| 摘要 |
Solid, orally administrable pharmaceutical drug delivery system (A) comprises 5-chloro-N ({(5S)- 2-oxo-3-[4-(3-oxo-4-morpholinyl)- phenyl]-1,3-oxazolidine-5-yl}-methyl)-2-thiophene carboxamide (I) with a fast release of the active substance, where the active substance (I) is in amorphous form and 80% of the active substance (I) is released within less than 2 hours, according to United State Pharmacopeial drug release procedure with apparatus 2 (Paddle). Independent claims are included for: (1) a method for the preparation of (A) comprising preparing the active substance (I) containing a mixture by a melt process, mixing the obtained mixture in powder form with further auxiliary materials and subsequently filling the mixture as sachet or capsules, or after mixing with tableting additives, preferably by direct tableting and press-molding to tablets, which is subsequently polished; (2) a mutli-particulate pharmaceutical drug delivery system; (3) a pharmaceutical drug delivery system comprising the multi-particulate pharmaceutical drug delivery system; (4) a method for the preparation of multi-particulate pharmaceutical drug delivery system comprising preparing active substance (I) with an extrudate by melt extrusion process and cutting the obtained mixture; and (5) a method for prophylaxis, secondary prophylaxis and/or treatment of thromboembolic diseases comprising administering (A). ACTIVITY : Thrombolytic; Cardiant; Antianginal; Vasotropic; Cerebroprotective; Anticoagulant. MECHANISM OF ACTION : Factor Xa inhibitor. |
