Dabigatran etexilate pharmaceutical composition and preparation method thereof

Abstract

The invention particularly relates to a dabigatran etexilate pharmaceutical composition. The dabigatran etexilate pharmaceutical composition comprises: 1) an organic acid layer containing a pellet core having the outer layer coated with an organic acid, an adhesive and an anti-sticking agent; 2) an isolation layer arranged outside the organic acid layer; 3) a medicine applying layer arranged outside the isolation layer and prepared by mixing an active ingredient dabigatran etexilate or a pharmaceutically acceptable salt or hydrate thereof, an anti-sticking agent and an adhesive; and 4) a protective layer arranged outside the medicine applying layer. The dabigatran etexilate composition prepared by the invention can be stably dissolved out in an in-vivo absorption process, so good bioavailability is achieved.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a dabigatran etexilate pharmaceutical composition and a preparation method thereof. Background technique [0002] The chemical name of the dabigatran etexilate active substance of the present invention is 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1- Methyl-1H-benzimidazole-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester and its salts and hydrates. The chemical structure of dabigatran etexilate is shown in the following scheme I. It is a new type of synthetic non-peptide thrombin inhibitor, which is the prodrug of dabigatran (dabigatran), and is mainly used for the prevention of venous thrombosis after surgery. After oral administration, dabigatran etexilate is converted into dabigatran with direct anticoagulant activity after gastrointestinal absorption. Dabigatran binds to the fibrin-specific binding site of thrombin, preventing fibrinogen from bei...

AI Technical Summary

Problems solved by technology

[0005] The application number is 201310047056.8, and the patent name is a medicinal combination containing dabigatran etexilate or its salt and hydrate. Isolation layer or outer coating layer, because dabigatran etexilate is pH-dependent, the lower the pH value, the better the solubility, the patent wraps the active ingredient ball core material in the organic acid layer, and the organic acid layer will dissolve faster Solubility of dabigatran etexilate cannot be promoted

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