Pharmaceutical formulation comprising ezetimibe

摘要

The present invention relates to novel formulations comprising ezetimibe as active ingredient. In particular the invention relates to a pharmaceutical composition comprising 5 to 20 wt-% ezetimibe, 50 to 85 wt-% diluent, 3 to 25 wt-% disintegrant, 1 to 10 wt-% binder, and 0.5 to 1 wt-% lubricant, characterized in that the ezetimibe has a particle size distribution of d(0.9) of 5 μm to 35 μm and d(0.5) of 3 μm to 20 μm, as well as methods for preparing said formulations.

主权项

1. A pharmaceutical composition comprising:
5 to 20 wt-% ezetimibe particles (1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone), 50 to 85 wt-% diluent, 3 to 25 wt-% disintegrant, 2 to 5 wt-% solubility enhancer 1 to 10 wt-% binder, and 0.5 to 1 wt-% lubricant,wherein the ezetimibe particles have a particle size distribution characterized by a d(0.9) value of 9 μm to 20 μm and a d(0.5) value of 3 μm to 50 μm.