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Method for preparing rivaroxaban solid composition

A solid composition, rivaroxaban technology, applied in the field of medicine, can solve the problems of high calorie consumption, increase production cost, etc., and achieve the effect of increasing the dissolution rate

Inactive Publication Date: 2014-04-09
CHINA RESOURCES SAIKE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The most commonly used mechanical methods are ball milling and airflow crushing. After secondary crushing, the particle size can no longer be reduced to 15 μm. The above process refers to the patent EP 2308472A1; while the spray drying method requires high heat consumption and increases production costs. And the particle size cannot be controlled below the required 5μm

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] The concrete content of this embodiment is as follows:

[0018] (1) Pulverize the rivaroxaban API (API) with a jet mill, and measure its particle size with a Malvern laser particle size analyzer.

[0019] (2) The rivaroxaban raw material is mechanically sheared and pulverized, and its particle size is measured by a Malvern laser particle size analyzer.

[0020] (3) Mix the rivaroxaban raw material drug with sodium lauryl sulfate and hypromellose with water evenly, pulverize it with a high-speed bead mill, and measure its particle size with a Malvern laser particle size analyzer.

[0021] See attached table 1 for particle size measurement results.

[0022] Schedule 1

[0023] d（0.1） d（0.5） d（0.9） jet mill crushing 3.508 7.468 14.644 mechanical shear crushing 5.211 9.564 17.051 High-speed stirring ball mill crushing 0.53 1.62 4.17

Embodiment 2

[0025] In this embodiment, rivaroxaban tablets are prepared by airflow pulverization of rivaroxaban API. The rivaroxaban solid composition is made of the following raw materials: rivaroxaban API 10g, microcrystalline cellulose PH101 40g, monohydrate Lactose 27.9g, hypromellose 3g, croscarmellose sodium 3g, sodium lauryl sulfate 0.5g, magnesium stearate 0.6g. The preparation method comprises the following steps:

[0026] 1) Mix rivaroxaban API (not micronized), HPMC E5, sodium laurylsulfate and about 50ml of water to obtain suspension solution Ⅰ;

[0027] 2) Put the suspension solution I into a high-speed stirring bead mill for wet grinding and pulverization to obtain the suspension solution II;

[0028] 3) Add microcrystalline cellulose PH101, lactose monohydrate, and croscarmellose sodium into the fluidized bed, and fluidize and mix evenly;

[0029] 4) Spray the suspension solution II into the diluent of the composition in step 3) using a fluidized bed, and dry to prepa...

Embodiment 3

[0033] The formulation of the rivaroxaban solid composition described in this example is the same as that in Example 2. The API is jet milled and the rivaroxaban-containing granules are prepared by high-shear wet granulation. The preparation method comprises the following steps:

[0034] A. Pulverize the rivaroxaban API by airflow to obtain granule I;

[0035] B. Prepare hypromellose and sodium lauryl sulfate into a clear aqueous solution to obtain solution I;

[0036] C. Add granule I, microcrystalline cellulose PH101, lactose monohydrate, and croscarmellose sodium into a high-shear wet granulator, and mix well to obtain granule II;

[0037] D. Add solution I to granule II, and through shearing, prepare granule III containing rivaroxaban solid composition

[0038] E. drying the above granules to obtain granules IV;

[0039] F. Add granule IV to magnesium stearate and mix evenly to obtain granule V;

[0040] G. Granules Ⅴ Compression and coating.

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PUM

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Abstract

The invention discloses a method for preparing a rivaroxaban solid composition. The method comprises the following steps: crushing rivaroxaban by adopting a wet crushing method, and simultaneously preparing a suspension solution; spraying the suspension solution into other auxiliaries to prepare grains with proper sizes; further preparing minimum medical dosage units. The method has the beneficial effects that: the problem that the grain diameter cannot be reduced to 5mu m when rivaroxaban particles are prepared by adopting a conventional crushing method can be solved, and the dissolution speed of the rivaroxaban preparation can be increased.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to a preparation method of a rivaroxaban solid composition. Background technique [0002] Rivaroxaban is used to prevent the development of deep vein thrombosis (DVT) and pulmonary embolism (PE) in patients after hip and knee replacement surgery. 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. The drug was first approved by Bayer Pharmaceuticals in Canada in 2008, marking a milestone for the most widely used drug of its kind. [0003] Rivaroxaban is a poorly soluble drug with a solubility in water of 5-7 μg / ml. The bioavailability of a drug in the body is greatly affected by the dissolution of the drug. Therefore, in the preparation of its preparation, micronized rivaroxaban particles are often used, and the particle size is controlled bel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61P7/02A61P11/00A61P9/10
Inventor 苏小楠蒋玲敏高超杨琰王文峰
Owner CHINA RESOURCES SAIKE PHARMA
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