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Preparation method of rivaroxaban-containing pharmaceutical composition

A technology of rivaroxaban and composition, applied in the field of preparation of rivaroxaban pharmaceutical composition, capable of solving the problems of complex preparation process, slow dissolution of rivaroxaban, incomplete dissolution, etc.

Inactive Publication Date: 2020-03-20
QILU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] In order to solve the problems of complex preparation process, slow dissolution and incomplete dissolution of rivaroxaban in the prior art, the present invention provides a compound with simple composition, convenient and environmentally friendly process, suitable for industrial production, and capable of rapid dissolution of rivaroxaban. Oral solid pharmaceutical composition and preparation method thereof

Method used

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  • Preparation method of rivaroxaban-containing pharmaceutical composition
  • Preparation method of rivaroxaban-containing pharmaceutical composition
  • Preparation method of rivaroxaban-containing pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1. Fluidized bed granulation method: the specification is 20 mg, and the prescription quantity is 1000 tablets.

[0039] 1.1 Tablet composition (mg / tablet)

[0040]

[0041] Film coating (Opadry)

[0042]

[0043]

[0044] 1.2 The preparation steps of embodiment 1:

[0045] (1) Preparation of granulation solution: Dissolve sodium lauryl sulfate in water, disperse micronized active substance (I) in the solution, and then disperse croscarmellose sodium in the solution ,spare;

[0046] (2) Fluidized bed granulation: spray the above granulation solution onto lactose and microcrystalline cellulose until the solution is completely sprayed; continue to dry until the moisture content of the granules is ≤3%;

[0047] (3) Grain granulation; use 1.2mm round hole sieve for granulation;

[0048] (4) mixing: magnesium stearate is mixed with the above-mentioned granules;

[0049] (5) Tablet pressing: use 7mm round punching tablet, hardness control 30N-70N;

...

Embodiment 2

[0052] Embodiment 2. Fluidized bed granulation method: the specification is 20 mg, and the prescription quantity is 1000 tablets.

[0053] 2.1 Tablet composition (mg / tablet)

[0054]

[0055] Film coating (Opadry)

[0056]

[0057] 2.2 The preparation steps of embodiment 2:

[0058] (1) Preparation of granulation solution: Dissolve sodium lauryl sulfate in water, disperse micronized active substance (I) in the solution, and then disperse croscarmellose sodium in the solution ,spare;

[0059] (2) Fluidized bed granulation: spray the above granulation solution onto lactose, hypromellose and microcrystalline cellulose until the solution is completely sprayed; continue to dry until the moisture content of the granules is ≤3%;

[0060] (3) Grain granulation; use 1.2mm round hole sieve for granulation;

[0061] (4) mixing: magnesium stearate is mixed with the above-mentioned granules;

[0062] (5) Tablet pressing: use 7mm round punching tablet, hardness control 30N-70N; ...

Embodiment 3

[0065] Example 3. High-shear wet mixing granulation method: the specification is 20 mg, and the prescription quantity is 1000 tablets.

[0066] 3.1 Tablet composition (mg / tablet)

[0067]

[0068] Film coating (Opadry)

[0069]

[0070] 3.2 The preparation steps of embodiment 3:

[0071] (1) Premixing: Mix lactose and microcrystalline cellulose evenly in high-shear wet mixing granulation;

[0072] (2) Wet granulation: Dissolve sodium lauryl sulfate in water, disperse micronized active substance (I) in the solution, then disperse cross-linked carmellose sodium in the solution to obtain A granulation solution containing the active substance (I); adding the above granulation solution to the premixed material until all the addition is complete; passing the wet granules through a 5mm×4mm square hole sieve for wet sizing;

[0073] (3) Drying: move the wet granules into a fluidized bed for drying, adjust the parameters according to the fluidization state of the material, and...

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Abstract

The invention relates to a preparation method of a rivaroxaban-containing pharmaceutical composition. The preparation method of the rivaroxaban-containing pharmaceutical composition comprises the following steps: treating active substances by granulation liquid containing a solvent, a wetting agent and an optional disintegrating agent, and granulating pharmaceutically acceptable auxiliary materials by using liquid containing the active substances through a wet granulation process so as to obtain the pharmaceutical composition with remarkably improved dissolution. The preparation method has thecharacteristics of simple process and suitability for industrial production, and is favorable for ensuring the safety, effectiveness and long-term storage of clinical medicines.

Description

technical field [0001] The invention relates to a preparation method of a rivaroxaban pharmaceutical composition, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Rivaroxaban (Rivaroxaban) is a low molecular weight oral anticoagulant with high selectivity and direct inhibitory factor Xa, jointly developed by Bayer and Johnson & Johnson, the trade name is It was launched in Europe and Canada in 2008, in China in 2009, and in the United States in 2011. There are currently seven approved indications for rivaroxaban: (1) prevention of stroke and systemic embolism and one or more risk factors in adult patients with nonvalvular atrial fibrillation (AF); (2) adult pulmonary embolism ( (3) treatment of deep vein thrombosis (DVT) in adults; (4) prevention of recurrent PE and DVT in adults; (5) prevention of venous thromboembolism (VTE) in adult patients undergoing elective hip replacement surgery (6) prophylaxis of (VTE) in adult patie...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K9/20A61K47/38A61K47/20A61K31/5377A61P7/02
CPCA61K9/2013A61K9/2054A61K9/2866A61K31/5377A61P7/02
Inventor 赵娜娜郑晓清汪文化杨清敏张明会
Owner QILU PHARMA CO LTD