Local pharmaceutical antibacterial composition of active biometallic complexes

FIELD: medicine.

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

 

The invention relates to medicine, namely to pharmaceutical drug used in the treatment of wounds and burns, purulent-inflammatory diseases of the skin, to accelerate and improve healing.

Known gel cleanser "Metrogyl dent", which as the active substance contains metronidazole and chlorhexidine. Excipients: disodium edetate, menthol, saccharin sodium, propylene glycol, carbomer-940, purified water.

The disadvantages of gel Metrogylum dent" can be attributed to its use only for the treatment and prevention of infectious-inflammatory diseases of the oral cavity.

Known remedy ointment the vegetable "levomekol, FS 42-2922-98 widely used for the local treatment of purulent infection. As active substances ointment the vegetable "levomekol contains chloramphenicol and methyluracil and cooked on hydrophilic polietilenoksidnoy basis. Used for the treatment of wounds infected with a mixed flora, including staphylococci, Pseudomonas aeruginosa and Escherichia coli.

The closest is the gel Metrogylum", approved by the Pharmacological Committee SRF March 1, 2004, street No. 56, reference number: P # 011666/04. As the active substance gel Metrogylum contains metronidazole and excipients: propylhydroxybenzoate, propylene glycol, carbomer-940, edetate disodium, sodium GI is roxid, water.

The disadvantages of gel Metrogylum" can be attributed to only intervaginal application and should not be used in otorhinolaryngology.

The disadvantages of this drug is that it does not possess local anesthetic action.

High feasibility in the development of new methods for the speedy cleansing wounds from microorganisms and their metabolic products, necrotic tissue is well known.

Targeted elimination devitalizirovannaya tissue drainage and sorbents, proteolytic enzymes and new chemical antiseptics - actively studied [1, 3].

There is a method of treatment of purulent wounds by surface sorption-application of detoxicative described in the monograph by M. R. lubarsky, A. Letyagin, V.H. Gabitova R. U., V.V. Semko and A.A., Palienko - "Sorption operationally drugs in septic surgery [2], based on the use of operatingrange sorbent SUMS-1 immobilizerturning on it nigedasi and hyaluronidase.

There is a method of treatment of purulent wounds by local sorption-application treatment (patent RU 2195291 C2, the authors Bogomolov M.I., Cherednik AV, Blinov NV, Bogomolov N.N., published 27.12.2002 bull. No. 36) [3], based on the use of the sorbent granules RIVERTWIN saturated solution hypochlo the ITA sodium.

In the inventive pharmaceutical preparation to improve the efficiency of the purification process of purulent wounds and cuts treatment time by increasing the activity of sorption therapy in the first phase of wound healing additionally include a hydrogel of metiltselyulozy acid (enterosgel).

Object of the present invention is to provide a pharmaceutical preparation for topical application in the form of soft medicinal forms based on new active biometeorological.

Technical results that may be obtained by using the present invention: the expansion of the scope; increased therapeutic activity; improved ease of use; reducing consumption of biologically active substances; giving the anaesthetic effect; improvement of microcirculation in wound tissue; the anti-inflammatory effect; stimulation of reparative processes.

To solve this problem is proposed pharmacological drug topical application "Nimesil" in the form of soft medicinal forms, consisting of one or a mixture of biologically active metal complexes, for example, derivatives of 5-intorimidazole and β is pyridineboronic acid (hereinafter "Biometeorology") and a framework to provide soft dosage form of the drug, when following the m ratio of components wt.%:

active biomechatronics
and/or a mixture of biometeorological0,1-2,0
- basisrest

The proposed remedy for topical application in the form of soft medicinal forms additionally contains a special additive that is compatible with bimetallicheskie, in the following ratio, wt.%:

active biomechatronics
and/or a mixture of biometeorological0,10-2,00
additives target3,11-9,00
baserest

As the target additives can be used local anesthetic substance, and/or stimulator of reparative processes, and/or antiseptic.

With the aim of providing an anesthetic effect in the proposed pharmaceutical preparation may contain a local anesthetic substance in the following ratio, wt.%:

active biomechatronics
and/or a mixture of biometeorological0,10-2,00
local anesthetic substance3,00-5,00
baserest

This local anesthetic substance can be, for example three-machain, piromekain, lidocaine, or their mixture.

In addition, the proposed pharmacological drug may include a stimulator of reparative processes in the following ratio, wt.%:

active biomechatronics
and/or a mixture of biometeorological0,10-2,00
stimulator reparative processes0,10-3,00
baserest

This substance, which is a stimulator of reparative processes may be, for example, methyluracil, atsemin, solcoseryl, cuts spirulina (Spirulina piftensis), ascorbic acid, nicotinic acid or their mixture.

We offer pharmaceutical preparation may contain IU toyesterday substance and stimulant of reparative processes in the following ratio of components, wt.%:

active biomechatronics
and/or a mixture of biometeorological0,10-2,00
local anesthetic substance3,00-5,00
stimulator reparative processes0,10-3,00
baserest

We offer pharmaceutical preparation may contain a local anesthetic agent, stimulant reparative processes and antiseptic in the following ratio, wt.%:

active biomechatronics
and/or a mixture of biometeorological0,10-2,00
local anesthetic substance3,00-5,00
stimulator reparative processes0,10-3,00
antiseptic0,01-1,00
baserest

In this matter, I have laudisa antiseptic, may be, for example, Miramistin, dioxidine, chlorhexidine or their mixture.

In accordance with the invention of soft medicinal forms are buttery soft dosage forms (ointments and gels.

In the proposed pharmacological basis of preparation contains generatively and a mixture of hydrophilic substances in the following ratio, wt.%:

Mixture No. 1 ("Nimages-1")

gelling4,00-8,00
(modified derivatives of cellulose and additionally
include a hydrogel of metiltselyulozy acid (enterosgel) ratio
component 3:1, respectively)
dimexide5,00-10,00
glycerin5,00-10,00
waterrest

Mixture No. 2 ("Nimesil-2")

gelling4,00-8,00
(modified derivatives of the cellulite, tighten the PS and additionally
include polyvinylpyrrolidone in the ratio
component 1:1, respectively)
dimexide10,00-20,00
glycerin5,00-10,00
Aerosil2,50-5,00
waterrest

Blend # 3 ("Nimesil-3")

policlinical-15005,0-of 17.0
policlinical-40020,0-68,0
dimexide5,0-10,0
glycerin5,0-10,0
waterthe rest of it.

Features alloy PEO-400 and PEO-1500 in the ratio 8:2, respectively, as the most optimal for the preparation of ointments used in the treatment of purulent-inflammatory processes and meet all the requirements of the basics of this type.

One of the major problems in the local treatment of wounds and burns is the hearth is of pain. With this purpose in the proposed pharmacological drug used local anesthetic agent.

As anaesthetic substances can be used: lidocaine, trimekain (retains its activity in an acidic environment, which is characterized by a purulent wound), piromekain or their mixture.

With the purpose of providing additional stimulation of repair processes in the wound proposed pharmaceutical preparation may contain methyluracil, atsemin, solcoseryl, cuts spirulina (Spirulina platensis), ascorbic acid or their mixture.

Plastic surgery does not provide a local irritant, accelerates the processes of cell regeneration, reduces the healing time of wounds, stimulates cellular and humoral defense factors, anti-inflammatory, stimulates Erythro - and leucopoiesis.

The atsemin - accelerates tissue regeneration and epithelialization processes and is used for the treatment of nonhealing wounds and burns.

Solcoseryl - extract blood of cattle, released from proteins and non-antigenic activity. Accelerates the growth of granulation and capitalizatio wounds, improves metabolic processes in the tissues.

Cuts spirulina (Spirulina platensis)as a stimulator of reparative processes. Grown technology NPP "S", Samara. Contains balanced the amounts needed for human essential amino acids, vegetable fats with a predominance of unsaturated fatty acids, vitamin A (in the form of beta carotene), B1B2B12E, Inositol, minerals and trace elements, natural biologically active pigments (chlorophyll, phycocyanin, and others); normalizes metabolism, stimulates the immune system, promotes the excretion of toxins, accelerates regeneration and epithelization of tissues.

Ascorbic acid (vitamin C) is a white crystalline powder sour taste. Easily soluble in water, soluble in alcohol; has pronounced antioxidase properties involved in the formation of tetrahydrofolic acid and regeneration of the tissues, the synthesis of steroid hormones, collagen, procollagen.

Aerosil colloidal silica, when applied externally, is not irritating to the skin, respects skin's metabolism. Fine micronized powder with a particle size of from 4 to 40 microns (generally 10-30 μm), a density of 2.2 g/cm3has a large specific surface area of 50 to 400 m2/year In water and in alcohol concentration 1-3% form a turbid suspension, with liquids having a refractive index of 1.45 forms a transparent system (glycerin, vaseline oil and so on).

From a microbiological point of view due to the presence of an external polysaccharide membranes and hydrophilic capsules in gram-negative bacteria, the cat is which prevent the penetration of microbial cells hydrophobic antibacterial substances, the hydrophilic base is preferable, as are conductors of medicines in the microbial cell.

The hydrophilic base, as a rule, contain purified water, hydrophilic non-aqueous solvents include polyethylene oxide, for example PEO-400, glycerin, Dimexidum, and water-soluble polymers include polyethylene oxide, for example PEO-1500.

A greater role for local therapy of wounds play a substance capable of providing outflow of purulent exudate from the wound, to provide anti-inflammatory effect due to absorption of fluid and reduce swelling of the wound, as well as to protect the tissue from overhydration. Often, these substances contribute to the enhanced activity of antibacterial substances. Such substances include oxides - water-soluble polymerization products of ethylene oxide, which are physiologically indifferent compounds. In this class include hydrophilic nonaqueous solvents (polyethylene oxide, for example, PEO-400; glycerin, Dimexidum) and polymers (polyethylene oxide, e.g. the PEO-1500, modified cellulose derivatives, polyvinylpyrrolidone). These substances are easily applied on the wound surface, and evenly distributed on it, improving contact with the juvenile tissues and content wounds, mix well with wound exudate and retain their homogeneity, low toxicity and do not render section is agusega action on the tissues, do not violate their physiological functions.

Dimexide 30%solution of dimethyl sulfoxide (DMSO) is a colorless transparent liquid or colorless crystals, melting at a temperature of 18.5°C, with a specific smell, hygroscopic. Miscible in all proportions with water and alcohol, has a local anesthetic, local anti-inflammatory, antimicrobial (antiseptic) and fibrinolytic action. Fast and good penetration through biological membranes, including the skin and mucous membranes, increases their permeability to other medicines. Changes the sensitivity of microflora that are resistant to antibiotics. Used in combination with other medicinal substances for better and deeper penetration in tissue (Case of medicines). The disadvantages of dimexide should include the fact that it dries quickly.

Glycerol (1,2,3-propanetriol) - a Colorless, viscous liquid, sweet taste without smell. Miscible in all proportions with water, ethanol, methanol, acetone, insoluble in chloroform and ether, soluble in mixtures with ethanol. Absorbs moisture from the air (up to 40% by weight).

Hydrogencitrate acid (enterosgel) - interestbecause, enveloping, Antidiarrhoeal, detoxification preparation based on organic silicon designed for you is edenia toxic substances from the body and the gastrointestinal tract.

Enterosgel selectively absorbs from the blood of the weight of endogenous and exogenous toxic substances of different nature: bacterial toxins, allergens, antigens, viruses, drugs and poisons. Adsorbs some products of metabolism. Not adsorb trace elements. Relieves symptoms of dysbiosis, helps normalize the function of hematopoietic and immune systems. In the selective adhesion Enterosgel destroys pathogens and outputs them particles containing endo - and exotoxins. It has anti-inflammatory and regenerating action on the mucous membrane of the stomach and intestines, prevents the occurrence of erosive damage, non-toxic and harmless, has the organic nature of the surface and is fully compatible with the tissues and substrates of the body, in terms of the body chemically inert. Applies when the intoxication of different origin: poisoning, alcohol intoxication, intestinal infection, food intoxication, dysbiosis, food and drug Allergy, toxicoinfection liver injury, septic processes, burn disease in the phase of intoxication and other

Nicotinic acid is a vitamin and lipid-lowering agent. The body turns into nicotinamide, which is associated with the coenzyme to the dehydrogenase type I and II (NAD and NADP), transferring the hydrogen is involved in the metabolism of fats, proteins, amino acids, purines, tissue respiration, glycogenolysis, synthetic process. Compensate for the deficit of vitamin PP, normalize the concentration of lipoproteins in the blood, dilates small blood vessels, improve microcirculation, providing weak anticoagulante action. Used in Hypo - and avitaminosis PP, chronic infections, long-term healing wounds and trophic ulcers.

Additional stimulation of repair processes in the wound in the proposed pharmacological tool can be applied both in the form of monocomponent, and a mixture of components with different mechanism and spectrum of activity, a substance that stimulates reparative processes in the wound.

The use of hydrophilic bases, consisting of a mixture of oxides or modified cellulose derivatives, polyvinylpyrrolidone in the proposed pharmacological tool for fast delivery of active substances to microbial cells and the cells of the tissue that enhances therapeutic activity of the proposed drug. In addition, the de-hydration of the hydrophilic base cells of gram-positive microorganisms reduces their resistance, which also increases therapeutic activity of the proposed drug. The use of PEO, glycerin, Dimexidum additionally str is cSet microcirculation in the tissues of the wound due to their dehydrating steps, as well as providing additional anti-inflammatory effect due to absorption of fluid and reduce swelling of the wound.

The hydrophilic base, such as oxides, which can dissolve in the secrets of the mucous membranes, completely releasing the drug substance is not irritating when this mucous, have a long shelf-life and high physiological indifference.

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

Example 1. The ointment.

100 g of ointment contains:

Active biomechatronics and/or a mixture of biocomplexes0,10-2,00
Baserest

As a medicinal ointment or gel contains at least one component selected from the group including antimicrobial drugs: metronidazole and/or bio-complex with zinc, and/or bio-complex with copper and/or bio-complex with cobalt or a mixture thereof, and optionally comprising nicotinic acid β-pyridylcarbonyl acid (vitamin PP), and/or bio-complex with cobalt, and/or bio-complex with zinc, and/or bio-complex with silver, and/or bio-complex with copper.

Biometeorology PR is svodnik intorimidazole and β is pyridylcarbinol acids are expressed antimicrobial properties against studied in vitro and in vivo microorganisms (Stapliylococcus aureus ATCC 653 8-P, Staphylococcus aureus 209-P, Escherichia coli ATCC 25922, Bacillus cereus, Pseudomonas aeruginosa ATCC 27853, Proteus vulgaris ATCC 4636, Candida albicans, and also have immunostimulatory effects contributing to the activation of reparative processes in the wound.

The use of the proposed drug metronidazole and/or its biometeorological and nicotinic acid and/or its biometeorological as monocomponent, in the form of a mixture of components, significantly enhances therapeutic effect of the proposed pharmacological tools.

Composition 1. Ointment

100 g of ointment contains:

active biomechatronics and/or mix
biometeorological0,10-2,00
modified derivatives of cellulose and hydrogel
metiltselyulozy acid (enterosgel)
the mixing ratio 3:1, respectively4,00-8,00
purified water95,90-90,00

Part 2. Ointment

100 g of ointment contains:

active biomechatronics and/or mix
biometeorological0,10-2,00
modified derivatives of cellulose and hydrogel
metiltselyulozy acid (enterosgel) ratio
component 3:1, respectively4,00-8,00
trimekain3,00-5,00
purified water92,90-85,00

Part 3. Ointment

100 g of ointment contains:

active biomechatronics and/or mix
biometeorological0,10-2,00
modified derivatives of cellulose and hydrogel
metiltselyulozy acid (enterosgel)
the mixing ratio 3:1, respectively4,00-8,00
trimekain3,00-5,00
microbodies the spirulina (Spirulina platensis) 0,10-3,00
purified water92,80-82,00

Part 4. Ointment

100 g of ointment contains:

active biomechatronics and/or
a mixture of biometeorological0,10-2,00
modified derivatives of cellulose and hydrogel
metiltselyulozy acid (enterosgel)
in ratio 3:1, respectively4,00-8,00
trimekain3,00-5,00
cuts spirulina (Spirulina platensis)0,10-3,00
chlorhexidine digluconate0,01-1,00
purified water92,79-81,00

Part 5. Ointment

100 g of ointment contains:

active biomechatronics and/or mix
biomechatronics the 0,10-2,00
modified derivatives of cellulose and hydrogel
metiltselyulozy acid (enterosgel) ratio
component 3:1, respectively4,00-8,00
trimekain3,00-5,00
cuts spirulina (Spirulina platensis)0,10-3,00
chlorhexidine digluconate0,01-1,00
dimexide5,00-10,00
glycerin5,00-10,00
purified water82,79-61,00

Part 6. Ointment

100 g of ointment contains:

bio-complex of zinc with metronidazole0,05-1,0
bio-complex of copper with nicotinic acid0,05-1,0
modified derivatives of cellulose and hydrogel
metiltselyulozy acid enterosgel) ratio
component 3:1, respectively4,00-8,00
trimekain3,00-5,00
cuts spirulina (Spirulina platensis)0,10-3,00
chlorhexidine digluconate0,01-1,00
dimexide5,00-10,00
glycerin5,00-10,00
purified water82,79-61,00

Example 2. Gel

Part 7. The gel.

100 g of gel contains:

active biomechatronics
and/or a mixture of biometeorological0,10-2,00
modified cellulose derivatives3,00-6,00
polyvinylpyrrolidone3,00-6,00
purified water93,90-of 86.00

Part 8. Gel

100 g of gel contains:

active biomechatronics and/or mix
biometeorological0,10-2,00
modified cellulose derivatives3,00-6,00
polyvinylpyrrolidone3,00-6,00
trimekain3,00-5,00
purified water90,90-81,00

Part 9. Gel

100 g of gel contains:

active biomechatronics and/or mix
biometeorological0,10-2,00
modified cellulose derivatives3,00-6,00
polyvinylpyrrolidone3,00-6,00
trimekain3,00-5,00
cuts spirulina (Spirulina platensis)0,10-3,00
purified water90,80-78,00

10. Gel

100 g of gel contains:

active biomechatronics and/or mix
biometeorological0,10-2,00
modified cellulose derivatives3,00-6,00
polyvinylpyrrolidone3,00-6,00
trimekain3,00-5,00
cuts spirulina (Spirulina platensis)0,10-3,00
chlorhexidin digluconate0,01-1,00
purified water90,79-77,00

Composition 11. Gel

100 g of gel contains:

active biomechatronics and/or mix
biometeorological0,10-2,00
modified cellulose derivatives3,00-6,00
polyvinylpyrrolidone3,00-6,00
trimekain3,00-5,00
cuts with arolina (Spirulina platensis) 0,10-3,00
chlorhexidin digluconate0,01-1,00
dimexide5,00-10,00
glycerin5,00-10,00
Aerosil2,50-5,00
purified water78,29-52,00

12. Gel

100 g of gel contains:

biomechatronics zinc metronidazole0,05-1,0
biomechatronics copper with nicotinic acid0,05-1,00
modified cellulose derivatives3,00-6,00
polyvinylpyrrolidone3,00-6,00
trimekain3,00-5,00
cuts spirulina (Spirulina platensis)0,10-3,00
chlorhexidin digluconate0,01-1,00
dimexide5,00-10,00
glycerin 5,00-10,00
Aerosil2,50-5,00
purified water78,29-52,00

Example 3. Ointment

Composition 13. Ointment

100 g of ointment contains:

active biomechatronics and/or mix
biometeorological0,10-2,00
the polyethylene oxide - 15005,00-17,00
the polyethylene oxide - 40020,0-68,0
purified water74,9-13,00

Composition 14. Ointment

100 g of ointment contains:

active biomechatronics and/or mix
biometeorological0,10-2,00
the polyethylene oxide - 15005,00-17,00
the polyethylene oxide - 40020,00-68,00
trimekain3,00-5,00
purified water 71,90-80,00

15. Ointment

100 g of ointment contains:

active biomechatronics and/or mix
biometeorological0,10-2,00
the polyethylene oxide - 15005,00-17,00
the polyethylene oxide - 40020,00-68,00
trimekain3,00-5,00
cuts spirulina (Spirulina platensis)0,10-3,00
purified water71,80-5,00

The composition 16. Ointment

100 g of ointment contains:

active biomechatronics and/or mix
biometeorological0,10-2,00
the polyethylene oxide - 15005,00-17,00
the polyethylene oxide - 40020,00-68,00
trimekain3,00-5,00
cuts spirulina (Spirulina pltensis) 0,10-3,00
chlorhexidine digluconate0,01-1,00
purified water71,79-4,00

Part 17. The ointment.

100 g of ointment contains:

active biomechatronics and/or mix
biometeorological0,10-2,00
the polyethylene oxide - 15005,00-17,00
the polyethylene oxide - 40020,00-68,00
trimekain3,00-5,00
cuts spirulina (Spirulina platensis)0,10-3,00
chlorhexidine digluconate0,01-1,00
dimexide5,00-10,00
glycerin5,00-10,00
purified water61,79-4,00

18. Ointment

100 g of ointment contains:

biomechatronics zinc with metronid what SOLOM 0,05-1,0
biomechatronics copper with nicotinic acid0,05-1,00
the polyethylene oxide - 15005,00-17,00
the polyethylene oxide - 40020,00-68,00
trimekain3,00-5,00
cuts spirulina (Spirulina platensis)0,10-3,00
chlorhexidine digluconate0,01-1,00
dimexide5,00-10,00
glycerin5,00-10,00
purified water61,79-4,00

Study the specific activity of the proposed formulations of gels and ointments (table 1,2,3) conducted in vitro and in vivo.

Table 1.
Composite compounds ointments
№ p/pComponent nameNo. of composition of the wax composition
1 23456
1.Active biomechatronics and/or a mixture of biometeorological0,1-2,00,1-2,00,1-2,00,1-2,00,1-2,0-
- bio-complex of zinc with metronidazole-----0,05-1,0
- bio-complex of cobalt with metronidazole------
- bio-complex of copper with metronidazole------
- bio-complex of zinc with β-pyridineboronic acid-- ----
- bio-complex of cobalt with β-pyridineboronic acid------
- bio-complex of copper with β-pyridineboronic acid-----0,05-1,0
- bio-complex of silver with β-pyridineboronic acid------
2Modified cellulose derivatives3,0-6,03,0-6,03,0-6,03,0-6,03,0-6,03,0-6,0
3.The hydrogel of metiltselyulozy acid (enterosgel)1,0-2,01,0-2,0 1,0-2,01,0-2,01,0-2,01,0-2,0
4.Trimekain-3,0-5,03,0-5,03,0-5,03,0-5,03,0-5,0
5.Cuts spirulina (Spirulina platensis)--0,1-3,00,1-3,00,1-3,00,1-3,0
6.Chlorhexidine digluconate---0,01-1,00,01-1,00,01-1,0
7.Dimexide----5,0-10,05,0-10,0
8.Glycerin-- --5,0-10,05,0-10,0
9.Purified water95,90-90,0092,90-85,0092,80-82,0092,79-81,0082,79-61,0082,79-61,00

Table 2
Composite compounds gels
№ p/pComponent nameNo. of composition of the wax composition
123456
1.Active biomechatronics and/or a mixture of biometeorological0,1-2,00,1-2,00,1-2,00,1-2,00,1-2,0-
- bio-complex of zinc with metronidazole- ----0,05-1,0
- bio-complex of cobalt with metronidazole------
- bio-complex of copper with metronidazole------
- bio-complex of zinc with β-pyridineboronic acid------
- bio-complex of cobalt with β-pyridineboronic acid------
- bio-complex of copper with β-pyridineboronic acid--- --0,05-1,0
- bio-complex of silver with β-pyridineboronic acid------
2Modified cellulose derivatives3,0-6,03,0-6,03,0-6,03,0-6,03,0-6,03,0-6,0
3.Polyvinylpyrrolidone3,0-6,03,0-6,03,0-6,03,0-6,03,0-6,03,0-6,0
4.Trimekain-3,0-5,03,0-5,03,0-5,03,0-5,03,0-5,0
5.Cuts spirulina (Spirulina platensis)--0,1-3,0 0,1-3,00,1-3,00,1-3,0
6.Chlorhexidine digluconate---0,01-1,00,01-1,00,01-1,0
7.Dimexide----5,0-10,05,0-10,0
8.Glycerin----5,0-10,05,0-10,0
9.Purified water93,90-of 86.0090,90-81,0090,80-78,0090,79-77,0078,29-52,0078,29-52,00

tr>
Table 3
Composite compounds ointments
№ p/pComponent nameNo. of composition of the wax composition
123456
1.Active biomechatronics and/or a mixture of biometeorological0,1-2,00,1-2,00,1-2,00,1-2,00,1-2,0
- bio-complex of zinc with metronidazole0,1-2,00,1-2,00,1-2,00,1-2,00,1-2,00,05-1,0
- bio-complex of cobalt with metronidazole0,1-2,00,1-2,00,1-2,00,1-2,00,1-2,0-
- bio-complex of copper with metronidazole0,1-2,00,1-2,0 0,1-2,00,1-2,00,1-2,0-
- bio-complex of zinc with β acid0,1-2,00,1-2,00,1-2,00,1-2,00,1-2,0-
- bio-complex of cobalt with β-pyridineboronic acid0,1-2,00,1-2,00,1-2,00,1-2,00,1-2,0-
- bio-complex of copper with β-pyridineboronic acid0,1-2,00,1-2,00,1-2,00,1-2,00,1-2,00,05-1,0
- bio-complex of silver with β-pyridineboronic acid0,1-2,00,1-2,00,1-2,00,1-2,00,1-2,0-
2The polyethylene oxide-15005,0-of 17.0 5,0-of 17.05,0-of 17.05,0-of 17.05,0-of 17.05,0-of 17.0
3.The polyethylene oxide-40020,0-68,020,0-68,020,0-68,020,0-68,020,0-68,020,0-68,0
4.Trimekain-3,0-5,03,0-5,03,0-5,03,0-5,03,0-5,0
5.Cuts spirulina (Spirulina platensis)--0,1-3,00,1-3,00,1-3,00,1-3,0
6.Chlorhexidine digluconate---0,01-1,00,01-1,00,01-1,0
7.Dimexide- ---5,0-10,05,0-10,0
8.Glycerin----5,0-10,05,0-10,0
9.Purified water74,90-13,0071,90-8,0071,80-5,0071,79-4,0061,79-4,0061,79-4,00

Study of antimicrobial activity of the proposed pharmacological preparations, carried out by the method of diffusion in agar on solid nutrient media by analyzing the zones of inhibition of growth of test organisms used for the determination of antimicrobial action of medicines. Research conducted in relation to the following standard strains of microorganisms: Staphylococcus aureus ATCC 653 8-P, Staphylococcus aureus 209-P, Escherichia coli ATCC 25922, Bacillus subtillis ATCC 6633, Candida albicans ATCC 865-653. Pseudomonas aeruginosa ATCC 27853, Proteus vulgaris. It is established that a pronounced antimicrobial effect is evident for all the above test cultures.

The results obtained allowed to establish Wuxi is giving antimicrobial action due to the joint presence of metronidazole and/or biocomplex metronidazole with zinc, and/or biocomplex metronidazole with cobalt and/or biocomplex metronidazole with copper, nicotinic acid and/or its biocomplex with cobalt and/or its biocomplex with copper and/or its biocomplex with silver, anesthetic, stimulant reparative processes, antiseptic, Dimexidum, glycerol and hydrophilic bases - modified derivatives of cellulose, including additional enterosgel and polyvinylpyrrolidone or polyethylene oxides (table 4, 5, 6)

Table 4
The results of the study of antimicrobial activity ointment
№ p/pThe research objectsZones of growth inhibition, mm
Staphylococcus aureus ATCC 6538-PEscherichia coli ATCC 25922Bacillus subtillis ATCC 6633
1.Official ointment the vegetable "levomekol25,2±0,422,3±0,226,9±0,3
2.Part 632,4±0,335,5±0,441,2±0,4

Table 5
The results of the study of antimicrobial activity gels
№ p/pThe research objectsZones of growth inhibition, mm
Staphylococcus aureus ATCC 6538-PEscherichia coli ATCC 25922Bacillus subtillis ATCC 6633
1.Gel Metrogylum"18,3±0,216,4±0,220,4±0,4
2.1232,8±0,335,2±0,341,1±0,5

Table 6
The results of the study of antimicrobial activity ointment
№ p/pThe research objectsZones of growth inhibition, mm
Staphylococcus aureus ATCC 6538-PEscherichia coli ATCC 25922 Bacillus subtillis ATCC 6633
1.Official ointment the vegetable "levomekol25,2±0,422,3±0,226,9±0,3
2.1837,3±0,439,2±0,343,2±0,4

Local anesthetic activity developed ointments and gels studied in experiments in vivo method Rainier-Jack, based on the change in the sensitivity of the cornea of the rabbit when applied to the sample, expressed in response to a stimulus in the form of a clamping century.

In into the conjunctival eye bag rabbit was introduced with a syringe 0.1 g of the investigated materials. Using a calibrated hairs on the cornea caused rhythmic stimulation with a frequency of 100 beats per minute through 1, 2, 5, 8, 10, 12, 15 min and then every 5 min prior to the closing of the eyelids.

The speed of onset of local anesthesia took time between introduction of the sample ointments and early manifestations of pharmacological action.

The relative strength of anesthetic action is expected, according to the index Rainier, summing the number of stimuli in 13 dimensions, starting with the 8th min, in the course of an hour.

Indicator full anesthesia midrange is Tali no blink reflex for 1 min at 100 contacts calibrated hairs with the cornea of the eye.

The duration of General anesthesia was characterized by time since the beginning of anesthesia until the full restoration of sensitivity.

The obtained results were processed by the method of variation statistics (GF XI, M, 1987, vol.1, s).

The time development of the anaesthetic effect is 1-5 minutes, the time for complete anesthesia 55-70 minutes, index Rainier-1100-1400 used, the recovery time sensitivity of 70-80 minutes.

High index values Rainier, duration of General anesthesia for the proposed pharmacological compositions of gels and ointments (compared with control) indicate not only synergistic action of trimekainom and metronidazole and/or biocomplex metronidazole with zinc and/or biocomplex metronidazole with cobalt and/or biocomplex metronidazole with copper, nicotinic acid and/or its biocomplex with zinc and/or biocomplex with cobalt and/or its biocomplex with copper and/or its biocomplex with silver, but also about the prolongation of anesthetic effect.

Example 4. Study of wound healing of soft medicinal forms.

Study of wound healing of soft medicinal forms were carried out on outbred white rats-males weighing 200-250 g at the conventional model of infected wounds. For the experiment the animals were divided into groups: control (untreated), comparison (treatment oficialnoi,2% ointment the vegetable "levomekol) and experimental (treatment developed by pharmacological means). The treatment of infected wounds started from the third day after the development of the RAS. Planimetric indicators RAS were removed according to the following scheme: day of the beginning of the experiment; after 5 applications; after 10 applications; in subsequent periods by groups noted the percentage of healing, calculated in relation to the original parameters.

During the experiment it was found that both planimetric characteristics and the time of healing in the group of animals treated developed by pharmacological means (6, 12, 18) on the model of an infected wound condition RAS significantly improved to 12-13-day came complete healing.

The total percentage reduction of area of the wound in the dynamics in the experimental group to the 12th sucka experiment amounted to 95.6%of that in the comparison group - 60.4% and in contorling group - 43.7 per cent.

The average time of cleansing wounds in the experimental groups when applying the Compositions: 6,12,18(3,9±0.3 days) were significantly(p<0,05) shorter than in the comparison group (8,1±0.4 days). Normalization of the pH of the wound exudate compared to the comparison group occurred respectively 6.5±0.9 and a 10.1±1.5 days, and phagocytosis to the ceiling of 5.60±0,31 and 8.7±0,9 days. The appearance of granulations marked by 4.1 ą 0.2 and 7.5±0.4 days, respectively.

According to the dynamics of changes in the area of RAS, clinical, microbiological and histological indicators installed expressed therapeutic de is due to pharmacological agents compared with officinal ointment the vegetable "levomekol.

Thus, the proposed pharmacological tools in comparison with the prototype in the early stages of treatment have a higher antimicrobial activity, a strong local anesthetic action and accelerate the healing of wounds for 3-4 days because of the combination of antimicrobial drug metronidazole and/or its active biometeorological, nicotinic acid and/or its active biometeorological, local anesthetic and hydrophilic bases containing modified cellulose derivatives, and optionally comprising a hydrogel of metiltselyulozy acid and polyvinylpyrrolidone, or the oxides, potentiating the action of each other. Developed an optimal method of preparation of the proposed compounds ointments and gels, in which the maximum therapeutic efficacy.

The proposed pharmacological compositions of gels and ointments help to expand the range of available drugs used for local treatment of purulent-inflammatory processes of the skin, burns and mucous membranes of various etiologies.

The invention provides multiple therapeutic effect on inflammatory processes, pharmacological tools are highly efficient from the point of view of biological availability.

The invention provides a reduction cf the Cove treatment by reducing the time want to restore the integrity of the skin.

On the basis of the proposed solutions can be created a number of new drugs in the form of soft medicinal forms, such as gels and ointments containing the active Biometeorology derivative of 5-intorimidazole and β is pyridineboronic acid and/or their mixture.

Thus, the use of systemic approach in the treatment of purulent wounds with mandatory in-depth study of specific features of the phase currents of the wound healing process and application in connection with these characteristics differentiated approach in the treatment and the selection of drugs can achieve the best results and minimize the time of healing.

The sources of information.

1. Kuzin M.I., Kostyuchenok BM Wounds and wound infection : a guide for physicians. - M.: Medicine, 1990, - s

2. Lubarsky, MS, Letyagin AJ.., Gabitov V.H., Semko CENTURIES, Palienko A.A. Sorption operationally drugs in septic surgery. - publishing house "Ilim", Novosibirsk - Saint-Petersburg - Bishkek, 1994, - p.42, 76.

3. Feldstein M.M. and other Polymer coatings for the treatment of wounds and burns. "The results of science and technology". Ser. "Chemistry and technology of macromolecular compounds". VINITI, 1981, t.16., s.

1. Pharmaceutical composition for topical application having antibacteria inim and reparative action, containing a mixture of active biometeorological, characterized in that the mixture of biometeorological presented in the form of a biocomplex of zinc with the derived 5-intorimidazole and biocomplex copper derived from β-pyridineboronic acid, and the composition comprises a hydrophilic base, represented as a modified derivative of cellulose and a hydrogel of metiltselyulozy acid (enterosgel) in the ratio 3:1, respectively, or a modified derivative of cellulose and polyvinylpyrrolidone in the ratio of 1:1, respectively, or an alloy oxides (PEO-400 and PEO-1500) in the ratio 8:2, respectively; and a blend of special additives - Dimexidum and glycerol in a ratio of 1:1 in the following ratio, wt.%: bio-complex of zinc with the derived 5-intorimidazole 0,05-1,00, bio-complex of copper with the derived β-pyridineboronic acid 0,05-1,00, dimexide 5,00-10,00, glycerin 5,00-10,00, hydrophilic base - the rest.

2. The pharmaceutical composition according to claim 1, characterized in that it additionally contains one of the following special additives from the series: the local anesthetic agent, an antiseptic, a stimulant of reparative processes or their mixture in the following ratio, wt.%: bio-complex of zinc with the derived 5-intorimidazole 0,05-1,00, bio-complex of copper with the derived β-pyridineboronic acid 0,05-1,00, mestnoanestezirutm the substance abuser - 3,00-5,00, antiseptic - 0,01-1,00, stimulator of reparative processes - 0,10-3,00, hydrophilic base - the rest.

3. The pharmaceutical composition according to claim 2, characterized in that as a local anesthetic substances it contains a substance selected from the group trimekain, piromekain, lidocaine, or their mixture.

4. The pharmaceutical composition according to claim 2, characterized in that it contains an antiseptic substance selected from the group Miramistin, dioxidine, chlorhexidine digluconate, or their mixture.

5. The pharmaceutical composition according to claim 2, characterized in that as a stimulator of reparative processes it contains a substance selected from the group: methyluracil, atsemin, solcoseryl, ascorbic acid, and cuts spirulina (Spirulina platensis) or their mixture.



 

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FIELD: medicine, pharmaceutics.

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15 cl, 3 tbl, 7 ex

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2 dwg, 1 tbl, 1 ex

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2 ex

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68 cl, 1 tbl, 8 ex

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2 cl, 3 ex

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1 ex

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4 dwg, 7 ex

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SUBSTANCE: invention refers to biotechnology. A fibrin powder is prepared by the known method. Fibrin is recovered from a blood clot and transformed into powder. It is added with an aqueous solution of neutral catholyte having pH 9 or more, reduction-oxidation potential - 300 - 500 mV and containing the active ingredients O2, HO2, HO2., H2O2, H, OH', in ratio: fibrin powder 1.0 g per 1.5-2.0 ml of the aqueous solution of neutral catholyte. It is mixed to form a plastic mixture.

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5 cl, 9 ex, 9 dwg, 1 tbl

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6 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel medication for treatment of purulent-inflammatory processes of skin and mucous membranes of different etiology. Medication is made in form of gel and contains the following ingredients with the following ratio of components in g per 100 g: biocomplex of cobalt (II) with metronidasole 0.20-0.50. biocomplex of cobalt (II) with ampicillin 0.20-0.50, trimecaine 3.00-5.00, methyluracyl 1.00-3.00, dimexide 10.00, glycerol 5.00-10.00, hydrophilic base 3.00-7.00, water 77.60-64.00.

EFFECT: extension of assortment of wound-healing medications.

3 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel medication for treatment of purulent-inflammatory processes of skin and mucous membranes of different etiology. Medication is made in form of gel and contains the following ingredients with the following ratio of components in g per 100 g: biocomplex of metronidazole with zinc 0.5-2.0, biocomplex of furacilinum with copper 0.1-0.2, trimecaine 3.0-5.0, vitamins (vitamin A, vitamin E, vitamin PP, vitamin C or their mixture) 0.1-1.0, dimexide 10.0, hydrogel of methylsiliconic acid 1.0-5.0, hydrophilic base 3.0-7.0, water 82.3-69.8.

EFFECT: extension of assortment of wound-healing medications.

2 tbl, 1 ex

Anti-burn gel // 2481121

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely an anti-burn gel. The anti-burn gel for external application containing chitosan, salicylic acid, a biological regulator recovered from a bovine blood serum and represented an acidic protein fraction within the range of pH<3.0 and water taken in the specific relation.

EFFECT: formulation provides manifested healing activity.

7 dwg, 9 ex

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EFFECT: invention allows enhancing stimulation of the metabolic processes and hepatoprotective function of the liver.

3 tbl

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