Anthelmintic formulations

Details Anthelmintic formulations Anthelmintic formulations

1999-01-06

2000-12-26

Weddington, Kevin E.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514248, 514249, 514250, 514724, A61K 3170, A61K 3150, A61K 3145

Patent

active

061659878

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD OF THE INVENTION

This invention relates to solutions containing the anthelmintic, praziquantel.


BACKGROUND

In recent years the new anthelmintic compounds of the macrolide group such as avermectins and milbemycins have been drugs of choice for the treatment of internal parasites of sheep, cattle and other farm animals. These compounds offer not only the control of many internal parasites but also external parasites and therefore have become known as endecticides. Their popularity has increased because of their dual activity and because of increasing resistance to other traditional anthelmintics like levamisole and the benzimidazoles.
However, unlike the benzimidazoles, the macrolide anthelmintics need to be administered as solutions to be bio-available as in their solid form they are poorly absorbed by the animal. It has therefore been the practice to formulate these compounds by dissolving them in solvents before administration.
Some types of parasites, particularly trematodes, that are not controlled by the macrolide endecticides. Important trematodes in sheep for example are Liver Fluke (Fasciola hepatica) and Tapeworm (Monezia spp.).
Previous methods of incorporating anthelmintics that have activity against trematodes have relied on suspending a compound like praziquantel that controls Monezia spp. in an anthelmintic solution. It is more desirable to have dual formulations as solutions as this allows wider application as injectables or drenches.


OBJECT

It is an object of this invention to provide a composition containing an effective amount of praziquantel and at least one of the active anthelmintics of the macrolide group or at least one that provides the public with a useful choice.


STATEMENT OF INVENTION

In one aspect the invention comprises veterinary composition containing: the group comprising the avermectins and the milbemycins; and non-human animals.
Preferably the solvent is an ester or ester-like compound. Certain esters and similar compounds have the benefit of dissolving both praziquantel and the avermectins and milbemycins without being toxic to animals.
More preferably the solvent is selected from the group consisting of glycerol formal, ethyl lactate, benzyl alcohol, N-methyl-2-pyrrolidone and the like.
Preferably the composition is further dissolved in a carrier selected from the group consisting of monoproylene glycol, oil, water and the like.
Preferably the composition is a solution.
Preferably the macrolide anthelmintic is present in the composition in the range from 0.1-2% w/v and the praziquantel is preferably present in the composition in the range from 1-10% w/v.
Alternatively the composition is a paste containing: at least one macrolide anthelmintic selected from the group comprising the avermectins and the milbemycins, and a suitable organic solvent; and
Preferably the thickener is a solid carrier onto which the solution is absorbed and is selected from the group comprising oat meal flour, methancel, and xanthan gum.
Preferably the macrolide anthelmintic is present in the paste in the range from 0.1-2% w/v and the praziquantel is preferably present in the composition in the range from 1-10% w/v.
In another aspect the invention provides a method for the treatment of endo- and ectoparasites in a non-human animal by administering to an animal a composition as described above at the rate of 1 ml/5-20 kg of bodyweight.
Preferably the animal is treated every 6-8 weeks or more often as required.
Preferably the composition is administered to the animal as a drench, by injection or as an oral paste.


PREFERRED EMBODIMENT

These and other aspects of this invention, which should be considered in all its novel aspects will be apparent from the following examples.


EXAMPLE 1



______________________________________ Ingredient % w/v ______________________________________ Ivermectin 0.2 Praziquantel 4.0 Tween 80 10.0 Glycerol Formal 10.0 Benzyl Alcohol 4.0 Propyl Gallate 0.009 Monopropylene Glycol 40.0 Deionised water 20.0 Disodium EDT

REFERENCES:
patent: 4113867 (1978-09-01), Seubert et al.
patent: 5089480 (1992-02-01), Gibson et al.
patent: 5824653 (1998-10-01), Beuvry et al.
International Search Report, International Application No. PCT/NZ97/00096.

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