Pellet medicine composition containing pradaxa or salt and hydrate thereof

Abstract

The invention discloses a medicinal combination containing pradaxa or salt and hydrate thereof. The medicinal combination comprises an active substance pellet core material containing an active ingredient pradaxa or pharmaceutically acceptable salt or hydrate thereof and filler and/or adhesive, an organic acid pellet core material containing organic acid and filler and/or adhesive, and an isolation layer which is arranged outside the active substance pellet core material and the organic acid pellet core material as shown in a figure I. By means of screening, the pradaxa active substance and organic acid are respectively prepared into pellet cores, and the pellet cores are respectively coated with the isolation layer, and the two pellets are prepared in a proportion to form the pradaxa oral medicine composition. The process is stable and controllable, and the preparation has good solubility and dissolution rate.

Description

technical field [0001] The invention relates to a pellet pharmaceutical composition of dabigatran etexilate or its salt and hydrate, belonging to the technical field of medicine. Background technique [0002] The chemical formula of dabigatran etexilate 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 structural formula is as shown in I below. [0003] [0004] Dabigatran etexilate is another new type of oral anticoagulant drug approved by the US Food and Drug Administration after warfarin. It is a non-peptide thrombin inhibitor, which specifically and selectively blocks thrombin (free or bound) activity to exert anticoagulant effect. It has the characteristics of oral administration, strong potency, no need for special medication monitoring, and few drug interactions. It is a major progress in the field of...

AI Technical Summary

Problems solved by technology

Compared with the previous process, the active substance is made into a ball core, which avoids the defect of fluidized drug application, but does not avoid the long-term contact between the active substance and the organic acid, and still needs to be isolated between the active substance ball core and the organic acid layer. Layer, the process is complicated and difficult to control, and it is impossible to avoid the contact between the drug and the active substance caused by the rapid breakdown of the isolation layer, resulting in the degradation of the active substance

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