Method of producing antimicrobial and antitumor therapeutic agent

 

(57) Abstract:

The invention relates to medicine and veterinary medicine. Mix polyvinylpyrrolidone in the amount of 60-99 wt.% and triode alkylbenzenes General formula

< / BR>
where R1and R3= alk;

R2= alk or H,

The mixture is dissolved in an organic solvent to dissolve the components. Then the solvent is evaporated and the resulting product is ground to a powder. The method allows to increase the stability of the injection solution remedies. 1 C.p. f-crystals, 3 tables.

The invention relates to methods for therapeutic compositions, in particular, to contain organic active ingredients that can be used as antimicrobial and anticancer drugs for the treatment of humans and animals.

A method of obtaining compounds having antimicrobial and antitumor action of antibiotics, which consists in the production of these substances by microorganisms, followed by separation from biomass (Chemistry of antibiotics., M., Academy of Sciences of the USSR, 1961, 2 h, c. 675).

However, the known method requires sophisticated equipment multicomponent media, quickly to the invention analogous to the same destination on essential features, adopted for the prototype, is a method for antimicrobial treatment drug, which is mixed polyvinylpyrrolidone (Pharmacopeia 42-1194-78), for example, triiodide 1,3-diethylbenzamide (TU 2492-002-02825526-97) and autoclave at a temperature of 100-150oC and a pressure of 1-1,5 ATM. for 0.5-1.5 hours, Get crystalline powder brick odourless, which is Packed in sealed containers (Patent RF N 2033164, IPC6A 61 K 33/18// (A 61 K 33/18/, 31: 00, 31:79, 1992).

However, a solution of the product obtained in a known manner, not durable, is formed by dissolving a small amount of fine-grained sediment of the black color, which can lead to undesirable effects when used as a therapeutic agent. The disadvantages of the prototype are high energy and complex equipment.

The objective of the invention is to improve the quality and effectiveness as a therapeutic agent, the resulting product is antimicrobial and antitumor compositions, optimization and reduction of the technological process of its receipt.

The technical result, which can be obtained by carrying out the invention consists in the>

The essence of the proposed method of producing antimicrobial and antitumor therapeutic composition, which is mixed polyvinylpyrrolidone, 60-99 wt.%, iodine-containing substance, is that the mixture is dissolved in an organic solvent to dissolve the components, and then the solvent is evaporated, and the resulting product is ground to powder.

As the iodine-containing substance used triiodide 1,2,3-dialkylanilines, 1-40 wt.%, the General formula

< / BR>
where R1, R2, R3= alk, H.

The use of organic solvent for dissolving a mixture of polyvinylpyrrolidone and iodine-containing substances, for example, triiodide 1,2,3-trialkylamines, in the present method improves the stability of injection solution of the product obtained by the above method, and allows you to enter in the human body (animal) active iodine in doses greater than 0.34 g/kg of body weight parenterally, that is qualitatively new, because so far intravenous dose of active iodine 0.001 g/kg body weight was subconsiously (I. E. the Brain. Pharmacology. - M.: Kolos, 1969, S. 282).

In the prior art have not identified a technical solution that W is of the claimed invention, therefore, it corresponds to a condition of patentability "novelty."

The invention meets the condition of "inventive step", as it is for professionals is not obvious from the prior art.

The inventive method of producing antimicrobial and antitumor therapeutic compositions may be implemented, for example, as follows. In a glass bottle - glass 1 liter mix 200 g of polyvinylpyrrolidone with 50 g of triiodide 1,3-diethylbenzamide. The resulting mixture was dissolved in 250 ml of ethyl alcohol 95othen the solution is evaporated, and the resulting product is ground in a mill to a powder.

The achievement of the technical result is proved as follows. For the use of therapeutic compositions obtained by the present method, when parenteral administration is prepared solution of dry powdered drug in saline or water, or glucose solution intended for injection. The specified solution can be administered intramuscularly, intravenously, intraperitoneally, and can also be used for oral administration (therapeutic dose of 0.1-5 mg/kg body weight), as the solution dried minced drugs is so

Antitumor activity of the composition obtained by the present method, was studied in experiments on mice-the first generation hybrids BDFI with melanoma B-16. Melanoma were vaccinated subcutaneously with 10% suspension of tumor cells. In our experiments we used mice weighing 20-25 g (with approximately equal weight for each group at the age of 1.5-2 months). The number of animals in the control was 8-9, the number of mice in experimental groups 6-7.

Efficacy criterion was the percentage increase of life span (UPI) mice and the percentage of inhibition of the tumor (SRW) relative to the untreated control. Active in tumor was considered to be drugs, increasing life expectancy by 25% and inhibiting tumor growth by 50% (table. 1, 2).

When determining in vitro antimicrobial activity obtained by the claimed method of compositions containing polyvinylpyrrolidone 80%, triiodide 1,2,3-dialkylanilines 20%, used the Museum strains of microorganisms: Staphylococcus aureus-209p, Escherichia coli-88, Candida albicans-674 and field strains isolated from sick animals: Clostridium perfringens, Pseudomonas aeruginosa, Salmonella typhi suis.

The results showed that all tested strains of micro-organisms sensitive to the tested tx2">

1. Method of producing antimicrobial and antitumor therapeutic agent, characterized in that mix of 60 to 99 wt.% polyvinylpyrrolidone with 1 to 40 wt.% triiodide alkylbenzenes General formula

< / BR>
where R1and R3- alk;

R2- alk or H,

the mixture is dissolved in an organic solvent to dissolve the components, and then the solvent is evaporated and the resulting product is ground to powder.

2. The method according to p. 1, characterized in that the organic solvent used ethanol.

 

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