Rivaroxaban-containing pharmaceutical preparation

A technology of rivaroxaban and pharmaceutical preparations, which is applied in the field of pharmaceutical preparations containing rivaroxaban and its preparation, achieving the effect of good stability

Active Publication Date: 2015-02-11
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to provide a rivaroxaban preparation that breaks through the conventional dosage of a disintegrant without adding a hydrophilic binder, so as to solve the problem that rivaroxaban needs to add a hydrophilic binder to improve the dissolution rate

Method used

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  • Rivaroxaban-containing pharmaceutical preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1. Preparation of Tablets Without Hydrophilic Binder (3.5% Disintegrant)

[0038] 1.1 Composition of Tablets (mg / tablet)

[0039]

[0040]

[0041] 1.2 Preparation

[0042] Dissolve sodium lauryl sulfate in water. The micronized rivaroxaban was added to the solution and stirred to make it dispersed uniformly to obtain a rivaroxaban suspension. The prepared suspension was added to an excipient consisting of microcrystalline cellulose, lactose and croscarmellose sodium for wet granulation. After drying, granulate with a 24-mesh sieve and then add magnesium stearate to mix. Then, the obtained granules are compressed into tablets with a hardness of 5-9 kg by using a punching die with a diameter of 6 mm, and coated, and the weight gain of the coating is controlled to be 3%.

[0043] 1.3 Evaluation

[0044] Method: Chinese Pharmacopoeia 2010 edition two X C second method paddle method

[0045] Medium: 900ml pH4.5 acetate buffer (containing 0.2% sodium dode...

Embodiment 2

[0056] Example 2. Preparation of Tablets Without Hydrophilic Binder (7% Disintegrant)

[0057] 1.1 Composition of Tablets (mg / tablet)

[0058]

[0059] 1.2 Preparation

[0060] Dissolve sodium lauryl sulfate in water. The micronized rivaroxaban was added to the solution and stirred to make it dispersed uniformly to obtain a rivaroxaban suspension. The prepared suspension was added to an excipient consisting of microcrystalline cellulose, lactose and croscarmellose sodium for wet granulation. After drying, granulate with a 24-mesh sieve and then add magnesium stearate to mix. Then, the obtained granules are compressed into tablets having a hardness of 5-9 kg by using a punching die with a diameter of 6 mm, and are coated with a coating weight gain of 3%.

[0061] 1.3 Evaluation

[0062] The dissolution measurement method is the same as that in Example 1. The result is as image 3 As shown, although the disintegration time of this product is longer than that of the tab...

Embodiment 3

[0070] Example 3. Preparation of Tablets Without Hydrophilic Binder (15% Disintegrant)

[0071] 1.1 Composition of Tablets (mg / tablet)

[0072]

[0073] 1.2 Preparation

[0074] Dissolve sodium lauryl sulfate in water. The micronized rivaroxaban was added to the solution and stirred to make it dispersed uniformly to obtain a rivaroxaban suspension. The prepared suspension was added to an excipient consisting of microcrystalline cellulose, lactose and croscarmellose sodium for wet granulation. After drying, granulate with a 24-mesh sieve and then add magnesium stearate to mix. Then, the obtained granules are compressed into tablets having a hardness of 5-9 kg by using a punching die with a diameter of 6 mm, and are coated with a coating weight gain of 3%.

[0075] 1.3 Evaluation

[0076] The dissolution measurement method is the same as that in Example 1. The result is as Figure 5 As shown, the disintegration time of this product is 5-6 minutes, and the dissolution t...

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Abstract

The invention relates to a rivaroxaban-containing pharmaceutical preparation. Specifically, the pharmaceutical preparation is composed of 3-30% of rivaroxaban, 7-50% of a disintegrant, 45-90% of a diluent, 0.1-5% of a wetting agent and 0.1-1% of a lubricant, wherein the sum of the weight percentages of the components is 100%. The conventional content of the disintegrant is broken, the viscous component proportion is increased, the disintegration time is prolonged so as to increase the wetting time of rivaroxaban, the problem of poor dissolvability of the insoluble drug rivaroxaban is solved, and simultaneously, the stability of the preparation is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a rivaroxaban-containing pharmaceutical preparation for treating adult patients undergoing elective hip or knee joint replacement surgery to prevent venous thrombosis (VTE) and a preparation method thereof. Background technique [0002] Rivaroxaban, developed and marketed by Bayer and Ortho-McNeil Pharmaceutical (a Johnson & Johnson subsidiary), is an oral factor Xa inhibitor. It was first listed in Europe in 2008, listed in the United States in 2011, and approved for listing in China in 2010. The trade name is Xarelto, which is produced by Bayer. [0003] According to the European Medicines Agency (EMA) drug evaluation report for Xarelto, rivaroxaban is a class II drug (low solubility, high permeability) in the Biopharmaceutical Classification System (BCS), solubility It will become an obstacle to its in vitro dissolution and in vivo absorption, which is overcome by pos...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K31/5377A61K47/38A61K47/32A61K47/36A61P7/02
Inventor 孙运栋孙长安王小雷
Owner JIANGSU HANSOH PHARMA CO LTD
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