ANTIPARASITIC FORMULATIONS
Fipronil formulations and fipronil/S-methoprene co-formulations are provided herein. These formulations optionally contain one or more additional active ingredient(s). The formulations comprise an organic solvent, an alcohol co-solvent, and one or more antioxidants and without any crystallization inhibitor. The formulations provided herein are antiparasitic, and can be used, for example, to combat dog and cat parasites, such as, fleas and ticks.
1 . A parasiticidal spot-on formulation comprising
fipronil or a veterinary acceptable salt thereof, which is present from about 9% to about 11% by weight of the formulation;
at least one C 1 -C 6 alcohol co-solvent, wherein the total amount of the at least one C 1 -C 6 alcohol co-solvent is up to about 5% by weight of the formulation;
one or more antioxidants, wherein the total amount of the one or more antioxidants is about 0.005% to about 1.0% by weight of the formulation;
at least one organic solvent which is one or more glycol ethers selected from the group consisting of diethylene glycol monoethyl ether, ethylene glycol monoethyl ether, dipropylene glycol n-butyl ether, dipropylene glycol monomethyl ether, and combinations thereof, wherein the total amount of the at least one organic solvent makes up the balance of the formulation; and
the formulation does not contain a surfactant or a crystallization inhibitor.
2 . The formulation of claim 1 , wherein fipronil or a veterinary acceptable salt thereof is present at about 9.8% w/w of the formulation.
3 . The formulation of claim 1 , wherein the at least one C 1 -C 6 alcohol co-solvent is selected from the group consisting of ethanol, propanol, isopropanol, and a combination thereof.
4 . The formulation of claim 1 , wherein the at least one C 1 -C 6 alcohol co-solvent is present from about 3% to about 5% w/w of the formulation.
5 . The formulation of claim 1 , wherein the at least one C 1 -C 6 alcohol co-solvent is present at about 5% w/w of the formulation.
6 . The formulation of claim 1 , wherein the at least one C 1 -C 6 alcohol co-solvent is ethanol, and is present at about 5% w/w of the formulation.
7 . The formulation of claim 1 , wherein the at least one C 1 -C 6 alcohol co-solvent is isopropanol, and is present at about 5% w/w of the formulation.
8 . The formulation of claim 1 , wherein the one or more antioxidants are selected from the group consists of butylated hydroxylanisole (BHA), butylated hydroxyltoluene (BHT), and α-Tocopherol.
9 . The formulation of claim 1 , wherein the one or more antioxidants are butylated hydroxylanisole (BHA) and butylated hydroxyltoluene (BHT).
10 . The formulation of claim 9 , wherein BHA is present at about 0.02% w/w and BHT is present at about 0.01% w/w of the formulation.
11 . The formulation of claim 1 , wherein the one or more antioxidants are butylated hydroxylanisole (BHA), butylated hydroxyltoluene (BHT), and α-Tocopherol.
12 . The formulation of claim 11 , wherein BHA is present at about 0.02% w/w, BHT is present at about 0.01% w/w, and α-Tocopherol is present at about 0.01% w/w of the formulation.
13 . The formulation of claim 1 , wherein the at least one organic solvent is diethylene glycol monoethyl ether.
14 . The formulation of claim 1 , wherein the at least one organic solvent is present from about 76% to about 90% w/w of the formulation.
15 . The formulation of claim 13 , wherein diethylene glycol monoethyl ether is present from about 76% to about 86% of the formulation.
16 . The formulation of claim 1 , further comprising S-methoprene, or a veterinary acceptable salt thereof.
17 . The formulation of claim 16 , wherein S-methoprene is present at about 8.8% w/w of the formulation.
18 . The formulation of claim 1 , which comprises
about 9.8% w/w of fipronil;
about 5% w/w of ethanol;
about 0.02% w/w of BHA;
about 0.01% w/w of BHT;
about 0.01% w/w of α-Tocopherol; and
balance diethylene glycol monoethyl ether.
19 . The formulation of claim 18 , which further comprises about 8.8% w/w of S-methoprene.
20 . The formulation of claim 16 , further comprising a knock-down agent.
21 . The formulation of claim 20 , wherein the knock-down agent is permethrin or a veterinary acceptable salt thereof.
22 . The formulation of claim 1 , further comprising pyriproxyfen or a veterinary acceptable salt thereof.
23 . The formulation of claim 22 , wherein the pyriproxyfen is present from about 3% to about 10% by weight of the formulation.