Solid composition containing rivaroxaban and preparation method thereof

A solid composition, the technology of rivaroxaban is applied in the directions of medical preparations containing active ingredients, medical preparations without active ingredients, drug combinations, etc. Rivaroxaban has problems such as large particle size, and achieves the effect of small total impurities, ensuring safety and good stability

Inactive Publication Date: 2018-03-09
CHONGQING ZEN PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The rivaroxaban is pulverized by airflow. During the pulverization process, the adhesion of rivaroxaban is enhanced, and it is easy to adhere to the inside of the equipment, prolonging the pulverization time and reducing the yield; the particle

Method used

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  • Solid composition containing rivaroxaban and preparation method thereof
  • Solid composition containing rivaroxaban and preparation method thereof
  • Solid composition containing rivaroxaban and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Embodiment 1: prepare with 50,000 prescription quantities

[0067] Product Prescription:

[0068]

[0069] Preparation Process:

[0070] 1. Crushing of raw materials: mix rivaroxaban and lactose monohydrate at a ratio of 1:2, pass through a 60-mesh sieve twice, and grind to a particle size (D 90 ) is less than 10 μm, to obtain micronized rivaroxaban monohydrate lactose mixture;

[0071] 2. Dissolve the prescribed amount of hypromellose and sodium lauryl sulfate in purified water to obtain solution I;

[0072] 3. Mixing: Weigh the prescription amount of micronized rivaroxaban lactose monohydrate mixture, microcrystalline cellulose PH101, and croscarmellose sodium and mix them in a mixer, stir and mix at a low speed for 5 minutes, until dry mixed powder;

[0073] 4. Granulation: Add solution Ⅰ into the dry mixed powder under low-speed stirring to make soft material, and granulate the soft material with a oscillating granulator (16-mesh nylon screen) to obtain wet g...

Embodiment 2

[0085] Embodiment 2: prepare with 50,000 prescription quantities

[0086] Product Prescription:

[0087]

[0088] Preparation Process:

[0089] 1. Grinding of raw materials: mix rivaroxaban and lactose monohydrate at a ratio of 1:3, pass through a 60-mesh sieve twice, and grind to a particle size (D 90) is less than 10 μm, to obtain a micronized rivaroxaban monohydrate lactose mixture;

[0090] 2. Dissolve the prescribed amount of hypromellose and sodium lauryl sulfate in purified water to obtain solution I;

[0091] 3. Mixing: Weigh the prescribed amount of micronized rivaroxaban lactose monohydrate mixture, microcrystalline cellulose PH101, and croscarmellose sodium, mix them in a mixer, stir and mix at a low speed for 8 minutes, and dry mixed powder;

[0092] 4. Granulation: Add solution Ⅰ into the dry mixed powder under low-speed stirring to make soft material, and granulate the soft material with a oscillating granulator (16-mesh nylon screen) to obtain wet granule...

Embodiment 3

[0101] Embodiment 3: Prepare with 50,000 prescription quantities

[0102] Product Prescription:

[0103] Micronized rivaroxaban monohydrate lactose mixture

2500g

Microcrystalline Cellulose PH101

1367g

hypromellose

127g

Croscarmellose Sodium

170g

Sodium dodecyl sulfate

43g

Magnesium stearate

43g

batch

50000 pieces

[0104] Preparation Process:

[0105] 1. Crushing of raw materials: mix rivaroxaban and lactose monohydrate at a ratio of 1:5, pass through a 60-mesh sieve twice, and grind to a particle size (D 90 ) is less than 10 μm, to obtain a micronized rivaroxaban monohydrate lactose mixture;

[0106] 2. Dissolve the prescribed amount of hypromellose and sodium lauryl sulfate in purified water to obtain solution I;

[0107] 3. Mixing: Weigh the prescription amount of micronized rivaroxaban lactose monohydrate mixture, microcrystalline cellulose PH101, and croscarmellose sodium and mix them in a mix...

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Abstract

The invention discloses a solid composition containing rivaroxaban. The solid composition is prepared from the following components in percentage by weight: 20 percent to 80 percent of a micronized rivaroxaban lactose monohydrate mixture, wherein in the micronized rivaroxaban lactose monohydrate mixture, the weight percent ratio of rivaroxaban to lactose monohydrate ranges from (1 to 2) to (1 to 10); the solid composition is prepared from the following components: 20 percent to 80 percent of a diluting agent, 1 percent to 10 percent of a bonding agent, 2 percent to 8 percent of a disintegrating agent, 0.5 percent to 8 percent of a surfactant and 0.5 percent to 5 percent of a lubricant. Furthermore, the invention further provides a preparation method of the solid composition containing therivaroxaban; the preparation method comprises the following steps: crushing crude drugs, mixing, granulating, drying, totally blending, tabletting and coating. Compared with the prior art, a crushingmethod of the crude drugs has high yield and the crude drugs have small granularity and are uniformly micronized; rivaroxaban tablets disclosed by the invention have a high dissolution rate, the content of a single impurity and total impurities is lower and the stability is high; the production quality is ensured.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a solid composition containing rivaroxaban and a preparation method thereof. Background technique [0002] Rivaroxaban is a highly selective drug that interrupts the intrinsic and extrinsic pathways of the coagulation cascade by directly inhibiting factor Xa, inhibiting the generation of thrombin and the formation of thrombus. [0003] Rivaroxaban, developed by Bayer, is a chemically synthesized small molecule compound, English name: Rivaroxaban, chemical name: 5-chloro-N-({(5S)-2-oxo-3-[-4-(3- Oxygen-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl})-2-thiophene-carboxamide, the structural formula is: [0004] Rivaroxaban is a poorly soluble drug with a solubility in water of about 10 mg / mL at room temperature. In the biopharmaceutical classification system (BCS), it belongs to class II, that is, low solubility and high permeability. The solubility of the drug has a grea...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K31/5377A61K47/26A61P7/02
CPCA61K9/2018A61K9/2054A61K9/2095A61K9/2806A61K31/5377
Inventor 叶敏肖玉梅罗礼平商露陈波
Owner CHONGQING ZEN PHARMACEUTICAL CO LTD
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