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Rivaroxaban tablets and preparation method for same

A technology of rivaroxaban and prescription, which is applied in the direction of medical formula, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of slow disintegration and dissolution of azilsartan tablets, and achieve compression Good formability, uniform particle size, and the effect of improving production efficiency

Inactive Publication Date: 2015-11-25
JIANGSU ZHONGBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The present invention also provides a preparation method of the aforementioned rivaroxaban tablets, which solves the problem of slow disintegration and dissolution of azilsartan tablets

Method used

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  • Rivaroxaban tablets and preparation method for same
  • Rivaroxaban tablets and preparation method for same
  • Rivaroxaban tablets and preparation method for same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] 10mg tablet specifications:

[0053] Element

Content (mg)

Rivaroxaban

10

lactose monohydrate

30

Microcrystalline Cellulose (ph101)

40

Sodium dodecyl sulfate

2

Hydroxypropyl Methyl Cellulose (5cps)

2.2

Croscarmellose sodium (additional)

1.8

Croscarmellose sodium (additional)

1.8

Magnesium stearate

0.5

[0054] The preparation method is as follows:

[0055] 1) Micronizing the rivaroxaban raw material to a particle size D90≤15 μm;

[0056] 2) Lactose, microcrystalline cellulose, sodium lauryl sulfate, and croscarmellose sodium are passed through a 60-mesh sieve;

[0057] 3) Preparation of binder: prepare an 8% solution according to the ratio of hydroxypropyl methylcellulose (5cps):purified water=8:100 (W:V);

[0058] 4) Weigh and mix the processed rivaroxaban, lactose, microcrystalline cellulose, sodium lauryl sulfate, and partly added croscarmellose sodium acco...

Embodiment 2

[0067] 5mg tablet specifications:

[0068] Element

Content (mg)

Rivaroxaban

5

lactose monohydrate

20

Microcrystalline Cellulose (ph101)

30

Sodium dodecyl sulfate

1

Hydroxypropyl Methyl Cellulose (5cps)

2

Croscarmellose sodium (additional)

1.5

Croscarmellose sodium (additional)

1.5

Magnesium stearate

0.3

[0069] The preparation method is as follows:

[0070] 1) Micronizing the rivaroxaban raw material to a particle size D90≤15 μm;

[0071] 2) Lactose, microcrystalline cellulose, sodium lauryl sulfate, and croscarmellose sodium are passed through a 60-mesh sieve;

[0072] 3) Preparation of binder: prepare an 8% solution according to the ratio of hydroxypropyl methylcellulose (5cps):purified water=8:100 (W:V);

[0073] 4) Weigh and mix the processed rivaroxaban, lactose, microcrystalline cellulose, sodium lauryl sulfate, and partly added croscarmellose sodium accordin...

Embodiment 3

[0083] 20mg tablet specifications:

[0084] Element

Content (mg)

Rivaroxaban

20

lactose monohydrate

40

Microcrystalline Cellulose (ph101)

50

Sodium dodecyl sulfate

3

Hydroxypropyl Methyl Cellulose (5cps)

2.5

Croscarmellose sodium (additional)

2

Croscarmellose sodium (additional)

2

Magnesium stearate

0.8

[0085] The preparation method is as follows:

[0086] 1) Micronizing the rivaroxaban raw material to a particle size D90≤15 μm;

[0087] 2) Lactose, microcrystalline cellulose, sodium lauryl sulfate, and croscarmellose sodium are passed through a 60-mesh sieve;

[0088] 3) Preparation of binder: prepare an 8% solution according to the ratio of hydroxypropyl methylcellulose (5cps):purified water=8:100 (W:V);

[0089] 4) Weigh and mix the processed rivaroxaban, lactose, microcrystalline cellulose, sodium lauryl sulfate, and partly added croscarmellose sodium accordin...

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Abstract

The invention provides rivaroxaban tablets and a preparation method for the same, and belongs to the field of pharmacy. Each rivaroxaban tablet is prepared from the following components in percentage by mass: 8.16 to 16.63 percent of rivaroxaban, 30.00 to 35.00 percent of lactose monohydrate, 41.56 to 48.94 percent of microcrystalline cellulose (ph101), 1.63 to 2.49 percent of sodium dodecyl sulfate, 2.08 to 3.26 percent of hydroxypropyl methyl cellulose, 3.32 to 4.9 percent of croscarmellose sodium and 0.49 to 0.67 percent of magnesium stearate. According to the novel rivaroxaban tablets and the internal and external disintegrant addition mixed-tabletting preparation method, croscarmellose sodium is internally and externally added, so that the problem of slow disintegration and dissolution of azilsartan tablets is solved; with adoption of a fluidized bed top-spraying granulation method, three procedures of mixing, granulation and drying in a conventional process are implemented by one step, so that production efficiency is improved, prepared granules are uniform in granularity and high in flowability and compression formability, and in addition, the problems of sticking, loosening and the like in a tabletting process are also solved.

Description

technical field [0001] The invention relates to the field of pharmacy, discloses an oral preparation containing rivaroxaban, and also discloses a method for granulating rivaroxaban. Background technique [0002] Rivaroxaban is a highly selective oral drug that directly inhibits factor Xa; by inhibiting factor Xa, it can interrupt the intrinsic and extrinsic pathways of the blood coagulation cascade, inhibit the generation of thrombin and thrombus formation. [0003] Chinese name: Rivaroxaban; English name: Rivaroxaban; Structural formula: [0004] [0005] Rivaroxaban is the world's first oral direct factor Xa inhibitor, which can highly selectively and competitively inhibit free and bound factor Xa and prothrombin activity, and prolong the activated partial thromboplastin time plate in a dose-dependent manner (PT) and prothrombin time (aPTT), thereby prolonging the coagulation time and reducing thrombin formation. It has the characteristics of high bioavailability, bro...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/32A61K31/5377A61K47/38A61P7/02A61J3/00
Inventor 徐强夏彬许林菊绳则翠杨健
Owner JIANGSU ZHONGBANG PHARMA
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