Drug

 

(57) Abstract:

The invention relates to the field of medicine and relates to a medicinal product for the treatment and prevention of specific and nonspecific infectious and inflammatory diseases. The invention lies in the fact that the drug consists of the active component - benzyldimethyl[3-(myristoylation)ammonium chloride monohydrate pharmaceutical diluent (water, alcohol, any vegetable, animal or synthetic). The invention provides the use of a drug that has disastrous effects on pathogens of infectious and inflammatory diseases (bacteria, viruses, fungi, protozoa), without causing side effects on the part of the body in its application. 2 C.p. f-crystals. 17 table.

The present invention relates to medicine, and more specifically relates to a drug for the prevention and treatment of specific and nonspecific inflammatory diseases of different etiology and localization, as well as using it as a means of influencing the herpes viruses and human immunodeficiency, antiseptic, disinfectant, immunoadjuvants and spermacides tools.

Surface-active washes the roll, katamin AB, ceriel, demised, chlorhexidine digluconate and others (Mashkovsky, M. D., Medicines. - M.: Medicine, 1999). The limited application of surfactants in medicine stems from the fact that many of them along with antimicrobial properties have irritant effect on the skin and mucous membranes, as well as toxic effects on the body. In addition, has not been fully elucidated the mechanism of their action at the micro - and macro, not developed simple and informative methods to rapidly and accurately characterize the harmless actions, there is no information about the mutagenic properties, remains a contentious issue about their Carcinogenicity (Krivoshein Y. S. et al., Antibiotics, 1984, No. 7, S. 519-526; Skuratovich A. A. et al. Journal of dermat. and Vener., 1983, No. 11, S. 29-32).

Known means of prevention specific (venereal) diseases, potassium permanganate, furatsilin, chlorhexidine, preparations of silver, corrosive sublimate and other (Ovchinnikov N. M. et al., Journal of dermatology and venereology, 1978, N 6, S. 49; Skuratovich A. A. Act. the matters. term. and Venus. Minsk, 1980, S. 172-175).

For the treatment of diseases of the genitourinary system widely used antibiotics, boric acid, zinc sulfate, osarsol, imidazole and other compounds. However, none of perich diseases of the genitourinary system, most of them are irritating to the skin and mucous membranes of the genital organs, some expensive, it produces resistance in microorganisms.

It is known the use of antiseptics in the treatment of inflammatory diseases of the nasopharynx. To do this, use furatsilin, potassium permanganate, rivanol, hansol, chlorhexidine digluconate, octenisept and other Main drawback of these tools is their suppression of motor activity of ciliated epithelium of the upper respiratory tract, local immune responses, and also expressed irritation (Piskunov, Z. et al. Russian rhinology, 1996, No. 5, S. 23-25; Piskunov S. H. et al. Russian rhinology, 1995, N 3-4, S. 6-11).

Antiseptics are used in ophthalmology for the treatment of conjunctivitis and prevention of post-traumatic and postoperative oslojnenii (furatsilin, boric acid, decamethoxin, zinc sulfate, and others). The effectiveness of treatment with these drugs is not very high, in addition, often there are irritating and allergic reactions (Michuk Y. F. Allergic diseases of the eye. - M.: Medicine, 1983, 224 S.). These drugs are not effective for chlamydia and herpes eye lesions.

full-time means, containing these compounds, and their use for prevention of HIV infection in humans (Wainberg, M. A. et al. Inactivaition of Human Immunodeficiency Virus Type 1 in Tissue Culture Fluid and in Genital Secretions by the Spemicide Bensalkonium Chloride; J. of Clin. Environ., 1990, N 1, 156-159; B. Polsky et al. In vitro inactivation of HIV-I by contraceptive sponge containing Nonoxynol-9. The Lanctt, 1988, 1 N 8600, p. 1456, J. Kreiss et al. Efficacy of Nonoxynol-9 Contraceptive Sponge Use in Preventing Heterosexual Acquisition of HIV in Nairobi Prostitutes., JAMA, 1992, N 4,477-482).

However, until now not found a reliable means for the above purposes.

The purpose of the invention is the development of a medicinal product (PL), which has a detrimental effect on pathogens of infectious and inflammatory diseases (bacteria, viruses, fungi, protozoa), without causing side effects on the body when it is applied.

The task is solved by the fact that a drug based on benzyldimethyl[3-(myristoylation)propyl]ammonium chloride monohydrate (PL) the following chemical formula

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as a means for the treatment and prevention of infectious and inflammatory diseases, including specific and nonspecific diseases of the genitourinary system, nose, throat, eyes, and means for preventing herpes and HIV infection through sexual transmission, the specification of the component PL pharmaceutical diluent.

PL get known by the reaction of condensation of militarycapabilities with benzyl chloride with subsequent cleaning to the required qualifications.

The resulting substance is a white crystalline powder, odorless, soluble in water, low molecular weight alcohols, acetone, chloroform.

For the purposes of treatment and prevention are encouraged to use PL pharmaceutical diluent mass fractions of 0.01 to 1.0% when razbaviteli may be water, an organic solvent, and any vegetable, animal or synthetic basis in the following ratio of components, %:

Pharmaceutical diluent - 99,0 - 99,9

PL - 1,0 - 0,01

Such dosage forms provide protection against bacterial, viral, fungal and protozoal infections, sexually transmitted diseases, as well as a reliable therapeutic effect when retroprosthetic, sinusitis, conjunctivitis and other inflammatory diseases of different localization.

The offered product can be produced in the form of 0.01 to 1.0% solution of distilled water in a special bottle with a nozzle made of polyethylene, and in the form of ointment, gel, suppositories, pills and sprays.

The data obtained showed that the PL is the most active against gram-positive bacteria, vegetative forms of bacilli and fungi, and agents of dermatomycoses (of 0.0001 to 0.01%). The range of antimicrobial effect of PL on gram-negative bacteria was for most crops in the range of 0.002 to 0.05%. The growth of bacteria of the genera Proteus, Providencia and Mycobacterium was suppressed at concentrations of 0.5 - 2.0%. Simple - Trichomonas vaginalis was sensitive to the concentration of PL 0,002 - 0,02%. PL showed a high virucidal properties in complex viruses (herpes viruses, HIV-1, influenza, adenoviruses and other) (see tab. 1 and 2).

It is revealed that the PL was the most active anti-HIV-1 agent compared with other disinfectants, tested for inactivation of the virus. Our data coincide with the results obtained by other researchers (table. 3).

Antimicrobial properties of PL stored for a long time under conditions of room temperature, refrigerator (observation period up to 5 years). Bactericidal act is lased, determining the pathogenic properties of bacteria (Hly, Ent, R and others).

The mechanism of antimicrobial and antiviral action PL, studied using electron microscopy, physico-chemical and biochemical methods, showed that it is caused by disintegration of the surface glycoproteins of the cell wall, as well as a breach in the cell enzyme systems. These processes are parallel and dependent on the dose of the drug.

Immunomodulating properties of PL.

Using generally accepted valuation methods humoral and cellular immunity in vitro and in vivo revealed that the drug PL has dose-dependent effect on the immune system. In the working concentrations PL causes immunoadjuvant effect, which is manifested in the strengthening of primary and secondary immune response; in higher concentrations - immune suppressing the immune response. The stimulating effect is manifested on opsonophagocytosis mechanism and indicators such as phagocytic number, phagocytic index, HCT-test. The observed increase in the level of EA-ROCK and The ROCK; rbtl with PHA stimulates the functional activity of T-T and T-B-induced helper cells, reducing the activity of T-T and T-B - induced suppressor. Thus, we have proved the dose is item microbicides, the expression of monocytic cells receptor for Fc fragment of immunoglobulins and C-component of complement. On the basis of obtained data we can conclude that the PL has not only an antiseptic, but also immunomodulatory properties.

Toxicology

Acute toxicity was determined by LD50on white mice and rats after a single intragastric or subcutaneous administration of the drug according to the standard technique. The data obtained showed that LD50PL after intragastric administration to mice, 1000 mg/kg and the rat 1200 mg/kg Subcutaneous injection of the drug caused the death of animals from smaller doses - LD50accounted for mice 628 m/kg and rats - 670 mg/kg LD50intravenous PL accounted for mice of 38.5 mg/kg and rats to 42.5 mg/kg

On the basis of obtained data we can conclude that PL refers to drugs with low toxicity - IV class of danger [GOST 12.1.007-76. Toxic effect of substances on the body (hazard classes)].

Chronic toxicity PL was studied on rabbits, which within 45 days was applied daily to 3 times daily to the shaved skin of 0.01% - 0,1% -1,0% solutions. Each dose was taken on 5 animals. Ointment containing 0 is s 1 month. Concentrate aerosol PL was administered to rabbits in the vagina at a dose of 1 ml per animal daily (7 animals). Glue (0,5%) appliciable rats according to the method of application of the ointment.

Assessment of body condition of animals in experiments conducted on the following parameters: common condition, survival, body weight, peripheral ECG, blood tests, characterizing the functional state of the liver and kidneys, the ratio of the weight of internal organs and their morphological status. In rats, in addition to the above indicators, studied reactions, tragedie the Central nervous system; in rabbit pulmonary ventilation and blood pressure. Some animals have investigated the activity of leukocyte peroxidase using reactions Graham, the content of glycogen by the method of Hotchkiss and Sabadash, conducted temperature-perturbation differential spectrophotometry serum albumin.

Based on the analysis of numerous data, it was concluded that the PL at concentrations up to 1.0% with long-term ingestion (chronic experiment) through the skin and mucous membranes do not adversely affect the vital organs and systems of animals, i.e., is not toxic to organismic pigs and rabbits, and on the mucous membranes of the urethra and urinary bladder in dogs.

The data obtained showed that apicale solutions PL on the skin in concentrations of 0.01 - 0.5% in the next 40 days did not cause any visual or histological changes. The increase of drug concentration to 1.0% resulted in 30 day applications to small, dry skin and slight atrophy of the epidermis. Large concentrations of LP (3-5%) ranging from 10 - 15 days caused significant changes in the skin.

Drops solution PL in the eyes of rabbits and Guinea pigs for 10 days at concentrations of 0.01 - 0.05% of irritating action on the mucous is not caused (score on a scale of Draize - 0, according to the classification Ogura - group a). Higher concentrations caused a phenomenon irritation of eyes (on the scale of Draize 8 - 10 points, according to the classification Ogura - group).

After instillation of 0.01 - 0.05% solution of PL in the urethra of male dogs 20 ml in 10 days, 4 times per day did not observe any changes in the behavior of animals. Analysis of urine, blood and histological examination of the mucosa of the urethra, bladder and other organs of dogs revealed no abnormalities.

Not identified as morphological and histological changes serotinous action PL was studied on 40 Mature Guinea pigs male weighing 300-400 g The obtained data showed that as primary contact and secondary contact areas of the skin not once during the observation period are not visually marked irritation. On histological sections of the skin and other organs of animals slaughtered at 41 days of the experiment, were no inflammatory microreactor or other changes. Therefore, the PL has no effect.

Thus, Toxicological studies have concluded that PL is a substance with low toxicity (class IV hazardous substances). In the working concentrations (0.01 to 1.0%) of the drug does not have an irritating effect on the skin, the mucous membranes of the eyes, the urethra, bladder and allergenic properties. Some side effects occur only when using the PL in doses much larger than the working concentration. Long-term intake of PL in the body does not cause any noticeable deviations in the functioning of vital organs and systems in experimental animals.

Study of mutagenic. embryotoxic action and carcinogenic properties of PL was carried out according to who recommendations. Mutagenic properties were investigated on microbial test systems by B. Ames, J. Based on the obtained data, it was concluded that PL does not have direct mutagenic effect and does not form compounds with mutagenic properties with metabolic activation in vitro and in vivo.

Studies of embryotoxic action of PL and its impact on reproductive function were performed on rats. In the first group of female rats in the period from the sixth to the eighteenth day of pregnancy were introduced storerelease solution PL. Total each animal received up to 1000 mg/kg of the drug. In the second group PL was administered from day to end a pregnancy once a day. In the third group, the drug was instillirovti males over 60 days, females - 30 days, then spent mating.

On the basis of the conducted research it can be concluded that the PL has no teratogenic, embryotoxic effect does not reduce the reproductive function and does not infringe on the development of offspring in the postnatal period of life.

Carcinogenic properties of the drug was investigated by introducing it into the bladder of dogs in a mixture with the rapidly solidified plastic nonagria-65, as well as in mice and rats, which are 3-5 times a week, put the solution on freshly shaved skin areas in mo natural death, dogs were scored over 2.5 years, spent their pathologic-anatomical and histological studies.

Summarizing the data, we can conclude that PL does not cause the formation of tumors or typical for this pathology changes in the urinary bladder, skin and other internal organs of animals, i.e., does not have carcinogenic activity.

The study spermacides actions were conducted by the method recommended by the who. To do this, the sperm of people was mixed with various concentrations of PL and the microscope was controlled by their mobility, and also examined other indicators (pH, reduction of methylene blue, a test contact with the cervical mucus, the level of fructose and other). Just was studied 27 sperms in men aged 18 - 23 years. The results of the experiments showed that the optimal concentration of PL, stopping sperm motility after 30 seconds is 0,02%. Higher concentrations result in immediate immobilization of sperm, but their lysis.

The effect of PL on the function of the mucociliary transport. It is proved that mucociliary clearance plays a leading role in the protective functions of the nose and paranasal sinuses. Many drugs by podvezko practice.

The effect of PL on the function of the mucociliary transport was studied in experiments on mucous of esophagus frogs, as well as in the clinic for people with some saccharine sample of the polymer film with methylene blue and saccharin and using radionuclide label. It is proved that at concentrations of 0.01 and 0.05% PL does not affect the transport function of ciliated epithelium, and in patients with sinusitis normalizes mucociliary clearance.

The study of preventive and curative effects of PL on animals

Preventive action is Concerned with sexually transmitted diseases studied in experimental syphilis in rabbits. The experiments were conducted on 156 rabbits breed chinchilla, which were infected with freshly prepared suspension pale treponemes (strains Nichols, CKVI-8) cutaneous way. After 30, 60, 120, 180 and 240 min after infection were treated skin of the infected area of 0.01 to 1.0% solution PL. Rabbits of the control group was treated with distilled water. All animals were housed on clinical and serological monitoring of 6 - 12 months. For control used Wasserman (PB), REBT and the REEF, which was set to 1.5 months after infection every 2-3 months. Also methods were used passage of lymph nodes and re-Zara is different rabbits 0.01 to a 1.0% solution of PL in the period from 30 minutes to 2.5 hours from the moment of infection leads to 100% protection of animals against syphilis.

Therapeutic effect on models of purulent wounds and peritonitis in experimental animals (rats, rabbits, Guinea pigs, dogs are more than 500 animals) was performed according to the conventional methods using biological, morphological, histological and immunological methods.

The data obtained showed a high therapeutic activity of PL used in aqueous solution, ointment and spray with purulent-inflammatory diseases and peritonitis in experimental animals. PL was more effective drug in the treatment of purulent wounds in comparison with the widely used antiseptic chlorhexidine-digluconate (PL. 4).

Statistically proven that the observed positive effect in experimental animals due to the stimulating effect of PL on the factors of resistance - phagocytic index and bactericidal activity of neutrophils. Antiseptic chlorhexidine digluconate such has no action (table. 5).

Analyzing the data obtained using a 0.5% ointment pharmaceuticals for the treatment of purulent experimental the n bactericidal, the reduction of microbial load, enhancing the regeneration and stimulation of the local immune response action.

Investigation of antifungal action of ointment PL. On models of candidiasis in Guinea pigs, played by intradermal injection of Candida albicans followed by scarification and trichophytia caused by rubbing cells Trichophyton rubnim (strain 796) in pre-depilitory and clarificatory area of skin on the side, studied therapeutic effect of a 0.5% ointment. For comparison, we used official antifungal ointments undecen, clotrimazole and tikungan.

Summarizing the obtained results, we can conclude that therapeutic efficacy of the ointment containing 0.5% PL, is quite high and exceeds the efficiency ointments comparison. So, for the 4th day of applying ointment 2 times reduction in the size of lesions caused by Candida albicans and Trichophyton, there was a cleansing of the center of the hearth from ulcers, erosions crusts, decreased colonization of tissues by pathogenic fungi 1-2 orders and 8-th day was a clinical recovery. Summarizing the research results, we can conclude that the ointment PL is an effective antifungal agent, which has advantages over the oppo is Inoi back surface caused by contact thermal burn using the standard device. Treatment was started 24 hours after the burn ointment and spray with 0.5% PL. For comparison used officinal ointment, levocin. The results obtained are presented in table. 6.

As can be seen from the data table. 6, a statistically significant decline in the area of RAS in the treatment ointment and spray with PL begins after the 8th day, which was 4 days earlier than in the control. It can be argued that this reduction is due to the acceleration of the transition from the phase of inflammation to the phase of repair and it is associated with anti-inflammatory and immunoadjuvant properties PL.

Action PL when inflammatory lesions of the cornea. The experiments were conducted in 14 rabbits of the chinchilla breed weighing 2-2 .5 kg Purulent-inflammation of the cornea caused by the introduction into the cornea suspension of the daily culture of Staphylococcus aureus strain 209 P. 2-4 days in 13 rabbits on the cornea of the eye formed of an ulcer the size of 3 x 6 mm with purulent discharge at the bottom, and also observed phenomena inflammatory reactions: conjunctivitis, blepharospasm and other

Taken in the experience of the rabbits were divided into three groups. Animals of the first group was treated with a solution of LP (eye drops based on PL - LPGC), the second official decamethonium eye drops (DHA), and Tr animals is ayvali three times daily throughout the experiment.

All animals have conducted daily monitoring, controlling the dynamics of changes in the cornea of the eye test and control animals in the previously described methodology. In addition, conducted crops swabs from the cornea of rabbits for meat-peptone broth for detection of S. aureus 209 p. the results of the experiments are presented in table. 7.

These data indicate that purulent discharge and detection of S. aureus stopped at 4 and 6 days in all animals treated with LPGC and DHA, respectively. At the same time among untreated animals purulent discharge was observed during the whole period of the experiment.

Resorption of purulent infiltration quickly began and ended in all animals treated with LPGC (3 day) and DHA - 5 day from the start of treatment. In the animals treated with LPGC and DHA, the start and end time of resorption of purulent infiltration were respectively 4 and 10 days from the start of treatment. Epithelization of the cornea occurred in all animals to 10 and 16 days after starting treatment LPGC and DHA, respectively.

Thus, from the above data it can be concluded that LPGC are highly effective in the treatment of inflammatory lesions of the cornea glasnost.

Clinical studies

Clinical study of PL as a means of individual prevention of sexually transmitted diseases was conducted in 7 leading STI institutions, and as an antiseptic for the treatment and prevention of inflammatory processes in 20 clinics surgical, obstetric-gynecology, ophthalmology, otorhinolaryngology, combustionengines profile.

Analysis of reports from medical institutions, showed that the PL in different dosage forms had no harmful side effects on the human body, did not cause irritation of the skin or mucous membranes, as well as allergic reactions.

Venereology. Application of 0.01% solution of pharmaceuticals for the prevention of sexually transmitted diseases by treating the urethra, vagina and vulva protects patients in 100% of cases if the drug was applied no later than 2.5 hours after intercourse. All under supervision were more than 1000 patients at risk.

Urology. Application of PL in the treatment of acute and chronic retroprosthetic specific and nonspecific etiology revealed its high efficiency, which was confirmed by the P in the treatment of chlamydial retroprosthetic.

Surgery. The use of different dosage forms PL (solutions of water and alcohol, ointments, gels, aerosols, glue) for the treatment and prevention of inflammatory processes of various etiology and localization revealed their high efficacy and lack of adverse reactions.

Drugs were applied with a positive effect in festering wounds of traumatic and postoperative, brushes and fingers, pleuro-pulmonary and burn, paleontology obliterative vascular diseases of the extremities (table. 9), fistulas, ulcers, and venous ulcers, as well as in peritonitis (table. 10).

Aqueous or alcoholic solutions of PL tested as antiseptics for hand surgeon and the surgical field. Glue PL was vysokoeffektivnyi for the prevention of suppurative complications microtraumas and bespomoschnogo the management of postoperative wounds.

Obstetrics and gynecology. Drugs PL showed high efficiency in the treatment and prevention of inflammatory processes that occur after breaks prominate and vagina in childbirth after cesarean section, vaginal hysterectomy, the conservative vaginal plastic surgeries, prevention of puerperal infection in women with About the coy (chlamydia, herpes and other) etiology - vulvovaginitis, colpitis, cervicitis, etc.

Otolaryngology. Extensive testing of the PL in ENT practice showed its high effectiveness in the treatment of inflammatory diseases of the paranasal sinuses acute and chronic sinusitis, rhinosinusitis, as well as angina, laryngopharyngitis and others (PL. 12). The observed effect is due to the antiseptic and immunoadjuvant properties of the drug, and the fact that it does not inhibit mucociliary clearance of mucous membrane.

Ophthalmology. Drugs PL in the form of eye drops (0.01% solution PL 0.9% sodium chloride solution) tested for the treatment of non-specific conjunctivitis (chlamydia, gonococcal) etiology. Set high clinical (90.4%), and etiological (63,7%) efficiency etiopathogenetic therapy ophthalmoplegia with local application in the form of instillation in the conjunctival cavity 0,01% LPGC.

LPGC was also effective in preparing patients for intraocular operations and postoperative their responsibility for the prevention of inflammatory complications.

The observed effect, in our opinion, due to the antiseptic, protivovospalitelnoe conjunctiva of the eye.

Dermatology. Various dosage forms PL tested in dermatology for mono - and complex therapy of bacterial and fungal skin diseases. High efficiency possess drugs PL in the form of ointment and gel in the treatment of strepto - and stafilodermy, mycosis of the skin and mucous membranes, mycoses and large folds, including disgestrotical shapes and forms, complicated by pyoderma, dermatitis smooth skin, onychomycosis and keratomycosis, including depriving. In patients with different clinical forms piodermitov positive effect was achieved in 98.3% of cases, which reduces the treatment time is 2-3 days compared with traditional therapies. Positive therapeutic effect on acne and herpes skin lesions and mucous membranes (table. 13).

Immunoadjuvant properties LP in the treatment of purulent-inflammatory diseases in humans

It is well known that patients with purulent-inflammatory processes, as a rule, develops immunological failure in violation of local and systemic immune responses (Kuzin, M. I., Kostyuchenok B. M. Wounds and wound infection. A guide for physicians. - M.: Medicine. 1990, 591 S.; Theory and practice in local treatment of GN is ical methods research reliably shows the positive therapeutic effect of PL at purulent inflammatory processes due not only to its antimicrobial properties, but also a stimulating effect on the immune response of the body.

In the treatment of 68 patients with chronic uretroprostatitis using PL has been reliably significant stimulation of the absorption capacity of urethral neutrophilic granulocytes (table. 14). Positive therapeutic effect when therapy PL amounted to 92.8 per cent and previal effect obtained by applying the immunomodulator of adjuvant (86,9%). In the group of patients who received basic therapy without immunoadjuvants, a positive effect was observed only in 52,9% of cases.

In the treatment of 235 patients with different clinical forms piodermitov included in the complex therapy of 0.5% ointment PL has allowed to obtain a positive clinical effect in 98.3% of cases, whereas in the comparison group, this effect was achieved in 89.2% of cases.

Patients pyodermia changed the parameters of immunological reactivity of the organism. PL has a stimulating effect on opsona-phagocytic mechanism and other indicators of immunity (see tab. 15). Based on data presented, we can conclude that th is and the activity oxybiotic systems microbicides with a parallel increase their reserves in phagocytic cells, changes antigenic stimulation of the receptor apparatus of monocytes and lymphocytes, stimulation fibonaccisequence function of leukocytes and other

A similar effect on the immune factors of various forms of PL were obtained in the treatment of patients with purulent-inflammatory diseases of different etiology and localization in surgical, obstetric, ophthalmological, otorhinolaryngological, and other clinics.

The results of numerous experimental and clinical studies indicated that PL is more efficient than the widely used antiseptics: chlorhexidine digluconate, furatsilin, iodide, etc. and can be recommended for widespread use in clinical practice.

Disinfectant activity PL

The use of pharmaceuticals for surgical antisepsis

Experimental substantiation of the use of 0.1% water and 0.1% alcohol solution of pharmaceuticals for surgical antiseptics. Experiments were performed under conditions relevant to the practical application of antiseptics. Used method M. Rotter (Rotter M. L. Hygienic Hand Desinfection // Infect. Contr. 1984. N 1. P. 18 - 22.) on the people-volunteers with the calculation of the coefficient of reduction after contaminate the alcoholic solution of chlorhexidine digluconate (gibian), in accordance with the applicable regulations (Order of the USSR Ministry of health N 720-78; instruction USSR Ministry of health, N 06-14/10 from 3.08.84).

Ramanantsoa aftereffect PL was installed in the model P. Michand et al. (R. Michaud, MS. Grath, M., Goos W. Application of a glaved - hand model for multiparameter measurements of skin - determing activity // J. Klin. Microb. 1976. N 3. H. 406-413.)

The data analysis shows that contamination of the hands of the test strains of E. coli in 1 ml rinse is an average of 1,4105microbial bodies (the logarithm 5,15). Treatment arms 70% alcohol, Pervoural, 0.5% alcohol solution of chlorhexidine digluconate, as well as alcohol and aqueous solutions of LP, led to the reduction of contamination, but in varying degrees. The least effective of the investigated solutions was 70% alcohol (reduction coefficient 3,47 lg10). Antimicrobial effect, corresponding to the requirements of antiseptics used for surgical treatment, legal documents, obtained by the tests of 0.1% water and 0.1% alcohol solution PL. Exposure to contaminated hands in 0.1% aqueous antiseptic solution for 3 and 5 min gave the same results: the coefficients of reduction was equal 5,11 lg10. The highest reduction coefficient (5,15 lg10) was obtained using a 0.1% sportowo lg10and 0.5% alcoholic solution of chlorhexidine digluconate - 5,04 lg10.

High efficiency of 0.1% aqueous solution of PL was confirmed in experiments on 20 volunteers without artificial contaminaci standard test culture of their hands, and when testing solutions PL in clinical practice. Crops swabs from the skin of the hands of all 20 volunteers, treated with 0.1% aqueous and alcohol solutions of PL given the coefficients of a reduction from 2.5 lg10to 3.3 lg10.

Ramanantsoa aftereffect solutions PL was examined on 10 volunteers, whose hands after contamination with E. coli and processed by the corresponding drug was put on sterile surgical gloves, and then immediately and after 1, 2 and 3 hours did the sowing with the skin, counting the number of grown E. coli and determined the coefficient of reduction.

The data obtained show that the coefficients of reduction when using both solutions LP were high (5,22-a 5.25 lg10) and remained at these levels for three hours.

Analysis of the results of experiments on the effectiveness of treatment of the skin of the surgical field and the elbow bends 84 volunteers showed that the desired decontamination effect is achieved by using 0.1% spirolog is), that is consistent with accepted standards.

Summarizing the results of the research, we can conclude that 0.1% water and 0.1% alcohol solution PL in their properties comply with the requirements of antiseptics used in surgical practice, they provide a quick disinfecting effect. The coefficients of reduction solutions LP, as well as ramanantsoa aftereffect superior to those of Parvomay and chlorhexidine digluconate, drugs, currently used for surgical antisepsis (PL. 16).

There was also a high disinfecting activity of 0.1% alcohol solution PL when processing the surgical field and leather elbow bends.

In any case, the use of 0.1% water and 0.1% alcohol solution PL no observed adverse adverse local or systemic reactions. The positive point is the stability of working solutions the PL to the influence of external factors and long term preservation (observation period 3 years).

Preventive action solutions PL when infected wounds.

In the experiment, studies were performed on rats, whose wounds were modeled according to the standard technique, infinera is and using common indicators (see table. 17). Analysis of the data shows that the best preventive effect achieved when applying for treatment of infected wounds of water and alcohol solutions of PL compared with solutions of chlorhexidine digluconate and iodine.

Clinical trials of water and alcohol solutions of PL for the prevention of suppurative complications of micro traumas held in the factory in the workshops increased injuries for 3 years. Of the 107 people with microtrauma and abrasions, applied to the plant clinic, after processing solutions PL a secondary infection was observed only in 5 patients (4.5 percent). In the control group (128), where the processing of micro traumas were conducted dyes (brilliant green, fukortsin, methylene blue), as well as iodine, secondary infection was observed in 49 (34,6%). It is noted that the healing of micro traumas in individuals treated with solutions of PL, occurred in the period from 3 to 6 days (average 3,50,6 days), while in the group, which used dyes, these periods ranged from 5 to 8 days (average 5,50,3 days).

The observed effect of solutions of PL in the prevention of suppurative complications of microtrauma caused severe CLASS="ptx2">

1. Medicinal product for the treatment and prevention of infectious and inflammatory diseases, comprising the active ingredient and a pharmaceutical diluent, characterized in that it contains an effective amount of the active component, representing benzyldimethyl [3-(myristoylation)propyl]ammonium chloride monohydrate pharmaceutical diluent.

2. Drug under item 1, characterized in that as a pharmaceutical diluent it contains water and/or alcohol and benzyldimethyl[3-(myristoylation)propyl]ammonium chloride monohydrate in quantities of 0.01 to 1.0%.

3. Drug under item 1, characterized in that as a pharmaceutical diluent it contains any vegetable, animal and synthetic basis in the following ratio of components, %:

Vegetable, animal or synthetic - 99,0 - 99,9

Benzyldimethyl[3-(myristoylation)propyl] ammonium chloride monohydrate - 1,0 - 0,01

 

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Antiseptic // 2118174

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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