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Dabigatran etexilate self-emulsifying dispersible tablets and preparation method thereof

A technology of dabigatran etexilate and self-emulsification, which is applied in the field of pharmaceutical preparations and can solve the problems of low oral bioavailability

Inactive Publication Date: 2015-06-17
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] For the deficiencies of existing preparations, the object of the present invention is to provide a self-emulsifying dispersible tablet of dabigatran etexilate and a preparation method thereof, which solves the technical problem of low oral bioavailability of dabigatran etexilate

Method used

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  • Dabigatran etexilate self-emulsifying dispersible tablets and preparation method thereof
  • Dabigatran etexilate self-emulsifying dispersible tablets and preparation method thereof
  • Dabigatran etexilate self-emulsifying dispersible tablets and preparation method thereof

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Effect test

Embodiment 1

[0024] Embodiment 1 dabigatran etexilate self-emulsifying dispersible tablet

[0025] Specification 1000 pieces

[0026]

[0027] Preparation:

[0028] 1. Precisely weigh macrogol-32 laurate, ethylene glycol monoethyl ether, glycerol monolinoleate and medium chain triglyceride according to the weight ratio, vortex to mix evenly, add Dabiga Esteroid, ultrasound, so that all the drugs are dissolved.

[0029] 2. Take the above self-emulsifying solution and absorb it with microcrystalline cellulose PH 102 to form a solid self-emulsifying composition.

[0030] 3. Pass all solid auxiliary materials through a 100-mesh sieve in advance, add spray-dried lactose, crospovidone and pregelatinized starch in a weight ratio to the above-mentioned solid adsorption mixture, combine and mix according to a certain proportion, and then add micropowder silica gel , talcum powder and polyethylene glycol 4000, the mixture passed through an 80-mesh sieve for 3 times, and mixed evenly. Press th...

Embodiment 2

[0031] Embodiment 2 dabigatran etexilate self-emulsifying dispersible tablet

[0032] Specification 1000 pieces

[0033]

[0034] Preparation:

[0035] 1. Precisely weigh macrogol-32 laurate, ethylene glycol monoethyl ether, glycerol monolinoleate and medium chain triglyceride according to the weight ratio, vortex to mix evenly, add Dabiga Esteroid, ultrasound, so that all the drugs are dissolved.

[0036] 2. Take the above self-emulsifying solution and absorb it with microcrystalline cellulose KG 802 to form a solid self-emulsifying composition.

[0037] 3. Pass all solid auxiliary materials through a 100-mesh sieve in advance, add microcellulose, crospovidone and hydroxypropyl cellulose in a weight ratio to the above-mentioned solid adsorption mixture, combine and mix according to a certain proportion, and then add Micropowder silica gel and magnesium stearate, pass the mixture through an 80-mesh sieve for 3 times, and mix well. Press the mixed powder into dispersible t...

Embodiment 3

[0038] Embodiment 3 dabigatran etexilate self-emulsifying dispersible tablet

[0039] Specification 1000 pieces

[0040]

[0041] Preparation:

[0042] 1. Precisely weigh macrogol-32 laurate, ethylene glycol monoethyl ether, glycerol monolinoleate and medium chain triglyceride according to the weight ratio, vortex to mix evenly, add Dabiga Esteroid, ultrasound, so that all the drugs are dissolved.

[0043] 2. Take the above self-emulsifying solution and absorb it with micropowder silica gel to form a solid self-emulsifying composition.

[0044] 3. Pass all solid auxiliary materials through a 100-mesh sieve in advance, add pregelatinized starch, crospovidone, and microcrystalline cellulose in a weight ratio to the above-mentioned solid adsorption mixture, mix them according to a certain proportion, and then add talc Powder, sodium stearyl fumarate and polyethylene glycol 4000, the mixture passed through an 80-mesh sieve for 3 times, and mixed evenly. Press the mixed powd...

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Abstract

The invention relates to the technical field of medicament preparations, and discloses dabigatran etexilate self-emulsifying dispersible tablets and a preparation method thereof. The preparation method comprises the following steps: combining a certain proportion of dabigatran etexilate, an emulsifier and an assistant emulsifier into a dabigatran etexilate self-emulsifying solution; adsorbing by using a solid adsorbent to further obtain a solid self-emulsifying composition; and preparing the dabigatran etexilate self-emulsifying dispersible tablets by adopting a powder direct tabletting method. The dabigatran etexilate self-emulsifying solution and the self-emulsifying dispersible tablets prepared by the method disclosed by the invention can be self-emulsified in vivo after being orally taken to form a micro emulsion of which the particle size is about 200nm, so that the in vitro dissolution rate and in vivo intestinal absorption of dabigatran etexilate are significantly improved, and the in vivo bioavailability is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a dabigatran etexilate self-emulsified liquid, a self-emulsified dispersible tablet and a preparation method thereof. Background technique [0002] Atrial fibrillation, referred to as atrial fibrillation, is the most common rapid supraventricular arrhythmia, and its incidence increases with age, and the prevalence rate of people over 75 years old can reach 10%. Anticoagulation is the most important principle in the treatment of atrial fibrillation. In 2014, the American Heart Association, American College of Cardiology, and American Heart Rhythm Society (AHA / ACC / HRS) issued guidelines for the management of atrial fibrillation, which highly emphasized the importance of anticoagulant therapy for atrial fibrillation. [0003] The commonly used anticoagulant drug warfarin (vitamin K antagonist) is an oral drug used for anticoagulation in atrial fibrillation for...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4439A61P7/02A61P9/06
CPCA61K9/107A61K31/4439
Inventor 郑春丽丁亚飞张雅捷刘建平朱家壁
Owner CHINA PHARM UNIV
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