Rivaroxaban-containing tablets

A rivaroxaban and tablet technology, which is applied in the directions of medical preparations containing active ingredients, pill delivery, and non-active ingredients medical preparations, etc. Internal and external differences, poor drug dissolution, etc., to achieve the effects of rapid dissolution, convenient operation, and simple preparation process

Active Publication Date: 2015-06-24
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The chemical name of rivaroxaban is 5-chloro-nitrogen-((5S)-2-oxo-3-[-4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidine -5-yl-2-thiophene-carboxamide, which is slightly soluble in acetone, polyethylene glycol 400, and almost insoluble in water, so the existing rivaroxaban solid oral preparation has a very low dissolution rate
In order to solve the problem of poor drug dissolution, a large number of surfactants have been added to the marketed rivaroxaban tablets
Since a large number of surfactants may cause individual differences in vivo and in vitro, improving the dissolution rate of active ingredients in formulations is still a difficult problem for those skilled in the art
[0004] At present, the prior art has not reported a kind of rivaroxaban tablet with higher dissolution rate and its preparation method

Method used

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  • Rivaroxaban-containing tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1 Rivaroxaban tablet preparation

[0020] Prescription and preparation process

[0021]

[0022] Mix rivaroxaban and lactose evenly, ultrafinely pulverize, D90<25 μm, then mix evenly with microcrystalline cellulose, sodium carboxymethyl starch, magnesium stearate, and directly compress into tablets.

Embodiment 2

[0023] Embodiment 2 Rivaroxaban tablet preparation

[0024] Prescription and preparation process

[0025]

[0026]

[0027] Mix rivaroxaban and mannitol evenly, ultrafinely pulverize, D90<5 μm, then mix evenly with sodium carboxymethyl starch, granulate, add magnesium stearate, mix evenly, and compress into tablets to obtain.

Embodiment 3

[0028] Example 3 Preparation of Rivaroxaban Tablets

[0029] Prescription and preparation process

[0030]

[0031] Mix rivaroxaban and lactose evenly, ultrafinely pulverize, D90<0.1 μm, then mix evenly with crospovidone, granulate, add magnesium stearate, mix evenly, and compress into tablets.

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PUM

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Abstract

The present invention discloses rivaroxaban-containing tablets, which are prepared from a raw material containing micronized rivaroxaban and an auxiliary material containing a water soluble filler, wherein a weight ratio of the rivaroxaban to the water soluble filler is 1:0.5-50, and the water-soluble filler is one or a plurality of materials selected from lactose, mannitol, sorbitol and sucrose. According to the present invention, the hydrophilicity of the rivaroxaban is significantly improved, the rapid dissolution the rivaroxaban in the gastrointestinal tract body fluid is easily achieved, the preparation process is simple, the operation is convenient, and the method is suitable for industrial large-scale production.

Description

technical field [0001] The invention belongs to the technical field of western medicine preparations, in particular to a solid preparation of rivaroxaban, in particular to a tablet containing rivaroxaban. Background technique [0002] Rivaroxaban is a highly selective, oral agent that directly inhibits factor Xa. Inhibition of factor Xa can interrupt the intrinsic and extrinsic pathways of the blood coagulation cascade, inhibit the generation of thrombin and thrombus formation. The drug can be used to prevent the formation of deep vein thrombosis (DVT) and pulmonary embolism (PE) in patients after hip and knee replacement, and can also be used to prevent stroke and non-central nervous system embolism in patients with non-valvular atrial fibrillation. Reduce the risk of coronary artery syndrome recurrence, etc. [0003] The chemical name of rivaroxaban is 5-chloro-nitrogen-((5S)-2-oxo-3-[-4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidine -5-base-2-thiophene-carboxamide, which...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/5377A61K47/26A61K47/10A61P7/02
Inventor 赵志全郝贵周张庆刚
Owner SHANDONG NEWTIME PHARMA
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