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WO2001011961A1 - Lutte contre les ectoparasites au moyen de spinosynes - Google Patents

Lutte contre les ectoparasites au moyen de spinosynes Download PDF

Info

Publication number
WO2001011961A1
WO2001011961A1 PCT/US2000/017869 US0017869W WO0111961A1 WO 2001011961 A1 WO2001011961 A1 WO 2001011961A1 US 0017869 W US0017869 W US 0017869W WO 0111961 A1 WO0111961 A1 WO 0111961A1
Authority
WO
WIPO (PCT)
Prior art keywords
formulation
sheep
ppm
spinosyn
wool
Prior art date
Application number
PCT/US2000/017869
Other languages
English (en)
Inventor
Kristina Clare Hacket
Lionel Barry Lowe
James Terence Rothwell
Original Assignee
Eli Lilly And Company
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Eli Lilly And Company filed Critical Eli Lilly And Company
Priority to AU66053/00A priority Critical patent/AU6605300A/en
Publication of WO2001011961A1 publication Critical patent/WO2001011961A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
    • A01N43/02—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms
    • A01N43/04—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom
    • A01N43/22—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atoms with one hetero atom rings with more than six members

Definitions

  • This invention relates to A83543 compounds including analogues and
  • insects have been caused, and continues to be caused, by pests such as insects. Insects particularly
  • insects Approximately 1% of insects
  • insects are considered to be the carriers of more than 250 viruses
  • insecticide compositions It is estimated that there are at least 35,000 formulated
  • insecticide products worldwide with chemicals as the active ingredients.
  • Such insecticide products include antimicrobials, larvicides, insecticides, animal dips,
  • Plant-derived insecticides such as nicotine, rotenone, veratrine and
  • pyrethrum have also been used as natural contact insecticides to kill insect pests.
  • organophosphates are potentially toxic to sheep, goats, other small ruminants
  • organophosphate synthetic pyrethroid or insect growth regulator insecticides
  • Aqueous wool scouring produces high volumes of effluent containing
  • insecticide residues can kill
  • That wool in a greasy form. That wool may be scoured and processed in many
  • Tissue residues are also a major concern when considering use of
  • insecticides are not without their problems, such as the difficulty in applying them, as
  • Chemosterilants which sterilise large segments of insect pest
  • Fermentation product A83543, also known as spinosyn includes a
  • spinosyns produced by Saccharopolyspora spinosa.
  • spinosyns B Compared to spinosyn A, spinosyns B
  • strains of S.spinosa produce a mixture of spinosyns, the primary components of
  • spinosyn A 50-85%
  • spinosyn D 15-50%)
  • spinosad refers to a mixture of spinosyn A and spinosyn D.
  • the present invention provides an insecticidal formulation for
  • the formulation may additionally
  • the amount of the spinosyn comprises another insecticidal agent.
  • the amount of the spinosyn comprises another insecticidal agent.
  • present in the formulation is such that the spinosyn residue in any wool, milk or tissue
  • the amount of spinosyn in the formulation is selected from the formulation.
  • the amount of spinosyn in the formulation is selected from the formulation.
  • a preferred amount is 25 g/L.
  • this invention relates to an article of manufacture
  • a topical unit dose of a formulation of this invention i.e. one comprising an
  • This invention further relates to a use of a formulation of this
  • this invention provides the use of a formulation of
  • this invention i.e. one comprising an elective amount of a spinosyn, or an analogue
  • ectoparasite infestation in a small ruminant animal selected from a sheep, goat, or
  • camellid comprising topically administering the formulation to the animal.
  • This invention further provides a method of controlling an ectoparasite
  • a formulation of the invention i.e., one comprising an
  • the amount of spinosyn in the formulation is such that the spinosyn residue in any
  • the present invention provides formulations and methods of
  • insects and arachnids in small ruminant animals such as sheep, goats and camellids
  • A83543 compounds by applying one or more A83543 compounds in an acceptable carrier or diluent.
  • Another aspect of this invention is a method for preventing, controlling
  • insects including ectoparasites in small ruminant animals by
  • insecticide including one or more
  • the invention also provides a method for controlling an ectoparasitic
  • the ectoparasite includes lice, fleas, ked, mites, itch mites, ticks
  • spinosyn or an analogue or derivative thereof, at a concentration of about 50 ppm or
  • concentration of about 50 ppm of spinosyn is achieved by administering an amount of
  • the invention further provides a method for controlling an
  • ectoparasitic infestation wherein the ectoparasite includes lice, ked and blowfly
  • sheep are about 10, 3, and 1 ppm of spinosyn in the formulation.
  • the invention provides a method for controlling an
  • the spinosyn in the sheep is present in an environmentally acceptable amount
  • sheep are about 25, 20, or 10 ppm.
  • Still another aspect of this invention provides a method for controlling
  • Another aspect of this invention provides a method for controlling an
  • an analogue or derivative thereof at a concentration of about 50 ppm or less , such
  • 'insect' is defined to include, but is not
  • Phthiraptera and Acarina, and parasites and other insects which are parasitic during
  • 'small ruminant' or 'small ruminant animal' refers to sheep
  • goats or camellids including alpacas, llamas and vacuna, etc.
  • A83543 compound is also used herein to mean an
  • controlling an insect infestation refers to preventing onset
  • 'effective amount means the amount which is sufficient to
  • the term 'short wool sheep' means sheep with 6 weeks or less growth
  • 'withholding period means the period after treatment during
  • the withholding period of course differs in respect of the chemical nature of the
  • Meat (mammalian in the fat) has an
  • allowable amounts depend on the aquatic toxicity profile of the chemical.
  • concentration of spinosad is estimated to be approximately 15 mg/kg or higher.
  • This invention is based on the surprising discovery in sheep that the
  • spinosyns i.e. a spinosyn factor or an analogue and derivative thereof, exhibit
  • insecticidal activity at very low concentrations, much lower than those used or
  • spinosyn compounds have 100% efficacy as insecticides, particularly ectoparasiticides.
  • Spinosyn compounds are usually in the form of either an emulsion
  • formulations can be supplied as dilute ready-to-use
  • invention is of utility against parasite populations on sheep or small ruminants that
  • formulations of the present invention can be any formulations of the present invention having existing levels of resistance to currently used products.
  • the formulations of the present invention can be any formulation of the present invention having existing levels of resistance to currently used products.
  • the formulations of the present invention can be any formulation of the present invention having existing levels of resistance to currently used products.
  • camellids including alpacas, llamas and vacuna etc.
  • Such pests include
  • ectoparasites such as blowfly strike, lice, ked, mites, itch mite, sheep scab, screw
  • the spinosyns can be
  • Formulations containing the spinosyns are generally administered
  • Topical application can take the form of
  • Topical insecticidal formulations include spot-ons, pour ons, sprays,
  • suspensions are preferred. More preferred are dip wash formulations, jetting fluid
  • the active component-the spinosyn factor/compound- may be present
  • A83543A and A83543D or a mixture of at least one A83543 compound
  • One preferred active component used in the method of the present invention is
  • spinosad which is a product comprised of 50-85% spinosyn A and 50-15% spinosyn
  • the active component-the spinosyn factor/compound- may also be any active component-the spinosyn factor/compound-.
  • spinosyn A can be any organic compound having the same side chain prepared using standard procedures for salt preparation.
  • spinosyn A can be any organic compound having the same side chain prepared using standard procedures for salt preparation.
  • spinosyn A can be any organic compound having the same side chain prepared using standard procedures for salt preparation.
  • salts formed by reaction with either an organic or inorganic acid such as, for example
  • the spinosyn factor/s or analogues or derivatives thereof can be mixed
  • compositions of the present invention can take the form of
  • the formulations of the active spinosyn compound are in
  • emulsifiable formulations are generally liquids, generally called emulsifiable
  • the active formulations are in the form
  • Emulsifiable concentrates and solution concentrates as
  • a preferred concentration range is 1-500 g/L of
  • concentration range is selected from the
  • Useful organic solvents include aromatics
  • terpenic solvents including rosin derivatives, aliphatic ketones such as
  • SC Suspension concentrates
  • water-insoluble compound including one or more spinosyn compounds
  • an aqueous vehicle at a concentration in the range of from about 1-500 g/L.
  • concentration range is selected from the group consisting of about 1-
  • suspensions are prepared by finely grinding
  • surfactants chosen from such types as nonionic, sulfonated lignins and alkylsulfates
  • suspending agents such as xanthan and guar gums.
  • Other inert ingredients may be used.
  • the suspension concentrates and emulsions are preferably diluted with
  • the active A83543 compounds can also be any active A83543 compounds applied in the methods of the invention.
  • the active A83543 compounds can also be any active A83543 compounds.
  • composition In such compositions, the active spinosyn compound is dissolved in an
  • inert carrier which is a propellant mixture.
  • formulations of the invention include dust carriers, solvents, emulsif ⁇ ers, wetting and
  • the insecticide takes the form of an
  • Wettable powders can be used as spray
  • carrier such as an absorbtive clay
  • the method of the invention can be applied as an early
  • the active spinosyn compound or compounds are any active spinosyn compound or compounds.
  • ppm 25 ppm, 20 ppm, 10 ppm, 5 ppm, 4 ppm, 3 ppm, 2 ppm, or 1 ppm.
  • a preferred composition for use in the present methods of treatment is
  • a dispersant may be added to improve suspendability.
  • a preferred formulation contains the following ingredients: Ingredient Percent (w/w) Sample batch (2)
  • the spinosyn is wet-
  • grind batch i.e., spinosad, surfactant, water, and antifoam as needed.
  • a "hydrated suspension batch” is also formed by blending a hydrated
  • a typical hydrated suspension batch contains the
  • a particularly useful mineral thickener is colloidal magnesium
  • aluminum silicate such as VEEGUM, that disperses and wells in water.
  • xanthan gum in one that is heat stable with a good tolerance for strongly acidic and
  • emulsifiable concentrates containing spinosad can be made and used for
  • emulsifiable concentrate can be prepared in an aromatic hydrocadrbon such as
  • Aromatic 150 containing the following ingredients: spinosad (90% active ingredient,
  • treating ectoparasites in sheep can be performed in the following manner:
  • sheep should be hand jetted with about 25 ppm spinosad; 0.5 L should be used per
  • Example 1 Spinosad Dip Formulations for the Control of Bovicola Ovis on Sheep
  • Subsections (a) - (g) provide the lice counts observed with the control animals and
  • Example 2a Dose determination for the treatment of sheep body lice
  • emulsifiable concentrate was diluted 1 :1000 in water to obtain formulations of 0, 1.0,
  • suspension concentrate (25 g/L) was diluted in water to give 0, 2, 5, 15 and 45 ppm
  • control sheep i.e., those treated with 0 ppm
  • Example 2b Evaluation of spinosad for the treatment of blowfly strike on sheep caused by Lucilia cuprina
  • spinosad were diluted 1 : 1000 in water to give emulsions of 2, 5, 15, 45 and 135 ppm.
  • maggots Each site was examined for maggot survival and development 24, 48 and 72
  • Example 2c Evaluation of spinosad for the treatment of sheep ked (M. ovinus)
  • Example 3a Dose confirmation and protection period for the treatment of sheep body lice (Bovicola ovis) i) Short wool sheep, application ⁇ six (6) weeks after shearing in the form of a dip
  • ppm spinosad were sampled on days 1, 2, 4, 7, 9, 11, 14, 17 and 21 post treatment
  • Example 5 Spinosad residues in sheep meat, fat and offal four days following dipping in 50 ppm spinosad dip formulation
  • Two previously sheared sheep were dipped in an aqueous suspension dip formulation containing 50 ppm spinosad for 30 seconds, with the head being dunked twice, and then placed in a floor pen for four days.
  • the sheep were sacrificed and necropsied at the end of those four days; and samples of kidney, liver, muscle, perirenal and abdominal fat were collected.
  • the tissues were transferred to a -20°C freezer until processing.
  • the tissue samples were chopped, frozen with dry ice and then ground using a hammermill. The samples were then placed in a -20°C freezer until assay.
  • Example 6 Measurement of the residue decay profile of spinosad in sheep wool following dipping in 10 ppm spinosad and jetting with 25 ppm spinosad.
  • the wool in a processing lot is made up of wools treated in early season, wools treated in late season, untreated wools, and wools treated with other chemicals. This blending will allow the spinosad residue from any farm to be diluted by these other wools. Therefore treatment of sheep with spinosad at the recommended rates will not cause wool residues to breach any wool scour environmental parameters and will not require the establishment of a wool with-holding period following treatment.
  • Spinosad has a high margin of safety for farm workers due to the short half-life of spinosad in wool grease, the very low level of dermal absorption and low mammalian toxicity of the active ingredient. Sheep treated with spinosad present no risk to shearers, wool handlers or other farm workers.
  • Example 7 Tissue residues following dipping in 10 ppm spinosad and jetting with 25 ppm spinosad. Thirty seven fine wool Merino ewes and wethers with 6 weeks wool
  • the limit of quantification (LOQ) was 0.01 mg/kg and the limit of detection (LOD)

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  • Life Sciences & Earth Sciences (AREA)
  • Agronomy & Crop Science (AREA)
  • Pest Control & Pesticides (AREA)
  • Plant Pathology (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Dentistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Environmental Sciences (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention concerne des formulations permettant de lutter contre les insectes et animaux nuisibles chez de petits ruminants tels que des camélidés, des ovins et des caprins. Ces formulations renferment une dose efficace de spinosyne, ou bien un analogue ou un dérivé de cette substance ainsi qu'un excipient ou un diluant acceptable. L'invention concerne également des méthodes de lutte contre ces insectes, notamment l'application topique de ces formulations sur un ruminant.
PCT/US2000/017869 1999-08-12 2000-07-31 Lutte contre les ectoparasites au moyen de spinosynes WO2001011961A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU66053/00A AU6605300A (en) 1999-08-12 2000-07-31 Control of ectoparasites using spinosyns

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14852499P 1999-08-12 1999-08-12
US60/148,524 1999-08-12

Publications (1)

Publication Number Publication Date
WO2001011961A1 true WO2001011961A1 (fr) 2001-02-22

Family

ID=22526135

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/017869 WO2001011961A1 (fr) 1999-08-12 2000-07-31 Lutte contre les ectoparasites au moyen de spinosynes

Country Status (3)

Country Link
AU (1) AU6605300A (fr)
CO (1) CO5221104A1 (fr)
WO (1) WO2001011961A1 (fr)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6664237B1 (en) 1999-08-12 2003-12-16 Eli Lilly And Company Oral treatment of companion animals with ectoparasiticidal spinosyns
US6927210B1 (en) 1999-08-12 2005-08-09 Eli Lilly And Company Ectoparasiticidal aqueous suspension formulations of spinosyns
US6933318B1 (en) 1999-08-12 2005-08-23 Eli Lilly And Company Topical organic ectoparasiticidal formulations
US6955818B1 (en) 1999-12-02 2005-10-18 Eli Lilly And Company Pour-on formulations
WO2005112950A1 (fr) * 2004-04-29 2005-12-01 Eli Lilly And Company Spinosynes pour la guérison des blessures
KR100855417B1 (ko) * 2006-10-27 2008-08-29 일라이 릴리 앤드 캄파니 스피노신을 포함하는 상처 치유용 제약 조성물
SG159395A1 (en) * 2004-04-29 2010-03-30 Lilly Co Eli Use of spinosyns for wound healing
US7772194B2 (en) 2001-09-17 2010-08-10 Eli Lilly And Company Pesticidal formulations

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0375316A1 (fr) * 1988-12-19 1990-06-27 DowElanco Composés macrolides
WO1998023158A1 (fr) * 1996-11-26 1998-06-04 Zeneca Limited Compositions insecticides et procedes
US5767253A (en) * 1992-11-06 1998-06-16 Dow Agrosciences Llc A83543 Compounds; factors Q, R, S, and T

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0375316A1 (fr) * 1988-12-19 1990-06-27 DowElanco Composés macrolides
US5767253A (en) * 1992-11-06 1998-06-16 Dow Agrosciences Llc A83543 Compounds; factors Q, R, S, and T
WO1998023158A1 (fr) * 1996-11-26 1998-06-04 Zeneca Limited Compositions insecticides et procedes

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
ABSTR.PAP.AM.CHEM.SOC. (217 TH NATIONAL MEETING OF THE AMERICAN CHEMICAL SOCIETY; MARCH 21-25, 1999) *
DATABASE BIOSIS BIOSCIENCES INFORMATION SERVICE, PHILADELPHIA, PA, US; *
DATABASE CROPU [online] D.H.DA ET AL.: "Dermal absorption and metabolism of spinosad in lactating goats", XP002153532, retrieved from EPOQUE accession no. PREV199900165412 *

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6664237B1 (en) 1999-08-12 2003-12-16 Eli Lilly And Company Oral treatment of companion animals with ectoparasiticidal spinosyns
US6927210B1 (en) 1999-08-12 2005-08-09 Eli Lilly And Company Ectoparasiticidal aqueous suspension formulations of spinosyns
US6933318B1 (en) 1999-08-12 2005-08-23 Eli Lilly And Company Topical organic ectoparasiticidal formulations
US6955818B1 (en) 1999-12-02 2005-10-18 Eli Lilly And Company Pour-on formulations
US8048861B2 (en) 2001-09-17 2011-11-01 Eli Lilly And Company Pesticidal formulations
US7772194B2 (en) 2001-09-17 2010-08-10 Eli Lilly And Company Pesticidal formulations
EA010975B1 (ru) * 2004-04-29 2008-12-30 Эли Лилли Энд Компани Применение спинозинов для заживления ран
SG159395A1 (en) * 2004-04-29 2010-03-30 Lilly Co Eli Use of spinosyns for wound healing
US7709447B2 (en) 2004-04-29 2010-05-04 Eli Lilly And Company Use of spinosyns for wound healing
AU2004319804B2 (en) * 2004-04-29 2010-08-05 Elanco Us Inc. Use Of Spinosyns For Wound Healing
WO2005112950A1 (fr) * 2004-04-29 2005-12-01 Eli Lilly And Company Spinosynes pour la guérison des blessures
US8536142B2 (en) 2004-04-29 2013-09-17 Eli Lilly And Company Spinosyns for wound healing
KR100855417B1 (ko) * 2006-10-27 2008-08-29 일라이 릴리 앤드 캄파니 스피노신을 포함하는 상처 치유용 제약 조성물

Also Published As

Publication number Publication date
AU6605300A (en) 2001-03-13
CO5221104A1 (es) 2002-11-28

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