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Oral slow/controlled-release preparation containing febuxostat and preparation method thereof

A technology for controlled release preparations and febuxostat, which is applied in the directions of medical preparations containing active ingredients, pill delivery, pharmaceutical formulations, etc. Improve the efficacy, reduce the incidence of adverse reactions, and avoid the effect of sudden release effects

Active Publication Date: 2010-07-14
QINGDAO HUANGHAI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The present invention provides a kind of oral sustained and controlled release preparation containing febuxostat and preparation method thereof, prepares long-acting oral sustained and controlled release preparation of febuxostat The preparation can solve the problem of increasing the incidence of adverse reactions in the common preparations in the prior art due to their rapid dissolution and burst release effect

Method used

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  • Oral slow/controlled-release preparation containing febuxostat and preparation method thereof
  • Oral slow/controlled-release preparation containing febuxostat and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Matrix-type sustained-release tablet

[0037] Febuxostat 80mg

[0038] Hypromellose (K15M) 15mg

[0039] Hypromellose (K4M) 15mg

[0040] Lactose 85mg

[0041] 5% Povidone K30 in 75% ethanol 60mg

[0042] Magnesium Stearate 2mg

[0043] (The 75% ethanol solution of 5% povidone K30 refers to the 75% ethanol solution containing 5% povidone K30 by mass);

[0044] Preparation

[0045] After crushing febuxostat, pass it through a 100-mesh sieve, and then mix it with hypromellose (K15M), hypromellose (K4M) and lactose, then add 5% povidone K30 in 75% ethanol solution , use HLSH2-6 wet mixing granulator to prepare soft materials, sieve wet granules with 24 mesh, dry the wet granules by blasting at 50 ℃ ~ 60 ℃, dry granules with a 22 mesh sieve, add magnesium stearate and mix After uniformity, use ZP10A tablet press for tableting.

Embodiment 2

[0046] Example 2 Coated sustained and controlled release tablet

[0047] Chip formula

[0048] Febuxostat 80mg

[0049] Calcium hydrogen phosphate 25mg

[0050] Microcrystalline Cellulose 110mg

[0051] 2% Hypromellose K15M in water 40mg

[0052] Magnesium Stearate 2mg

[0053] coating material

[0054] 15% ethyl cellulose dispersion in water 116mg

[0055] Preparation Process

[0056] After crushing febuxostat, pass it through a 100-mesh sieve, and then mix it with calcium hydrogen phosphate and microcrystalline cellulose evenly, add 2% hypromellose K15M aqueous solution, and use HLSH2-6 type wet mixing granulator to prepare Soft material, 24 mesh sieve to make wet granules, the wet granules are air-dried at 50 ℃ ~ 60 ℃, the dry granules are granulated with a 22 mesh sieve, after adding magnesium stearate and mixing evenly, use a ZP10A tablet machine for tableting, hardness Range 35-85N, and then coat with 15% aqueous ethyl cellulose dispersion.

Embodiment 3

[0057] Embodiment 3 skeleton type slow-release capsule

[0058] Febuxostat 80mg

[0059] Hypromellose (K15M) 15mg

[0060] Hypromellose (K4M) 15mg

[0061] Microcrystalline Cellulose 85mg

[0062] 5% Povidone K30 in 75% ethanol 60mg

[0063] Micronized silica gel 2mg

[0064] Preparation

[0065] After crushing febuxostat, pass it through a 100-mesh sieve, and then mix it with hypromellose (K15M), hypromellose (K4M), and microcrystalline cellulose, and then add 75% of 5% povidone K30. % ethanol solution, use HLSH2-6 wet mixing granulator to prepare soft material, and then add JBZ-300 multifunctional granulation coating machine to extrude and spheronize to prepare pellets. The pellets are prepared at 50℃~60℃ Blast dry, add micropowder silica gel and mix evenly, then fill into No. 0 capsule shell.

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Abstract

The invention provides an oral slow / controlled-release preparation containing febuxostat and a preparation method thereof, which prepare the febuxostat into the long-acting oral slow / controlled-release preparation and can solve the problem that the incidence of an adverse reaction is increased because of the quicker dissolving-out and the burst effect of a common preparation existing in the prior art. The invention has the technical scheme that the oral slow / controlled-release preparation containing the febuxostat comprises the following components by weight percent: 5 to 60 percent of febuxostat, 10 to 50 percent of slow / controlled-release material, 20 to 80 percent of filling auxiliary material, 0.3 to 20 percent of adhesive and 0.1 to 7 percent of lubricant or glidant. Compared with a common quick-release preparation, the slow / controlled-release preparation can keep the effective and stable blood concentration for a longer time, avoids the burst effect of the quick-release preparation, lowers the incidence of the adverse reaction and enhances the application safety.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an oral sustained and controlled release preparation containing febuxostat for treating hyperuricemia and a preparation method thereof. Background technique [0002] The chemical name of febuxostat is 2-[3-cyano-4-(2-isobutoxy)]-4-methylthiazole-5-carboxylic acid, and the molecular formula is C 16 H 16 N 2 O 3 S, relative molecular mass: 316.374, CAS registration number: 144060-53-7. Its structure is as follows: [0003] [0004] Febuxostat is a novel and highly effective nonpurine selective inhibitor of xanthine oxidase. It is clinically used for the prevention and treatment of hyperuricemia and the gout caused by it. It was applied for listing in Japan by Teijin in early 2004 and in the United States at the end of the same year. The European Union approved its listing in May 2008. The drug can effectively reduce the level of uric acid in...

Claims

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Application Information

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IPC IPC(8): A61K31/426A61K9/52A61K9/32A61K9/36A61K9/24A61P19/06
Inventor 王芳曹瑞山李振霞胡杰马德宝陈颖于华芝
Owner QINGDAO HUANGHAI PHARM CO LTD
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