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Preparation method of oral slow/controlled-release preparation containing febuxostat

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., to avoid burst release effects, improve safety, and reduce the incidence of adverse reactions.

Active Publication Date: 2012-06-20
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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  • Preparation method of oral slow/controlled-release preparation containing febuxostat
  • Preparation method of oral slow/controlled-release preparation containing febuxostat

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1 skeleton type sustained and controlled release tablet

[0038] Febuxostat 80mg

[0039] Hypromellose (K15M) 15mg

[0040] Hypromellose (K4M) 15mg

[0041] Lactose 85mg

[0042] 5% povidone K30 in 75% ethanol solution 60mg

[0043] Magnesium Stearate 2mg

[0044] (The 75% ethanol solution of 5% povidone K30 refers to that in the ethanol solution that the mass percentage concentration is 75%, containing the povidone K30 that the mass percentage is 5%);

[0045] Preparation

[0046]After crushing febuxostat, pass through a 100-mesh sieve, mix well with hypromellose (K15M), hypromellose (K4M) and lactose, add 5% povidone K30 in 75% ethanol solution , using HLSH2-6 wet mixing granulator to prepare soft materials, 24 mesh sieve to make wet granules, wet granules to be air-dried at 50℃~60℃, dry granules to granulate with 22 mesh sieves, add magnesium stearate and mix After homogeneity, use ZP10A tablet press for tablet compression.

Embodiment 2

[0047] Embodiment 2 Coating type sustained and controlled release tablet

[0048] Tablet formulation

[0049] Febuxostat 80mg

[0050] Calcium hydrogen phosphate 25mg

[0051] Microcrystalline Cellulose 110mg

[0052] 2% hypromellose K15M aqueous solution 40mg

[0053] Magnesium Stearate 2mg

[0054] Coating material

[0055] 15% aqueous dispersion of ethylcellulose 116mg

[0056] Preparation Process

[0057] After pulverizing febuxostat, passing through a 100-mesh sieve, mixing evenly with calcium hydrogen phosphate and microcrystalline cellulose, adding 2% hypromellose K15M aqueous solution, and preparing it with a HLSH2-6 wet mixing granulator Soft material, 24 mesh sieve to make wet granules, wet granules are air-dried at 50℃~60℃, dry granules are granulated with 22 mesh sieves, after adding magnesium stearate and mixing evenly, use ZP10A tablet machine for tableting, hardness The range is 35-85N, and then coated with 15% ethylcellulose aqueous dispersion.

Embodiment 3

[0058] Embodiment 3 skeleton type sustained and controlled release capsules

[0059] Febuxostat 80mg

[0060] Hypromellose (K15M) 15mg

[0061] Hypromellose (K4M) 15mg

[0062] Microcrystalline Cellulose 85mg

[0063] 5% povidone K30 in 75% ethanol solution 60mg

[0064] Micronized silica gel 2mg

[0065] Preparation

[0066] After pulverizing febuxostat, pass it through a 100-mesh sieve, mix it with hypromellose (K15M), hypromellose (K4M) and microcrystalline cellulose evenly, add 75% of 5% povidone K30 % ethanol solution, use HLSH2-6 wet mixing granulator to prepare soft materials, then add JBZ-300 multifunctional granulation and coating machine to extrude and spheronize to prepare pellets. Blow 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 priorart. 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 a preparation method of an oral slow-controlled release preparation containing febuxostat for treating hyperuricemia. 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 new and highly effective non-purine xanthine oxidase selective inhibitor. It is clinically used to prevent and treat hyperuricemia and the gout caused by it. Teijin Corporation of Japan applied for listing in Japan 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 blood uric acid level of patients with hyperu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/32A61K9/24A61K31/426A61K9/36A61P19/06A61K9/52
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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