Pharmaceutical compositions for demodex related blepharitis and eyelid crusting

Inventors

TAN, Tiang Hin JerryPOR, Yong Ming

Assignees

Jerry Tan Eye Surgery Pte LtdTarsus Pharmaceuticals Inc

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Publication Number

US-12257263-B2

Patent

Publication Date

2025-03-25

Expiration Date


Abstract

Formulation of ectoparasiticidal and antibiotic “compositions into pharmaceutical compositions useful for the treatment of eyelid inflammation, in particular demodex related blepharitis and eye crusting.

Core Innovation

The disclosed invention relates to a method for the treatment of demodex blepharitis and eyelid crusting by identifying a presence of demodex mites in eyelash follicles of an individual. The method includes topically administering every night for a month onto the eyelash follicles of the individual in need of such treatment and removing with water in the morning. The treatment is sufficient to eliminate the presence of demodex mites in the eyelash follicles of the individual.

The topically administered treatment is a topical pharmaceutical composition formulated as an emulsion. The composition comprises an effective amount of ivermectin and an additional antibiotic selected from a group consisting of a tetracycline, an oxytetracycline, a macrolide, a fluoroquinolone, an aminoglycoside and metronidazole, together with water.

The emulsion additionally includes a humectant comprising sorbitol; a mixture of emollients comprising cyclopentasiloxane and ethylhexyl stearate; an additional agent as an emulsifier; a mixture of preservatives comprising methylchloroisothiazolinone and disodium EDTA; an antioxidant comprising tocopheryl acetate; and a solvent comprising propylene glycol. The disclosed formulation is directed to eyelash follicles for eliminating demodex mites and improving demodex blepharitis and eyelid crusting.

Claims Coverage

The document contains one independent claim directed to a method of treating demodex blepharitis and eyelid crusting, with dependent claims refining the composition by concentration ranges and by narrowing the class of the additional antibiotic. Overall, the independent claim couples mite identification and a nightly month-long topical emulsion regimen with a specific multi-component formulation centered on ivermectin plus a selected additional antibiotic.

Mite identification and nightly emulsion treatment to eliminate demodex mites

Identifying a presence of demodex mites in eyelash follicles of an individual, and topically administering every night for a month onto the eyelash follicles and removing with water in the morning, wherein the topically administering is sufficient to eliminate the presence of demodex mites in the eyelash follicles.

Ivermectin plus additional antibiotic in an emulsion topical pharmaceutical composition

Administering a topical pharmaceutical composition formulated as an emulsion comprising an effective amount of ivermectin and an additional antibiotic selected from a group consisting of a tetracycline, an oxytetracycline, a macrolide, a fluoroquinolone, an aminoglycoside and metronidazole, together with water, wherein the emulsion is used as part of the nightly month-long treatment to eliminate demodex mites.

Sorbitol humectant, cyclopentasiloxane/ethylhexyl stearate emollients, and formulation component set

Providing the emulsion with a humectant comprising sorbitol; a mixture of emollients comprising cyclopentasiloxane and ethylhexyl stearate; an additional agent as emulsifier; a mixture of preservatives comprising methylchloroisothiazolinone and disodium EDTA; an antioxidant comprising tocopheryl acetate; and a solvent comprising propylene glycol.

Ivermectin concentration range

Having ivermectin present at 1% to 5% by weight in the topical pharmaceutical composition.

Additional antibiotic concentration range

Having the additional antibiotic present at 1% to 5% by weight in the topical pharmaceutical composition.

Additional antibiotic selected as tetracycline class

Using an additional antibiotic that is a tetracycline antibiotic.

Additional antibiotic selected as fluoroquinolone class

Using an additional antibiotic that is a fluoroquinolone antibiotic.

Additional antibiotic selected as aminoglycoside class

Using an additional antibiotic that is an aminoglycoside antibiotic.

Claim coverage centers on a method to treat demodex blepharitis and eyelid crusting by identifying demodex mites in eyelash follicles and performing nightly month-long topical administration of a specified emulsion that eliminates the mites. The key formulation inventive features are the combination of ivermectin with a selected additional antibiotic class, plus a defined emulsion component set that includes sorbitol humectant, cyclopentasiloxane and ethylhexyl stearate emollients, emulsifier, specified preservatives, tocopheryl acetate antioxidant, and propylene glycol solvent, with dependent claims further constraining ivermectin and additional antibiotic weight ranges and narrowing the additional antibiotic classes.

Stated Advantages

Eliminates the presence of demodex mites in the eyelash follicles.

Documented Applications

Treatment of demodex blepharitis and eyelid crusting by topical administration onto eyelash follicles.

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