Oral pharmaceutical composition comprises the thrombin inhibitor ethyl 3-(2-(4-(hexyloxycarbonylamidino)phenylaminomethyl)-1-methyl-1H-benzimidazole-5-carbonyl)-2-pyridylamino)propionate and an organic acid

摘要

Pharmaceutical composition for oral administration comprises ethyl 3-(2-(4-(hexyloxycarbonylamidino)phenylaminomethyl)-1-methyl-1H-benzimidazole-5-carbonyl)-2-pyridylamino)propionate (I), or a salt of (I), and an organic acid (II) with a water-solubility of more than 1 g/250 ml at 20 degreesC. Independent claims are also included for: (1) production of such a composition by forming cores from (II), optionally with addition of binders or other additives, by: (a) granulation, pelletization or extrusion/spheronization; (b) coating the cores with an insulating layer comprising a water-soluble polymer and optionally plasticizer, release agent and/or pigment; (c) applying a dispersion containing (I), binder and optionally release agent and simultaneously or subsequently drying the dispersion; (d) optionally applying a coating of film former, plasticizer and optionally pigment; and (e) filling hard capsules with the resulting pellets; (2) the methanesulfonate salt of (I).