US2018028598A1PendingUtilityA1

Compostions for Treating Dry Eye Disease

65
Assignee: UNIV CALIFORNIAPriority: May 7, 2008Filed: Jul 10, 2017Published: Feb 1, 2018
Est. expiryMay 7, 2028(~1.8 yrs left)· nominal 20-yr term from priority
Inventors:Benjamin SullivanTannin A. SchmidtDavid A. Sullivan
A61P 37/08A61P 27/04A61P 27/02A61P 27/00A61P 27/14A61P 29/00A61K 31/568A61K 38/1709A61K 38/1841A61K 47/02A61K 31/688A61K 31/715A61K 38/17A61K 9/0051A61K 9/0048A61K 31/728A61K 38/14A61K 31/685A61K 38/13A61K 47/24A61K 45/06A61K 2300/00
65
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Claims

Abstract

The present invention provides a pharmaceutical composition, and methods of use thereof, for treating ocular boundary deficiency, symptoms associated therewith, or an undesired condition that is associated with or causes ocular boundary deficiency at the ocular surface. The pharmaceutical composition of the present invention comprises a human PRG4 protein, a lubricant fragment, homolog, or isoform thereof, suspended in an ophthalmically acceptable balanced salt solution. The pharmaceutical composition of the present invention may also comprise one or more ophthalmically acceptable agents selected from the group consisting of an ophthalmically acceptable demulcent, excipient, astringent, vasoconstrictor, emollient, sodium hyaluronate, hyaluronic acid, and surface active phospholipids, in a pharmaceutically acceptable carrier for topical administration.

Claims

exact text as granted — not AI-modified
1 .- 12 . (canceled) 
     
     
         13 . A pharmaceutical composition suitable for topical application to an ocular surface of an individual, comprising:
 PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration effective to reduce tear osmolarity upon topical application of the pharmaceutical composition to the ocular surface of the individual so as to relieve dysfunction of a tear film or dry eye disease or symptoms associated therewith,   a polysorbate surfactant, and   one or more ophthalmically acceptable agents selected from the group consisting of a salt solution, a demulcent, an excipient, an astringent, a vasoconstrictor, and an emollient.   
     
     
         14 . The pharmaceutical composition of  claim 13 , comprising PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration of 10-10,000 μg/mL. 
     
     
         15 . The pharmaceutical composition of  claim 13 , comprising PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration of 50-500 μg/mL. 
     
     
         16 . The pharmaceutical composition of  claim 13 , further comprising sodium hyaluronate or hyaluronic acid. 
     
     
         17 . The pharmaceutical composition of  claim 16 , wherein the sodium hyaluronate or the hyaluronic acid is present at a concentration of 10-100,000 μg/mL. 
     
     
         18 . The pharmaceutical composition of  claim 16 , wherein the sodium hyaluronate or the hyaluronic acid is present at a concentration of 500-5,000 μg/mL. 
     
     
         19 . The pharmaceutical composition of  claim 13 , further comprising a surface active phospholipid selected from the group consisting of L-α-dipalmitoylphosphatidylcholine, phosphatidylcholine, phosphatidylethanolamine and sphingomyelin. 
     
     
         20 . The pharmaceutical composition of  claim 19 , wherein the phospholipid is present at a concentration of 10-10,000 μg/mL. 
     
     
         21 . The pharmaceutical composition of  claim 13 , wherein the salt solution comprises at least three different electrolytes selected from the group consisting of sodium phosphate, sodium chloride, potassium chloride, sodium bicarbonate, potassium bicarbonate, calcium chloride, magnesium chloride, sodium acetate, sodium citrate, hydrochloric acid, and sodium hydroxide. 
     
     
         22 . The pharmaceutical composition of  claim 13 , wherein the PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) has an average molecular mass of between 50 kDa and 400 kDa. 
     
     
         23 . The pharmaceutical composition of  claim 13 , wherein the PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) is a recombinant molecule. 
     
     
         24 . The pharmaceutical composition of  claim 13 , wherein the PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) is a purified naturally occurring molecule. 
     
     
         25 . The pharmaceutical composition of  claim 13 , wherein PRG4 is made from the amino acid sequence of SEQ ID NO: 1. 
     
     
         26 . The pharmaceutical composition of  claim 13 , comprising PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration of 10-500 μg/mL. 
     
     
         27 . The pharmaceutical composition of  claim 13 , comprising PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration of 100-300 μg/mL. 
     
     
         28 . The pharmaceutical composition of  claim 13 , comprising PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration of 100 μg/mL. 
     
     
         29 . The pharmaceutical composition of  claim 13 , comprising PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration of 200 μg/mL. 
     
     
         30 . A method of managing ocular lubrication, comprising administering to an ocular surface of an individual in need an effective amount of a pharmaceutical composition suitable for topical ophthalmic application, the pharmaceutical composition comprising:
 PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration effective to reduce tear osmolarity upon topical application of the pharmaceutical composition to the ocular surface of the individual so as to relieve dysfunction of a tear film or dry eye disease or symptoms associated therewith,   a polysorbate surfactant, and   one or more ophthalmically acceptable agents selected from the group consisting of a salt solution, a demulcent, an excipient, an astringent, a vasoconstrictor, and an emollient.   
     
     
         31 . The method of  claim 30 , the pharmaceutical composition comprising PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration of 10-10,000 μg/mL. 
     
     
         32 . The method of  claim 30 , the pharmaceutical composition comprising PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration of 50-500 μg/mL. 
     
     
         33 . The method of  claim 30 , the pharmaceutical composition further comprising sodium hyaluronate or hyaluronic acid. 
     
     
         34 . The method of  claim 33 , wherein the sodium hyaluronate or the hyaluronic acid is present at a concentration of 10-100,000 μg/mL. 
     
     
         35 . The method of  claim 33 , wherein the sodium hyaluronate or the hyaluronic acid is present at a concentration of 500-5,000 μg/mL. 
     
     
         36 . The method of  claim 30 , the pharmaceutical composition further comprising a surface active phospholipid selected from the group consisting of L-α-dipalmitoylphosphatidylcholine, phosphatidylcholine, phosphatidylethanolamine and sphingomyelin. 
     
     
         37 . The method of  claim 36 , wherein the phospholipid is present at a concentration of 10-10,000 μg/mL. 
     
     
         38 . The method of  claim 30 , wherein the salt solution comprises at least three different electrolytes selected from the group consisting of sodium phosphate, sodium chloride, potassium chloride, sodium bicarbonate, potassium bicarbonate, calcium chloride, magnesium chloride, sodium acetate, sodium citrate, hydrochloric acid, and sodium hydroxide. 
     
     
         39 . The method of  claim 30 , wherein the PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) has an average molecular mass of between 50 kDa and 400 kDa. 
     
     
         40 . The method of  claim 30 , wherein the PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) is a recombinant molecule. 
     
     
         41 . The method of  claim 30 , wherein the PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) is a purified naturally occurring molecule. 
     
     
         42 . The method of  claim 30 , wherein PRG4 is made from the amino acid sequence of SEQ ID NO: 1. 
     
     
         43 . The method of  claim 30 , the pharmaceutical composition comprising PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration of 10-500 μg/mL. 
     
     
         44 . The method of  claim 30 , the pharmaceutical composition comprising PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration of 100-300 μg/mL. 
     
     
         45 . The method of  claim 30 , the pharmaceutical composition comprising PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration of 100 μg/mL. 
     
     
         46 . The method of  claim 30 , the pharmaceutical composition comprising PRG4 or a lubricating fragment thereof comprising glycosylated repeats of the sequence KEPAPTT (SEQ ID NO:4) at a concentration of 200 μg/mL.

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