JP2002363008A - Method for controlling ectoparasite on animal - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a method for controlling ectoparasites on animals by which effectiveness can be sustained over a relatively long period. SOLUTION: The ectoparasites on host animals are controlled by administering a suppository comprising an insect growth controlling substance such as a juvenile hormone, a juvenile hormonal substance, an ecdysonelike substance or a chitin formation inhibitor or an insecticide such as an insecticidal antibiotic substance, a neonicotinoid compound or a phenylpyrazole compound to the anus of the host animals.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a method for controlling ectoparasites in animals.

[0002]

2. Description of the Related Art Conventionally, in order to control animal ectoparasites such as fleas, an insecticidal method using an active ingredient having an effect of controlling adults, such as organophosphorus compounds, carbamate compounds, and pyrethroid compounds, has been proposed. Was used.

However, in these methods, eggs in the environment,
A sufficient control effect was not obtained because the larval control effect was insufficient.

A method for administering an insect growth regulator such as a juvenile hormone, a juvenile hormone-like substance, a chitin formation inhibitor or the like to a host animal and controlling ectoparasites through the blood of the host animal is disclosed in 63-72631, JP-A-2-8855
7. Known in Japanese Patent Application Laid-Open No. 6-221792, etc., and these methods have made it possible to efficiently control animal ectoparasites such as fleas.

However, oral administration, which is a preferred method of administration to a host animal described in these publications, is effective in that many of the active ingredients are metabolized and decomposed or excreted in the body of the host animal. It has been difficult to control ectoparasites such as fleas via the blood of the host animal.

[0006]

SUMMARY OF THE INVENTION An object of the present invention is to provide a method for controlling ectoparasites in animals, which can maintain the efficacy for a relatively long period of time.

[0007]

According to the present invention, one or more insect growth regulators selected from juvenile hormone, juvenile hormone-like substance, ecdysone-like substance, chitin formation inhibitor and the like are contained as active ingredients. By administering a suppository to the anus of a host animal, ectoparasites of the host animal can be controlled for a relatively long period of time.

[0008]

BEST MODE FOR CARRYING OUT THE INVENTION Examples of the insect growth regulator used as an active ingredient in the present invention include the following juvenile hormones, juvenile hormone-like substances, ecdysone-like substances, chitin formation inhibitors and the like. Can be.

The juvenile hormone and the juvenile hormone-like substance include, for example, the following. (1) Methyl-10,11-epoxy-7-ethyl-
3,11-dimethyl-2,6-tridecadienoate (2) 4-phenoxyphenyl 2- (2-pyridyloxy) propyl ether (generic name: pyriproxyfen) (3) ethyl 2- (4-phenoxyphenoxy) ) Ethyl carbamate (generic name: phenoxycarb) (4) Isopropyl (2E, 4E) -11-methoxy-3,7,11-trimethyl-2,4-dodecadienoate (generic name: methoprene) (5) Ethyl (2E, 4E) -3,7,11-trimethyl-2,4-dodecadienoate (generic name: hydroprene)

[0010] Examples of the ecdysone-like substance include the following. (6) N-tert-butyl-N '-(4-ethylbenzoyl) -3,5-dimethylbenzohydrazide (generic name: tebufenozide)

[0011] Examples of the chitin formation inhibitor include the following. (7) 1- (2,6-difluorobenzoyl) -3-
[2-Fluoro-4- (1,1,2,3,3,3-hexafluoroproxy) phenyl] urea (8) 1- (2,6-difluorobenzoyl) -3-
[2-Fluoro-4- (1,1,2,2-tetrafluoroethoxy) phenyl] urea (9) 1- (2,6-difluorobenzoyl) -3-
[2-Fluoro-4- (trifluoromethyl) phenyl] urea (10) 1- [3,5-dichloro-4- (3-chloro-
5-trifluoromethylpyridin-2-yloxy) phenyl] -3- (2,6-difluorobenzoyl) urea (general name: chlorofluazuron) (11) 1- [2,5-dichloro-4- (1 , 1,2,
3,3,3-hexafluoroproxy) phenyl] -3
-(2,6-difluorobenzoyl) urea (generic name:
Lufenuron) (12) 1- (4-chlorophenyl) -3- (2,6-
Difluorobenzoyl) urea (generic name: diflubenzuron) (13) 1- (3,5-dichloro-2,4-difluorophenyl) -3- (2,6-difluorobenzoyl) urea (generic name: teflubenzuron) (14) 1- (2-chlorobenzoyl) -3- (4-trifluoromethoxyphenyl) urea (generic name: triflumuron) (15) 1- [4- (2-chloro-4-trifluoromethylphenoxy) -2 -Fluorophenyl] -3-
(2,6-difluorobenzoyl) urea (generic name: flufenoxuron) (16) 1- [α- (4-chloro-α-cyclopropylbenzylideneaminooxy) -p-tolyl] -3-
(2,6-difluorobenzoyl) urea (generic name: flucycloxuron) (17) 1- [3,5-dichloro-4- (1,1,2,2
2-tetrafluoroethoxy) phenyl] -3- (2,
6-difluorobenzoyl) urea (generic name: hexaflumuron) (18) N-cyclopropyl-1,3,5-triazine-2,4,6-triamine (generic name: cyromazine)

The insecticide used as an active ingredient in the present invention includes, for example, insecticidal antibiotics such as milbemycin, abamectin, selamectin and ivermectin;
-[(6-chloro-3-pyridyl) methyl] -N2-cyano-N1-methylacetamidine (generic name: acetamiprid), N-[(6-chloro-3-pyridylmethyl)
Neonicotinoid compounds such as -N-ethyl-N'-methyl-2-nitrovinylidenediamine (generic name: nitenpyram), phenylpyrazole compounds and the like can be mentioned.

Further, the insect growth controlling substance and the insecticide used as the active ingredients in the present invention can be used simultaneously.

For the host animal, it is administered to the anus in the form of a suppository. The suppository of the present invention is prepared by mixing the present compound, if necessary, with a solid dispersion composed of an enteric polymer, stirring and uniformly dispersing the compound in a suitable base previously melted, and dispersing the compound in a conventional manner. It is manufactured by molding according to.

As the base used in the suppository of the present invention, commonly used bases can be used, and animal and vegetable oils and fats (olive oil, corn oil, castor oil, cottonseed oil, wheat germ oil, cacao oil, tallow, tallow, etc.) , Wool fat, turtle fat, squalene, hardened oil, etc.), mineral oils (vaseline, white petrolatum, solid paraffin, liquid paraffin, dehydrated lanolin, silicone oil, etc.), waxes (jojoba oil, carnauba wax, beeswax, lanolin, etc.) In addition to the above, partially or totally synthetic glycerin fatty acid esters (intermediate, such as linear saturated fatty acids such as lauric acid, myristic acid, palmitic acid, and stearic acid, and linear unsaturated fatty acids such as oleic acid, linoleic acid, and linoleic acid, etc.) Or higher fatty acids,
Di- or triglycerides).

Examples of commercially available glycerin fatty acid esters include mono-, di-, and triglycerides of saturated fatty acids having 12 to 18 carbon atoms such as Witepsol (manufactured by Dynamit Nobel) and Phosco (manufactured by Maruishi Pharmaceutical). Mono-, di-, saturated fatty acids having 10 to 18 carbon atoms, such as celite mixture, pharmazol (manufactured by NOF Corporation), isocacao (manufactured by Kao Corporation), SB (manufactured by Kaneka Corporation), Nopata (manufactured by Henkel) A triglyceride mixture of a saturated fatty acid having 8 to 12 carbon atoms such as a triglyceride mixture, a miglyol (manufactured by Dynamit Nobel) and the like can be mentioned. These may be used alone or as a mixture as necessary.

The amount of these bases is from 50 to 99% by weight of the whole.

The suppository used in the present invention may contain, if necessary, excipients, preservatives, surfactants, fragrances, coloring agents, p
It is also possible to add an H adjuster, purified water and the like.

The dosage form used in the present suppository may be a rectal suppository which is solid at normal temperature and melts at body temperature, an ointment or an enema liquid dispersed in a liquid base, such as a soft capsule for rectal administration and injection for rectal administration. A dosage form using a container or the like is used. The suppository is preferably stored in a refrigerator.

The content of the present compound in the suppository of the present invention varies depending on the efficacy of the active ingredient used and the animal species to be administered, but it is usually 0.1 mg to 1000 mg per suppository.
0 mg, preferably in the range of 1 mg to 1000 mg.

The present compound is usually used in an amount of 0.01 mg to 100 mg / kg body weight of the host animal to which the suppository is administered to the anus.
It is administered in a dose of 0 mg, preferably 0.1 mg to 100 mg.

The ectoparasites to be controlled by the control method of the present invention are, in particular, Musca herv which are ectoparasites of domestic animals such as cattle and sheep and pets such as dogs and cats.
ei), Housefly (Musca bezzii), Fly (Ha)
ematobia irritans)
s), bovine squid (Culicoides oxystoma), cattle flies (Tabanus chrysurus), Culex pipiens,
Diptera pests such as Aedes albopictus, lice such as Boema lice (Haematopinus eurysternus) and sheep lice (Damalinia ovis), Haemaphyxalis longicornis, and Boom ticks
Pests such as philus microplus, cat flea (Ctenoc)
ephalides felis, dog flea (Ctenocephalides cani)
s) and flea insect pests such as Xenopslla cheopis.

The target animals include domestic animals and pets. For example, livestock such as cattle and sheep, and the pets include rodents such as mice, rats, hamsters and squirrels, and rabbits such as rabbits. , Dogs, cats, ferrets, and other carnivores, and ducks, chickens, pigeons, and other birds.

[0024]

Next, the present invention will be described in more detail with reference to examples.

[0025]

Formulation Example 1 90 mg of 4-phenoxyphenyl 2- (2-pyridyloxy) propyl ether (generic name: pyriproxyfen) and Phosco S-55 (manufactured by Maruishi Pharmaceutical Co., Ltd., containing saturated fatty acids having 12 to 18 carbon atoms) Things, di,
1160 mg of a triglyceride mixture) is melt-mixed at 100 ° C., poured into a suppository mold, and solidified by cooling to obtain a suppository weighing 1250 mg per piece.

[0026]

[Test Example 1] (Cat anal administration test) Cat flea (Cten
One suppository of Preparation Example 1 was administered to a cat (30 kg / kg body weight as pyriproxyfen) to a cat (live weight 3 kg, female) infested with 80 adult ocephalides felis. The cat is a metal cage (760 mm wide, 540 deep)
mm, height 610 mm, bottom part was equipped with a movable tray) and fed with water and food (solid feed). One week after the administration, 60 cat flea eggs born in a tray attached to the lower part of the cage were collected, transferred to a resin petri dish, stored at a temperature of 26 ° C. and a humidity of 90%, and hatched after 7 days. The situation was investigated. One week after the administration, all the parasitic flea adults were removed from the cat using a flea comb. Eight weeks after the administration, 80 new cat flea adults were parasitized in the cat, and hatching status was similarly examined on the produced cat flea eggs. In addition, a placebo suppository containing no active ingredient was administered to the cat's anus, and the same investigation as above was conducted. The hatching inhibition rate (%) of Formulation Example 1 was determined from the hatching rates of the obtained groups by the following formula. Hatching inhibition rate (%) = {(CT) {C} × 100 C: Hatching rate (%) of placebo administration group T: Hatching rate (%) of formulation example 1 administration group The results are shown in Table 1.

[0027]

[Table 1]

[0028]

[Comparative Test Example 1] (Cat oral administration test) A predetermined amount (30 mg / kg body weight) based on the live weight of a cat was placed on a cat (live weight 3 kg, female) in which 100 cat flea (Ctenocephalides felis) adults had been infested in advance. 4-phenoxyphenyl 2- (2-pyridyloxy) propyl ether (generic name: pyriproxyfen) was added and the whole mixed food was taken. In the same manner as in Test Example 1, the hatching status of flea spawning eggs was examined one week after administration and eight weeks after administration.
In addition, cats fed the diet without pyriproxyfen were taken as the non-added group, and the same investigation as above was conducted. The hatch inhibition rate (%) was determined from the hatch rates of the obtained groups in the same manner as in Test Example 1. Table 2 shows the results.

[0029]

[Table 2]

As shown in the test results of Test Example 1 and Comparative Test Example 1, 4-phenoxyphenyl 2- (2-pyridyloxy) propyl ether (generic name: pyriproxyfen) which is an insect growth controlling substance Does not inhibit the hatching effect of parasitized adult laying eggs when administered orally to host animals, but when suppositories are administered to the anus, the effect was markedly sustained. .

[0031]

According to the method for controlling ectoparasites of animals of the present invention, ectoparasites of animals can be effectively controlled over a long period of time.

 ──────────────────────────────────────────────────続 き Continued on the front page (72) Inventor Tomohiro Teramae 4-2-1 Takashi, Takarazuka-shi, Hyogo Prefecture (72) Inventor Hitoshi Kawada 4-2-1 Takashi, Takarazuka-shi, Hyogo F-term (reference) 4H011 AC01 BA01 BB09 BB14 BC06 DA11 DD07

Claims (6)

[Claims] 1. A substance selected from a juvenile hormone, a juvenile hormone-like substance, an ecdysone-like substance, a chitin formation inhibitor and the like.
A method for controlling ectoparasites of a host animal by administering to the anus of the host animal a suppository containing at least one species of insect growth regulator as an active ingredient. 2. The method according to claim 1, wherein the juvenile hormone-like substance is 4-phenoxyphenyl 2- (2-pyridyloxy) propyl ether. 3. The method for controlling an animal ectoparasite according to claim 1, wherein the chitin formation inhibitor is a benzoylurea compound. 4. The method according to claim 1, wherein the benzoylurea compound is 1- (2,6-
Difluorobenzoyl) -3- [2-fluoro-4-
(1,1,2,3,3,3-hexafluoro proxy)
Phenyl] urea, 1- (2,6-difluorobenzoyl) -3- [2-fluoro-4- (trifluoromethyl) phenyl] urea, 1- [3,5-dichloro-4-
(3-chloro-5-trifluoromethylpyridine-2-
Yloxy) phenyl] -3- (2,6-difluorobenzoyl) urea, 1- [2,5-dichloro-4-
(1,1,2,3,3,3-hexafluoro proxy)
The method for controlling animal ectoparasites according to claim 3, which is [phenyl] -3- (2,6-difluorobenzoyl) urea. A suppository containing as an active ingredient at least one insecticide selected from insecticidal antibiotics, neonicotinoid compounds, phenylpyrazole compounds and the like by administering to the anus of a host animal a suppository. A method for controlling ectoparasites of a host animal. 6. An ectoparasite of a host animal is controlled by administering to the anus of a host animal a suppository containing the insect growth controlling substance of claim 1 and the insecticide of claim 5 simultaneously. how to.