Composition antimicrobial, anti-inflammatory and regenerative actions

 

(57) Abstract:

Use in medicine, particularly in pharmacology in veterinary medicine to treat wounds and burns. Effect: anti-microbial anti-inflammatory and regenerative effect of the composition due to the easy access of the active principle in the affected tissue, the lack of resistance of microorganisms, broadening the spectrum of biological actions, reduction in the consumption of the active principle. The inventive composition antimicrobial anti-inflammatory and regenerative action contains, wt%:

Triiodide 1,3-diethylbenzamide - 0,5-2,9

Organic dipolar dissociable (polar) basically soft aprotic solvent is 1.0 to 5.8

Lanolin - 0,6-1,2

Vaseline - Rest

Technical result achieved: create a composition antimicrobial anti-inflammatory and regenerative action by introducing an organic solvent, thus facilitating the access of the active principle in the affected tissue. 3 table.

The invention relates to medicine, in particular to pharmacology for veterinary medicine for the treatment of burns and wounds.

Famous liniment of syntomycin (emulsion of syntomycin), antibio is of CIN, 1985, S. 255).

Lack of liniment is the resistance of pathogenic microorganisms that reduces the chances of recovery. The high cost of funds (3.5 times higher offer).

Known Vishnevsky ointment for the treatment of ulcers and burns (Mashkovsky M. D. Medicines. So 2, M.: Medicine, 1985, S. 414).

The disadvantage of the ointment is the lack of a broad-spectrum antimicrobial action, the ointment has a sharp, unpleasant smell.

The closest composition to the same destination on essential features is an ointment containing as active principle triode 1,3-dimethylbenzimidazole (thesis: "Synthesis and study of iodine-containing biologically active compounds". The dissertation on competition of a scientific degree of candidate of biological Sciences, Lewicki Century. And., Cover, 1982).

A disadvantage of the known ointment is that as the basis of a mechanical mixture of crushed crystals of the active start and fundamentals that contains petrolatum and lanolin. Specified hinders the access of the active principle in the affected tissue and reduces efficiency. Not specified no ointment resistance of microorganisms. Narrower spectrum of biological which defines its purpose, is improving the treatment of burns and wounds.

The technical result of the claimed invention, which can be achieved by its implementation is antimicrobial, anti-inflammatory and regenerative its effect by facilitating access of the active principle in the affected tissue, the lack of resistance of microorganisms, broadening the spectrum of biological activity, reduction of consumption of the active agent.

This technical result can be achieved using the composition antimicrobial, anti-inflammatory and regenerative effect which contains a mechanical mixture of finely - crystalline biologically active agent and a base, including petrolatum and lanolin, a feature of which is that it contains as active principle triode 1,3-diethylbenzamide structural formula

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and additionally contains organic dipolar dissociable (polar) basically soft aprotic solvent for the active agent with the following ratios, wt.%:

Triode 1,3-diethylbenzamide - 0,5 - 2,9

Anhydrous lanolin - 0,6 - 1,2

Organic dipolar dissotsiiruut component composition, containing biologically active ingredient in the compositions set forth in the sources of information through research, showed the following. As a biologically active agent in the composition of the claimed composition is proposed triode 1,3-diethylbenzamide, physico-chemical constants which are given in table. 1. The specified component are described in the following sources: N.F. Shcherban and other Triiodide 1,2,3-dialkylanilines possessing antimicrobial activity. USSR author's certificate N 770021, 1980; B. I. Levitskii, the dissertation on competition of a scientific degree of candidate of biological Sciences, "Synthesis and study of iodine-containing biologically active compounds". Cover, 1982.

The active principle of the proposed composition contains chetyrehkolenny basic nitrogen in the composition of the organic cation and hypervalent associated triode-anion I3-. The biological activity of triode 1,3-diethylbenzamide due to the presence of patterns . Triode-anion capable of generating oppositely charged particles containing a biologically active iodine: I2, I3-IO-I+I-. Electron cloud (density) is distributed so that the cation associated three RDA. The atoms of iodine in triode-anion indistinguishable because of the excess electron is non-localized plates of three-centered orbitals This balance is disturbed in the presence of substrate that can accept the specified electron (biochemical substances).

Research active principle found the following types of biological activity: antibacterial, anti-inflammatory, regenerative.

To create compositions antimicrobial anti-inflammatory and regeneration steps, the access in which the active agent in the affected tissue is facilitated, crystalline active principle is administered in lipophilic (fat) is the basis of the composition (vaseline) as part solvate solution with organic dipolar dissociable (polar) soft key aprotic solvent, emulsified by an emulsifier (anhydrous lanolin) in the specified base.

In the proposed invention the organic dipolar dissociable (polar) basically soft aprotic solvent, which solvent the current start and improve its penetration into living tissue.

Specific interaction with the anions and cations by Rastko dielectric constant (>15) a large dipole moment (>2.5). The dipolar solvent molecules possess a permanent dipole moment. Aprotic solvent does not contain a proton-donor action group (hydroxy-, amino-, carboxy-, amide group). The solvent acts as a dissociative (polar), as it has a sufficiently high dielectric constant and can reduce the strong electrical attraction between two oppositely charged ions of the dissolved substance - triiodide 1,3-diethylbenzamide so that could be a separate ions: large organic cation (containing chetyrehkolenny basic nitrogen) and triode-anion I-3. The polarity of the solvent is determined on the basis of his Salvaterra ability, which depends on the sum of all interactions between the molecules of the dissolved substance and the proposed solvent (Coulomb force orientation induction dispersion interaction, interaction with charge transfer). The proposed solvent, though contains hydrogen atoms, is not a hydrogen donor for the formation of hydrogen bonds.

The solvent refers to p-donors, this solvent has neisvaziuosiu, unshared pair of electrons, the region is recitalist.

Solvation occurring with regard to ion-dipole, dipole-dipole and other interactions, caused by dissociation of the respective groups of molecules dissolved triiodide 1,3-diethylbenzamide and the proposed solvent, solvation includes a variety of forces of interaction (see above). Solvent molecules to solvate shells behave almost as loosely linked substituents. Of particular importance for the solvation have p-donor solvents. Is a chemical rule: like dissolves like.

Soft dipolar aprotic solvent with a high polarizability collateral mostly large, easily polarizable anions, including type I3-. Large soft cation containing chetyrehkolenny basic nitrogen (as part of triiodide 1,3-diethylbenzamide) is also better collaterals soft dipolar aprotic donor solvent. Used solvent is a penetrant is able to easily penetrate all barriers of the body (through the cell membrane), evenly distributed in the body, simultaneously transporting biologically active start and releasing it into the living tissues of the basics (vaseline). When the lo in the proposed solvent, translate crystalline active principle at the molecular level, getting a molecular-disperse system (solvate solution).

Received solvate solution triiodide 1,3-diethylbenzamide injected into the lipophilic core emulsified using an emulsifier anhydrous lanolin. Lanolin easily penetrare through the skin, as proposed solvent, causing resorption (return of the active agent from the substrate with subsequent absorption in living tissue. Lanolin is gidrofiliziruyuschim component fatty basis (vaseline) and a pin of the day to improve its compatibility with the proposed solvent by emulsification in the last part of the solvate of the solution. Lanolin is also a thickener.

Petrolatum and lanolin prolong the action of the active principle, provide adhesion (adhesion) with the damaged tissues.

When creating the claimed composition introduction to lipophilic (fat) is the basis of the composition (vaseline) anhydrous lanolin as an emulsifier solvate of a solution of the active principle leads to a hydrophilic-lipophilic composition. As a result of making fat base hydrophilizing properties vozmojnimi transmembrane transfer), that facilitates access of active agent in the lesion tissue. Mixing components of the composition under appropriate conditions is anhydrous alloy lipophilic bases with emulsifier with which the basis of the introduced active principle, solvated in the proposed solvent. Get the song related to the dispersion (structured dispersions) with plastic or prugovecki environment with thixotropy. The composition and its lipophilic (fat) basis are plastic systems with two different structures: 1) fragile condensation and crystallization, 2) dispergation-coagulation (reversible thixotropic). The rheological properties of the composition depend on the quantitative proportions of all its components.

The proposed composition has a resistance. Drugs active iodine (which include triode 1,3-diethylbenzamide) there is no resistance in microorganisms (Mochnacz O. C. Iodine and problems of life. Leningrad, Nauka, 1974).

Justification of the selected limits is the following. When the concentration of the active agent is less than 0.5 wt.% prolonged healing time of damaged tissue and skin.

When the concentration of Accho (polar) primary soft aprotic solvent less than 1 wt.% was the lowest for the dissolution of the active principle.

When the concentration of the solvent over 5.8 wt.% the composition is stratified, and the excess solvent.

At a concentration of lanolin less than 0.6 wt.% not achieved Miscibility fat basis (vaseline) with a solution of active Nicola.

At a concentration of lanolin more than 1.2 wt.% possible oxidation of fatty acids in lanolin iodine active principle.

Vaseline - filler to 100 wt.%.

The claimed invention meets the requirement of "novelty", as in the prior art unknown technical solution to the same destination with the declared set of essential features.

Ointment itapiranga antiseptic, bactericidal action against a broad spectrum of gram-positive and gramatically microorganisms known (VFS 42-2075-91). It contains as active principle yodopiron - yellowish-brown amorphous powder, which is a water-soluble complex of polyvinylpyrrolidone I2with KI (contains 6-8% active iodine). In the register of medicines of 1996 not specified ointment base.

The present invention is a composition antimicrobial, anti-inflammatory and regenerative actions, contains>and additionally contains organic dipolar dissociable (polar) basically soft aprotic solvent specified active principle in the following ratio, wt.%:

Triode 1,3-diethylbenzamide - 0,5 - 2,9

Anhydrous lanolin - 0,6 - 1,2

Organic dipolar dissociable (polar) basically soft aprotic solvent is 1.0 to 5.8

Vaseline - Rest

The claimed invention meets inventive step, as in the prior art is not identified solutions with signs consistent with its hallmarks.

The implementation of the invention is confirmed by the following.

Example 1.

The crystals are dark brown triiodide 1,3-diethylbenzamide in the amount of 0.5 wt. % dissolved in an organic solvent: dimethylsulfoxide (DMSO) (Pharmacopeia 42-2980 - 93), taken in an amount of 1 wt.%. Lanolin anhydrous (GFH, article 373), in the amount of 0.6 wt.% and 1/4 of medical vaseline (GOST 13037-67) melted in a water bath at a temperature of 45oC. In the melt injected a solution of 1,3-diethylbenzamide in DMSO under vigorous stirring until complete homogeneity and enter the main vaseline when normalinogo actions (ointment).

Example 2.

The crystals are dark brown triiodide 1,3-diethylbenzamide in the amount of 2.9 wt.% dissolved in an organic solvent: DMSO (Pharmacopeia 42-2980-93), taken in an amount of 5.8 wt.%. Lanolin anhydrous (GFH, article 373) in an amount of 1.2 wt.% and 1/3 of medical vaseline (GOST 13037-67) melted in a water bath at a temperature of 45oC. In the melt is injected solution triiodide 1,3-diethylbenzamide in DMSO, with vigorous stirring until complete homogeneity enter the rest of the vaseline at normal temperature and again mix. Get the song antimicrobial, anti-inflammatory and regenerative actions (ointment).

Both compositions have the following types of biological activity: antibacterial, anti-inflammatory and regeneration.

Antimicrobial activity was confirmed by the data table. 2.

Anti-inflammatory biological activity is confirmed by the fact that as a model of inflammation was used a burn injury. The healing of burns in rats occurred at different times. The fastest rejection formation, epithelialization and wound healing was observed in rats 4-th group. The group, with the task composition antimist attachaudio areas of necrosis in rats of the 2nd and 3rd groups. It should be noted that in all animals the 4th group in 2-3 days from start of treatment dramatically decreased the inflammation in the hearth: swelling and infiltrate tissues, blood, began marginal epithelization. These animals felt much better than animals of the 2nd and 3rd groups, their behavior did not differ from the behavior of intact animals.

Weighing rats after 7 and 14 days after burn noted that the animals of the 2nd and 3rd groups almost no added weight. At the same time, the animals of the 4th group weight gain was 72-85% of the weight gain in the intact animal during this same time. Composition antimicrobial, anti-inflammatory and regenerative action has a pronounced anti-inflammatory and healing properties in the treatment of burn injuries. Data are table. 3.

Regenerative biological activity is confirmed by the fact that the comparison of the results of studies by different groups of rats suggests that faster speed rejection scab on the remaining areas of the newly formed connective tissue that replaces the skin defect) and quality (speed differentiation of the newly formed young connective tissue in Mature with pucciniales) healing of burns occur in the application of the composition. The research results were presented in table. 3.

Examples of specific application possibilities of the invention and the achievement of the technical result confirm the compliance of the claimed invention, the condition of "industrial applicability".

Composition antimicrobial, anti-inflammatory and regenerative effect which contains a mechanical mixture of finely divided crystalline biologically active agent and a base, including petrolatum and lanolin, characterized in that the active agent it contains triode 1,3-diethylbenzamide structural formula

< / BR>
and the composition additionally contains organic dipolar dissociable (polar) basically soft aprotic solvent for the active agent in the following ratio, wt.%:

Triode 1,3-diethylbenzamide - 0,5 - 2,9

Anhydrous lanolin - 0,6 - 1,2

Organic dipolar dissociable (polar) basically soft aprotic solvent is 1.0 to 5.8

Vaseline - Rest

 

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FIELD: agriculture, animal husbandry, organic chemistry.

SUBSTANCE: antiseptic ointment comprises cationic surface-active substance, lower glycols, polyethylene glycols, water and ethylene glycol monophenolic ester and higher polyethylene glycols taken in the definite ratio of components. As cationic surface-active substance ointment comprises N-alkyl-N-alkoxycarbonylmethylhexahydroazipinium chloride or alkyldimethylbenzylammonium chloride, or cetylpyridinium bromide, or cetylpyridinium chloride, or 1,2-ethylenebis-(N-methylcarbdecyloxymethyl)ammonium dichloride, or ethylhexadecyldimethylammonium chloride, or chlorhexidine; as lower glycol ointment comprises 1,2-propylene glycol or polyethylene glycol-300, or polyethylene glycol-400; as higher polyethylene glycol ointment comprises polyethylene glycol-1500 or polyethylene glycol-3000, or polyethylene glycol-4000, or polyethylene glycol-6000. Ointment elicits the high antibacterial activity, broad spectrum of bactericidal effect and low irritating effect with respect to udder skin. Invention can be used for sanitary-hygienic treatment of udder of lactating cows for prophylaxis and rapid healing external damages of udder and nipples (arising cracks), prophylaxis of mastitis, enhancing milk purity by microbiological indices.

EFFECT: valuable antiseptic properties of ointment.

2 cl, 1 tbl, 22 ex

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