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Febuxostat enteric preparation

A febuxostat preparation technology, applied in the field of enteric-coated preparations of febuxostat, can solve the problems of gastrointestinal irritation, gastric ulcer, easy damage to gastric mucosa, etc., and achieve the effect of fast dissolution and absorption and high bioavailability

Active Publication Date: 2010-06-02
BEIJING KONRUNS PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the drug has serious adverse reactions such as gastrointestinal irritation and damage to the gastric mucosa, which can easily cause gastric ulcers.
In particular, this type of anti-gout drugs need to be taken for a long time, which is more likely to damage the gastric mucosa

Method used

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  • Febuxostat enteric preparation
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Enteric-coated Febuxostat Tablets

[0022] (1) chip core

[0023] Prescription 1000 tablets

[0024] Febuxostat 80g

[0025] 20g pregelatinized starch

[0026] Hydroxypropyl Cellulose 10g

[0027] Preparation: Take febuxostat, pregelatinized starch, and hydroxypropyl cellulose and pulverize them into an 80-mesh sieve respectively, weigh and mix according to the prescription amount, and use 2% ethanol aqueous solution of hydroxypropyl methyl cellulose (80% ) appropriate amount, the soft material is passed through a 16-mesh sieve, granulated, dried at 50-60°C, and granulated with a 18-mesh sieve. Measure the content of granules, press into tablets, and obtain. Each tablet weighs 120mg and contains 80mg of febuxostat.

[0028] (2) isolation layer

[0029] prescription

[0030] Hypromellose Phthalate 2g

[0031] Tween-80 2g

[0032] Ethanol 80ml

[0033] water 20ml

[0034] Dosing: Take the prescribed amount of hypromellose phthalate and disperse it in...

Embodiment 2

[0043] Example 2 Enteric-coated febuxostat pellets

[0044] (1) Prescription of pellets

[0045] Febuxostat 80g

[0046] Lactose 250g

[0047] Silicified Microcrystalline Cellulose 50g

[0048] Preparation: take three kinds of raw materials and auxiliary materials, and prepare it with 2% polyvinylpyrrolidone aqueous solution, and the diameter is 0.5-0.6mm.

[0049] (2) Package isolation layer

[0050] prescription

[0051] Hydroxypropyl Methyl Cellulose Phthalate 5g

[0052] Tween-80 3g

[0053] Ethanol 80ml

[0054] water 20ml

[0055] Preparation and coating are the same as in Example 1, the rotating speed of the coating pan is adjusted to 50 rpm, the air temperature is controlled at about 40°C, the gap is sprayed with an isolation layer, the weight of the pellets is increased by 2%, and it is taken out and dried at 40°C.

[0056] (3) Enteric coating

[0057] prescription

[0058] Polyvinyl acetate phthalate 12g

[0059] Diethyl phthalate 2g

[0060] Stearic acid ...

Embodiment 3

[0063] Example 3 Enteric-coated Febuxostat Tablets

[0064] (1) chip core

[0065] Prescription 1000 tablets

[0066] Febuxostat 120g

[0067] 40g pregelatinized starch

[0068] Hydroxypropyl Cellulose 20g

[0069] Preparation: Same as Example 1, each tablet weighs 180 mg, containing 120 mg of febuxostat.

[0070] (2) isolation layer

[0071] prescription

[0072] Hypromellose Phthalate 10g

[0073] Tween-80 5g

[0074] Ethanol 80ml

[0075] water 20ml

[0076] Dosing: with embodiment 1

[0077] Preparation: with embodiment 1

[0078] Weight gain 4mg per tablet

[0079] (3) Enteric coating

[0080] prescription

[0081] Cellulose acetate 10g

[0082] Phthalic acid 6g

[0083] Ethanol 80ml

[0084] water 20ml

[0085] The preparation and coating are the same as the isolation layer, each tablet has a weight gain of 18 mg, and then taken out and dried overnight at 40°C.

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Abstract

The invention provides a Febuxostat enteric preparation comprising a medicament inner core, an isolated layer and a casing layer. The Febuxostat enteric preparation adopts hypromellose phthalate ester to wrap an isolated coat and selects cellulose acetate propionate (CAP) and polyvinylacetate phthalate of an enteric-coated material dissolvable in a pH value range of 5-6.8 to wrap an enteric coat. The enteric preparation does not leak after being orally taken into the stomach of a human being, is rapidly dissolved and disintegrated after entering the pylorus with a pH value larger than 5 and releases the Febuxostat medicament for the ntestinal tract to rapidly absorb so as to achieve the aim of improving the bioavailability and the healing effect. Compared with a common Febuxostat tablet or capsule, the invention has the advantages of stability in gastric juice, rapid dissolution and absorption in the ntestinal tract and high bioavailability, is prepared by general process and is easy to realize the industrialized production.

Description

technical field [0001] The invention relates to an enteric-coated preparation of febuxostat, belonging to the technical field of western medicine preparations. Background technique [0002] The prevalence of gout is affected by various factors such as economic development, environment, eating habits, race, and statistical methods, so reports vary greatly from country to country. Available data show that the prevalence of gout in all countries in the world is increasing year by year, and the prevalence of hyperuricemia and gout in my country also shows a linear upward trend. Statistics in recent years have shown that the total prevalence of gout in all age groups is about 0.84%. [0003] The incidence of gout is closely related to the living standard. In the past, the living standard of our people was low, and the animal food in the diet was less, so the prevalence rate of gout was low. With the improvement of living standards, the proportion of foods related to gout, mainl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/48A61K31/426A61P19/06
Inventor 王锡娟
Owner BEIJING KONRUNS PHARMA TECH CO LTD
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