RU2844058C2 - Aqueous antiseptic with reparative activity based on natural components - Google Patents

Abstract

FIELD: pharmaceutics.

SUBSTANCE: invention refers to pharmaceutics, namely to an aqueous antiseptic with reparative activity. Aqueous antiseptic with reparative activity, containing 0.1% of usnic acid as an antiseptic agent, as reparant 1% sodium alginate, as well as 0.9% sodium chloride and 98% distilled water.

EFFECT: invention makes it possible to create a composition having high antimicrobial and reparative activity and an improved form for ease of use.

1 cl, 2 tbl, 1 ex

Description

The invention relates to the field of medicine, namely pharmacology.

In modern therapeutic practice, dermatology for the prevention and treatment of skin lesions of various etiologies, compositions are used that include film-forming solutions of polymer compositions, medicinal substances, antimicrobial agents. When treating a wound after the solvent evaporates, a thin protective polymer film remains on the wound surface, containing medicinal and antimicrobial substances.

There are known dosage forms of compositions that include film-forming solutions of polymer compositions (as a base), medicinal substances, antimicrobial agents that are widely used in medicine for local prevention and treatment of wounds. Such industrially produced drugs include compositions containing active components, such as nitrofuran, hydroxymethylquinoxylinedioxide, trimecaine, iodovidone, miramistin (benzyldimethyl[3-(myristoylamino)propyl]ammonium chloride), amitrozole, levomycetin, methyluracil, hydrocortisone acetate, neomycin sulfate, heliomycin.

The description of patent RU No. 2028158 proposes a composition for the treatment and prevention of wound surfaces, containing an aqueous solution of sodium alginate and an enzyme - terrilitin and calcium gluconate. The disadvantage of this composition is the enzyme content, which can cause allergic reactions.

Patent RU No. 2123843 proposes a composition for treating wounds, containing a base - polyethylene oxides, water and additionally - lanolin, active substances - G-acetylaminocaproic acid and sodium hydrogen carbonate. Patent RU No. 2301056 proposes a composition containing a methacrylic copolymer (selected from EUDRAGIT RL or EUDRAGIT RS or a mixture thereof) and a therapeutic agent. The composition ensures the transport of the therapeutic agent into the body tissues, mechanical protection of wounds and a barrier to bacteria. Invention application RU No. 2007116956 proposes a composition for obtaining a medicinal product for treating open wounds and burns. The binding components of the composition can be - liquid polyol, polymer binder, silicon dioxide, resin or a combination thereof. The composition includes an active component selected from salts containing metal cations (lithium, sodium or potassium) and halogen oxides that form anions. The disadvantage of these compositions is the introduction of polymers that have a low spectrum of antimicrobial activity.

Patent RU #2177314 proposes a composition with antiseptic, reparative and analgesic properties. The composition on a hydrophilic base contains trimecaine, the antiseptic miramistin, D-panthenol and/or calcium pantothenate. Mixtures of various polyethylene oxides and propylene glycol are used as a hydrophilic base. Description of patent RU #2312658 proposes a composition containing a film-forming substance, an antiseptic preparation in a polar solvent, and a local anesthetic substance. The composition is intended for treating wounds and has protective, anesthetic and disinfectant properties. The composition contains a film-forming component in the form of a polysiloxane-polycarbonate block copolymer, an antiseptic preparation in a polar solvent, an anesthetic substance and a block copolymer solvent in the form of chloroform. The following are used as an antiseptic: brilliant green, blue, iodopyrone and some other iodine-containing compounds. The disadvantages of these compounds include their components, which can exhibit negative properties. Chloroform (trichloromethane) has an irritating and allergic effect, has a hepatoxic effect on the human body (liver and kidney dysfunctions are possible), and is slowly eliminated from the body. The antiseptic drug - brilliant green (synthetic dye of the triphenylmethane series) does not have a wide spectrum of action and the required level of antimicrobial activity, is active only against gram-positive bacteria, and causes skin irritation. The antiseptic drug - iodopyrone (povidone-iodine and potassium iodide) causes dry skin, skin itching, allergic reactions (skin hyperemia, urticaria), does not have the necessary selective action, and is contraindicated for use in hyperthyroidism, thyroid adenoma, cardiac and chronic renal failure.

There are known compositions containing silver sulfadiazine and sodium piperacillin (Patent US 4535078, published 1985), or wound healing materials containing animal tissues impregnated with silver salt of sulfadiazine (Patent US 4599226, published 1987). The technical solution for patent RU No. 2155047 proposes a preparation for the treatment of wounds and burns, consisting of an aqueous solution containing: basic copper acetate, sodium acetate, acetic acid and water. The therapeutic effect is associated with analgesic, anti-inflammatory, bactericidal action. Also, patent RU No. 2379042 proposes a biologically active bactericidal preparation for the treatment of wounds, burns, tumors. The preparation is a suspension of particles of copper, iron and zinc powders with a particle dispersion of 180-220 nm. The disadvantages of these compositions are metal salts, which have an allergic and toxic effect, as well as salts and complex compounds of metals, metal powders do not exhibit biological compatibility with skin tissues.

The closest is patent RU 2588968 composition for biologically active gel dressing containing sodium alginate and powder of natural zeolite rocks, preferably clinoptilolite-smectite, with a size of preferably 10-100 μm, but not less than 200 nm, while in the composition of the mixture the content of natural zeolite rocks is 60-70% of its weight, the rest is sodium alginate powder based on the volume of the composition. The main disadvantages of this composition include the presence of zeolite rocks with low antibacterial activity, as well as the method of application in the form of a dressing.

The objective of the present invention is to create an effective antimicrobial aqueous composition with reparative activity from natural compounds. The technical result is achieved in creating a composition with high therapeutic activity, namely antimicrobial and reparative activity of processes and an improved form for ease of use.

To solve the set tasks, it is proposed to create a composition of usnic acid, which has high antibacterial activity, and sodium alginate with high reparative activity, in the form of a spray presented in Table 1.

According to the invention, usnic acid is a yellow crystalline substance with a dibenzofuran skeleton, has high activity against many pathogenic organisms of viral, bacterial and fungal nature, and due to its properties is used in cosmetics, dentistry and other areas of medicine. A good source of usnic acid are various types of lichens, such as lichens of the genera Usnea and Cladonia, in which this compound is the main metabolite.

Sodium alginate is a natural polysaccharide obtained from sea brown algae, has a pronounced hemostatic, anti-inflammatory and reparative effect.

Determination of biological (pharmacological) activity of an antiseptic with reparative activity

The experiment was performed on mongrel rats of both sexes weighing 200+/-40 grams. On the wound process model - a flat aseptic wound obtained according to the method in animals, under ether anesthesia, on the pre-depilated skin of the back, after treating the surgical field with iodopyrone and 70% alcohol in the interscapular region according to a stencil with a diameter of 2 cm, a standard flat wound with a depth of 2 mm was formed with a scalpel.

Example 1. The regenerative capacity of an antiseptic with reparative activity is reflected in Table 2.

For this experiment, 20 laboratory rats with a superficial aseptic wound were taken. They were divided into a control (10 individuals), which were not treated with anything, and 10 individuals, to which an antiseptic with reparative activity was applied to the wound once a day for 1 dose (experiment). Histological preparations were prepared on the 3rd, 7th and 14th days and stained with hematoxylin and eosin. The effector cells (lymphocytes, neutrophils, fibroblasts) were counted under a MIKMED 5 microscope (Russia) at a magnification of ×100. The number of vessels was counted in a large square of the Academician G.G. Avtandilov grid at a magnification of ×40.

Based on the data obtained, a significant decrease in the inflammatory reaction in the wound area was established when using an antiseptic with reparative activity on the 3rd day of the experiment (Table 2). At the same time, an increase in the number of fibroblasts and vessels in the wound area was established, which characterizes the development of restorative regenerative processes. Intensive growth of new blood and lymphatic vessels occurs in the wound, blood circulation improves, hypoxia decreases, and the inflammatory reaction subsides. New vessels are formed in the wound, young granulation tissue matures, which helps eliminate the wound tissue defect.

Claims (1)

An aqueous antiseptic with reparative activity, containing 0.1% usnic acid as an antiseptic agent, 1% sodium alginate as a reparant, as well as 0.9% sodium chloride and 98% distilled water.