RU2227025C2 - Antiparasitic preparation with broad spectrum of effect - Google Patents

Abstract

FIELD: veterinary science. SUBSTANCE: invention is designated for treatment and prophylaxis of fascioliasis, nematodosis and diseases caused by gadfly larval stage in ruminant animals. Antiparasitic preparation comprises the following components, wt.-%: rafoxanide, 7.0-15.0; dimethylacetamide, 20.0-60.0; benzyl alcohol, 1.0-5.0; triethanolamine, 1.0-5.0, and polyethylene glycol, the balance. The preparation is effective against both mature and non-mature fascioles, nemathelminthes of mixed species and gadfly larval stages in ruminant animals. EFFECT: valuable properties of preparation. 1 tbl, 8 ex

Description

The invention relates to veterinary medicine, is intended for the treatment and prevention of fascioliasis, nematodoses and diseases caused by the larval stage of gadfly in ruminants.

In livestock practice, especially with grazing, cattle and sheep are often affected by both different (mixed) types of nematodes, sexually mature and immature fascioli, and larval stages of gadflies.

For the treatment of fascioliasis, the faskoverm drug is known containing closantelle as the active substance [1].

Known antiparasitic drug ursovermit, which is a 2.5% suspension of rafoxanide [2] is a prototype.

The disadvantages of the known drugs is the need for their oral administration and manifestation of the therapeutic effect only in high doses against fasciol and nematodes, as well as the lack of therapeutic effect against the larval stages of cattle and sheep gadfly.

During mass veterinary treatments with preparations requiring oral administration, as a rule, the preparations are mixed with food and assigned to a group of animals, while animals consume different amounts of food, therefore it is practically impossible to maintain the exact dosage of the drug. In this case, preparations for injectable administration are preferable, with the introduction of which it is easy to ensure exact compliance with the recommended doses.

The objective of the present invention is to expand the spectrum of antiparasitic drugs with a wide spectrum of action, by creating a drug for injection, which is highly effective against various types of nematodes, sexually and immature fascioli, and larval stages of cattle hypodermis and oestrus ovules, since practically ruminants are simultaneously infected mixed types of pathogens: fascioli, nematodes of various species, hypoderm larvae (large horned sk from), larvae of estruses (sheep).

The solution to this problem is achieved by creating a drug that contains rafoxanide as an antiparasitic active substance; as auxiliary substances, dimethylacetamide, benzyl alcohol, triethanolamine, polyethylene glycol are used in the following ratios of components, wt.%:

Rafoxanide (flucanide, ranid, MK - 990) -3'-chloro-4 '- (n-chlorophenoxy) -3-5-diiodosalicylanilide - a powder with antiphosphacy effect, melting point 175 ° С, content of organic matter - 99.4% [3].

Dimethylacetamide - a carboxylic acid amide solvent;

Benzyl alcohol - solvent, odor control, antiseptic;

Triethanolamine - a surfactant, amino alcohol;

Polyethylene glycol is a binding component in the pharmaceutical industry, it is soluble in many organic solvents.

The technical result provided by the invention is to obtain a new drug, stable during storage and having a wide spectrum of action. The drug is active against sexually mature and immature forms of fasciol, against mixed types of nematodes and larval stages of gadfly in a low dose.

The preparation according to the invention is illustrated by the following examples, which, however, do not cover, and moreover do not limit the entire scope of the claims of this invention.

Example 1. In a mixer with a capacity of 100 l, 40% by weight of dimethylacetamide is poured and heated to 45 ° C, 10% of rafoxanide, 3% of benzyl alcohol and 3% of triethanolamine are gradually added with constant stirring, while stirring until the rafoxanide is completely dissolved, then the solution is cooled and up to 100% polyethylene glycol is added.

Get the drug of the following composition, wt.%:

Rafoxanide 10.0

Dimethylacetamide 40.0

Benzyl alcohol 3.0

Triethanolamine 3.0

Polyethylene glycol rest

Example 2. The drug is obtained analogously to example 1. Use 20% by weight of dimethylacetamide, 7% rafoxanide, 1% benzyl alcohol and triethanolamine and add up to 100% polyethylene glycol.

Get the drug of the following composition, wt.%:

Rafoxanide 7.0

Dimethylacetamide 20.0

Benzyl alcohol 1.0

Triethanolamine 1.0

Polyethylene glycol rest

Example 3. The drug is obtained analogously to example 1. Use 5% by weight of rafoxanide, 5% benzyl alcohol and triethanolamine, 60% dimethylacetamide and add up to 100% polyethylene glycol.

Get the drug of the following composition, wt.%:

Rafoxanide 5.0

Dimethylacetamide 60.0

Benzyl alcohol 5.0

Triethanolamine 5.0

Polyethylene glycol rest

The antiparasitic composition, which has received the commercial name of aphasil, according to examples 1-3, is tested on ruminants (sheep, cattle, goats) against different stages of fasciol, mixed species of nematodes and gadfly larvae.

Example 4. Of the 20 goals of young cattle, spontaneously invaded by sexually mature fascioli, 4 equal groups were formed. Group I animals subcutaneously, once introduced the composition of example 1 at a dose of 1 ml / 40 kg, (2.5 mg / kg DV) - 10% solution of the drug; II-nd - the composition of example 2-1 ml / 40 kg (1.75 mg / kg DV) - 7% solution of the drug; III-th - the composition of example 3-1 ml / 40 kg - (1.25 mg / kg in terms of active ingredient, i.e. according to rafoxanide) of the animal mass - 5% solution of the drug. Young animals of group VI did not receive the drug and served as a control. When the results were taken into account by coproscopy 30 days after treatment, all animals of the control group secreted fasciol eggs, animals of the first and second groups freed from helminths and did not secrete fasciol eggs, and fasciol eggs were isolated in the third group of 2 animals.

Example 5. Of the 15 lambs grazed on a pasture unfavorable for fascioliasis, 5 equal groups were formed, three of which were administered once, subcutaneously, in July, a 10% solution of the preparation according to Example 1, in a dose, respectively; 1 ml / 40 kg (2.5 mg / kg DV), 1 ml / 30 kg (3.75 mg / kg DV), 1 ml / 20 kg (5 mg / kg DV), animals of the fourth group were asked orally once according to the instructions of ursovermit at a dose of 15 mg / kg in terms of DV, i.e. on rafoxanide, and the fifth drug did not receive and served as a control. 60 days after treatment, all the lambs were killed, opened and a complete helminthological examination of the liver and gastrointestinal tract was performed. In untreated animals, an average of 23 immature fascioli, 105 gemonkhov, 27 nematodir, 1020 trichostrongil, 5 haberthia were found. Lambs of the second and third groups were free from all types of helminths. In lambs of the first group, 4 immature fascioli, 5 gemonkhs, 6 nematodir and 29 trichostrongil were found. In lambs of the fourth group, 7 immature fascioli, 32 gemonkh, 27 trichostrongil, 11 nematodir, 2 habertium were found.

Example 6. To 50 fattening bulls grazing in a pasture unsuccessful for hypodermatosis, before putting them on a stall in October, they introduced a 10% solution of the preparation according to Example 1 at a dose of 1 ml / 40 kg, (2.5 mg / kg in DV ); 50 - at a dose of 1 ml / 50 kg (1.875 mg / kg DV); 50 1 ml / 60 kg (1.25 mg / kg in terms of DV, i.e. according to rafoxanide); 50 goals were not treated and they served as a control. Groups of animals had special labels. The result was taken into account in April of the following year. Among untreated gobies, 38 heads with gadfly nodules on the back and sides in an amount of 2 to 11 specimens were identified. The treated animals of the first two groups were healthy, and in three gobies of the third group, 2 gadfly nodules were found on the back.

Example 7. 100 sheep grazed on a pasture unsuccessful for estrosis, were introduced a 10% solution of the preparation according to example 1 at a dose of 1 ml / 20 kg (5 mg / kg DV); 100 sheep -1 ml / 40 kg (2.5 mg / kg DV); 100 ml of the drug was administered at a dose of 1 ml / 60 kg (1.25 mg / kg in terms of DV, i.e. according to rafoxanide); 50 sheep were not treated and they served as a control. When the results were taken into account, after 3 days, 3 sheep from each group were killed and when examining the nasal passages and frontal sinuses, no estrus larvae were detected, i.e. received a 100% effect from the drug in the first two groups, while 38 gadfly larvae at different stages of development were found in untreated animals. In one sheep of the third group, 3 estrus larvae were found.

Example 8. 50 goats, spontaneously infested with different species of strongilates and trichocephalus, were injected subcutaneously once with a 10% solution of the drug in a dose of 1 ml / 20 kg (5 mg / kg in DV, 50 in a dose of 1 ml / 40 kg ( 2.5 mg / kg DV; 50 goats were not given the drug and served as a control.When the results were taken into account, 10 days after treatment, they obtained 100% anti-dictiocaula and strong gastrointestinal tract effect by double coproscopy, 80% ny - against nematodir and 40% against trichocephalus in goats of group I, 80, 60 and 20%, respectively, in goats of group II. Noah group isolated eggs of different species of nematodes.

As a result of a series of experiments conducted on a large number of animals, it was found that an injectable antiparasitic drug, the active substance of which is rafoxanide (according to Example 1), exhibits new properties and the spectrum of action of antiparasitic drugs expands. The drug exhibits a therapeutic effect against sexually mature and immature fascioli, various types of nematodes at 2-3 times lower doses (2.5-5.0 mg / kg body weight according to rafoxanide) in comparison with pure rafoxanide and prototype (5-15 mg / kg). For the first time, the therapeutic effect of the claimed preparation was obtained at a dose of 1 ml / 40 kg (2.5 mg / kg in terms of DV) of body weight against the larval stages of gadflies - cattle hypoderm larvae and sheep estrus larvae.

Thus, the claimed drug allows you to achieve an unobvious result: firstly, with high efficiency against various types of nematodes, mature and immature fasciol, achieve a dose reduction of the drug in terms of the active substance (rafoxanide) by 2-3 times in comparison with the known drug- prototype, which is achieved due to the synergistic action of the components of the drug; secondly, to obtain the therapeutic effect of a drug based on rafoxanide against the larval stages of cattle and sheep gadfly, which was not known and does not follow with obviousness from the prior art.

When using the proposed drug, the death of various types of nematodes, sexually and immature fascioli, and larval stages of cattle and sheep gadfly is simultaneously achieved, which allows using one drug instead of two or three and, accordingly, reducing the number of animal veterinary treatments.

Thus, the task is solved to expand the spectrum of antiparasitic drugs with a wide spectrum of action.

Sources of information

1. Abuladze K.I., Demidov N.V., Nepoklonov A.A. Parasitology and invasive diseases of agricultural animals. - M .: Agropromizdat, 1990, p. 55.

2. Demidov N.V. Anthelmintics in veterinary medicine. - M .: Kolos, 1982, p. 184, 313-315.

3. Knunyants I.L., Vonskoy E.V. and others. Chemical encyclopedic dictionary. - M .: Soviet Encyclopedia, 1983, c. 169, 69, 598, 470.

Claims (1)

A broad-spectrum antiparasitic preparation containing rafoxanide, characterized in that it additionally contains dimethylacetamide, benzyl alcohol, triethanolamine and polyethylene glycol in the following ratio, wt.%: Rafoxanide 7.0-15.0 Dimethylacetamide 20.0-60.0 Benzyl alcohol 1.0-5.0 Triethanolamine 1.0-5.0 Polyethylene glycol rest