Topical localized isoxazoline formulation
This invention provides topical localized formulations comprising an isoxazoline compound and a pharmaceutically or veterinary acceptable liquid carrier vehicle comprising N,N-diethyl-3-methylbenzamide as a solvent and an improved method for controlling, and preventing parasite infestation in animals.
1. A topical localized formulation for the treatment of parasite infestation in animals which comprises an effective amount of at least one isoxazoline compound of the Formula (I)
wherein
R 1 is 3-CF3, and 5-C1; n is 2;
R 2 is CF 3 ;
T is
Q is X-NR 3 R 4 ;
X is C(O);
R 3 is -CH 2 -C(O)-NH-CH 2 -CF 3 ;
and R 4 is H
or
R 1 is 3-, 4-, and 5-Cl; n is 3;
R 2 is CF 3 ;
T is
Q is X-NR 3 R 4 ;
X is C(O);
Y is methyl;
R 3 is -CH 2 -C(O)-NH-CH 2 -CF 3 ;
and R 4 is H;
and a veterinary acceptable liquid carrier vehicle wherein the liquid carrier vehicle comprises N,N-diethyl-3-methylbenzamide as a solvent.
2. The topical localized formulation according to claim 1 , wherein the formulation comprises 1 to 50% N,N-diethyl-3-methylbenzamide.
3. The topical localized formulation according to claim 1 wherein the liquid carrier vehicle comprises N,N-diethyl-3-methylbenzamide as solvent and a co-solvent selected from the group consisting of dimethyl sulfoxide, acetone, dimethylacetamide, ethyl alcohol, eucalyptol, dipropylene glycol monomethyl ether, methylethyl ketone, glycofurol, ethyl-L-lactate, and a mixture of at least two of these co-solvents.
4. The topical localized formulation according to claim 3 wherein the liquid carrier vehicle comprises N,N-diethyl-3-methylbenzamide as solvent and a mixture of at least two of acetone, ethyl-L-lactate, dimethyl sulfoxide, dimethylacetamide and glycofurol.
5. The topical localized formulation according to claim 3 wherein there is a weight/weight ratio of the cosolvent/solvent in the spot-on composition and the weight/weight ratio of the cosolvent/solvent is between 4/1 and 1/5.
6. The topical localized formulation according to claim 1 , wherein the formulation further comprises an effective amount of one or more compounds selected from a macrocyclic lactone compound or an insect growth regulator compound.
7. The topical localized formulation of claim 3 , wherein the formulation further comprises an effective amount of one of more compounds selected from a macrocyclic lactone compound or an insect growth regulator compound.
8. The topical localized formulation of claim 7 , wherein the macrocyclic lactone compound is selected from ivermectin, moxidectin, milbemycin, selamectin, emamectin, latidectin and lepimectin or a salt thereof and the insect growth regulator compound is selected from fenoxycarb, lufenuron, diflubenzuron, novaluron, triflumuron, fluazuron, cyromazine, methoprene and pyriproxyfen.
9. The topical localization formulation of claim 3 , wherein the veterinary acceptable liquid carrier comprises a co-solvent of at least two of ethyl-L-lactate, dimethyl sulfoxide, dimethylacetamide and glycofurol.
10. The topical localized formulation of claim 1 , wherein
R 1 is 3-CF 3 , and 5-Cl; n is 2;
R 2 is CF 3 ;
T is
Q is X-N R 3 R 4 ;
X is C(O);
R 3 is -CH 2 -C(O)-NH-CH 2 -CF 3 ;
and R 4 is H.
11. The topical localized formulation of claim 1 , wherein
R 1 is 3-, 4-, and 5-C1; n is 3;
R 2 is CF 3;
T is
Q is X-N R 3 R 4 ;
X is C(O);
Y is methyl;
R 3 is -CH 2 -C(O)-NH-CH 2 -CF 3 ;
and R 4 is H.
12. A method for treatment of parasite infestation of an animal comprising spot-on or pour-on administration of a localized topical formulation of claim 1 .
13. The method of claim 12 wherein the veterinary acceptable liquid carrier comprises a co-solvent of at least two of acetone, ethyl-L-lactate, dimethyl sulfoxide, dimethylacetamide and glycofurol.
14. The method of claim 12 wherein the topical localized formulation comprises additionally an effective amount of a macrocyclic lactone compound and/or an insect growth regulator compound.
15. The method of claim 14 wherein the macrocyclic lactone compound is selected from ivermectin, moxidectin, milbemycin, selamectin, emamectin, latidectin and lepimectin or a salt thereof and the insect growth regulator compound is selected from fenoxycarb, lufenuron, diflubenzuron, novaluron, triflumuron, fluazuron, cyromazine, methoprene and pyriproxyfen.