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Endoparasiticial composition

A technology for endoparasites and compositions, applied in the field of endoparasite-killing compositions, can solve problems such as inability to control roundworms, hookworms, whipworms and the like

Inactive Publication Date: 2004-03-24
BAYER IP GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these studies also showed that ivermectin, even at high doses for several days, was ineffective against hookworm and whipworm infections in patients (see Otteson & Campbell, Journal of Antimicrobial Chemotherapy, vol. 34 , 1994, pp.195-203)
[0015] These reasons clearly indicate that avermectins from macrolides, 22,23-dihydrovermectin B1 (isovermectin) and milbemycin, whether alone or in combination with intestinal The combination of insecticides has not yet been able to simultaneously prevent roundworms, hookworms and whipworms in the gastrointestinal tract of dogs and cats at low doses

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment A

[0169] In vivo nematode test

[0170] Nematode Nematospiroides dubius in mice

[0171] Mice were experimentally infected with the nematode Nemotospiroides dubius. The method of infection was oral administration of 60 filamentous larvae of Nematospiroides dubius.

[0172] After the incubation period, the active substance in suspension was administered orally on the 12th day after infection.

[0173] Activity assay:

[0174] Mice were selected on day 20 post-infection. Count parasites in mouse duodenum using a press. The dose-treated group was successful relative to the no-dose control group.

[0175] Tables A and B below show the effect of the conjugates on the nematode Nematospiroides dubius in mice.

[0176] Active substance and dosage [mg / kg]

[0177] Active substance and dosage

Embodiment B

[0179] In vivo nematode test

[0180] Nematode Heterakis spumosa in mice

[0181] Mice were experimentally infected with the Heterakis spumosa nematode. The method is to take 90 capsules of fertilized eggs of Heterakis spumosa orally.

[0182] After the incubation period, the active substance in suspension was administered orally on day 46 after infection.

[0183] Activity assay:

[0184] Mice were selected on day 59 post-infection. Microscopic enumeration of parasites in mouse colon and cecum. The dose-treated group was successful relative to the no-dose control group.

[0185]Tables C and D below show the effect of the conjugates on the Heterakis spumosa in mice.

[0186] Active substance and dosage [mg / kg]

[0187] Active substance and dosage [mg / kg]

Embodiment C

[0189] In vivo nematode test

[0190] Ancylostoma caninum in dogs

[0191] Small game puppies were experimentally infested with Ancylostoma caninum. The dosage is 250 L 3 larva.

[0192] After the incubation period, when the adult worms had reached the gastrointestinal tract of the dogs, the dogs were given orally a capsule of the pure active compound tested.

[0193] Drug efficacy determination is carried out according to the following two methods:

[0194] 1. Enumeration of eggs in dog feces before and after treatment

[0195] 2. Use the following formula to calculate the percentage efficiency of the critical test

[0196]

[0197] Table E shows the effect of the conjugates against the hookworm Ancylostoma caninum in dogs.

[0198] Active substance and dosage [mg / kg]

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PUM

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Abstract

The present invention relates to mixtures of avermectines, 22,23-dihydroavermectines B1 (ivermectines) and milbemycines from the macrocyclic lactone class in combination with cyclic depsipeptides, possibly in the presence of praciquantel or epsiprantel, to enhance the endoparasticidal action in endoparasticidal agents.

Description

technical field [0001] The present invention relates to avermectin, 22,23-dihydro avermectin B, from the class of macrolides conjugated to a cyclic depsi peptide 1 A mixture of (vermectin) and milbemycin which enhances the insecticidal action of an endoparasiticidal composition when optionally ciclopraziquantel or exetel is present. Background technique [0002] In most cases, gastrointestinal nematode infections in dogs are caused by three families of nematodes, namely Ascaridae, Anticostomidae and Trichuridae. For cats, mainly two types of nematodes distributed worldwide are Ascaridaceae and Anticostomataceae. Nematodes pass through a series of developmental stages in various tissues of the host body, culminating in overt infection in the gastrointestinal tract. In the course of overt or pre-overt infections, roundworm, hookworm and whipworm parasitic diseases cause a lot of trouble, especially in young developing dogs, cats and humans. Therefore, both therapeutic and p...

Claims

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Application Information

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IPC IPC(8): C07D273/00A61K31/395A61K38/15A61P33/00A61P33/10C07D493/22
CPCA61K38/15A61P33/00A61P33/10A61K31/70A61K31/55A61K31/495A61K2300/00
Inventor N·门克A·哈德尔P·耶斯克B·赫尔帕
Owner BAYER IP GMBH
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