane-1,3-diol, 3-methylbutane-1,3-diol, 2-methylbutane-1,4-diol, hexane-1,2-diol, hexane-1,6-diol, 2-methylpentane-1,5-diol, 3-methylpentane-1,5-diol, 2-methyl-2,4-pentane, heptane-1,7-diol, heptane-1,2-diol, octane-1,2-diol and octane-1,8-diol.

In the context of the present description and the attached formula assumes that the chlorhexidine includes different forms of chlorhexidine. Such forms include, but are not limited to, chlorhexidine in its free form, salts of chlorhexidine, such as Digi rochloride, the diacetate or D-digluconate, solvate chlorhexidine and solvated salt of chlorhexidine.

One embodiment of the present invention relates to compositions, such as pharmaceutical composition comprising chlorhexidine and C3-Salkantay, such as C3-Sdil. In one particular embodiment of this C3-Salkantay selected from pentane-1,5-diol, propane-1,2-diol, butane-1,3-diol, pentane-1,2-diol, hexane-1,2-diol, hexane-1,6-diol and 2-methylpentan-2,4-diol. In one other specific embodiment of this C3-Salkantay selected from propane-1,2-diol and pentane-1,5-diol.

In yet another embodiment according to the examples below, C3-Salkantay is a pentane-1,5-diol.

According to the present invention provided that the synergistic antimicrobial effect is achieved when combining chlorhexidine with C3-Selenderom, such as pentane-1,5-diol. Thus, it was envisaged that the composition containing chlorhexidine, and C3-Salkantay, such as pentane-1,5-diol, has a stronger antimicrobial effect than compositions containing the same concentration of either chlorhexidine or C3-Calandil, such as pentane-1,5-diol.

Specifically, a synergistic effect between chlorhexidine and pentane-1,5-diola shown in the examples below. Although WO 07/063065 reveals that the pentane-1,5-diol, using DL is reduce odor from a mammal, can be combined with an antiseptic agent, he says nothing about any possible synergistic effect. In addition, WO 07/063065 says nothing about what the concentrations of these components are suitable for use in pharmaceutical compositions. According to WO 07/063065 you should use at least 0.1% of the mass. pentane-1,5-diol. However, as here disclosed, this concentration is too low for it to have any synergistic effect when combined with chlorhexidine.

However, it is possible that a synergistic effect is also achieved when combining chlorhexidine and C3-Calandil, non-pentane-1,5-diol, but pentane-1,5-diol is preferred, as it is well known in the preferred Toxicological profile, low risk in relation to sensitivity and irritation of the skin. Thanks to a synergistic antimicrobial effect, you can use less of each component and still get the desired effect. In addition, thanks to the use of smaller amounts of each component, each component may cause fewer side effects and less severe side effects than when used separately. Composition containing chlorhexidine and pentane-1,5-diol, is more effective against microorganisms, che the composition, containing only one active component.

Without being bound by any theory, it can be assumed that the mechanism of action of chlorhexidine, i.e. the destruction of the lipid membrane, supported characteristic hydrophobicity C3-Calendarof. In particular hydrophobicity pentane-1,5-diol is largely appropriate in this regard. In addition, the solubilizing properties of C3-Calendarof can be important in this context. Alternatively, the antimicrobial effect of C3-Calendarof improves the simultaneous destruction of the lipid membrane, caused by chlorhexidine. Another theory is that the mechanism of action of antimicrobial effect of C3-Calendarof consists in dissolving the lipid membrane, which results in improving the ability of chlorhexidine to destroy the specified lipid membrane, and Vice versa. Possible solvent effect and hydrophobicity pentane-1,5-diol promote chlorhexidine way that maximizes the synergistic effect between them.

Pharmaceutical composition comprising chlorhexidine and pentane-1,5-diol, can be used in therapy. When used in therapy can be entered locally. Such input topical composition can be used for treatment of various infections, such as infections affecting the skin or mucous membranes. Examples of the same, the skin infections include impetigo, secondarily infected atopic dermatitis and other dermatoses with secondary infection. Chlorhexidine and pentane-1,5-diol can also be used to treat fungal infections of the skin and mucous membranes, such as athlete's foot, trichophytosis smooth skin, dermatophytic onychomycosis, Candida infections of the skin and mucous membranes, etc. and viral infections, such as infection by a herpes virus (e.g labial herpes), papilloma and poxvirus skin or mucous membranes.

Pharmaceutical composition comprising chlorhexidine and pentane-1,5-diol, also can be used for inactivation of microorganisms selected from the group consisting of gram-positive and gram-negative bacteria, fungi, including yeast, fungi and dermatophytes, and virus. Examples of such microorganisms include, but are not limited to, Staphylococcus aureus, P. acnes, Streptococci, gram-negative bacilli, Candida albicans, Candida glabrata, Malassezia, mould fungus Aspergillus fumigatus and the dermatophytes Trichophyton rubrum, T. mentagrophytes, Epidermophyton floccusum, Microsporum canis, the human papilloma virus, herpes virus and poxvirus. It was shown that the composition comprising chlorhexidine and pentane-1,5-diol is particularly effective when exposed to Staphylococcus aureus and P. acnes, that is, destroy, control, or prevention of Staphylococcus aureus and P. acnes, as disclosed in the examples below.

Songs which I for local injection may take the form of or be included in the liquid, semi-solid or solid disinfectant, bacteriostatic or bactericidal solution, lotion, cream, soap, shampoo, ointment, paste, wet towel, sanitary ware, plaster, diaper or similar protective device for personal hygiene.

If it is intended for application to the skin or mucous membranes, the composition according to embodiments of the invention may contain one or more agents to control the tone or wetting agents such as sodium chloride, urea and lactic acid, water-absorbing agents, dyes, such as calcium carbonate and zinc oxide, and flavoring substances, such as essential oil. The composition according to the invention may also contain cationic, neutral or anionic detergent, in particular a salt of fatty acid.

Preferably, the composition comprising chlorhexidine and C3-Salkantay, and preferably pentane-1,5-diol, also contains the media. The carrier may be aqueous media or lipid carrier, which may optionally contain a thickener. Such thickeners may be selected from cellulose derivatives, in particular methylcellulose, hydroxymethylcellulose, hydroxyethylmethylcellulose. According to an additional embodiment of the invention, the medium contains a salt of fatty acid.

Another embodiment of the invention, apply the to pharmaceutical compositions, as disclosed above, which further include one or more than one pharmaceutically acceptable adjuvant or excipient. Such pharmaceutical compositions can be obtained by a method known in this field, and they are sufficiently stable during storage and suitable for administration to humans and animals.

Pharmaceutical composition, as here disclosed, is subject to local introduction, may take the form of ointments, lotions, pastes, creams, gels, talc, sprays, solutions and emulsions, as easily understood by a person skilled in the art. Such ointments, lotions, creams and gels may contain excipients such as animal and vegetable fats, waxes, paraffins, starch, tragacanth gum, cellulose derivatives, polyethylene glycols, silicones, bentonites, silicic acid, talc and zinc oxide or mixtures of these substances. Talc and sprays can contain excipients, such as lactose, talc, silicic acid, aluminum hydroxide, calcium silicate and polyamide powder or mixtures thereof. Sprays can also contain propellants such as chlorofluorocarbons. Solutions and emulsions can contain excipients, such as solvents, solubilizing agents and emulsifiers, such as water, ethyl alcohol, isopropyl alcohol, ethylcarbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene alcohol, di is malformed, oils, such as cottonseed oil, peanut oil, germ oil corn, olive oil, castor oil and sesame oil, glycerol, glycerolphosphate, tetrahydrofurfuryl alcohol, polyethylene glycols and esters of fatty acids, such as sorbitan, or mixtures thereof.

Pharmaceutical composition, as disclosed here, you can enter the patient in a pharmaceutically effective dose. By "pharmaceutically effective dose" means a dose that is sufficient to obtain the desired effects in relation to the condition for which it is injected. The exact dose depends on the activity of the compound, the route of administration, nature and severity of the disorder, age and body weight of the patient, and may be you need a different dose. The dose can be performed as a single introduction in the form of a single unit dose, or several smaller dose units or multiple introductions divided doses at intervals of time.

The term "patient" for the purposes of the present invention includes both human and other mammal. Thus, these methods are applicable to both human therapy and veterinary applications.

One additional embodiment of the present invention relates to compositions, such as pharmaceutical composition comprising at least 0,000001% of the mass, as in the example, at least 0,00005% of the mass. chlorhexidine and at least 1% of the mass. C3-Calandil, such as pentane-1,5-diol.

Another embodiment of the present invention relates to compositions, such as pharmaceutical composition comprising from 0.000001% of the mass. up to 5 wt. -%, as for example, from 0,00005% of the mass. up to 5% of the mass. or from 0,00005% of the mass. up to 1% of the mass. chlorhexidine and from 1 to 75 wt. -%, as for example, from 1 to 25 wt. -%, from 2 to 15% wt. or from 3 to 15% of the mass. C3-Calandil, such as pentane-1,5-diol.

Another embodiment of the present invention relates to compositions, such as pharmaceutical composition comprising at least 0,00001% of the mass. chlorhexidine and at least 3% of the mass. pentane-1,5-diol. Despite the fact that it is possible to use lower concentrations of the antimicrobial effect is more pronounced at these or at higher concentrations.

Another embodiment of the present invention relates to compositions, such as pharmaceutical composition containing at least 0.0001% per masschelein and at least 5% of the mass. pentane-1,5-diol.

Since higher concentrations may increase the risks of side effects, another embodiment of the present invention relates to compositions, such as pharmaceutical composition comprising from 0.0001 to 5 wt. -%, as for example, from 0.001 to 2.5% of the mass. chlorhexidine and from 3 to 25 wt. -%, as for example, the 5 to 15% of the mass. pentane-1,5-diol.

Another embodiment of the present invention relates to pharmaceutical compositions containing at least 0.001% of the mass. chlorhexidine and C3-Salkantay, such as pentane-1,5-diol.

Another embodiment of the present invention relates to pharmaceutical compositions containing chlorhexidine and at least 2% of the mass. C3-Calandil, such as pentane-1,5-diol.

Another embodiment of the present invention relates to pharmaceutical compositions containing chlorhexidine and at least 5% of the mass. C3-C8 arcangioli, such as pentane-1,5-diol.

When combined together chlorhexidine and pentane-1,5-diol show synergistic antibacterial effects, as shown in the examples below. These synergistic effects allow the use of smaller amounts of the respective compounds at the same time obtaining the desired effect. The combination of chlorhexidine and pentane-1,5-diol is effective in preventing the growth of various microorganisms. Such microorganisms include bacteria, fungi and viruses. Such bacteria include, but are not limited to, S. aureus and P. acnes.

Similarly, chlorhexidine, the composition comprising chlorhexidine and C3-Salkantay, can also be used for General cleansing of the skin, such as surgical scrubs pre-processing is expected. Disinfection is achieved by applying such a composition will be more effective than disinfection when using only one of chlorhexidine. In addition, well-known water-binding effect of the diols makes them excellent moisturizers of the skin and, consequently, will make it less rude when applied to the skin.

In addition, the composition comprising chlorhexidine and C3-Salkantay, can be used with other types of disinfection and cleaning. Without limitation, such disinfection may include the treatment of various surfaces, such as floors, walls, bench tops, surfaces, benches, supplementary boards sliding tables and surgical instruments. Such disinfection can also be combined with autoclaving, or they may even replace it. In one such embodiment include disinfection disinfection of the skin, but another embodiment, related to disinfection, disinfection eliminates parts of the body of man or animal. Such disinfection, excluding disinfection of body parts of a human or animal, should be distinguished from therapeutic method.

In the embodiment where the composition comprising chlorhexidine and C3-Salkantay, is used for disinfection and/or cleaning the surface, and not part of the body of man or animal, the content of C3-Calandil can be 1-95 wt. -%, and the content of orexigen - from 0.000001% to 10% of the mass.

Although the present invention has been described above with reference to specific illustrative embodiments, does not mean that it is limited to the specific described here form. Rather, the invention is limited only by the accompanying claims and, other embodiments than the specific embodiments described above are equally possible within the scope of this appended claims.

In the claims the term "contains/containing" does not exclude the presence of other varieties or stages. In addition, despite the fact that some distinctive features can be included in different claims, these may mainly can be combined, and the inclusion in different claims does not imply that the combination of distinctive features is not possible and/or useful. In addition, references in the singular does not exclude many. The terms "first", "second" etc. do not exclude set.

Examples

The following examples are intended only to further illustrate the invention and are in no way intended to limit the scope of the present invention, as defined by the attached claims.

Example 1. MICK pentane-1,5-dio is and chlorhexidine against S. aureus

Minimum inhibitory concentration (MIC) pentane-1,5-diol, chlorhexidine against S. aureus was determined using concentrations of bacteria 6×106(20 µl, engraved on the Cup with DST-agar). The results are described below in table 1 and 2.

Table 1
MICK pentane-1,5-diol against S. aureus and P. acnes
Pentane-1,5-diol (% wt.)MICK (S. aureus)
5+++a
6++
7++
8+
9-
10-
20-
30-
Control (without pentane-1,5-diol)+++
and: +++: The same is the OST, as the control Cup without any amount of chlorhexidine and/or pentane-1,5-diol
++: Reduced growth compared to control
+: Very weak growth
-: No growth
Table 2
MICK digluconate chlorhexidine against S. aureus
Chlorhexidine (% wt.)MICK
0,00001+++

0,00005++
0,0001-
0,0005-
0,001-
0,005-
0,01-
0,02-
0,05-
0,1-
0,5-
1
Control (without chlorhexidine)+++

Example 2. MICK pentane-1,5-diol in combination with chlorhexidine against S. aureus

Minimum inhibitory concentration (MIC) pentane-1,5-diol, combined with chlorhexidine against S. aureus was determined using concentrations of bacteria 6×106(20 µl, engraved on the Cup with DST-agar). The results are described below in table 3.

-
Table 3
MICK pentane-1,5-diol, combined with digluconate chlorhexidine against S. aureus
Chlorhexidine is 0.0001%MICKChlorhexidine 0,00005%MICKChlorhexidine 0,00001%MICK
9% pentane-1,5-diol-9% pentane-1,5-diol-9% pentane-1,5-diol-
8% pentane-1,5-diol-8% pentane-1,5-diol8% pentane-1,5-diol-
7% pentane-1,5-diol-7% pentane-1,5-diol-7% pentane-1,5-diol+
6% pentane-1,5-diol-6% pentane-1,5-diol-6% pentane-1,5-diol++
5% pentane-1,5-diol-5% pentane-1,5-diol-5% pentane-1,5-diol+++

As can be seen from tables 1-3, it is evident there is a synergistic antibacterial effect when combined pentane-1,5-diol with digluconate chlorhexidine. While neither chlorhexidine at a concentration of 0,00005% or below or pentane-1,5-diol at a concentration of 8% or below are not effective against S. aureus, the combination 0,00005% chlorhexidine 5% or more of pentane-1,5-diol is effective. In addition, even such low concentrations of chlorhexidine and pentane-1,5-diol, like 0,00001% and 7%, respectively, are effective when combined. Example 3. MICK pentane-1,5-diol and chlorhexidine against P. acne Minimum inhibitory concentration (MIC) pentane-1,5-diol and chlorhexidine against R. acnes was determined using concentrations of bacteria 6×106(20 µl, applied to plates with agar with blood). The results are described below in table 4 and 5.

Table 4
MICK pentane-1,5-diol against P. acnes
Pentane-1,5-diol (% wt.)MICK
1+++
3++
5+
6-
7-
10-
20-
30-
Control (without pentane-1,5-diol)+++
Table 5
MICK digluconate chlorhexidine against P. acnes
MICK
0,00001+++
0,00005++
0,0001-
0,0005-
0,001-
0,005-
0,01-
0,02-

0,05-
0,1-
0,5-
1-
Control (without chlorhexidine)+++

Example 4. MICK pentane-1,5-diol in combination with chlorhexidine against P. acnes

Minimum inhibitory concentration (MIC) pentane-1,5-diol, combined with chlorhexidine against P. acnes was determined using concentrations of b is cteri 6×10 6(20 µl, applied to plates with agar with blood). The results are described below in table 6.

Table 6
MICK pentane-1,5-diol, combined with digluconate chlorhexidine against P. acnes
Chlorhexidine is 0.0001%MICKChlorhexidine 0,00005%MICKChlorhexidine 0,00001%MICK
6% pentane-1,5-diol-6% pentane-1,5-diol-6% pentane-1,5-diol+
5% pentane-1,5-diol-5% pentane-1,5-diol-5% pentane-1,5-diol++
3% pentane-1,5-diol-3% pentane-1,5-diol-3% pentane-1,5-diol+++
1% pentane-1,5-diol-1% pentane-1,-diol ++1% pentane-1,5-diol+++

As can be seen from tables 4-6, it is clear there is a synergistic antibacterial effect when combined pentane-1,5-diol with digluconate chlorhexidine. While neither Chlorhexidine at a concentration of 0,00005% or below or pentane-1,5-diol at a concentration of 5% or lower are not effective against P. acnes, the combination 0,00005% chlorhexidine 3% or more of pentane-1,5-diol is effective.

Example 5. MICK pentane-1,5-diol in combination with chlorhexidine against S. pvogenes A CCUG 4208

Minimum inhibitory concentration (MIC) pentane-1,5-diol, combined with chlorhexidine against S. pvogenes A CCUG 4208 was determined using concentrations of bacteria 6×107(20 µl, applied to plates with agar with blood). The results are described below in table 7 and 8.

Table 7
MICK digluconate chlorhexidine and 1,5-pentanediol against S. pyogenes
1,5-pentanediol (%)MICKDigluconate chlorhexidine (%)MICK
2 +++0,00001+++
4++0,00005+++
6+0,0001+
7-0,0005-
8-0,001-
9-0,005-
10-0,01-
15-0,05-
0,1-
0,5-
The positive control (cups with agar without substance) showed the importance of MICK corresponding +++.
Table 8
MICK pentane-1,5-diol, combined with digluconate chlorhexidine against S. pyogenes
1,5-pentanediol (2%)MICK
#1 digluconate chlorhexidine0,00001%++
#2 digluconate chlorhexidine0,00005%+
#3 digluconate chlorhexidine0,0001%-
1,5-pentanediol (4%)MICK
#4 digluconate chlorhexidine 0,00001%+
#5 digluconate chlorhexidine0,00005%-
#6 digluconate chlorhexidine0,0001%-
1,5-pentanediol (6%)MICK
#7 digluconate chlorhexidine0,00001%-
#8 digluconate chlorhexidine0,00005%-
#9 digluconate chlorhexidine0,0001%-

As can be seen from tables 7 and 8, it is obvious there is a synergistic antibacterial effect when combined pentane-1,5-diol with digluconate chlorhexidine. While neither chlorhexidine at a concentration of 0.0005% or below or pentane-1,5-diol at a concentration of 6% or below are not effective against S. pyogenes, the combination 0,00001% chlorhexidine 4% or more of pentane-1,5-diol is effective.

Example 6. MICK pentane-1,5-diol in combination with chlorhexidine

This study used the solution digluconate chlorhexidine (CHG), 20%in water, C9394-25ML (Sigma, St. Louis, USA) and PD (BASF AG, Ludwigshafen, Germany) and tested the following reference strains: C. albicans (CCUG 5594), S. aureus (CCUG 17621) and P. acnes (CCUG 1794).

Minimum inhibitory concentration of CHG and pentane-1,5-diol (PD) was determined by the method of dilution in agar. A dilution series of each compound was prepared in a medium with agar and blood for P. acnes and agar for diagnostic sensitivity testing (DST) (Oxoid, Basingstoke, UK) for C. albicans and S. aureus. A series of breeding with each agent was done with freshly prepared agar at 48-50°C. Intervals, the final concentrations were as follows: solution CHG from 0.00001 to 1% (wt./about.) and PD 1-30% (vol./vol.). The resulting Cup was used immediately after solidification of the agar.

For each body received the inoculum by growing the organisms on agar with blood. Colonies suspended in phosphate-saline buffer solution (PBS), and the suspension was brought to approximately 6×106CFU/ml (colony forming unit/ml) for C. albicans and P. acnes, and 6×105CFU/ml for S. aureus. Cups were inoculable 20 µl plates and incubated for one day for C. albicans and S. aureus, and three days for P. acnes. Then determined the MIC as the lowest concentration of compounds inhibitory to the growth of the isolates.

In-p is pout, for each microorganism was determined MICK CHG and PD, respectively. Then, on each microorganism tested interval of the combined concentrations of CHG and PD to determine whether there was a synergistic activity. The definition of synergy is: "effect that is greater than the sum of the effects of two drugs, such as the equation: 1+1...". Each isolate was tested twice.

CHG was effective against all micro-organisms (table 9). MICK CHG was 0,0005 (% wt./about.) against C. albicans and 0.0001 (% wt./about.) against S. aureus and P. acnes.

PD showed activity against C. albicans, S. aureus and P. acnes in 5, 9 and 6% vol./about., respectively. MICK CHG was significantly lower than for PD with a multiplier of 1×10-4for C. albicans, 6×10-5for S. aureus and 9×10-5for P. acnes (table 9).

When combining CHG and PD in lower concentrations than their corresponding MICK, their antimicrobial activity was increased. MICK CHG decreased from 0.0005 to 0,00005 (%, mass./vol.), and MICK PD from 5 to 3 (%, vol./about.) to prevent growth of C. albicans. MICK CHG decreased from 0.0001 to 0,00001 (%, mass./vol.), and MICK PD - 9 to 8 (%, vol./about.) for S. aureus. MICK CHG decreased from 0.0001 to 0,00005 (%, mass./vol.), and MICK PD from 6 to 3 (%, 06./about.) to prevent the growth of P. acnes (table 9).

Table 9
Minimum inhibitory concentration (MIC) of digluconate chlorhexidine (CHG) (% wt./about.) and pentane-1,5-diol (PD) (% vol./about.) individually or in combination against .albicans, S. aureus and P. acnes by the method of dilution in agar. The ratio shows a decrease MICK CHG and PD individually and in combination
StrainsMICK oneMICK UnitedAttitude (single/combined)
CHGPDCHGPDCHG/CHG+PDPD/PD+CHG
.albicans CCUG 55940,000550,00053102
S. aureus CCUG 176210,000190,000018101
P. acnes CCUG 17940,000160,000053 22

1. Antimicrobial composition containing chlorhexidine and pentane-1,5-diol, where the number of chlorhexidine is from 0.000001 to 5 wt.%, and the number of pentane-1,5-diol is from 1 to 75 wt.%.

2. The composition according to claim 1, where the number of chlorhexidine is from 0.00001 to 5 wt.%, and the number of pentane-1,5-diol is from 3 to 25 wt.%.

3. The composition according to claim 2, where the number of chlorhexidine is from 0.001 to 2.5 wt.%, and the number of pentane-1,5-diol is from 5 to 15 wt.%.

4. The composition according to claim 1, where the specified composition is a pharmaceutical composition.

5. The composition according to claim 4, where this composition is intended for topical administration.

6. The composition according to claim 4, where the specified composition comprises a carrier and a thickener.

7. The composition according to claim 1 for use in therapy.

8. The use of a composition according to claim 1 in non-therapeutic disinfection.

9. Composition according to any one of claims 1 to 6 for use in the treatment of infections.

10. The composition according to claim 9, where this infection is an infection that hits the skin.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to dentistry and may be used for making hygienic and therapeutic products for daily dental and oral care, namely to mouth rinses. A mouth rinse formulation contains troxerutin 0.1-0.3 wt % in a combination with ectoin 0.01-1.0 wt %, nicotinamide 0.05-0.1 wt % and a complex of bisabolol and ginger extract 0.01-0.03 wt %, as well as a cosmetically acceptable base containing a water-retaining additive, a structure-forming agent, a filming agent, an anti-caries additive, a flavouring agent and a target additive in the amounts to provide performing the above functions, a biologically active additive consisting of Aloe Vera and herbal infusion, while a medium is water.

EFFECT: formulation provides the effective repair action on the periodontal tissues and high cleansing properties when using the mouth rinse.

14 cl, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetology and represents a sun-protection cream consisting of aqueous-alcohol extract of grape skins, CO2-extract of grape skins, olive oil, isopropyl myristate, higher synthetic primary fatty alcohols C16-C20 fraction, polyethylene glycol-400 stearate, bee wax, glycerol, stearine, triethanolamine, benzyl alcohol, a preserving agent, a flavouring agent and water with the ingredients of the cream are found in certain proportions, wt %.

EFFECT: invention provides a higher rate of sun-protective action of the sun-protection cream.

4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetic industry and represents an oil-in-water emulsion composition for UV protection, containing: (a) octocrylene, (b) bis- ethylhexyloxyphenol methoxyphenyl triazine, (c) hexyldiethylamino-hydroxybenzoyl benzoate, (d) 4-tert-butyl-4'-methoxybenzoyl methane, wherein the amount of the ingredients (a), (b), (c) and (d) makes 1 - 40 wt/wt %, (e) a water-soluble polymer in the amount of 0.01-5 wt/wt %, (f) a water-swellable clay mineral in the amount of 0.01-4 wt/wt %, (g) an oil ingredient having NOB 0.05 or more in the amount of 1 - 70 wt/wt %, (h) a higher fatty acid in the amount of 0.1-10 wt/wt %, (i) a surfactant in the amount of 0.1-10 wt/wt %, (j) water - the rest, wherein all the amounts are presented as a percentage of the total amount in the oil-in-water emulsion composition.

EFFECT: invention provides developing the composition having the good UV protection effect, exhibiting the emulsion stability and pleasant sensation.

6 cl, 8 ex, 4 tbl, 1 dwg

FIELD: medicine.

SUBSTANCE: invention refers to cosmetology and represents a cosmetic product for face and body skin care containing a basic component presented by dry feed rye spent wash with syrup, as well as at least one paste-forming component specified in a group: water, liquid soap and optionally at least one component specified in a group of: sugar-free cultured milk product, rye flour, vegetable oil, honey.

EFFECT: invention provides preparing the high efficacy natural dry cosmetic product for face, hand and body skin cleansing, nourishment and regulation.

7 cl, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: claim describes a cosmetic or dermatological composition in the form of cream, foam, spray, gel, gel spray, lotion, oil, oil gel or mousse. The composition contains at least one active substance, at least one molecular imprinted polymer in the presence of the same active substance, and at least one oil phase. The polymer contains a) a monoethylene-saturated mono- or dicarboxylic acid or α,β-ethylene-unsaturated mono- or dicarboxylic acid esters with diols and b) methacrylic acid esters of at least dihydric alcohols. The molar ratio of the compounds a) and b) makes 1:2 to 1:4, and the polymer is prepared in the medium of a solvent wherein monomers, but not the polymer to be prepared is dissolved in the presence of the active substance.

EFFECT: combination of the molecular imprinted polymer prepared by precipitative polymerization, and the oil phase provides the release of the active substance both in the water phase, and in the oil phase which ensures the best contact with a lipophilic surface, such as skin.

3 cl, 3 dwg, 7 tbl, 37 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a polyphenol derivative formulation and is used in cosmetics, nutrition science and therapy. The polyphenol derivative formulation possessing antioxidant and antiradical activity and having an effect on carbonyl stress. A method for preparing the formulation. The cosmetic formulation possessing antioxidant and antiradical activity and having an effect on carbonyl stress. Using the formulation in nutrition science. The formulation to be used as a therapeutic agent possessing antioxidant and antiradical activity and having an effect on carbonyl stress. The pharmaceutical formulation possessing antioxidant and antiradical activity and having an effect on carbonyl stress.

EFFECT: formulation has an effect on carbonyl stress.

23 cl, 11 dwg, 5 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to cosmetology and represents an oil-in-water emulsion sun-protection cosmetic composition containing: (A) 1 to 7.5 wt % of octyl methoxycinnamate; (B) 1 to 4 wt % of tret-butyl methoxydibenzoyl methane and/or 2-hydroxy-4-methoxybenzophenone; (C) 0.5 to 3 wt % of a polyoxyethylene/polyoxyalkylene alkyl ester block copolymer; (D) 10 wt % or more of a nonpolar oil relative to the total amount of the oil component; wherein an average emulsion particle diameter makes not more than 700 nm.

EFFECT: invention provides developing the stable sun-protection composition having improved ultraviolet blocking capability and good usability.

4 ex, 4 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to cosmetology, particularly a composition enriched with silver nanoparticles and a method of producing said composition. The composition is intended to replace water as the basic component for producing cosmetic products (shampoos, Balsams, masks, intimate hygiene agents, creams etc). The composition contains a dry 65% whey protein concentrate, a micellar solution of silver nanoparticles in form of an aqueous solution having concentration of 500 mg/l in amount of 0.01-0.5% and additionally water. The method of producing said composition involves heating water to temperature of 50-55°C, adding the whey protein concentrate to the heated water in portions, recirculating the obtained mixture for 15 minutes using a cam-driven pump, adding the micellar solution of silver nanoparticles to the stirred mixture and cooling the obtained mixture to 30°C.

EFFECT: invention enables to obtain cosmetic material which protects skin from inflammatory processes and ageing, controls and maintains the skin water-oil balance.

2 cl, 2 ex

FIELD: medicine.

SUBSTANCE: invention refers to cosmetology, particularly to hair colouring products. The present invention represents a keratin fibre lightener characterised by the fact that it contains in a cosmetic carrier: 4-acetyl-1-methylpyridinium-n-toluene sulphonate, at least one toxicologically sage additional lightening activator and/or a pharmacologically acceptable salt thereof, and hydrogen peroxide.

EFFECT: using the hair lightener according to the invention enables providing the improved blonding ability and reduced hair damage.

13 cl, 2 ex, 5 tbl

FIELD: chemistry.

SUBSTANCE: present inventions relate to protein engineering, plant molecular biology and pest control, as well as a hybrid insecticide protein and use thereof. Described is a hybrid insecticide protein which includes from the N-end to the C-end an N-end portion of Cry3A protein which is fused with the C-end portion of Cry1Ab protein, wherein the position of the crossover of the Cry3A protein and the Cry1Ab protein is located in a conservative block 2, in a conservative block 3 or in a conservative block 4 and has anti-western corn rootworm activity. Also disclosed are nucleic acid molecules which code the novel proteins, methods of producing proteins, methods for use thereof, as well as transgenic plants and seeds thereof which contain such proteins.

EFFECT: inventions enable to obtain cheap means of controlling Diabrotica worms.

39 cl, 8 dwg, 9 tbl, 46 ex

FIELD: biotechnologies.

SUBSTANCE: inventions refer to polynucleotide sequence coding the structured pertactin protein (Prn); a vector including such a sequence and compositions containing protein or vector. The characterised polynucleotide sequence codes 300 first amino acids that are the closest to N-end of this type of natural mature Prn (PrnX300), and amino-acid sequence including 620 last amino acids that are the closest to C-end of this type of natural mature Prn (PrnY620) so that structured pertactin PrnX300-PrnY620 of Bordetella class is obtained. Structured molecules Prn include polymorphisms of different B. Pertussis strains and cause immune responses with increased protective ability and opsonophagocytic activity, which exceed the corresponding properties of the preceding vaccines.

EFFECT: protein obtained as per the presented invention can be used in medicine and veterinary as a component of antibacterial vaccines against Bordetella pertusis.

12 cl, 3 dwg, 2 tbl, 4 ex

FIELD: biotechnologies.

SUBSTANCE: invention proposes compounds of labyrinthpeptins A1, A2, or A3 of formula (I) , where {A}, {B}, {C}, R1-R6, m and n have the values specified in the formula of the invention. Compounds are obtained at fermentation of Actinomadura namibiensis DSM 6313 strain under acceptable conditions in cultural environment till one or more compounds of formula (I) are formed. The invention proposes the deoxyribonucleic acid (DNA) coding preprolabyrinthpeptin A2, and the deoxyribonucleic acid (DNA) coding preprolabyrinthpeptin A1, as well as preprolabyrinthpeptins A1 and A2, and prolabyrinthpeptins A1 and A2. Labyrinthpeptins of formula (I) are used for therapy of infections caused by gram-positive bacteria, virus infections and/or neuropathic pain caused by inflammation.

EFFECT: improving therapy efficiency.

24 cl, 4 tbl, 20 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and concerns a combined pharmaceutical composition having antibacterial activity. As an active substance, the composition contains a clindamycin salt or ester, a base which is a combination of a hydrophobic ingredient, a hydrophilic ingredient and an emulsifier, and a gelling polymer. A method of preparing the declared composition involves the fact that a solution of the clindamycin salt or ester in a part of the hydrophilic ingredient is added with the gelling polymer, then the emulsion prepared of a residual part of the hydrophilic ingredient, the hydrophobic ingredient and the emulsifier, and the prepared mixture is agitated until smooth.

EFFECT: new pharmaceutical formulation is characterised by a high level of antibacterial activity, stability both at storage temperature (25°C), and at temperature of use (37°C), good packaging extrusion.

15 cl, 1 dwg, 2 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and concerns a solid dosage form containing azithromycin dihydrate as an active substance in the amount of 83.2-93.2% and pharmaceutically acceptable target additives. A tablet core is film-coated in the amount of 2.5-5.0% of tablet weight. The new dosage form of azithromycin contains the high absolute (1000 mg) and relative (88.2%) concentration of the active substance that enables reaching the immediate therapeutic effect.

EFFECT: therapeutic preparation is storage-stable and complies with the Pharmacopoeia requirements.

FIELD: medicine, pharmaceutics.

SUBSTANCE: powder composition for intrapulmonary administration contains particles of ciprofloxacin betaine 3,5-hydrate and an excipient. The particles have a mass median aerodynamic diameter making from approximately 1 to approximately 5 mcm; a pulmonary half-life of betaine 3,5-hydrate makes min. 1.5 h; while a roughness of the composition falls within the range of 3 to 10.

EFFECT: composition may be used to treat an endobronchial infection, such as an infection caused by Pseudomonas aeruginosa, and it is most applicable for treating mucoviscidosis.

6 cl, 8 dwg, 16 tbl, 12 ex

FIELD: medicine.

SUBSTANCE: invention refers to using Furacilin as a photosensitiser.

EFFECT: invention enhances the antimicrobial activity of Furacilin when exposed to light the spectral range of which corresponds to the electronic absorption spectrum of Furacilin.

1 tbl, 2 dwg

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and chemical-pharmaceutical industry, namely to a pharmaceutical composition of levofloxacin. The technical result is ensured by using Klucel and a combination of desintegrants, including sodium starch glycolate and sodium croscarmellose in the composition, with the first desintegrant being introduced before wet granulation, and the second one - after dry granulation together with an antifriction agent that is magnesium stearate.

EFFECT: composition possesses a better combination of bioavailability and appearance of tablets, including in storage; as additives, the composition contains microcrystalline cellulose (MCC), sodium starch glycolate, sodium croscarmellose, calcium carbonate, hydroxypropyl cellulose and stearic acids and/or salts thereof.

10 cl, 8 ex, 4 tbl

FIELD: medicine.

SUBSTANCE: invention refers to a vaccine containing a combination of non-living antigens of Lawsonia intracellularis, Mycoplasma hyopneumoniae and porcine circovirus, and a pharmaceutically acceptable carrier. The invention also refers to a kit comprising a first container with the non-living antigens of Lawsonia intracellularis, one or more other containers with the antigens of Mycoplasma hyopneumoniae and porcine circovirus, and an instruction for mixing the antigens of Lawsonia intracellularis, Mycoplasma hyopneumoniae and porcine circovirus for preparing one combined vaccine for systemic vaccination.

EFFECT: group of inventions provides the more effective prevention of the diseases caused by these pathogens.

8 tbl, 3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to preparing a mouthwash containing water, a moisturiser in the amount of 5 wt % to 15 wt % and 0.01 wt % - 5 wt % of a compound presented by the structure (III), wherein R1 and R2 are independently specified in hydrogen atoms, C2-6 -alkenyl group and C1-6 - alkyl group; and the compound (III) is dissolved in ethanol.

EFFECT: invention involves a method for reducing bacterial population on the substrate by substrate contact with the composition containing the compound of the structure (IV), wherein R1 and R2 are independently specified in the substituted or unsubstituted methyl group, substituted or unsubstituted ethyl group and substituted or unsubstituted butyl group.

11 cl, 1 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: intratympanic composition used for treating an ear disease contains: (a) an antimicrobial agent consisting of a number of particles; and (b) a polyoxyethylene and polyoxypropylene copolymer; the composition (i) is a liquid at room temperature; (ii) has a gelling point within the range of 19°C to 42°C; (iii) has a gel viscosity of 15000 sP to 1000000 sP; (iv) has an osmolarity less than 1000 mOsm/l; and the intratympanic composition release the antimicrobial agent in an ear for at least 5 days, and it is introduced at room temperature.

EFFECT: effective treatment of the ear diseases; the composition is non-toxic and has a non-irritating effect on the ear structures, provides the permanent prolonged release of the active agent with a reduced dose rate and reduces the risk of a potential tympanum damage.

13 cl, 9 tbl, 5 dwg, 30 ex

FIELD: medicine.

SUBSTANCE: invention refers to medicine. What is described is a wipe, a hygienic wipe such as a baby wipe, a female hygiene wipe, an incontinence wipe, a hand care wipe, a foot care wipe with said wipe containing a composition with oxidised lipids and a deodorising substance. Lipids are oxidised in the controlled environment to provide peroxide number at least 20 mecv/kg. Lipids represent, e.g. fatty acid triglycerides. Note: when publishing the grant of the patent, the initial description and the examination corrected abstract shall be used.

EFFECT: wipe shows better deodorising properties.

10 cl, 12 tbl, 2 ex

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