RU2375057C2 - Anthelmintic preparation for treating small cattle - Google Patents

Abstract

FIELD: veterinary science.

SUBSTANCE: invention refers to veterinary medicine, particularly to anthelmintic preparations for treating small cattle and can be used for treatment and prevention of helminthic invasions accompanied by reduced immunobiological properties. The anthelmintic preparation for treating small cattle contains albendazole, 40% Echinacea tincture, 4% methylcellulose - 100 and sorbic acid and distilled water in the ratio as follows, wt %: albendazole 2.5-5.0; 40% Echinacea tincture 9-12; 4% methylcellulose-100 20-25; sorbic acid 0.5-1.0; distilled water - the rest.

EFFECT: higher effectiveness and lower toxicity of the preparation.

2 tbl, 4 ex

Description

The technical field to which the invention relates.

The invention relates to veterinary medicine, in particular to anthelmintic drugs for the treatment of small cattle, and can be used for the treatment and prevention of helminthic invasions, accompanied by a decrease in the immunobiological properties of the body.

BACKGROUND

Known anthelmintic agent "Azinox plus", including the active ingredient praziquantel, nilverm and chlorpromazine. Fillers: lactose, calcium stearate and starch with a mass ratio of praziquantel: nilverm: chlorpromazine: lactose: calcium stearate and starch 1: 0.625-0.875: 0.0625-0.1: 3.5: 0.0375: 7.375-9.625 (cm Patent Ru No. 2100022, IPC A61K 31/00, publ. 12/27/1997 g).

The disadvantage of this tool is a decrease in the immunobiological properties of the body.

Known anthelmintic agent, including benzimidazole carbamate, while it contains an active substance complex of albendazole and copper, which is additionally included in multicapsules of cellulose acetate at a ratio of albendazole, copper sulfate and cellulose acetate 1: 1: 0.5, respectively, as the starting products for its preparation (see patent RU No. 2195280, IPC A61K 31/415, A61K 31/47, A61K 31/495, A61K 9/127, A61P 33/10, published on 12/27/2002).

The disadvantage of this tool is the low effectiveness of the treatment.

The use of albendazole with vitamin E is known (see Sidorkin V.A., Tagaeva M.S. Efficacy of albendazole preparations for oral use against Dicrocoelium Lanceatum. - Mat. Scientific Conf. "Theory and practice of controlling parasitic diseases." - Vol. 7: M. 2006).

The disadvantage of this drug is the rapid deposition of the active substance to the bottom of the bottle, which creates inconvenience in the use of the drug by specialists and the additional use of immunostimulants.

SUMMARY OF THE INVENTION

The objective of the invention is the development of an anthelmintic drug for the treatment of small cattle with high immunostimulating properties, which helps to intensify the treatment and prevention of a number of helminthic invasions, accompanied by a decrease in the immunobiological properties of the body, as well as a cheaper and more effective drug.

The technical result that can be achieved using the present invention is to increase the immunostimulating properties of the organism of small cattle, the effectiveness of the drug and low cost.

The technical result is achieved using an anthelmintic drug for the treatment of small cattle, including albendazole and distilled water, while it additionally contains tincture of echinacea 40%, a solution of methylcellulose-100 (MTs-100) 4% and sorbic acid in the following ratio in wt.%:

Albendazole 2.5-5.0 Echinacea tincture 40% 9-12 Solution MTs-100 4% 20-25 Sorbic acid 0.5-1.0 Distilled water Rest

Thus, the technical result - increasing the immunostimulating properties of the body - is achieved by the inclusion of tincture of Echinacea purpurea, which, according to the instructions for the use of medications, contains active substances that enhance the body's natural defenses and act as non-specific stimulants, increasing the number of leukocytes (granulocytes) and activating phagocytosis. That according to Daugalieva E.Kh .: “In cells protecting against helminthic invasion, cells capable of phagocytosis are of great importance. Particular importance is attached to the state of cellular enzymes and especially to the level of alkaline phosphatase as an indicator of the protective function of granulocytes. There is a natural increase in the level of this enzyme in inflammatory processes. The reaction of phagocytosis, taking into account the digesting ability of phagocytes, is a reliable test that reflects the state of the macroorganism’s immune system with various helminthiases ”(see Daugalieva E.Kh., Filippov VV. Immune status and ways of its correction for helminthiases of farm animals. M: Agropromizdat. 1991).

Aqueous solutions of meticellulose have a large binding, thickening, gelling ability. Non-toxic, resistant to various chemical agents, physiologically inert, have biological resistance (see WWW.Usolieximprom.ru).

The essence of the preparation of an anthelmintic drug for the treatment of small cattle is as follows.

Sorbic acid is used as a preservative in the food and medical industries.

A solution of methylcellulose-100 4% (MC-100) is prepared. To do this, a measured amount of distilled water is heated to 50-60 ° C, then a weighed amount of MC-100 is poured into it and mixed for uniform wetting, left to swell for 5-10 minutes, then placed in a refrigerator, which is kept for 30- 35 minutes to obtain a uniform gel.

Prepare a tincture of Echinacea 40%. To do this, take a weighed amount of Echinacea herb 200 wt.%, Pour 40% ethyl alcohol to 1 liter and insist in a dark place for 10 days.

Albendazole is placed in a container in an amount of 2.5-5.0 wt.%, Tincture of echinacea 40% in an amount of 9-12 wt.%, Triturated to obtain a homogeneous mushy mass, add a solution of MC-100 4%, while simultaneously continuing to rub the mass, add sorbic acid in an amount of 0.5-1.0 wt.%, then the resulting thick suspension is diluted with constant stirring with the rest of the water distilled to 100 wt.%.

EXAMPLES OF OBTAINING AN ANTIHELMINTH DRUG FOR TREATMENT OF SMALL CATTLE

EXAMPLE 1. To obtain an anthelmintic drug, a 0.5% solution of MC-100 is prepared, for this a measured amount of 950 wt.% Distilled water is heated to 50-60 ° C. Then, a weighed amount of MTs-100 0.5 wt.% Is poured into it and mixed for uniform wetting. Leave for swelling for 5-10 minutes, then placed in a refrigerator, which is kept for 30-35 minutes until a homogeneous gel is obtained.

Prepare a tincture of Echinacea 40%. To do this, take a weighed amount of echinacea herb, for example, 200 wt.%, Pour 40% ethyl alcohol to 1 liter and insist in a dark place for 10 days.

Albendazole is placed in a container in an amount of 2.0 wt.%, 40% echinacea tincture is poured in an amount of 0.8 wt.%, Triturated to obtain a homogeneous mushy mass, a solution of MC-100 0.5% in an amount of 2 is added , 0 wt.%. Then, while continuing to rub the mass, add sorbic acid in an amount of 0.3 wt.%. The resulting thick suspension is diluted with constant stirring with the rest of the water distilled to 100 wt.%.

The obtained anthelmintic drug turned out to be unstable, since the active substance precipitated out, after shaking the homogeneous consistency remained for 5-7 minutes, a suspension of light gray was observed at the bottom of the container.

EXAMPLE 2. Carried out analogously to example 1, but prepare a solution of MC-100 4%, while the ratio of components in wt.% Take the following:

Albendazole 2.5 Echinacea tincture 40% 9 Solution MTs-100 4% twenty Sorbic acid 0.5 Distilled water 68

The obtained anthelmintic drug turned out to be stable, for a long time 10-20 hours, the emulsion is uniform, a uniform distribution of a suspension of light gray color, a light viscous consistency was observed throughout the container.

EXAMPLE 3. Carry out analogously to example 1, but prepare a solution of MC-100 4%, while the ratio of components in wt.% Take the following:

Albendazole 5,0 Echinacea tincture 40% 12 Solution MTs-100 4% 25 Sorbic acid 1,0 Distilled water 57

The resulting anthelmintic drug turned out to be stable, for a long time 10-20 hours, the emulsion is uniform, a uniform distribution of a suspension of light gray color, light consistency was observed throughout the container.

EXAMPLE 4. Carry out analogously to example 1, but prepare a solution of MC-100 5%, while the ratio of components in wt.% Take the following:

Albendazole 5,0 Echinacea tincture 40% 12 Solution MC-100 5% 25 Sorbic acid 1,0 Distilled water 57

The obtained anthelmintic drug turned out to be stable, for a long time 10-20 hours, the emulsion is homogeneous, but does not differ in physical properties from examples 2 and 3, but in this example there is an overspending of MC-100, echinacea, sorbic acid.

Thus, the most optimal is the anthelmintic drug according to examples 2-3.

TEST RESULTS OF AN ANTIHELMINTH DRUG

FOR TREATING SMALL CATTLE

A series of experiments was conducted to study the toxicity of a 5% suspension of albendazole in MC with the addition of an immunostimulant. Initially, the experiment was conducted on 15 nonlinear white mice (males weighing 17-24 g), which were once orally administered a 5% suspension of albendazole at a dose of 740 mg / kg body weight. As a result of studies, it was found that within 7 days after the administration of the drug, not a single fatal outcome was noted. At the same time, the state of the mice throughout the entire observation time remained satisfactory.

Thus, based on the results of the experiment, LD ₅₀ (Lethal dose 50 is the dose of a substance that causes the death of half of the animals) for a 5% suspension of albendazole with an oral route of administration to nonlinear white mice exceeds 740 mg / kg.

In the second series of experiments on 30 nonlinear white mice with an average weight of 21-22 g, acute toxicity was studied with the introduction of a 5% suspension of albendazole in increasing doses, starting with a dose of 740 mg / kg body weight (Table 1). The animals were kept on a starvation diet for 18 hours before the experiment. All mice were divided into 5 groups of 6 animals each. White mice of the first group were injected with a dose of 0.5 ml through a gastric tube; the second group - 1.0 ml; the third group of 1.5 ml; animals of the fourth group received 1.0 ml twice, with an interval of 1.5 hours and the fifth group of 1.5 ml twice, with an interval of 1.5 hours.

The determination of LD ₅₀ was carried out according to the formula

E - the sum of the works of ZD;

Z is the interval between adjacent doses;

D is the arithmetic mean of the number of animals in which the presence of death was observed under the influence of every two adjacent doses;

n is the number of animals in the group;

LD ₁₀₀ - the dose causing death in all animals in the group.

Using the Kerber method, LD _{50 was} calculated from the results of the experiment.

Table 1
Determination of acute toxicity of a 5% suspension of albendazole with tincture of echinacea Dose mg / kg 740 1850 3700 5550 7400 Survived 6 3 2 one 0 Fell 0 3 four 5 6 Z 1.5 3.5 4.5 5.5 D 1110 1850 1850 1850 Zd 1665 6475 8325 10175

In the experiment, LD ₅₀ was 2960 mg / kg of mouse body weight. Therefore, a 5% suspension of albendazole with an immunostimulant belongs to low-toxic substances (hazard class IV)

The study of anthelmintic efficacy of new dosage forms

Together with the Pyatigorsk State Pharmaceutical Academy a suspension was prepared at the MC with the addition of an immunostimulant.

The aim of the study was to study the anthelmintic efficacy of an albendazole suspension. 32 heads of small cattle, spontaneously invaded by the main helminthiases of the gastrointestinal tract, were selected for the experiment. According to the principle of analogues, animals were divided into 4 groups of 8 animals each. During the experiment, the animals were in the same conditions.

The first group of animals received valbazene at a dose of 7.5 mg / kg, the second group received a suspension of albendazole at a dose of 7.5 mg / kg, the third group received a suspension of albendazole at a dose of 10.0 mg / kg, and the fourth group received a suspension of albendazole at a dose 15.0 mg / kg.

Intensivity (IE%) - the ratio of the average number of killed or released Ny parasites to the average number available before Nu treatment, expressed as a percentage, and Extensivity (EE%) - the ratio of the number of animals completely freed from invasion x ₁ to the number of treated animals in the group x ₂ multiplied by 100%, was determined by coprological studies 10 days after giving the drug.

The results are presented in table 2.

table 2
Anthelmintic activity of dosage forms of albendazole in sheep (n = 120) Preparations Dose mg / kg DV Intensity / Extensivity% Efficiency Strongilat Wildcatel Moniesius Valbazen 7.5 98.4 / 87.5 70.3 / 45 - Suspension of albendazole on MC + immunostimulant 7.5 100/100 63.0 / 20 - 10.0 100/100 79.0 / 50 100/100 15.0 100/100 100/100 100/100

An analysis of the studies showed that a suspension of albendazole in therapeutic doses has a high degree of effectiveness in the main helminthiases of the gastrointestinal tract.

The invention in comparison with the prototype and other known technical solutions has the following advantages:

- high degree of efficiency;

- simplicity of the cooking process

- resistance of the suspension;

- environmental Safety;

- immunostimulating properties;

- the cost of the suspension is lower than the proposed analogues;

- refers to low toxic compounds (hazard class IV).

Claims (1)

Anthelmintic drug for treating small cattle, including albendazole and distilled water, characterized in that it additionally contains tincture of Echinacea 40%, a solution of methylcellulose-100 4% and sorbic acid in the following ratio, wt.%:
Albendazole 2.5-5.0 Echinacea tincture 40% 9-12 The solution of methyl cellulose-100 4% 20-25 Sorbic acid 0.5-1.0 Distilled water rest