Medicinal composition containing rivaroxaban and preparation method thereof

A technology of rivaroxaban and composition, applied in the field of oral solid pharmaceutical composition, capable of solving the problems of slow dissolution of rivaroxaban and complex preparation process, etc.

Active Publication Date: 2014-02-05
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In order to solve the problems of complex preparation process and slow dissolution of rivaroxaban in the prior art, the present invention provides an oral solid pharmaceu

Method used

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  • Medicinal composition containing rivaroxaban and preparation method thereof
  • Medicinal composition containing rivaroxaban and preparation method thereof
  • Medicinal composition containing rivaroxaban and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] The prescription composition was the same as that of Comparative Example 1. The lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, and sodium lauryl sulfate were mixed uniformly in a high-shear wet granulator, and a binder solution was added. Go through a 2.0mm sieve and sizing, and dry in a fluidized bed until the loss on drying (LOD) is less than 3.0%. The dry granules are sized through a 1.2mm sieve, then add the micronized rivaroxaban and mix well, then add the hard Magnesium fatty acid blend. The mixed granules are compressed into tablets with a diameter of 6mm and a hardness of 2-6kp.

[0034] The tablet weight, hardness, disintegration time limit, and friability of the samples of Comparative Examples 1 to 2 and Example 1 were tested, and the results were as follows:

[0035] Sample

Average tablet weight / mg

Average hardness / kp

Disintegration time limit

Friability

Comparative Example 1

85.4

4.5

15s

0.19％

Comparative Example 2

85.0

4.9 ...

Embodiment 2

[0040]

[0041] Mix lactose monohydrate, microcrystalline cellulose, croscarmellose sodium and sodium lauryl sulfate in a high-shear granulator, and add povidone in ethanol (95%) solution to granulate. Go through a 2.0mm sieve and sizing, and dry in a fluidized bed until the loss on drying (LOD) is less than 3.0%. The dry granules are sized through a 1.2mm sieve, then add the micronized rivaroxaban and mix well, then add stearic acid Magnesium blend. The mixed granules are compressed into tablets with a diameter of 6mm and a hardness of 2-6kp.

Embodiment 3

[0043]

[0044] Povidone is dissolved in 95% ethanol to make a binder solution. The lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, and polyoxyethylene hydrogenated castor oil are placed in a fluidized bed. In the fluidized state, spray the binder solution to granulate, and dry to LOD≤3.0%, pass through a 1.2mm sieve to obtain blank granules, add micronized rivaroxaban and mix well, then add magnesium stearate to mix . The mixed granules are compressed into tablets with a diameter of 6mm and a hardness of 2-6kp.

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Abstract

The invention relates to a quickly releasing oral solid medicinal composition containing rivaroxaban and a preparation method thereof. Proper medical auxiliaries are treated by a wet granulation process, and are mixed with active components of rivaroxaban to obtain the medicinal composition with remarkably improved dissolution. The preparation method has the characteristics of simple process and industrial production, and solves the problem of complicated preparation process in the prior art.

Description

Technical field [0001] The present invention relates to a method for preparing an oral solid pharmaceutical composition containing a coagulation factor Xa inhibitor (such as rivaroxaban). Background technique [0002] Rivaroxaban is a low-molecular-weight oral anticoagulant with high selectivity and direct inhibition of factor Xa. It is used for the prevention and / or treatment of various embolic diseases (see WO01 / 47919). Xarelto is well known and its chemical name is 5-chloro-nitrogen-((5S)-2-oxo-3-[-4-(3-oxo-4-morpholinyl)phenyl]-1,3- Azolidine-5-yl-2-thiophene-carboxamide has the following chemical structure: [0003] [0004] There are many crystal forms of Rivaroxaban. As described in the publications of WO2007 / 039132 and CN101282968A, there are crystal forms I, II, III and hydrates, NMP solvates and THF-containing clathrates, among which the crystal forms II has four times the solubility of crystalline form I, but due to the complicated process of preparing pure metastable ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/5377A61P7/02
Inventor 张晓花陈浩杜江永李巧霞
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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