EA022327B1 - Injection veterinary preparation as a solution for combating animal polyinvasions and method for production thereof - Google Patents

Abstract

The invention relates to veterinary, in particular to parasitology, and concerns a medical veterinary preparation and a method for production thereof for treating and prophylaxis of helminthiasis caused by both mono- and polyinvasions of animals. The veterinary preparation is provided as a solution for combating animal polyinvasions, comprising albendazol or ricobendazol, clozantel and a solvent, wherein as a solvent a mixture of propylene glycol, polyvinylpyrrolidone, ethylenediaminetetraacetic acid (EDTA), tri(mono) ethanolamine and urea is used with the following component ratio, wt.%: albendazol or ricobendazol - 5-10; clozantel - 5-10; propylene glycol - 45-55; polyvinylpyrrolidone - 3.5-4.5; EDTA - 0.1-0.2; tri(mono)ethanolamine - 0.5-1.5; urea - 27.8-30.9.

Description

The invention relates to veterinary medicine, in particular to parasitology, and relates to medicines for the treatment and prevention of helminthiasis caused by both mono-and polyinvasions, and can be used for the prevention and treatment of diseases caused by ecto- and endoparasites of animals.

Intensive research is currently underway to develop new drugs to combat animal polyinvasions and their more effective forms. The injectable form of veterinary medicines has advantages over powder, because the use of a veterinary preparation in the form of a powder is ineffective due to its low bioavailability, the impossibility of uniform dosing when administered to animals and the inconvenience of use.

The use of derivatives of diethylaminoalkyl esters of benzyl and diphenylacetic acid and their salts of the formula

SvNb — CH — CO — O — CH — CH — Ν— CeH5

ΟθΗε II SW ₅

Κι Kg where Κι is H or alkyl;

K ₂ - H or alkyl, as a means for the prevention and treatment of helminthiases [1]. The proposed drug has a narrow spectrum of action, it is not intended for the treatment of fascioliasis.

Also known is a drug for controlling animal polyinvasion of clozalbene [2], which is a prototype of the claimed invention. The specified preparation contains, wt.%: Benzimidazole derivatives - 0.025-95, closantel - 0.5-95, solvents, or fillers, or stabilizers, preservatives - up to 100.

The description of this patent indicates that the drug can be used in the form of solutions: injectable, oral, skin, in the form of suspensions, as well as in the form of powders, boluses, tablets and pastes. The following are descriptions of known solvents, stabilizers and preservatives that can be used in the preparation of the claimed composition. However, in examples of specific performance, confirming the possibility of implementing the claimed invention, information on the full composition of the injection form of the mixture is missing.

When obtaining stable solutions of this drug, a serious problem is that the weak acid - closantel must be combined with a weak base - albendazole or ricobendazole. In practice, when trying to obtain such a solution using any of the solvents listed in [2], insoluble complexes precipitate. Those. the injection form of the drug is unstable, which leads to the impossibility of the practical production of the drug in the form of a solution when using the components listed in the above source. For this reason, the drug Klosalben is available only in powder form, which makes it difficult to use this dosage form of the drug.

The objective of the present invention is to develop an injectable form of a veterinary composition containing albendazole or ricobendazole and closantel, effective for mixed polyinvasions and stable over the shelf life, as well as a method for its preparation.

The problem is solved by a composition for combating animal polyinvasions, including as an active ingredient a mixture of closantel and albendazole or ricobendazole, propylene glycol, polyvinylpyrrolidone, ethylenediaminetetraacetic acid, three (mono) ethanolamine, urea and masene in the following ratio: or ricobendazole - 5-10, closantel - 5-10, propylene glycol - 45-55, polyvinylpyrrolidone - 3.5-5.5, ethylenediaminetetraacetic acid - 0.1 - 0.2, three (mono) ethanolamine - 0.5- 1.5, urea - 27.8-30 ,nine.

A method of obtaining the claimed composition consists in the fact that polyvinylpyrrolidone, ethylenediaminetetraacetic acid, three (mono) ethanolamine and urea are successively added to propylene glycol with stirring at a temperature of at least 120 ° C, after which closantel is added to the resulting mixture with stirring using a high-speed stirrer at least 3000 rpm at a temperature of at least 120 ° C, and after receiving a clear solution, albendazole or ricobendazole is introduced and the process is conducted at a temperature of at least 120 ° C agitating with a high speed mixer at a rate of at least 3000 rev / min to give the object product.

The resulting product, visually representing a homogeneous transparent viscous solution from light yellow to brown, is a finished veterinary composition. The solution retains its properties, appearance, pH, the content of active substances for two years. The veterinary composition in the form of a solution is used for injection.

The following are examples of specific implementation, not limiting the scope of the claimed invention.

Example 1

55 kg of propylene glycol, 5.5 kg of polyvinylpyrrolidone, 0.2 kg of ethylenediaminetetraacetic acid (EDTA), 4.5 kg of tri (mono) ethanolamine and 30.9 kg of urea are successively introduced into the reactor with stirring and heating to 120 ° C. Then in the resulting mixture at a temperature of at least 120 ° using

- 1 022327 high-speed stirrers (revolutions of at least 3000 rpm) disperse 5 kg of closantelum, and at the end of its dissolution under the above conditions, 5 kg of albendazole. A preparation of the following composition is obtained,%: albendazole - 5, closantel - 5, propylene glycol - 55, polyvinylpyrrolidone - 5.5, ethylenediaminetetraacetic acid - 0.2, triethanolamine - 1.5, urea - 30.9.

The resulting preparation has the following physicochemical characteristics: mass fraction of albendazole 0.049 g / cm ³ ; mass fraction of closantel 0.044 g / cm ³ ; density 1.0 g / cm ³ , pH 1.5.

The resulting solution is stable for two years in the original packaging.

Example 2

45 kg of propylene glycol, 3.5 kg of polyvinylpyrrolidone, 0.1 kg of EDTA, 0.5 kg of three (mono) ethanolamine and 27.8 kg of urea are successively introduced into the reaction mixture with stirring and heating to 120 ° C. Then, in the resulting mixture at a temperature of at least 120 ° C using a high-speed stirrer (rotational speed of at least 3000 rpm), 10 kg of closantel are dispersed, and at the end of its dissolution under the above conditions, 10 kg of albendazole. Get the drug of the following composition,%: albendazole - 10, closantel - 10, propylene glycol - 45, polyvinylpyrrolidone - 3.5, ethylenediaminetetraacetic acid - 0.1, triethanolamine - 0.5, urea - 27.8.

The resulting preparation has the following physicochemical characteristics: mass fraction of albendazole 0.097 g / cm ³ ; mass fraction of closantel 0.094 g / cm ³ ; density 1.1 g / cm, pH 1.9.

The resulting solution is stable for two years in the original packaging.

The resulting preparation is active against trematodes, gastrointestinal nematodes, gadfly larvae, scabies mites in cattle and small cattle.

The extensity-effectiveness (EE) of the drug was 95.8-98.3% for cattle strongylatosis, 93.3-95.4% for cattle fascioliasis, and for cattle dicroceliosis, the EE was 95.6-99.1%.

Information sources:

1. KI 2015696 C1, 1994.

2. KI 2140267 C1, 1999.

Claims (2)

CLAIM 1. An injectable veterinary agent in the form of a solution for combating the polyinvasion of an animal containing albendazole or ricobendazole, closantel and a solvent, characterized in that the solvent used is a mixture of propylene glycol, polyvinylpyrrolidone, ethylenediaminetetraacetic acid (EDTA), triamines and monoethane the following ratio of components, wt.%: albendazole or ricobendazole - 5-10, closantel - 5-10, propylene glycol - 45-55, polyvinylpyrrolidone - 3.5-5.5, EDTA - 0.1-0.2, three ( mono) ethanolamine - 0.5-1.5, urea - 27.8-30.9. 2. The method of obtaining funds according to claim 1, which consists in the fact that, with stirring at a temperature of at least 120 ° C, polyvinylpyrrolidone, EDTA, three (mono) ethanolamine and urea are successively added, after which closantel is added to the resulting mixture with stirring using a high-speed mixer at a speed of at least 3000 rpm at a temperature of at least 120 ° C, and after receiving a clear solution, albendazole or ricobendazole is introduced and the process is conducted at a temperature of at least 120 ° C with stirring using high -velocity stirrer at a speed of at least 3000 rev / min to give the object product.