EP1215964A4 - Traitement cutane par deversement pour mouton - Google Patents

Traitement cutane par deversement pour mouton

Info

Publication number
EP1215964A4
EP1215964A4 EP20000963179 EP00963179A EP1215964A4 EP 1215964 A4 EP1215964 A4 EP 1215964A4 EP 20000963179 EP20000963179 EP 20000963179 EP 00963179 A EP00963179 A EP 00963179A EP 1215964 A4 EP1215964 A4 EP 1215964A4
Authority
EP
European Patent Office
Prior art keywords
formulation
pour
previous
active
sheep
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP20000963179
Other languages
German (de)
English (en)
Other versions
EP1215964A1 (fr
Inventor
Colin Manson Harvey
Morgan John Mcarthur
Ivor Blair Loveridge
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ashmont Holdings Ltd
Original Assignee
Ashmont Holdings Ltd
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 Ashmont Holdings Ltd filed Critical Ashmont Holdings Ltd
Publication of EP1215964A1 publication Critical patent/EP1215964A1/fr
Publication of EP1215964A4 publication Critical patent/EP1215964A4/fr
Withdrawn legal-status Critical Current

Links

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
    • A01N43/90—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system

Definitions

  • This invention relates to the field of veterinary compositions, and more panicularly anthelmintic compositions suitable for topical application to ovine.
  • the present invention relates to a pour-on formulation suitable for administration to sheep for the control internal and external parasites, which includes an active selected from the group of avermectins and milbemvcins. at least one solvent, and one or more penetratins agents.
  • the pour on formulation as claimed is capable of registration (or is registered) as a licensed Animal Remedy (by this we mean that it meets the regulatory requirements of a veterinary product (typically called an Animal Remedy) in the country in which it is to be sold/used. For example in New Zealand this has hitherto involved registration as a licensed 5 Animal Remedy under the Animal Remedies Act. or in Australia it requires registration with the National Registration Authority.
  • the active is selected from the group comprising abamectin, ivermectin, doramectin and moxidectin.
  • the active is present in the range 1 -4%w/v.
  • the penetrating agent is selected from the group including polyethylene glycol, glycol ethers and aromatic solvents.
  • the penetrating agent is dipropylene glycolmethyl ether, xylene. toluene or butyl dioxitol (also known as diethylene glycol butyl ether (DGBE).
  • DGBE diethylene glycol butyl ether
  • a panicularly preferred glycol ether is butyl dioxitol.
  • composition will include a water soluble organic solvent for dissolving the anthelmintic.
  • the solvent is selected from the group comprising benzyl alcohol, ethyl lactate and glvcerol formal.
  • the pour-on formulation also includes a spreading agent.
  • the solvent is present in the range of 1 -50% w/v.
  • the composition is able to safely deliver a dose of 2-4 m/kg of active to control internal and external parasites.
  • composition provides effective blood levels of active in the range of 2-5 ng/ml.
  • the endo parasites controlled are parasitic gastro-intestinal nematodes of ovine and the control achieved results in at least a 95% reduction in faecal egg counts.
  • the formulation is effective where the ecto parasites to be controlled are lice and psoroptic mange.
  • the invention provides a stable pour-on formulation for treatment of both internal and external parasites of sheep containing an active selected from the class of avermectins and milbemycins.
  • the formulation is designed to rapidly penetrate the fleece to provide a measurable therapeutic blood level of the active, and wherein the formulation contains: (i) a solvent selected from the group comprising benzyl alcohol, ethyl lactate and glycerol formal, and (ii) a penetrating agent selected from the group comprising propylene glycol. glycol ethers and aromatic solvents, and (iii) a spreading agent.
  • the active is one or more of abamectin. ivermectin, doramectin or moxidectin.
  • the penetrating agent is a glycol ether and the formulation is capable of achieving effective blood levels in sheep of active in the range of 2-5ng/ml of blood, when the pour on is administered at a dose rate of 2-4mg of active per Kg of body weight.
  • the abamectin is dissolved In a premix of benzyl alcohol at 50°C. Crodamol GTCC is added and the formulation Is made up to volume with Butyl Dioxitol.
  • the formulation was found to be stable at both temperatures. Both batches were also subject to a BP microbiological challenge and were shown to be robust for general use.
  • the sheep were restrictively randomly allocated on the basis of sex and weight to groups as follows: ten animals to Group 1. fifteen animals to Group 2. Groups 1 and 2 were treated on Day 0 with Abamectin Pour-on formulation of Example 1 at a dose rate of 4mg avermectin Bi a /kg bodyweight. All lambs were 3 '/_ weeks off shears at the time of treatment.
  • Wool specimens were collected from animals in Group 1 immediately prior to treatment and on Days 1. 5. 1 1. 20. 40. 81 and 120 after treatment. The wool specimens were collected in 13-15 cm wide bands clipped around the circumference of the body between the withers and rump.
  • Wool specimens were analysed by WRONZ Developments. Wales. New Zealand. Plasma was harvested from the blood specimens and analysed, along with the tissue specimens by Amdel NZ Ltd. Auckland. New Zealand. All specimens were analysed for avermectin B ! a using HPLC with fluorescence detection.
  • the results obtained show the maximum mean plasma avermectin B i a concentration for animals treated with the pour-on formulation was reached 24 hours after treatment. This ranged from 12 to 72 hours in individual animals.
  • the mean plasma concentration was just above the limit of qtiantitation (LOQ) for the analytical method by Day 1 1 after treatment.
  • LOQ qtiantitation
  • avermectin B ⁇ d concentrations were elevated within 6 hours of treatment.
  • the group mean concentrations were at their highest 24 hours after treatment ( Figure 1 and Table 1 ).
  • the group mean concentration was just above the limit of quantitation of 1 ng/mL.
  • Table 1 Mean plasma avermectin B a concentrations (ng/mL) of sheep treated with Formulation 1 on Day 0
  • the pharmacokinetic parameters, including Cmax. Tmax, T ) 2 and AUC. are shown in Table 2.
  • the Cmax in most animals was reached at 24 hours, but this ranged from 12 to 72 hours in individual animals.
  • the Cmax was also variable, from 1 ng/mL in animal 510, to 26.3 ng/mL, in animal 519.
  • n a number of animals
  • the control group of animals had comparative parasite burdens to the other test animals but remained untreated throughout the trials.
  • the triflumuron treatment consisted of the application of a 2.5% composition of triflumuron.
  • the triflumuron was applied as a spray on.
  • a dose of 20ml per animal was applied.
  • diflubenzuron concentrate was diluted to 0.0625% and jetted onto target animals at a rate of 1 L per animal.
  • a 1% abamectin oil based composition was applied as a pour-on at a dose rate of 4mL/10kg.
  • the pour-on was applied at skin level along the midline of the back.
  • Trial 1 is the only one of the trials, which did not include the diflubenzuron treatment. As can be seen from Figure 2 there were no significant differences between the numbers of lice on sheep between the various treatment groups before treatment. However after lice treatments were administered all animals treated showed decreases in lice numbers. This was confirmed at the 1 month lice count. The most effective of the treatments at the 1 month stage was Formulation 1 which showed a 99% decrease in lice numbers. The triflumuron treatment similarly showed a decrease although this did not reach 98% until the lice count at the end of month 2. From month 3 to 5 the lice kill was 100%) for both treatments.
  • Trial 2 involved 40 female hoggets. Comparison was made between treatments as described above (treatments 2-4). Specifically the 40 animals were randomly allocated to 5 groups, 1 untreated control group, a second treated with EXITTM (triflumuron spray-on), a third with FleeceMasterTM (diflubenzuron jetting fluid) and a fourth group treated with the formulation. The final group was an untreated control group used to provide louse challenge to the treated group. The untreated control groups were run separately from the treated groups.
  • This trial was similar to trial 2 in that all three treatments were compared. However only one control (untreated) group was used. All three treated groups were run together. The untreated control group was run separately.
  • the formulations of the present invention advantageously provides stable safe formulations of active that rapidly penetrate the fleece to obtain therapeutic blood levels as well as spreading quickly within the animal achieving a high level of control of ecto as well as endoparasites in ovine.
  • formulations of the present invention are stable over time to allow their practical use on sheep.
  • the formulations are safe for both sheep and man. There is no undue irritation and residue levels that result from the use of the present invention reach acceptable levels in a practical time for farmers.
  • the formulations do not damage the valuable wool present on the animal or attract dust or other foreign matter to the fleece.
  • the formulations give measurable therapeutic blood levels of the active and give a high level of control in excess of 95% of the population of external parasites such as lice and internal nematodes of all major species.
  • formulations may be varied by using a variety of different spreading agents or thickeners, in addition to or in place of those described herein.
  • Suitable spreading agents for inclusion in the compositions of the present invention include crodamol GTCC and dowanol DPM.
  • SuittlBle thickeners for inclusion in the compositions of the present invehtidii ihtlttde oat tiled flour, methancel and xanthan gum.
  • a solvent may function as both a solvent and penetrating agent, although in all of our examples we have used different ingredients for these two functions.
  • Additional penetrating agents may be used in conjunction with the general class of penetrating agents mentioned in the description and in the claims.

Landscapes

  • 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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne une préparation pour traitement cutané par déversement destiné au traitement des endoparasites et des ectoparasites chez un mouton. L'actif est une avermectine ou une milbemycine. La préparation est conçue pour pénétrer rapidement dans la toison de manière à fournir une concentration sanguine thérapeutique de l'actif pouvant être mesurée. La préparation contient de l'alcool benzylique comme solvant; du butyl dioxitol comme agent de pénétration, et un mouillant tel qu'un crodamol GTCC et un dowanol DPM.
EP20000963179 1999-09-22 2000-09-22 Traitement cutane par deversement pour mouton Withdrawn EP1215964A4 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
NZ33795299 1999-09-22
NZ33795299 1999-09-22
PCT/NZ2000/000185 WO2001020994A1 (fr) 1999-09-22 2000-09-22 Traitement cutane par deversement pour mouton

Publications (2)

Publication Number Publication Date
EP1215964A1 EP1215964A1 (fr) 2002-06-26
EP1215964A4 true EP1215964A4 (fr) 2002-11-05

Family

ID=19927520

Family Applications (1)

Application Number Title Priority Date Filing Date
EP20000963179 Withdrawn EP1215964A4 (fr) 1999-09-22 2000-09-22 Traitement cutane par deversement pour mouton

Country Status (4)

Country Link
EP (1) EP1215964A4 (fr)
AU (2) AU7463000A (fr)
WO (1) WO2001020994A1 (fr)
ZA (1) ZA200202557B (fr)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA05010659A (es) * 2003-04-04 2005-12-12 Merial Ltd Formulaciones veterinarias antihelminticas topicas.
AU2013201461B2 (en) * 2007-11-26 2015-10-29 Boehringer Ingelheim Animal Health USA Inc. Solvent systems for pour-on formulations for combating parasites
WO2009070687A1 (fr) * 2007-11-26 2009-06-04 Merial Limited Systèmes de solvants pour solutions à application cutanée, utilisables dans le cadre de la lutte contre les parasites
GB2516398B (en) * 2012-05-03 2020-04-29 Norbrook Lab Ltd Avermectin pour-on formulation with reduced withdrawal time

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0146414A2 (fr) * 1983-12-22 1985-06-26 Merck & Co. Inc. Formulation non-aqueuse antiparasitaire contenant une avermectine ou une milbémycine
GB2275193A (en) * 1993-02-17 1994-08-24 Merck & Co Inc Formulations for the topical delivery of avermectins
WO1995005812A1 (fr) * 1993-08-24 1995-03-02 Ashmont Holdings Limited Formulations anti-helminthiques
US5550153A (en) * 1994-11-14 1996-08-27 Kerz; Phillip D. Method for treating heartworm-infected canines
WO2000004906A1 (fr) * 1998-07-24 2000-02-03 Norbrook Laboratories Limited Composition vermifuge non aqueuse
WO2000061068A2 (fr) * 1999-04-14 2000-10-19 Ashmont Holdings Limited Composition anthelmintique

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ209100A (en) * 1983-08-22 1987-01-23 Ici Australia Ltd Topical compositions for control of endoparasites
AU664134B2 (en) * 1994-01-28 1995-11-02 Wyeth Holdings Corporation Pour-on formulations effective for the control of internal and external parasites of homothermic animals
US5773422A (en) * 1996-01-29 1998-06-30 Komer; Gene Avermectin formulation
EP0836851A1 (fr) * 1996-10-21 1998-04-22 Virbac S.A. Composés d'amidine pour le traitement des maladies ecto-/u endoparasitaires et compositions systémiques pour le contrÔle des parasites
DE19654079A1 (de) * 1996-12-23 1998-06-25 Bayer Ag Endo-ekto-parasitizide Mittel
RU2124895C1 (ru) * 1998-05-28 1999-01-20 Головкина Любовь Павловна Противопаразитарная мазь "авермектиновая"
GB9825402D0 (en) * 1998-11-19 1999-01-13 Pfizer Ltd Antiparasitic formulations

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0146414A2 (fr) * 1983-12-22 1985-06-26 Merck & Co. Inc. Formulation non-aqueuse antiparasitaire contenant une avermectine ou une milbémycine
GB2275193A (en) * 1993-02-17 1994-08-24 Merck & Co Inc Formulations for the topical delivery of avermectins
WO1995005812A1 (fr) * 1993-08-24 1995-03-02 Ashmont Holdings Limited Formulations anti-helminthiques
US5550153A (en) * 1994-11-14 1996-08-27 Kerz; Phillip D. Method for treating heartworm-infected canines
WO2000004906A1 (fr) * 1998-07-24 2000-02-03 Norbrook Laboratories Limited Composition vermifuge non aqueuse
WO2000061068A2 (fr) * 1999-04-14 2000-10-19 Ashmont Holdings Limited Composition anthelmintique

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; CHEN, XIZHAO ET AL: "Study on pour-on preparation of abamectin", XP002216644, retrieved from STN Database accession no. 128:175852 CA *
See also references of WO0120994A1 *
ZHONGGUO NONGYE KEXUE (BEIJING) (1997), 30(3), 74-78, 1997 *

Also Published As

Publication number Publication date
AU7463000A (en) 2001-04-24
AU733095B3 (en) 2001-05-03
WO2001020994A1 (fr) 2001-03-29
ZA200202557B (en) 2002-08-28
EP1215964A1 (fr) 2002-06-26

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