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

A solid preparation, the technology of febuxostat, which is applied to mixed crystal form and amorphous micronized tablet and its preparation, and the field of single crystal form of febuxostat, can solve the problem of insufficient guarantee to prepare bioavailability and high preparation And other issues

Active Publication Date: 2009-07-08
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 appropriate amount

[0060] Preparation Process:

[0061] 1. Treat the febuxostat raw material to an average particle size range of 1-3.5 μm, and set aside;

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

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

[0064] 4. Mix febuxostat, lactose, microcrystalline cellulose and croscarmellose sodium evenly, add a binder to make a soft material, sieve the soft material to obtain wet granules, and dry at 50°C to 60°C. After the dried granules are sieved and sized, magnesium stearate and croscarmellose sodium are added and mixed evenly to obtain a semi-finished pro...

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 appropriate amount

[0073] Preparation Process:

[0074] 1. Treat the febuxostat raw material to an average particle size range of 3.5-10 μm, and set aside;

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

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

[0077] 4. Mix febuxostat, lactose, microcrystalline cellulose and croscarmellose sodium evenly, add a binder to make a soft material, sieve the soft material to obtain wet granules, and dry at 50°C to 60°C. After the dried granules are sieved and sized, magnesium stearate and croscarmellose sodium are added and mixed evenly to obtain a semi-finished pr...

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 appropriate amount

[0086] Preparation Process:

[0087] 1. Treat the febuxostat raw material to an average particle size range of 10-20 μm, and set aside;

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

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

[0090] 4. Mix febuxostat, lactose, microcrystalline cellulose and croscarmellose sodium evenly, add a binder to make a soft material, sieve the soft material to obtain wet granules, and dry at 50°C to 60°C. After the dried granules are sieved and sized, magnesium stearate and croscarmellose sodium are added and mixed evenly to obtain a semi-finished pro...

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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 present invention relates to a solid preparation containing febuxostat with high bioavailability and a preparation method thereof, in particular to febuxostat single crystal form (H, I, J crystal form), mixed crystal form (H, I, A mixed crystal form of J or a mixed crystal form of crystal A and crystal C), an amorphous micronized tablet and a preparation method thereof. technical background: [0002] Febuxostat is a drug developed by Teijin Corporation for the treatment of intermittent and chronic gout. This product is a xanthine oxidase inhibitor, which can inhibit the conversion of xanthine into uric acid and reduce the concentration of uric acid in the blood, thereby achieving The purpose of treating gout. Febuxostat has been submitted for new drug registration in the US FDA and has been approved for marketing by EMEA. It is used to treat diseases related to hyperuricemia, such as gout, and to reduce blood uric acid levels. [0003] The chemi...

Claims

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Application Information

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Patent Type & Authority Applications(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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