# US 10,864,193 B2 · Parasiticidal compositions comprising fipronil at high concentrations

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- Number: US 10,864,193 B2
- Document ID: US10864193B2
- Status: Granted
- Kind: B2
- Application number: 15/522,647
- Filed: 2015-10-30
- Published: 2017-11-23
- Granted: 2020-12-15
- Earliest claimed: 2014-10-31
- Assignees: Boehringer Ingelheim Animal Health USA Inc.
- Applicants: Boehringer Ingelheim Animal Health USA Inc.
- Inventors: James Pate; Natalya Shub
- Web page: https://patentgrep.com/patent/US10864193B2

## CPC

- A61K 31/415: 1,2-Diazoles
- A01N 43/40: six-membered rings
- A01N 47/02: the carbon atom having no bond to a nitrogen atom
- A01N 49/00: Biocides, pest repellants or attractants, or plant growth regulators, containing compounds containing the group [IMAGE cpc-sch-A01N-0948.gif], wherein m+n>=1, both X together may also mean —Y— or a direct carbon-to-carbon bond, and the carbon atoms marked with an asterisk are not part of any ring system other than that which may be formed by the atoms X, the carbon atoms in square brackets being part of any acyclic or cyclic structure, or the group [IMAGE cpc-sch-A01N-0949.gif], wherein A means a carbon atom or Y, n>=0, and not more than one of these carbon atoms being a member of the same ring system, e.g. juvenile insect hormones or mimics thereof (containing hydrocarbons A01N27/00)
- A61K 9/0017: {Non-human animal skin, e.g. pour-on, spot-on}
- A61K 31/215: of carboxylic acids
- A61P 33/10: Anthelmintics
- A61P 33/14: Ectoparasiticides, e.g. scabicides
- A01N 43/56: 1,2-Diazoles; Hydrogenated 1,2-diazoles
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A01N: PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF (preservation of food or foodstuff A23); BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES (preparations for medical, dental or toiletry purposes which kill or prevent the growth or proliferation of unwanted organisms A61K); PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention provides for spot-on formulations comprising fipronil in a high concentration for the treatment or prophylaxis of parasites of mammals and birds, and in particular, cats, dogs, horses, chickens, sheep and cattle with the aim of ridding these animals of all the parasites commonly encountered by birds and mammals. The invention also provides for effective and lasting destruction of ectoparasites, such as fleas, ticks, itch mites and lice, and of endoparasites, nematodes, such as filariae, and roundworms of the digestive tract of animals and humans.

## Claims

### Claim 1

A topical veterinary composition comprising:
(a) from about 16% to about 18% (w/v) fipronil;
(b) optionally, about 5% to about 15% (w/w) (S)-methoprene;
(c) about 14% to 18% (w/v) of a crystallization inhibitor which is a combination of polyvinylpyrrolidone and polyoxyethylene (20) sorbitan monooleate in a weight:weight ratio of about 2:1 to about 1.7:1;
(d) an organic co-solvent selected from the group consisting of methanol, ethanol, and isopropanol;
(e) an organic solvent which is butyl diglycol, dipropylene glycol n-butyl ether, ethylene glycol monoethyl ether, ethylene glycol monomethyl ether, dipropylene glycol monomethyl ether, liquid polyoxyethylene glycols, propylene glycol monomethyl ether, propylene glycol monoethyl ether, diethylene glycol monoethyl ether, or any combination thereof; and
(f) optionally, about 0.01% to about 2.0% of an antioxidant wherein the organic solvent (e) is present in the overall composition in a proportion representing a compliment to 100% of the composition;
wherein, the organic co-solvent to organic solvent is in a weight:weight ratio of between 1/15 and 1/2; and
wherein composition results in less than 10 crystals when placed on a glass slide at 20° C. for 24 hours.

### Claim 2 (depends on 1)

The topical veterinary composition of claim 1, wherein the organic co-solvent is ethanol.

### Claim 3 (depends on 1)

The topical veterinary composition according to claim 1 wherein the antioxidant is BHA or BHT, or a combination thereof.

### Claim 4 (depends on 1)

The topical veterinary composition of claim 1, wherein the composition is in the form of a spot-on formulation.

### Claim 5

A topical veterinary composition comprising:
(a) from about 16% to about 18% (w/v) fipronil;
(b) optionally, about 5% to about 15% (w/w) (S)-methoprene;
(c) about 14% to about 18% (w/v) of a crystallization inhibitor which is a combination of polyvinylpyrrolidone and polyoxyethylene (20) sorbitan monooleate in a weight:weight ratio of about 2:1 to about 1.8:1;
(d) an organic co-solvent which is ethanol;
(e) an organic solvent which is diethylene glycol monoethyl ether; and
(f) optionally, about 0.01% to about 2.0% of an antioxidant wherein the organic solvent (e) is present in the overall composition in a proportion representing the compliment to 100% of the composition;
wherein, the organic co-solvent to organic solvent is in a weight:weight ratio of between 1/15 and 1/2; and
wherein composition results in less than 10 crystals when placed on a glass slide at 20° C. for 24 hours.

### Claim 6 (depends on 5)

The topical veterinary composition according to claim 5, which comprises about 15% (w/v) of the crystallization inhibitor.

### Claim 7 (depends on 5)

The topical veterinary composition according to claim 5, wherein the antioxidant is BHA or BHT, or a combination thereof.

### Claim 8 (depends on 5)

The topical veterinary composition of claim 5, wherein the composition is in the form of a spot-on formulation.