ANTIHELMINTIC PASTE
The present invention is concerned with an anthelmintic paste in form of an aqueous suspension, comprising a veterinarily effective amount each of praziquantel and a macrocyclic lactone selected from avermectins, milbemycins and derivatives thereof; a cyclodextrin; a thickener; and water. The suspension formulations of the present invention are useful for controlling endoparasites in warm-blooded animals such as companion animals.
1 - 16 . (canceled)
17 . An anthelmintic paste in form of an aqueous suspension, comprising
a veterinarily effective amount of praziquantel;
a macrocyclic lactone selected from avermectins, milbemycins and derivatives thereof;
a cyclodextrin;
a thickener; and
water.
18 . The paste according to claim 17 , wherein the macrocyclic lactone is of formula
wherein X is —C(H)(OH)—; —C(O)—; or —C(═N—OH)—; Y is —C(H 2 )—; ═C(H)—; —C(H)(OH)—; or —C(═N—OCH 3 )—; R 1 is hydrogen or one of radicals
R 4 is hydroxyl, —NH—CH 3 or —NH—OCH 3 ; and R 2 is hydrogen, —CH 3 , —C 2 H 5 , —CH(CH 3 ) 2 , —CH(CH 3 )—C 2 H 5 , —C(CH 3 )═CH—CH(CH 3 ) 2 or cyclohexyl; and if the bond between atoms 22 and 23 represents a double bond the carbon atom in 23-position is unsubstituted so that Y is ═C(H)—, or if the bond between atoms 22 and 23 is a single bond the carbon atom in 23-position is unsubstituted or substituted by hydroxy or by the group ═N—O—CH 3 so that Y is —C(H 2 )—; —C(H)(OH)—; or —C(═N—OCH 3 )—; in free form or in the form of a physiologically acceptable salt.
19 . A paste according to claim 17 , wherein the macrocyclic lactone is ivermectin or milbemycin oxime.
20 . A paste according to claim 17 , comprising
0.5 to 20% by weight of praziquantel;
0.1 to 8% by weight of a macrocyclic lactone;
0.5 to 40% by weight of a cyclodextrin;
0.1 to 10% by weight of a thickener; and
ad 100% by weight water.
21 . A paste according to claim 17 , comprising
2.0 to 7.5% by weight of praziquantel;
1.0 to 2.5% by weight of a macrocyclic lactone,
2.0 to 7.5% by weight of a cyclodextrin;
1.0 to 5.0% by weight of a thickener; and
ad 100% by weight water.
22 . A paste according to claim 21 , wherein the macrocyclic lactone is milbemycin oxime.
23 . A paste according to claim 17 , comprising one or more additional components selected from the group consisting of humectants, preservatives, pH-adjusting agents, colors and flavors.
24 . A paste according to claim 17 , comprising a water content of ≧50% by weight, based on the entire formulation.
25 . A paste according to claim 24 , comprising a water content of ≧60% by weight, based on the entire formulation.
26 . A paste according to claim 17 , which is devoid of oils, polyglycols, glycol ethers, glycerol formal and surfactants.
27 . A paste according to claim 18 , consisting of
1.0 to 10% by weight of praziquantel;
0.5 to 5% by weight of milbemycin oxime;
1.0 to 20% by weight of a cyclodextrin;
0.5 to 7.5% by weight of thickeners;
1.0 to 10% by weight of humectants;
0.5 to 5% by weight of preservatives;
2.5 to 20% by weight of flavors;
0 to 5.0% by weight colors; and
ad 100% by weightwater and acid.
28 . A paste according to claim 17 , wherein the paste has a specific gravity from 1.05 to 1.15.
29 . A paste according to claim 17 , wherein the paste is thixotropic.
30 . Process for the manufacture of an anthelmintic paste according to claim 17 , comprising
(i) providing the water and optionally further ingredients which are water-soluble,
(ii) adding the cyclodextrin and disperse and/or partly dissolve it in the water,
(iii) adding the praziquantel and disperse it in the water/cyclodextrin mixture,
(iv) dispersing the macrocyclic lactone, optional further ingredients and a thickener consecutively, and
(v) stirring the dispersion until a homogeneous paste is formed.
31 . A method of controlling endoparasites in a warm-blooded animal, which comprises administering an anthelmintic paste according to claim 17 orally to the warm-blooded animal.
32 . A method according to claim 31 , wherein the warm-blooded animal is a dog or cat.