US2007021507A1PendingUtilityA1

Aqueous eye drops with accelerated intraocular migration

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Assignee: SAWA SHIROUPriority: Nov 5, 2004Filed: Nov 4, 2005Published: Jan 25, 2007
Est. expiryNov 5, 2024(expired)· nominal 20-yr term from priority
Inventors:Shirou SawaTomoko Fujimoto
A61P 37/02A61P 43/00A61P 27/14A61P 27/02A61P 29/00A61K 31/185A61K 31/133A61K 31/196
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Claims

Abstract

An aqueous eye drop comprising 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof and an organic amine (for example, aminoethylsulfonic acid or trometamol) or a salt thereof is useful as an eye drop for once a day administration for treating inflammatory diseases of the external segment or the anterior segment of the eyes, since such aqueous eye drop can maintain a therapeutically effective concentration of 2-amino-3-(4-bromobenzoyl)phenylacetic acid in anterior aqueous humor for at least 24 hours by once a day administration.

Claims

exact text as granted — not AI-modified
1 . A method for treating inflammatory diseases of the external segment or the anterior segment of the eyes, which comprises administering an aqueous eye drop comprising 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof once a day, and maintaining a therapeutically effective concentration of 2-amino-3-(4-bromobenzoyl)phenylacetic acid in the anterior aqueous humor for at least 24 hours after the intraocular administration.  
   
   
       2 . The method according to  claim 1 , wherein the aqueous eye drop comprising 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof comprises an organic amine or a salt thereof, and the content of the aforementioned organic amine or salt thereof is an amount to allow the octanol-water partition coefficient of 2-amino-3-(4-bromobenzoyl)phenylacetic acid to be 0.7 to 4.  
   
   
       3 . The method according to  claim 1 , wherein the concentration of 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof in the aqueous eye drop is 0.01 to 0.5 w/v %.  
   
   
       4 . The method according to  claim 2 , wherein the organic amine is at least one member selected from the group consisting of an amino acid, an alkanolamine, a diamine, a piperazine, and an aminoalkylsulfonic acid.  
   
   
       5 . The method according to  claim 2 , wherein the organic amine is an amino acid and its concentration is 0.35 to 5 w/v %.  
   
   
       6 . The method according to  claim 2 , wherein the organic amine is an alkanolamine and its concentration is 0.15 to 0.95 w/v %.  
   
   
       7 . The method according to  claim 6 , wherein the alkanolamine is trometamol.  
   
   
       8 . The method according to  claim 2 , wherein the organic amine is a diamine and its concentration is 0.05 to 5 w/v %.  
   
   
       9 . The method according to  claim 2 , wherein the organic amine is a piperazine and it is contained at a concentration of 0.05 to 5 w/v % in the aqueous eye drop.  
   
   
       10 . The method according to  claim 2 , wherein the organic amine is an aminoalkylsulfonic acid and its concentration is 0.05 to 5 w/v %.  
   
   
       11 . The method according to  claim 10 , wherein the aminoalkylsulfonic acid is aminoethylsulfonic acid.  
   
   
       12 . A method for promoting intraocular penetration of 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, which comprises administering an aqueous eye drop comprising 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof comprises an organic amine or a salt thereof, wherein the content of said organic amine or salt thereof is an amount to allow the octanol-water partition coefficient of 2-amino-3-(4-bromobenzoyl)phenylacetic acid to be 0.7 to 4.  
   
   
       13 . An aqueous eye drop for once a day administration for treating inflammatory diseases of the external segment or the anterior segment of the eyes, characterized in that a therapeutically effective concentration of 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof is maintained in the anterior aqueous humor for at least 24 hours by once a day administration.  
   
   
       14 . The aqueous eye drop according to  claim 13 , wherein the concentration of 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof in the aqueous eye drop is 0.01 to 0.5 w/v %.  
   
   
       15 . The aqueous eye drop according to  claim 13 , wherein the aqueous eye drop comprising 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof comprises an organic amine or a salt thereof, and the content of said organic amine or salt thereof is an amount to allow the octanol-water partition coefficient of 2-amino-3-(4-bromobenzoyl)phenylacetic acid contained in the aqueous eye drop to be 0.7 to 4.  
   
   
       16 . The aqueous eye drop according to  claim 15 , wherein the organic amine is at least one member selected from the group consisting of an amino acid, an alkanolamine, a diamine, a piperazine, and an aminoalkylsulfonic acid.  
   
   
       17 . The aqueous eye drop according to  claim 15 , wherein the organic amine is an amino acid and its concentration is 0.35 to 5 w/v %.  
   
   
       18 . The aqueous eye drop according to  claim 15 , wherein the organic amine is an alkanolamine and its concentration is 0.15 to 0.95 w/v %.  
   
   
       19 . The aqueous eye drop according to  claim 18 , wherein the alkanolamine is trometamol.  
   
   
       20 . The aqueous eye drop according to  claim 15 , wherein the organic amine is a diamine and its concentration is 0.05 to 5 w/v %.  
   
   
       21 . The aqueous eye drop according to  claim 15 , wherein the organic amine is a piperazine and it is contained at a concentration of 0.05 to 5 w/v % in the aqueous eye drop.  
   
   
       22 . The aqueous eye drop according to  claim 15 , wherein the organic amine is an aminoalkylsulfonic acid and its concentration is 0.05 to 5 w/v %.  
   
   
       23 . The aqueous eye drop according to  claim 22 , wherein the aminoalkylsulfonic acid is aminoethylsulfonic acid.  
   
   
       24 . An aqueous eye drop for once a day for treating inflammatory diseases of the external segment or the anterior segment of the eyes, characterized in that a therapeutically effective concentration of 2-amino-3-(4-bromobenzoyl)phenylacetic acid is maintained in the anterior aqueous humor for at least 24 hours by once a day administration of 0.01 to 0.5 w/v % 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof and 0.05 to 5 w/v % aminoethylsulfonic acid.  
   
   
       25 . A method for producing an aqueous eye drop which is to be administered once a day, characterized in that the aqueous eye drop comprising 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof is administered once a day, and a therapeutically effective concentration of 2-amino-3-(4-bromobenzoyl)phenylacetic acid is maintained in the anterior aqueous humor for at least 24 hours by once a day administration to treat inflammatory diseases of the external segment or the anterior segment of the eyes.  
   
   
       26 . The method according to  claim 25 , wherein the concentration of 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof in the aqueous eye drop is 0.01 to 0.5 w/v %.  
   
   
       27 . The method according to  claim 25 , wherein the amount of the organic amine or its salt used is an amount to allow the octanol-water partition coefficient of 2-amino-3-(4-bromobenzoyl)phenylacetic acid to be 0.7to 4.  
   
   
       28 . The method according to  claim 27 , wherein the organic amine is at least one member selected from the group consisting of an amino acid, an alkanolamine, a diamine, a piperazine, and an aminoalkylsulfonic acid.  
   
   
       29 . The method according to  claim 27 , wherein the organic amine is an amino acid, and its concentration is 0.35 to 5 w/v %.  
   
   
       30 . The method according to  claim 27 , wherein the organic amine is an alkanolamine, and its concentration is 0.15 to 0.95 w/v %.  
   
   
       31 . The method according to  claim 30 , wherein the alkanolamine is trometamol.  
   
   
       32 . The method according to  claim 27 , wherein the organic amine is a diamine, and its concentration is 0.05 to 5 w/v %.  
   
   
       33 . The method according to  claim 27 , wherein the organic amine is a piperazine, and it is contained at a concentration of 0.05 to 5 w/v % in the aqueous eye drop.  
   
   
       34 . The method according to  claim 27 , wherein the organic amine is an aminoalkylsulfonic acid, and its concentration is 0.05 to 5 w/v %.  
   
   
       35 . The method according to  claim 34 , wherein the aminoalkylsulfonic acid is aminoethylsulfonic acid.

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