Apixaban tablet composition and preparation method thereof

A technology of apixaban tablets and apixaban, which is applied in the field of medicine and can solve the problems of water solubility not being affected by pH value, slow dissolution rate of apixaban tablets, and low content of active ingredients of the main drug , to achieve the effect of reducing medical costs, determining the curative effect and stable quality

Pending Publication Date: 2021-12-03
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, since apixaban is a white to light yellow crystalline powder, its solubility in water is 0.030mg / ml, and its solubility in pH1.2-pH6.8 aqueous solution is 0.027-0.032mg / ml. The property is not affected by the pH value, and the specifications of apixaban tablets are 2.5mg and 5mg, and the content of the active ingredient of the main drug is relatively low, so the dissolution rate of apixaban tablets is slow, the dissolution rate in vitro is low, and the content is not high. Problems such as uniformity have a great impact on the efficacy of drugs

Method used

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  • Apixaban tablet composition and preparation method thereof
  • Apixaban tablet composition and preparation method thereof
  • Apixaban tablet composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1: Apixaban tablet composition

[0054] Tablet core prescription composition:

[0055]

[0056] Preparation:

[0057] (1) Preparation of raw and auxiliary materials

[0058] ①Preparation of adhesive: prepare 7.2% aqueous solution of povidone K30;

[0059] ②The average particle size of microcrystalline cellulose PH101 is 65 microns; the average particle size of PH102 is 130 microns; the D90 of apixaban is 6.2 microns;

[0060] (2), premixing, wet granulation

[0061] Add apixaban, lactose, microcrystalline cellulose PH101, croscarmellose sodium, and sodium lauryl sulfate into a wet mixing granulator for premixing, and then add the binder under stirring conditions, Wet granulation; parameters of premixing and wet granulation are as follows:

[0062]

[0063] (3) Drying: Dry at 50-55°C to a moisture content of 1.6%;

[0064] (4), granulation: add the dried granules into the granulator for granulation, and the rotating speed is 600rpm; after finishing...

Embodiment 2

[0071] Embodiment 2: Apixaban tablet composition

[0072] Tablet core prescription composition:

[0073]

[0074] Preparation:

[0075] (1) Preparation of raw and auxiliary materials

[0076] ①Preparation of adhesive: prepare 7.2% aqueous solution of povidone K30;

[0077] ②The average particle size of microcrystalline cellulose PH101 is 65 microns; the average particle size of PH102 is 130 microns; the D90 of apixaban is 6.2 microns;

[0078] (2), premixing, wet granulation

[0079] Add apixaban, lactose, microcrystalline cellulose PH101, croscarmellose sodium, and sodium lauryl sulfate into a wet mixing granulator for premixing, and then add the binder under stirring conditions, Wet granulation; parameters of premixing and wet granulation are as follows:

[0080]

[0081] (3) Drying: Dry at 50-55°C to a moisture content of 1.8%;

[0082] (4), granulation: add the dried granules into the granulator for granulation, and the rotating speed is 600rpm; after finishing...

Embodiment 3

[0089] Embodiment 3: Apixaban tablet composition

[0090] Tablet core prescription composition:

[0091]

[0092] Preparation:

[0093] (1) Preparation of raw and auxiliary materials

[0094] ①Preparation of adhesive: prepare an aqueous solution of 8.0% povidone K30;

[0095] ②The average particle size of microcrystalline cellulose PH101 is 65 microns; the average particle size of PH102 is 130 microns; the D90 of apixaban is 6.2 microns;

[0096] (2), premixing, wet granulation:

[0097] Add apixaban, lactose, microcrystalline cellulose PH101, croscarmellose sodium, and sodium lauryl sulfate into a wet mixing granulator for premixing, and then add the binder under stirring conditions, Wet granulation; parameters of premixing and wet granulation are as follows:

[0098]

[0099] (3) Drying: Dry at 50-55°C to a moisture content of 1.4%;

[0100] (4), granulation: add the dried granules into the granulator for granulation, and the rotating speed is 500rpm; after finis...

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Abstract

The invention provides an apixaban tablet composition and a preparation method thereof. The apixaban tablet composition comprises a tablet core and a coating, wherein the tablet core comprises the following components in percentage by weight: 2.5% of apixaban, 50%-52% of lactose, 31.5%-41.5% of microcrystalline cellulose, 4.5%-5.5% of croscarmellose sodium, 0.5%-1.5% of lauryl sodium sulfate, 2.8%-3.2% of povidone and 0.5%-1.5% of magnesium stearate; and an apixaban tablet is prepared by adopting a wet granulation method, the process parameters of mixing and size stabilization in the preparation process are optimized, the dissolution rate and content uniformity of the tablet are improved, the stability is improved, and the apixaban tablet which is remarkable in medicine effect and stable in quality is obtained. The apixaban tablet composition disclosed by the invention is simple in production process and good in process tolerance. The uniformity in dissolution batches is good, the RSD (Relative Standard Deviation) of dissolution in the dissolution batches in four dissolution media within 5 minutes is less than 15%, and the RSD is less than 10% after 10 minutes.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to an apixaban tablet composition and a preparation method thereof. Background technique [0002] Apixaban (Apixaban), is a highly selective, reversible direct coagulation factor Xa inhibitor; suitable for adult patients undergoing elective hip or knee replacement; prevention of venous thromboembolic events. [0003] [0004] At present, about 1.8 to 2 million cases of artificial joint replacement operations are performed in the world every year. In western developed countries, the replacement rate of artificial joints is 1 / 1000, that is, 1 person in 1,000 people has had artificial joint replacements. No less than 200,000 cases of artificial joint replacement operations. In the 1990s, Stalberg SN and Hul RD reported that the incidence of deep vein thrombosis (DVT) in lower extremities was as high as 92% and pulmonary embolism (PE) was 42% in total hip replacement (THR) without pr...

Claims

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Application Information

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IPC IPC(8): A61K9/30A61K31/4545A61K47/38A61P7/02
CPCA61K31/4545A61K9/282A61K9/2054A61P7/02
Inventor 倪萍杨建学王亚楠吴蓉李翠娟赵东明谷晓彤
Owner CSPC OUYI PHARM CO LTD
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