Long-acting injectable formulations comprising an isoxazoline active agent, methods and uses thereof
AssigneeBoehringer Ingelheim Animal Health USA Inc.
InventorsSusan Mancini Cady, Peter Cheifetz, Izabela Galeska, Loic Le Hir de Fallois
Life of this patent
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Abstract
This invention relates to long-acting injectable formulations for combating parasites in animals, comprising at least one isoxazoline active agent, a poloxamer, and a co-solvent. This invention also provides for improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the long-acting injectable formulations of the invention to the animal in need thereof.
Claims21
A long-acting injectable formulation for the treatment of parasite infestations or infections in an animal comprising:
- a) about 5% to 30% (w/v) of an isoxazoline compound of Formula (Ib):
- or a pharmaceutically acceptable salt thereof
- wherein:
- R2 independently is halogen, C1-C6 alkyl or C1-C6 haloalkyl;
- R4 is H or C1-C6 alkyl;
- R5 is C1-C4 alkyl optionally substituted with one or more R7;
- and R7 is C2-C7 alkylcarbonyl, C2-C7 alkoxycarbonyl, C2-C7 alkylaminocarbonyl, C3-C9 dialkylaminocarbonyl, C2-C7 haloalkylcarbonyl, C2-C7 haloalkoxycarbonyl, C2-C7 haloalkylaminocarbonyl, C3-C9 dihaloalkylaminocarbonyl;
- and n is 0, 1 or 2;
- b) poloxamer 124 or poloxamer 181;
- c) about 5% to 40% (w/v) of a co-solvent selected from the group consisting of liquid polyethylene glycol, ethanol, isopropanol, and a mixture thereof;
- d) optionally, about 0.01% to about 2.0% (w/v) of an antioxidant;
- and
- e) optionally about 0.01% to about 5.0% (w/v) of a pharmaceutically acceptable additive, excipient or mixtures thereof;
- wherein the only pharmaceutically acceptable polymer present in said long-acting injectable composition is said poloxamer and wherein the poloxamer is present in the overall composition in a proportion representing the complement to 100% of the composition;
- and
- wherein the formulation treats parasitic infestations or infections for about 3 to 6 months.
A long-acting injectable formulation for the treatment of parasite infestations or infections in an animal comprising:
- a) about 5 to 30% (w/v) of an isoxazoline active compound of formula (Ia):
- or a pharmaceutically acceptable salt thereof;
- b) at least one pharmaceutically acceptable polymer which is a liquid poloxamer at room temperature (20-25° C.), wherein the liquid poloxamer is poloxamer 124 or poloxamer 181;
- c) about 5% to 40% (w/v) of a co-solvent selected from the group consisting of liquid polyethylene glycol, ethanol, isopropanol, and mixtures thereof;
- d) optionally, about 0.01% to about 2.0% (w/v) of an antioxidant;
- and
- e) optionally, at least one pharmaceutically acceptable additive, excipient or mixtures thereof;
- wherein no other pharmaceutically acceptable polymers are present;
- and wherein a single injection of the formulation provides at least 80% efficacy against parasitic infestations or infections for at least 3 months.
Dependencies are inferred from the claim text.