High concentration topical insecticides containing pyrethroids

a topical insecticide and high concentration technology, applied in the field of insecticides, can solve the problems of unpleasant smell, high undesirable infestation of animals with fleas, ticks, flies and the like, and avoid many common deleterious side effects, and achieve the effect of safe us

Inactive Publication Date: 2005-11-03
SUMMIT VETPHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006] Generally speaking, in accordance with the invention, a topical insecticide, particularly one for use on pets, especially dogs, is provided. Formulations in accordance with the invention can be safe to use and can avoid many common deleterious side effects of conventional topical insecticides.
[0007] The invention provides a topical insecticide which contains a combination of insecticides and insect growth regulators which can be effective to kill fleas, flea eggs, flea larvae, ticks, tick eggs, tick larvae and tick nymphs. The selection of the combination of insecticides and insect growth regulators produces an insecticide having high insecticidal activity while allowing for a lower total amount of insecticide to be applied to the animal, compared to the effectiveness and amount required of the individual insecticides when used alone to achieve the same kill rate. The compositions derived herein can also be useful to improve the speed of result and decrease the reoccurrence, compared to other formulations.
[0008] The invention can provide an insecticidal composition which contains a combination of a first insecticide component in an insecticidally effective amount to achieve at least, e.g., an 80%, preferably 90% kill rate for fleas, a second insecticide component in an insecticidally effective amount to achieve at least, e.g. an 80%, preferably 90% kill rate for ticks, and a growth regulating effective amount of an insect growth regulator (IGR). In certain embodiments of the invention, the second insecticide is not a neo-nicotinoid, which is considered only effective against fleas. The combination of the two insecticide components and the insect growth regulator increases the effectiveness of the first and second insecticide compared to the effectiveness of the first and second insecticides when used alone and reduces the effective amount of the first and second insecticide compared to the effective amount of the first and second insecticide when used alone.
[0016] Accordingly, it is an object of the invention to provide an improved topical insecticide composition that is highly effective against fleas, flea larvae, flea eggs, and ticks.

Problems solved by technology

The infestation of animals with fleas, ticks, flies and the like is highly undesirable.
This can cause considerable mess and can lead to an unpleasant smell.
Additionally, if the dosage of a topical insecticide is in a large volume, it can be easily shaken off by the animal, thereby reducing the effectiveness of the insecticide formulation.
Also, when the animal is a house pet, there is a further complication in that the insecticide should be safe for human contact.

Method used

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  • High concentration topical insecticides containing pyrethroids
  • High concentration topical insecticides containing pyrethroids
  • High concentration topical insecticides containing pyrethroids

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of 1-{(tetrahydro-3-furanyl)methyl}-2-nitro-3-methylguanidine (dinotefuran)

[0110] A mixture comprising 10.0 g of (tetrahydro-3-furanyl)methanol, 29.5 g of trifluoromethanesulfonic anhydride, 10.0 g of pyridine and 200 ml of dichloromethane was stirred for an hour at room temperature. Water was poured into the reaction solution to separate the organic layer, which was washed with 1 N hydrochloric acid, water and a saturated saline solution, dried, and concentrated to obtain 20 g of 3-tetrahydro-furanylmethyl triflate. 3.25 g of 60% sodium hydride were added to 12.5 g of 1,5-dimethyl-2-nitroiminohexahydro-1,3,5-triazine and 60 ml of DMF at room temperature, followed by stirring for an hour. 20.0 g of the 3-tetrahydrofuranylmethyl triflate were added thereto, and the mixture was stirred at 50° C. for 2 hours. After cooling the mixture to room temperature, 50 ml of 2N hydrochloric acid were added thereto, followed by stirring at 50° C. for 2 hours. The resultant mixture was...

example 2

Preparation of Insecticide Formulation Containing Dinotefuran and Pyriproxyfen

[0111] 25 g of dinotefuran was added to 100 ml phenyl methanol with stirring until it dissolved. 1 g of pyriproxyfen was added to the solution with stirring to produce a clear, homogeneous solution of high insecticide concentration.

[0112] The resulting solution can be spot applied to companion animals, such as dogs and will kill fleas, ticks and other insects.

example 3

Preparation of Insecticide Formulation Containing Permethrin, Dinotefuran and Pyriproxyfen

[0113] Permethrin (65 g) was added to a clean container. Safflower oil (35 g) was added with stirring until the solution was homogeneous. This solution containing permethrin and safflower oil was added to one of the chambers in the package in the appropriate volume based on the dosage required.

[0114] Pyriproxyfen (1 g) and Mackemium KP (1 g) were added to a clean container, and gently heated until the pyriproxyfen liquefied. Water (27.6 g) was added with stirring, followed by the addition of ethyl lactate (55.4 g). Dinotefuran (15 g) was added and the solution was mixed and heated at 50° C. until the dinotefuran dissolved. The solution was cooled to room temperature and the pH adjusted to 5.5 by the addition of sodium carbonate (0.15 g of a 25% aqueous solution). This solution was added to the other chamber in the package in the appropriate volume based on the dosage required.

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Abstract

A topical insecticide preparation is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. The topical insecticide contains a combination of a first pyrethroid insecticide effective for killing fleas, a second pyrethroid insecticide effective for killing ticks, and an insect growth regulator (IGR). The topical insecticide preparation can be packaged together or packaged so that the first and second pyrethroid insecticides are stored separately prior to administration of the insecticide preparation to the animal. The combination of the first and second pyrethroid insecticides with an insect growth regulator results in an insecticide preparation formulated to have enhanced insecticidal activity against fleas and ticks compared to the effectiveness of the first and second insecticides used alone. Further, the combination of the first and second pyrethroid insecticides with an insect growth regulator produces an insecticide preparation having enhanced insecticidal activity against fleas and ticks while advantageously minimizing the total amount of insecticide needed for its effectiveness.

Description

[0001] This application is a continuation-in-part of and claims priority to U.S. application Ser. No. 10 / 910,542, filed Aug. 3, 2004, which claims priority benefit to U.S. Provisional Application No. 60 / 493,976, filed Aug. 8, 2003, and U.S. Provisional Application No. 60 / 554,563, filed Mar. 19, 2004, and is also a continuation-in-part of U.S. application Ser. No. 10 / 242,551, filed Sep. 12, 2002, now U.S. Pat. No. 6,867,223, the contents of all of which are incorporated herein by reference.BACKGROUND OF INVENTION [0002] The invention relates generally to insecticides and more particularly to a topical insecticide, such as one suitable to use on house pets such as dogs. [0003] The infestation of animals with fleas, ticks, flies and the like is highly undesirable. Accordingly, it has become common to administer both topical and internal insecticides to livestock and pets. Topical applications can be desirable, in that many insecticides are acceptably safe when used topically, but not w...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A01N25/34A01N37/18A01N37/34A01N43/08A01N43/40A01N53/00
CPCA01N25/34Y10S514/97A01N53/00A01N47/40Y10S514/875A01N43/40A01N49/00A01N51/00A01N57/12A01N2300/00A01N25/02A61P33/14
Inventor COTTRELL, IAN W.AHN, ALBERTFISHER, RICHARDMONRO, CHRISTINEJOSEPH, PIERRE
Owner SUMMIT VETPHARM
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