US2021077465A1PendingUtilityA1

Isoxazoline parasiticide formulations and methods for treating blepharitis

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Assignee: TARSUS PHARMACEUTICALS INCPriority: Dec 15, 2017Filed: Nov 16, 2020Published: Mar 18, 2021
Est. expiryDec 15, 2037(~11.4 yrs left)· nominal 20-yr term from priority
A61P 17/00A61K 31/155A61P 27/02A61P 33/14A61K 47/26A61K 9/0048A61K 9/08A61K 31/422A61K 31/42
76
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Claims

Abstract

Disclosed herein are methods for treating or preventing ophthalmic and dermatologic conditions in a patient, including ocular surface conditions such as blepharitis. The methods can include topically administering directly to an ocular surface of one or more eyes of a patient in need of treatment thereof an effective amount of an isoxazoline parasiticide, formamidine parasiticide, or other active ingredient, formulated into an ophthalmic composition, the ophthalmic composition further comprising a pharmaceutically acceptable vehicle. Compositions are also disclosed.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A method for treating blepharitis in a patient, comprising:
 topically administering directly to an ocular surface of one or more eyes of a patient in need of treatment thereof an effective amount of an isoxazoline parasiticide, formulated into an ophthalmic composition, the ophthalmic composition further comprising a pharmaceutically acceptable vehicle,   wherein the ophthalmic composition is sterile and non-irritating to the eye,   wherein the isoxazoline parasiticide is the sole active ingredient of the ophthalmic composition.   
     
     
         2 . The method of  claim 1 , wherein from about 0.01% to about 1% of the isoxazoline parasiticide with respect to the total weight of the composition is administered. 
     
     
         3 . The method of  claim 1 , wherein about 0.03% by weight of the isoxazoline parasiticides with respect to the total weight of the composition is administered. 
     
     
         4 . The method of  claim 1 , wherein about 0.10% by weight of the isoxazoline parasiticides with respect to the total weight of the composition is administered. 
     
     
         5 . The method of  claim 1 , wherein the ophthalmic composition comprises an eye drop. 
     
     
         6 . The method of  claim 1 , wherein the ophthalmic composition does not include any essential oils. 
     
     
         7 . The method of  claim 1 , wherein the isoxazoline parasiticide is selected from the group consisting of: fluralaner, sarolaner, lotilaner, afoxolaner, and fluxametamide. 
     
     
         8 . The method of  claim 1 , wherein the ocular surface comprises at least one of the conjunctiva or cornea of the one or more eyes of the patient. 
     
     
         9 . The method of  claim 1 , wherein the ophthalmic composition comprises a polysorbate. 
     
     
         10 . A method for treating blepharitis in a patient, comprising:
 topically administering directly to one or more of the eye, eyelids, or eyelashes of a patient in need of treatment thereof an effective amount of an isoxazoline parasiticide, formulated into an ophthalmic composition further comprising a pharmaceutically acceptable vehicle, wherein the ophthalmic composition is sterile and non-irritating to the eye,   wherein the isoxazoline parasiticide is the sole active ingredient of the ophthalmic composition.   
     
     
         11 . The method of  claim 10 , wherein the patient's eyes are closed upon topically administering the ophthalmic composition, such that the composition contacts orifices of Meibomian glands of the patient and outside of eyelid margins of the patient. 
     
     
         12 . The method of  claim 11 , further comprising spreading the composition onto the eyelashes and follicles of the eyelashes. 
     
     
         13 . The method of  claim 11 , further comprising spreading the composition onto the eyelashes and follicles of the eyelashes with an applicator. 
     
     
         14 . The method of  claim 10 , wherein from about 0.001% to about 1% of the isoxazoline parasiticide is administered. 
     
     
         15 . The method of  claim 10 , wherein from about 0.001% to about 1% of the isoxazoline parasiticide is administered. 
     
     
         16 . The method of  claim 10 , comprising topically administering the ophthalmic composition at least once daily for at least about 2 weeks. 
     
     
         17 . The method of  claim 10 , comprising topically administering the ophthalmic composition at least once daily for at least about 4 weeks. 
     
     
         18 . A method for treating an ocular  Demodex  infestation in a patient, comprising,
 topically administering directly to one or more of the eyes, eyelids, or eyelashes of one or more eyes of a patient in need of treatment thereof, an effective amount of an isoxazoline parasiticide, formulated into an ophthalmic composition further comprising a pharmaceutically acceptable vehicle,   wherein the ophthalmic composition is sterile and non-irritating to the eye,   wherein the isoxazoline parasiticide is the sole active ingredient of the ophthalmic composition.   
     
     
         19 . The method of  claim 18 , further comprising receiving a first assessment of a quantity of  Demodex  mites on an anatomical structure of the patient, and topically administering the ophthalmic composition if the quantity of  Demodex  mites is greater than a predetermined value. 
     
     
         20 . The method of  claim 18 , wherein the ophthalmic formulation causes an abdomen and tail of  Demodex  mites on the patient to stop moving more quickly relative to a cephalothorax of the  Demodex  mites.

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