Agent for treatment of articulation diseases

FIELD: medicine, arthrology, pharmacy.

SUBSTANCE: agent comprises glucosamine salt as saccharide, dimethylsulfoxide, ointment base and ibuprofen or nimesulide, or piroxicam, or meloxicam, or diclofenac salt, or indometacin, or ketoprofen as a nonsteroid anti-inflammatory agent. Glucosamine hydrochloride, glucosamine sulfate sodium, potassium or calcium salt is used as glucosamine, and diclofenac potassium or sodium salt is used as diclofenac salt. New ointment shows high perfusion rate of active substances to the articulation zone and enhanced effectiveness. Invention expands assortment of agents used in treatment of articulations.

EFFECT: improved, enhanced and valuable medicinal properties of agent.

2 cl, 14 ex

 

The invention relates to medicine, namely, preparations for external use for the treatment of diseases of the joints. Disease affects about 70% of the population older than 45 years. They are manifested as pain in the joint, aggravated by motion, sensation of tightness. Inflammatory processes are accompanied by swelling, change in shape of the joints.

In addition, when astrologicheskih diseases of the joints gradually destroys the cartilage covering the articular surfaces, as well as bone tissue and the inner surface of the articular capsule.

Currently widespread in the world of medical practice for the treatment of diseases of the joints (arthritis, arthrosis, osteochondrosis, etc.) received drugs on the basis of saccharides (salts of glucosamine, chondroitin sulfate), mainly in the form of tablets and injections. Treatment with these drugs not only reduce inflammation and pain in the joints, but also produces the restoration of damaged cartilage tissue [Nasonov EL Clinical guidelines and algorithms for medical practitioners. Rheumatology. M., 2004; K.Pavelka, Archives Internal Medicine, №10, 2002, №7, 2003].

Widespread previously found drugs exterior - ointment dosage forms based on a derivative of diclofenac. Recently, however, despite their known therapeutic effect of interest to this group is sharply reduced due to their high gastroepiploic activity and a number of complications. However, it is established that the concomitant use of separate preparations of diclofenac and saccharide - glucosamine provides an unexpected synergistic therapeutic effect of diclofenac, which allows to decrease the dose (Vguderqa. Protective agents. Kiev: Health Of Ukraine, 2004).

Closest to the claimed composition is a preparation containing as active ingredients saccharide - fractions polysulphate, diclofenac sodium and transdermal agent is dimethyl sulfoxide on the known ointment bases [RF patent №2085194, class a 61 K 31/73, A 61 K 9/06, publ. 27.07.1997].

The disadvantages of this tool are that when used as a chondroprotective component of the polysaccharide fractions of polysulfate, which is unstable in the chemical synthesis of semisynthetic connection is not established structure (basis of preparation ARTEPARON, which is withdrawn from registration in the Russian Federation due to the high toxicity) polydisperse and has a high molecular weight (10000-100000 daltons), sharply limited the diffusion of the substance in the joint area, which significantly reduces the pharmacokinetics of the drug, the effect of inhibition of the process of destruction of cartilage and its regeneration.

The problem solved by the invention is the development of tools for the treatment of diseases of the joints, combining the Honda is protective, anti-inflammatory and analgesic action with labile high pharmacokinetic parameters and expanding Arsenal of drugs for the treatment of joints.

The technical result from the use of the invention is to improve the effectiveness of the drug due to the low molecular weight Monomeric saccharide and, consequently, increase the rate of diffusion of the active substances in the joint area and the expansion of the means to treat diseases of the joints due to use as anti-inflammatory compounds one representative of the group of NSAIDs: ibuprofen, nimesulide, piroxicam, meloxicam, diclofenac, indometacin, Ketoprofen, each of which socetanii with saccharide - glucosamine salt exhibits a synergistic effect.

The specified result is a tool for the treatment of diseases of the joints, with chondroprotective, anti-inflammatory and analgesic action, containing a saccharide, a compound selected from the group of nonsteroidal anti-inflammatory drugs, dimethylsulfoxide and the ointment base according to the invention it contains as saccharide salt of glucosamine and as nonsteroidal anti-inflammatory agents it contains ibuprofen, or nimesulide, or piroxicam or meloxicam or diclofenac salt, or indomethacin, or getprop the n in the following components, wt.%:

Glucosamine salt0.5 to 10.0
Ibuprofen0,1-10,0
or Nimesulide0,1-1,0
or Piroxicam0,1-1,0
or Meloxicam0,1-1,0
or Diclofenac salt0,1-5,0
or Indometacin0,1-10,0
or Ketoprofen0,1-5,0
The sulfoxide1,0-20,0
Ointment baseRest

Preferably, as salts of the product contains glucosamine hydrochloride glucosamine, or sodium, or potassium, or calcium salt of glucosamine sulfate, as well as salts of diclofenac its potassium or sodium salt.

These ranges of concentrations of active ingredients are optimally acceptable, pharmacologically meaningful and accepted in medical practice for similar ointment form of this pharmacological group.

As salts of glucosamine tool may contain a known pharmaceutical substance (registered in the Russian Federation, such as the Fund 42-0314-1478-01, or imported, the relevant requirements of United States Pharmacopeia 27 editions): glucosamine hydrochloride, sodium, potassium and allevia salt of glucosamine sulfate.

Preferred is the disodium salt of glucosamine sulfate and glucosamine hydrochloride.

Low molecular weight of these saccharides (573,3 and 215,0 daltons, respectively) and their high pharmacological activity in the treatment of diseases of the joints ensure the creation of effective chondroprotective drugs [Eszteca. Scientific-practical rheumatology, 2003, No. 2].

As an anti-inflammatory component agent contains a compound selected from the group of NSAIDs: ibuprofen, or nimesulide, or piroxicam or meloxicam or diclofenac salt, or indomethacin or Ketoprofen, advantage each of which is of high anti-inflammatory and analgesic activity.

As a salt of diclofenac, the tool may contain its potassium or sodium salt, for example, ND 42-3714-01.

The use of dimethyl sulfoxide as one of the components of the drug due to the fact that it has anti-inflammatory and analgesic action in diseases of the musculoskeletal system. In addition, the sulfoxide is able to penetrate biological membranes, including skin barriers, thereby increasing the diffusion of drugs through the skin of the patient. Used dimethyl sulfoxide, for example, FS 42-2980-98.

As ointment bases can be COI is used basis, used to obtain the actual ointments, gels, liniments, creams, pastes.

To neutralize the acidity of the used salts of sulphate glucosamine (pH of 1.5-4.0) to a physiologically acceptable pH values ointments (pH 4.0 to 8.0) in the basis in the preparation can be optionally added base such as sodium hydroxide or known pharmaceutical amines, e.g., ethanolamines - diethanolamin (2, 2'-iminodiethanol), triethanolamine, trolamine.

The proposed tool refers to the pharmacological group - 8.8, concealer metabolism of bone and cartilage (Register of medicines of the Russian Federation, 2004).

Receive offer tools operate in a known manner by mixing the active ingredients with acceptable ointment base with subsequent packaging.

Control the quantitative content of the active ingredients in preparations carried out by known methods adopted for similar legform registered in the Russian Federation and contains glucosamine, ibuprofen, nimesulide, piroxicam, meloxicam, diclofenac salt, indomethacin, Ketoprofen, dimethylsulfoxide (spectrophotometric, potentiometric or titration values).

Examples of receipt of the proposed tools.

Example 1. 4.0 g disodium salt of glucosamine sulfate and 1.6 g of nimesulide dissolve when heated in 32 ml of distillirovannoi water. Separately melted at a temperature of 50-70°With 24 g of anhydrous lanolin and 80 g of vaseline. Salt solution, a mixture of lanolin and vaseline, 16 g of dimethyl sulfoxide separately filtered and mixed with constant stirring at a temperature not exceeding 65°C to obtain a homogeneous mass, bring the pH to 4.0 to 8.0 by adding sodium hydroxide and cooled. The drug is Packed in tubes or cans. 1 g of the end product contains 25 mg of disodium salt of glucosamine sulfate (2.5 wt.%), 10 mg of nimesulide (1.0 wt%), 100 mg of dimethyl sulfoxide (10.0 wt%), 150 mg lanolin, 500 mg of vaseline and 200 mg of water.

Example 2. Example 2 is carried out, as the example 1, except that as a compound from the group of NSAIDs use piroxicam.

Example 3. Example 3 is carried out, as the example 1, except that as a compound from the group of NSAIDs use meloxicam.

Example 4. 10.0 g of glucosamine hydrochloride and 0.1 g of diclofenac potassium is dissolved in 19 ml of distilled water. Weigh 20 g of polyethylene oxide with a molecular weight of 4000 (PEO-4000) and 40 g of polyethylene oxide with a molecular weight of 600 (PEO-600) and melting the mixture in a water bath at a temperature not exceeding 65°C. To the molten mixture with constant stirring, a solution of glucosamine hydrochloride and diclofenac potassium in water, and then 10 g of dimethyl sulfoxide and 10 g of glycerin. The mixture is stirred for 3 h (200 rpm) until the floor is wow cooling bring the pH to 4.0 to 8.0 by the addition of triethanolamine and Packed in tubes or cans. 1 g of the end product contains 100 mg of glucosamine hydrochloride (10.0 wt%), 1.0 mg of diclofenac potassium (0.1 wt.%), 10.0 mg of dimethyl sulfoxide (1.0 wt%), 100 mg of glycerol, 400 mg PEO-600, 200 mg PEO-4000 and 190 mg of water.

Example 5. Example 5 is carried out as example 4, only as a compound from the group of NSAIDs use ibuprofen.

Example 6. Example 6 is carried out, as the example 4, only as a compound from the group of NSAIDs use of nimesulide.

Example 7. Example 7 is carried out, as the example 4, only as a compound from the group of NSAIDs use piroxicam.

Example 8. Example 8 is carried out, as the example 4, only as a compound from the group of NSAIDs use meloxicam.

Example 9. Example 9 is carried out, as the example 4, only as a compound from the group of NSAIDs use indomethacin.

Example 10. Example 10 is carried out, as the example 4, only as a compound from the group of NSAIDs use Ketoprofen.

Example 11. 0.5 g of the calcium salt of glucosamine sulfate, 5.0 g of diclofenac sodium was dissolved in 25 ml of distilled water and poured to the resulting solution of 10.0 g of dimethyl sulfoxide (mixture 1). To 38 g of glycerin was added with stirring 5 g of sodium carboxymethyl cellulose (Na-CMC) and allowed to mix until complete dissolution of Na-CMC (mixture 2). 0.5 g krakhmalosushil with 8 ml of distilled water and added with stirring a mixture of 1 and 2 (mixture 3). 8 g of emulsifier No. 1 is melted in a water bath at a temperature of 60°and with stirring, add it to the pre-warmed to 60°With mixture 3. Left under stirring for 3 h, adjusted pH to 4.0 to 8.0 by the addition of triethanolamine and Packed in tubes or cans. 1 g of the end product contains 5.0 mg of the calcium salt of glucosamine sulfate (0.5%), 50.0 mg of diclofenac sodium (5.0 wt.%), 50 mg Na-CMC, 100 mg of dimethyl sulfoxide (10.0 wt%), 380 mg of glycerol, 80 mg of the emulsifier No. 1, 5.0 mg of starch and 330 mg of water.

Example 12. Example 12 is carried out, as the example 11, only as a compound from the group of NSAIDs use Ketoprofen.

Example 13. 5.0 g disodium salt of glucosamine sulfate, 10 g of ibuprofen, 20 g of dimethyl sulfoxide, 5 g of isopropyl alcohol, 20 g of ethanol, 4 g of carbopol 940 is dissolved at a temperature of 60°With 40 ml of distilled water. The solution is stirred (200 rpm) for 3 h until complete cooling, bring the pH to 4.0 to 8.0 by addition of diethanolamine and Packed in tubes or cans. 1 g of the end product contains 50 mg of disodium salt of glucosamine sulfate (5.0 wt.%), 100.0 mg of ibuprofen (10.0 wt%), 200 mg of dimethyl sulfoxide (20 wt%), 50 mg of isopropyl alcohol, 155 mg of ethanol, 40 mg of carbopol 940, 5 mg diethanolamine and 400 mg of water.

Example 14. Example 14 is carried out, as example 13, only as a compound from the group of NSAIDs use in metacin.

The effectiveness of the tools studied in models of post-traumatic osteoarthritis, the collapse of the ears of rabbits and aseptic inflammation of the limbs of rats.

When the subchondral defects of the femoral head in rats caused by surgical injury of the articular cartilage, the proposed tool significantly reduces the size of the defect compared to control animals.

When intravenous papain in rabbits there is a collapse of the ears - sagging their peripheral end. The use of the proposed tool allows you to restore turgor ears, which indicates the inhibition of the destruction of the cartilage of the ears.

Aseptic inflammation caused by injection of dextran under the aponeurosis of the hind paws of rats. Anti-inflammatory effect of the proposed tools is manifested in the inhibition of the development of aseptic swelling of the limbs of rats.

The harmlessness of the proposed tool was evaluated by its impact on the conjunctiva of the eyes and skin of rabbits. Studies have shown no irritant effect means on the conjunctiva of the eye and intact skin.

The toxicity of the tools investigated in the chronic experience (2 months) in 12 pigs by cutaneous applications. It is established that it is not toxic and does not cause violations of histologica is anyone of the epidermis, the dermis and subcutaneous tissue.

The proposed tool has been tested in a clinical setting in 11 patients with osteoarthritis and knee. As the test tools used the ointment of the following composition (wt.%): the disodium salt of glucosamine sulfate - 10,0, diclofenac sodium 0.1, dimethylsulfoxide - 1, ointment base - the rest (example 4 description of the application). The ointment was applied on the affected joint daily 3-4 times a day and creeping until completely absorbed within 3 weeks. Efficiency study was conducted double-blind method, where as the comparison drug used drug Ointment handaxe (5% chondroitin sulfate and 10% dimethyl sulfoxide in the ointment base).

The intensity of the pain syndrome according to the visual analogue scale YOUR alone decreased from 3.8 to 2.6 points when moving from 6.8 to 3.2 points, when walking on the stairs from 6.8 to 5.5 points in the control group, respectively with 3.75 to 2.8; from 6.9 to 4.1 and from 7.0 to 5.6 points). A functional index Lekena decreased from 12.7 to 8.2 points (control from 12.3 to 8.9 points).

The tests have demonstrated the effectiveness of the tested ointments almost 77% of patients versus 65% for ointment handaxe, and the positive effect was reduced by 44% on average due to the high pharmacokinetics Monomeric saccharide.

1. For the treatment of diseases of the joints, containing the e saccharide, a compound selected from the group of nonsteroidal anti-inflammatory drugs, dimethylsulfoxide and ointment base, characterized in that as it contains saccharide salt of glucosamine and as nonsteroidal anti-inflammatory agents it contains ibuprofen, or nimesulide, or piroxicam or meloxicam or diclofenac salt, or indomethacin or Ketoprofen at the following content, wt.%:

Glucosamine salt0.5 to 10.0
Ibuprofen0,1-10,0
or Nimesulide0,1-1,0
or Piroxicam0,1-1,0
or Meloxicam0,1-1,0
or Diclofenac salt0,1-5,0
or Indometacin0,1-10,0
or Ketoprofen0,1-5,0
The sulfoxide1,0-20,0
Ointment baseThe rest of it.

2. The tool according to claim 1, characterized in that salts of glucosamine use of glucosamine hydrochloride, sodium, potassium or calcium salt of glucosamine sulfate, as well as salts of diclofenac its potassium or sodium salt.



 

Same patents:

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of N-desacetylthiocolchicine of the formula (I):

wherein n represents a whole number from 0 to 8; Y represents group CH2 or if n = 1 then can mean group NH also. These compounds elicit an anti-proliferative activity. Also, invention describes pharmaceutical composition based on compounds of the formula (I).

EFFECT: valuable medicinal properties of derivatives.

4 cl, 1 tbl, 4 ex

Substituted indoles // 2255087

FIELD: organic chemistry, biochemistry.

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EFFECT: valuable biochemical properties of compounds.

3 cl, 3 tbl, 29 ex

FIELD: medicine, pharmacy.

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EFFECT: improved and valuable properties of formulation.

8 cl, 16 tbl, 39 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of adamantane of the general formula:

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or

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EFFECT: improved method for preparing and treatment, valuable medicinal properties of compounds.

13 cl, 88 ex

FIELD: medicine.

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FIELD: organic chemistry and pharmaceutical compositions.

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23 cl, 6 dwg, 1 tbl, 1 ex

FIELD: medicine.

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EFFECT: higher efficiency of application.

11 cl, 2 ex

FIELD: organic chemistry, steroids, medicine, pharmacy.

SUBSTANCE: invention relates to 3-methylene-steroid derivative of the general formula (1):

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EFFECT: valuable medicinal properties of compounds, improved method for treatment.

38 cl, 1 tbl, 18 ex

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

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EFFECT: valuable medicinal properties of compounds and composition.

9 cl, 2 sch, 2 tbl, 29 ex

FIELD: veterinary science.

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EFFECT: higher efficiency of correction.

6 dwg

FIELD: cosmetic industry, cosmetics.

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EFFECT: improved preparing method, improved and valuable medicinal and cosmetic properties of base.

2 cl, 1 tbl, 4 ex

FIELD: medicine, dermatology, chemical-pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to an antifungal gel pharmaceutical composition based on ketoconazole and clotrimazole that are derivatives of imidazole. The composition comprises ketoconazole or clotrimazole as an active component, polyethylene glycol-400 (PEG-400) as a solvent, carboxyvinyl polymer as a gel-forming agent, polyethylene glycol as a gel stabilizing agent, organic amine or inorganic bas as a regulator of pH and water taken in the definite ratio of components. The composition is prepared by dissolving active component in PEG-400, dispersing carboxyvinyl polymer in water, successive addition to dispersion propylene glycol as a stabilizing agent and regulator of pH and combination of prepared solution and gel followed by stirring the mixture up to preparing the gel composition with pH 5-7. Invention provides preparing antifungal composition with reduced adverse effect.

EFFECT: improved preparing method, valuable medicinal properties of composition.

2 cl, 1 tbl, 11 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to curative ointments with anti-inflammatory effect and with biostimulating properties for treatment of burns, suppurative and infected wounds of different etiology and to a method for treatment above said diseases using the ointment said. The proposed ointment comprising bee wax and greasy basis comprises colophony additionally. As greasy basis the ointment comprises butter and vegetable oil in the following ratio of components, wt.-%: bee wax, 20-30; butter, 30-40; vegetable oil, 15-25; colophony, 15-25. Method involves applying ointment by thin layer 0.5-3 mm on dense cotton fabric, its applying to damaged site, keeping and removing ointment with change of bandage 1-3 times per 24 h for 3-14 days. Method provides enhancing the therapeutic effectiveness of ointment due to significant acceleration the healing process of suppurative wounds and insidious furuncles being the ointment doesn't cause irritating effect.

EFFECT: improved and valuable medicinal properties of ointment.

2 cl, 4 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to medicinal preparations used for treatment of suppurative wounds. Invention involves applying boric acid (powder) and multi-component ointments on water-soluble base (Laevomecolum or Laevosinum) taken in the ratio 1:10 and used for treatment of suppurative wounds. Invention provides the development of agent exhibiting the expressed antibacterial, dehydrating and necrolytic effect.

EFFECT: valuable medicinal properties of agent.

2 ex

FIELD: medicine, in particular homoeopathic ointment for treatment of hemorrhoids, dermatitis and rhinitis.

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EFFECT: ointment for treatment of hemorrhoids, dermatitis and rhinitis of improved effect.

1 tbl

FIELD: medicine.

SUBSTANCE: the present innovation deals with preparing ointments to be applied at treating both surface and deeply penetrating cutaneous burns and other skin diseases, as well. Composition of the suggested ointment includes, weight%: 45…67% food sunflower oil, 15…37% food olive oil, 1…2% Calendulae officinalis extract, 0.8…1.8% labdanum, 2.5…8% colophony, 6.5…11.5% white bee wax, 0.7…1.8% the main bismuth gallate and 0.7…1.8% camphor. The suggested ointment is highly efficient for rapid and successful treatment of burns III and IV degree. It should be also applied for treating shin's ulcer and, also, in gynecology - for treating inflammation of uterine cervix.

EFFECT: higher efficiency of therapy.

4 ex

FIELD: pharmaceutics.

SUBSTANCE: the present innovation deals with cryoprotective ointment containing recombinant interferon-α2. The suggested cryoprotective ointment contains recombinant interferon-α2, glycerol, polyethylene glycol 300-6000, polyglucin, buffered 0.02%-Trilon B solution at pH of 5.5-7.0 and ointment foundation at a certain content of components per 1.0 g ointment. Additionally, cryoprotective ointment could contain glycine 3,7-bis(dimethylamino)phenothiazonium chloride, dry immunoglobulin preparation or dry immunoglobulin preparation for enteral application. Ointment foundation of cryoprotective ointment could contain water-free lanolin, Vaseline and Vaseline oil, at the following ratio of components: 2.5;3.5:1 - 6.5:0.5:1. The innovation provides maximal safety of recombinant interferon-α2 activity in cryoprotective ointment at multiple alteration of positive and negative environmental temperature and at keeping cryoprotective ointment under these conditions.

EFFECT: higher efficiency of application.

8 cl, 8 ex

FIELD: pharmaceutics.

SUBSTANCE: the suggested composition has got viscosity being below of about 15000 cP and pH being approximately 3.0-9.0 for treating human skin diseases. He suggested composition consists of (a) therapeutically efficient quantity of, at least, one compound being useful in treating the above-mentioned disease; (b) pharmaceutically acceptable, partially bound polymer of polyacrylic acid being compatible with the compound; (c) not obligatory, a solvent being mixed with water, (d) not obligatory, a conserving agent, (e) not obligatory, a component of butyric phase and acceptable surface-active substance, and (f) water. The suggested composition is useful to treat inflammatory skin disease, acne or acne erythematosa. The composition of low viscosity has got its advantage in the fact that it is applied more accurately when in contact with a container that doses the composition in the form of drops.

EFFECT: higher efficiency of application.

23 cl, 15 ex, 19 tbl

FIELD: medicine, gynecology, pharmacology, pharmaceutical industry.

SUBSTANCE: invention proposes a preparation that comprises bacterial mass of live microorganisms as an active component, protecting medium and fat base. The preparation comprises lactobacilli as bacterial mass and one or some eubiotic microorganisms taken among the following group: bifidobacteria, streptococci and lactococci taken in the amount per a single dose. Also, the preparation comprises additionally an acceptable sorbent and a biologically active supplement. Also, invention relates to a method for preparing this preparation that involves preparing firstly lactobacilli bacterial mass and one or some genus of eubiotic microorganisms taken among the following group: bifidobacteria, streptococci and lactococci. Then the prepared bacterial mass of microorganisms is immobilized on sorbent used in medicine in its ratio to bacterial mass of microorganisms = (9-1):(1-9) followed by addition of the protecting medium and biologically active supplement to formed mass in the necessary amount. Also, invention describes a method for prophylaxis and treatment of bacterial vaginitis that involves intravaginal administration of the preparation described above in the amount 1-3 doses, 1-3 times per 24 h. The treatment course is prescribed individually. Invention provides expanding assortment of agents used for treatment of bacterial vaginitis. Invention can be used in obstetric-gynecological practice.

EFFECT: improved method for vaginitis treatment, valuable medicinal properties of preparation.

13 cl, 4 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: the present innovation deals with medicinal preparation as an ointment for treating skin burns. The suggested preparation contains bee wax, propolis and vegetable oil. Thus, application of initially intact propolis and bee wax in combination with fatty foundation as vegetable oil enables to cheapen and simplify the technique to prepare the preparation, and optimally matched consistence provides prolonged safety of the preparation and accelerates healing of skin burns.

EFFECT: higher efficiency of therapy.

1 cl, 2 ex

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