Application of oxadiazon or preparations containing oxadiazon in the control of parasites on host animals.

Abstract

This invention belongs to the field of veterinary drug technology, specifically relating to the application of oxazolidinone or preparations containing oxazolidinone in the prevention and control of parasites on host animals, wherein the parasites are ticks, and oxazolidinone and its preparations have good control effects on tick parasites.

Description

Technical Field

[0001] This invention belongs to the field of veterinary drug technology, specifically relating to the application of oxazolidinone or a preparation containing oxazolidinone in the prevention and treatment of parasites on host animals. Background Technology

[0002] Ticks have a wide range of hosts; their larvae, nymphs, and adult males and females all feed on blood. In mammal farming, especially cattle, ticks easily infest animals, leading to malnutrition and disease transmission, causing significant economic losses to farmers, and are difficult to control. Therefore, there is an urgent need for an effective animal parasite control agent. Summary of the Invention

[0003] To address the aforementioned problems in the prior art, this invention provides the application of oxadiazon or a formulation containing oxadiazon in the prevention and control of parasites on host animals. The compound exhibits good control activity against parasites such as ticks.

[0004] The technical solution adopted in this invention is as follows:

[0005] The application of oxadiazon (CAS No.: 2892524-05-7) or a formulation containing oxadiazon in the prevention and control of parasites on a host animal, said parasite being an animal of the superfamily Ixodidae.

[0006] In another specific embodiment, the application includes administering oxadiazon or a formulation containing oxadiazon to a host animal via oral, parenteral, or dermal route.

[0007] In another specific embodiment, the formulation also includes conventional adjuvants.

[0008] In another specific embodiment, the conventional adjuvant includes a carrier.

[0009] In another specific embodiment, the formulation further includes other active ingredients.

[0010] The present invention also discloses a method for removing parasites from a host animal for non-therapeutic purposes, comprising the step of administering oxadiazon or a preparation containing oxadiazon to the host animal or its contact site or equipment to remove the parasites, wherein the parasites are ticks.

[0011] In another specific embodiment, the host animal is a mammal, such as a cow.

[0012] In this article, "superfamily Ixoidea" includes pests of the family Ixodidae: *Rhipicephalus microplus*, *Haemaphyxalis longicornis*, *Haemaphysalis japonica*, *Rhipicephalus linnaei*, *Boophilus microplus*, *Dermacentor recticulatus*, *Dermacentor taiwanensis*, *Haemaphysalis flava*, *Ixodes ovatus*, *Ixodes persulcatus*, *Ixodes scapularis*, *Ixodes holocyclus Neumann*, *Dermacentor nuttalli*, *Hyalomma asiaticum*, *Dermacentor variabilis*, and *Amblyomma*. Americanum Linnaeus, American blunt-eyed tick (Amblyo mma americanum), spotted blunt-eyed tick (Amblyo mma maculatum), Dermacentor andersoni, Dermacentor occidentalis, Dermacentor variabilis, Haemaphysalis campanulata, Haemaphysalis megaspinosa, Ixodes nipponensis, Ixodes pacifcus, Ixodes ricinus, Ixodes scapularis, and other soft ticks, as well as Ornithodoros papillipes, Ornithodoros turicata Duges, and Argas radiatus Raillet, etc.

[0013] There are no particular limitations on the method of using the composition for deworming host animals of the present invention as a parasite deworming agent, and commonly used methods can be used.

[0014] Specifically, for example, it can usually be used as follows: according to the commonly used formulation, it is combined with conventional excipients (including appropriate carriers (solid and / or liquid carriers) and other excipients as needed) in appropriate proportions to dissolve, suspend, mix, impregnate, adsorb or adhere to the formulation, and prepared into an appropriate dosage form according to the intended use.

[0015] As the solid or liquid carrier used in this invention, carriers commonly used in veterinary pharmaceuticals can be used. Considering ease of handling the target animal, a liquid carrier is preferred. Examples of liquid carriers include alcohols such as methanol, ethanol, isopropanol, tert-butanol, and benzyl alcohol; propylene carbonate; N-methyl-2-pyrrolidone; and water. As adjuvants, surfactants, antioxidants, and emulsifiers can be used. Examples of surfactants include polyoxyethylene alkyl aryl ethers, polyoxyethylene sorbitan monolaurate, alkyl allyl sorbitan monolaurate, alkylbenzene sulfonates, alkylnaphthalene sulfonic acids, lignin sulfonate higher alcohol sulfates, ethylene glycol monoalkyl ethers, and ethylene glycols; emulsifiers include sorbitan monooleate, sorbitan monolaurate, glyceryl caprylate, glyceryl decanoate, glyceryl isostearate, and propylene glycol monocaprylate; and antioxidants include BHA and BHT.

[0016] Examples of other adjuvants in the formulations of this invention, as known in the art, include stabilizers (e.g., antioxidants), spreading agents, preservatives, adhesion promoters, active solubilizers (e.g., oleic acid), viscosity modifiers, ultraviolet blocking or absorbing agents, and colorants. Surfactants may also be included, including anionic surfactants, cationic surfactants, nonionic surfactants, and amphoteric surfactants.

[0017] As is known in the art, the formulations of the present invention may comprise one or more other components conventionally included in pourable formulations. Examples of suitable other components are stabilizers (e.g., antioxidants), spreading agents, preservatives, adhesion promoters, active solubilizers (e.g., oleic acid), viscosity modifiers, UV blockers or absorbers, and colorants. The pourable formulation may also include surfactants, including anionic surfactants, cationic surfactants, nonionic surfactants, and amphoteric surfactants.

[0018] For the application of this invention, both oral and non-oral routes (parenteral or dermal) are acceptable.

[0019] When the medicine of the present invention is administered orally, it can be given to animals in the form of capsules, tablets, pills, powders, granules, fine granules, powders, syrups, enteric solvents, suspensions, pastes, or in combination with beverages or feed.

[0020] When used via non-oral routes (parenteral or dermal), it can be formulated as injections, drops, suppositories, emulsions, suspensions, drops, ointments, creams, liquid preparations, lotions, sprays, aerosols, poultices, or patches for administration to animals.

[0021] Methods of application to animals include spot-on treatment (applying drops to the skin on the back of the shoulder blade to repel external parasites), pour-on treatment (applying liquid medication along the dorsal midline of the animal to spread the medication on the body surface to control external parasitic pests), and other local treatment methods. In addition, methods include treatments that use collars to carry or release medication, treatments that directly apply liquid preparations or ointments to the body surface, methods that use sprayers to treat aerosols, methods that inject medications into the muscle or subcutaneous tissue, and methods that administer suppositories rectally.

[0022] When the compounds and formulations of the present invention are used as parasite exterminants, the optimal dosage varies depending on whether it is for treatment or prevention, the type of parasite, the type and severity of infection, the dosage form, etc. Generally, in the case of oral administration, the dosage ranges from approximately 0.0001 mg / kg to 10,000 mg / kg body weight per day. In the case of non-oral administration, the dosage ranges from approximately 0.0001 mg / kg to 10,000 mg / kg body weight per day, and it can be administered once or in divided doses.

[0023] The concentration of the active ingredient in the formulation of the present invention is typically 0.0001 to 100% by weight, preferably 0.001 to 99% by weight, and more preferably about 0.005 to 80% by weight. Parasite repellents are generally available in high concentrations and can be diluted to an appropriate concentration before use.

[0024] In this invention, pest control in places or equipment that cattle come into contact with includes killing or driving away parasites in places and equipment that cattle may come into contact with, such as pastures, pens, transport vehicles, slaughterhouses, feeding devices, milk pumps, and manure slats. Pest control can be carried out by spraying, pouring, soaking, wiping, and other methods.

[0025] In addition to oxadiazon, the formulation of this invention may further contain other commonly known active ingredients. Examples of other active ingredients include, for instance, pyrethroids such as benzyl chlorpyrifos, d-phenylephrine, allethrin, pyrethroids, propargite, deltamethrin, cypermethrin, fenvalerate, cypermethrin, tetrafluorobenzyl chlorpyrifos, methoxyfenozide, benzylfenozide, cypermethrin, cis-cypermethrin, bifenthrin, deltamethrin, lambda-cyhalothrin, d,d-trans-phenylephrine, methamidophos, and ethionyl chlorpyrifos; organophosphates such as dichlorvos, chlorpyrifos, fenthion, chlorpyrifos, methyl chlorpyrifos, malathion, methamidophos, fenitrothion, and diazinon. N-phenylpyrazole compounds such as fipronil; carbamate compounds such as propoxur, carbaryl, oxadiazon, oxadiazon, and sec-butylcarbamate; neonicotinoid compounds such as imidacloprid, thiamethoxam, thiamethoxam, acetamiprid, acetamiprid, and dinotefuran; diamide compounds such as chlorantraniliprole, bromocyanamide, and flufenoxuron; insect growth controllers such as acetamiprid, pyriproxyfen, clofenuron, phenoxycarb, chlorfenapyr, and cyclophosphamide; milbemime, milbemime, lepidocrocin, abamectin, ivermectin, slaquindine, spinosad, and rotenone. Detailed Implementation

[0026] The following examples are for illustrative purposes only and should not be construed as limiting the invention in any way. The scope of protection of this invention is defined by the claims.

[0027] The raw materials for preparing the compounds of this invention can be purchased commercially or prepared by methods known in the literature or as detailed in the description. Those skilled in the art will understand that the compounds of this invention can also be synthesized using other synthetic routes.

[0028] Bioactivity assay:

[0029] Bioactivity tests were conducted on different concentrations of the compound to evaluate its insecticidal activity against unfed larvae and fed females of the southern cattle tick (Rhipicephalus microplus) and unfed adults (males and females) of the brown dog tick (Rhipicephalus linnaei). The reagents used in the tests shown below are either commercially available or readily prepared by those skilled in the art.

[0030] (1) Immersion test of southern cattle tick (Rhipicephalus microplus) satiated with female ticks

[0031] The inhibition of oviposition by the compound on female ticks of the target pest was tested using a saturated female tick immersion test. Saturated female ticks were weighed using an analytical balance and divided into groups with similar weights (p>0.05) (each group contained 10 ticks). Then, the female ticks were immersed in 10 mL of solution for five minutes. The concentrations of the acaricide in the solution were 0.19, 0.39, and 0.78 ppm (=μg / mL), and a solvent control group was set up.

[0032] After immersion, each group of female ticks (one female = 1 experimental unit) was placed on a paper towel to remove excess solution, then weighed individually and transferred to cell culture plates (one tick per well = one replicate) to monitor biological parameters. The experimental groups were placed in a climate-controlled chamber. After oviposition and the death of satiated females, the egg masses laid by each female were weighed using an analytical balance, transferred to a plastic syringe, and placed in the climate-controlled chamber for hatching rate assessment.

[0033] The following biological parameters were evaluated: pre-oviposition female body weight (FWBO, mg), egg mass weight (EMW, mg), and larval hatching rate (LH, %). Based on these values, estimated reproductive index, control percentage, oviposition index, and oviposition inhibition index were calculated. The results of the control percentage and oviposition inhibition index are summarized in Table 1.

[0034] The calculation formula is as follows:

[0035]

[0036] Where: 1. EMW = Average egg mass weight – the average weight of the egg mass produced by each female.

[0037] 2. FWBO = Average weight of female insects before egg-laying – Average weight of female insects before they begin laying eggs after a period of satiating feeding.

[0038] 3. LH = Hatching Rate – The average visual estimate of the number of hatched larvae relative to the number of egg masses per female.

[0039] Table 1 Results of oviposition inhibition test on female southern cattle ticks (Rhipicephalus microplus)

[0040]

[0041] (2) Immersion test of unfed larvae of Rhipicephalus microplus

[0042] Fill a 1.5 mL conical plastic tube with the test solution and immerse approximately 500 unfed larvae in it for five minutes. During immersion, shake the tube vigorously, then pour out the solution. Add approximately 100 larvae to the center of filter paper, fold the filter paper in half, and seal the end with a clip. Perform five replicates (five filter paper packets containing approximately 100 larvae each). Test concentrations for each compound were 0.09, 0.19, and 0.39 ppm (μg / mL), with a solvent control group included. Each concentration was repeated five times.

[0043] The experiment was repeated four times. The filter paper packets were placed in a BOD incubator at a temperature of 27±1℃ and a relative humidity >80±5% for 24 hours. After this stage, the mortality rate was assessed and recorded in Table 2. The mortality rate is the percentage of dead larvae out of the tested larvae.

[0044] Table 2 Results of the kill test on the larvae of the southern cattle tick (Rhipicephalus microplus)

[0045]

[0046] (3) Immersion test of unfed brown dog ticks (Rhipicephalus linnaei)

[0047] An immersion test was conducted on unfed adult ticks. Five unfed adult ticks were immersed in a test tube containing 25 mL of solution for five minutes. During immersion, the plastic tube was shaken vigorously, and then the solution was poured out. The adult ticks were placed on a paper towel to remove excess solution. Subsequently, the ticks were transferred to a test tube without insecticide. The test concentrations were 3.12, 6.25, 25, 50, and 250 ppm (= μg / mL).

[0048] Each concentration was repeated five times (one replicate per test tube). Test tubes containing ticks were placed in a climate-controlled room at 27 ± 1°C and 85 ± 5% relative humidity (RH). Mortality was assessed at 24, 48, 72, and 96 hours and recorded in Table 3. Ticks that did not move after stimulation were considered dead. Mortality rate was the percentage of dead adult ticks out of the tested larvae.

[0049] Table 3 Results of the control test on adult brown dog ticks (Rhipicephalus linnaei)

[0050]

[0051] Note: N represents no data; control compound A: .

[0052] Meanwhile, numerous tests have shown that the compounds and their preparations described in this invention have a good killing effect on adult and larval parasites such as ticks on host cattle, and can also inhibit the egg-laying and hatching of female ticks, resulting in good prevention and control effects. Furthermore, no abnormalities were observed in the host cattle after the medication was administered.

Claims

1. The application of oxadiazon or a formulation containing oxadiazon in the control of parasites on host animals, characterized in that, The parasite is an animal of the superfamily Ixodidae.

2. The application according to claim 1, characterized in that, The ticks are selected from at least one of the following: *Rhipicephalus microplus*, *Rhipicephalus sanguineus*, *Boophilus microplus*, *Ixodes persulcatus*, *Dermacentornuttalli*, and *Hyalomma asiaticum*.

3. The application according to claim 1 or 2, characterized in that, The host animal is a cow.

4. The application according to any one of claims 1-3, characterized in that, The applications include administering oxadiazon or a formulation containing oxadiazon to a host animal via oral, parenteral, or dermal routes.

5. The application according to any one of claims 1-4, characterized in that, The formulation also includes conventional adjuvants.

6. The application according to claim 5, characterized in that, The conventional additives include carriers.

7. The application according to any one of claims 1-6, characterized in that, The formulation also includes other active ingredients.

8. A method for removing parasites from a host animal for non-therapeutic purposes, comprising the step of administering oxadiazon or a preparation containing oxadiazon to the host animal or its contact site or equipment for the removal of parasites, wherein the parasites are ticks.

9. The removal method as described in claim 8, characterized in that, The ticks are selected from at least one of the following: *Rhipicephalus microplus*, *Rhipicephalus sanguineus*, *Boophilus microplus*, *Ixodes persulcatus*, *Dermacentornuttalli*, and *Hyalomma asiaticum*.

10. The removal method as described in claim 8 or 9, characterized in that, The host animal is a cow.

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