Apixaban sustained-release tablet and preparation method thereof

A technology for apixaban and sustained-release tablets, applied in the field of apixaban sustained-release tablets and their preparation, can solve the problems of inconvenient packaging, transportation, storage, low drug release stability effect, and large gastrointestinal irritation. , to achieve the effect of improving bioavailability, small individual differences, and easy absorption

Inactive Publication Date: 2016-05-25
HARBIN SHENGJI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the existing products on the market have low drug release stability, high irritation to the gastrointestinal tract, low bioavailability, and inconvenient packaging, transportation, and storage. and complex preparation methods

Method used

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  • Apixaban sustained-release tablet and preparation method thereof

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Embodiment 1

[0025] An apixaban sustained-release tablet is characterized in that it is made of the following raw materials: 5 mg of apixaban, 50-95 mg of hypromellose, and 3-20 mg of lubricant.

[0026] The preferred weight ratio of the raw materials is: 5 mg of apixaban, 93 mg of hypromellose, and 5 mg of lubricant.

[0027] The hypromellose can be one or two of the following models: 75hd100cr hypromellose, 75hd4000cr hypromellose, 75hd15000cr hypromellose, 100000cr hypromellose.

[0028] The lubricant is one or both of magnesium stearate, talcum powder and silicon dioxide.

[0029] Its production method includes the following steps:

[0030] Step 1: Preparation of raw materials: according to the above mass ratio, apixaban is pulverized with a pulverizer, and passed through a 100-mesh sieve;

[0031] Step 2: Mixing: Weigh apixaban and hypromellose according to the above mass ratio and mix them in a three-dimensional mixer for 30 minutes to make drug subdivisions and take ...

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Abstract

The invention discloses an apixaban sustained-release tablet and a preparation method thereof. The apixaban sustained-release tablet comprises the following components: apixaban, hydroxypropyl methylcellulose, and a lubricant. The apixaban sustained-release tablet employs a novel sustained-release preparation and a pellets preparation, sustained release means that by prolonging drug release rate of a drug in a dosage form, the absorption rate of the drug in human body is reduced, so that more stable treatment effect can be realized; the tablet has the advantage of large distribution area of the drug on surface of gastrointestinal tract, reduces irritation, increases bioavailability, and does not be influenced by gastric emptying influence, the drug can be uniformly absorbed by human body, individual difference is little; simultaneous application of two advanced technologies enhances the technical advantage of the apixaban sustained-release tablet; compared with oral liquid, the apixaban sustained-release tablet has the advantages of good drug stability, convenient package, transport and storage, the preparation method is simple and easy to operate, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of chemical drug sustained-release preparations, in particular to an apixaban sustained-release tablet and a preparation method thereof. Background technique [0002] Apixaban is an oral selective activated factor X inhibitor, which can prevent thrombosis, but the adverse reaction of bleeding is lower than that of the old drug warfarin. It is used for the prevention of thrombosis in patients who have undergone hip or knee replacement surgery. [0003] At present, the existing products on the market have the disadvantages of low drug release stability, high irritation to the gastrointestinal tract, low bioavailability, inconvenient packaging, transportation, and storage, and complicated preparation methods. Contents of the invention [0004] The purpose of the present invention is to provide a drug release stable effect, less irritating to the gastrointestinal tract, high bioavailability, convenient packaging, transp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/4545A61P7/02
Inventor 马玉国
Owner HARBIN SHENGJI PHARMA
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