RU2359664C1 - Pharmaceutical injection composition on basis of tilorone for treatment of purulent-destructive processes with signs of immune insufficiency - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention concerns a chemicopharmaceutical industry, and also to medicine and veterinary science and represents a pharmaceutical injection composition for treatment of the purulent-destructive processes, characterised that it contains Tilorone and a hydrophylic dissolvent, where as a hydrophylic dissolvent it contains the substances chosen from a number: the emulsion of perfluoroorganic bonds, an isotonic solution of sodium chloride or their admixture, and in addition contains Novocainum; thereat, the components in the composition are in a certain mass parity.

EFFECT: tilorone application expansion, restoration of local immunity and a biocenosis of a skin and mucosas at treatment of purulent-destructive processes of skin and mucosas, especially at a deep locating of the centres of a lesion, depression of a secondary necrosis of tissues on the amased sites, cupping of inflammatory reactions, maintenance of local anesthetic effect, healing acceleration.

3 cl, 1 ex, 2 tbl

Description

The invention relates to the chemical and pharmaceutical industry, as well as medicine and veterinary medicine, namely to pharmaceutical preparations used in the treatment of purulent-destructive processes of the skin, mucous membranes, etc., especially with deep subcutaneous location of lesions with clinical and laboratory signs of immune deficiency for example, such as chronic recurrent furunculosis, herpetic lesions of the skin and mucous membranes, atopic dermatitis complicated by bacterial-fungal infections, trophic ulcers s, postoperative suppuration of wounds to promote healing.

The intensity of the infectious process depends on the number and virulence of the pathogen, the state of natural barriers and the resistance of the microorganism. Susceptibility for most infections is individual and usually due to a lack of immunity. The infectious factor takes a leading place in the pathogenesis of such common inflammatory diseases of the skin and soft tissues as acne, boils, carbuncles, impetigo, abscess, phlegmon, etc.

Infections caused by opportunistic microorganisms occur in people with deficits in the immune system, when a small dose of microorganisms that do not infect people with a normal immune system is enough. The balance between macro- and microorganisms can be disturbed by both exogenous and endogenous factors (impaired neuroendocrine system, immunodeficiency, depletion of the body's adaptation mechanisms, concomitant chronic pathology, etc.). Failure of the body's immune response to an infectious factor entails a chronicization of the infectious process.

The degree of pathogenicity of microorganisms is individual and determines the different activity of the body's immune response to them. It is associated with the ability to attach to sensitive cells (adhesion), multiply on their surface, penetrate into these cells or underlying tissues, overcome non-specific and specific factors of immunity, have an immunosuppressive effect (Kutasevich YF, Ogurtsova AN “The place of the outside preparations containing fusidic acid in the treatment of infectious 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 one of the most common pathologies in dermatovenereology. This is due to the borderline location of the skin, which leads to contact and interaction with various exogenous factors. The effect of a biological factor (microorganisms) on the skin is almost constant. Microorganisms located on the surface of the skin, under appropriate conditions, can penetrate the dermis, deposited in the structural units of the lymphatic system and take an active part in the formation of the toxic-allergic component in the complex system of development of various pathological conditions of the dermatological profile.

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

In the dermis of the skin and in the mucous membranes there is a network of lymphatic and blood vessels, cells of the immune system (T- and B-lymphocytes, dendrides cells, natural killers, etc.) are concentrated, which ensures the participation of the skin and mucous membranes in the immune response. With inflammation, especially with purulent-destructive processes, severe edema develops, the affected area is infiltrated by neutrophils, lymphocytes, eosinophils, free radicals and other toxic metabolic products accumulate in them, which further increase the destruction. Under these conditions, access to medications for inflammatory foci is extremely difficult with their oral administration, and with a deep location of the lesion foci - with external and local application.

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

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

An alternative way, devoid of the disadvantages inherent in exogenous interferon, is to stimulate the synthesis in the body of its own (endogenous) interferons. It is carried out using interferonogen preparations (www.provisor.com.ua/arhive/2000/N20/cyclopheron.htm).

Immunomodulating injectable preparations based on low molecular weight synthetic peptides with immunoregulatory properties are known, for example, thymogen, immunofan, glutoxim, thymalin, tactivin and others. These drugs have low efficiency due to the rapid destruction of low molecular weight peptides in the body. Their life time in the body is several minutes (www.mtu-net.ru/doctor99/5nklassifik1polioxidoniy2905.htm).

Known immunomodulating drug polyoxidonium, available in the form of a lyophilized mass, which is dissolved immediately before injection in an isotonic solution of sodium chloride or water for injection to prepare an injection solution. For intravenous (drip) administration, a mass of polyoxidonium is dissolved in 2-3 ml of an isotonic solution of sodium chloride, hemodesis, reopoliglyukin or glucose, sterilely transferred to bottles with the indicated solutions with a volume of 100-400 ml. This injection solution cannot be stored (www.mtu-net.ru/doctor99/5nklassifik1polioxidoniy2905.htm).

The process of preparing an injection form before medical procedures requires careful observance of sterility and dosage, as well as their control, which complicates the medical process and can lead to medical errors. In addition, this drug does not have a local anesthetic effect.

Known drug meglumine acridone acetate (trade name - cycloferon), which is a low molecular weight inducer of interferon, which has an antiviral, immunomodulating and anti-inflammatory effect. The main target cells of the drug are T and B lymphocytes. It stimulates the production of alpha, beta, and gamma interferons (up to 60-80 PIECES / ml and higher) by leukocytes, macrophages, epithelial cells, as well as tissues of the spleen, liver, lungs, brain, penetrates the cytoplasm and nuclear structures, activates synthesis of "early" interferons. The immunomodulatory effect is expressed in the correction of the immune status of the body in immunodeficiency states of various origins. The drug has a low toxicity. It has no mutagenic, teratogenic, embryotoxic and carcinogenic effects.

As a 12.5% (0.125 g / ml) aqueous solution for intramuscular and intravenous administration, cycloferon is used in the treatment of HIV infection, neuroviral infection (tick-borne meningitis, multiple sclerosis, arachnoiditis), viral hepatitis (A, B, C, D), CMV and herpes infections, influenza, acute respiratory viral infections, immunodeficiency conditions (postoperative period, burns, bronchitis, pneumonia, etc.), gastric ulcer and duodenal ulcer, cancer, rheumatoid arthritis, deforming osteoarthritis, spondylosis, skin diseases ( atonic dermatitis, eczema, dermatosis, viral papillomas) (Description of the drug, www.regmed.ru/InstrShow2.asp?InstrLinkNx=a86ba80ba84ba86b). The composition of a 12.5% solution includes 125 mg of methylglucamine acridone acetate (1 ampoule - 250 mg), water for injection up to 1 ml. Available in the form of 2 ml ampoules (www.znaharka.ru/index.php?productID=59289).

The drug is compatible with all drugs, including antibiotics, vitamins, chemotherapy, immunomodulators, interferons (Description of the drug. Www.regmed.ru/InstrShow2.asp?InstrLinkNx=a72ba78ba75ba74b). It is known that an immune response to the action of cycloferon is observed in no more than 40% of patients (www.mtu-net.ru/doctor99/5nklassifik1polioxidoniy2905.htm).

One of the most powerful inducers of endogenous interferon is known - tilorone (www.amixin.ru), which is available in the form of a preoral drug (trade name "Amiksin", instruction for the drug http://www.regmed.ru/InstrShow2.asp?InstrLinkNx= 41ba48ba44ba43b, and Lavomax, Preparation Instructions, http://www.regmed.ru/InstrShow2.asp?InstrLinkNx=a41ba48ba44ba43b). It is used in the treatment of viral hepatitis A, B, C; herpes and CMV infections, complex treatment of infectious-allergic and viral encephalomyelitis (multiple sclerosis, leukoencephalitis, uveoencephalitis), chlamydial infections of the urogenital and respiratory tract, influenza prevention, and other acute respiratory viral infections.

Tiloron is a low molecular weight synthetic inducer of interferon, stimulating the formation of alpha, beta and gamma interferons in the body. The main producers of interferon in response to oral administration of tilorone are intestinal epithelial cells, hepatocytes, T-lymphocytes, neutrophils and granulocytes. After oral administration, the maximum production of interferons is determined in the sequence of intestine-liver-blood after 4-24 hours.

Tiloron in human leukocytes induces the synthesis of interferon, stimulates bone marrow stem cells, depending on the dose, enhances antibody formation, reduces the degree of immunosuppression, and restores the ratio of T-suppressors and T-helpers. The mechanism of its antiviral action is associated with inhibition of the translation of virus-specific proteins in infected cells, as a result of which reproduction of viruses is suppressed. It is effective against pathogens of viral hepatitis, herpes viruses (including cytomegaloviruses). (Instruction for the drug, http://www.regmed.ru/InstrShow2.asp?InstrLinkNx=a41ba48ba44ba43b).

After oral administration, tilorone is rapidly absorbed from the gastrointestinal tract (GIT). When taken orally, its bioavailability is 60%. Tiloron quickly penetrates into the blood and is distributed in organs, tissues and body fluids. About 80% of tilorone binds to plasma proteins. The drug is excreted almost unchanged with feces (70%) and urine (9%) with a half-life of 48 hours. Tiloron in the body is not metabolized and does not cumulate (Information about the drug "Amiksin", http://www.vidal.ru/vidal_main/doc_5533.htm).

Tiloron, being a modulator of cytokine reactions and an antioxidant, is used orally in the secondary prevention of multiple sclerosis (V. I. Golovkin et al. “Secondary prevention of multiple sclerosis with the help of the domestic drug amixin - a modulator of cytokine reactions and antioxidant”, //home.peterstar.ru /nwams/amixin2.html).

Tiloron is orally used in the treatment of tick-borne encephalitis (V. Tarasov. “Tick-borne encephalitis.” Medical newspaper No. 34, 2003, www.neuronet.ru/bibliot/b001/mg34_03.html).

Tiloron is not only an effective antiviral agent, but also increases the body's resistance to infections caused by bacteria, fungi and protozoa. It has an activating effect on macrophages. At the same time, not only the absorptive capacity of phagocytes increases, but also the production of reactive oxygen species by these cells that have a bactericidal effect. Tiloron has a stimulating effect on the phagocytic and bactericidal functions of macrophages, while reducing the intensity of lipid peroxidation.

It activates natural killers, which play a leading role in the antitumor defense of the body. Tiloron has an antitumor effect against virus-induced tumors. In combination with antitumor drugs, it contributes to a more significant inhibition of the growth of neoplasms, reduces the frequency and degree of metastasis, sometimes completely preventing it. In large doses, tilorone directly inhibits tumor growth. Tiloron in combination with cytostatics can reduce their dosage by half without changing the quantitative characteristics of the antitumor effect. It also reduces the severity of side effects of radiation therapy, and when administered to patients before surgery, it provides faster healing of wounds, prevents metastasis and the development of infection.

Tiloron has anti-inflammatory activity, which allows its effective use 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, but exceeds its duration. When applied locally to skin and eyes damaged by herpes, it provides direct inactivation of the herpes virus (T.O. Filippova, N.Ya. Golovenko “TILORON: PROFILE OF BIOLOGICAL ACTIVITY I. PHARMACOLOGICAL PROPERTIES http://magazine.odmu.od.ua/antropo /2006/1/18.pdf).

Tiloron is well compatible with antibiotics and traditional viral diseases (www.amixin.com.ua).

Tilorone is readily soluble in water (about 10% at 20 ° C) and 95% ethanol (about 3.3% at 20 ° C) (Pharmacopoeia article of the enterprise FSP 42-0416-4243-03), which makes it promising for use in injectable preparations.

However, pharmaceutical preparations in the form of injectable dosage forms for subcutaneous, intramuscular and intravenous use containing tilorone as an active substance are not currently known.

The objective of the invention is the creation of injectable pharmaceuticals for subcutaneous, intramuscular and intravenous use based on a low molecular weight interferon inducer.

Technical results that can be obtained using the present invention: expanding the field of application of the known active substance - tiloron, restoring local immunity and biocenosis of the skin and mucous membranes in the treatment of purulent-destructive processes of the skin and mucous membranes, especially with a deep location of the lesion foci, reducing secondary tissue necrosis in the affected areas, relief of inflammatory reactions, providing a local anesthetic effect, accelerating healing.

To solve this problem, the present invention provides a pharmaceutical injection preparation containing, as an active substance, a low molecular weight interferon inducer and a solvent, which contains tilorone as a low molecular weight interferon inducer, for example, in the following ratio of components wt.%:

tiloron 0.001-10,000 solvent rest

At the same time, a heat-resistant emulsion of perfluororganic compounds for injection or a mixture with a hydrophilic osmolar solution, for example, an isotonic solution of sodium chloride, with a quantitative ratio in the composition of the preparation, wt.%:

tiloron 0.001-10.0 organofluorine emulsion 5.0-90.0 isotonic sodium chloride solution rest

To ensure local anesthesia, an anesthetic was introduced into the composition of the drug, for example, novocaine with a content of 0.25 to 5.00 wt.% In the preparation.

When living cells are destroyed (for example, during purulent-destructive processes), substances that stimulate the local immune system (T-lymphocytes) are released from the cells, activating the macrophages located next to the damage, which in turn synthesize and release various stimulants into the surrounding space cell division, contributing to the elimination of disorders of the cellular system (A. N. Decina. "Theory of soft cosmetic effects. Modern cosmetology", Novosibirsk, "Science", 2000, www.golkom.ru/book/48_1.htm).

To restore the immune function of the skin and mucous membrane, a low molecular weight interferon inducer, tilorone, can be used for subcutaneous or intramuscular administration. In the form of an injectable preparation for subcutaneous or intramuscular administration, it can be used for local therapy in dermatology in the treatment of purulent-destructive processes of the skin and soft tissues, such as recurring furunculosis, acne vulgaris, burns, long-term healing of soft tissue wounds, etc., especially with deep subcutaneous location of lesions. In addition, its use in the form of topical preparations in allergology and immunology for the complex treatment of allergic dermatoses, especially associated with fungal and herpetic infections, is promising.

With local exposure, tilorone increases the expression on the cell membranes of antigens of the major histocompatibility complex (HLA) of class 1 and class 2 (HLA-DR), increases the number and activity of NK cells, causes a targeted polarization Th0 → Th1, modulates the inflammatory response, depending on phases of inflammation, positively affects the state of local immunity, has a direct and indirect effect on viruses, intracellular bacteria, fungi.

To ensure local anesthesia of the lesion, a local anesthetic is introduced into the tissue surrounding the lesion and containing nerve conductors that innervate the area of the purulent-destructive process (conduction method of local anesthesia). Local infiltration anesthesia in the case of purulent-destructive lesions is contraindicated, as the anesthetic infiltration of inflamed tissues is very painful and contributes to the spread of infection (www.destreferat.ru/referat-65155.html).

To provide a stimulating effect on living cell metabolic processes (activation of redox, hydrolytic reactions, synthesis of nucleic acids, proteins, lipids, etc.), rapid detoxification, suppression of the inflammatory reaction and active proliferation of epidermal cells in the proposed preparation, an organofluorine emulsion is used as a solvent compounds.

An injectable preparation for subcutaneous and intramuscular administration containing tilorone, anesthetic and a solvent in the form of an emulsion of perfluorocarbon compounds or a mixture thereof with a hydrophilic osmolar solution is injected subcutaneously or intramuscularly around the inflamed tissues of the lesion site to ensure fast and efficient transport of the active substance to the cells responsible for stimulating local immunity and restoration of the immune properties of tissues in the area of the lesion, including with a deep subcutaneous location, and ie providing local anesthesia.

Tiloron, being a stable low molecular weight substance (molecular weight 483.5), dissolved in a hydrophilic solvent, easily penetrates deep into tissues with subcutaneous and intramuscular administration.

Tiloron, which has antioxidant properties, penetrates into the affected tissue from a hydrophilic solution, reducing secondary tissue necrosis around the lesion.

With intravenous administration, tilorone quickly spreads through the bloodstream throughout the body and easily penetrates into organs and tissues, stimulating cells that induce interferon.

It is known that emulsions of perfluororganic compounds for intravenous administration, such as perfluorane, were used in the complex treatment of wounds and wound infections (Krylov NL et al. “Hemosorption and infusion of perftoran in the complex treatment of wounds and wound infections.” Problems of intensive care in the clinic. Abstracts of a scientific conference. December 12-13, 1985 - M .: BI, 1985 - p. 12-13).

Experimental studies have shown that perfluorocarbon compounds have a membrane effect and have a stimulating effect on the metabolic processes of living cells (they activate redox, hydrolytic reactions, the synthesis of nucleic acids, proteins, lipids, etc.). The contact of perfluorocarbons with damaged cells leads to rapid detoxification, suppression of the inflammatory response and active proliferation of epidermal cells. A positive effect was obtained with the cutaneous use of perfluorocarbon compounds in the treatment of patients with atopic dermatitis, eczema, trophic ulcers, herpes, acne, and pyoderma. A characteristic property of perfluorocarbons is their antipruritic effect, which is not inferior to hormonal drugs (Umerov Zh.G., Filippov EA “Perfluorocarbon compounds are promising anti-inflammatory drugs for the treatment of skin diseases.” IX All-Union Congress of Dermatovenerologists. Almaty, September 23-27 1991 Abstracts of reports. - M., 1991, p. 354). Perfluorocarbons with gas transporting properties stimulate wound healing and / or improve metabolism in integumentary tissues, which is associated with their effect on gas exchange of adjacent tissues, since wound damage is accompanied by increasing tissue cell hypoxia and increasing acidosis (patent RU No. 2033163, АКК 33/16, 1995.04. twenty).

Organofluorine emulsions with gas-transporting properties are known (for example, patent RU No. 2088217, АКК 9/10, 1997.08.27), which can be stored at room temperature for at least 1 year.

Organofluorine emulsions are readily diluted with hydrophilic osmolar aqueous saline solutions. In pure form or in admixture with hydrophilic osmolar aqueous salt solutions, emulsions of organofluorine compounds can be used as a solvent for tilorone in injection preparations.

Dilution of emulsions of perfluororganic compounds with hydrophilic osmolar aqueous solutions, for example, 0.9% isotonic sodium chloride solution, reduces the cost of the drug (since concentrated emulsions of perfluororganic compounds have a high cost) and also increases the penetration of the drug into tissues due to the hyperosmolar properties of hydrophilic salt solutions.

An isotonic solution of sodium chloride in a concentration of 0.9% is commercially available and is used as a detoxification agent, for the dissolution of drugs, etc. (www.recipe.ru).

Novocaine (neocaine, pancaine, procaine) is the least toxic drug with a wide range of therapeutic effects. It is used for various types of local anesthesia in the form of a 0.25% -5.00% solution (www.destreferat.ru/referat-65155.html).

A hydrophilic aqueous salt solvent efficiently transports the active substance, tilorone, to the area of purulent-destructive lesion due to its osmolar properties.

A low molecular weight interferon inducer (synthetic immunomodulator) - tiloron in the proposed pharmaceutical injection for subcutaneous and intramuscular use restores local immunity of the skin and mucous membranes, which contributes to faster healing of purulent-destructive lesions, especially when they are deep subcutaneous, increases the body's resistance to skin diseases and diseases of the mucous membrane due to the suppression of viral, bacterial and fungal infections. The antioxidant properties of tilorone can accelerate healing by reducing tissue necrosis. The organofluorine emulsion also accelerates healing, reducing acidosis of the affected tissue. Anesthetics provide local anesthesia.

With intravenous use, tilorone restores the general immunity of the body.

The feasibility of the proposed injectable drug is confirmed by the following examples, but not limited to them.

Example 1

Obtaining an injectable drug based on tilorone and an emulsion of perfluororganic compounds is implemented according to the following scheme:

1. Weigh the components (powders) in the required amount.

2. Measure the required volume of heat-resistant emulsion of perfluororganic compounds.

3. The components are poured into the emulsion and dissolved, maintaining the temperature at dissolution of not more than + 60 ° C.

4. The prepared solution is cleaned of mechanical impurities by filtering through a filter system with a final filter having a pore diameter of at least 0.45 μm.

5. After filtration, the solution is poured into sterile 2 ml ampoules, the ampoules are sealed and checked for leaks.

6. After which the ampoules are placed in an autoclave and additionally sterilized for 30 minutes at a temperature of + 121 ° C.

All operations for the preparation of the solution, its filtration and ampulling are carried out under aseptic conditions in accordance with the requirements for the production of injection solutions.

The sterility of the solution of tilorone in ampoules is checked according to the method described in the State Pharmacopoeia (GF) XI, issue 2, p. 187.

The pH of the tilorone solution is measured potentiometrically according to GF XI, issue 1, p. 113.

According to this technology, 1000 pieces of ampoules with 0.1% aqueous solution of tilorone of reduced composition were made.

The composition of the drug is one ampoule, volume 2 ml Components amount Tiloron (mass, g) from 0.0018 to 0.0022 Emulsion of perfluororganic compounds (volume, ml) the rest is up to 2.15-2.25 ml

In the manufacture and control storage for 28 months, 1000 pieces of ampoules with a 0.1% solution of defective tilorone in terms of pH, transparency, and sterility were not detected.

Example 2. The preparation of an injectable 1% drug based on tilorone, an emulsion of perfluororganic compounds and a 0.9% isotonic sodium chloride solution is carried out according to the following scheme: the first 4 stages are carried out as described in Example 1, dissolving tiloron in an isotonic solution, then the following stage.

5. After preliminary filtration, the solution of tilorone in an isotonic solution is sterilized by filtering it at room temperature sequentially through a filter with a pore diameter of 0.2 μm, and then through a filter with a pore diameter of 0.1 μm.

6. After sterilizing filtration, a sterile emulsion of perfluororganic compounds is added to the solution in an amount necessary to ensure a concentration of tilorone in the solution of 1%.

7. After sterile homogenization, the mixture is poured into sterile 2 ml ampoules, the ampoules are sealed and checked for leaks.

8. After which the ampoules are placed in an autoclave and additionally sterilized for 30 minutes at a temperature of + 121 ° C.

All operations for the preparation of the solution, its filtration and ampulling are carried out under aseptic conditions in accordance with the requirements for the production of injection solutions.

The sterility of the solution of tilorone in ampoules is checked according to the method described in the State Pharmacopoeia (GF) XI, issue 2, p. 187.

The pH of the tilorone solution is measured potentiometrically according to GF XI, issue 1, p. 113.

Using this technology, 1000 units of ampoules with a 1% solution of tilorone of reduced composition were manufactured.

The composition of one ampoule, volume 2 ml Components amount Tiloron (mass, g) from 0.018 to 0.022 Procaine - procaine base (mass, g) from 0.018 to 0.022 0.9% isotonic sodium chloride solution (volume, ml) from 0.45 to 0.55 Emulsion of perfluororganic compounds (volume, ml) the rest is up to 2.15-2.25

In the manufacture and control storage for 28 months, 1000 pieces of ampoules with a 1% solution of defective tilorone in terms of pH, sterility was not detected.

The therapeutic activity of tilorone in an emulsion of organofluorine compounds or its mixture with aqueous saline solutions with the presence of anesthetics has not been known to date and does not follow from the prior art.

The proposed injectable preparation based on tilorone, anesthetic and a heat-resistant emulsion of perfluororganic compounds or its mixture with aqueous saline solutions significantly expands the field of application of the known active substance - tilorone, provides restoration of local immunity and biocenosis of the skin, as well as mucous membranes in the treatment of purulent-destructive processes of the skin and mucous membranes, especially with deep subcutaneous location of lesions, has a high therapeutic activity, relieves inflammation s responses, reduces secondary tissue necrosis in the affected areas associated with excess free radical oxidation, provides local analgesia accelerates healing.

The search for information did not reveal identical and similar technical solutions.

Until now, a similar solution has not been proposed, although the drug Tiloron has been known since 1970 (T.O. Filippova, N.Ya. Golovenko “TILORON: PROFILE OF BIOLOGICAL ACTIVITY I. PHARMACOLOGICAL PROPERTIES http://magazine.odmu.od.ua /antropo/2006/1/18.pdf).

Therefore, the applicant believes that the claimed pharmaceutical injection drug based on tilorone has an inventive step.

The inventive pharmaceutical preparation can be recommended in the treatment of purulent-destructive lesions of the skin and mucous membranes, especially with deep subcutaneous location of the lesion.

The proposed pharmaceutical injection preparation for subcutaneous, intramuscular and intravenous use on the basis of tilorone can be used for industrial serial production.

Claims (3)

1. A pharmaceutical injection composition for the treatment of purulent-destructive processes with signs of immune deficiency, characterized in that it contains tilorone and a hydrophilic solvent in the following ratio, wt.%:
tiloron 0.005-10,000 hydrophilic solvent rest 2. The pharmaceutical injection composition according to claim 1, characterized in that as a hydrophilic solvent it contains substances selected from the series: an emulsion of perfluororganic compounds, an isotonic sodium chloride solution, or a mixture thereof. 3. The pharmaceutical injection composition according to claim 1, characterized in that it additionally contains an anesthetic novocaine when its content in the composition is from 0.25 to 5.00 wt.%.