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Warfarin micro-tablet and preparation method thereof

A technology of warfarin and microtablets, which is applied in the direction of pharmaceutical formulas, medical preparations of non-active ingredients, pill delivery, etc., which can solve the problem of inability to meet the requirements of individualized medication, the dose cannot achieve the anticoagulant effect, and the accuracy cannot be achieved Drug administration and other issues, to achieve the ideal drug release rate, flexible and accurate dosage, and reduce the effect of high local blood drug concentration

Active Publication Date: 2018-10-23
北京科信聚润医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The therapeutic window of warfarin is narrow, and individual differences are large. If the dose is too low, the anticoagulant effect cannot be achieved, and if the dose is too high, the risk of bleeding will be increased, and even life-threatening
Existing warfarin dosage forms cannot meet the requirements of individualized medication, cannot be conveniently and accurately divided into doses, and cannot achieve precise drug administration, especially for children who need to be dosed by kilograms of body weight
In addition, when the existing pharmaceutical dosage form is taken, due to the excessive volume of the dosage form, the compliance of taking the medicine is poor for children, the elderly and patients who are inconvenient to swallow tablets.

Method used

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  • Warfarin micro-tablet and preparation method thereof
  • Warfarin micro-tablet and preparation method thereof
  • Warfarin micro-tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024]

[0025]

[0026] The preparation process is as follows: put warfarin sodium, pregelatinized starch, microcrystalline cellulose 102 and HPMC E3 in the pot of the wet granulator, turn on the paddle for 10 minutes of initial mixing, after mixing, turn on the paddle and spray in at the same time Purified water was used for wet granulation; after spraying the purified water, the granulation was continued for 2 minutes; then the obtained wet granules were subjected to wet granulation, and then put into a fluidized bed for drying. After drying, the granules were subjected to dry granulation; the dry granules were After being uniformly mixed with the prescribed amount of magnesium stearate, the mixed material is transferred to a high-speed rotary tablet press for tableting to obtain finished tablets.

Embodiment 2

[0028] name

[0029]Preparation process: put warfarin sodium, microcrystalline cellulose 102, lactose Flowlac100, and sodium alginate in the pot of the wet granulator, turn on the paddle for 10 minutes of initial mixing, after mixing, turn on the paddle and spray purified water at the same time Carry out wet process; continue to granulate for 2 minutes after the purified water is sprayed; then wet granules are subjected to wet sizing, and then put into a fluidized bed for drying, after drying, the granules undergo dry sizing; the dry granules are mixed with the prescription amount After the magnesium stearate is uniformly mixed, the mixed material is transferred to a high-speed rotary tablet press for tableting to obtain finished tablets.

Embodiment 3

[0031] warfarin sodium

[0032] Preparation process: Put warfarin sodium, microcrystalline cellulose 102 and sodium alginate in the pot of the wet granulator, turn on the paddle for 10 minutes of initial mixing, after the mixing is complete, turn on the paddle and spray purified water at the same time for wet granulation Continue granulation for 2min after the purified water is sprayed into; then the obtained wet granules are wet sized, then put into a fluidized bed for drying, and the dried granules are dry sized; After the magnesium is uniformly mixed, the mixed material is transferred to a high-speed rotary tablet press for tablet compression to obtain finished tablets.

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Abstract

The invention discloses a warfarin micro-tablet preparation and a warfarin micro-tablet preparation method, wherein warfarin, a binder, a diluent and other raw materials are subjected to top spray fluidized bed granulation and other processes to prepare the warfarin micro-tablet with good compressibility. According to the present invention, the warfarin micro-tablet can be administered multiple times in a small dose, especially can be subjected to counting taking by individuals with large metabolic differences, such as the elderly and young children, so as to achieve precise administration, and can provide improved medication compliance for people having difficulty in taking conventional preparations; and the method and the raw materials are suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a warfarin microtablet and provides a method for preparing the warfarin microtablet. Background technique [0002] Warfarin, whose chemical name is warfarin, has the following structural formula: [0003] [0004] Warfarin is a coumarin anticoagulant that acts against vitamin K in the body. It can inhibit the synthesis of coagulation factors Ⅱ, Ⅶ, Ⅸ and Ⅹ involved in vitamin K in the liver. There is no resistance to the existing coagulation factors II, VII, IX, and X in the blood. Therefore, it cannot be used as an anticoagulant in vitro, and the anticoagulant in vivo must be active after the consumption of coagulation factors to be effective, and the effect and maintenance time after the onset of effect are also relatively long. It is mainly used for the prevention and treatment of thromboembolic diseases. [0005] CN104490832A discloses a ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/37A61K9/48A61K47/38A61P7/02
CPCA61K9/2054A61K9/2059A61K9/2095A61K9/4808A61K31/37
Inventor 谷雨田崔一民阳国平牛秀丽李焕刘质静
Owner 北京科信聚润医药科技有限公司