Anthelmintic macrocyclic lactone compositions

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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Details

A61K 3170

Patent

active

060136367

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD OF THE INVENTION

This invention relates to compositions containing an anthelmintic chosen from the class of macrocyclic lactones including but not limited to the avermectins, ivermectin, doramectin, abamectin, milbemycin and moxidectin.


BACKGROUND

This class of anthelmintics are difficult to formulate. For example, the commercially available injectable antiparasitic agent based on an aqueous co-solvent formulation containing ivermectin, water and an organic co-solvent, has been shown to result in some precipitation of the ivermectin at the injection site, with the possibility of irritation to the animal, and possible loss of effectiveness as an anthelmintic. In pour-on formulations, water miscible formulations are diluted if there is rain after treatment.


OBJECT

It is an object of this invention to provide an improved injectable composition containing an anthelmintic, or one which will at least provide the public with a useful choice.


STATEMENT OF INVENTION

One aspect of the invention provides an injectable solution containing an anthelmintic chosen from the class of macrocyclic lactones including but not limited to the avermectins, ivermectin, doramectin, abamectin, milbemycin, and moxidectin, together with a vegetable oil and a co-solvent chosen from the group comprising alcohols having 4 or more carbon atoms.
Preferred alcohols are benzyl alcohol, ethyl benzyl alcohol, phenethyl alcohol and other aromatic monohydric alcohols.
The most preferred co-solvent is benzyl alcohol. More preferably the benzyl alcohol is present in the range of 1-30% by weight.
Preferred vegetable oils are soya bean oil, sesame oil and corn oil.
The most preferred oil is soya bean oil.
Preferably the anthelmintic is chosen from the group comprising abamectin and ivermectin.
More preferably the abamectin or ivermectin is present in the range from 0.5-5% by weight of the formulation.
Optionally, a wetting agent such as ethyl oleate may be used to assist in dissolving the anthelmintic in solution.
Optionally, oil soluble vitamins may be added.
In another aspect the invention provides a pour-on composition containing an anthelmintic chosen from the class of macrocyclic lactones including but not limited to the avermectins, ivermectin, doramectin, abamectin, milbemycin, and moxidectin, together with a vegetable oil and a co-solvent chosen from the group comprising alcohols having 4 or more carbon atoms.
Preferred alcohols are benzyl alcohol, ethyl benzyl alcohol, phenethyl alcohol and other aromatic monohydric alcohols.
The most preferred co-solvent is benzyl alcohol. More preferably the benzyl alcohol is present in the range of 1-30% by weight.
Preferred vegetable oils are soya bean oil, sesame oil and corn oil.
The most preferred oil is soya bean oil.
Preferably the anthelmintic is chosen from the group comprising abamectin and ivermectin.
More preferably the abamectin or ivermectin is present in the range from 0.5-5% by weight of the formulation.
Optionally, a wetting agent such as ethyl oleate may be used to assist in dissolving the anthelmintic in solution.
Optionally, oil soluble vitamins may be added.
In another aspect the invention provides a solution suitable for oral administration containing an anthelmintic chosen from the class of macrocyclic lactones including but not limited to the avermectins, ivermectin, doramectin, abamectin, milbemycin, and moxidectin, together with a vegetable oil and a co-solvent chosen from the group comprising alcohols having 4 or more carbon atoms.
Preferred alcohols are benzyl alcohol, ethyl benzyl alcohol, phenethyl alcohol and other aromatic monohydric alcohols.
The most preferred co-solvent is benzyl alcohol. More preferably the benzyl alcohol is present in the range of 1-30% by weight.
Preferred vegetable oils are soya bean oil, sesame oil and corn oil.
The most preferred oil is corn oil.
Preferably the anthelmintic is chosen from the group comprising abamectin and ivermectin.
More preferably the abamectin or ivermectin is present in the range from 0.1-10% by weigh

REFERENCES:
patent: 4916120 (1990-04-01), Roben et al.
patent: 5674897 (1997-10-01), Kim et al.
patent: 5756474 (1998-05-01), Furstenau
patent: 5773422 (1998-06-01), Komer

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