Isoxazoline parasiticide formulations
Inventors
Azamian, Bobak Robert • Ackermann, Douglas Michael • Hickok, Shawn D. • Vehige, Joseph G.
Assignees
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Publication Number
US-12364685-B2
Publication Date
2025-07-22
Expiration Date
Abstract
Disclosed herein are compositions which can be used in methods for treating or preventing ophthalmic and dermatologic conditions in a human subject, including ocular surface conditions such as blepharitis or rosacea. The compositions can be topically administered directly to an eye, eyelid, or eyelashes of the patient for targeted local activity.
Core Innovation
The invention relates to isoxazoline parasiticide ophthalmic compositions for treating or preventing Demodex-associated conditions. The document describes ophthalmic topical formulations in eye drop form and also in gel, ointment, or cream forms, where lotilaner is present as an isoxazoline parasiticide in a defined weight-percent range. The compositions are formulated for ophthalmic use.
The background problem addressed is Demodex-associated conditions, including blepharitis and ocular rosacea, in which Demodex folliculorum and Demodex brevis are implicated. The document associates the proposed antiparasitic activity with GABA-chloride antagonism that results in Demodex paralysis and/or death. The formulation aims to deliver the parasiticide in an ophthalmic topical form suitable for human ocular use.
The document emphasizes formulation characteristics for ophthalmic use, including sterility and non-irritancy, improved solubility/stability, and local targeted delivery to ocular structures such as the eyelids and eyelashes and the meibomian gland orifices. The compositions are also described as only locally therapeutically effective in certain embodiments, and some embodiments exclude essential oils such as tea tree oil.
The compositions are further described with specific formulation components such as hydrogenated castor oil and polysaccharide thickeners, including hydroxypropyl methylcellulose and/or carboxymethyl cellulose, together with other ophthalmic excipients and pH considerations. The document also describes diagnostic and observational aspects for Demodex quantification and mite immobilization, including use of sampling and nucleic acid quantification approaches, and ex vivo observations of mite behavior.
Claims Coverage
Independent claims are directed to ophthalmic compositions containing lotilaner as an isoxazoline parasiticide, with each independent claim specifying key formulation and dosage-form limitations. Across the independent claims, the main inventive features total four distinct categories: composition concentration for lotilaner, selected formulation components, dosage form and local therapeutic limitation, and additional formulation exclusions or constraints.
Isoxazoline parasiticide ophthalmic eye drop containing lotilaner within a defined range
An isoxazoline parasiticide ophthalmic composition comprising lotilaner, wherein the lotilaner is present from about 0.10% to about 0.50% by weight with respect to the total weight of the composition, wherein the composition is in eye drop form and is formulated for ophthalmic use.
Isoxazoline parasiticide ophthalmic composition with hydrogenated castor oil and polysaccharide thickener
An isoxazoline parasiticide ophthalmic composition comprising lotilaner, wherein the lotilaner is present from about 0.10% to about 0.50% by weight with respect to the total weight of the composition; a hydrogenated castor oil; and a polysaccharide thickener, wherein the composition is formulated for ophthalmic use.
Locally therapeutically effective isoxazoline parasiticide ophthalmic eye drop
An isoxazoline parasiticide ophthalmic composition comprising lotilaner, wherein the lotilaner is present from about 0.10% to about 0.50% by weight with respect to the total weight of the composition; wherein the ophthalmic composition is in eye drop form and is formulated for ophthalmic use, and wherein the ophthalmic composition is only locally therapeutically effective.
Locally therapeutically effective isoxazoline parasiticide ophthalmic gel, ointment, or cream
An isoxazoline parasiticide ophthalmic composition comprising lotilaner, wherein the ophthalmic composition is formulated as a gel, an ointment, or a cream, and wherein the ophthalmic composition is only locally therapeutically effective.
The independent claims cover ophthalmic topical formulations based on lotilaner as an isoxazoline parasiticide, with defined lotilaner content ranges and specific dosage forms. Additional claim coverage includes inclusion of hydrogenated castor oil and polysaccharide thickeners, and limitations to only local therapeutic effectiveness in certain dosage forms.
Stated Advantages
Sterility and non-irritancy.
Improved solubility/stability.
Local targeted delivery to ocular structures such as the eyelids and eyelashes and the meibomian gland orifices.
Only locally therapeutically effective in certain embodiments.
Documented Applications
Treating or preventing Demodex-associated conditions.
Treating or preventing blepharitis.
Treating or preventing ocular rosacea.
Human ocular use.
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