Pharmaceutical preparation for local and external application based on low-molecular interferon inducer

FIELD: medicine.

SUBSTANCE: invention relates to medicine and pharmacology and represents pharmaceutical composition for treating purulent destructive lesions of mucous membrane and skin, characterised by containing tilorone mixed with soft formable base, where as soft formable base it contains hyperosmolar substances selected from group.

EFFECT: invention ensures recovery of local immunity and biocoenosis of skin and mucous membranes in case of purulent destructive skin processes, reduction of secondary tissue necrosis on affected sections, high therapeutic activity and convenience in use.

7 cl, 19 ex

 

The invention relates to chemical-pharmaceutical industry, as well as to medicine and veterinary medicine, namely, pharmaceutical preparations for external and local application in the treatment of purulent-destructive processes of the skin with clinical and laboratory signs of immune deficiency, such as chronic recurrent furunculus, herpetic lesions of the skin and mucous membranes, atopic dermatitis, bacterial pneumonia-fungal lesions, ulcers, postoperative suppuration of wounds, to accelerate and improve healing.

The intensity of infection depends on the number and virulence of the pathogen, the state of the natural barriers and the resistance of the microorganism. Susceptibility for most infections is an individual and is usually caused by a lack of immunity. Infectious factor occupies a leading position in the pathogenesis of these common inflammatory diseases of the skin and soft tissues, as acne, boils, carbuncle, impetigo, abscess, cellulitis and other

Infections caused by opportunistic microorganisms occur in people with defects in the immune system, on the one hand, and of the changed biological properties of conditionally pathogenic microorganisms and their multiple resistance to antibi the ticks, on the other hand. The balance between macro - and micro-organism may be affected by exogenous and endogenous factors (disturbance of activity of the neuroendocrine system, immune deficiency, depletion mechanisms of adaptation associated with chronic pathology and others). The failure of the immune response of the organism to infectious factor entails a chronic infectious process.

The degree of pathogenicity of microorganisms is individual and defines the different activity of the immune answer of an organism to them. It is associated with the ability to attach to sensitive cells (adhesion), to multiply on their surface, to penetrate into these cells or underlying tissues, to overcome nonspecific and specific immunity factors, to exert an immunosuppressive effect (kutasevich AF, her A.N. "The place of external preparations containing guideway acid in the treatment of infectious and inflammatory diseases of the skin and soft tissues" www.consilium.com.ua/stuff/doctor/dermatovenerologiya/Infekcii-koji-i-podkojnoi-kletchatki/Mesto-narujnyh-preparatov/).

Inflammatory skin diseases are among the most frequent pathologies in dermatology. This is due to the edge location of the skin, which leads to the contact and interaction with a variety of exogenous factors. The impact of biological factors (microor is Anisimov) on the skin is almost constant. The microorganisms present on the skin surface, under appropriate conditions can penetrate into the dermis, deponeras in the structural units of the lymphatic system and taking an active part in the formation of toxic-allergic component in the complex system the development of various pathological conditions dermatological profile.

Activated saprofita the microflora of the skin during development dermatopathologist processes has a significant impact on the development and course of primary skin diseases. Many drugs local and systemic application used in the treatment of dermatoses, inhibit the reactivity and immune defense of the organism, increasing the virulence and activity of saprophytic microorganisms. Resident microflora begins to take an active part as a background or pathogenic factor that has a significant impact on the development and course of many diseases ("Evaluation of the effectiveness of drug Fusiderm with pustular skin infections and acne", www.consilium.com.ua/stuff/doctor/dermatovenerologiya/Infekcii-koji-i-podkojnoi-kletchatki/fuziderm-preparat/).

In the treatment of purulent-destructive processes in the skin are widely used for the local application of antibiotics and combination with steroids such as ointment or cream Triderm" - whom inromania steroid remedy, containing a glucocorticoid (betamethasone), antimycotics (clotrimazole) and an antibiotic (gentamicin). Contraindications for the purpose of topical corticosteroids are fungal, meningitis, viral diseases of the skin, perioral dermatitis. With long-term use of halogenated steroids observed skin atrophy, telangiectasia, steroid acne, hypertrichosis, secondary infection. When used on large areas of skin may develop systemic side effects typical of glucocorticosteroids (Aghasyan "Drugs for the treatment of dermatitis", www.remedium.ru/drugs/drugs/detail.php&ID=t).

Preparations containing corticosteroids (ointments, drops)should not be used in viral diseases of the eyes and skin (including drugs with the addition of antibacterial agents), as well as in connection with the suppression of regeneration processes, the formation of common salt (Handbook of drugs. Hormones of the adrenal cortex and their synthetic analogs", http//pharm.stirol.net/med_search.php?action=show&namenum=751).

Using steroids can disrupt T-cell immune system, which plays an important role in the development of pyoderma (Taaloole, Mpharane. Bacterial skin infection: the problem of choosing the optimal antibiotic", www.rmj,ru/articles_3825.htm).

Thus, m is local treatment glucocorticosteroids in combination with antibacterial drugs do not always lead to the desired result, as it does not restore the immune function of the skin and even more disturbed by her microbiocenosis.

In the dermis of the skin and mucous membranes is a network of lymphatic and blood vessels, are cells of the immune system (T and b-limfocitica, Dandridge cells, natural killer cells and others)that ensures the participation of the skin and mucous membranes in the immune response. Inflammation, especially when purulent-destructive processes, develops a pronounced swelling, skin or mucous membrane infiltrate neutrophils, lymphocytes, eosinophils, they accumulate free radicals and other toxic products of metabolism, which enhance the degradation. In these conditions it is extremely difficult drug to inflammatory foci in their oral and injectable use.

Interferons (alpha, beta and gamma) protect the body from infection by viruses, bacteria and protozoa, inhibit the growth of malignant cells potentiate lymphotoxin. The action of interferon is carried out through a system of cellular synthesis of nucleic acids by a series of enzymes and inhibitors, leading to degradation of foreign genetic information. Interferons stimulate phagocytosis, the activity of natural killer cells, antigen expression. On the other hand, they can ENT is a thief in the formation of antibodies, the development of anaphylactic shock, inflammation, hypersensitivity of the delayed type, which makes interferons true immunomodulators, and interferon - important in the regulation of cellular homeostasis (//med.rehaexpo.ru/2005/participants/direct/production_4073.stm).

Exogenous interferons have drawbacks - allergenicity, toxicity, high price.

An alternative way, devoid of the disadvantages of exogenous interferon, is a stimulation of the synthesis of the body's own (endogenous) interferons. It is with drugs-interferonogenous (www.provisor.com.ua/arhive/2000/N20/cyclopheron.htm).

Known drug tricresol, which is an adaptogen and an immunomodulator, which when used in the form of tablets in complex therapy reduces the period of resuscitation in the treatment of patients with purulent-necroticism wounds, inhibits the growth of herpes, improving the immune status of the organism (Mgorshkov, Mrs. "Traceson - founder of a new class of immunomodulators and Immunostimulants (review)". Chemical and pharmaceutical journal. Volume 41, No. 1, 2007, p.3-7.). Traceson has interference activity. In the first hours after administration of trekrezan produced alpha - interferon, which later through the day is replaced by interferon - gamma (Pdelab and other "Immunomodulator Traceson: profile of General and immunotropic asset of the spine", http://www.nitek-group.ru/ru/innovations/trecrezane/profile.htm).

Antioxidant properties of trekrezan used in cosmetic compositions for topical use (Lifting cream "Traceson", http://old.ros-expo.com/wares_full/7486.html). However, tricresol not modulate the production of beta-interferon, which reduces its immunomodulatory effects, in comparison with other immunomodulators.

In currently known drugs for local and external use on the basis of trekrezan restoring the immune properties of the skin and mucous membranes in the treatment of purulent-destructive processes.

Known drug meglumine acridonacetate (trade name - cycloferon), which is a small molecule inducer of interferon, which has antiviral, immunomodulatory and anti-inflammatory effect. The main cells of the target of the drug is T - and b-lymphocytes. It stimulates the production of alpha-, beta - and gamma-interferon (up to 60-80 IU/ml and above) by leukocytes, macrophages, epithelial cells, and tissues of the spleen, liver, lungs, brain, enters the cytoplasm and nuclear structure, activates the synthesis of "early" interferons. Immunomodulatory effect is expressed in the correction of immune status in immunodeficiency States of various origins.

The drug has low toxicity. It has no Muta the military, teratogenic, embryotoxic and carcinogenic effects. In the form of tablets of 0.15 g (Description of the preparation of meglumine acridonacetate, (http://www.regmed.ru/InstrShow2.asp?InstrLinkNx=a51ba56ba55ba60b and in the form of 12.5% (0.125 g/ml) aqueous solution for intramuscular and intravenous cycloferon is used for the treatment of HIV infection, nairoviruses infection (serous meningitis tick-borne nature, multiple sclerosis, arachnoiditis), viral hepatitis (A, B, C, D), CMV and herpes infections, flu, cancer, immunodeficiency (postoperative period, burns, bronchitis, pneumonia and other), gastric ulcer and 12 duodenal ulcer, cancer, rheumatoid arthritis, deforming osteoarthrosis, spondylosis, skin diseases, atopic dermatitis, eczema, dermatitis, viral papillomas (Description of the drug, www.biomedservis.ru/preparat/pr_cycloferon_limment.htm). Its use enhances the antibacterial effect of antibiotics used in the treatment of acute intestinal infections (http://www.biomedservice.ru/preparat/pr_cycloferon_tabl.htm).

In the form of liquid ointment - liniment containing 5% N-metilglyukaminovoy salt greenexpo acid, 0.1% of an antiseptic katapola and 1,2-propilengikolya as the basis to 100%, cycloferon is used topically for the treatment of genital herpes, urethritis, balanoposthitis (nonspecific, Candida, gonorrhea, and Trichomonas etiology), Vagin is the bacterial and Candida), trichomonosis, skin diseases (drug Description www.znaharka.ru/index.php?productID=92430).

The drug is compatible with all drugs (including antibiotics, vitamins, drugs, immunomodulators, interferons (Description of the drug www.regmed.ru/ InstrShow2.asp?InstrLinkNx=a72ba78ba75ba74b).

Set high antibacterial and antichlamydial effect of the drug due to the activation of the immune system, as well as anti-inflammatory and antiproliferative effect of the drug. Immunomodulatory effect of cycloferon in the form of liniment is expressed in the correction of local immunity in immunodeficient States of different origin and autoimmune diseases. (Description of the drug www.znaharka.ru/index.php?productID=92430). The main cells producing interferon after administration of the drug in the form of liniment are lymphoid elements of the mucous membrane: macrophages, T - and b-lymphocytes, and epithelial cells (http://www.biomedservice.ru/preparat/pr_cycloferon_liniment.htm). The main area of application of 5% of cycloferon liniment is a topical treatment of herpes simplex and genital infections, sexually transmitted diseases.

It is known that the immune response to the action of cold is not more than 40% of patients (www.mtu-net.ru/doctor99/5nklassifik1polioxidoniy 2905.htm). The drug is available for local and external use in the form of liniment. This form is convenient for wew is wretling introduction, but inconvenient for external use, as it is not fixed on the surface of the affected area or wounds and dries quickly.

Known for one of the most powerful low-molecular inducers (endogenous) interferon - Celoron (www.amixin.ru), which is available as they orally drug (trade name "Amiksin", the statement on the drug http://www.regmed.ru/InstrShow2.asp?InstrLinkNx=41ba48ba44ba43b or "Lawmax", the statement on the drug http://www.regmed.ru/InstrShow2.asp?InstrLinkNx=a41ba48ba44ba43b).

It is used in the treatment of viral hepatitis a, b, C, Kirpichenko and CMV infection, the treatment of infectious-allergic and viral encephalomyelitis (multiple sclerosis, leukoencephalitis, weanteefult), chlamydial infections of the urogenital and respiratory tract, prevention of influenza and other acute respiratory viral infections.

Tilaran is a low molecular weight synthetic inducer of interferon stimulated in the body of interferons alpha, beta and gamma. The main producers of interferon in response to oral administration of tilorone are cells of the intestinal epithelium, hepatocytes, T-lymphocytes, neutrophils and granulocytes. After oral ingestion, the maximum production of interferons is in the sequence of intestine - liver blood through 4-24 hours. Tilaran in human leukocytes induces the synthesis of interferon stimulates stole the s cells in the bone marrow, depending on the dose increases antibody production, reduces the degree of immunosuppression, restores the balance of T-suppressor and T - helper cells. The antiviral mechanism of action is associated with inhibition of translation of virus-specific proteins in infected cells, resulting in suppression of reproduction of viruses. It is effective against pathogens of viral hepatitis, herpes viruses (including cytomegalovirus). (Instructions on the drug, http://www.regmed.ru/InstrShow2.asp?InstrLinkNx=a41ba48ba44ba43b). After oral administration tilaran rapidly absorbed their digestive tract. Oral bioavailability is 60%.

Tilaran quickly into the blood and distributed in organs, tissues and biological fluids. About 80% of tilorone associated with plasma proteins. Report the drug virtually unchanged in faeces (70%) and urine (9%) with a half-life of 48 hours. Tilaran in the body does not undergo metabolism and is not cumulated (Information about the drug "Amiksin", http://www.vidal.ru/vidal_main/doc_5533.htm).

Tilaran as a modulator of cytokine reactions and antioxidant, oral is used in secondary prophylaxis of multiple sclerosis (Vigalance and other "Secondary prevention of multiple sclerosis using the domestic drug Amiksin modulator of cytokine reactions and antioxidant",//home.peterstar.ru/nwams/amixin2.html).

Tilaran oral is used in complex therapy of tick-borne encephalitis (V. Tarasov "encephalitis". Medical paper No. 34, 2003, www.neuronet.ru/bibliot/b001/mg34_03.html).

Tilaran is not only effective antiviral agent, but also increase the body's resistance to infections caused by bacteria, fungi and protozoa. He has an activating effect on macrophages. This increases not only the absorption capacity of phagocytes, but also development of these cells reactive oxygen species, providing a bactericidal effect. Tilaran has a stimulating effect on the phagocytic and bactericidal function of macrophages, while reducing the intensity of the reaction of lipid peroxidation. It activates natural killer cells, which play a leading role in antitumor defense of the organism.

Tilaran as an inducer of interferon possesses an antitumor effect against virusinduced tumors. In combination with anticancer drugs, it encourages a more significant inhibition of tumor growth, reduces the frequency and degree of metastasis, sometimes completely preventing it. In large doses tilaran directly suppresses tumor growth. Tilaran in combination with cytotoxic drugs can reduce their dosage in half without changing the quantitative characteristics of the IR antitumor effect. It also reduces the severity of side effects of radiation therapy, and the introduction of patients before surgical intervention provides a more rapid healing of wounds, prevents metastasis and the development of infection.

Tilaran has anti-inflammatory activity, allowing you to use it effectively in the treatment of diseases such as multiple sclerosis, rheumatoid arthritis, silicosis. It inhibits platelet aggregation, while the magnitude of the effect is not inferior to aspirin, and the duration exceeds it. The local application on the damaged herpes skin and eyes he provides direct inactivation of herpes virus. (Toolipohja, Naholosko. "TILARAN: PROFILE of BIOLOGICAL ACTIVITY I. PHARMACOLOGICAL PROPERTIES http://magazine.odmu.od.ua/antropo/2006/1/18 .pdf).

Tilaran well compatible with antibiotics and traditional means of treatment of viral diseases (www.amixin.com.ua).

Tilaran easily soluble in water (about 10% at 20°C) and 95% ethanol (about 3.3% at 20°C) (Pharmacopeia enterprise Fund 42-0416-4243-03). This makes it promising for use in preparations for local and external use.

However, at present not known pharmaceutical preparations in the form of finished dosage forms for local and external use containing the active substance - tilaran.

Objectives the th present invention is the creation of pharmaceutical products for local and external use on the basis of low-molecular inducer of interferon as an active substance.

Technical results that may be obtained by using the present invention: expanding the field of application of the known active substances - tilorone, restoration of local immunity and biocenosis of the skin and mucous membranes in the treatment of purulent-destructive processes of the skin and mucous membranes, reduction of secondary necrosis of the tissues in the affected areas, improvement of microcirculation in the lesion, inflammation reactions, ensuring a high therapeutic activity and convenience in use, acceleration and improvement of healing.

To solve the stated problem, the present invention features a pharmaceutical product for local and external use, containing as active substance is a small molecule inducer of interferon and the basis, which as a low molecular weight interferon inducer contains Celoron, for example, in the following ratio of components (wt.%):

tilaranis 0.001-10,000;
base- the rest.

In accordance with the invention dosage forms for topical use on the basis of tilorone are liquid dosage forms, such as actuary for local use, suspensions and emulsions in the form of liniments, buttery soft medicinal forms, such as ointments, gels, creams, and also formed of soft medicinal forms suppositories and capsules for rectal or vaginal application.

As the basis in the preparation for topical application containing tilaran offers hyperosmolar substances or physiologically acceptable mixture of hyperosmolar substances, in combination with components that are specified, for example, rheological, Foundation requirements, depending on the dosage form of the drug.

It is known that in the intact Horny layer of the epidermis there are no channels through which could penetrate deep into the skin particles with sizes above 10 nm. Moreover, the larger the molecule, the lower its permeability through the TRANS-epidermal water barrier. It is established that substances with molecular weight of 100 kilodaltons not overcome TRANS-epidermal water barrier, i.e. this value is the limit of the permeability of the skin. Through the microchannels, which determine the permeability of the skin, characterized by the most probable intercellular path of transport of substances through the upper scaly keratin layer of the epidermis.

The most important role in the implementation of barrier-protective functions in the permeability of the skin plays state of water molecules present in microca illerich holes Horny and shiny skin layers. Water inside the microchannels is substantially in the structured condition, which significantly slows down the process of Brownian motion, which is responsible for the alignment of the concentration gradient, i.e. the permeability. Ordered structural organization of water in the micro capillary holes of the stratum corneum prevents intensive water evaporation from the skin surface, creating an additional barrier to the dehydration process. Nevertheless, water, oxygen, nitrogen and other low-molecular substances sufficiently easily diffuse through the skin. When this substance is able to react (contact) with fragments of the epidermis, including cellular systems, initially reach saturation in the epidermis, and then begin to interact with the deeper layers of the skin.

The intercellular substance of the epidermis and dermis gel is formed, for example, hyaluronic acid or of substances similar to it. This kind of gel, having a mesh structure is convenient to associate a variety of low - and high-molecular substances (salts, sugars, amino acids, vitamins, peptides, proteins, metabolic products of the cells of the epidermis and so on). The living cells of the epidermis with greater or lesser efficiency of the delayed portion of the substances that pass through the horn and flashing the s layers.

With regular use the same type of drug and cosmetics for external use processed these funds fragments of skin are in a constant state of saturation at which the concentration in the skin remains virtually unchanged. However, many low molecular weight components of the applied drug may quite easily overcome TRANS-epidermal water barrier. 60% plasma and 45% of the plasma proteins penetrate daily from microcapillaries of the circulatory system tissues, including the epidermis. Returning to the circulatory and lymphatic system, they carry with them associated protein metabolites (products of cell activity - toxins) and catabolites (biologically active substances, peptides, proteins, etc. are synthesized inside the cell). Substances to break the TRANS-epidermal water barrier, also appear in the blood and, accordingly, affect all tissues of the body.

When the destruction of living cells of the skin (for example, when purulent-destructive processes) of the cells are substances that stimulate, first of all, the local immune system (T-lymphocytes), activating located close to the damage of macrophages (Langerhans cells), which, in turn, synthesize and release into the environment a variety of stimulators of cell division, sposobstvovali violations of the cellular system. Langerhans cells reside in the basal layer of the epidermis. They have from 2 to 5 processes, penetrating to the granular layer and penetrating into the basement membrane. The role of these cells in the first place, is reduced to the speed regulation of cell division in the basal layer, in a variety of types of violations of its structure (Angelina. "theory of soft cosmetic effects. Modern cosmetology", Novosibirsk, "Nauka", 2000, www.golkom.ru/book/48_1.htm).

Thus, a basic requirement for products for local and external use with tilorone is the efficient transport of active substances to the cells responsible for the stimulation of local immunity and the immune properties of the skin and mucous membranes.

When local treatment of purulent-destructive skin lesions is important to the transport of active agents to the lesion through the TRANS-epidermal water barrier in the case of subcutaneous location of the hearth or in the depth of the wound if its superficial location. In addition, an important factor in successful therapy of purulent-destructive skin lesions is effective transport of toxic products of metabolism from the lesion to the skin surface. Most fully satisfy these requirements hydrophilic base with hyperosmolar properties.

Osmolar hydrophilic solvents, in the example aqueous solutions of salts, alcohols and aqueous solutions (in particular, ethyl or isopropyl), glycerine, low molecular weight polyethylene oxides (in particular, PEO-400), propylene glycols (in particular, 1,2-propylene glycol), and others, can easily penetrate transepidermal barrier or deep wounds, transporting dissolved active substance to the lesion, and displacing toxic products of metabolism out of the affected area. Due to their Smolarek properties they bind the water in the cellular systems subulate and granular layers, which leads to decreasing of cellular systems, and consequently increase the intercellular space and the cross section of microchannels, i.e. to increase the permeability of the epidermis. In addition, they thin the hyaluronic acid gel that fills the intercellular space, which is an additional factor increasing the permeability of the epidermis.

If hyperosmotic conditions are created by adding salt systems, the permeability of the epidermis which will increase even further due to changes in the structure of the micro capillary channels Horny and shiny layers, since the saturation of the cavities channels positively charged metal ions (like Na+structure of the channels are transformed into the structure (mechanism type "flip-flop") with the increased diameter of the channel for which no electrostatic repulsion of the positive charges, localized on the metal atoms (Angelina. "theory of soft cosmetic effects. Modern cosmetology", Novosibirsk, "Nauka", 2000, www.golkom.ru/book/48_1.htm).

To restore the immune function of skin and mucous membrane in the present invention is used for local and external use of small molecule inducer of interferon - tilaran. In the form of drugs for local and external application it can be used in dermatology in the treatment of purulent-destructive processes of the skin and soft tissues, such as recurrent furunculus, acne vulgaris, burns, nonhealing wounds of soft tissues, etc. in Addition, promising its use as drugs for local and external use in Allergology and immunology in complex treatment of allergic dermatoses, especially associated with fungal and herpes infection, and the treatment of urogenital infections, sexually transmitted diseases.

The local impact of tilaran increases expression on the cell membrane antigens major histocompatibility complex (HLA) class 1 and class 2 (HLA-DR), increases the quantity and improves the activity of NK-cells, causes targeted polarization Th0->Th1, modulates the inflammatory response, depending on the phase of inflammation, has a positive influence on the state of local immunity, today the direct and indirect effect on viruses, intracellular bacteria, fungi.

Celoron, being a low-molecular substance (molecular weight 483,5), dissolved in a hydrophilic liquid and hyperosmolar basis, with local and external use easily penetrates deep to the skin and mucous membranes, responsible for local immunity in the area of impact of the drug.

Tilaran having antioxidant properties, penetrates into the affected tissue of the hydrophilic base, reducing secondary tissue necrosis around the wound or lesion.

Using liquid low molecular weight hydrophilic and hyperosmolar basics and tilorone made solutions for local applications, lotions, liniments, emulsions and suspensions having a high penetrating power.

Adding hydrophilic solvents hydrophilic thickeners with sorption properties, such as high molecular weight polyethylene oxides (e.g., PEO-1500), proxamol (for example, proxanol is chosen-268), polyvinylpyrrolidone medical (for example, with molecular weight of 12600±2700 or 8000±2000), or other substances that have sorption properties (e.g., alginate calcium or magnesium), enhances the transport of toxic products of metabolism from the hearth subcutaneous lesions or depth of the wound to the skin surface.

So, for example, molecules PEO-1500 through DOS is high enough molecular weight stably retain the primary localization: they remain in the microchannels of the stratum corneum of the epidermis or in the wound cavity and actively associated inflammatory exudate, conveying it to the skin surface, with which the liquid evaporates. The released molecules PEO-1500 newly added to the water itself, and the process is repeated ("Theory and practice of local treatment of purulent wounds". Edited by Prof. Bamzatenka. Kiev, Health, 1995, str-235).

Soft hydrophilic and hyperosmolar basis consisting of low molecular weight hydrophilic solvent with hyperosmolar properties, hydrophilic thickener-sorbent and tilorone, are made of mild forms for local and external use: ointments, creams, gels, suppositories, with high penetration and absorption capacity.

From a microbiological point of view due to the presence of an external polysaccharide membranes and hydrophilic capsules in gram-negative and gram-positive bacteria, which prevent the penetration of microbial cells hydrophobic antibacterial substances, hydrophilic base is preferable, as are the conductors of medicines in the microbial cell ("Theory and practice of local treatment of purulent wounds". Edited by Prof. Bamzatenka. Kiev, Health, 1995, str).

The hydrophilic base, which can be applied tilorone in the proposed drug, divided into two groups:

water - soluble bases which, as a rule, contain purified water, hydrophilic nonaqueous R is storytale: polyethylene oxide, for example PEO-400, 1,2-propylene glycol, glycerin, ethyl cellosolve, dimexide, and water-soluble polymers include polyethylene oxide, for example PEO-1500, proxanol is chosen, for example proxanol is chosen-268, polyvinylpyrrolidone, for example 8000±200 or 12600±2700;

- vodosnabzhenie basis, which, in addition to water-soluble polymers and hydrophilic non-aqueous solvents, contain lipophilic substances: higher fatty alcohols, vaseline, vaseline oil, lanolin, waxes. These are the basics, as a rule, are of the emulsion type oil/water and require the presence of emulsifier type oil/water).

Basics with hyperosmolar properties play an important role in the local treatment of purulent-destructive lesions. They provide an outflow of purulent exudate from a wound or lesion, have anti-inflammatory effect due to absorption of fluid and reduce swelling, and also protect tissues from overhydration. Often they contribute to the strengthening of action of antibacterial agents.

For substances with high hyperosmolar properties include oxides - water-soluble polymerization products of ethylene oxide, which are physiologically indifferent compounds. In this class of substances are hydrophilic nonaqueous solvents (polyethylene oxide PEO-400, 1,2-propylene glycol, glycerin, ethyl cellosolve, dimexide) and emery (polyethylene oxide, for example, the polyethylene oxide PEO-1500, proxanol is chosen-268, polyvinylpyrrolidone). They are easy to apply on the wound surface and evenly it is distributed, improving the contact with the juvenile tissues and content wounds, mix well with wound exudate and retain their homogeneity, low toxicity and have no irritant action on the tissues, do not violate their physiological functions.

The ability of polyethylene oxides (PEO) to provide antimicrobial drug interstitial action fundamentally distinguishes this ointment base from fat frameworks or solutions of antibiotics (antiseptics), antimicrobial action of which is limited only by the surface of the wound, although it was deep microflora determines the intensity and direction of flow of a purulent process.

The main property of PEO is that they have a strong dehydrating (water-absorbing) action on the fabric. Due to its high ability to hydrogenate itself these polymers actively absorb wound exudate, and with it, and microbial toxins, Pro-inflammatory cytokines, products of tissue destruction, as well as various biologically active substances of lysosomal enzymes and other mediators of the inflammatory process, thereby interrupting its progressive course. Of fundamental importance is the fact that in festering wounds is or subcutaneous lesion dehydrating effect PEO applies not only to the fabric, but contained in the wound or lesion microbial cells.

Dehydration of microbial cells leads to a significant reduction of their biological activity, including resistance to the action of certain medicines. Therefore, in the presence of PEO tenfold increases antimicrobial activity of antibiotics. Is also important that the dissolution of antibiotics, sulfonamides and other substances in PEO increases their dispersion with increasing therapeutic activity, which also contributes to a more rapid release of the fundamentals of antimicrobial substances.

PEO is an active conductor of drugs through the skin barrier. Importantly, this penetrating without damage to the cells the ability of PEO increases in conditions of inflammation.

The hydrophilic base on the oxides can dissolve in the secrets of the mucous membranes, to fully release the medicinal substance, not to irritate, have a long shelf-life, high physiological indifference, which facilitates their use in liquid, buttery and formed of soft medicinal forms.

Important biomedical requirement ointment soft medicinal forms, is the ability to moisten the wound surface and to spread it, also decided that the Leno surface-active properties of solvents, polymers, surfactants and bases in General. The most pronounced surface activity are alcohols and ethyl cellosolve, which is unsuitable for inclusion in the composition of the base in high concentrations.

From glycols preferably the use of 1,2-propylene glycol and PEO-400 compared with glycerol, with a weak surface-active properties.

When mixed solvent PEO-400 polymer PEO-1500 latter acts as a thickener, which, depending on the number in the total mass is the desired consistency created the dosage form. In addition, PEO-1500 is an osmotically active substance, absorbing purulent exudate due to the binding of water molecules with hydroxyl and ether groups.

Proxanol is chosen-268 - oxides block copolymers of propylene and ethylene as osmotically active substance provides a more uniform nature of the absorption and has a longer period of osmotic action. The total mass of absorbed water solutions proxanol is chosen-268 24 hours significantly exceeds that in the case of the use of PEO-1500. This is due to the higher mass of proxanol is chosen-268 (8.7 times greater than that of PEO-1500).

The kinetics of water absorption solvents and polymers depends on their molecular weight, concentration, and molecular structure. For example, the EA-400 absorbs more water than 1,2-glycol, and has a longer period of osmotic action. Sorption activity of 1,2-propylene glycol is maintained for 4-6 hours. This is due both to lower its molecular weight compared to the PEO-400, and a lower hydrophilic-lipophilic balance (products HLB), which for propylene glycol is 9,38. The products HLB value is greater, the greater the hydrophilicity has substance. Therefore, the above products HLB and molecular weight, the stronger and longer will be apparent osmotic effect of a substance at a given concentration. 1,2-propylene glycol, PEO-400, PEO-1500, proxanol is chosen-268 can be preservatives in developing dosage forms ("Theory and practice of local treatment of purulent wounds". Edited by Prof. Bamzatenka. Kiev, Health, 1995, str; 227-235).

On the basis of polyethylene oxide PEO-1500 industrial produced hydrogel "Geco", representing colorless gel-like mass formed by ionizing radiation to a solution of polyethylene oxide in water. The gel is biologically inert, non-toxic. Is variable in a wide range of structural viscosity. Diluted when you add alcohol, glycerin, with vigorous stirring, the pH of a 20% aqueous suspension of 4.0 to 8.0. Chemical composition: PEO - 1500-3,5%; distilled water - 96,0%; preservative (sodium benzoate) is 0.5%. Used in the when asked the basis for the production of ointments, creams, gels, liniments in the pharmaceutical and cosmetic industry www.medpeterburg.ru/news/Out.aspx?Item=21284). The gel has on the enzyme stabilizing effect (patent RU №2089177, AK 7/48, 1997.09.10).

Dimexide - 30% solution of dimethyl sulfoxide (DMSO) is used as an anti-inflammatory drug for external use, inactivating hydroxyl radicals and improves the course of metabolic processes in inflammation. He also has a local anesthetic, analgesic and antimicrobial effects, has a moderate fibrinolytic activity. Penetrates the skin, mucous membranes, membrane microbial cells increases their sensitivity to antibiotics) and other biological membranes without damaging them and can hold a variety of medicines in the depth of the wound. ("Theory and practice of local treatment of purulent wounds". Edited Bamzatenka. Kiev, Health, 1995, 172-174).

Polyvinylpyrrolidone is a synthetic polymer that is inert to the body and not splitting enzyme systems, is the basis of detoxification blood fluid connecting toxic substances of different patterns and prints them out of the body. (Crosslease fluid, www.nedug.ru/libraru/doc.aspx?item=38053).

Hyaluronic acid is a polysaccharide from the family of glucosaminoglycans, has the ability to communicate with all possible is 1000 times more water than she weighs. Hyaluronic acid has the highest water absorption compared to other moisturizing agents such as glycerin and sorbitol. This absorbed water is retained within the gel and does not evaporate even at lower relative humidity of the surrounding air. Due to its high hydrophilicity, hyaluronic acid forms with water a high-viscosity gel that moisturizes the skin and mucous membranes. Hyaluronic acid is non-toxic. In the composition of the gels of hyaluronic acid has antimicrobial, wound healing and anti-inflammatory effect, helps the regeneration of the epithelium, prevents the formation of granulation tissue, adhesions, scarring, normalize circulation, does not cause clinical complications.

Hyaluronic acid has a positive effect on the course of local inflammatory processes, binds microflora, as well as the products of its decay and life, has a pronounced anti-inflammatory action and local anesthetic effect. At the same time, hyaluronic acid performs and mechanical protection of the Russian Academy of Sciences, as it forms thin film that prevents the penetration into the wound environmental factors - disease-causing agents. Gels based on hyaluronic acid used for the treatment of local and systemic inflammatory processes, term is ical and chemical burns, trophic ulcers in chronic venous insufficiency, radiation skin lesions, cracks, abrasions, and also for the treatment of nonhealing wounds of different etiology (patent RU №2195262, AK 9/06, 2002.12.27).

Sodium hyaluronate is the sodium salt of hyaluronic acid is soluble in water to form a viscous colorless gel with a pH of 6.0 and 7.5 (0.1% solution). In its activity of sodium hyaluronate complete analogue of hyaluronic acid, promotes tissue regeneration without the formation of scars, has the ability to stimulate cell migration and proliferation. Used in concentrations ranging from 0.01 to 0.5%.

Crasneanscki glycerokinase - new ointment base for cosmetic and medicinal preparations outdoor applications, as it combines the beneficial properties inherent in many other ointment bases. This gel is a good conductor of various drugs, anti-inflammatory, antitumor and antioxidant activity, capable to protect the tissue from drying out, fill them with oxygen, it is non-toxic, economical, stable during storage. The presence of silicon is beneficial for all types of tissues: epithelial, connective, skin, bone, contributes to reduction processes, increases blood flow. Due to the fact that glycerate silicon and glycerolic the gels based on them easily penetrate through the skin and conduct the medicinal substance, the dose of these substances in the pharmaceutical compositions can be lowered (www.uran.ru/gazetanu/2007/04/nu11/wvmnu_p3_11_042007.htm). Given the high transcutaneous activity kremniiorganicheskie of glycomolecules it can be used to create drugs local and external use, transdermal therapeutic systems. This gel can be used as a source of essential trace elements - silicon regulation silicon metabolism in the body (Bojakowska YEAR "Development crasneanscki of glycerokinase and comparative evaluation of their transcutaneous activity, dissertation, www.vita.chel.su/files/docs/diss/bojakovskii.doc).

View of the dosage form of the proposed pharmaceutical product depends on the molecular weight used hyperosmolar substances, their ratio in the mixture, the rheological properties of the mixture, and the quantitative ratio of hyperosmolar basis with other components of a pharmaceutical product. Based on these quantitative ratios and rheological properties of the mixture, dosage form of the proposed pharmaceutical product for local and external use can be a liquid, gel, cream, ointment or suppository.

Liquid and soft hydrophilic compositions on hyperosmolar basis also filled gelatin capsules for rektalnogo vaginal application.

Most preferred for external use is an ointment form, as it is well recorded and retained on the wound surface, longer has therapeutic activity, cheaper to manufacture, convenient in use, which increases the motivation of the patient to treatment.

Using tilorone and hydrophilic bases with hyperosmolar properties of the proposed composition of hydrophilic liquids for external and local use, hydrophilic ointments, hydrophilic creams, hydrophilic gels, which can also be used for the manufacture of suppositories and gelatin or other capsules for rectal and vaginal application.

Hydrophilic liquid, as hyperosmolar (solutions, emulsions, suspensions in the form of liniments), increase the permeability of the skin, effectively conveying the active substance - tilaran in the area of purulent-destructive lesions.

Hydrophilic ointments are hyperosmolar, resulting in the application, in addition to efficient transport of active substances in the area of purulent-destructive lesions may absorb a significant amount of exudate and bring it to the surface of the skin or mucous membrane.

Hydrophilic creams prepared on the basis of emulsions of the water/oil or water/oil/water, stabilized appropriate the emulsifiers. It also includes colloidal disperse system consisting of a dispersed in water or mixed water-glycol solvents, higher fatty alcohols or acids, stable hydrophilic surface-active substances. Creams are a two - or multiphase dispersed system, a dispersive medium which when installed the storage temperature, as a rule, has a Newtonian type currents and low values of rheological parameters. The effect of hydrophilic creams on the basis of similar effect ointments, hydrophilic on the basis of, but they have a lower viscosity than ointments, therefore, more easily penetrate transepidermal barrier and the depth of the wound. On rheological properties they occupy an intermediate position between the liquid and ointment.

Hydrophilic gels (hydrogels) prepared on bases consisting of water, hydrophilic or mixed non-aqueous solvent (glycerol, 1,2-propylene glycol, polyethylene oxide PEO-400) and the hydrophilic gelling (carbomer, derivatives of cellulose, tragakant, sodium hyaluronate, hyaluronic acid and others). In addition, the currently developed new hydrophilic gels mentioned above. Gels are one-, two - or multiphase dispersed liquid dispersive medium, the rheological properties of which m is owley the presence of geleobrazovanie in relatively small concentrations. In this dosage form, geleobrazovanie additionally can act as stabilizers of disperse systems: suspensions or emulsions.

Hydrophilic gels, containing bound water, do not have such a dehydrating effect, as liquids, creams or ointments, hydrophilic on the basis hyperosmolar properties. They moisturize the inflammation, protecting the wound from drying out. This reduces heat dissipation gel-coated part of the surface, causing it to warm. Under a layer of gel, the moisture does not evaporate, the top layers of skin or mucous membrane marirosa (razmokajut), which promotes absorption through the thickness of the skin of various medicinal substances contained in the composition of the gel. When this active substance and the target of the additive contained in the hydrophilic layer of gel on the skin surface or mucous membrane, diffuse through transepidermal barrier. Gels are appropriate to apply in the process of healing, when there is no need for drainage of lesion of toxic products purulent-destructive lesions.

Hydrophilic suppositories prepared on hydrophilic hyperosmolar the basics, easy to dissolve in the rectal or vaginal application, homogeneously distributed mucous medicinal substances have on the body, both local and resorb the passive action.

Gelatin capsules for rectal and vaginal application of more promising compared to suppositories with technology, biopharmaceutical and economic point of view. Gelatinous sheath protects the medicinal substance from the effects of environmental factors and has advantages over the suppositories, as it can capsulitis substances in the form of ointment, liniment, cream, gel, emulsion, suspension, etc.

Drug release is faster and easier than suppositories, as under the influence of a slightly alkaline environment (pH of 7.3 and 7.6) mucous membranes of the gelatinous shell swell, and in this state, even a weak impact on them is sufficient to rupture and release the contents. The amount of medicinal substance in the capsule, providing the desired therapeutic effect, is a double dose suppositories.

Thus, the production of rectal and vaginal funds in the gelatin shell saves costly biologically active ingredients and to reduce the cost of drugs. Rectal gelatin capsules with the proposed pharmaceutical product meet all the requirements of an ideal suppositories and can be used in medicine for the treatment of proctologic diseases, and vaginal gelatine capsules what is for the treatment of diseases of the genitourinary system in women.

Small molecule inducer of interferon (synthetic immunomodulator) - tilaran in the proposed pharmaceutical drug restores the local immunity of the skin and mucous membranes, which promotes more rapid healing of purulent-destructive lesions, increases the body's resistance to skin diseases and diseases of the mucous membrane due to the suppression of viral, bacterial and fungal infections. Antioxidant properties of tilorone also promote faster healing by reducing tissue necrosis.

The use of hydrophilic and hyperosmolar basis in the proposed pharmaceutical product ensures fast delivery of the active substance as to microbial cells and to the cells of the tissue that enhances therapeutic activity of the proposed drug. In addition, digidrive hydrophilic base cells of gram-positive and gram-negative microorganisms reduces their resistance to the damaging effects of substances with antibacterial activity against gram-positive and/or gram-negative bacteria. It also enhances therapeutic activity of the preparations.

The use of hyperosmolar basics additionally improves microcirculation in the loci for the e destruction due to its dehydrating action, as well as providing additional anti-inflammatory effect due to absorption of fluid and reduce swelling of the lesion. Hyperosmolar Foundation provides outflow of purulent exudate from the lesion and prevents tissue from overhydration. It can easily be applied to the surface of the lesion, well it is charged evenly it is distributed, improving the contact with the juvenile tissues and contents of the lesion, it penetrates beneath the scab, mixes well with wound exudate, while maintaining its homogeneity, low-toxic and does not intrude on the fabric, does not violate their physiological functions.

The dissolution of the active substance in polietilenoksidnoy basis improves their dispersibility and the ability to more rapid release of the framework, thereby increasing therapeutic activity of the proposed drug. This basis is the conductor of the active substances through the skin barrier, with such penetrating without cell damage ability is enhanced in conditions of inflammation. Hydrophilic is based on the oxides can dissolve in the secrets of the mucous membranes, completely releasing the drug substance is not irritating when this mucous has a long shelf-life and high physiological indifference.

The drug is ucaut by mixing the components with known methods.

The implementation of the present invention is illustrated by the following examples, but is not limited to them.

Example 1. Solution for external and local application No. 1.

100 g of 5% solution contains:

tilaran- 5,00;
sodium chloride- 0,60;
calcium chloride- 0,01;
magnesium chloride- 0,0005;
zinc chloride- 0,00025;
manganese chloride- 0,00055;
polyvinylpyrrolidone 8000±2000- 6,00;
purified waterto 100 g

Example 2. Solution for external and local application No. 2.

100 g of 3% solution contains:

tilaran- 3,0;
the polyethylene oxide-400- 10,0;
purified waterto 100 g

Example 3. Solution for external and local PR the changes No. 3.

In 100 g of 2% solution contains:

tilaran- 2,00;
dimexide- 5,00;
nipagin- 0,08;
glycerin- 20,00;
purified waterto 100 g

Example 4. Liniment No. 1.

100 g of 5% liniment contains:

tilaran- 5,0;
1,2-propylene glycol- 60,0;
purified waterto 100 g

Example 5. Liniment No. 2.

100 g of 3% liniment contains:

tilaran- 3,0;
1,2-propylene glycol- 50,0;
proxanol is chosen-268- 10,0;
purified waterto 100 g

Example 6. Liniment No. 3 (emulsion).

In 100 g of 2% emulsion contains:

tilaran- 2,0;
the gel of polyethylene oxide-1500- 20,0;
purified waterto 100 g

Example 7. Cream No. 1.

100 g of 5% cream contains:

tilaran- 5,00;
vaseline- 22,00;
glycerin- 17,00;
1,2-propylene glycol- 12,00;
emulsifier No. 1- 10,00;
phosphate buffer solution- 14,00;
purified waterto 100 g

Example 8. Cream No. 2.

100 g of 3% cream contains:

tilaran- 3,00;
vaseline- 22,00;
glycerin- 17,00;
1,2-propylene glycol- 12,00;
- 10,00;
phosphate buffer solution- 14,00;
purified waterto 100 g

Example 9. Cream No. 3.

In 100 g of 2% cream contains:

tilaran- 2,00;
1,2-propylene glycol- 35,00;
PEO-400- 25,00;
proxanol is chosen-268- 18,00;
purified waterto 100 g

Example 10. Ointment No. 1.

100 g of 5% ointment contains:

tilaran- 5,0;
proxanol is chosen-268- 18,00;
1,2-propylene glycol- 42,00;
the polyethylene oxide PEO-400- 28,00
purified waterto 100 g

Example 11. Ointment No. 2.

100 g of 3% ointment contains:

tilaran- 3,0;
the polyethylene oxide PEO-400- 67,0;
the polyethylene oxide PEO-1500- 17,0
purified waterto 100 g

Example 12. Ointment No. 3.

In 100 g of 2% ointment contains:

tilaran- 2,00;
nipagin- 0,08;
glycerin- 20,00;
the sodium carboxymethyl cellulose- 3,50;
zinc oxide- 3,00;
purified waterto 100 g

Example 13. Gel No. 1.

100 g of 5% gel contains:

tilaran- 5,00;
the gel of polyethylene oxide 1500to 100 g

Example 14. Gel No. 2.

100 g 3% gel contains:

tilaran- 3,00;
nipagin- a 0.1
the polyethylene oxide PEO-400- 30,00;
sodium hyaluronate- 0,50;
purified waterto 100 g

Example 15. Gel No. 3.

In 100 g of 2% gel contains:

tilaran- 2,00
glycerokinase based glycerate silicon- 50,0;
purified waterto 100 g

Example 16. The mixture for the preparation of suppositories No. 1.

100 g of a 5% mixture for the preparation of suppositories contain g:

tilaran- 5,0;
proxanol is chosen-268- 68,0;
the polyethylene oxide-400- 17,0;
purified waterto 100 g

From this mixture made 300 pieces rectal suppositories in the form of "cigars" with a diameter of 10 mm, a weight of 2.5 g containing tilorone 0.125 g in one suppositories. Rastvorimo the e suppositories in the hydrophilic base is not more than 1 hour at a temperature of (37±1)°C, that meets the requirements of the global Fund XI (stapostol, p.151-153).

Example 17. The mixture for the preparation of suppositories No. 2.

100 g of a 5% mixture for the preparation of suppositories contain g:

tilaran- 5,0;
the polyethylene oxide-1500- 68,0;
the polyethylene oxide-400- 17,0;
purified waterto 100 g

From this mixture made 300 pieces rectal suppositories in the form of "cigars" with a diameter of 10 mm, a weight of 2.0 g containing tilorone 0.1 g in one suppositories. The solubility of the hydrophilic suppositories basis is no more than 1 hour at a temperature of (37±1)°C, which complies with the requirements of the global Fund XI (Art. Suppositories, p.151-153).

Example 18. The mixture for the preparation of suppositories No. 3.

100 g of a 5% mixture for the preparation of suppositories contain g:

tilaran- 5,0;
dimexide- 3,0;
proxanol is chosen-268- 66,0
the polyethylene oxide-400 - 8,0
purified waterto 100 g

From this mixture made 300 pieces rectal suppositories in the form of "cigars" with a diameter of 10 mm, a weight of 2.5 g containing tilorone 0.125 g in one suppositories. The solubility of the hydrophilic suppositories basis is no more than 1 hour at a temperature of (37±1)°C, which complies with the requirements of the global Fund XI (Art. Suppositories, p.151-153).

Example 19. Gelatin capsules.

Ointment of example 10 is filled 500 piece gelatin capsules No. 00, the volume of 0.95 ml Raspadaemost received capsules less than 20 min, which meets the requirements of the global Fund XI (Art. Capsules, str).

Based on the proposed solutions created a number of new drugs in the form of liquid and soft dosage forms containing the active substance tilaran.

The proposed remedies on the basis of tilorone and hydrophilic hyperosmolar basis significantly expand the scope of application of the known active substances - tilorone, ensure restoration of local immunity and biocenosis of the skin and mucous membranes in the treatment of purulent-destructive processes of the skin and mucous membranes, reduce secondary tissue necrosis in the affected areas associated with excessive free radical oxidation, improve microcirculation in the lesion, cropped inflammatory reactions in to the e, have a high therapeutic activity, convenient to use.

Still similar or identical solution has not been proposed, although the drug tilaran known since 1970 (Toolipohja, Naholosko. "TILARAN: PROFILE of BIOLOGICAL ACTIVITY I. PHARMACOLOGICAL PROPERTIES http://magazine.odmu.od.ua/antropo/2006/1/18 .pdf).

The above set of features of the proposed pharmaceutical product (composition of the drug, the quantitative ratio of the components and dosage form) was not previously known, which indicates the novelty of the proposed solution.

The set of essential features of the claimed pharmaceutical preparation for external use on the basis of tilorone should not be explicitly studied the prior art, has significant differences from the one considered analogues. Therefore, the applicant believes that the proposed pharmaceutical product for local and external application on the basis of tilorone involves an inventive step.

The inventive pharmaceutical preparation may be recommended in the treatment of purulent-destructive lesions of skin and mucous membranes.

We offer pharmaceutical preparation for topical application on the basis of tilorone can be used for industrial mass production of liquid and soft medicinal forms, such as solutions, emulsions, suspense and, liniments, ointments, creams, gels, as well as for industrial production generated soft medicinal forms: suppositories and gelatin capsules for rectal and vaginal application.

1. Pharmaceutical composition for treatment of purulent-destructive lesions of the mucous membrane, characterized in that it contains tilaran mixed with soft formed the basis and in the form of a rectal or vaginal suppositories in the following ratio, wt.%:

tilaranof 0.05-10,000
soft formed the basisrest

2. The pharmaceutical composition according to claim 1, characterized in that as a mild form bases it contains hyperosmolar substances selected from the range: proxanol is chosen-268, polyethyleneoxide-1500, polyethylene oxide-400, or their physiologically acceptable mixture with components that provide rheological requirements for soft-generated basis.

3. Pharmaceutical composition for treatment of purulent-destructive lesions of skin and mucous membrane, characterized in that it contains Celoron, mixed with soft base, and is made in soft form: ointment or cream or gel in the following ratio, wt.%:
tilaranof 0.005-10,000soft baserest

4. The pharmaceutical composition according to claim 3, characterized in that as soft bases it contains hyperosmolar substances selected from the range: proxanol is chosen-268, polyethyleneoxide-1500, dimexide, glycerin, 1,2-propylene glycol, a polyethylene oxide gel 1500, glycerokinase based glycerate silicon or their physiologically acceptable mixture, purified water in a mixture with components that provide rheological requirements for soft base, selected from the range: sodium carboxymethyl cellulose, sodium hyaluronate, vaseline, emulsifier No. 1, zinc oxide.

5. Pharmaceutical composition for treatment of purulent-destructive lesions of skin and mucous membrane, characterized in that it contains Celoron, mixed with a liquid base, and comes in a liquid form: suspension or emulsion in the following ratio, wt.%:

tilaranof 0.005-10,000
liquid Foundationrest

6. The pharmaceutical composition according to claim 5, characterized in that as the liquid base it contains hyperosmolar the substances, chosen from a number of: polyvinylpyrrolidone, polyethylene oxide-400, 1,2-propylene glycol, glycerol, proxanol is chosen-268, polyethyleneoxide-1500, polyethylene oxide gel-1500 or their physiologically acceptable mixture.

7. Gelatin capsules for rectal or vaginal application, characterized by the fact that they filled the pharmaceutical composition according to claim 3 or 5.



 

Same patents:

FIELD: beiotechnology.

SUBSTANCE: invention concerns production of items with expressed bioactivity and can be applied as healing and preventive medicine in medical cosmetology, balneology, medicine and veterinary. Method involves extraction of bioactive substances from unossified antlers at 40°C or lower temperature, conservation and gelatinisation agent addition to obtain aqueous solution of conservation agents represented by methylparaben and propylparaben. Extraction of bioactive substances is performed by conservation agent extraction to the solution by ultrasonic method in cavitation mode at weight ration of unossified antlers to aqueous solution of 1:1-10 for time period sufficient to obtain required extract concentration. Carbopol is used as gelatinisation agent and mixed with distilled water preliminarily and aged till imbibition, then neutralising agent is added in amount sufficient to form gel mass, further neutralised by adding citric acid solution to 6-7.5, and aqueous solution of unossified antlers and 1-30 wt % of water retentive component are added to obtained gel mass in portions with stirring.

EFFECT: obtaining high-quality gel based on aqueous solution of unossified antlers by ultrasonic extraction of bioactive substances.

2 cl, 5 ex, 2 tbl

Wound dressing // 2349348

FIELD: medicine.

SUBSTANCE: invention concerns medicine, particularly media of surfacial wound and burn treatment, and can be applied in surgery, traumatology, therapy, ophthalmology, veterinary and adjoining fields. Wound healing medium is superexpanding polymer matrix including collagenase in amount of 1-10 wt % of matrix weight. Superexpanding polymer matrix is a matrix obtained by copolymerisation of at least two monomers of group including maleic, crotonic and acrylic acids and/or their derivatives in the presence of binding agent.

EFFECT: efficient wound healing agent viable for composition standardisation.

5 cl, 3 tbl, 4 ex

FIELD: medicine.

SUBSTANCE: method of obtaining wound bandage material is claimed. Method involves obtaining protein polymer by protein reaction with polyfunctional spacer or its activated derivative. Preferred polyfunctional spacer is polycarboxylic acid, especially dicarboxylic acid. Protein polymers obtained with such spacers can be applied in a wide range of therapeutic purposes, including wound bandage materials, therapeutic agent delivery to organism, and bioadhesive and sealing substances.

EFFECT: obtaining material taking exact shape of wound filling wound hollow completely without irritation of exposable tissues.

27 cl, 2 dwg, 13 tbl, 12 ex

FIELD: medicine; pharmacology.

SUBSTANCE: invention represents pharmaceutical composition for treatment of purulo-destructive affections of skin and mucous membranes, applied for external and local use and characterised by that it contains Tilorone and base additives chosen from group: substance of antibacterial activity in respect to gram-positive and/or gram-negative bacteria, antimicotic, local anaesthetic, reparative process stimulator, hypooxidiser, biogenic elements and base, or their mixture in certain ratio.

EFFECT: extended application of Tilorone, restored local immunity and biocoenosis of skin and mucous membranes associated with treatment of purulo-destructive skin processes, provided anaesthetic effect; additional stimulation of reparative processes; improved microcirculation in lesion focus, reduced inflammatory reactions, ensured high therapeutic activity and useability, accelerated and improved healing.

10 cl, 19 ex

FIELD: medicine; dermatology.

SUBSTANCE: in addition to Griseofulvin, Pioployphage is introduced orally in dosage 30-50 ml or on 1-2 tablets twice a day within 14 days.

EFFECT: antibacterial action, nonspecific phagocytosis stimulation, intensified immune response on infestant antigen, escaping complications associated with secondary pyogenic infection.

4 tbl, 2 ex

FIELD: medicine; phlebology.

SUBSTANCE: to treat chronic indolent trophic ulcers of different genesis, chloroquine is administered during 4 weeks: by 0.5 g during first and second week, and by 0.25 g during third and fourth week. Additionally, prednisolone is injected by 10-15 mg during first and second week, then dose is reduced by 2.5 mg every week until the drug is repealed; as well, vasoprostane intravenous infusion is conducted by 20 mcg in physiologic solution, twice a day, during 10 to 20 days.

EFFECT: effective treatment for chronic indolent trophic ulcers of different genesis due to tissue perfusion increase, humoral and cellular regulating mechanisms activation by complex medicines action.

3 ex

FIELD: medicine; pharmacology.

SUBSTANCE: treatment-and-prophylactic glutinous Pasta contains N - (β-oxyethyl)-4,6-dimethyl-dihydro-pyrimidon-2 (ximedon), Hidrocortizonum hemisuccinate, boracic acid, zinc oxide, glycerine, gelatin and distilled water.

EFFECT: prevention of complications development, reduction of terms of treatment.

2 ex

FIELD: medicine.

SUBSTANCE: means include biopolymer carrier and cells, applied on carrier mentioned, and characterised as follows: the biopolymer carrier represents collagen-chitosan film, or crumbs of collagen-chitosan film, or high polymer gel in form of 5% macrogol-1500 solution; the cells are diploid human lung strain "ФЭЧ" 16-1 cells, or diploid human musculo-cutaneous tissue strain "ФЭЧ" 16-2 cells in concentration 2.0-3.0×105 to 1 cm2 of film or crumb carrier, or 1.0×106 to 1 ml carrier in form of 5% macrogol solution high polymer gel.

EFFECT: novel means production for replacement therapy based on standard certified cell material, possibility of optimal means form selection, reducing therapy duration, and widening field of application in replacement therapy.

3 cl, 17 ex, 3 tbl

FIELD: medicine.

SUBSTANCE: preparation represents mix of calendula flowers oil extract, cottonweed herb, camomile flowers, dog-rose seeds, and St. John's wort herb, taken in proportion as follows, in g to 3.0 l unrefined sunflower oil: calendula (flowers) 100.0, cottonweed (herb) 100.0, camomile (flowers) 100.0, St. John's wort (herb) 150.0, dog-rose (seeds) 35.0, unrefined sunflower oil 3.0 l; and 40% alcohol solution, containing 0.5% Novocain injection solution, 50% analgin injection solution, 70% calendula tincture, aloe juice, menthol powder, anesthesin powder, taken in proportion as follows, in ml: 0.5% Novocain injection solution 25.0, 50% analgin injection solution 10.0, 70% calendula tincture 20.0, aloe juice 25.0, menthol (powder) 12.0 g, anesthesin (powder) 12.0 g, 40% alcohol solution 500.0; 8.0 ml of the oil extract being added to 40% alcohol solution.

EFFECT: quickened wound epithelisation, quickened necrotic tissues rejection, shortened wound repair period, and stimulation of new granulation tissue development with rapid maturation.

3 ex

FIELD: medicine; dermatology.

SUBSTANCE: preliminary wound sanitization by 2-5% aqueous argovit solution is carried out. Then silver electrophoresis is performed with the use as anode of padding polyester stripes modified by silver. After that a dressing by 2-5% argogel is carried out.

EFFECT: effective treatment due to antibacterial influence prolongation and trophicity improvement in damage zone.

5 ex

FIELD: medicine; pharmacology.

SUBSTANCE: invention represents pharmaceutical composition for treatment of purulo-destructive affections of skin and mucous membranes, applied for external and local use and characterised by that it contains Tilorone and base additives chosen from group: substance of antibacterial activity in respect to gram-positive and/or gram-negative bacteria, antimicotic, local anaesthetic, reparative process stimulator, hypooxidiser, biogenic elements and base, or their mixture in certain ratio.

EFFECT: extended application of Tilorone, restored local immunity and biocoenosis of skin and mucous membranes associated with treatment of purulo-destructive skin processes, provided anaesthetic effect; additional stimulation of reparative processes; improved microcirculation in lesion focus, reduced inflammatory reactions, ensured high therapeutic activity and useability, accelerated and improved healing.

10 cl, 19 ex

FIELD: medicine; phthisiology.

SUBSTANCE: in addition to standard antituberculous therapy, hydrogen peroxide is injected to patient from the first day of treatment in homeopathic potency 6 CH by 5 granules 3 times per day for four months.

EFFECT: reduction of abacillation terms and closure of decay cavities due to higher activity of catalase, lower level of endogeneous hydrogen peroxide level and production of destructive factors, and activation of isoniazid under effect of potentiated hydrogen peroxide.

2 tbl, 2 ex

FIELD: medicine; pharmacology.

SUBSTANCE: are offered application of Safinamid from 0.5 to 1,2,3,4 or 5 mg/kg/day, in a combination with levodopa/PDI (peripheral antioxidant of decarboxylase: levodopa plus carbidopa (SINEMET®), levodopa plus carbidopa of controlled release (SINEMET-CR®), levodopa plus benserazide (MADOPAR®), levodopa plus benserazide of controlled release (MADOPAR-HBS) for treatment of Parkinson's disease, the corresponding set and the pharmaceutical composition.

EFFECT: additional effect of increase in frequency of revealing of the patients reacting to treatment with dopamine agonist.

8 cl, 2 tbl

FIELD: medicine; pharmacology.

SUBSTANCE: invention concerns medical product for metabolic regulation associated with magnesium deficiency in organism. Medical product is solid dosage form containing magnesium di-(L-asparaginate) in amount 200 to 1000 mg and pyridoxine hydrochloride in amount 2 to 20 mg per unit dose (magnesium di-(L-asparaginate) and pyridoxine hydrochloride in weight ratio 50:1 to 200:1).

EFFECT: medical product provides high ion bioavailability and decreased excretory system burden.

8 cl, 5 ex, 3 tbl

FIELD: medicine, in particular balneology and physical therapy.

SUBSTANCE: claimed additive contains dihydroquercetin or mixture of dihydroquercetin and milky whey in ratio from 2:1 to 1:2 as biologically active additive for balneological bath agent. Dalneological bath agent includes base, osmolytically active components such as glycerol and inorganic salts, as well as biologically active additive of plant and/or animal origin, wherein osmolytic activity is 7700-11000 mOsm/l. As biologically active additive of plant and/or animal origin it contains dihydroquercetin or mixture of dihydroquercetin and milky whey in ratio from 2:1 to 1:2 and as the base it contains water and/or concentrated milk in the next component ratio (mass %): glycerol 25.0-30.0; inorganic salts 10.0-15.0; dihydroquercetin or mixture of dihydroquercetin and milky whey 0.2-1.0; and balance: water and/or concentrated milk up to 100 %.

EFFECT: new effective additive for balneological bath agent.

5 cl, 9 ex

FIELD: medicine, gastroenterology, pharmacy.

SUBSTANCE: invention relates to a pharmaceutical composition used in treatment of diseases of digestive tract accompanying with disturbance of acid formation in stomach and/or ulceration of stomach and/or duodenum mucosa. The composition comprises sucralfate in a single dose from 0.25 g to 1.0 g or aluminum phosphate in a single dose from 3.8 g to 16.0 g, and prebiotic - fructooligosaccharide in a single dose from 2.5 g to 16.0 g and this composition is taken 1-3 times per 24 h. Also, invention relates to a method for preparing and using this composition. Proposed pharmaceutical composition promotes to acceleration of ulcer defect epithelization being independently on areas of ulcer defect and acidity of the stomach content.

EFFECT: improved and valuable medicinal properties of pharmaceutical composition.

8 cl, 8 tbl, 8 ex

FIELD: medicine.

SUBSTANCE: method involves cutting out mucoperiosteal flap, making curettage and antiseptic treatment. Bone defect is filled with medical composition comprising Furacilin, aminocapronic acid, dimethylsulfoxide, glycerol, Chitosan, gelatin and water. Membrane cover is applied. The membrane has Furacilin, dimethylsulfoxide, acetic acid, glycerol, Aerosyl, Chitosan and water. The wound is covered with the mucoperiosteal flap and sutured.

EFFECT: enhanced effectiveness of treatment; prolonged hemostatic, antimicrobial and wound-healing action.

FIELD: veterinary science.

SUBSTANCE: invention proposes using disinfecting preparation "Lesiptik" as a preparation for prophylaxis or respiratory diseases in calves. Invention provides enhancing safety of claves to 100% and increasing daily average gains by 24.5%.

EFFECT: valuable properties of preparation.

1 tbl, 3 ex

The invention relates to medicine, in particular to abdominal surgery

The invention relates to beekeeping, in particular can be used to treat bees from varroa

FIELD: veterinary science.

SUBSTANCE: invention proposes using disinfecting preparation "Lesiptik" as a preparation for prophylaxis or respiratory diseases in calves. Invention provides enhancing safety of claves to 100% and increasing daily average gains by 24.5%.

EFFECT: valuable properties of preparation.

1 tbl, 3 ex

Up!