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Febuxostat double-layer enteric-coated tablet and preparation method thereof

A technology of febuxostat and enteric-coated tablets, which is applied in the direction of non-central analgesics, anti-inflammatory agents, pill delivery, etc., and can solve problems such as unbearable pain and additional burden on patients

Active Publication Date: 2013-03-20
GUIZHOU XINBANG PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the early stage of taking febuxostat, due to the rapid decline in serum uric acid concentration, it can promote the mobilization of uric acid deposited in the tissue, so it is very easy to have symptoms similar to gout attacks, and the pain is unbearable, which adds an extra burden to the patient

Method used

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  • Febuxostat double-layer enteric-coated tablet and preparation method thereof
  • Febuxostat double-layer enteric-coated tablet and preparation method thereof
  • Febuxostat double-layer enteric-coated tablet and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0077] Embodiment 1: The double-layer enteric-coated tablet comprises febuxostat 60g, ibuprofen 40g, microcrystalline cellulose 120g, lactose 35g, croscarmellose sodium 16g, magnesium stearate 2g, starch 45g and micronized silica gel 3g. Pass 60g of febuxostat through a 80-mesh sieve, mix evenly with 120g of microcrystalline cellulose, 35g of lactose, and 7g of croscarmellose sodium, add an appropriate amount of purified water to make a soft material, pass through a 18-mesh sieve for granulation, and Dry at ℃, pass through a 18-mesh sieve for granulation, add 2g of magnesium stearate and 9g of croscarmellose sodium, and mix evenly; take 40g of ibuprofen, mix with 45g of starch, 2g of micropowder silica gel, add starch slurry to make soft material, granulated through a 18-mesh sieve, dried at 60-65°C, taken out, cooled to room temperature, granulated through a 18-mesh sieve, and 1g of micropowder silica gel was added; the mixture obtained above was compressed using a double-lay...

Embodiment 2

[0078] Embodiment 2: The double-layer enteric-coated tablet comprises febuxostat 90g, ibuprofen and its pharmaceutically acceptable salt 10g, microcrystalline cellulose 165g, lactose 60g, croscarmellose sodium 27g , magnesium stearate 3g, starch 10g and micronized silica gel 1g. Pass 90g of febuxostat through a 80-mesh sieve, mix evenly with 165g of microcrystalline cellulose, 60g of lactose, and 12g of croscarmellose sodium, add an appropriate amount of purified water to make a soft material, pass through a 18-mesh sieve to granulate, and 70 Dry at ℃, pass through a 18-mesh sieve for granulation, add 3g magnesium stearate and 15g croscarmellose sodium, mix well; take 10g ibuprofen and its pharmaceutically acceptable salt, 10g starch, 0.5g micropowder silica gel Mix well, add starch slurry to make soft material, pass through 18-mesh sieve to granulate, dry the granules at 60-65°C, take out, cool to room temperature, pass through 18-mesh sieve for granulation, add 0.5g micro-po...

Embodiment 3

[0079] Example 3: The double-layer enteric-coated tablet contains 50 g of febuxostat, 25 g of ketoprofen, 25 g of aspirin, 95 g of microcrystalline cellulose, 20 g of lactose, 10 g of croscarmellose sodium, and magnesium stearate 1g, starch 60g and micropowder silica gel 4g. Pass 50g of febuxostat through a 80-mesh sieve, mix evenly with 95g of microcrystalline cellulose, 20g of lactose, and 4g of croscarmellose sodium, add an appropriate amount of purified water to make a soft material, pass through a 18-mesh sieve to granulate, 70 Dry at ℃, pass through a 18-mesh sieve for granulation, add 1g magnesium stearate and 6g croscarmellose sodium, and mix well; take 25g ketoprofen, 25g aspirin, mix with 60g starch, 2g micropowder silica gel, add starch slurry Make soft material, pass through 18-mesh sieve to granulate, dry the granules at 60-65°C, take them out, cool to room temperature, pass through 18-mesh sieve for granulation, add 2g of micropowder silica gel; use double-layer ...

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Abstract

The invention discloses a febuxostat double-layer enteric-coated tablet and a preparation method thereof. The tablet comprises the following components in parts by weight: 50 to 90 parts of febuxostat, 10 to 50 parts of non-steroidal anti-inflammatory drugs and proper medical auxiliary materials. Compared with the prior art, after the interaction of drugs and medicament adverse response pathogenetic mechanism are investigated, febuxostat and non-steroidal anti-inflammatory drugs are adopted, and pains of a patient in the treatment process can be effectively reduced while the drug effect of removing uric acid is not influenced in the combined action of ibuprofen, ketoprofen, aspirin and the like; and the enteric-coated tablet prepared from febuxostat is advantages to prevention of first pass effect, so that the bioavailability is improved, the maximum drug effect can be produced with minimum dosage, infection, nausea, diarrhea and other adverse responses of a human body caused by high-dosage febuxostat can be avoided, and the adaptability of the patient to medicaments can be improved.

Description

technical field [0001] The invention relates to a febuxostat double-layer enteric-coated tablet and a preparation method thereof, belonging to the technical field of medicines. Background technique [0002] Febuxostat, chemical name 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methyl-5-thiazolecarboxylic acid, is an aromatic thiazole derivative , can selectively inhibit XO activity (significant inhibitory effect on both oxidized and reduced XO enzymes), and has the therapeutic effect of reducing serum uric acid. Among the traditional uric acid-lowering drugs, one class mainly reduces uric acid production by inhibiting xanthine oxidase, which is suitable for the treatment of refractory tophi gout; the other class is drugs that promote uric acid excretion, such as Probenecid, sulfazone, and benzbromarone are not suitable for the treatment of refractory tophi gout due to the presence of a large number of tophi or severe renal insufficiency (creatinine clearance <50 mL / min). All...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/426A61K31/616A61P19/06A61P29/00A61K31/192
Inventor 张观福
Owner GUIZHOU XINBANG PHARMACEUTICAL CO LTD
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