Antiparasitic isoxazoline compounds, long-acting injectable formulations containing them, methods and uses thereof

By developing long-acting injectable compositions containing isoxazoline compounds, liquid PEGs and neutral oils, the problems of insufficient bioavailability and large stimulation of injection sites in the prior art are solved, and rapid and efficient prevention and control of fleas and ticks are achieved, and parasite control of various animals and crops are suitable for parasite control.

CN114573573BActive Publication Date: 2025-07-25BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC
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Patent Information

Application Number
CN202210192289.6
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Priority Date
2016-08-25
Filing Date
2017-02-24
Publication Date
2025-07-25
Estimated Expiration
2037-02-24

AI Technical Summary

Technical Problem

The existing isoxazoline active agent compositions have shortcomings in terms of bioavailability and sustained efficacy, especially in long-acting injectable compositions, the prevention and treatment of fleas and ticks is poor, and the injection site is highly irritated.

Method used

Develop long-acting injectable compositions containing an antiparasitic effective amount of isoxazoline compound, liquid PEG and pharmaceutically acceptable neutral oil, combined with optional co-solvents and additives, avoiding the use of pharmaceutically biodegradable polymers, increasing bioavailability and reducing injection site irritation.

Benefits of technology

It has achieved rapid onset and long-term prevention and control of parasites such as fleas and ticks, reduced stimulation at the injection site, and provided a suitable safety spectrum, suitable for parasite control in a variety of animals and crops.

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Abstract

The present invention relates to a long-acting injectable composition for combating parasites in animals, which comprises at least one isoxazoline active agent, a liquid PEG and / or a neutral oil, an optional co-solvent, and an optional pharmaceutically acceptable additive or excipient. The present invention also provides a new isoxazoline active agent having a persistent effect against ectoparasites. The present invention further provides an improved method for eradicating, controlling and preventing parasite infections and infestations in animals, which method comprises administering to an animal in need thereof the new isoxazoline compound and the long-acting injectable composition of the present invention.
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