RU2505285C1 - Method for increasing biocidal and therapeutic action of suspension-cream with linco-spectin - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention represents a method for increasing biocidal and therapeutic action of a suspension-cream with linco-spectin consisting in detoxification and polymerisation of linco-spectin 100 g in water 300 ml by 0.15±0.05% glutaric aldehyde 0.15±0.05% alkyldimethyl benzylammonium chloride at 38-40°C for 2-3 days.

EFFECT: linco-spectin resistance to the enzymatic degradation of a microbial cell, lower toxicity, faster tissue regeneration and manifested biocidal action on the pathogenic bacteria, viruses, and moulds for 3 years.

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Description

The invention relates to biotechnology, antibiotic therapy and pharmacology.

It was studied that lincomycin and spectinomycin are active against staphylococci, streptococci, E. coli, salmonella, mycoplasmas and are used to treat arthritis, respiratory and gastrointestinal diseases.

Linkospectin - 100 contains lincomycin - 22.2 g, spectomycin 44.4 g. The mechanism of action of lincomycin is based on the inhibition of protein synthesis of microbial cells with impaired formation of peptide bonds. The action of spectomycin is based on inhibition of protein at the level of ribosomes. Linkospectin is available in a 12.5% solution containing 4.2 g of lincomycin and 8.4 g of spectomycin. One 150-gram bag after dissolving in 150-200 liters of water is used from 3 to 7 days (25 mg. For 1 kg. Live weight). In general, linkospectin under the trade name "linesol" has a wide spectrum of action on a number of microorganisms resistant to linkospectin and other antibiotics.

To overcome the drug resistance of microorganisms, the 4th generation of antibiotics has been developed, fluorine, piperazive radical, clavulanic acid, a number of organic acids are introduced into their composition and various combinations of drugs are used. However, microbes develop resistance to new antibiotics against the background of increased nephro-, hepato-, neuro-, ototoxicity.

The authors of the application for the first time on the principle of producing toxoids by detoxification and polymerization with formic acid aldehyde - formaldehyde and glutaral or succinic aldehyde separately and in combination with quaternary ammonium compounds - ethonium, Biopag-D, alkyldimethylbenzylammonium chloride and only a number of antibiotics, reduced antibiotic antibiotic efficiency against bacteria, including mycobacterium tuberculosis, but also viruses and molds. In connection with the foregoing, glutaraldehyde was used to detoxify and enhance the biocidal action of linkospectin.

Glutaraldehyde is an aldehyde of glutamic amino acid, has a greater virucidal and sporocidal activity than formaldehyde, and is especially used in the manufacture of vaccines, toxoids and as a disinfectant when combined with bis-quaternary ammonium compounds.

A known method of manufacturing ointments, suspensions, emulsions using antibiotics on a petrolatum base (Muravyov I.A. Technology of medicines and galenic preparations. Medgiz, 1971. M., p. 650-700; The prototype is a method of manufacturing ointments-suspensions, emulsions, Reference "Vidal Veterinarian" - Medicines for veterinary use in Russia, M.,; Astra-Farmservis, 2011. S.202-230).

The disadvantage of the tablet, powder and water-soluble forms of linkospectin is the lack of action on viruses, molds, the emergence of resistant microorganisms against the background of increased toxicity and the reduction of shelf life, accumulation in meat, eggs.

Currently, the source of most infectious diseases is the association of some microorganisms with others (viruses with bacteria, etc.).

The established decrease in toxicity and the increase in the biocidal action of a number of antibiotics including linkospectin with the help of 0.2-0.3% formaldehyde solution with 0.2-0.3% ethonium solution, and then the higher efficiency with the decrease in toxicity with glutaraldehyde was used in the manufacture and testing of a solution of linkospectin (Evglevsky A.A. et al. A method for increasing the effectiveness of antibiotics. Patent No. 2400218, September 27, 2010 and Patent No. 2425668, August 10, 2011)

An object of the invention is to ensure the resistance of linkspectin to enzymatic cleavage of the microbial cell, reducing toxicity, accelerating tissue regeneration and the manifestation of biocidal action against pathogenic bacteria, viruses, and molds.

The task is achieved by dissolving 100 g of the drug in 300 ml. water for detoxification and polymerization of initially 0.15 ± 0.05% glutaraldehyde with 0.15 ± 0.05% alkyldimethylbenzylammonium chloride at 38-40 ° C for 2-3 days. To obtain a cream suspension in molten petroleum jelly (80%) and vegetable oil (10%) or gel for suspension. As additional components, 0.1% dimethyl sulfoxide and flavor are added. After emulsification, the cream suspension is packaged in jars, syringes or aluminum tubes. In general, 1 g of ointment, gel contains 30 mg. linkspectin. The drug retains biocidal and therapeutic properties for 3 years when stored from 0 ° C to 25 ° C.

The invention is illustrated by the following examples.

Example 1. The study of the shelf life.

The packaged cream suspension preserves the appearance and properties for 3 years when stored from 0 to 25 C.

Example 2. Determination of sensitizing (allergenic) properties of a cream suspension.

Daily single rubbing, lubrication of the surface of the nipples and udders of 28 cows and 10 goats for 7-10 days did not cause an increase in temperature, inflammation and scratching in animals. The skin at the place of rubbing the cream suspension remained elastic, and the cracks on the surface of the nipples and udder disappeared.

Example 3. The effectiveness of the treatment of cows with mastitis.

Daily single intracisternal administration to 27 cows after milking with a 3-5 ml syringe. cream-suspension in each nipple and lubrication of the skin of the udder for 3-4 days ensured the cessation of flow from the nipples and the healing of cracks on the surface of the nipples and udder.

Example 4. The effectiveness of the treatment of burn wounds in 3-4-month-old piglets.

Burn wounds were caused by application for 2-3 minutes to the shaved side surfaces of the gauze skin, soaked in 4-5% solution of phenol (carbolic acid) in 12 shaved pelvic surfaces. The size of burn wounds was 4-5 cm. Complete healing of burn wounds without purulent outflows occurred after 9-10 days with daily 2-3 times lubrication of the affected surface of the skin with a cream-suspension.

Example 5. The study of the biocidal action of an aqueous solution of linkospectin (30 mg / ml) with 0.15 ± 0.05% glutaraldehyde with 0.15 + 0.05% alkyldimethylbenzylammonium, in relation to a suspension of laboratory and freshly isolated microorganisms - staphylococci, salmonella, Escherichia coli (100 thousand in 1 ml.) IGBP, molds - Asp. niger and Asp. flavus, and causative agents of fibromatosis and myxomatosis in rabbits, plague and enteritis viruses in dogs, cat panleikemia and cattle rhinotracheitis containing 10 ³ -10 ⁵ infectious doses in 1 ml.

In this case, the initial volume and concentration of 30 mg / ml of linkospectin, glutaraldehyde and alkyldimethylbenzylammonium chloride after mixing with an equal volume of a suspension of microorganisms with MPGB decreased by half. The results obtained indicate a 100% biocidal effect of the modified polymerization and detoxification of linkospectin in relation to the above types and concentrations of microorganisms.

Claims (1)

A method of increasing the biocidal and therapeutic effect of a cream suspension with linkospectin, which consists in the detoxification and polymerization of 100 g of linkospectin in 300 ml of water with 0.15 ± 0.05% glutaraldehyde solution with 0.15 ± 0.05% alkyl dimethylbenzylammonium chloride at 38-40 ° C for 2-3 days, and then adding to the molten petroleum jelly (80%) and vegetable oil (10%) or gel for suspension, and as additional components, 0.1% dimethyl sulfoxide and flavor are added.