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Aspirin and rivaroxaban compound preparation and preparation method thereof

A technology of rivaroxaban and aspirin, which is applied in the field of compound preparations of aspirin and rivaroxaban and its preparation, and can solve problems such as no cases of successful development

Active Publication Date: 2021-03-09
LEPU PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In view of the characteristics of rivaroxaban, it is a great technical challenge to develop a sustained-release formulation to be taken once a day, and no successful case has been seen so far

Method used

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  • Aspirin and rivaroxaban compound preparation and preparation method thereof
  • Aspirin and rivaroxaban compound preparation and preparation method thereof
  • Aspirin and rivaroxaban compound preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] Example 1: Preparation of Rivaroxaban Sustained-release Tablets (I)

[0077] Table 1 Composition of Rivaroxaban Sustained-release Tablets (I)

[0078]

[0079] Preparation Process:

[0080] Granulation: add the other materials of the plain tablet except magnesium stearate into the wet granulator, the speed of the stirring paddle is 300rpm, the cutting knife is 500rpm, and mix for 5min; Finish adding in about 7 minutes; the speed of the stirring blade is 250rpm, the cutter is 1200rpm, and the granulation is 2min; the material is discharged, the screen of the granulator is 3×3mm, the speed is 400rpm, and the granules are wet granulated; the wet granules are added to the fluidized bed, and the air is 60°C , air volume 30Hz, drying, when the temperature of the material reaches 40°C, take a sample to measure the moisture, stop heating when the moisture is lower than 2.0%, cool and discharge; the screen diameter of the granulator is 1.0mm, the speed is 400rpm, dry granula...

Embodiment 2

[0084] Example 2: Preparation of Rivaroxaban Sustained-release Tablets (II)

[0085] Table 2 Composition of Rivaroxaban Sustained-release Tablets (Ⅱ)

[0086] Name of raw material model Unit prescription (mg / tablet) Rivaroxaban D90<15um

5 Hypromellose 2280 K100M 6 Hypromellose 2910 E50 24 microcrystalline cellulose SH-101 25 lactose monohydrate 200 mesh 16 Hypromellose EXF 3.2 Magnesium stearate / 0.8 Hypromellose 2910 E5 3.2 polyethylene glycol PEG6000 0.8

[0087] Preparation Process:

[0088] Granulation: add the other materials of the plain tablet except magnesium stearate into the wet granulator, the speed of the stirring paddle is 300rpm, the cutting knife is 500rpm, and mix for 5min; Finish adding in about 7 minutes; the speed of the stirring blade is 250rpm, the cutter is 1200rpm, and the granulation is 2min; the material is discharged, the screen of the granulator is 3×3mm, the s...

Embodiment 3

[0092] Example 3: Preparation of Rivaroxaban Sustained-release Tablets (Ⅲ)

[0093] Table 3 Composition of Rivaroxaban Sustained-release Tablets (Ⅲ)

[0094] Name of raw material model Unit prescription (mg / tablet) Rivaroxaban D90<15um

1.25 Hypromellose 2280 K100M 2.5 Hypromellose 2910 E50 6 microcrystalline cellulose SH-101 4.1 lactose monohydrate 200 mesh 5.25 Hypromellose EXF 0.8 Magnesium stearate / 0.1 Hypromellose 2910 E5 1.6 polyethylene glycol PEG6000 0.4

[0095] Preparation Process:

[0096] Granulation: add the other materials of the plain tablet except magnesium stearate into the wet granulator, the speed of the stirring paddle is 300rpm, the cutting knife is 500rpm, and mix for 5min; Finish adding in about 7 minutes; the speed of the stirring blade is 250rpm, the cutter is 1200rpm, and the granulation is 2min; the material is discharged, the screen of the granulator is 3×3mm,...

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Abstract

The invention discloses an aspirin and rivaroxaban compound preparation and a preparation method thereof. The compound preparation is prepared by filling aspirin micro-tablets and rivaroxaban micro-tablets into capsules, wherein aspirin is released in an enteric manner, rivaroxaban is released in a slow-release manner, and aspirin and rivaroxaban are used for treating thrombolysis and preventing thrombosis and other related diseases; the aspirin micro-tablets are enteric-coated tablets, the specification is 25-100 micrograms / tablet, and each capsule is filled with 1-4 aspirin micro-tablets; and the specification of the rivaroxaban micro-tablets is 1.25-20 micrograms / tablet, and each capsule is filled with 1-8 rivaroxaban micro-tablets. According to the compound solid preparation, differentmedicines and different types of micro-tablets are filled into the same capsule to prepare the compound preparation, so that the compound preparation is convenient for patients to take, and the riskof missing taking is reduced. Moreover, the capsule is convenient to open, and the micro-tablet filled capsule has a more flexible administration mode.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a compound preparation of aspirin and rivaroxaban and a preparation method thereof. Background technique [0002] Aspirin is a commonly used antithrombotic drug on the market. Its antithrombotic mechanism is: irreversibly inhibiting the synthesis of cyclooxygenase, reducing the production of prostaglandins and inhibiting the production of platelet thromboxane A2, thereby inhibiting platelet adhesion and aggregation, affecting Formation of thrombus. [0003] Rivaroxaban is an oral anticoagulant that directly inhibits factor Xa with high selectivity. By directly inhibiting factor Xa, the intrinsic and extrinsic pathways of the coagulation cascade can be interrupted, thrombin generation and thrombus formation can be inhibited. Rivaroxaban was developed by Bayer Pharmaceuticals, Germany, and was approved for marketing by the European Union on September 30, 2008. It w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/616A61K9/62A61K9/58A61P7/02A61P9/10A61P9/00A61P9/06A61K31/5377A61K9/36A61K9/32
CPCA61K31/616A61K31/5377A61K9/5084A61P7/02A61P9/10A61P9/00A61P9/06A61K9/2846A61K9/2866A61K2300/00
Inventor 付晓宁骆献丽朱建中刘文省
Owner LEPU PHARMACEUTICAL CO LTD
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