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

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

US20050245582A1Inactive Publication Date: 2005-11-03SUMMIT VETPHARM

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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

Patent Timeline
03 Nov 2005
Publication
US20050245582A1
IPC
A01N25/34; A01N37/18; A01N37/34; A01N43/08; A01N43/40; A01N53/00
CPC
A01N25/34; Y10S514/97; A01N53/00; A01N47/40; Y10S514/875; A01N43/40; A01N49/00; A01N51/00
Inventors
COTTRELL, IAN W.; AHN, ALBERT