Stabilised topical composition possessing comedolytic and antibiotic action

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to medicine and cosmetics, more specifically to a topical pharmaceutical composition possessing comedolytic and antibiotic action, comprising an effective amount of the antibiotic clindamycin, salicylic acid and excipients. The pharmaceutical composition is presented in the form of a gel. The excipients are as follows: acrylate copolymer emulsion Salcare SC80, allantoin, antioxidant dihydroquercetin preservative Sharomix MCI, propylene glycol, cyclomethicone DC 345, tocopherol phosphate, UV filter Escalol 567, emulsifier DC 5329, trometamol and thermal water.

EFFECT: stabilised composition has strong comedolytic and antibiotic action, comprises the protective SPF factor which protects inflamed skin against the negative effects of UV radiation and has a shelf life of at least 3 years.

3 ex, 4 tbl

 

The invention relates to the field of medicine and cosmetics, specifically to pharmaceutical compositions for local application with protivougrevoe and antibiotic action, containing an effective amount of the antibiotic clindamycin, salicylic acid and excipients. The pharmaceutical composition is made in the form of a gel (hereinafter - gel).

Acne is an inflammatory skin disease caused by changes in pilosebaceous structures (composed of the hair follicle and sebaceous gland). Hyperkeratinization and the formation of plaques made of keratin and sebum leads to an increase in sebaceous glands, especially during the maturation of the skin in the pubertal period. Increased production of sebum occurs when adrenarche, when increased production of DHEA. The accumulation of sebum can lead to the development of infection. The immune system destroys bacteria and pus "wrapped" in clusters under the epidermis. Ill try to get rid of pustules, removing them alone and in non-sterile conditions. Such damage subject to layers violates the fine structure of the dermis and creates a weakened area, which attack bacteria. In the immune system leads to the spread of acne. The term "acne" is derived from the Greek "άκμή" is the culmination break skin (the AV Yarova et al., 2005).

The causes of the disease remain unclear. In the mechanism of development play a major role oily, reducing the bactericidal effect of the sebum and resulting in activation of coccal flora. Important role in the mechanism of acne is given to the bacteria Propionibacterium acnes and the products of its life activity. Acne ordinary (acne vulgaris, acne) develops in boys and girls during puberty and gradually disappear by 25-30 years. On the emergence and exacerbation of acne also affects menstruation, stress, heat, humidity and genetic factors. It is known that also cause acne are cosmetics containing lanolin and paraffin. Also, acne can be a side effect of some medications.

There are different types of acne: pathomorphological marked seborrhea, sebaceous gland hyperplasia, hypersecretion of sebum, hyperkeratosis, leading to the formation of comedones - balance-Horny plugs in the ducts of the sebaceous glands with partial or complete blockage with the appearance of black spots.

For effective impact on Propionibacterium acnes it is necessary to use antibiotics. One of the best on the degree of impact is clindamycin.

Clindamycin (Clindamycin) - 7-glottochronology of lincomycin. Available in the form of hydrochloride for ingestion and phosphate - DL the injection. On chemical structure, mechanism and spectrum of antimicrobial action close to lincomycin, but against certain types of microorganisms (especially bacteroids and nesporoobrazuyushchikh anaerobes) more active (2-10 times). It penetrates the tissues and fluids of the body, undergoes biotransformation in the liver, excreted in urine and bile (Mashkovsky PPM, 2007).

For effective acne treatment you need to keratinized layers of the skin went much faster than the natural process. This requires the use of hydroxy-acids. One of the most effective in this regard is salicylic acid.

Salicylic acid (Acidum salicylicum) - ortho-hydroxy-benzoic acid. White fine needle crystals or light crystalline powder, odorless. Few soluble in cold water, soluble in hot water, easily soluble in alcohol. Used externally as an antiseptic, distracting and keratolytic agent in ointments, pastes and alcohol solutions (Mashkovsky PPM, 2007).

Salicylic acid is often used in combination with fruit acids to enhance exfoliation. Occurs naturally in the form of esters in the birch bark and the leaves of gaultheria (Hernandez H., 2003).

There are pharmaceutical compositions for local application, designed for the treatment of acne. Such compositions are sold lekarstvennyh forms of cream, gel, ointment, powder or solution.

Known composition clindamycin and benzoyl peroxide for acne treatment, kit for the preparation of compositions, method of preparation and method of treatment (application for invention of the Russian Federation No. 94040385 from 10.11.1996), comprising as active substances clindamycin and benzoyl peroxide. Kits for preparing the compositions comprise a solution of clindamycin in the first container, the suspension in the gel benzoyl peroxide in the second container.

The main disadvantages of this tool is difficult to use, lack of effectiveness in the treatment of acne due to the lack of modern auxiliary substances.

There are pharmaceutical compositions for local application containing protivougrevoe connection and antibiotic compound (RF patent No. 2404759 from 27.11.2010)containing a therapeutically effective amount adapalene, or its pharmaceutically acceptable salt, or a complex ester, clindamycin, or its pharmaceutically acceptable salt, or ester, and a hydrophilic matrix in an amount of from 0.1 to 5.0 wt.%, containing carbomer. The invention provides a constant and uniform release of the active pharmaceutical ingredients, increased efficiency and fewer side effects.

The disadvantage of this invention is the use of carbomer 940 (Carbopol 940) and mate the parabens as preservative.

Carbopol 940 is the aggregate state of powder, which, when used, must be subject to the preliminary stage of swelling. Stage swelling carbomer requires heat the water up to 40°C and extracts 1-3 hours for uniform flow of the process. After exposure requires intensive mechanical mixing, requiring significant energy costs.

Parabens are ineffective against bacteria and are active mainly against fungi and completely inactivated nonionic surfactants, and also possess estrogenic activity (Belikov PU et al., 2003).

If you already use parabens, they must be used together (several types): commonly used esters of para-hydroxy-benzoic acid with different radicals (methyl-, ethyl-, propyl-, and butylparaben), which have different impact on the microflora, but not one methylparaben.

Parabens do not dissolve in water, so they are added into the lipid phase, from which it is slowly released and, basically, this impact is not enough. In the presented formulation of the water almost 67 wt.% and the need to use water-soluble preservative for effective protection follows logically.

Closest to the claimed technical essence and the achieved result, selected as a prototype, is cartenna the ointment Conduit (manufacturer JSC "Akrikhin", Russia), which has an antibacterial effect. The ointment contains as active pharmaceutical substances, the antibiotic clindamycin, the basis consists of: methyl parahydroxybenzoate (nipagin), allantoin, tocopherol phosphate lauryldimethylamine disodium, propylene glycol, macrogol 400 (polyethylene oxide 400), carbomer (copolymer, interpolymer), sodium hydroxide, purified water.

The ointment Conduit is one of the most effective means for the treatment of acne, of presents on the Russian market, but this tool has a few shortcomings.

The main disadvantages of the prototype are insufficient transdermal penetration of the active substance is clindamycin, used as a preservative methyl ester p-oksibenzoynoy acid (nipagina), which refers to the parabens.

Used as the basis of the polyethylene oxide 400 deprecated and does not give the necessary rheological characteristics (tactile sensation after application, the degree of stickiness).

The prototype also contains a UV filter to protect damaged skin from ultraviolet radiation, which is especially important when the treatment of inflammatory processes.

The technical result of the invention is achieved by using as the active components of the antibiotic clindamycin and salicylic acid, ka is este auxiliary substances - propylene glycol, UV filter Escalol 567, cyclomethicone DC 345, allantoin, tocopherol phosphate, antioxidant dihydroquercetin, acrylate emulsion Salcare SC80, silicone emulsifier PEG-12 Dimethicone DC 5329, preservative Sharomix MCI, trometamol and thermal water.

Propylene glycol is used to dissolve clindamycin and salicylic acid. The process is conducted at a temperature of 40-50°C. Propylene glycol is used as a humectant and solubilizer in the production of cosmetics and pharmaceuticals. In this case, propylene glycol functions as the solubilizer and improves penetration of active substances through the stratum corneum of the skin (Stratum Corneum) in the dermis.

Allantoin (5-Bridgeton) - colourless crystals, soluble in water. Allantoin has astringent effect and as binders for outdoor applications included in the list of local anesthetics, astringents and anti-inflammatory drugs of the world Health Organization.

Allantoin is also widely used in the cosmetic industry in various creams, has two opposite effects on the skin: softens the stratum corneum, promoting the separation of dead cells, and stimulates tissue regeneration. Usually introduced in the composition of cosmetic products for tightening pores, soften the skin, including PR is naznacheniya to care for chapped or burned by the sun (inflamed) skin.

Tocopherol phosphate (Vitamin E) is a fat - soluble vitamin. It is an antioxidant, protects cells from pathological lipid peroxidation, which leads to aging and death. Lipid peroxidation plays an important role in the development of malignant processes in the body, so it is believed that antioxidants protect against cancer. The lack of vitamin E cells become susceptible to the action of toxic substances, fail faster, weakens the immune system.

Vitamin E is needed by all body tissues. It protects blood cells red blood cells, improving the transport of oxygen to the tissues. Due to the effect on blood clotting prevents the formation of blood clots in the vessels. Used for prevention of atherosclerosis.

Tocopherol phosphate improves the nutrition of the skin and mucous membranes, allowing prevents skin dryness and promotes the "rejuvenation" of the body.

To stabilize the gel is introduced organic UV filter Escalol 567 Benzophenone-3 (INCI name: Benzophenone-3), active in the ranges "a" and "b" ultraviolet radiation and antioxidant dihydroquercetin.

Main parameters determining the effectiveness of sunscreens are minimal erythema dose (MED) and the factor sun protection - SPF (Sun Protection Factor".

Erythema, or redness of the skin, is easy the second quantitative characteristic - MED. Minimal erythema dose (biodata) is the dose that causes minimal visible eye redness, which develops after a certain period of time after exposure (usually within 24 hours). EDR can also be defined as the exposure time is sufficient for the induction of minimal erythema. To find out how effective this tool protects from sunburn, measure the MED of unprotected skin and compare it with EDR skin, which is applied to the monitoring tool. The value of the SPF indicates how much EDR protected skin exceeds the MED of unprotected skin.

As an antioxidant used dihydroquercetin native form, obtained from the wood of Siberian larch (Larix sibirica Ledeb.) and Dahurian larch (Larix Dahurica Nurcz.).

The gel is added to silicone oil - cyclomethicone DC 345 (INCI name: Cyclomethicone). Cyclomethicone is a mixture of cyclic polydimethylsiloxanes with low viscosity of 0.65 CST, which ensures hydration and increased turnover on the skin surface and, as a consequence, the reduction of the pharmaceutical gel.

As the basis for the pharmaceutical gel of the selected aqueous anionic acrylic emulsion copolymer Salcare SC80 (INCI name: Steareth-10Allyl Ether/Acrylates Copolymer), which is a carbomer. Salcare SC80 compatible with a wide range of active Pharm is sitechecker substances. Salcare SC80 convenient to use due to its emulsified form, allowing you to quickly obtain a transparent gel.

To enhance the transfer of biologically active substances into the dermis used silicone emulsifier PEG-12 Dimethicone (INCI name: PEG-12 Dimethicone). When the emulsification forms instead of micelles vesicular structures - Nozomi who are able to transfer biologically active substances deep into the dermis.

Nozomi are vesicles consisting of a membrane in the form of water-insoluble double layer non-ionic emulsifier (surfactant). In this case, surfactants are a group of substances Dimethicone of Kaprielov representing ethers of polyethylene glycol and polydimethylsiloxane basis. Thus, the Dimethicone copolyol represent a hybrid of silicon and carbon. In contrast to liposomes, made on the basis of phospholipids, Nozomi have a number of advantages for the delivery of active pharmaceutical ingredients (API). The presence of the covalent bond of Si-Oh in the hydrophobic part of the molecule polydimethylsiloxanes basis of emulsifier, which has high elasticity, can be directed to deliver a wide range of ASF.

The use of water-soluble preservative Sharomix MCI (INCI name: 5-cloro-2-methyl-4-isothiazolinone and 2-methyl-4-isothiazolinone) helps to better protect the pharmaceutical gel than use the use of fat-soluble preservative (for example, parabens), due to the high content of the aqueous phase and the ability of microorganisms to reproduce it in the aqueous phase and the interface.

Stabilization of the concentration of hydrogen ions (pH) is trometamol (2-Amino-2-(hydroxymethyl)-1,3-propandiol), which, unlike other amino thickeners, such as di - and triethanolamines, has no irritant properties and less toxic, so you can use it even in injecting drugs (for example, a solution trisamina for injection).

thermal water contains mineral salts and a variety of trace elements (bromine, iodine, iron, magnesium, sodium and so on), the concentration of which corresponds to those in the human body, when environmental conditions are favorable for maintaining balance. That is, thermal water is a way to support broken under stress the natural composition of water in our body. Thermal water contributes to maintaining normal rate of cell metabolism, increases resistance to adverse environmental influences, supports skin hydration, as well as its protective properties at the required level and normalizes water-lipid balance.

All tools are manufactured in the laboratory NPO "Saitek"made on the basis of thermal water produced at the well No. 1 in the village of Suvo what's Stavropol region.

The source of thermal mineral water Suvorov No. 1 is a typical representative of the alkaline clomipramine deep water with high flow rate and temperature 53-56°C, was discovered and drilled in 1959 at a depth 1253 m and has a half-century tradition of healing people.

Enablement of the claimed invention is confirmed by examples of specific performance.

Example 1.

As active pharmaceutical ingredients, the gel contains clindamycin and salicylic acid, which is dissolved in propylene glycol at a temperature of 40-50°C.

In the base means includes: UV filter Escalol 567, cyclomethicone DC 345, antioxidant dihydroquercetin, allantoin, tocopherol phosphate, acrylate emulsion Salcare SC80, silicone emulsifier PEG-12 Dimethicone DC 5329, preservative Sharomix MCI, trometamol and thermal water.

Phase preparation and formulation of gels in examples 1-3 are presented in table 1.

Phase And is prepared at room temperature by mechanical mixing the following components in the mixer: acrylate emulsion copolymer Salcare SC80 - 1.0 wt.%, allantoin - 0.1 wt.%, antioxidant dihydroquercetin - 0.02 wt.%, preservative Sharomix MCI - 0.1 wt.%. Thermal water is made up to 100 wt.% from the total mass of the gel (i.e. Phases a, B, C and D).

Phase B contains as active formats ticheskoj substance clindamycin in number - 0.5 wt.%, salicylic acid - 4.0 wt.%, dissolved in propylene glycol 20.0 wt.% at a temperature of 40-50°C.

Phase B is added to Phase And cooled to a temperature of 30-50°C With mechanical stirring in a mixer.

Phase is prepared separately by intensive mechanical mixing and includes lipid components: cyclomethicone DC 345 - 5.0 wt.%, tocopherol phosphate is 0.01 wt.%, emulsifier DC 5329 - 1.0 wt.%. UV filter Escalol 567 is included in the mixture in an amount of 40.0 wt.%, providing SPF 40.

Phase b is introduced into the mixture (A+B) under vigorous stirring and at room temperature.

Phase G consists of a single component - trometamol, which when added to the amount of 1.0 wt.% neutralizes acrylate emulsion and, as a result, formed the consistency of a gel. Trometamol is introduced into the mixture at the last turn and is pH regulator.

The obtained pharmaceutical gel soft texture of white or white with a yellowish tint, with low specific smell, pH from 4.50 to 6.0.

Example 2.

Is similar to example 1, except that the following components are used in the amount of: acrylate emulsion copolymer Salcare SC80 - 2.0 wt.%, allantoin - 2.0 wt.%, antioxidant dihydroquercetin - 0.04 wt.%, preservative Sharomix MCI - 0.3 wt.%, clindamycin - 3.0 wt.%, salicylic acid - 8.0 wt.%, profiling icol - 10.0 wt.%, cyclomethicone DC 345 - 15.0 wt.%, tocopherol phosphate 0.1 wt.%, emulsifier DC 5329 - 3.0 wt.%, trometamol - 2.0 wt.%. UV filter Escalol 567 is included in the mixture in an amount of 8.0 wt.%, providing SPF 8 (table 1).

Example 3.

Is similar to example 1, except that the following components are used in the amount of: acrylate emulsion copolymer Salcare SC80 - 3.5 wt.%, allantoin - 1.0 wt.%, antioxidant dihydroquercetin - 0.1 wt.%, preservative Sharomix MCI to 0.5 wt.%, clindamycin - 5.0 wt.%, salicylic acid and 0.5 wt.%, propylene glycol - 15.0 wt.%, cyclomethicone DC 345 20.0 wt.%, tocopherol phosphate - 0.04 wt.%, emulsifier DC 5329 - 4.0 wt.%, trometamol - 2.5 wt.%. UV filter Escalol 567 is included in the mixture in an amount of 1.0 wt.%, providing SPF 1 (table 1).

Developed gel was physico-chemical, Toxicological tests in FGUZ "Center of hygiene and epidemiology in the Stavropol region" of Rospotrebnadzor. Studies have attested to the safety of use and high quality gel.

Due to the presence of salicylic acid, UV filter Escalol 567, antioxidant dihydroquercetin, allantoin and silicone emulsifier DC 5329, capable of forming vesicles-Nozomi, the recovery process of the skin (Acne treatment) was significantly faster.

Thus, the claimed stable composition which I has a pronounced protivougrevoe and antibiotic action, contains protective SPF, which protects the inflamed area of the skin from the negative effects of ultraviolet radiation.

Sources of information

1. The application for the invention of the Russian Federation No. 940403 85 from 10.11.1996.

2. RF patent №2404759 from 27.11.2010.

3. A.V. Maiorova, Shapovalov B.C., Akhtyamov S.N. Acne in the practice of the doctor-dermatologist. M., "Firm Clavel", 2005; 6-85.

4. Hernandez H. Cosmetic peels: theoretical and practical aspects. A collection of articles. - M, LLC firm "Clavel", 2003. - 214 S.

5. Mashkovsky PPM Medicines. - 15-ed., - M.: RIA "New wave", 2007. - 1206 S.

6. Belikov PU, Puchkova T.V. Preservatives in cosmetics and personal hygiene products, M.: Izd. "School of cosmetic chemists", 2003. - 250 S.

Salicylic acid
Table 1.
Phase preparation and formulation of stabilized compositions local application with protivougrevoe and antibiotic action
№ p/pIngredient nameContent in wt.%
Example 1Example 2Example 3
1Thermal waterto 100 by weight gelto 100 by weight gelto 100 by weight gel
2Preservative (Sharomix MCI)0,10,30,5
3Acrylate emulsion copolymer (Salcare SC80)1,02,03,5
4Antioxidant dihydroquercetin0,020,040,1
5Allantoin0,12,01,0
Phase B
6Propylene glycol20,010,015,0
7Clindamycin0,53,05,0
84,08,00,5
Phase
9Cyclomethicone (DC 345)5,015,020,0
10Silicone emulsifier (DC 5329)1,03,04,0
11UV filter (Escalol 567)40,08,01,0
12Tocopherol phosphate (Vitamin E)0,010,10,04
Phase G
13Trometamol1,02,02,5

Stable composition for local application in the form of gel, with protivougrevoe and antibiotic action, contain a therapeutically effective amount of clindamycin, tocopherol phosphate, allante is, basis, preservative, solvent propylene glycol, characterized in that it further contains salicylic acid, antioxidant dihydroquercetin, cyclomethicone, UV filter Escalol 567, silicone emulsifier DC 5329, as the basis of acrylate emulsion copolymer Salcare SC80, as preservative Sharomix MCI, as solvent - thermal water and the next content, wt.%:

Clindamycin0,5-5,0
Salicylic acid0,5-8,0
Propylene glycol10,0-20,0
UV filter Escalol 567from 1.0 to 40.0
Cyclomethicone DC 3455,0-20,0
Silicone emulsifier DC 53291,0-4,0
Antioxidant dihydroquercetin0,02-0,1
Allantoin0,1-2,0
Tocopherol phosphateof 0.01-0.1
Acrylate emulsion copolymer Salcare SC801,0-3,5
Trometamol1,0-2,5
Preservative Sharomix MCI0,1-0,5
Water thermalTo 100.0



 

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8 cl, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely an antiviral agent. An agent for influenza virus comprises an active substance in the form of an alcohol extract of bee moth larvae, an alcohol extract of propolis and an ointment base containing styrene maleic anhydride copolymer, Vaselin, emulsifier T-2, Cremophore RH-40 and Lutrol F-68, and purified water in certain proportions.

EFFECT: ointment shows manifested antiviral action on influenza virus.

3 dwg, 3 tbl, 6 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to chitosan carboxyalkylamide hydrogel and may be used for cosmetic and dermatological treatment of skin burns. Chitosan carboxyalkylamide hydrogel of pH close to that of skin and making 6.5 to 7.2 contains 40 to 90 mole % of the groups of N-carboxyalkylaminde D-glucosamine of formula (I) wherein n represents an integer 1 to 8, 60 to 10 mole % of the protic groups of D-glucosamine, and 5 to 15 mole % of the groups of N-acetyl-D-glucosamine. A method for preparing said hydrogel involves preparing an acid solution of chitosan of a degree of acetylation of 85 to 95%, providing a reaction of produced additive chitosan salt in an aqueous solution of diorganic acid and correcting pH of the prepared solution.

EFFECT: preparing the anhydrous product of chitosan carboxyalkylamide prepared by hydrogel dehydration.

12 cl, 1 dwg

FIELD: medicine.

SUBSTANCE: what is presented is the use of xenon in the form of an agent for external therapy of chronic recurrent inflammatory dermatopathies prepared by extra pure grade xenon saturation of a fatty base.

EFFECT: what is shown is considerable reduction of an inflammatory reaction on the second therapeutic day in such polygenic chronic inflammatory diseases, as psoriasis, atopic dermatitis, acne, acne rosacea, eczema.

4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmacy, namely agents based on herbal raw material possessing pecilomycotic action. A sage kerosene ointment contains kerosene extract of air-dried sage leaves, Vaselin taken in certain proportions.

EFFECT: ointment possess effective antimycotic action.

4 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to medicine, namely to a pharmaceutical composition for local application. The composition contains chondroitin sulphate, hyaluronidase, glucosamine hydrochloride, liposome and pharmaceutically acceptable carriers and excipients in the amounts specified in the patent claim. The composition may additionally contain capsaicin.

EFFECT: pharmaceutical composition according to the invention is characterised by fast skin penetration of the ingredients.

3 cl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine and pharmaceutical industry, and concerns a combined pharmaceutical composition with antibacterial and antifungal activity. The composition comprises clindamycin phosphate, butoconazole nitrate as active ingredients. As a basis, the composition comprises a combination of a hydrophobic ingredient, a hydrophilic ingredient and an emulsifier and a gelling agent. A method of preparing the declared composition involves that a solution of clindamycin salt or ester in a part of the hydrophilic ingredient is added with the gelling polymer, then the emulsion prepared of a solution of butoconazole in the remained part of the hydrophilic ingredient, the hydrophobic ingredient and the emulsifier, and the prepared mixture is agitated until smooth.

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

13 cl, 1 tbl, 4 ex

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