Oral formulations of deferasirox

Abstract

Orally administerable deferasirox formulations are disclosed having reduced release under gastric conditions and fast release at near neutral pH or at neutral pH.

1 - 36 . (canceled) 
     
     
         37 . A method of treatment of chronic iron overload in a patient comprising directly orally administering 90 mg deferasirox or a pharmaceutically acceptable salt thereof in a solid swallowable dosage form wherein the dosage form is a whole and intact tablet. 
     
     
         38 . A method of treatment of chronic iron overload in a patient comprising directly orally administering 180 mg deferasirox or a pharmaceutically acceptable salt thereof in a solid swallowable dosage form wherein the dosage form is a whole and intact tablet. 
     
     
         39 .- 46 . (canceled) 
     
     
         47 . A method of treatment of chronic iron overload in a patient comprising directly orally administering an amount of deferasirox selected from the group consisting of 90, 180, and 360 mg in a solid swallowable dosage form, wherein the dosage form is a whole and intact tablet, and wherein the tablet comprises
 (i) at least one filler selected from the group consisting of microcrystalline cellulose, and ethylcellulose in an amount of 10% to 40% by weight based on total weight of the tablet,   (ii) at least one disintegrant selected from the group consisting of polyvinylpyrrolidone (crospovidone), starch, CMC-Ca, CMC-Na, microcrystalline cellulose, alginic acid, sodium alginate, and guar gum in an amount of 1% to 10% by weight based on the total weight of the tablet; and,   (iii) at least one binder selected from the group consisting of polyvinylpyrrolidone (PVP), hydroxypropylmethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, microcrystalline cellulose, hypromellose, and starch in an amount of 1% to 5% by weight based on the total weight of the tablet.   
     
     
         48 . A method according to  claim 47  wherein the tablet comprises about 1-55% microcrystalline cellulose. 
     
     
         49 . A method according to  claim 37  wherein the tablet comprises about 1-55% microcrystalline cellulose. 
     
     
         50 . A method according to  claim 38  wherein the tablet comprises about 1-55% microcrystalline cellulose. 
     
     
         51 . A method of treatment of chronic iron overload in a patient comprising directly orally administering an amount of deferasirox selected from the group consisting of 90, 180, and 360 mg in a solid swallowable dosage form, wherein the dosage form is a whole and intact tablet, and wherein the tablet comprises at least one binder selected from the group consisting of polyvinylpyrrolidone (PVP), hydroxypropylmethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, microcrystalline cellulose, hypromellose, and starch in an amount of 1% to 5% by weight based on the total weight of the tablet. 
     
     
         52 . A method according to  claim 51  wherein the tablet comprises about 32-33% Microcrystalline Cellulose and about 8-10% polyvinylpyrrolidone.