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Oral solid preparation of Febuxostat with high-bioavailability and preparation method thereof

A technology of febuxostat and solid preparations, which is applied in the mixed crystal form and amorphous micronized tablet and its preparation, and in the field of febuxostat single crystal form, which can solve the problem of high preparation and not enough to ensure the preparation of bioavailability And other issues

Active Publication Date: 2014-07-02
JIANGSU WANBANG BIOPHARMLS +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Finally, it was found that controlling the average particle size of febuxostat raw materials within the large range of 1-50 μm (including 3-50 μm) is not enough to ensure the preparation of highly bioavailable and stable preparations

Method used

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  • Oral solid preparation of Febuxostat with high-bioavailability and preparation method thereof
  • Oral solid preparation of Febuxostat with high-bioavailability and preparation method thereof
  • Oral solid preparation of Febuxostat with high-bioavailability and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] prescription:

[0054] Febuxostat (H crystal form) 120mg

[0055] Lactose 240mg

[0056] Microcrystalline cellulose 60mg

[0057] Croscarmellose Sodium 15mg

[0058] Magnesium stearate 4.5mg

[0059] 1% hypromellose aqueous solution

[0060] Preparation Process:

[0061] 1. Treat the febuxostat raw material to an average particle size range of 1~3.5μm, and use it for later use;

[0062] 2. Pass the lactose, microcrystalline cellulose, croscarmellose sodium and magnesium stearate through an 80-mesh sieve for use;

[0063] 3. Mix hypromellose with purified water to a concentration of 1% for later use;

[0064] 4. Mix febuxostat, lactose, microcrystalline cellulose and croscarmellose sodium uniformly, add the binder to make the soft material, the soft material is sieved to make wet granules, and dried at 50℃~60℃, After the dried granules are sieved and granulated, magnesium stearate and croscarmellose sodium are added and mixed to obtain a semi-finished product. Determine the content of...

Embodiment 2

[0066] prescription:

[0067] Febuxostat (H crystal form) 120mg

[0068] Lactose 240mg

[0069] Microcrystalline cellulose 60mg

[0070] Croscarmellose Sodium 15mg

[0071] Magnesium stearate 4.5mg

[0072] 1% hypromellose aqueous solution

[0073] Preparation Process:

[0074] 1. Treat the febuxostat raw material to an average particle size range of 3.5-10μm for use;

[0075] 2. Pass the lactose, microcrystalline cellulose, croscarmellose sodium and magnesium stearate through an 80-mesh sieve for use;

[0076] 3. Mix hypromellose with purified water to a concentration of 1% for later use;

[0077] 4. Mix febuxostat, lactose, microcrystalline cellulose and croscarmellose sodium uniformly, add the binder to make the soft material, the soft material is sieved to make wet granules, and dried at 50℃~60℃, After the dried granules are sieved and granulated, magnesium stearate and croscarmellose sodium are added and mixed to obtain a semi-finished product. Determine the content of the semi-finishe...

Embodiment 3

[0079] prescription:

[0080] Febuxostat (H crystal form) 120mg

[0081] Lactose 240mg

[0082] Microcrystalline cellulose 60mg

[0083] Croscarmellose Sodium 15mg

[0084] Magnesium stearate 4.5mg

[0085] 1% hypromellose aqueous solution

[0086] Preparation Process:

[0087] 1. Treat the febuxostat raw material to an average particle size in the range of 10-20μm for use;

[0088] 2. Pass the lactose, microcrystalline cellulose, croscarmellose sodium and magnesium stearate through an 80-mesh sieve for use;

[0089] 3. Mix hypromellose with purified water to a concentration of 1% for later use;

[0090] 4. Mix febuxostat, lactose, microcrystalline cellulose and croscarmellose sodium uniformly, add the binder to make the soft material, the soft material is sieved to make wet granules, and dried at 50℃~60℃, After the dried granules are sieved and granulated, magnesium stearate and croscarmellose sodium are added and mixed to obtain a semi-finished product. Determine the content of the semi-f...

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Abstract

The invention relates to a high bioavailability febuxostat oral solid dosage and a preparation method thereof. The invention is characterized in that the solid dosage comprises: a) febuxostat is C, H, I or J crystal form; b) the average grain diameter of the febuxostat crystal form ranges from 3.5-10mum, preferably 3.5-7mum. The preferable oral solid dosage is tablet, has the advantages of simple preparation technique, low cost and relatively high bioavailability, and can be used for treating diseases relative to extremely-high uric acid, such as gout, and reducing uric acid in blood.

Description

Technical field: [0001] The invention relates to a solid preparation containing febuxostat with high bioavailability and a preparation method thereof, and specifically relates to a single crystal form (H, I, J crystal form) and mixed crystal form (H, I, The mixed crystal form of J or the mixed crystal form of crystal A and crystal C) and amorphous micronized tablets and preparation methods thereof. technical background: [0002] Febuxostat is a drug for the treatment of intermittent and chronic gout developed by Japan’s Teijin Company. This product is a xanthine oxidase inhibitor that can inhibit the conversion of xanthine into uric acid and reduce the concentration of uric acid in the blood. The purpose of treating gout. Febuxostat has submitted a new drug registration in the US FDA and has obtained EMEA certification and approval for marketing. It is used to treat diseases related to hyperuric acid, such as gout, and to reduce blood uric acid content. [0003] The chemical stru...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/426A61K9/20A61K9/00A61P19/06
Inventor 王立张涛林宁石瑞娜欧云国牟才华邓杰
Owner JIANGSU WANBANG BIOPHARMLS
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