Apixaban sustained-release pellet and preparation method thereof

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

Inactive Publication Date: 2016-06-15
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 pellet and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] An apixaban sustained-release pellet, comprising a coating layer and drug-containing pellets; it is characterized in that: the coating layer is wrapped on the outside of the drug-containing pellets; the coating layer includes: 35-175mg Utera Qi NE30D, 5-53 mg talc powder; the drug-containing pellets include: 2.5 mg apixaban, 80 mg blank core, 197.5-252.5 mg filler, 10-50 mg lubricant, 5-25 mg binder.

[0028] The coating layer also includes trace amounts of one or both of sodium lauryl sulfate and polyethylene glycol.

[0029] The preferred weight ratio in the coating layer is: 132mg Eudragit NE30D, 7mg talcum powder.

[0030] The preferred weight ratio of the drug-containing pellets is: 2.5 mg of apixaban, 80 mg of blank core, 237.5 mg of filler, 20 mg of lubricant, and 10 mg of binder.

[0031] The filler is microcrystalline cellulose, the lubricant is talcum powder, and the binder is hypromellose.

Embodiment 2

[0033] Its production method includes the following steps:

[0034] 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;

[0035] Step 2: Mixing: Weigh apixaban and microcrystalline cellulose according to the above mass ratio, put them into a three-dimensional mixer and mix for 30 minutes to make drug subdivisions, and take them out for later use;

[0036] Step 3: Preparation of adhesive: Weigh an appropriate amount of hypromellose according to the above mass ratio, add an appropriate amount of hot water to prepare an adhesive with a concentration of 2%, and set aside;

[0037] Step 4: Pill making: Subdivide the drug into the feed tank of the centrifugal pellet machine, put the adhesive into the liquid supply tank, put the blank pellet core into the pot, turn on the machine, adjust the parameters, and start spraying the liquid. When the ball core feels wet, start to su...

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Abstract

The invention discloses an apixaban sustained-release pellet and a preparation method thereof. The apixaban sustained-release pellet includes a coating layer and a drug-containing pellet, wherein the coating layer includes Eudragit NE30D, talcum powder, and lauryl sodium sulfate or polyethylene glycol; and the drug-containing pellet includes apixaban, a blank pellet core, a filling agent, a lubricant and a bonding agent. In the invention, the novel sustained-release preparation and the pellet preparation are employed, wherein the sustained release means that the drug release rate of the drug from the preparation is sustained to reduce the absorption rate of the drug in human body, thereby achieving more stable treatment effect. The pellet increases the distribution area of the drug on surface of gastrointestinal tract, reduces irritation, improves bioavailability, is free of the influence of the gastric emptying factor, enables the drug to be absorbed uniformly in body and is less in individual difference. The two advanced technologies are employed together to improve technical advantages of the drug. The sustained-release pellet, compared with an oral liquid, is good in stability, is convenient to package, transport and store, is simple in preparation method and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of chemical drug sustained-release preparations, and in particular relates to apixaban sustained-release pellets 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 packagi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4545A61P7/02
Inventor 马玉国
Owner HARBIN SHENGJI PHARMA
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