Solid, orally administrable pharmaceutical composition
View Patent ↗The present invention relates to a process for the preparation of a solid, orally administrable pharmaceutical composition, comprising 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide in hydrophilized form, and its use for the prophylaxis and/or treatment of diseases.
1. A process for the preparation of a solid, orally administrable pharmaceutical composition comprising an active compound (I) that is 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide in hydrophilized form, comprising the following steps:
(a) first preparing granules comprising the active compound (I) in hydrophilized form using fluidized bed granulation for moist granulation;
(b) and converting the granules into the pharmaceutical composition, if appropriate with addition of pharmaceutically suitable additives.
2. The process according to claim 1 , wherein the active compound (I) is employed in crystalline form.
3. The process according to claim 2 , wherein the active compound (I) is employed in micronized form.
4. The process according to claim 1 , wherein the active compound (I) suspended in the granulating liquid is introduced into the moist granulation.
5. The process according to claim 1 , wherein the resulting pharmaceutical composition is a tablet rapidly releasing the active compound (I).
6. A solid, orally administrable pharmaceutical composition comprising an active compound (I) that is 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide in hydrophilized form prepared by a process comprising the following steps:
(a) first preparing granules comprising the active compound (I) in hydrophilized form using fluidized bed granulation for moist granulation;
(b) and converting the granules into the pharmaceutical composition, if appropriate with addition of pharmaceutically suitable additives.
7. The pharmaceutical composition according to claim 6 , comprising the active compound (I) in crystalline form.
8. The pharmaceutical composition according to claim 7 , comprising the active compound (I) in micronized form.
9. The pharmaceutical composition according to claim 6 , wherein the active compound (I) is present in a concentration of 1 to 60% based on the total mass of the composition.
10. The pharmaceutical composition according to claim 6 , further comprising sodium lauryl sulphate as a wetting agent.
11. The pharmaceutical composition according to claim 10 , wherein said sodium lauryl sulphate is present in a concentration of 0.1 to 5%, based on the total mass.
12. The pharmaceutical composition according to claim 6 , further comprising hydroxypropylmethylcellulose as a hydrophilic binding agent.
13. The pharmaceutical composition according to claim 12 , wherein said hydroxypropylmethylcellulose is present in a concentration of 1 to 15%, based on the total mass.
14. The pharmaceutical composition according to claim 6 that is in the form of a tablet.
15. The pharmaceutical composition according to claim 14 that is in the form of a rapid-release tablet.
16. The pharmaceutical composition according to claim 15 , characterized in that the tablet is covered with a coating.
17. A method for the prophylaxis and/or treatment of thromboembolic diseases comprising administering an effective amount of the pharmaceutical composition of claim 6 to a patient in need thereof.