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Apixaban composition and preparation method thereof

A technology of apixaban and apixaban tablets, applied in the field of apixaban pharmaceutical preparations

Inactive Publication Date: 2015-05-27
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it was determined that formulations prepared using wet granulation methods as well as formulations prepared using large particles of the apixaban drug product yielded suboptimal exposures, which could create quality control challenges

Method used

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  • Apixaban composition and preparation method thereof
  • Apixaban composition and preparation method thereof
  • Apixaban composition and preparation method thereof

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preparation example Construction

[0031] The dry granulation process for preparing crystalline apixaban granules having an average particle size equal to or less than about 70 μm is believed to be novel and is therefore provided as a further feature of the present invention. Therefore, the present invention provides a pharmaceutical product preparation method, comprising the following steps:

[0032] (1) blending the raw materials prior to granulation;

[0033] (2) Granulate the raw materials of step 1 using dry or wet granulation methods;

[0034] (3) blending the granules of step 2 with extragranular raw material;

[0035] (4) compressing the blend of step 3 into tablets; and

[0036] (5) Film-coat the tablets in step 4.

[0037] In another embodiment, the present invention provides a method for preparing a pharmaceutical product, comprising the steps of:

[0038] (1) blending the raw material with apixaban of controlled particle size;

[0039] (2) Including intragranular portions of binder, disi...

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PUM

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Abstract

The invention relates to an apixaban composition which contains crystalline apixaban particles with D90 equal to or smaller than 70 microns and a pharmaceutical carrier. The apixaban composition is basically bioequivalent and can be used for treating and / or preventing thromboembolic diseases.

Description

technical field [0001] The present invention relates to pharmaceutical formulations of apixaban comprising crystalline apixaban particles with a maximum size cutoff (cutoff), and methods of using them, e.g. for the treatment and / or prevention of thromboembolic disorders method. Background technique [0002] Apixaban is a known compound with the following structure: [0003] [0004] The chemical name of Apixaban is 4,5,6,7-tetrahydro-1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-piperidine- 1-yl)phenyl]-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (CAS name) or 1-(4-methoxyphenyl)-7-oxo-6- [4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (IUPAC name). [0005] Apixaban is disclosed in U.S. Patent 6,967,208 (according to U.S. Patent Application 10 / 245,122 filed September 17, 2002), which is hereby incorporated by reference in its entirety, which has the clotting factor Use of Xa inhibitors, developed as oral administration for various in...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/4545A61P7/02
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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