# US 12,213,964 B2 · Isoxazoline parasiticide formulations

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- Number: US 12,213,964 B2
- Document ID: US12213964B2
- Status: Granted
- Kind: B2
- Application number: 18/325,910
- Filed: 2023-05-30
- Published: 2023-09-28
- Granted: 2025-02-04
- Earliest claimed: 2017-12-15
- Assignees: Tarsus Pharmaceuticals, Inc.
- Applicants: Tarsus Pharmaceuticals, Inc.
- Inventors: Bobak Robert Azamian; Douglas Michael Ackermann; Shawn D. Hickok; Joseph G. Vehige
- Web page: https://patentgrep.com/patent/US12213964B2

## CPC

- A61K 31/422: not condensed and containing further heterocyclic rings
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/42: Oxazoles
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 27/02: Ophthalmic agents
- A61P 33/14: Ectoparasiticides, e.g. scabicides
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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

### Claim 1

An ophthalmic composition comprising:
an effective amount of an isoxazoline parasiticide,
wherein the isoxazoline parasiticide is present at between about 0.10% and about 0.50% by weight with respect to the total weight of the composition;
a hydrogenated castor oil;
a polysaccharide thickener;
and glycerin,
wherein the glycerin is present at between about 0.5% and about 4% by weight with respect to the total weight of the composition.

### Claim 2 (depends on 1)

The ophthalmic composition of claim 1, wherein the ophthalmic composition is in eye drop form.

### Claim 3 (depends on 1)

The ophthalmic composition of claim 1, wherein the combination of the hydrogenated castor oil and the polysaccharide thickener forms a long-lasting film layer.

### Claim 4 (depends on 1)

The ophthalmic composition of claim 1, wherein the ophthalmic composition is characterized by a viscosity, wherein the viscosity is sufficiently high to cause the ophthalmic composition to spread over meibomian gland orifices on upper and/or lower lid margins upon blinking or closing of the eye and to slow evacuation of the ophthalmic composition through the puncta of the eye for at least 20 seconds.

### Claim 5 (depends on 1)

The ophthalmic composition of claim 1, wherein the isoxazoline parasiticide comprises lotilaner.

### Claim 6 (depends on 1)

The ophthalmic composition of claim 1, wherein the isoxazoline parasiticide is present at about 0.25% by weight with respect to the total weight of the composition.

### Claim 7 (depends on 1)

The ophthalmic composition of claim 1, wherein the hydrogenated castor oil comprises polyoxyl 35 castor oil.

### Claim 8 (depends on 1)

The ophthalmic composition of claim 1, wherein the hydrogenated castor oil is present at about 5% by weight with respect to the total weight of the composition.

### Claim 9 (depends on 1)

The ophthalmic composition of claim 1, wherein the polysaccharide thickener comprises hydroxypropyl methylcellulose.

### Claim 10 (depends on 1)

The ophthalmic composition of claim 1, wherein the polysaccharide thickener comprises carboxymethyl cellulose.

### Claim 11 (depends on 1)

The ophthalmic composition of claim 1, wherein the polysaccharide thickener is present at between about 0.1% and about 0.5% by weight with respect to the total weight of the composition.

### Claim 12 (depends on 1)

The ophthalmic composition of claim 1, wherein the polysaccharide thickener is present at about 0.2% by weight with respect to the total weight of the composition.

### Claim 13 (depends on 1)

The ophthalmic composition of claim 1, further comprising a preservative agent, wherein the preservative agent comprises potassium sorbate.

### Claim 14 (depends on 13)

The ophthalmic composition of claim 13, wherein the preservative agent does not comprise lauralkonium chloride or benzalkonium chloride.

### Claim 15 (depends on 1)

The ophthalmic composition of claim 1, further comprising a preservative agent, wherein the preservative agent comprises lauralkonium chloride.

### Claim 16 (depends on 1)

The ophthalmic composition of claim 1, further comprising a preservative agent, wherein the preservative agent comprises benzalkonium chloride.

### Claim 17 (depends on 1)

The ophthalmic composition of claim 1, further comprising a preservative agent, wherein the preservative agent is present at between about 0.15% and about 0.4% by weight with respect to the total weight of the composition.

### Claim 18 (depends on 1)

The ophthalmic composition of claim 1, wherein the ophthalmic composition does not comprise tea tree oil.

### Claim 19 (depends on 1)

The ophthalmic composition of claim 1, wherein the isoxazoline parasiticide is the sole active ingredient of the ophthalmic composition.

### Claim 20 (depends on 1)

The ophthalmic composition of claim 1, wherein the ophthalmic composition is only locally therapeutically effective.

### Claim 21 (depends on 1)

The ophthalmic composition of claim 1, wherein the ophthalmic composition is formulated as a gel.
