JPH0120125B2 - - Google Patents

Description

[Detailed description of the invention]

There are relatively few ectoparasitic insecticides currently commercially available. The most well-known lice-killing poisons are lindane (γ-benzene hexachloride), malathion [(S-1,2-dicarbuethoxymethyl)-0,0-dimethylphosphorodithionate], which has a synergistic effect. Added pyrethrin and kyuplex (tetrahydronaphthalene,
A combination of copper oleate and acetone (although acetone is not active)
It is. Sulfur, LINDANE, vesil and crotamiton are some of the best known drugs. Research into new safe and effective ectoparasiticides has recently increased due to increased public concern regarding the safety of certain known toxins against ectoparasites. It has now been discovered that certain polyols are effective as insecticidal and ovicidal agents for ticks and, depending on the formulation, as insecticides for lice. Although polyols are known substances, their insect and/or egg combating activity was previously unknown. 2-ethyl-1,3
-Hexanediol is known as an insect harassing agent (US Pat. Nos. 2,407,205 and 3,836,672) and has been widely used commercially as such. The object of the present invention is to provide a new method for insects and their eggs.
The goal is to provide safe and effective poisons. This and other objects of the invention will be better understood from the description provided below. The present invention relates to a poison for killing ectoparasites and a composition for controlling ectoparasites, other biting insects, and lice. More particularly, the present invention relates to the use of certain polyols as poisons for lice, mites and/or their eggs, and to toxic compositions containing such polyols. It has been found that certain polyols, preferably 1,3-diols, which are diols in which the hydroxyl groups are not in adjacent positions, exhibit satisfactory activity. Representative polyols are 2-methyl-2,4-pentanediol, 2-ethyl-1,3-hexanediol, 1,3-butanediol, 1,3-heptanediol and 1,3-nonanediol. One or a combination of the toxic polyols of this invention can be incorporated into active toxic compositions.
The compositions may be combined with inert carriers by known procedures to form liquids, powders, lotions, creams, etc.
It may be in the form of a gel, aerosol spray, or foam. Any pharmaceutically acceptable carrier, aqueous or non-aqueous, can be used as long as it is inert to the active ingredients. By inert is meant that the carrier does not substantially adversely affect the insecticidal and ovicidal activity of the active ingredient against insects, mites, or eggs. The active polyol is present in effective insecticidal and ovicidal amounts in toxic compositions used to treat substrates, such as humans, animals, or inanimate objects, which require such treatment or are desired to be treated as a preventive measure. only. The amount means an amount that kills at least 50% of extracorporeal parasites or their eggs. Two standard two-minute soak test methods for lice and their eggs are described below.
The minimum concentration of polyol in the composition that corresponds to an effective insecticidal and ovicidal amount varies widely depending on the type of polyol used, the type of inert carrier and other ingredients used. Thus, in some cases a concentration of 10% is sufficient, while in other cases higher concentrations, such as 30-40%, are required to obtain an effective toxicant dose. The above two-minute immersion test was conducted as follows. Insecticidal power: Add tap water to a 50ml beaker and bring to room temperature (approx.
Leave it until it reaches 24℃. 10 young adult male lice and 10 young adult female lice of the same age from colonies of the same stock (Pediculus humanus corpolis)
corperis) on a 2 x 2 cm coarse patch (small piece of cloth). The test sample, kept at room temperature, is shaken to homogenize and placed in a 50 ml beaker. Immediately thereafter, the patch is placed in the sample, immersed for 2 minutes, taken out, and immediately thrown into the beaker containing tap water. The patch is then vigorously stirred every 10 seconds, and after 1 minute, the patch is removed and placed on a paper towel. The lice are then transferred to a 4 x 4 cm black kohl cloth patch, and this point is designated as time zero. After that, put this coal-tempered patch into a Petri dish, cover it, and store it in a constant temperature room at 30°C. Ovicidal power: 15 adult female lice (Pedeicylus hyumanus corpolis, 5-10 days old)
Pediculus humanus corporis) was placed on a 2 x 2 cm nylon mesh patch in a Petri dish.
Cover and keep in a thermostat at 30°C for 24 hours. Next, remove the adult lice and record the number of fat, viable eggs and shriveled, thin eggs on the patch. The test sample, kept at room temperature, is shaken to homogenize and placed in a 50 ml beaker. Immediately after that, put the patch into this beaker and let it soak. Take it out after 2 minutes and immediately return it to room temperature (approximately 24
Pour into a 50ml beaker containing tap water (℃). The patch is vigorously stirred every 10 seconds, and after 1 minute, the patch is taken out and left on a paper towel for 1 minute. Next, put the patch into a Petri dish, cover it, and store it in an incubator at 30℃. After 14 days, note the number of eggs that hatched and the number of shriveled eggs that did not hatch. For both insecticidal and ovicidal 2-minute immersion tests,
The control is run in the same manner as above, but using tap water at room temperature (24°C) instead of the test sample. It is recognized that the polyols of the present invention may also be utilized as co-toxicants in insecticidal and ovicidal compositions. In such compositions, the term "effective insecticidal and ovicidal amount" means an amount that increases the mortality of in vitro parasites exposed to a 2-minute soak test by at least 20% as compared to the same composition without the polyol. means. EXAMPLES Table 1 below shows the insecticidal and ovicidal power against lice and eggs of several polyols tested in undiluted form in a 2 minute immersion test. Comparison results for other polyols (sorbitol, 1,2-ethanediol, 1,2-propanediol as comparative examples) are also shown.

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Table 1 shows that the polyol of the present invention is an excellent ovicidal agent. Hexanediol is also an excellent lice poison. An even more surprising discovery was that while pentanediol does not have lice-killing properties in its undiluted form, it can impart lice-killing properties to compositions by forming it in a different form, i.e. in aliphatic alcohol or fatty acid ester solutions. It happened. This fact is illustrated by the following data. Additionally, this polyol is an effective toxicant against rabbit ear mites and is an in vitro surrogate for testing toxicity against rabbit ear mites. The diols of the invention can therefore also be used to formulate compositions that are effective both as ovicides and as insecticides, and in the case of hexanediol, at the same time as lice insecticides. Table 2 shows the results of testing three 15% polyol solutions in combination with 25% isopropanol, 60% water. For comparison, it should be noted that the same test with a combination of 25% isopropanol and 75% water resulted in 0% lice kill.

[Table] All 1,3-butanediol 44 5
Table 3 below shows the 2 minute soak test results for the three compounds at 25% concentration in combination with 15% isopropyl myristate and 60% water. It is noteworthy that for comparison, 15% isopropyl myristate emulsified in 85% water exhibits 0% lice killing activity.

[Table] All 1,3-butanediol 100 0
As a function of concentration, the ovicidal power of a 2-minute soak in 2-ethyl-1,3-hexanediol was reduced to 25% (w/
w) Determined in a formulation solution made up to 100% with isopropanol and the balance water. The results are shown in Table 4. Table 4 Concentration % (w/w) Egg mortality rate % 5 9.4 10 9.7 15 17 20 66 30 100 40 100 Table 5 shows the concentration of five types of polyols as a function of concentration when 100% in water. The results of the ovicidal power 2-minute immersion test are shown.

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[Table] The tick-killing power of this poison was determined as follows. In a 30 cm ³ chamber kept at room temperature, 10 adult ticks of mixed sexes (Psoroptes equi var. cuniculi) were placed in a microscope concave mounting glass with a lid. This mounting glass was placed 25 cm horizontally and 10 cm vertically below the activator of the mechanical spray device, and the lid was removed. Each press of the activator of the mechanical spray device sprays 50 micrograms of sample. The sample kept at room temperature was stirred until homogeneous and placed into the mechanical spray apparatus. The activator was depressed twice to introduce 100 micrograms of spray mist into the adjacent chamber. The mist was allowed to settle, and the glass plate containing the body was taken out and covered. This point was defined as zero time. Keep at room temperature for 24 hours. After 0, 1, 3 and 24 hours, observation was made using a microscope. Comparative tests were similarly performed using water or diluent and the % net mortality was reported. Table 6 Polyol mite killing rate % 1,3-butanediol 100 (w) 2-methyl-2,4-pentanediol 90 (w) 2-ethyl-1,3-hexanediol 100 (I) 1,3 -Heptanediol 100(I) 1,3-nonanediol 100(I) Typical end-use formulations of the polyol of the present invention are as follows (all wt%). : Clear liquid suitable for mechanical spray application or lubricating of lice insecticides and mite insecticides: 2-Ethyl-1,3-hexanediol 75 Isopropanol 25 Clear liquid shampoo for ovicidal use: 1,3-butane Diols 50 Triethanolamine lauryl sulfate 20 Water 30 Rapidly breaking ovicidal aerosol foams: Mono- and diglycerides from edible fat glycerides 8 Isopropanol 25 1,3-nonanediol 20 1,2,3-propanetriol 5 Water 34 Isobutane 8 Aerosol spray for ovicidal: 2-methyl-2,4-pentanediol 50 Isopropanol 25 Water 10 Isobutane 15 Cream for ovicidal: Cetyl alcohol 3.0 2-ethyl-1,3-hexanediol 30.0 Glyceryl monostearate 8.0 Sorbitan Monostearate 8.0 Xanthan Gum 0.3 Water 50.7 Various changes and modifications may be made in the present invention without departing from its spirit and scope. The various specific examples disclosed herein are intended to clarify the present invention and are not intended to limit the invention itself. Throughout this specification, all temperatures are in degrees Celsius and parts and percentages are by weight unless otherwise indicated.

Claims (1)

[Scope of Claims] 1. An insecticidal and/or ovicidal and/or acaricidal composition for extracorporeal parasites, which comprises an effective amount of an active poison and an inert carrier which causes no problems in preparation, wherein the active poison is 2 -Methyl-2,4-pentanediol, 1,3-butanediol, 1,3-
A composition comprising at least one diol selected from the group consisting of heptanediol and 1,3-nonanediol, and in the case of 2-methyl-2,4-pentanediol, the inert carrier contains isopropyl myristate. thing. 2. The composition according to claim 1, wherein the active poison is 1,3-heptanediol. 3. The composition of claim 1, wherein the active poison is 1,3-nonanediol. 4. The acaricidal composition according to claim 1, wherein the active poison is 2-methyl-2,4-pentanediol. 5. The acaricidal composition according to claim 1, wherein the active poison is 1,3-butanediol. 6 The concentration of isopropyl myristate is 15% by weight
The composition according to claim 1. 7 Claim 1 in which the carrier is an aqueous carrier
Compositions as described in Section.