Process for the preparation of a pharmaceutical composition comprising ezetimibe

摘要

The present invention belongs to the field of pharmaceutical industry and relates to a process for preparing dosage forms containing ezetimibe, comprising the steps of:
a) providing a composition comprising ezetimibe,b) sieving a composition comprising a composition of step (a),c) shear mixing of the composition after step (b), preferably the mixing of the composition is carried out by high shear mixing,d) formulation into a dosage form.;The present invention also relates to dosage forms containing ezetimibe and ezetimibe and simvastatin, which have been prepared according to the process according to the invention.

主权项

1. A process for preparing a dosage form, the process consisting essentially of the steps:
(a) providing a starting composition of particulates of ezetimibe and a hydrophilic excipient, (b) sieving a composition provided by step (a), (c) high shear mixing of the composition after step (b), and (d) formulation into a dosage form by direct compression, wherein said high shear mixing is carried out at a paddle speed of at least 100 RPM; wherein step (b) occurs before step (c); wherein the size of the particles d (0.9) of ezetimibe in the starting composition is between 8 and 25 μm and is essentially unchanged during the process; wherein the process is conducted under dry conditions without a solvent; wherein after (c) no further ingredients are added and no further mixing or sieving is performed; and wherein, when the produced dosage form is analyzed in a USP Apparatus 2 (paddles) in 0.01 M HCl and 0.25% sodium lauryl sulfate, more than 50% dissolves within 15 minutes.