Pharmaceutical compositions for demodex related blepharitis and eyelid crusting

a technology of eyelid crusting and pharmaceutical compositions, which is applied in the field of ectoparasiticidal and antibiotic compositions, can solve the problems of little data on how eye care practitioners treat the disease, failure to eradicate the demodex parasite, and loss of lashes, so as to remove all crusts and debris

Inactive Publication Date: 2017-08-17
TARSUS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0054]The following examples are merely illustrative, and not limitative of the remainder of the disclosure in any way whatsoever. These examples are illustrative of the effectiveness of the invention.
[0055]Several patients had itching in the eyes and crusting around the eyelids. The presence of demodex mites was then confirmed. The confirmation was done by gently pulling on the eyelashes, and then transferring the presenting demodex mites onto a piece of cellophane tape. The said cellophane tape was then affixed onto a microscope slide. These demodex mites were viewed at 100 times of magnification, and counted to determine the mite density per lash follicle.
[0056]In treating the affected patients, the eyelids were first cleaned with hot compresses and a clean towel to remove all crusts and debris. The cream or ointment was then applied directly onto the affected area, by using a clean finger or a cotton-tipped applicator. The cream or ointment covered the entire eyelashes and roots.
[0057]The cream or ointment was left on the affected area for the entire night, and then washed away in the morning. This process was repeated on a nightly basis, for a month. The patients were then re-assessed for the presence of demodex mites, and no demodex mites were found on the eyelash roots of any patients. Before the treatment, many patients experienced itching on the eyelid margins. These patients were free of any symptoms, at the 1-month follow up.
[0058]Some cases were treated solely with ivermectin. However, these studies also demonstrate the necessity of antibiotics, in some cases.

Problems solved by technology

It may also result in loss of lashes.
Despite the prevalence of blepharitis in both presentation and contribution to ocular conditions, there is little data on how eye care practitioners treat the disease.
However, these treatments frequently fail to eradicate the demodex parasite and the infestation persists.
Tea tree oil treatments, however, suffer from several disadvantages.
Tea tree oil can easily lead to eye irritation and cause stinging sensations.
Even a small amount will induce tearing, if it reaches the ocular surface.. Due to the reflex tearing, dilution occurs and efficacy is reduced.
However, this is an expensive medication regimen and requires repeated dosing.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0059]This 52 year old Chinese gentleman had a long history of facial skin rashes that occurred along the nasolabial fold (also commonly known as “smile lines” or “laugh lines”) as well as around the ears. He had previously been treated by dermatologists for a diagnosis of seborrhoeic dermatitis with various creams including topical steroids. He presented with increasing crusting around the eyelashes and intermittent eye irritation. On examination, erythematous macules and papules were noted along the glabellar area as well as the nasolabial folds bilaterally. Marked crusting and many demodex mites were found in the eyelash follicles. A sample retrieved from one eyelash revealed 5 demodex folliculorum in the single follicle. He was treated with Ivermectin (only comprising 1%) cream nightly to the eyelid margins (as prescribed), as well as the inflamed areas of his face. One month later the eyelid margin crusting had resolved, as had the facial rash. No demodex mites were found in th...

example 2

[0060]This 44 year old Caucasian gentleman had recurring redness of the eyes associated with itching and burning sensations for the past 6 years. On examination, eyelash crusting together with lid margin erythema and many demodex mites were seen. He was first treated with oral Ivermectin (Stromectol) 12 mg and was advised to do scrubs using Tea Tree Oil on the eyelids twice a day. Over the next 2 months, the demodex mites reduced in numbers but were not completely eliminated, despite 4 subsequent doses of oral Ivermectin and continuing Tea Tree Oil scrubs. Tea Tree Oil applications were also performed on the patient. Owing to the persistence of the mites, dosages of Ivermectin (1%) cream was prescribed instead. After nightly applications of this cream for one month (as prescribed), no demodex mites were seen in the eyelash follicles and his ocular inflammation had markedly improved.

example 3

[0061]This 28 year old Chinese gentleman had recurring redness on the left eyelids for the past 9 years and had been treated previously with a variety of topical antibiotics including Framycetin. On examination, he had asymmetric disease, with severe inflammation of the left eyelid margins and corneal punctate erosions. Some demodex mites were seen in the eyelash follicles. He was treated with a combination of Ivermectin (1%) cream as well as Tetracycline eye ointment to the eyelids. Oral Doxycycline 100 mg twice a day was prescribed. Demodex mites resident in the lash follicles were eradicated after 1 month of nightly Ivermectin cream applications, as prescribed. Although eyelid inflammation was reduced, it was not entirely eliminated and the topical and oral tetracycline treatment was continued for the next 2 months. 4 months after initial presentation, the eyelids were much improved and inflammation had subsided. He was followed up for 2 years, and during this time remained free ...

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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.

Description

TECHNICAL FIELD[0001]The present invention relates to the formulation of ectoparasiticidal and antibiotic compositions into topical pharmaceutical compositions useful for the treatment of eyelid inflammation, in particular demodex related blepharitis and eyelid crusting. This invention also relates to a topical pharmaceutical composition suitable for the treatment of mammalian ectoparasites.DESCRIPTION OF BACKGROUND AND / OR RELATED AND / OR PRIOR ART[0002]Blepharitis represents one of the most common anterior segment disorders encountered in ophthalmology. Blepharitis produces a red-rimmed appearance at the margins of the eyelids. It affects both the upper and lower eyelids. Blepharitis tends to recur and can become chronic.[0003]Blepharitis is inflammation usually involving the part of the eyelid where the eyelashes grow. The eyes can eventually become red, itchy and irritated, with dandruff-like crusts appearing on the eyelashes (also known as “crusting”). It may also result in loss ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/7048A61K9/00A61K47/24A61K47/14A61K47/06A61K47/18A61K47/22A61K47/10A61K31/65A61K9/107A61K47/44
CPCA61K31/7048A61K9/107A61K9/0048A61K47/24A61K47/14A61K47/06A61K47/183A61K47/22A61K47/10A61K31/65A61K47/44A61K9/0014A61K45/06A61K47/26A61K9/06A61K47/34A61K2300/00
Inventor TAN, TIANG HIN JERRYPOR, YONG MING
Owner TARSUS PHARMA INC
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