Antiseptic

 

(57) Abstract:

The invention relates to medicine and relates to an antiseptic for the treatment and prevention of diseases, including sexually transmitted. The invention consists in that the antiseptic agent is a solution of surface-active substances, comprising the following ingredients : benzyldimethyl [3-(myristoylation)propyl]ammonium chloride, monohydrate 0.1 g purified water up to 1000,0, the Invention provides a receiving means with no side effects and no contraindications and having high antibacterial activity. 11 table.

The invention relates to medicine and relates to an antiseptic for the treatment and prevention of sexually transmitted infections, including sexually transmitted diseases: syphilis, gonorrhea, trichomoniasis, lamidos, genital herpes, etc. According to the invention antiseptic is a broad-spectrum antiseptic from the class of cationic surfactants.

Known antiseptic agent from the class of surfactants is a derivative of chlorhexidine: 1,6-bis-5-[(para-chlorophenyl)-biguanide]hexane, vypuskaem drugs in Russia 1997, Attraversare, page B-644-B,-178--179).

The drug is effective against vegetative forms of gram-negative and gram-positive bacteria and yeasts, dermatophytes and lipophilic viruses. On the spores of the bacteria is effective only at high temperatures. Cleans and disinfects the skin. Used in gynecology and obstetrics. This drug is well established as a disinfectant and is used today means the prevention of sexually transmitted diseases.

The disadvantage of this antiseptic is allergic irritant effect on skin and mucous membranes, sometimes combined with photosensitivity, it is not recommended to apply it to patients with hypersensitivity to chlorhexidine.

The present invention solves the problem of expanding Arsenal of effective antiseptic funds with no side effects and no contraindications and having high antibacterial activity, significantly stronger expressed in comparison with commonly used antiseptics, as Lodovico, furatsilin, chlorhexidine, Rockall, hydrogen peroxide solution, polemoniaceae prophylaxis of diseases, representing the solution of surface-active substances containing the following ingredients in the following proportions, g/1000 g:

Benzyldimethyl [3-(myristoylation)propyl] ammonium chloride, monohydrate - 0,1

Purified water Up to 1000

Antiseptic drug benzyldimethyl [3-(myristoylation)propyl]ammonium chloride, monohydrate (hereafter BM), contains not less than 99,0% and not more than 101,0% C26H47ClN2O, calculated on the anhydrous substance. The drug is in the form of a white crystalline powder, odorless, easily (slowly) soluble in water, 95% alcohol, chloroform. Colorless, transparent aqueous solution with shaking forms on the surface of the foam. The activity of the solution is not reduced when stored under normal conditions, resistant to boiling and autoclaving.

0.01% solution BM has a pronounced antimicrobial action against gram-positive and gram-negative, aerobic and anaerobic, spore-forming and asporogenic bacteria in the form of monocultures and microbial associations, including hospital with MDR strains to antibiotics. The drug is more effective against gram-positive bacteria (Staphylococcus, Streptococcus, and others), acts of the se is, is lamidey, and herpes viruses, human immunodeficiency, - structured viruses and other, has an antifungal effect on yeast-like fungi, dermatophytes, records of Ascomycetes and other pathogenic fungi.

The basis of the biological actions of BM is its effect on the cell membrane. The bacterial cell has a shell and namebrand structure consisting of glycolipids, glycoproteins and fine chemicals, which are subject to the effects of BM. The predominant mechanism is the hydrophobic interaction BM related to surfactants (surface active substances), with the lipid membrane structures of microorganisms, leading to their fragmentation and destruction. The nonpolar part of the molecule BM, plunging into the hydrophobic part of the membrane, first, destroys namebrands layer, loosens the membrane, increasing its permeability to macromolecular substances and, secondly, because the membrane structures fixed most of the enzymes, BM modifies the enzymatic activity of the cells, inhibiting the enzymatic system. The hydrophobic radical BM corresponds to the maximum binding of the detergent with the cell membrane of the microorganism, i.e., this interaction is most adical BM first decreases, and then neutralizes the charge of the cell wall. Thus, as a result of exposure BM is the violation of the structure and function of membranes of bacterial cells and viral cells. BM has no effect on the membrane of human cells, because they have a much greater length of lipid radicals and hydrophobic interactions with molecules BM does not occur. In the basis of the immunomodulating activity of the BM is the increased permeability of the membranes of immune cells (lymphocytes) that triggers the activation mechanism of non-specific immune response.

It is established that the minimum concentration at which there comes a stillness treponem within 2-5 min, and Trichomonas - 5-10 min, BM is 0.01% solution. With increasing concentration of the BM stiffness of pathogens occurs faster. The effect does not depend on the solvent. This concentration is optimal for the complete suppression of the growth of cultures of gonococci, regardless of the type of solvent, the strain of the agent and retention solution. The results of the study of the prophylactic effectiveness of 0.01% solution of BM on experiments with experimental syphilis showed that all control animals already in the second month after infection development were serological reactions of blood. All experimental animals during the entire period of observation serological reactions of blood were negative. Syphilis has not developed any animal.

Listed below are the comparative characteristics of 0.01% solution of BM and 0.02% solution of HCG.

Example 1. Table 1 shows the comparative characteristics of antimicrobial activity of 0.01% solution of BM and 0.02% solution of HCG.

Antimicrobial activity of BM solutions on culture most often detected in sinusitis microorganisms was studied on solid nutrient media by the method of "wells" (N.M. Datsenko, 1989). Presented in table 1, the results showed higher antimicrobial activity of 0.01% solution of BM compared with 0.02% solution of HG.

Example 2. Table 2 shows the comparative analysis of the results of treatment of patients with infected wounds and trophic ulcers of the lower extremities of 0.01% solution of BM and 0.02% solution of HCG.

Example 3. Table 3 shows the comparative analysis of results of treatment and the average length of stay of patients.

The results are shown in tables 2 and 3 show higher efficiency BM compared to HCG in the treatment of purulent wounds and ulcers limb is wounds and ulcers, that promotes rapid wound cleansing, the appearance of granulation and epithelialization. The results of skin grafting and conservative treatment using BM better than when using HCG.

Example 4. Table 4 shows the results of treatment of patients spilled peritonitis with inclusion in the complex treatment of 0.01% solution of BM and 0.02% solution of HCG.

The use of BM in the complex treatment of peritonitis, helps to reduce the duration of treatment of patients by 7.7 bed days, reduced postoperative mortality, reduce the number of postoperative inflammatory complications.

Example 5. Table 5 shows the rate of mucociliary transport in patients with sinusitis in the dynamics of treatment.

Example 6. Table 6 shows the number kolonialismus units in 1 ml (CFU/ml) of the material under investigation in patients with sinusitis in the dynamics of treatment.

Example 7. Table 7 shows the average deviation from the norm indicators of immunity at the end of treatment (100% accepted deviation at start of treatment).

Example 8. Table 8 presents the level of eosinophilia in the dynamics of treatment of patients allergic sinusitis.

Exposure to 0.01% of the races in healthy people and patients with various forms of sinusitis.

The use of BM contributes to a more severe normalization investigated parameters of immunity in patients with chronic sinusitis than the solution of HG (table 5, 6, 7, 8).

Example 9. Table 9 shows changes in immunological parameters in patients with chronic uretroprostatitis in the treatment of BM and HCG.

Example 10. Table 10 shows the efficiency of treatment of chronic and torpid gonorrheal urethritis.

Example 11. Table 11 presents the indicators of the effectiveness of treatment of patients with Trichomonas urethritis.

The inclusion of 0.01% solution of BM in the complex treatment of urethritis and retroprosthetic various etiologies leads to a more rapid normalization of immunological and clinical parameters in patients than using a 0.02% solution of HG (tables 9, 10, 11).

Antiseptic BM according to the invention has a high antibacterial activity, significantly stronger expressed in comparison with commonly used antiseptics, as Lodovico, furatsilin, chlorhexidine, Rockall, hydrogen peroxide solution, polymer preparations of iodine, nitrofuranovye antiseptics, atony, decamethoxin, octenisept; has Shet immunostimulating effect; stimulates reparative processes; reduces the resistance of microorganisms to antibiotics; reduces recovery time.

BM has immunoadjuvant action, strengthens local protective response, regenerative processes due to modulation of cellular and local humoral immune response, has no local irritating action and has no properties, revealed no teratogenic, embryotoxic effects. The drug does not have carcinogenic and mutagenic properties.

Antiseptic for the prevention of diseases, which represent the solution of surface-active substances, characterized in that the solution contains benzyldimethyl [3-(myristoylation)propyl]ammonium chloride, monohydrate, purified water in the following ratio of ingredients, g/1000 g:

Benzyldimethyl [3-(myristoylation)propyl]ammonium chloride monohydrate - 0,1

Purified water To 1000,0

 

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