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Preparation method of ambrisentan tablet

A technology of Sentan tablets and Ambrisentan, which is applied in the production field of Ambrisentan tablets, can solve the problems affecting the safety and effectiveness of drugs, low ambrisentan content, and large dissolution differences in batches, etc., and achieve dissolution The effect of small difference, fast dissolution rate and easy operation

Pending Publication Date: 2020-03-13
CHANGZHOU HANSOH PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Ambrisentan is a poorly soluble drug, in water and 0.1mol L -1 Almost insoluble in hydrochloric acid solution, the problem of low or even unqualified dissolution is often encountered in the actual production of tablets; and because the content of ambrisentan in the preparation is low, it is difficult to fully mix during preparation, so the dissolution There are often problems of high and low, and large dissolution differences between tablets, especially when expanding production, the dissolution of each batch is more different, which directly affects the safety and effectiveness of the drug.
Even if it is produced by the original GlaxoSmithKline company, there is also the problem of large batch-to-batch dissolution differences. Therefore, a product that meets the requirements for dissolution and has small dissolution differences between batches of tablets can be industrially produced. Technology is a technical problem that needs to be solved urgently

Method used

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  • Preparation method of ambrisentan tablet
  • Preparation method of ambrisentan tablet
  • Preparation method of ambrisentan tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Embodiment 1 Ambrisentan particle size investigation

[0067] Table 1

[0068]

[0069]

[0070] Conclusion: By investigating the angle of repose, difference in tablet weight, mixing uniformity, content uniformity of plain tablet and dissolution rate of plain tablet, when the particle size of ambrisentan is 20um≤d(0.9)≤50um, the obtained plain tablet Tablet weight variation is small, and it has good content uniformity, mixing uniformity and drug dissolution rate.

Embodiment 2

[0071] Embodiment 2 hardness is investigated

[0072] Table 2

[0073]

[0074] Conclusion: Through the investigation of the appearance, friability and dissolution rate of the plain tablets, the hardness of the ambrisentan tablets ranges from 5.00 to 10.00 kg / cm 2 At the same time, the obtained tablet is complete and smooth, uniform in color, free from missing corners and broken, and the drug dissolves quickly.

Embodiment 3

[0076] Tablet prescription:

[0077]

[0078]

[0079] Preparation Process:

[0080] (1) Pretreatment of raw and auxiliary materials: sieve ambrisentan micropowder, control d(0.9) to 33.3um, and pass lactose and microcrystalline cellulose through a 60-mesh sieve;

[0081] (2) Put the prescribed amount of ambrisentan and half of the prescribed amount of lactose into the hopper mixer, set the speed at 10 rpm, and mix for 5 minutes;

[0082] (3) Add the intermediate material obtained in (2) into a granulator for granulation, set the aperture screen of the granulator to 1.0 mm, and the rotating speed of the rotary knife to be 300 to 400 rpm;

[0083] (4) Add the sized intermediate material and the other half of the prescription amount of lactose into the hopper mixer, set the speed at 10 rpm, and mix for 5 minutes;

[0084] (5) Add microcrystalline cellulose and croscarmellose sodium in the prescribed amount into the hopper mixer, set the speed at 10 rpm, and mix for 15 mi...

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Abstract

The invention provides a preparation method of a ambrisentan tablet, the method is simple in preparation process, easy to operate, low in cost, good in reproducibility and suitable for industrial large-scale production, and the obtained ambrisentan tablet is smooth in surface, good in content uniformity, high in dissolution rate, small in dissolution difference among batches, and high in in-vivo bioavailability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a method for producing ambrisentan tablets. Background technique [0002] Pulmonary arterial hypertension (PAH) is a group of diseases characterized pathologically by abnormally elevated pulmonary artery pressure and progressive occlusion of the pulmonary vascular bed, including idiopathic PAH (IPAH), which is caused by extensive pulmonary lesions PAH caused by pulmonary arteriolar hypoxic spasm, left ventricular disease correlation, hypoxia and pulmonary disease, chronic thromboembolic embolism, etc., eventually lead to progressive increase in vascular resistance and right heart failure. At present, pulmonary arterial hypertension drugs are mainly divided into phosphodiesterase-5 (PDE-5) inhibitors, prostacyclins and endothelin receptor antagonists according to different mechanisms of action. Among them, endothelin receptor antagonists can completely bind to endotheli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K47/38A61K47/26A61K31/505A61P11/00A61P9/12
CPCA61K9/2866A61K9/2095A61K9/2054A61K9/2018A61K31/505A61P11/00A61P9/12
Inventor 杨文艳王小雷陈玮琦黄蓉王艳军
Owner CHANGZHOU HANSOH PHARM CO LTD
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