SUBSTANCE: invention refers to pharmaceutical industry and represents a preparation possessing the anti-inflammatory action, stimulating the mucosa regeneration, and containing magnesium-chloride mineral bischofit brine 1.27±0.01 g/ml with normalised specific gravity, slastiline, menthol, thymol, and a stabilising agent differing by the fact that it contains magnesium-chloride mineral bischofit brine free from technogenic impurities, with the ingredients in the preparation are taken in specific proportions, g.
EFFECT: reducing acute daily oral toxicity in 1,7-1,9 times.
The invention relates to the field of medicine, new medicines, exhibiting anti-inflammatory, antimicrobial, wound healing and stimulating phagocytosis action.
It is widely known and used in the clinical practice of medicine "Policeman", which are standardized by the specific gravity of 1.27±0.01 g/ml of brine chlorimines mineral bischofite, optionally containing corrector taste slastion, antiseptics menthol and thymol, stabilizer tween-80 or gelatos [RF Patent №2053774 (1996). Spasov AA, Temkin ES, O. Ostrovski, Skorokhodova E.N., Vdovin G.P., Perevozchikov GG, Gerchikov L.N., Borovsky E.V., Ermakov VA // Drug having anti-inflammatory and stimulating regenerative processes in the mucous membranes of the action (AC 33/00) / bul. Fig. - 1996. No. 4]. Shown high efficiency of application of Polycatan in dental practice, dermatology in inflammatory diseases of the upper respiratory tract, sensorineural hearing loss, hypertension and other diseases [Spasov AA Magnesium in clinical practice. - Volgograd: Publishing House. LLC "Lad", 2000. - 272].
Mineral bischofite is a uranyl magnesium chloride formula MgCl2×6H2O Deposit discovered large areas of the Caspian is hollow and Volga monocline at depths of 1000-2000 m Industrial production bischofite is produced by the method of underground vysalivaniya that allows you to extract 75-85%bischofite brine. The resulting brine is diluted with water to the required concentration and standardize density. However, the presence of a number of natural and man-made impurities in the solution of bischofite significantly limits its medical use. Developed drug and Spa facilities on the basis of bischofite, including "Balikatan, only apply topically in the form of mouthwashes, baths, compresses, solutions for electrophoresis, ointments, liniments, pastes, or patches. Impurities included in the bischofite include the salts associated alkaline earth metals (beryllium, calcium, barium), iron and heavy metals [Spasov AA, Orobinskaya T.A., L.A. Smirnova // Success Fiziol. Sciences. - 1997. - So 28. - V.2. - S-93]. In addition, iron is the most significant man-made mixture as a product of corrosion of steel reinforcement wells. A particularly large impact on the quality of bischofite have impurities of petroleum products, which are mandatory auxiliary component in the production of bischofite and pumped into the well. In this regard, the application of bischofite as the basis for drugs used orally, without additional deep cleaning is impossible.
The development of otany our earlier method of purification of bischofite [RF Patent №2442593 (2012). Petrov V.I., Spasov AA, Ozerov A.A., sysouev B.B. // cleaning Method bischofite (AC 33/14, 01F 5/00, SW 1/00) / bul. Fig. - 2012. No. 5] provides a significant decrease in the content of iron and other impurities. This allows you to create based on purified bischofite new drug and Spa tools, including for enteral application.
The purpose of the proposed invention is the development of medicines "Policeman"with less toxicity and suitable for oral administration.
The invention consists in the use of brine chlorimines mineral bischofite, free from man-made impurities, to obtain drugs "Policeman".
To conduct Toxicological studies have been made in accordance with [RF Patent №2053774 (1996). Spasov AA, Temkin ES, O. Ostrovski, Skorokhodova E.N., Vdovin G.P., Perevozchikov GG, Gerchikov L.N., Borovsky E.V., Ermakov VA // Drug having anti-inflammatory and stimulating regenerative processes in the mucous membranes of the action (AC 33/00) / bul. Fig. - 1996. No. 4] samples of the medicinal product "Balikatan" based on purified and unpurified bischofite with the same quantitative composition:
|Brine mi is erala bischofite (density of 1.27±0.01 g/ml)||- 100|
|Slastion (aspartame, E 951)||- 0,01|
|Stabilizer (tween 80)||- is 0.0002|
The definition of acute daily toxicity of the proposed medicinal product "Balikatan" based on purified brine mineral bischofite, and known means "Policeman", produced from the crude brine mineral bischofite, were performed in the laboratory of medicinal safety research Institute of pharmacology, Volgograd state medical University. The experiments were performed on rats of both sexes, which investigational drugs were administered intragastrically in various doses in accordance with [Manual on experimental (preclinical) study of new pharmacological substances", Ed. Rugarama. - Ed. 2. - M.: JSC "Publishing house "Medicine", 2005. - 832]. It is established that the death of animals was recorded after the introduction of them "Balikatan" based on purified bischofite in the dose range from 4.0 to 9.5 ml/kg, and the introduction of Polycatan" based on crude bischofite in doses ranging from 2.0 to 6.0 ml/kg per animal. The magnitude of LD50 at the same time slightly differed for female rats and rats-males (table 1).
|Sharp daily toxicity of the medicinal product "Balikatan" after intragastric administration|
|№ p/p||Medication||Acute toxicity, LD50ml/kg|
|1||"Balikatan" based on purified bischofite||6,30(4,95-8,65)||7,20(5,86-9,05)|
|2||"Balikatan" based on crude bischofite||3,79(2,85-4,95)||3,72(3,05-4,59)|
For clinic manifestations of toxic effects was characterized by the presence of sedation, inhibition of mobility, breathing, muscle relaxation, reduction in body temperature, reactions to pain and audio stimuli. These signs occurred in animals mainly after the introduction of Polycatan" after 10-15 min in toxic doses. Death was preceded by tonic twitching limbs, lateral position, sudden respiratory depression. The death of the animals ü noted in the first day during the first 4 hours of observations. The restoration of the physical and behavioral activity in animals that remained alive were observed at the end of the second day of observations. In subsequent timing observations of mortality were noted. According to the results of the registration of the dynamics of body weight of the rats was recorded decrease in weight gain in the experimental animals (on average by 10% in comparison with control) in the first week and gradually restore it to the end of the 2-week observation period.
Thus, the use of brine chlorimines mineral bischofite, free from man-made impurities, to obtain drugs "Balikatan allows 1.7-1.9 times lower acute toxicity of the drug compared with Polycatenar", obtained on the basis of the crude bischofite.
Drug, has anti-inflammatory and stimulating regenerative processes in the mucous membranes of the action, containing standardized by the specific gravity of 1.27±0.01 g/ml of brine chlorimines mineral bischofite, slastion, menthol, thymol and stabilizer, characterized in that it contains brine chlorimines mineral bischofite, free from man-made impurities, in the following ratio of components, g:
|brine chlorimines mineral bischofite||100|
SUBSTANCE: azithromycin infusions are combined with the daily administration of metronidazole. Azithromycin is administered in a single dose of 1.0 g on the 5th post-infusion day. The treatment is combined with the daily administration from the first day of the metronidazole therapy twice a day in a dose of 500 mg for 14 days.
EFFECT: effective treatment ensured by reducing a dose and risk of side effects.
SUBSTANCE: combination contains fulvic acid or a salt thereof, and an antibiotic representing oxacillin or gentamycin, or a combination thereof. The invention also refers to a method of treating or inhibiting a bacterial infection in an individual that involves administering an effective amount of a composition containing the above combination.
EFFECT: invention provides the synergetic effect of the combination of fulvic acid and antibiotics.
16 cl, 1 tbl, 7 dwg, 2 ex
SUBSTANCE: invention refers to a new derivative of β-lactam ceftriaxone antibiotic, which is presented with general formula (I), containing group R1=3-[[(2-methyl-6-oxide-5-oxo-2,5-dihydro-1,2,4-triazine-3-il)sulphanyl]methyl] (a), where R2=sodium, R3=2-amino-3-mercaptopropionate ion -HOOC-CH(NH2)-CH2-S-. Compound is synthesised with interaction of β-lactam ceftriaxone antibiotic with amino acid with cysteine.
EFFECT: derivative of β-lactam ceftriaxone antibiotic, which shows antibacterial properties in relation to bacteria Staphylococcus aureus 25923 and Escherichia coli 25922.
2 cl, 1 tbl
SUBSTANCE: invention refers to a number of bicyclic nitroimidazole-replaced phenyloxazolydinones of the following structural formula (I):
containing nitroimidazole circle, or to its pharmaceutically acceptable salt; where R1 represents hydrogen, (C1-C6)alkyl or aryl; n is equal to 0, 1 or 2; X1 and X2 independently represent H, CF3, CI, OCF3 or F; G represents -OH, triazole or -NHCOR2; R2 represents (C1-C6)alkyl, cycloalkyl or aryl; and L represents a bond or a linker group chosen from any combination 2-3 of the following groups: 1) (C1-C6)alkylene, 2) (C3-C8)cycloalkylene, 3) arylene, arylene-replaced CN, ore arylene-replaced F, 4) group chosen from the group consisting of
where R10 represents H, CF3, hydroxyl, amino, alkyl, alkylamino, alkoxy or aryl, and R13 represents H, hydroxyl, amino, alkyl, alkyl amino, alkoxy or aryl, or R13 in combination with nitroimidazole circle can form spiral-shaped structure, 5) -C(=O)-, 6) -O-, 7) -S(O)n-, in which n is equal to 0.1 or 2, 8) -N(R3)-, 9) -C(R4)=C(R5)-, R3 represents hydrogen, (C1-C6) alkyl or aryl, and R4 and R5 represent hydrogen, (C1-C6) alkyl or aryl, or R4 and R5 can be combined together so that they can form a bond. Besides, the invention refers to pharmaceutical composition for treatment of bacterial infection based on compounds of formula I, as well as to a bacterial infection treatment method.
EFFECT: invention describes new compounds that have antibacterial activity against a line of wild type and stable lines of pathogenic microorganisms, and as a result, are suitable for prevention, control and treatment of a number of human and mammal bacterial infections caused by these pathogenic microorganisms such as bacillus Kochii.
15 cl, 93 ex, 1 tbl, 22 dwg
SUBSTANCE: invention relates to a water-soluble amide derivative of salicylic acid, specifically a sodium salt of ethyl ether of N-salicyloylglycine (2-[(2-ethoxy-2-oxoethl)carbomoyl]sodium phenolate) , and can be used in chemical and pharmaceutical industry.
EFFECT: sodium salt of ethyl ether of N-salicyloylglycine, having antibacterial, antifungal and antilysozymic activity.
3 tbl, 4 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to field of pharmaceutical industry and medicine, in particular, intended for treatment and care of oral cavity, which contains quantity of antioxidant, presenting ratio of extract weight to weight of antioxidant in range 1:1 to 5:1, and magnolia extract.
EFFECT: composition according to the claimed invention ensures enhanced antimicrobial action.
13 cl, 2 tbl, 4 ex
SUBSTANCE: invention relates to medicine, namely to maxillofacial surgery and traumatology and can be applied for formation of antimicrobial coating in manufacturing titanium-based intra-tissue endoprostheses. For this purpose preliminary preparation of silver-containing solution, preliminary preparation of implant surface and coating formation are carried out. In the process of preparation of silver-containing solution first hydroxyapatite powder is placed into 0.04% solution of AgNO3. After that, powder is kept in air at room temperature for the time necessary for qualitative soaking of hydroxyapatite particles with AgNO3 solution. Then, sediment is filtered and washed with hot water, and dried at 200°-300°C for 4-6 hours and annealed at 600°-700°C for 2-3 hours. Preliminary preparation of implant surface is performed by jet processing of surface with electrocorundum powder under pressure. Formation of coating is carried out by plasma sputtering of first titanium sublayer and then silver-containing hydroxyapatite powder. Plasma sputtering of titanium sublayer is performed at voltage 35 V, current intensity 450 A, distance of sputtering 100 mm and titanium powder dispersion 100-120 mcm, consumption of argon being 55-60 l/min. Plasma sputtering of silver-containing hydroxyapatite powder is performed at current intensity 450 A, voltage 36 A, distance 80 and 120 mm, dispersion 70-75 mcm and argon consumption 65-70 l/min.
EFFECT: method ensures obtaining implant coating, contributing to fast and reliable osteointegration of the implant due to formation of developed surface morphology and creation of antimicrobial effect in tissues adjacent to endoprosthesis.
4 tbl, 2 dwg
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical compositions for treating a microbial disorder in an individual. As an agent, the pharmaceutical compositions (formulations) contain an antimicrobial peptide (AMP) containing IL-22 with a preset amino acid sequence and a nucleotide sequence coding AMP, or a modulator thereof specified in a group consisting of IL-6, IL-18, IL-23, REG lα, REG Iβ, HIP/PAP, REG III, REG IV, RS and lymphotoxin (LF), or agonist IL-22 in an effective amount and a pharmaceutically acceptable carrier. Using agonist IL-22 in the compositions provides higher IL-22 expression and/or activity with the agonist specified in the group of polypeptide, nucleic acid, and antibody. The therapeutic compositions are applicable for the intravenous administration.
EFFECT: using the compositions according to the invention provides higher expression of the antimicrobial pectin representing REGIIIβ and/or REGIIIγ that provides the protection of the intestinal epithelial barrier integrity, induces healing of wounds caused by the microbial disorder.
29 cl, 28 dwg, 10 ex
SUBSTANCE: invention refers to medicine, namely surgery and intensive care, and may be used in treating the patients with developed sepsis with underlying abdominal and retroperitoneal diseases. For this purpose, the management starts with a session of endotoxin absorption. That is followed by the intravenous administration of a bactericidal antibiotic, e.g. such as β-lactam or fluoroquinolone in the amount of 1.1-1.5 daily dose; then 30-60 minutes later, endotoxin sorption is combined with de-hydration hemofiltration in a dose of 45 ml/kg/h for 6-8 hours. The whole procedure is accompanied by the infusion therapy using active solutions specified in a group of low- and high-molecular hydroxyethyl starch and dextran in the amount of 5-10 ml/kg/h. Before the beginning of endotoxin sorption, as well as one day after the termination of hemofiltration and sorption, the blood endotoxin concentration is controlled. If the recorded endotoxin concentration is decreased at least by 60%, another procedure is performed.
EFFECT: method provides higher survival rate in the patients suffering the above pathology, as well as reduces a risk of septic shock ensured by the pathogenically caused regimen of the combination of various human body effects providing a degree of systemic endotoxemia to be decreased.
2 cl, 2 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: group of inventions refers to medicine. An antimicrobial composition contains chlorhexidine and pentane-1,5-diol, wherein the amount of chlorhexidine makes 0.000001 to 5 wt %, while the amount of pentane-1,5-diol makes 1 to 75 wt %. The composition is applicable for local administration; it contains a carrier and a gelling material.
EFFECT: group of inventions enables applying the composition for non-therapeutic disinfection, in treating skin infections.
SUBSTANCE: invention refers to derivatives of oxazolopyrimidine in any of their stereoisomeric forms, or in the form of a mixture of stereoisomeric forms specified in Claim 1.
EFFECT: oxazolopyrimidine derivatives having agonistic activity in relation to Edg-1 receptor.
5 tbl, 319 ex
SUBSTANCE: invention relates to medicine, namely to general surgery, and can be applied in prevention of purulent-inflammatory complications of anterior abdominal wall wounds in case of strangulated ventral hernias. For this purpose, 10% solution of colloidal nanosilver is introduced into operation wound after elimination of strangulation, with preliminary injections on perimetre of hernial orifice edges in dose 0.1 ml of solution per 1 cm2 of aponeurosis. After that, after fixation of synthetic implant, injections are made along the line of sutures on periphery in dose 0.1 ml per 1 cm2 of suture. After that, subcutaneous adipose cellular tissue is infiltrated with solution of colloidal nanosilver in dose 0.1 ml of solution per 1 cm2 of wound.
EFFECT: method ensures considerable reduction of risk of development of purulent-inflammatory complications in patients with said pathology, as well as acceleration of processes of tissue reparation due to application of biologically active colloidal solution of nanosilver, producing selective impact only on pathogenic microorganisms, on all layers of anterior abdominal wall and zone of synthetic implant fixation.
5 cl, 1 ex
SUBSTANCE: invention refers to medicine, namely purulent surgery, and may be used for treating infected wounds. That is ensured by surgical treatment of suppurative focuses and exsection of necrotised tissues. Then the whole wound surface is treated with 10% colloidal nanosilver. The subcutaneous fat is infiltrated with 10% colloidal nanosilver at 0.1 ml of the solution per 1 cm2 of the wound. Additionally, the wound is covered with a sterile 10% colloidal nanosilver wipe.
EFFECT: method enables reducing the length of wound granulation and epithelisation ensured by using the biologically active colloidal nanosilver solution coating all wound layers and rendering selective action on pathogens only.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to pharmaceutical industry, specifically to an agent showing antimicrobial activity.
EFFECT: agent possessing antimicrobial action and representing robinia (Robinia pseudaacacia L) seed essence prepared by collecting the seeds in October and extracting them three times in petroleum benzene under certain conditions.
2 tbl, 1 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: group of inventions refers to medicine, particularly to ophthalmology. One of the objects is using 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diole (compound A), its separate isomers and a mixture of the same isomers, or pharmaceutically acceptable salts, solvates and hydrates thereof for preparing an agent for treating keratoplasty or refractive keratoplasty consequences. The second object is a method of treating the keratoplasty or refractive keratoplasty consequences in an individual in need thereof that involves administering a therapeutically effective amount of 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diole (compound A), its separate isomers and mixtures of the same, pharmaceutically acceptable salts, solvates and hydrates thereof into the above individual.
EFFECT: invention provides treating the eye disorder consequences.
SUBSTANCE: invention refers to medicine, and may be used for treating septic wounds and burns. A composition possessing antibacterial action contains active metal biocomplexes with 5-nitroimidazole and β-pyridine carboxylic acid and a base providing a soft dosage form. As a gelling agent, there may be used modified cellulose derivatives, additionally comprising methyl monosilane hydrogel (enterosgel) and/or polyvinylpyrrolidone, or an alloy of polyethylene oxide-400 and polyethylene oxide-1500. As a mixture of hydrophilic substances, the base contains substances specified in a group of: polyethylene oxides, dimexide, glycerol and aerosol, may comprise at least one target additive of: anaesthetic - trimecaine, pyrromecaine, lidocaine, or a mixture thereof, a repair process stimulator - methyluracil, acemine, solcoseryl, Spirulina microalgae (Spirulina platensis), or a mixture thereof, antiseptic - miramistine, chlorhexidine digluconate, dioxidine or a mixture thereof. The composition is presented in the form of an ointment or gel.
EFFECT: invention provides the improved microcirculation in wound tissues, as well as anti-inflammatory action, repair process stimulation.
5 cl, 6 tbl, 4 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to microencapsulation of drugs through the example of rivanol which can be used as an antimicrobial, antifungal topical preparation. A method for preparing microcaplues of rivanol in a water-soluble polymer representing polyvinyl alcohol or polyvinyl pyrrolidone is implemented by physical-chemical precipitation with a solvent wherein a precipitant is acetone. The process is carried out at 25°C with no special equipment required.
EFFECT: method for preparing the microcapsules of rivanol provides simplifying the process of microencapsulation.
13 dwg, 5 ex
SUBSTANCE: invention relates to medicine, namely to surgery and can be used for prevention of postoperative wound suppuration. For this purpose perforated tube is placed on the bottom of wound surface and its ends are brought outside through formed on patient's skin counteropenings with further fixation of tube to skin and their hermetic closing. Starting from the following after operation day and further on 2-3 postoperative days, 100-150 ml of antiseptic solution are forced fractionally once daily into wound through one of tube ends, the second one being closed. Intra-wound hydraulic compression of antiseptic is created and increased to such a degree that partial leakage of solution between skin sutures takes place. After that, compressed second end of tube is opened and all antiseptic is drained from wound. Then, remaining wound and drainage tube content is aspirated completely. After that from 3-4 to 9-10 days washing of wound in flow manner without element of hydraulic compression is continued on the same daily single time basis.
EFFECT: method makes it possible to reduce number of postoperative wound suppurations, thus ensuring wound healing with primary intention.
FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention refers to new substituted phenoxyacetic acids of general formula 1 possessing the properties of a selective antagonist inhibiting A2a adenosine receptor activity. The compounds may be used in preventing and treating central nervous system diseases, such as cognitive disorders, Parkinson's disease, or depression, tumour diseases, inflammatory processes. The invention also refers to an agent for intensification of immune response or action of drug preparations in the combination treatment of the diseases. In general formula
, R1, R2 and R3, optionally simultaneously represent hydrogen. C1-C5alkyl, C3-C5alkenyl or C3-C5-alkynyl; R4 represents hydrogen, a halogen atom, hydroxyl, C1-C3alkyl, C1-C3alkyloxy; R5 represents hydrogen, C1-C3alkyl, the group -C(O)R6;R6 represents hydroxyl, C1-C5alkyloxy, C3-C5alkenyloxy, C3-C5alkynyloxy optionally substituted by an amino group wherein the substitutes optionally identical are specified in hydrogen, C1-C3alkyl optionally substituted by a mono- or dialkylaminogroup, an alkyloxygroup, 5-6-member saturated heterocyclyl containing 1-2 heteroatoms specified in nitrogen and oxygen: pyridyl, phenyl optionally substituted by 1-3 methoxygroups; or optionally substituted 6-member, optionally annulated with 5-member unsaturated heterocyclyl, saturated heterocyclyl containing 2 nitrogen atoms wherein the substitutes are specified in C1-C3alkyl optionally substituted by 5- member heteroaryl containing 1-3 heteroatoms specified in nitrogen and oxygen; or 6- member optionally saturated heterocyclyl containing 1-2 nitrogen atom optionally substituted by C1-C3alkyl, oxo, optionally substituted by phenyl; a dashed line with an accompanying continuous line represents a single, double or triple bond.
EFFECT: preparing new substituted phenoxyacetic acids of general formula 1 possessing the properties of the selective agonist inhibiting A2a adenosine receptor activity.
15 cl, 3 tbl, 7 ex
SUBSTANCE: invention refers to medicine, namely surgery, and may be used for treating abscesses, festered residual cavities and ganglions. The cavity contents are daily aspirated through a catheter in laboratory animals (male rabbits) suffering simulated hepatic abscesses of the diameter of 1.5 cm. Then the abscess cavity is filled with copper nanoparticle suspension in 0.9% physiologic saline of the concentration of 1 mcg/ml. A laser light guide provided with a diffuser is placed in the cavity centre to expose to laser light at wave length 630 nm in a continuous mode, output power 35 mWt for 3 minutes.
EFFECT: method enables intensifying antimicrobial action of copper nanoparticles under laser light, starting treating without specifying an agent, suppressing pathogenic microogranisms over a relatively short time, stimulating repair processes successfully, reducing toxic action of nanoparticles on macroorganism, considerably reducing a length of treating festered cavities.
2 dwg, 1 tbl, 1 ex
SUBSTANCE: in formula
each of R1 and R2 independently represents H or C1-6alkyl; or R1 and R2 together form C3-6cycloalkyl circle, which is optionally replaced with one or more R2'; R2' represents C1-6alkyl, hydroxy group, halogen, amino group, C1-6alkoxy group, C1-6hydroxyalkyl or C1-6haloalkyl; R3 represents H or N(R4)(R5); R4 represents H, C1-6alkyl or C(=O)OR4'; R4' and R5 represents H or C1-6alkyl; represents H or C1-6alkyl; or R2 and R3 together form 5-membered heterocycle containing 1 atom of N in the amount of heteroatom, which is optionally replaced with one or more R2'; Q represents CH or N; Z1 represents (CH2)u; u and v mean 1; Z2 represents (CH2)v; m, n, p, r, q mean 0; Y1 represents CH(Y1'); Y1' represents H or C1-6alkyl; Y2 represents H or represents C1-6alkyl. Invention also refers to compounds of structural formulae (II), (IV) and to pharmaceutical composition containing the above compounds.
EFFECT: improving inhibiting activity in relation to JNK kinase.
10 cl, 4 tbl, 23 ex