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Rivaroxaban tablet and preparation method thereof

A technology for rivaroxaban and tablets, which is applied in the directions of pill delivery, pharmaceutical formulations, and non-active ingredients medical preparations, etc., can solve the problems of limited wide application, safety problems, large changes in substances, etc., and achieves good fluidity. , The effect of improving stability and high dissolution

Inactive Publication Date: 2016-01-27
SHIJIAZHUANG KANGHEWEI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] It has been found through research that the current rivaroxaban tablets have poor stability and relatively large changes in related substances, which have potential safety problems and limit their wide clinical application

Method used

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  • Rivaroxaban tablet and preparation method thereof
  • Rivaroxaban tablet and preparation method thereof
  • Rivaroxaban tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1 Preparation of rivaroxaban according to the present invention

[0031] Weigh 10 g of crude rivaroxaban, add it into 50 mL of dioxane: acetonitrile: water = 1:2.5:1 mixed solvent, stir, heat to reflux, dissolve completely, reflux for 20 minutes, and then Lower the temperature of the reaction solution to 10°C at a cooling rate of 10°C, stir at this temperature for 1 hour at a stirring speed of 50 rpm, filter, and dry the obtained solid at 35°C overnight to obtain 9.85 g of rivaroxaban, Yield 98.5%.

[0032] In the X-ray powder diffraction pattern of rivaroxaban prepared in this example, the 2θ is 11.0±0.2, 12.9±0.2, 13.3±0.2, 13.6±0.2, 14.5±0.2, 16.0±0.2, 17.7±0.2 , 18.5±0.2, 21.3±0.2, 21.7±0.2, 22.5±0.2, 22.9±0.2, 25.5±0.2, 26.3±0.2, 26.75±0.2 have characteristic absorption peaks, such as figure 1 shown.

[0033] The rivaroxaban differential scanning calorimetry method determines that rivaroxaban has an endothermic peak at 204.3°C to 212.6°C, and the peak...

Embodiment 2

[0035] Embodiment 2 Preparation of rivaroxaban according to the present invention

[0036] Weigh 10g of the crude product of rivaroxaban, add it into 30ml of dioxane: acetonitrile: water = 1:2.5:1 mixed solvent, stir, heat up to reflux, completely dissolve, reflux for 20 minutes, at 10°C per hour Reduce the temperature of the reaction solution to 10°C at the cooling rate, stir at this temperature for 1 hour at a stirring speed of 50 rpm, filter, and dry the obtained solid at 35°C overnight to obtain 9.61 g of rivaroxaban. The rate is 96.1%.

[0037] The X-ray powder diffraction pattern, differential scanning thermogram, and thermogravimetric pattern of the rivaroxaban prepared in this example are the same as in Example 1.

Embodiment 3

[0038] Embodiment 3 Preparation of rivaroxaban according to the present invention

[0039] Weigh 10 g of the crude product of rivaroxaban, add it into 70 ml of dioxane: acetonitrile: water = 1:2.5:1 mixed solvent, stir, heat up to reflux, completely dissolve, reflux for 20 minutes, at 20 ° C per hour Reduce the temperature of the reaction solution to 10°C at a cooling rate of 10°C, stir at this temperature for 1 hour at a stirring speed of 50 rpm, filter, and dry the obtained solid at 35°C overnight to obtain 9.55 g of rivaroxaban. The rate is 95.5%.

[0040] The X-ray powder diffraction pattern, differential scanning thermogram, and thermogravimetric pattern of the rivaroxaban prepared in this example are the same as in Example 1.

[0041] Test Example 1 High Temperature Stability Test

[0042] Take the rivaroxaban prepared in the above-mentioned Examples 1-3, put it in a flat weighing bottle, spread it into a thin layer with a thickness of ≤5mm, and put it in a thermostat ...

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Abstract

The invention relates to a Rivaroxaban tablet and a preparation method thereof, and belongs to the technical field of medicinal preparations. The Rivaroxaban tablet is prepared from, by weight, 10-20 parts of Rivaroxaban, 4 parts of internally-added superfine silica powder, 21-25 parts of internally-added microcrystalline cellulose, 22.9-24.9 parts of lactose-monohydrate, 2 parts of internally-added croscarmellose sodium, 10-14 parts of externally-added microcrystalline cellulose, 1 part of externally-added croscarmellose sodium, 3 parts of hydroxypropyl methyl cellulose 5cp, 0.5 part of lauryl sodium sulfate and 0.6 part of externally-added superfine silica powder. According to the Rivaroxaban tablet, the mutual synergistic effect is achieved at the specific matching, and the stability of tablet products is greatly improved; in addition, the dissolution rate is high, the quality problem existing in existing products all the time is solved, the safety, effectiveness and long-term storage of clinical medication can be better guaranteed.

Description

technical field [0001] The invention relates to a tablet and a preparation method thereof, in particular to a rivaroxaban tablet and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] The chemical name of rivaroxaban is 5-chloro-nitrogen-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazole Alk-5-yl}-methyl)-2-thiophenecarboxamide has the following chemical structure. [0003] [0004] Rivaroxaban is a low molecular weight oral anticoagulant with high selective inhibition of factor Xa, used to prevent deep vein thrombosis and pulmonary embolism in patients after hip or knee replacement. [0005] It has been found through research that the current rivaroxaban tablet has poor stability, and the related substances have changed greatly, which has potential safety problems, which limits its wide clinical application. Contents of the invention [0006] In view of the deficiencies in the prior ar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/5377A61K47/38A61P7/02C07D413/14
Inventor 刘宏果刘广慧席宁韩天佼田英涛周静
Owner SHIJIAZHUANG KANGHEWEI PHARMA
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