Preparation method and pharmaceutical preparation of deferasirox solid dispersion

A technology of solid dispersion and deferasirox, applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve problems such as adverse reactions, short half-life, and restrictions on widespread use

Active Publication Date: 2016-08-17
安士制药(中山)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In the past many years, the only iron-expelling drug available in China was deferoxamine. Because it cannot be absorbed orally and has a short half-life, it must be infused subcutaneously, 5-7 days a week, and each infusion is 8-12 hours , it is time-consuming and inconvenient to use, and there are many adverse reactions, resulting in poor long-term medication compliance of patients, which also limits their wide use

Method used

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  • Preparation method and pharmaceutical preparation of deferasirox solid dispersion
  • Preparation method and pharmaceutical preparation of deferasirox solid dispersion
  • Preparation method and pharmaceutical preparation of deferasirox solid dispersion

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Mix deferasirox and povidone uniformly, and extrude them with Thermo Fisher Pharma 11 twin-screw hot melt extruder. The screw speed is 10-30 rpm. The heating temperature is controlled as shown in the table below. After the extrudate is cooled, use FITZ-MILL The hammer mill is crushed into particles with a screen aperture of 1.0mm; the particles are mixed evenly with crospovidone, lactose, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate, and sodium lauryl sulfonate. Compressed into tablets.

[0039]

Embodiment 2

[0042] Mix deferasirox and povidone uniformly, and extrude them with Thermo Fisher Pharma 11 twin-screw hot melt extruder. The screw speed is 10-30 rpm. The heating temperature is controlled as follows. After the extrudate is cooled, use FITZ-MILL The hammer mill is crushed into particles with a screen aperture of 1.0mm; the particles are mixed evenly with crospovidone, lactose, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate, and sodium lauryl sulfonate. Compressed into tablets.

[0043]

Embodiment 3

[0046] Mix deferasirox and povidone uniformly, and extrude them with Thermo Fisher Pharma 11 twin-screw hot melt extruder. The screw speed is 10-30 rpm. The heating temperature is controlled as shown in the table below. After the extrudate is cooled, use FITZ-MILL The hammer mill is crushed into particles with a screen aperture of 1.0mm; the particles are mixed evenly with crospovidone, lactose, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate, and sodium lauryl sulfonate. Compressed into tablets.

[0047]

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PUM

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Abstract

The invention provides a preparation method and a pharmaceutical preparation of deferasirox solid dispersion. The preparation method includes uniformly mixing deferasirox with pharmaceutically acceptable carriers, heating the mixture to melt, cooling and grinding to obtain the deferasirox solid dispersion, wherein the pharmaceutically acceptable carriers are selected from povidone, hydroxypropyl methyl cellulose and copovidone. The invention further discloses a deferasirox tablet containing the deferasirox solid dispersion. The preparation method free of organic solvents is beneficial to lowering safety risks and environmental protection pressure, reduces production cost and is conducive to commercial production of products.

Description

Technical field [0001] The invention relates to a preparation method of deferasirox solid dispersion and its pharmaceutical preparation Background technique [0002] Deferasirox (deferasirox) is an oral active chelating agent, and iron (Fe 3+ ) Is highly selective. Developed by Novartis, it was first listed in the United States in 2005 under the trade name Exjade. Mainly used for the treatment of chronic iron overload disease caused by blood transfusion for 2 years and older; chronic iron overload treatment for patients with blood transfusion-independent thalassemia (NTDT) over 10 years old. [0003] Deferarox is an iron chelating agent with high affinity for ferric ions. 2 molecules can interact with 1 Fe 3+ Combine. It can replace the body's organs to remove the accumulated iron and reduce the disease caused by long-term iron accumulation. [0004] The chemical name of deferasirox is 4-[3,5-bis-(2-hydroxyphenyl)-1H-[1,2,4]-triazol-1-yl]benzoic acid and has the following structur...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/32A61K47/38A61K31/4196A61K9/20A61P3/12
CPCA61K9/146A61K9/2054A61K31/4196
Inventor 何健兴孙建民刘宝莲
Owner 安士制药(中山)有限公司
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