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Versatile high load concentrate compositions for control of ecto-parasites

A technology for cyfluramid and a composition is applied in the field of general high-load concentrated compositions for controlling ectoparasites containing cyfluramid, and can solve the problems of insolubility and instability of cyfluramid, which are difficult to prepare and the like

Inactive Publication Date: 2008-05-14
WYETH LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is particularly advantageous as it provides 4-6 weeks of protection from fleas and ticks in companion animals, but it will potentially be useful in many other species if appropriate formulations can be developed
However, the insolubility of metaflumizone in many solvents and its instability in the presence of primary alcohols make it difficult to formulate

Method used

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  • Versatile high load concentrate compositions for control of ecto-parasites

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0038] Preparation of high-loading concentrates of metaflumizone suitable for use as spray-on drops

[0039] 10 g DMSO was added to 40 g gamma-caprolactone. 20 g of metaflumizone was added to this solvent mixture. Slight heating (40°C) may be used to facilitate the dissolution process. While stirring, 6 g of Synperonic(R) NCA 830 brand alcohol alkoxylate surfactant was added to the resulting solution. The volume was brought to 100 ml with gamma-caprolactone.

[0040] Compositions so formulated can be applied to cats as "spray-on" (small topical doses) treatments.

[0041] The efficacy of this formulation is given in the following efficacy table:

[0042] days after processing

example 2

[0044] Preparation of metaflumizone pour-on from high loading concentrate (Example 1)

[0045] Sufficient 100 ml of gamma-caprolactone was added to 25 ml of the high load concentrate prepared in Example 1. This provided a pour-on formulation with sufficient metaflumizone and volume to treat 5 cattle weighing 200 Kg each at a dose rate of 5 mg / kg.

example 3

[0047] Preparation of high-capacity concentrates for use as concentrates for the preparation of metaflumizone sprays or feed / water supplements

[0048] 12.59 g of metaflumizone were added to the dimethylisosorbide using mild heating (approximately 40°C). While stirring, 109.92 g of Cremophor(R) EL (polyethoxylated castor oil, sold by Basf Aktiengesellschaft) were added to this solution, followed by a sufficient quantity of 200 ml of 1-methoxy-2-propyl acetate. The resulting solution was stored until ready to use, after which it could be diluted with water for use as a spray (17ml concentrate to 3500ml with water) or water for use as a feed / water additive (at about the same ratio).

[0049] The formulation was diluted with water to a concentration of 10 mg / kg (body weight) of metaflumimid and applied to sheep at 1500 ml / animal to test the effect of metaflumimid on biting white lice.

[0050] days after processing

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PUM

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Abstract

The invention relates to high load concentrate compositions comprising metaflumizone, an optional bridging agent, a surfactant, and a suitable carrier solvent. These compositions may be topically administered to animals, and are useful for preventing or treating ectoparasitic infestations in warm-blooded animals for prolonged periods of time. Additionally, they may be further diluted to provide other types of formulations useable for both topical and oral administration.

Description

[0001] This application claims priority from co-pending Provisional Application Serial No. 60 / 683,949, filed May 24, 2005, the entire disclosure of which is incorporated herein by reference. technical field [0002] none Background technique [0003] Arthropod ectoparasites that commonly infect warm-blooded animals include ticks, mites, white lice, fleas, blowflies, the ectoparasite Lucilia sp. of sheep, including the sheep tick (Melophagus ovinus )) biting insects and migratory dipteran larvae (such as Hypoderma sp. and Dermatobia on cattle, Gastrophilus on horses and yellow flies on rodents ( Cuterebra sp.)). [0004] Metaflumizone is useful in the prevention and control of infections caused by ectoparasites in warm-blooded animals. Topical administration of the active agent is a preferred method of administering the compound. [0005] To provide useful protection against ectoparasitic infection or infection in warm-blooded animals requires the use of formulations with ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/175A01N47/34
CPCA61K47/44A61K9/0017A61K9/08A01N47/34A61K31/175A61P33/00A61P33/14A01N25/02A01N25/30A01N2300/00
Inventor 罗伯特·B·奥尔布赖特肖芭恩·萨布尼斯
Owner WYETH LLC
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