Parasiticidal collar comprising isoxazoline compounds
Inventors
Allan, James • BELL, Samuel David • EPE, Christian Helmut • Le Hir de Fallois, Loic Patrick • LEE, Willy W. • Locklin, Jason J.
Assignees
University of Georgia Research Foundation Inc • Boehringer Ingelheim Animal Health USA Inc
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Publication Number
US-12161089-B2
Publication Date
2024-12-10
Expiration Date
Abstract
Provided herein are long-acting antiparasitic devices comprising parasiticidal isoxazoline active agent for external use on an animal to treat and/or prevent parasitic infestations by ectoparasites, and in some embodiments, also parasitic infections. The disclosure also describes methods and uses of the antiparasitic external devices to treat and/or prevent parasitic infestations and/or infections in an animal.
Core Innovation
The invention relates to an antiparasitic external device for the treatment and/or prevention of a parasitic infection or infestation in an animal. The device comprises an effective amount of an isoxazoline active agent of formula (Ia) or (Id), including (S)-Ia or (S)-Id, dispersed in a polymer matrix comprising ethylene-vinyl acetate copolymer (EVA).
In embodiments, the EVA polymer matrix is specified by vinyl acetate content, including EVA with 5-50% vinyl acetate, and the formulation optionally comprises a plasticizer, and optionally a stabilizer and/or an antioxidant. The document also refers to stereoisomeric active agents, enantiomeric excess concepts, enrichment of a biologically more active (S)-enantiomer relative to the (R)-enantiomer, and named example tigolaner.
The disclosed formulations are presented as long-acting wearable external devices, notably an antiparasitic collar. The document describes long-duration and broad-spectrum antiparasitic activity against ectoparasites such as fleas and ticks.
Claims Coverage
Two independent claims are provided. The inventive features center on an antiparasitic external device in which an isoxazoline active agent of formula (Ia) or (Id) is dispersed in an EVA polymer matrix, with one claim broader and the other specifying EVA with 5-50% vinyl acetate and optional formulation components.
Isoxazoline active agent dispersed in EVA polymer matrix external device
An antiparasitic external device for the treatment and/or prevention of a parasitic infection or infestation in an animal comprising an effective amount of an isoxazoline active agent of formula (Ia) or (Id) and a polymer matrix comprising ethylene-vinyl acetate copolymer (EVA), wherein said isoxazoline active agent is dispersed in said polymer matrix.
EVA polymer matrix with vinyl acetate content and optional formulation components
An antiparasitic external device for the treatment and/or prevention of a parasitic infestation or infection in an animal comprising an effective amount of at least one parasiticidal active agent, which is a compound of formula (Ia) or (Id), and a polymer matrix which consists of ethylene-vinyl acetate copolymer (EVA) with 5-50% vinyl acetate, wherein said parasiticidal active agent is dispersed in said polymer matrix, optionally including a plasticizer and optionally including a stabilizer and/or an antioxidant.
The claims focus on an antiparasitic external device containing an isoxazoline active agent of formula (Ia) or (Id) dispersed in an EVA polymer matrix, with the second independent claim adding a 5-50% vinyl acetate limitation and optional plasticizer, stabilizer, and antioxidant.
Stated Advantages
Provides an antiparasitic external device for the treatment and/or prevention of parasitic infection or infestation in an animal.
Long-acting use as an antiparasitic external device is stated in the document.
Long-lasting efficacy is described for ectoparasites including fleas and ticks.
Broad-spectrum activity is described against ectoparasites such as fleas and ticks.
Drug distribution and pharmacokinetics are discussed in connection with measurable systemic levels after topical collar use, including presence of drug in dog hair and permeation through skin to blood.
Documented Applications
Animal treatment and/or prophylaxis using an antiparasitic external device with isoxazoline active agents dispersed in an EVA polymer matrix.
Treatment of a parasitic infestation and/or parasitic infection in an animal by applying the antiparasitic external device to an animal in need thereof.
Topical collar use.
Efficacy against ectoparasites including fleas and ticks, including in vitro flea efficacy and in vivo dog efficacy.
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