Dosing Preparation of Dabigatran Etexilate or a Salt Thereof and a Preparation Method Thereof

摘要

Disclosed is an oral dosing preparation of dabigatran etexilate or pharmaceutically acceptable salts thereof and a preparation method thereof.

主权项

1. A pharmaceutical composition for oral administration comprising:
a) one or more approximately spherically-shaped pellet cores consisting of a binder and pharmaceutically acceptable celluloses or sugars or starches or one or more component(s) consisting of microcrystalline celluloses or sugars or starches; b) a first active substance layer consisting of an active substance, and/or a disintegrant, and/or a filler and a binder, wherein the active substance is dabigatran etexilate or one pharmaceutically acceptable salt thereof; c) a first water soluble isolating layer surrounding the surface of the first active substance layer, wherein the layer material is selected from the group consisting of hydroxypropyl methyl cellulose, hydroxypropyl cellulose, starch, resin, and other organic polymer materials or combinations of these polymers; d) an acid layer consisting of a binder and a pharmaceutically acceptable organic acid, or consisting of an organic acid, wherein the organic acid has a solubility more than 1 g/250 ml in water at 20° C., and is selected from the group consisting of tartaric acid, fumaric acid, succinic acid, citric acid, malic acid, glutamic acid or aspartic acid or a hydrate or salt of glutamic acid or aspartic acid, and hemi-cysteine hydrochloride; e) a second water soluble isolating layer on the surface of acid layer, wherein the layer material is selected from the group consisting of hydroxypropyl methyl cellulose, hydroxypropyl cellulose, starch, resin and other water soluble polymers or combinations of these polymers; f) a second active substance layer consisting of an active substance, and/or a disintegrant, and/or a filler and a binder, wherein the active substance is dabigatran etexilate or one pharmaceutically acceptable salt thereof; and g) a third water soluble isolating layer on the surface of the second active substance layer, wherein the layer material is selected from the group consisting of hydroxypropyl methyl cellulose, hydroxypropyl cellulose, starch, resin, and other organic polymer materials or combinations of these polymers.