Antiseptic "katzel"

 

(57) Abstract:

The invention relates to pharmaceutical industry and relates to antiseptic compositions for the prevention and treatment of wounds, burns and infectious complications in skin diseases. The tool contains a water-soluble polyelectrolyte complex catamine AB and sodium carboxymethylcellulose, sodium chloride, glycerin and water in a ratio of components, wt.%: katamin AB 0,5 - 1,0, sodium carboxymethylcellulose 4,0 - 5,0, sodium chloride 2,5 - 3,5, glycerin 8,0 - 12,0, water - the rest. Effect: the invention expands the Arsenal of antiseptics. 1 Il., 6 table.

The invention relates to pharmaceutical industry and relates to antiseptic compositions for the prevention and treatment of wounds, burns and infectious complications in skin diseases.

Known antibacterial agent with a wide spectrum of action - alkyldimethylbenzylammonium chloride (ketamin AB), one of the dosage forms which Rockall, which is an aqueous 1 -10% solution alkildimetilbenzilammoniya chloride mixture is used as an antiseptic agent for treatment of the hands of the surgeon, the surgical field and wound poki, Drug, ch. II, M.: Medicine, 1993). Katamin AB called benzalkonium chloride comes in many foreign Pharmacopoeia (France, USA, UK). This drug is active against some gram-positive and gram-negative bacteria, some species of yeasts and filamentous fungi. He is an inhibitor of several enzymes of bacteria, microbial toxins.

However, this drug is highly toxic and skin-irritant effect.

Known drug katapola, representing a high molecular weight modified antiseptic, complex dimethylmethyleneammonium chloride (catamine AB) and a copolymer of vinylpyrrolidone with crotonic acid, (ed. St. USSR N 1517173, MKI4A 61 K 31/14). The katapola is less toxic and does not cause skin irritation, has a prolonged action.

However, the possibility of widespread use of katapola is limited, so as not established its industrial production due to the lack of domestic raw materials, namely crotonic acid. In addition, dosage form katapola (aqueous 10% solution) creates certain difficulties in its use since before use, there is a need to residentialstyle effective antiseptic medicines.

Created antiseptic drug katzel - soluble polyelectrolyte complex dimethylmethyleneammonium chloride (catamine AB) and sodium salt of carboxymethylcellulose (Na-CMC).

This polyelectrolyte complex (PEC) is obtained by the electrostatic interaction of natural polycation Na-CMC charged particles surface-active substances catamine AB with the formation of salt linkages between carboxyl groups polymer and Quaternary ammonium bases.

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The presence of the PEC is confirmed by a number of scientific experiments, in particular gel-chromatography of catocala on Sephadex in conditions preventing the dissociation of the complex. The zone of elution of catamine AB moved from the elution of low molecular weight substances in the area of the elution of high molecular weight substances, which confirms the increase in molecular weight due to the joining of high-molecular substance - Na-CMC.

In minakamikogen reactions may occur as soluble in water and insoluble complexes. Katzel - soluble complex, the conditions of education is determined by parameters of the reaction mixture, including Chesley (PL. 1).

In the preparation contains as the plasticizer is a polyhydric alcohol is glycerin, which when using katzela prevents drying of the resulting gel film.

The formation of new substances - katzel possessing antimicrobial activity of the respective components is not obvious, since such a high-molecular modification of the active principle (catamine AB) can lead to a reduction in antimicrobial activity. However, in our positive effects: local irritant action of catocala significantly decreased compared with Catalina AB, whereas high antimicrobial activity and a broad spectrum of action of catocala preserved.

Katzel contains katamin AB, Na-CMC, sodium chloride, glycerin and water in the following quantitative content, wt.%:

Katamin AB - 0,5 - 1,0

Na-CMC - 4,0 - 5,0

Sodium chloride is 2.5 - 3.5

Glycerin - 8,0 - 12,0

Water - the Rest

As auxiliary substances in the composition of the drug can be added in micromolecule Riboflavin, causing a yellowish color to give a more aesthetic appearance of the product, and for anesthetic action can be added to trimega the gel, which is easily Packed in tubes. The use of such dosage forms are also much more efficient and convenient as gel unlike the solution does not spread on absatively surface, and no additional before use, prepare a solution of desired concentration.

Raw materials from which prepares the drug is not scarce, Na-CMC requires no special synthesis and is widely used in pharmacy.

The technology of obtaining katzela simple and you can get a standard product. It includes the following stages:

- preparation of working solutions of catamine AB and Na-CMC;

- carrying out a reaction between Na-CMC with Catalina AB;

- adding a plasticizer and a colorant;

- thermal processing.

Getting preparation is illustrated by the following examples (table. 1).

Example 1.

In the chemical heat resistant glass contribute 4.0 g Na-CMC, pour 60 ml of hot 90oC water, mix thoroughly and leave for 3 - 4 hours to full swelling.

In a separate cups cooked solutions:

1 g of catamine AB (in terms of 100% substance) in 5 ml of water;

- 2.9 g of sodium chloride in 5 ml of water;

0.0005 g ri is enom stirring, add 10 g of glycerol and bring a lot of preparation up to 100 g

The content of catamine AB 1%, Na-CMC 4%.

Example 2.

In the chemical resistance of the glass contribute 4.0 g Na-CMC, pour 60 ml of hot 90oC water, mix thoroughly and leave for 3 - 4 hours to full swelling.

In a separate cups cooked solutions:

- 0.5 g catamine AB (in terms of 100% substance) in 5 ml of water;

- 2.9 g of sodium chloride in 5 ml of water;

0.0005 g of Riboflavin in 5 ml of water.

The obtained solutions are successively introduced into a solution of Na-CMC, mix thoroughly, and then add 10 g of glycerin, re-mix and make the mass of the drug to 100 g

The content of catamine AB of 0.5% Na-CMC 4%.

Example 3.

In the chemical heat resistant glass make 4 g Na-CMC, pour 60 ml of hot (about 90oC) of water, mix thoroughly and leave for 3 - 4 hours to full swelling.

In a separate cups cooked solutions:

5 g catamine AB (in terms of 100% substance) in 10 ml of water;

- 2.9 g of sodium chloride in 5 ml of water;

0.0005 g of Riboflavin in 1 ml of water.

The obtained solutions are successively introduced into a solution of Na-CMC, mix thoroughly, doba is, a CMC of 4%.

Example 4.

In the chemical heat resistant glass make 4 g Na-CMC, pour 60 ml of hot (about 90oC) of water, mix thoroughly and leave for 3 - 4 hours to full swelling.

In a separate cups cooked solution:

1 g of catamine AB (in terms of 100% substance) in 10 ml of water;

- 2.9 g of sodium chloride in 5 ml of water;

0.0005 g of Riboflavin in 1 ml of water;

5 g trimekainom in 10 ml of water.

The obtained solutions are successively introduced into a solution of Na-CMC, mix thoroughly, add 10 g of glycerin, re-mix and make the mass of the drug to 100 g

The content of catamine AB 1%, Na-CMC 4%, trimekainom 5%.

Table 1 contains data from 12 case studies of receipt of catocala. It was found that the increase in the content of the drug ketamine AB above the upper limit of the causes of drug use local irritant effect. The introduction of Na-CMC in a larger number causes the formation of lumps, as uniform swelling more Na-CMC requires more water. Reducing catamine AB and Na-CMC is lower than the lower limits does not allow to achieve the desired effect. The concentration of sodium chloride more than 3.5 and less than 2.5 leads to pomot the data limits changes the properties of the gel film, and the increase is not possible to enter in the necessary quantities of the other necessary ingredients.

Experimental animal studies indicate that the drug is effective and harmless drug that stimulates the process of regeneration in wounds of soft tissues.

The drug has an effect on gram-positive and gram-negative bacteria, including staphylococci, Escherichia, which can be recommended for the treatment of purulent pathology of the skin and soft tissues.

Trimekain, included in its composition, has an anaesthetic effect, reducing pain in the affected area.

The drug is hydrophilic plastic base, does not violate the gas and heat of skin, easy to remove (if necessary) with the wound surface water, hydrogen peroxide or other aqueous solutions.

The effectiveness of therapy is achieved by mechanical-chemical processes in place applications and antimicrobial properties. The high hydrophilicity of the drug gives you the opportunity to mix with the wound.

The use of catocala in experimental abscesses, purulent pathology of the skin and serous-mucous cavities showed rapid/P> Prolonged and repeated application of catocala on the skin does not cause pathological changes in the blood, urine, does not violate renal function and liver, has no effect on the immune system of experimental animals.

Experiments were conducted on 18 Guinea pigs (table. 2). Animals were simulated purulent process with lesions of the soft tissues of the back. The experiment used a culture of Staphylococcus aureus and Escherichia.

In experimental groups was marked by rapid suppression of contaminating microflora. Almost 3 days of microflora in the wound was absent. At the same time was relatively rapid subsidence of the inflammation, the early development of granulations and appearance of the area epithelialization along the edges of the skin wound. To 12 days in the healing process was pronounced, and by 20 days in 6 animals, the wound is closed, and 6 remained dense crust, fixed over a limited clean wound surface constituting not more than 20% from the initial one. Cytological studies have confirmed the beneficial effect of therapy on the course of the wound process, a significant difference in the experience of control.

The results of the study of catocala revealed a pronounced anti-inflammatory and antimicrobial Dane different etiology 1 m 2 phase of wound healing, pressure sores, infected leg ulcers, infected burn surfaces and other surgical pathology.

The efficacy in inhibiting the growth of various microflora in combination with a good plastic properties due to a special additive glycerin, allows us to recommend katzel also for hand surgeons, the surgical field, lubrication of small cracks, scratches, abrasions, cuts, etc.

Katzel suitable for use in military field conditions, injuries.

In the laboratory studies of sorption and kinetic characteristics of the drug katzel on the model of the wound surface, single-sided limited contact with model fluid (according to the method of I. M. pepper, 1979; B. M. Datsenko et al., 1989).

As model fluids were used citrate blood. The results of the study sorption capacity shown in the drawing.

As can be seen in the present drawing, katzel belongs to the group of drugs with moderate osmotic activity, which is manifested only for 4 - 5 hours and higher than in 2 times 10% sodium chloride and 5 times syntomycin emulsion.

Strains of these microorganisms were isolated from patients transferred from other hospitals in the Department of wounds and wound infection Institute of surgery. A. C. Wisniewski RAMS. Wounds of the soft tissues of the patients were clinically on 2 stages of wound healing. Infection of wounds, according to the quantitative research method was at the level of 103- 104m t 1 g of tissue.

Just been tested 200 strains, which were divided into 4 groups, each of which consisted of 25 strains of microorganisms separate species. The results are presented in table 3.

As can be seen from table 3, the highest antimicrobial activity was found against Staphylococcus. All 50 strains were susceptible to Catalu. Significantly weaker antimicrobial activity against E. coli is very low in relation to Pseudomonas aeruginosa and was absent on the Proteus.

At the Institute of surgery named A. C. Wisniewski RAMS were conducted clinical study of the drug katzel. The species composition of the microflora isolated from wounds of patients, selected on treatment with bandages with ketazolam of RAS was detected microflora, but, when analyzing these cases, it is revealed that the remaining number of microbes in 1 g of tissue wounds menee1.

All patients reported good tolerability of catocala. Any side effects immediately after dressing, or in a remote period, when changing the dressing was carried out through the day, there was none. The drug did not cause discomfort, quickly absorbed, easily removed from the wound surface.

In 4 cases a moderate amount of purulent discharge in the wound before applying katzela disappeared only to the end of the second week. All clinical observations bandage from sticking to the wound surface was not dry, not damaged granulation tissue.

As can be seen from table 5, the use of catocala in treatment of RAS helped in the short term to normalize the course of the wound process, significantly reduce the time epithelization and wound filling defect Mature, intense bleeding, bright red granulation tissue.

In the group of patients with severe pain (patients with nonhealing venous ulcers, traumatic wounds) using katzela with trimekainom within the wound is she in the wounds, ulcers. Did not require supplemental pain medications, as is done when used traditional medicines in the treatment of similar groups of patients.

The duration of stay of the patient in the hospital for the appointment of catocala compared with the control group, which used 5% syntomycin emulsion, were also significantly shorter due to the possibility to perform the final stage of surgical treatment autodermoplasty, to impose a prior-deferred or early secondary stitches on the wound.

Recovery and improvement in the course of the wound process was observed in 33 patients that were $ 91.7%.

Comprehensive clinical and laboratory study of the effectiveness of the drug katzel in the treatment of various groups of patients with poorly-granulating, nonhealing wounds of soft tissues, trophic ulcers showed that this drug belongs to the group of drugs that stimulate the regenerative process.

In the absence of abundant sickness, gram-negative microflora using katzela in complex treatment allows for 10 - 14 days to prepare the wound for plastic surgery or closing their secondary sutures.

Katzel with the addition of trimekainom has a local analgesic effect, so it can be used for the treatment of poorly-granulating, nonhealing wounds of soft tissues, trophic ulcers with severe pain.

The members of the St. Petersburg Center for the treatment of surgical infections was conducted clinical study of the drug katzel local surgical treatment of purulent diseases of soft tissues (cellulitis brush, chronic paraproctitis, purulent diseases of the soft tissues on the background of diabetes mellitus) in order to relieve the purulent process.

Pori assessment of the clinical course of purulent process in the local application of catocala drew the attention of abundant purulent wound. On average 2 - 3 days earlier was the cleansing of wounds from necrosis appeared granulation. Patients reported improvement in overall health.

In patients with acute purulent paraproctitis katzel began to apply in the early postoperative period, at the first dressing change. The process was characterized by the vastness of the destruction by area and depth. Typically after 6 hours after the start of treatment reported a decrease of hyperemia and edema of the wound edges, the disappearance of pain. H is their mass was rejected from the walls and bottom of the wound, the exudate was liquid. Patients reported a significant decrease in pain.

Drug katzel does not cause allergic reactions even in patients with intolerance to the drug-protein nature.

After local application of catocala was observed regenerative type of cell reactions. Decreased neutrophil count with a predominance of regenerative forms. The newly formed cellular elements were presented histogene cells with marked differentiation. This histogramm shows the subsidence of the inflammatory response and maturation of a young granulation tissue.

In the same period of observation on the background of local application of 10% sodium chloride cell response was characterized by degenerative and inflammatory type, and only 10 to 12 days acquired the regenerative nature.

The results of clinical trials of the drug katzel allow to draw the following conclusions:

- katzel can be used as a therapeutic agent for the treatment of purulent wounds of soft tissues;

- katzel has a strong bactericidal effect on the microflora of purulent during the day;

- katzel adding trimethylsily purulent process in reflexogenic areas (anorectal zone, the area of the face, brush);

- local application katzel leads to more rapid relief of the first phase of inflammation and phase reparative healing reactions;

- katzel is highly effective for the treatment of purulent-inflammatory diseases in patients with diabetes mellitus;

- katzel well tolerated and does not cause adverse reactions when applied topically within 14 days;

- katzel may be used topically as a prophylactic antimicrobial agent in infected wounds of different Genesis.

Antiseptic containing katamin AB, sodium chloride and water, characterized in that the polymer it contains sodium carboxymethylcellulose and optionally glycerin in the following ratios, wt%:

Katamin AB - 0,5 - 1,0

Sodium carboxymethylcellulose - 4,0 - 5,0

Sodium chloride is 2.5 - 3.5

Glycerin - 8,0 - 12,0

Water - The Rest

 

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