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Rivaroxaban tablet and preparation method thereof

A technology of saban tablets and rivaroxaban, which is applied in the field of medicine, can solve the problems of affecting dissolution rate and stability, high loss rate of raw materials, and reducing production efficiency, so as to avoid the influence of heating and moisture and clean equipment Convenience and the effect of improving production efficiency

Active Publication Date: 2019-03-05
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The preparation process of the above-mentioned rivaroxaban tablets adopts wet granulation, and rivaroxaban has a certain hygroscopicity, and the use of wet granulation will lead to tablet pitting, sticky punching, loose tablets, and unqualified disintegration Phenomena such as dissolution and stability
Moreover, the preparation process of the above-mentioned rivaroxaban tablet all micronizes the raw material drug of rivaroxaban separately
Because rivaroxaban has a certain hygroscopicity, it is easy to adhere to the crushing chamber during the individual micronization process, resulting in a high loss rate of raw materials
The API adhered to the crushing chamber is difficult to scrape off, which not only affects the cleaning of the equipment, but also significantly reduces the production efficiency and increases the production cost
[0011] In order to solve the problems of complex preparation process and high loss of raw materials in the prior art, the present invention provides a new method for preparing rivaroxaban tablets that is suitable for industrial production and can reduce the loss of raw materials

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

[0043] Example 1: Preparation of rivaroxaban tablets by wet granulation

[0044] prescription:

[0045]

[0046]

[0047] Coating accessories:

[0048]

[0049] Preparation Process:

[0050] 1. Dissolve hydroxypropyl methylcellulose (5cp) and sodium lauryl sulfate in water.

[0051] 2. The raw material drug of rivaroxaban is air-pulverized, and the micronized raw material drug of rivaroxaban is suspended in the solution obtained in step 1.

[0052] 3. The suspension prepared in step 2 is sprayed as a granulation liquid on the stock solution composed of microcrystalline cellulose, lactose monohydrate and cross-linked carboxymethyl cellulose in the fluidized bed granulation stage.

[0053] 4. Dried and sieved (0.8mm sieve aperture), the gained granules were added and mixed with magnesium stearate.

[0054] 5. Tablet, coating.

Embodiment 2

[0055] Example 2: Preparation of rivaroxaban tablets by direct compression

[0056] prescription:

[0057]

[0058] Coating accessories:

[0059]

[0060]

[0061] Preparation Process:

[0062] 1. Mix and sieve rivaroxaban raw material drug, hydroxypropyl methylcellulose (5cp) and sodium lauryl sulfate (the sieve aperture is 180 μm) to obtain mixture 1;

[0063] 2. The mixture 1 was subjected to jet milling, and then mixed with lactose monohydrate of one-third of the prescription amount and sieved (the aperture of the sieve was 250 μm) to obtain the mixture 2;

[0064] 3. Mix the mixture 2 and the remaining prescription amount of lactose monohydrate, microcrystalline cellulose, and croscarmellose sodium and sieve it (the sieve aperture is 250 μm) to obtain the mixture 3;

[0065] 4. Mix mixture 3 and magnesium stearate evenly, and the powder is directly compressed into tablets and coated.

Embodiment 3

[0066] Example 3: Preparation of Rivaroxaban Tablets by Direct Compression

[0067] prescription:

[0068]

[0069] Preparation Process:

[0070] 1. Mix and sieve rivaroxaban raw material, copovidone and sodium lauryl sulfate (the sieve aperture is 180 μm) to obtain mixture 1;

[0071] 2. The mixture 1 was subjected to jet milling, and then mixed with lactose monohydrate of one-third of the prescription amount and sieved (the sieve aperture was 250 μm) to obtain the mixture 2;

[0072] 3. Mix the mixture 2 and the remaining prescription amount of lactose monohydrate, microcrystalline cellulose, and croscarmellose sodium and sieve it (the sieve aperture is 250 μm) to obtain the mixture 3;

[0073] 4. Mix mixture 3 and sodium stearyl fumarate evenly, and the powder is directly compressed into tablets and coated.

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Abstract

The present invention discloses a method for preparing rivaroxaban tablets by direct compression. A rivaroxaban active pharmaceutical ingredient is pulverized through air flow together with a binder and a surfactant, so that the mixture is not liable to adhere to a pulverization chamber during a pulverization process, thereby significantly reducing the loss rate of the active pharmaceutical ingredient. In addition, the rivaroxaban tablets are prepared by direct compression, which has strong process adaptability and good reproducibility, avoiding influences of heating and moisture during the process, and improving the stability of the medicine.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to a rivaroxaban tablet and a preparation method thereof, in particular to a method for preparing a rivaroxaban tablet by direct compression. Background technique [0002] Rivaroxaban, a highly selective factor Xa inhibitor, is an oral anticoagulant drug that can be used to prevent the formation of deep vein thrombosis (DVT) and pulmonary embolism (PE) in patients after hip and knee arthroplasty. It can be used to prevent stroke and non-central nervous system embolism in patients with non-valvular atrial fibrillation, and reduce the risk of coronary artery syndrome recurrence. The drug was jointly developed by Bayer Pharmaceuticals and Ortho-McNeil Pharmaceuticals, a subsidiary of Johnson & Johnson. It has been approved in more than 100 countries around the world, and has been successfully marketed by Bayer in more than 75 countries. [0003] The chemical name of Rivaroxaban is: 5-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/5377A61K47/32A61K47/38A61K47/20A61P7/02A61P9/10
CPCA61K9/2013A61K9/2027A61K9/2054A61K9/2095A61K9/2866A61K31/5377
Inventor 彭淑娟翟允耀李莉江竹莲尹娣孙艳清
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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