Process for the Preparation of a Solid, Orally Administrable Pharmaceutical Composition
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, the pharmaceutical composition resulting from this process, and its use for the prophylaxis and/or treatment of thromboembolic diseases.
1 . 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 (I) in hydrophilized form, comprising the following steps:
(a) first preparing granules comprising the active compound (I) in hydrophilized form by 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 moist granulation method used is fluidized bed granulation.
3 . The process according to claim 1 , wherein the active compound (I) is employed in crystalline form.
4 . The process according to claim 3 , wherein the active compound (I) is employed in micronized form.
5 . The process according to claim 1 , wherein the active compound (I) suspended in the granulating liquid is introduced into the moist granulation.
6 . The process according to claim 1 , wherein the resulting pharmaceutical composition is a tablet rapidly releasing the active compound (I).
7 . A solid, orally administrable pharmaceutical composition prepared by the process according to claim 1 .
8 . A solid, orally administrable pharmaceutical composition, comprising active compound 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophene-carboxamide (I) in hydrophilized form.
9 . The pharmaceutical composition according to claim 8 , comprising the active compound (I) in crystalline form.
10 . The pharmaceutical composition according to claim 9 , comprising the active compound (I) in micronized form.
11 . The pharmaceutical composition according to claim 7 , wherein the active compound (I) is present in a concentration of 1 to 60% based on the total mass of the formulation.
12 . The pharmaceutical composition according to claim 7 , further comprising sodium lauryl sulphate as a wetting agent.
13 . The pharmaceutical composition according to claim 12 , wherein said sodium lauryl sulphate is present in a concentration of 0.1 to 5%, based on the total mass.
14 . The pharmaceutical composition according to claim 7 , further comprising hydroxypropylmethylcellulose as a hydrophilic binding agent.
15 . The pharmaceutical composition according to claim 14 , wherein said hydroxypropylmethylcellulose in a concentration of 1 to 15%, based on the total mass.
16 . The pharmaceutical composition according to claim 7 in the form of a tablet.
17 . The pharmaceutical composition according to claim 16 in the form of a rapid-release tablet.
18 . The pharmaceutical composition according to claim 16 , characterized in that the tablet is covered with a coating.
19 . A method for the prophylaxis and/or treatment of thromboembolic diseases comprising administering an effective amount of the pharmaceutical composition of claim 7 .
20 . A method for the prophylaxis and/or treatment of thromboemblic diseases comprising administering an effective amount of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophenecarboxamide (I) in hydrophilized form.
21 . (canceled)