Apixaban pellet and preparation method thereof

A technology of apixaban and pellets, which is applied in the field of apixaban pellets and its preparation, can solve problems such as difficulty in mass production, adverse reactions, and cumbersome steps, and achieve good stability, stable product quality, and particle size uniform effect

Inactive Publication Date: 2017-07-04
WATERSTONE PHARMA WUHAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this patent theoretically solves the dissolution problem of apixaban, its water-soluble carrier uses 10-20 parts of surfactant polyethylene glycol 6000, and the preparation process requires heating, vigorous stirring, low-temperature cooling and solidification, Drying under reduced pressure at room temperature, the steps are cumbersome and difficult to operate, and it is not easy to achieve mass production; the most important thing is that patients take a large amount of polyethylene glycol 6000 while taking medicine, which brings greater side effects and adverse reactions to patients
[0007] Therefore, the current apixaban preparations still need to be improved

Method used

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  • Apixaban pellet and preparation method thereof
  • Apixaban pellet and preparation method thereof
  • Apixaban pellet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Example 1 Preparation of Apixaban Micropills and Micropill Capsules by Fluidized Bed Liquid Layer Method

[0076]

[0077] Grinding of the raw material drug: the apixaban raw material is pulverized with a GTM-50 jet mill until its D90=6 μm; drug-loaded layer suspension preparation: measure 2250ml of water, dissolve povidone in it, and at this time the binder The concentration is about 2.0% by mass, then add the crushed apixaban raw material, microcrystalline cellulose and croscarmellose sodium in the prescribed amount, stir until uniformly dispersed, and pass through a 60-mesh sieve to obtain a suspension of the drug-loaded layer ; Use WBF-2G multifunctional fluidized bed for drug loading, the process parameters are as follows: air volume 100m 3 / h, liquid supply speed 6g / min, atomization pressure 1.7bar, air inlet temperature 50°C, material temperature 40°C, spacer height 10cm; fluidized bed drying for 30min after drug application, the parameters are as follows: air...

Embodiment 2

[0078] Example 2 Preparation of Apixaban Micropills and Micropill Capsules by Fluidized Bed Liquid Layer Method

[0079]

[0080] Grinding of the raw material drug: GTM-50 jet pulverizer is used to pulverize the apixaban raw material until its D90=6 μm; drug-loaded layer suspension preparation: measure 4500ml of water, dissolve povidone in it, and at this time the binder The concentration is about 1.0% by mass, then add the crushed apixaban raw material, microcrystalline cellulose and croscarmellose sodium in the prescribed amount, stir until uniformly dispersed, and pass through a 60-mesh sieve to obtain a drug-loaded layer suspension ; Use WBF-2G multifunctional fluidized bed for drug loading, the process parameters are as follows: air volume 100m 3 / h, liquid supply speed 6g / min, atomization pressure 1.7bar, air inlet temperature 50°C, material temperature 40°C, spacer height 10cm; fluidized bed drying for 30min after drug application, the parameters are as follows: air vo...

Embodiment 3

[0081] Example 3 Preparation of Apixaban Pellets and Pellet Capsules by Fluidized Bed Liquid Layer Method

[0082]

[0083] Grinding of the raw material drug: GTM-50 jet pulverizer is used to pulverize the apixaban raw material until its D90=6 μm; drug-loaded layer suspension preparation: measure 900ml of water, dissolve povidone in it, and at this time the binder The concentration is about 5.0% by mass, then add the crushed apixaban raw material, microcrystalline cellulose and croscarmellose sodium in the prescribed amount, stir until uniformly dispersed, and pass through a 60-mesh sieve to obtain a suspension of the drug-loaded layer ; Use WBF-2G multifunctional fluidized bed for drug loading, the process parameters are as follows: air volume 100m 3 / h, liquid supply speed 6g / min, atomization pressure 1.7bar, air inlet temperature 50°C, material temperature 40°C, spacer height 10cm; fluidized bed drying for 30min after drug application, the parameters are as follows: air ...

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Abstract

The invention relates to an apixaban pellet and a preparation method thereof. The apixaban pellet is composed of, from interior to exterior, a blank pellet core, a drug-containing layer and a coating layer, wherein the drug-containing layer is composed of micronized apixaban, a binder and a disintegrating agent. The apixaban pellet comprises, by weight, 60 to 84 parts of the blank pellet core, 2 to 7 parts of the micronized apixaban, 3 to 10 parts of the binder, 5 to 20 parts of the disintegrating agent and 2 to 8 parts of the coating layer. Thus, the apixaban pellet obtained in the invention has a rough and regular shape and uniform particle size; and compared with commercially available tablets, the apixaban pellet provided by the invention has better stability, faster dissolving-out rate and higher bioavailability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular, the invention relates to an apixaban pellet and a preparation method thereof. Background technique [0002] The chemical name of Apixaban (compound shown in formula 1) is 4,5,6,7-tetrahydro-1-(4-methoxyphenyl)-7-oxo-6-[4-(2- Oxo-1-piperidinyl)phenyl]-1H-pyrazolo[3,4-C]pyridine-3-carboxamide, is an oral selective inhibitor of active factor X, acting directly on coagulation factors Xa, jointly developed by Pfizer and Bristol-Myers Squibb, was approved by the FDA in 2012 and can prevent blood clots. [0003] [0004] However, because apixaban is insoluble in water, it has the disadvantages of slow dissolution rate, low in vitro dissolution rate, and low bioavailability, which have a great impact on the absorption of the drug. [0005] The active substance in the pharmaceutical composition provided by patent CN102770126A is the N-1 or H2-2 crystal form, which includes cr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4545A61P7/02
CPCA61K9/1652A61K9/1676A61K9/1694A61K31/4545
Inventor 金晶钱丽娜刘大鹏吴敏陈生辉
Owner WATERSTONE PHARMA WUHAN
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