| 摘要 |
PROBLEM TO BE SOLVED: To provide a pharmaceutical combination effective in treatment of hypertension, comprising aliskiren and amlodipine as active ingredients, wherein the dissolution of the active agents is controlled.SOLUTION: The present invention relates to a pharmaceutical oral fixed dose combination comprising a) 10 to 45 wt.% of a therapeutically effective amount of aliskiren, or a pharmaceutically acceptable salt thereof, b) 0.5 to 5 wt.% of a therapeutically effective amount of amlodipine, or a pharmaceutically acceptable salt thereof, and 2 to 15 wt.% of disintegrator, 1 to 60 wt.% of diluent, 1 to 20 wt.% of binder, 0.1 to 5 wt.% of lubricant and 0.05 to 5 wt.% of fluidity accelerator, wherein the pharmaceutical oral fixed dose combination shows an in vitro dissolution of component (a) of 60% or less after 10 minutes and 98% or less after 20 minutes, and a dissolution profile of component (b) of 50% or more after 20 minutes and 70% or more after 30 minutes at pH 2, and the pharmaceutical oral fixed dose combination is bioequivalent, or close to reaching bioequivalence, to a free dose combination of aliskiren and amlodipine. |
