Spot-on pesticide composition
View Patent ↗A spot-on pesticide composition for animals, specifically mammals, including dogs and cats, which composition comprises a combination of active components, including fipronil and a pyrethroid, and optionally an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area.
1. A spot-on pesticidal composition comprising about 1% to about 20% (w/w) fipronil, about 1% to 15% (w/w) cyphenothrin, about 1% to about 20% (w/w) insect growth regulator, and about 55% to about 85% (w/w) of an organic solvent, wherein the organic solvent has a dielectric constant ranging from about 1 to 40, a boiling point less than 100° C., and a density less than the density of water selected from the group consisting of acetyltributyl citrate, fatty acid esters, diisobutyl adipate, acetone, acetonitrile, benzyl alcohol, butyl diglycol, dimethylacetamide, dimethylformamide, dipropylene glycol n-butyl ether, ethanol, isopropanol, methanol, ethylene glycol monoethyl ether, ethylene glycol monomethyl ether, diethylene glycol monoethyl ether, monomethylacetamide, dipropylene glycol monomethyl ether, liquid polyoxyethylene glycols, propylene glycol, 2-pyrrolidones, N-methylpyrrolidone, ethylene glycol, diethyl phthalate, and ethoxydiglycol, and combinations thereof.
2. The spot-on pesticidal composition of claim 1 , wherein the insect growth regulator is selected from the group consisting of bistrifluron, buprofezin, chlorfluazuron, cyromazine, diflubenzuron, flucycloxuron, flufenoxuron, hexaflumuron, lufenuron, novaluron, noviflumuron, penfluron, teflubenzuron, triflumuron, epofenonane, fenoxycarb, hydroprene, kinoprene, S-methoprene, pyriproxyfen, triprene, and combinations thereof.
3. The spot-on pesticidal composition of claim 1 , comprising about 5% to about 15% (w/w) fipronil, about 2% to about 10% (w/w) cyphenothrin, and about 2% to about 15% (w/w) insect growth regulator.
4. The spot-on pesticidal composition of claim 1 , comprising about 8% to about 10% (w/w) fipronil, about 4% to about 6% (w/w) cyphenothrin, and about 7% to about 10% (w/w) insect growth regulator.
5. The spot-on pesticidal composition of claim 4 , wherein the insect growth regulator is S-methoprene.
6. The spot-on pesticidal composition of claim 1 , comprising about 8% to about 10% (w/w) fipronil, about 4% to about 6% (w/w) cyphenothrin, and about 3% to about 5% (w/w) insect growth regulator.
7. The spot-on pesticidal composition of claim 6 , wherein the insect growth regulator is pyriproxyfen.
8. The spot-on pesticidal composition of claim 1 , wherein the organic solvent is selected from the group consisting of acetyltributyl citrate, fatty acid esters, diisobutyl adipate, acetone, acetonitrile, benzyl alcohol, butyl diglycol, dimethylacetamide, dimethylformamide, dipropylene glycol n-butyl ether, ethanol, isopropanol, methanol, ethylene glycol monoethyl ether, ethylene glycol monomethyl ether, diethylene glycol monoethyl ether, monomethylacetamide, dipropylene glycol monomethyl ether, liquid polyoxyethylene glycols, propylene glycol, 2-pyrrolidones, ethylene glycol, diethyl phthalate, ethoxydiglycol, and combinations thereof.
9. The spot-on pesticidal composition of claim 1 , wherein the organic solvent is diethylene glycol monoethyl ether.
10. The spot-on pesticidal composition of claim 1 , wherein the composition further comprises an antioxidant.
11. The spot-on pesticidal composition of claim 10 , wherein the antioxidant is present in the composition at a concentration of about 1% to about 10% (w/w).
12. The spot-on pesticidal composition of claim 10 , wherein the antioxidant is a vitamin E compound.
13. The spot-on pesticidal composition of claim 10 , wherein the antioxidant is selected from the group consisting of tocopherol acetate, tocopherol linoleate, tocopherol nicotinate, tocopherol succinate, ascorbyl tocopherol phosphate, dioleyl tocopherol methylsilanol, tocophersolan, tocopherol linoleate/oleate, and combinations thereof.
14. The spot-on pesticidal composition of claim 1 , wherein the composition provides at least 90% efficacy against insect and pest pupae for a period of at least 30 days following administration of the composition to a mammal.
15. The spot-on pesticidal composition of claim 14 , wherein the mammal comprises a dog or cat.
16. A spot-on pesticidal composition, comprising:
a. 8% to 11% (w/w) fipronil;
b. 4% to 6% (w/w) cyphenothrin;
c. 8% to 12% (w/w) S-methoprene;
d. 65% to 70% (w/w) organic solvent; and
e. 4% to 6% (w/w) antioxidant.
17. A spot-on pesticidal composition, comprising:
a. 8% to 11% (w/w) fipronil;
b. 7% to 9% (w/w) cyphenothrin;
c. 8% to 12% (w/w) S-methoprene;
d. 65% to 70% (w/w) organic solvent; and
e. 4% to 6% (w/w) antioxidant.
18. A spot-on pesticidal composition, comprising:
a. 8% to 11% (w/w) fipronil;
b. 4% to 6% (w/w) cyphenothrin;
c. 3% to 5% (w/w) pyriproxyfen;
d. 75% to 80% (w/w) organic solvent; and
e. 4% to 6% (w/w) antioxidant.
19. A spot-on pesticidal composition, comprising:
a. 8% to 11% (w/w) fipronil;
b. 7% to 9% (w/w) cyphenothrin;
c. 3% to 5% (w/w) pyriproxyfen;
d. 75% to 80% (w/w) organic solvent; and
e. 4% to 6% (w/w) antioxidant.
20. A spot-on pesticidal composition, comprising about 5% to about 15% (w/w) fipronil, about 2% to about 10% (w/w) cyphenothrin, and about 1% to about 20% (w/w) insect growth regulator.
21. A spot-on pesticidal composition, comprising:
a. 9% to 11% (w/w) fipronil;
b. 5% to 9% (w/w) cyphenothrin;
c. 3% to 5% (w/w) pyriproxyfen; and
c. 75% to 80% (w/w) diethylene glycol monoethyl ether.
22. A method of killing insect and pest pupae and adults on an animal, which method comprises administering a localized cutaneous application between the shoulders of the animal, a spot-on composition comprising about 1% to about 20% (w/w) fipronil, about 1% to 15% (w/w) cyphenothrin, about 1% to about 20% (w/w) insect growth regulator, and about 55% to about 85% (w/w) organic solvent, wherein the composition is administered in a volume sufficient to deliver a dosage of fipronil, cyphenothrin, and insect growth regulator ranging from about 0.1 mg/kg to about 40 mg/kg of animal weight, and wherein at least 90% efficacy against insect and pest pupae is achieved.
23. The method of claim 22 , wherein the application is made as a one-time treatment.
24. The method of claim 22 , wherein the application is made every six weeks.
25. The method of claim 22 , wherein the application is made every five weeks.
26. The method of claim 22 , wherein the application is made every four weeks.
27. The method of claim 22 , wherein the application is made every week.
28. The method of claim 22 , wherein the animal is a mammal.
29. The method of claim 28 , wherein the mammal comprises a dog or a cat.
30. The method of claim 22 , wherein the spot-on composition additionally comprises about 1% to about 10% (w/w) of an antioxidant.
31. The method of claim 22 , wherein at least 95% efficacy is achieved.