RU2287332C2 - Preparation for preventing and treating helmintiases in animals - Google Patents

Abstract

FIELD: veterinary science.

SUBSTANCE: the suggested preparation for preventing and treating helminthiases in animals contains the compound out avermectines' group, pyrantel or its salt, praziquantel and a target additive at the following ratio of ingredients, weight%: compound out of avermectines' group:pyrantel or its salt:praziquantel:target additive=1.2:3.0:1.0:6.0. The innovation provides increased resistance to repeated infection in animals.

EFFECT: higher degree of prophylaxis and therapy.

3 cl, 12 ex, 2 tbl

Description

The invention relates to the field of veterinary medicine and can be used for the prevention and treatment of animal helminthiases.

There are known preparations containing an avermectin complex as an active substance (AI), and drugs that are chemically modified members of the avermectin family, obtained on the basis of the soil fungus Streptomyces avermitilis (abictin, avertin, aversect-2, bimec, bimectin, dectomax, duotin, ivermag, Ivermek, Iversect, Ivertin, Novomek), which are comprehensively studied and widely used in the fight against helminths [1, 2, 3].

The active substance ivermectin, obtained by fermentation of the fungus Streptomyces avermitilis, at a dose of 0.2 mg / kg subcutaneously once, completely prevents microfilariemia in dogs spontaneously invaded by dirofilaria [4].

However, the disadvantages of preparations containing avermectins or ivermectin as a DV are the high content of DV (1%) in the finished form and, accordingly, in a therapeutic dose of 20-30 mg per 100 kg of animal body weight [5], as well as the fact that they are inconvenient for use by small pets, such as small dogs and cats, due to difficulty in dosing. When using ivermectin, care must be taken, since it has a hepatotoxic effect. It was established that dogs of the Collie, Border Collie, Bobteil, Shelty breeds are especially sensitive to the action of ivermectin. The effect of ivermectin on the central nervous system of dogs was noted; in bracheocephalus (short-faced), the drug passes through the blood-brain barrier.

The closest analogue is a preparation containing avermectin and pyrantel or its salt and the target supplement [6].

However, increased doses of this drug can cause depression, tremor, ataxia, coma, and death. In addition, this drug provides animal resistance to reinfestation over a very short period of time.

The present invention is the development of a highly effective drug for the prevention and treatment of animal helminthiasis, which allows to increase the resistance of animals to reinfestation.

The problem is solved due to the fact that the drug for the prevention and treatment of animal helminthiasis, containing a compound from the group of avermectins, pyrantel or its salt and the target additive, according to the invention additionally contains praziquantel in the following ratio of ingredients, parts by weight: compound from the group of avermectins: pyrantel or its salt: praziquantel: target additive = 1.2: 3.0: 1.0: 6.0.

As a compound from the group of avermectins, the preparation may contain ivermectin, or abamectin, or doramectin, or moxidectin.

The preparation as a pyrantel salt may contain pyrantel pamoate, or pyrantel tartrate, or pyrantel embonate, or pyrantel hydrochloride.

As a target additive, the preparation contains a mixture consisting of ascorbic acid, sodium bicarbonate, starch, sugar, aerosil, talc, sodium lauryl sulfate and polyvinylpyrrolidone.

The technical result provided by the invention is to increase the resistance of animals to reinfestation.

The drug is given the name: DIRONET.

The drug is obtained by mixing or dissolving the components, and then granules, tablets, suspension, spot on or pur on are made.

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

Example 1

In the unit of the German company Glatt with a capacity of 100 kg, all the ingredients are poured in the following amount (in wt.%):

Abamectin 10.7 Pyrantel tartrate 26.8 Praziquantel 8.9 Vitamin C 6.3 Bicarbonate of soda 4,5 Starch 13,4 Sugar 13,4 Aerosil 1.7 Talc 3.6 Sodium lauryl sulfate 1.8 Polyvinylpyrrolidone Up to 100

As follows from the above example, the target additive contains ascorbic acid, sodium bicarbonate, starch, sugar, aerosil, talc, sodium lauryl sulfate and its content in the preparation is 53.6 wt.%.

The content of the components in the target additive is respectively (in wt.%):

Vitamin C 11.75 Bicarbonate of soda 8.4 Starch 25.0 Sugar 25.0 Aerosil 3.17 Talc 6.72 Sodium lauryl sulfate 3.36 Polyvinylpyrrolidone Up to 100

Thus in wt. parts of the composition of the drug is as follows (if we take the content of praziquantel for 1 wt.h.):

Compound from the group of avermectins: pyrantel or its salt: praziquantel: target additive = 1.2: 3.0: 1.0: 6.0.

The production of the drug is carried out in four stages:

1. The confusion.

2. Moisturizing.

3. Granulation.

4. Drying.

The mixing of the ingredients is carried out under pressure at a temperature of 65-75 ° C. Humidification and granulation of the drug is carried out in the unit at a temperature of 35-40 ° C using PVP, after granulation in the same unit, drying is carried out for 1 hour at a temperature of 70-80 ° C under pressure.

Example 2. Similar to example one, only add ivermectin, pyrantel embonate and praziquantel, in the following ratio of components (in wt.%):

Ivermectin 10.7 Pyrantel embonate 26.8 Praziquantel 8.9 Vitamin C 6.3 Bicarbonate of soda 4,5 Starch 13,4 Sugar 13,4 Aerosil 1.7 Talc 3.6 Sodium lauryl sulfate 1.8 Polyvinylpyrrolidone Up to 100

Example 3

Similar to the first example, only the drug contains doramectin, pyrantel hydrochloride and praziquantel, in the following ratio of components (in wt.%):

Doramectin 10.7 Pyrantel hydrochloride 26.8 Praziquantel 8.9 Vitamin C 6.3 Bicarbonate of soda 4,5 Starch 13,4 Sugar 13,4 Aerosil 1.7 Talc 3.6 Sodium lauryl sulfate 1.8 Polyvinylpyrrolidone Up to 100

Example 4

Similar to the first example, only the drug contains moxidectin, pyrantel pamoate and praziquantel, in the following ratio of components (in wt.%):

Moxidectin 10.7 Pyrantel embonate 26.8 Praziquantel 8.9 Vitamin C 6.3 Bicarbonate of soda 4,5 Starch 13,4 Sugar 13,4 Aerosil 1.7 Talc 3.6 Sodium lauryl sulfate 1.8 Polyvinylpyrrolidone Up to 100

Example 5

Similar to the first example, only ivermectin, pyrantel pamoate and praziquantel are added, in the following ratio of components (in wt.%):

Ivermectin 10.7 Pyrantel Pamoat 26.8 Praziquantel 8.9 Vitamin C 6.3 Bicarbonate of soda 4,5 Starch 13,4 Sugar 13,4 Aerosil 1.7 Talc 3.6 Sodium lauryl sulfate 1.8 Polyvinylpyrrolidone Up to 100

Example 6. Similar to example one, only add avermectin, pyrantel pamoate and praziquantel, in the following ratio of components (in wt.%):

Avermectin 10.7 Pyrantel Pamoat 26.8 Praziquantel 8.9 Vitamin C 6.3 Bicarbonate of soda 4,5 Starch 13,4 Sugar 13,4 Aerosil 1.7 Talc 3.6 Sodium lauryl sulfate 1.8

Examples characterizing the anthelmintic effectiveness of the drug.

Example 7

Combined therapy using preparative form (suspension) as active ingredients ivermectin, pyrantel pamoate and praziquantel, as well as a filler, solvent and stabilizer was performed on 9 dogs spontaneously invaded by Dirofilaria repens with an intensity of 232.3 ± 10.4 microfilaria in 20 mm ³ blood (table 1). Blood samples were examined 20, 30, 40, 45, 50, and 60 days after giving the drug at a dose of 6 μg / kg orally based on ivermectin. Studies have shown 100% extensibility (EE) of the drug. For the first time, single instances of microfilariae were found in the blood of animals after 45 days.

EE at 45 days was 98.8% after giving the drug at an intensity of 3.9 ± 0.6 ind. microfilariae in 20 mm ³ blood. The drug has microfilaricidal action for 45 days.

Thus, the proposed drug has a detrimental effect on dirofilariasis and can be used against microfilaria in the blood of dogs, taking into account the persistence of anthelmintic action with an interval of 6 weeks during the period of activity of the intermediate host - mosquitoes.

Table 1.
The effectiveness of the use of the drug Dironet in dog dirofilariasis A drug Number of animals The number of microfilariae in 20 mm ³ blood Efficiency% before treatment after treatment Dironet (ivermectin + pyrantel + praziquantel) 9 232.3 ± 10.4 0 one hundred Ivermectin (base drug) 9 229.6 ± 9.7 2.4 ± 0.5 99.06 Control group 9 231.2 ± 9.8 236.6 ± 9.9 -

Example 8

The preparative form of the drug dironet in the form of tablets containing ivermectin at a dose of 6 μg / kg, pyrantel pamoate and praziquantel (prepared in accordance with Example 5) as the active ingredients was used once, individually, in the morning feeding in a dose 1 tablet per 10 kg of animal weight, experimentally invaded by dirofilariae. The drug showed 100% effectiveness in dirofilariasis (table 2).

Table 2.
The effectiveness of the drug Dironet with dirofilariasis. A drug Number of animals The number of microfilariae in 20 mm ³ blood Efficiency% before treatment after treatment Dironet (ivermectin + pyrantel + praziquantel) 7 153 ± 7.6 0 one hundred Ivermectin (base drug) 7 152 ± 9.7 3.0 ± 0.5 98.02 Control group 7 154 ± 8.2 157 ± 7.8
-

Example 9

The preparation in the form of tablets (prepared in accordance with example 6) containing avermectin, pyrantel and praziquantel, based on praziquantel 50 mg, was used in the treatment of dogs at a dose of 1 tablet per 10 kg of animal weight, once, in which Echinococcus tape helminths were detected multilocularis, Mesocestodes spp., as well as microfilariae and adult dirofilaria Dirofilaria immitis. The treatment efficiency was 99.8% for dirofilariasis and 100% for cestodoses.

Example 10

The preparation (prepared in accordance with Example 5) in the form of tablets containing ivermectin (based on ivermectin 0.06 mg per tablet), pyrantel pamoate and praziquantel was used in dogs experimentally infested with dirofilaria and nematodes. The drug was administered once at a dose of 1 tab. per 10 kg of animal body weight. The treatment efficiency was 99.9%.

Example 11

The drug in the form of tablets containing ivermectin, pyrantel pamoate, praziquantel (see example 5) was used for dogs of the experimental groups in the spring-summer-autumn period in zones endemic for dirofilariasis: once before the summer of mosquitoes (March-April), then every month for the entire period from April to October, and the last time in a season - 1 month after the end of the mosquito summer (October-November). Dogs treated with the drug were not infected with dirofilariae compared with control animals.

Example 12

Dogs of the 1st group (5 goals) invaded by microfilariae dirofilaria (Stavropol) were administered the drug dironet (as in example 2) at a dose of 1 tablet per 10 kg of live weight. When blood samples from dogs of this group were examined on days 7, 14, 24, 36, no larvae of dirofilaria were found, indicating a high therapeutic efficacy of dironet in dogs dirofilariasis.

Dogs of the second group (5 goals), microfilariae infested with dirofilaria (Mikhailovsk) were given a dose of 1 tablet per 10 kg of live weight: the first time was June 6, 2005; the second time is July 1; the third time is August 1 and the fourth time is August 31. Blood for the presence of microfilariae was examined every 10-15 days (June 20, July 1 and 14, August 1, 16 and 31, September 15 and 30) - no dirofilaria larvae were found in any sample, which confirms the high preventive effect of dironet.

Due to the carefully selected composition of active substances and the target additive, the drug ensures the resistance of animals to re-infection for 7-8 months.

Thus, a highly effective drug was obtained, which allows to increase the resistance of animals to re-infection.

Information sources

1. Klenova I.F., Maltsev K.L., Yaremenko N.A., Arkhipov I.A. Veterinary drugs in Russia. M .: Selkhozizdat, 2004.V.1. S.367-384.

2. Vitebsky E.L., Revvo A.V., Trefilov A.A. Handbook of imported veterinary drugs. M .: Kolos, 1998.S. 140.

3. Mater. scientific production confer. on current issues of veterinary medicine and livestock. Kazan, 2001. Part 1. S.53-55.

4. Sudermann M.T., Craig T.M. Efficacy ofivermectictin against Dirofilaria immitis microfilariae in naturally infected dogs // Amer. J. Vet.Res. - V. 45, No. 5. - P.1031-1032.

5. Patent RU 2067861 C1, 10.20.1996.

6. Patent GB 2221621 A, 08.19.1992.

Claims (4)

1. A preparation for the prevention and treatment of animal helminthiasis, containing a compound from the group of avermectins, pyrantel or its salt and a target additive, characterized in that it additionally contains praziquantel in the following ratio of ingredients, parts by weight: compound from the group of avermectins: pyrantel or its salt : praziquantel: target additive = 1.2: 3.0: 1.0: 6.0. 2. The drug according to claim 1, characterized in that as a compound from the group of avermectins contains ivermectin, or abamectin, or doramectin, or moxidectin. 3. The drug according to claim 1, characterized in that the salt of the pyrantel contains pyrantel pamoate, or pyrantel tartrate, or pyrantel embonate, or pyrantel hydrochloride. 4. The drug according to claim 1, characterized in that as the target additive use a mixture containing, wt.%: Vitamin C 11.75 Bicarbonate of soda 8.4 Starch 25.0 Sugar 25.0 Aerosil 3.17 Talc 6.72 Sodium lauryl sulfate 3.36 Polyvinylpyrrolidone Up to 100