Pharmaceutical composition

摘要

Oral pharmaceutical formulations containing ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorders characterized by aberrant erbB family PTK activity.

主权项

1. An oral pharmaceutical formulation prepared by a process having the steps:
(a) admixing and fluidizing N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine ditosylate monohydrate and at least microcrystalline cellulose in a fluid bed granulator to form a fluidized mixture, wherein the N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine ditosylate monohydrate of the fluidized mixture is present in the range of 45 to 57 percent by weight, and the microcrystalline cellulose of the fluidized mixture is present in the range of 43 to 55 percent by weight; (b) granulating said mixture utilizing an aqueous solution of at least povidone to form active granules, wherein the aqueous solution is a 10 to 25 percent solution of povidone in purified water; (c) blending the active granules with at least sodium starch glycolate and at least magnesium stearate to form a compression blend, wherein the active granules are present in a range of 93 to 96 percent by weight, the sodium starch glycolate is present in a range of 3.5 to 5.5 percent by weight, and the magnesium stearate is present in a range of 0.8 to 1.2 percent by weight; (d) compressing the compression blend into a tablet form; and (e) film coating the tablet.