# US 4,395,407 A · Parasiticidal pour-on compositions

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- Number: US 4,395,407 A
- Document ID: US4395407A
- Status: Granted
- Kind: A
- Application number: 06/365,700
- Filed: 1982-04-05
- Granted: 1983-07-26
- Earliest claimed: 1981-05-08
- Assignees: Janssen Pharmaceutica NV
- Inventors: John M. Ballany; Andrew R. Galbraith
- Web page: https://patentgrep.com/patent/US4395407A

## CPC

- A61K 31/425: Thiazoles
- A01N 57/16: containing heterocyclic radicals
- A61K 31/66: Phosphorus compounds
- A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
- 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

## Abstract

The present invention relates to novel stable pour-on compositions for eradicating or controlling parasites in non-human animals, said compositions containing tetramisole and/or levamisole and an organophosphate along with an acid to improve the efficiency of the composition.

## Claims

### Claim 1

A pour-on or spot-on composition for eradicating or controlling parasites in non-human animals, said compositions comprising
(a) from 1 to 30% by weight of tetramisole and/or levamisole;
(b) from 2 to 15% by weight of phosmet; and
(c) one or more optionally substituted aliphatic carboxylic acids, having each a pK.sub.a -value comprised between 0.6 and 6 in a molar excess of 1.5:1 to 12:1 over tetramisole and/or levamisole
in a suitable solvent and/or carrier.

### Claim 2 (depends on 1)

A composition according to claim 1 wherein the amount of tetramisole and/or levamisole is comprised between 1 and 10% by weight and the amount of phosmet is comprised between 2 and 15% by weight.

### Claim 3 (depends on 1)

A composition according to claim 1 wherein the amount of tetramisole and/or levamisole is comprised between 3 and 7% by weight of tetramisole and/or levamisole and from 5 to 12% by weight of phosmet.

### Claim 4 (depends on 1)

A composition according to claim 1 comprising from 3 to 7% by weight of levamisole and from 5 to 12% by weight of phosmet.

### Claim 5 (depends on 1)

A pour-on or spot-on composition according to claim 1 for eradicating or controlling parasites in non-human animals, said composition comprising
(a) from 1 to 30% by weight of tetramisole and/or levamisole;
(b) from 2 to 15% by weight of phosmet; and
(c) at least one member selected from the group consisting of acetic acid, citric acid, formic acid, trichloroacetic acid and malonic acid in a suitable solvent and/or carrier.

### Claim 6 (depends on 5)

A composition according to claim 5 comprising from 1 to 10% by weight of actic acid and from 5 to 15% by weight of citric acid.

### Claim 7

A pour-on or spot-on composition for eradicating or controlling parasites in non-human animals, said composition comprising
(a) from 3 to 7% by weight of levamisole;
(b) from 5 to 12% by weight of phosmet;
(c) from 1 to 10% by weight of acetic acid; and
(d) from 5 to 15% by weight of citric acid
in a suitable solvent and/or carrier.

### Claim 8

A pour-on or spot-on composition for eradicating or controlling parasites in non-human animals, said composition comprising
(a) from 10 to 30% by weight of tetramisole and/or levamisole;
(b) from 2 to 15% by weight of phosmet; and
(c) one or more optionally substituted aliphatic carboxylic acids, having each a pK.sub.a -value comprised between 0.6 and 6 in a molar excess of 1.5:1 to 12:1 over tetramisole and/or levamisole.
in a medium comprising at least 50% by weight of a solvent and/or carrier consisting of one or more alcohols, having the formula
HO--(CH.sub.2 --CH.sub.2 --O).sub.m --R (III)
wherein m is the integer 1, 2 or 3; and R is lower alkyl.

### Claim 9 (depends on 8)

A composition according to claim 8 wherein the medium comprises at least 80% by weight of a solvent and/or carrier of formula (III).

### Claim 10 (depends on 8)

A composition according to claim 8 wherein the medium consists essentially of one or more alcohols of formula (III).

### Claim 11

A pour-on or spot-on composition for eradicating or controlling parasites in non-human animals, said composition comprising
(a) from 10 to 30% by weight of tetramisole and/or levamisole;
(b) from 2 to 15% by weight of phosmet; and
(c) one or more optionally substituted aliphatic carboxylic acids, having each a pK.sub.a -value comprised between 0.6 and 6 in a molar excess of 1.5:1 to 12:1 over tetramisole and/or levamisole
in a medium comprising at least 50% by weight of a solvent and/or carrier consisting of one or more alcohols having the formula
HO--(CH.sub.2 --CH.sub.2 --O).sub.2 --R (III-a)
wherein R is lower alkyl.

### Claim 12 (depends on 11)

A composition according to claim 11 wherein the medium comprises at least 80% by weight of a solvent and/or carrier of formula (III-2).

### Claim 13 (depends on 11)

A composition according to claim 11 wherein the medium consists essentially of one or more alcohols of formula (III-2).

### Claim 14

A pour-on or spot-on composition for eradicating or controlling parasites in non-human animals, said composition comprising
(a) from 10 to 30% by weight of tetramisole and/or levamisole;
(b) from 2 to 15% by weight of phosmet; and
(c) one or more optionally substituted aliphatic carboxylic acids, having each a pK.sub.a -value comprised between 0.6 and 6 in a molar excess of 1.5:1 to 12:1 over tetramisole and/or levamisole.
in a medium comprising at least 50% by weight of 2-(2-butoxyethoxy)-ethanol.

### Claim 15 (depends on 14)

A composition according to claim 14 wherein the medium comprises at least 80% of 2-(2-butoxyethoxy)ethanol.

### Claim 16 (depends on 14)

A composition according to claim 14 wherein the medium consists essentially of 2-(2-butoxyethoxy)ethanol.

### Claim 17

A pour-on or spot-on composition for eradicating or controlling parasites in non-human animals, said composition comprising
(a) from 3 to 7% by weight of levamisole;
(b) from 5 to 12% by weight of phosmet;
(c) from 1 to 10% by weight of acetic acid; and
(d) from 5 to 15% by weight of citric acid
in a medium comprising at least 50% by weight of 2-(2-butoxyethoxy)ethanol.

### Claim 18 (depends on 17)

A composition according to claim 17 wherein the medium comprises at least 80% of 2-(2-butoxyethoxy)ethanol.

### Claim 19 (depends on 17)

A composition according to claim 17 wherein the medium consists essentially of 2-(2-butoxyethoxy)ethanol.
