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A kind of rivaroxaban suspension and preparation method thereof

A technology of rivaroxaban and suspension, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of low solubility of rivaroxaban and achieve optimal preparation Process, enhanced stability, improved dispersibility

Active Publication Date: 2022-03-08
THE FIRST AFFILIATED HOSPITAL OF ZHENGZHOU UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Overcoming the deficiencies in the prior art, the invention provides a suspension of rivaroxaban, which solves the problem of low solubility of rivaroxaban by making the suspension of rivaroxaban, by optimizing the type of stabilizer, Optimizing the preparation process enhances the stability of rivaroxaban suspension and improves the bioavailability of the drug

Method used

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  • A kind of rivaroxaban suspension and preparation method thereof
  • A kind of rivaroxaban suspension and preparation method thereof
  • A kind of rivaroxaban suspension and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0037] Embodiment 1 rivaroxaban suspension (1000 doses)

[0038]

[0039] Preparation:

[0040] (1) Use a colloid mill to micronize rivaroxaban, add xanthan gum for liquid addition grinding, and grind to a particle size of 5-10 μm;

[0041] (2) Add tragacanth gum to the micronized rivaroxaban in step (1), and mix well;

[0042] (3) Add potassium chloride and sodium citrate to step (2), add water to 5000ml, and mix well.

Embodiment 2

[0043] Embodiment 2 rivaroxaban suspension (1000 doses)

[0044]

[0045] Preparation:

[0046] (1) Use a colloid mill to micronize rivaroxaban, add xanthan gum for liquid addition grinding, and grind to a particle size of 5-10 μm;

[0047] (2) Add tragacanth gum to the micronized rivaroxaban in step (1), and mix well;

[0048] (3) Add potassium chloride and sodium citrate to step (2), add water to 5000ml, and mix well.

Embodiment 3

[0049] Embodiment 3 rivaroxaban suspension (1000 doses)

[0050]

[0051] Preparation:

[0052] (1) Use a colloid mill to micronize rivaroxaban, add xanthan gum for liquid addition grinding, and grind to a particle size of 5-10 μm;

[0053] (2) Add tragacanth gum to the micronized rivaroxaban in step (1), and mix well;

[0054] (3) Add potassium chloride and sodium citrate to step (2), add water to 5000ml, and mix well.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to a rivaroxaban suspension and a preparation method thereof. The suspension includes rivaroxaban, a suspending agent, a wetting agent and a flocculant. The present invention solves the problem of low solubility of rivaroxaban by making rivaroxaban into a suspension, and strengthens the rivaroxaban by optimizing the type and proportion of auxiliary materials in the rivaroxaban suspension and optimizing the preparation process. The stability of the class suspension improves the bioavailability of the drug.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a rivaroxaban suspension and a preparation method thereof. Background technique [0002] Rivaroxaban is an odorless, non-hygroscopic, white to yellowish powder of low solubility and high permeability used to prevent deep vein thrombosis (DVT) and pulmonary embolism in patients after hip and knee arthroplasty (PE) formation. It can also 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. [0003] Rivaroxaban is an insoluble drug, slightly soluble in DMSO, DMF, acetonitrile, dichloromethane, chloroform, acetone and other organic solvents, and its solubility in water is 5-7 μg / ml. Solubility is the limiting factor for its absorption, and the bioavailability in vivo is greatly affected by the dissolution of the drug. Therefore...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/5377A61K47/02A61K47/04A61K47/10A61K47/12A61K47/26A61K47/36A61P7/02A61P9/10A61P9/14A61P11/00A61P25/00
CPCA61K31/5377A61K9/10A61K47/36A61K47/10A61K47/26A61K47/02A61K47/12A61P7/02A61P11/00A61P9/14A61P9/10A61P25/00
Inventor 王闯建
Owner THE FIRST AFFILIATED HOSPITAL OF ZHENGZHOU UNIV
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