Apixaban pharmaceutical composition and preparation method thereof

A technology of apixaban and a composition, applied in the field of pharmaceutical preparations, can solve problems such as being unsuitable for industrial production, agglomeration, etc., and achieve the effects of no fracture, no agglomeration, and good fluidity

Active Publication Date: 2021-08-17
CHANGZHOU HANSOH PHARM CO LTD
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This invention increases dissolution by reducing the particle size of raw materials, but if the particle size is too small, serious agglomeration often occurs, which is not suitable for industrial production

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Apixaban pharmaceutical composition and preparation method thereof
  • Apixaban pharmaceutical composition and preparation method thereof
  • Apixaban pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Tablet prescription:

[0054]

[0055]

[0056] Preparation Process:

[0057] (1) Pretreatment of raw and auxiliary materials: pulverize apixaban, its d(0.9) is 21.0 μm, pass lactose and microcrystalline cellulose through a 60-mesh sieve, and pulverize the sodium lauryl sulfate through a 60-mesh sieve;

[0058] (2) Add the prescribed amount of anhydrous lactose, microcrystalline cellulose, sodium lauryl sulfate, croscarmellose sodium and apixaban into the fixed hopper mixer, set the speed at 10 rpm, and mix for 20 minutes

[0059] (3) Mix the intermediate material obtained in (2) with the added magnesium stearate for 5 minutes.

[0060] (4) Add the intermediate material obtained in (3) to the dry granulator for granulation, adjust the frequency conversion of feeding in the range of 8-30Hz, adjust the frequency conversion of tabletting in the range of 10-30Hz, and adjust the frequency conversion of granulation in the range of 10-30Hz Adjust within the range, the ...

Embodiment 2

[0065] Tablet prescription:

[0066]

[0067]

[0068] Preparation Process:

[0069] (1) Pretreatment of raw and auxiliary materials: pulverize apixaban, its d(0.9) is 20.1 μm, pass lactose and microcrystalline cellulose through a 60-mesh sieve, and pulverize the sodium lauryl sulfate through a 60-mesh sieve;

[0070] (2) Add the prescribed amount of anhydrous lactose, microcrystalline cellulose, sodium lauryl sulfate, croscarmellose sodium and apixaban into the fixed hopper mixer, set the speed at 10 rpm, and mix for 20 minutes

[0071] (3) Mix the intermediate material obtained in (2) with the added magnesium stearate for 5 minutes.

[0072] (4) Add the intermediate material obtained in (3) to the dry granulator for granulation, adjust the frequency conversion of feeding in the range of 8-30Hz, adjust the frequency conversion of tabletting in the range of 10-30Hz, and adjust the frequency conversion of granulation in the range of 10-30Hz Adjust within the range, the ...

Embodiment 3

[0077] Tablet prescription:

[0078]

[0079] Preparation Process:

[0080] (1) Pretreatment of raw and auxiliary materials: pulverize apixaban, its d(0.9) is 12.8 μm, pass lactose and microcrystalline cellulose through a 70-mesh sieve, and pulverize the sodium lauryl sulfate through a 80-mesh sieve;

[0081] (2) Add anhydrous lactose, microcrystalline cellulose, croscarmellose sodium and apixaban into the fixed hopper mixer, set the speed at 10 rpm, and mix for 20 minutes

[0082] (3) Mix the intermediate material obtained in (2) with the added magnesium stearate for 5 minutes.

[0083] (4) Add the intermediate material obtained in (3) to the dry granulator for granulation, adjust the frequency conversion of feeding in the range of 8-30Hz, adjust the frequency conversion of tabletting in the range of 10-30Hz, and adjust the frequency conversion of granulation in the range of 10-30Hz Adjust within the range, the whole grain screen is 1.0mm.

[0084] (5) Add the intermedi...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle sizeaaaaaaaaaa
hardnessaaaaaaaaaa
hardnessaaaaaaaaaa
Login to View More

Abstract

The invention provides an apixaban pharmaceutical composition and a preparation method thereof. The obtained apixaban preparation not only has good stability, low friability, high dissolution rate, high bioavailability in vivo, and small dissolution difference among batches. 1. The amount of surfactant is small, and there is no agglomeration and sticking phenomenon in the preparation process, which is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an apixaban pharmaceutical composition and a preparation method thereof. Background technique [0002] Apixaban (Apixaban, trade name: Eliquis, Eliquis / Eliquis) is an oral anticoagulant jointly developed by Bristol-Myers Squibb and Pfizer. Venous thrombotic diseases including deep venous thrombosis (deep venous thrombosis, DVT) and pulmonary embolism (pulmonary embolism, PE). In May 2011, the European Union approved the marketing of apixaban (trade name Eliquis), an oral direct inhibitor of factor Xa, for the prevention of venous thromboembolic events (VTE) in adult patients undergoing elective hip or knee replacement surgery . [0003] The chemical formula of Apixaban is 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6, 7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide, the molecular formula is C25H25N5O4, the molecular weight is 459...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & AuthorityPatents(China)
IPC IPC(8): A61K9/36A61K47/38A61K47/26A61K31/4545A61P7/02
CPCA61K9/2018A61K9/2054A61K9/2095A61K9/2866A61K31/4545A61P7/02
Inventor黄道省陈玮琦王小雷丁纪钱徐丹
OwnerCHANGZHOU HANSOH PHARM CO LTD