Anti-leucosis and anti-microbial composition

FIELD: medicine.

SUBSTANCE: invention relates to veterinary and medicine, particularly substances with cytostatic and bactericidal properties; it can be applied in pharmaceutical industry. The water-soluble composition includes, in wt %: 0.007 to 0.7 metronidazole, 0.0085 to 0.85 silver hexamethylenetetramine nitrate, 0.0284 to 2.84 sodium thiosulphate, water or physiological solution to 100.

EFFECT: obtaining of composition with cytostatic and bactericidal activity, lowered toxicity, and expanded storage time; it is inexpensive, can be prepared in the field, and moreover effective in therapy for leucosis in cattle

4 tbl, 6 ex

 

The invention relates to the field of veterinary medicine, namely to substances with cytotoxic and bactericidal activity, and can be used for the pharmaceutical industry.

Known composition for the prevention of leukemia in cattle (cattle) on the basis of derivatives of 5-intorimidazole, including as a drug metronidazole in combination with iodized salt (U.S. Pat. RU # 2212887, 2003). The daily rate of metronidazole is 1.0 g/bird., iodized salt is from 70 to 90 g/bird., while metronidazole and iodized table salt used per os (via the gastrointestinal tract) courses once a day for 30 days every 6 months.

The drug provide animals with food, but it is not suitable for intravenous injection, the treatment process them very long and not very effective. Well-known drug used mainly as a means of prevention of disease of young cattle.

Closest to the claimed solution on purpose, essential features and the achieved effect is cytotoxic and antiviral medication that contains (wt.%): hexamethylenetetramine, or imidazole, or an antipyrine - 0,007-0,70; silver nitrate - 0,0085-0,85; sodium thiosulfate - 0,0284-2,84; water or eziologicheskie solution to 100% (U.S. Pat. EN 2094048, 1997). Known from the patent No. 2094048 composition selected for the prototype.

Famous drug is quite effective in the treatment and prevention of leukemia cattle. The disadvantage of the prototype is a small storage period: in dissolved form, it is stored not more than two months. In a mixture of powders of this composition is not stored, because the main components when mixed react and there is a qualitative change in the properties of the composition. Currently, due to the presence of more efficient means hexamethylenetetramine is not widely implemented, and phenazone is deprecated dosage form and removed from production. Part of the silver salt has a relatively high toxicity.

The objective of the invention is to develop more effective compositions based on salts of silver with cytotoxic and antibacterial activity, reduced toxicity and increased shelf life.

This task is solved by the fact that according to the proposed solution anti-leukemia and anti-bacterial composition comprising a salt of silver, sodium thiosulfate and water or saline solution as the basis, instead of the inefficient contains hexamethylenetetramine as the actual beginning of metronidazole (trichopol), and instead of silver nitrate contains discotex is know salt silver - nitrate hexamine silver in the following ratio, wt.%:

metronidazole0,007-0,7
nitrate hexamine silver0,0085-0,85
sodium thiosulfate0,0284-2,84
water or salinethe rest is up to 100

Our studies showed that the storage of powders in a mixture of the components proposed composition of the fully retains its properties over 12 months. Due to this, there is a possibility of its application in various pharmaceutical forms such as solutions for injection, powders, ointments. In the treatment of leukemia injection of metronidazole is more effective than the use of per os, as in counterparts. Through the blood, it is distributed in many tissues and body fluids, in particular in bone and blood. In the treatment of leukemia property is used metronidazole easy to penetrate into the cerebrospinal fluid (up to 43% of the concentration in the blood plasma). Binding to plasma proteins is less than 20%. Up to 50-60% of metronidazole is metabolized in the liver by hydroxylation and linking with glucuronic acid, the main metabolite (2-oxymoronical) also provides the anti-Christ. protozone and antimicrobial effects. It is also important that part of the proposed composition of nitrate hexamine silver is almost 4 times less toxic than silver nitrate used in the prototype.

Specific examples.

If you run the examples used an aqueous solution of the composition, including known drugs: metronidazole, sodium thiosulfate and nitrate hexamine silver with structural formula

when various quantitative combinations of components.

Example 1. To the mixture 0,007 g of metronidazole, 0,0085 g nitrate hexamine silver, 0,0284 g sodium thiosulfate, water is added to 100, Get a clear solution, which examined the cytotoxic and antiviral activity.

Example 2. 0.07 g of metronidazole mixed with 0,284 sodium thiosulfate, type of 0.085 g of nitrate hexamine silver dissolved in 99,561 g of water. Get a transparent liquid, which examined the cytotoxic and antibacterial activity.

Example 3. 0,85 g nitrate hexamine silver mixed with 0.7 g of metronidazole, add 2,84 g of dissolved sodium thiosulfate.

The toxicity of the composition increases the toxicity of the cytotoxic drug cisplatin.

Example 4. 0.001 g of nitrate hexamine silver and 0.003 g of metronidazole mix is, add 0,0284 g of sodium thiosulfate dissolved in water. Low toxicity, with the lack of bactericidal activity.

Example 5. 0.9 g of nitrate hexamine silver mixed with 0.8 g of metronidazole and added 2.9 g of sodium thiosulfate dissolved in water. In solution noticeable residue, disappearing when heated to 40°C.

Example 6. 1.0 g of nitrate hexamine silver mixed with 0.07 g of metronidazole, add 1.1 g sodium thiosulfate dissolved in water. The composition is examined for cytotoxic and antibacterial activity.

Experimental evidence of the materiality of the declared characteristics, are given in tables.

Studies of acute toxicity of the optimal composition according to example 2 was conducted on 75 mice BALB/c mice with intraperitoneal administration of the composition in aqueous solution in the range from 20 mg/kg to 100 mg/kg (table 1). Observation of the animals was carried out within 30 days. For comparison, the selected known drugs: silver nitrate and cisplatin. The toxicity of the claimed composition is markedly lower than the toxicity of known drugs. So, at the dosage of 60 to 70 mg/kg body weight toxicity is not detected at the dose of 80 mg/kg in comparison with nitrate of silver it is below 2.5 times.

Table 2 contains the data for the study of antitumor activity of this Declaration, the act of composition and related drugs without metronidazole in CBA mice with Ehrlich carcinoma (with three times intraperitoneally). From table 2 it is seen that the use of the proposed composition causes statically significant (P<0.001) increase in 2 times the lifespan of CBA mice with Ehrlich carcinoma in comparison with control (untreated).

Assessed the antitumor cytotoxic activity of the claimed composition in comparison with cisplatine on culture leukemia cell line K-562, cultivated in the medium PMI-1640 with 15%fetal calf serum, after dyeing dye Trifanova blue after 48 h of incubation. The proposed structure has a pronounced inhibitory effect on the proliferation of leukemia (tumor) cells, static reliability of the results P<0,001, and cytotoxic activity of the composition is comparable with known drug cisplatin (table 3).

Antibacterial activity the proposed composition was determined by the method of serial dilutions of drugs in bacterial cultures at various concentrations (table 4). The results of the experiments considered after 24 h incubation at body temperature of a sick animal. From the data of table 4, it follows that the claimed composition has a pronounced cytotoxic effect on bacterial cells, causing 100%mortality at the stated concentrations (90% on the boundary of the range).

The analysis of the level of drugs, held suavitel is m, has allowed to establish that available in the patent and medical sources there are no analogues characterized by a set of characteristics is identical for all features of the claimed matter. Therefore, the claimed invention meets the condition of patentability "novelty".

Search known solutions in this and related fields in order to identify characteristics that match with the distinctive features of the prototype, not identified solutions having attributes that exactly match the distinctive features of the invention. Fame and the obvious influence of the declared distinctive signs on the achievement of the technical result is not confirmed. This allows to speak about the compliance of the claimed solution to the condition of patentability "inventive step".

Sources used

1. Pat. RU # 2212887, MKI AC 31/00. Method for the prevention and treatment of leukemia in cattle. Publ. 2003.09.27.

2. Pat. EN 2094048, MKI AC 33/38. Cytotoxic and antiviral composition. Publ. 27.10.97, the Prototype.

3. Belenky, M. elements of a quantitative evaluation of the pharmacological effect. Riga, 1963. - 130 C.

Table 1

The toxicity of the claimed composition
dose, mg/kgThe number is pitnych animals The number of dead animals,%
the inventive compositionAgNO3cisplatinthe inventive compositionAgNO3cisplatin
2055505/100%5/100%
4055505/100%5/100%
6055505/100%5/100%
805552/40%5/100%5/100%
1005555/100%5/100%5/100%

Example 2
Table 3
Cytotoxic activity of the claimed composition in comparison with cisplatine.
Activity
Type of cellThe claimed compositionCisplatin (mg/mlControl (tumor cells without drugs)
Example 1Example 620,20,02
K-562174,8+36,2284,2+39,9479,5+52,1189,5+32,4372,6+44,7677,3±54,18507,5±604

Table 4

Antibacterial activity of the claimed composition
№ p/pThe claimed composition% inhibition of growth of bacteria
StaphylococcusStreptococcusE. coli
1The composition of example 19090100
2The composition of example 2 (optimum)100100100
3The composition of example 6100100100

Anti-leukemia and anti-bacterial composition comprising a salt of silver, sodium thiosulfate and water/saline solution as a base, characterized in that it additionally contains metronidazole, as well as salts of silver nitrate hexamine silver under the following ratios, wt.%:

metronidazole0,007-0,7
nitrate hexamine silver0,0085-0,85
sodium thiosulfate0,0284-2,84
water or salinethe rest is up to 100



 

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