CN101711751A - Febuxostat dispersing tablet preparation and preparation method thereof - Google Patents
Febuxostat dispersing tablet preparation and preparation method thereof Download PDFInfo
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- CN101711751A CN101711751A CN200910231562A CN200910231562A CN101711751A CN 101711751 A CN101711751 A CN 101711751A CN 200910231562 A CN200910231562 A CN 200910231562A CN 200910231562 A CN200910231562 A CN 200910231562A CN 101711751 A CN101711751 A CN 101711751A
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Abstract
The invention relates to a febuxostat dispersing tablet preparation and a preparation method thereof. The febuxostat dispersing tablet preparation is especially suitable for patients having poor adaptability or difficulties in taking common solid preparations, such as tablets and capsules and is prepared from the following materials in parts by weight: 40-150 parts of febuxostat, 50-200 parts of microcrystalline cellulose, 5-20 parts of croscarmellose sodium, 10-30 parts of polyvinylpolypyrrolidone, 50-200 parts of lactose, 1-10 parts of aspartame, 0.5-5 parts of magnesium stearate and 0.5-5 parts of hydroxypropyl methylcellulose. The preparation method of the febuxostat dispersing tablet preparation ahs the steps of: sieving the raw materials by a 100-mesh sieve, weighting the raw materials in proportion and and uniformly mixing, tabletting, crushing, sizing by 24 meshes, adding magnesium stearate in proportion, mixing and tabletting. The invention can be rapidly disintegrated and dispersed in water into an even suspended solution and have the advantages of good taste, stable quality, high bioavailability, convenient taking, and the like.
Description
Technical field
The present invention relates to a kind of Febuxostat preparation, be used to take common solid preparation such as tablet, capsule is had any problem or the dispersible tablet of the patient's of poor compliance Febuxostat and preparation method thereof.
Background technology
Febuxostat is the effective antigout drug of a class, chemical name: 2-[3-cyano-4-isobutoxy phenyl]-the 4-methylthiazol-5-formic acid.This product is almost insoluble in water, be unfavorable for absorbing, at present in this product world wide listing have only conventional tablet because this product poorly water-soluble and take inconvenience can not satisfy dissimilar patients' medication demand, the patient of solid preparation such as tablet difficulty particularly, therefore, effectively increase its stripping, improve its bioavailability by the preparation means, improve the mouthfeel of taking medicine, effectively improve patient's compliance of taking medicine and show necessary especially.
Febuxostat dispersing tablet preparation is not seen research and listing report both at home and abroad as yet.
Summary of the invention
Technical problem to be solved by this invention provides a kind of Febuxostat dispersing tablet preparation and preparation method thereof, the product good absorbing, and mouthfeel is good, steady quality, the patient who is specially adapted to child, old man and can not swallows solid preparation.
A kind of Febuxostat dispersing tablet preparation of the present invention, it is characterized in that by the principal agent Febuxostat, add filler, disintegrating agent, binding agent, correctives and mix lubricant are formed, and the composition of supplementary material and proportioning are: 40～150 parts of Febuxostats, 100～400 parts of filleies, 15～50 parts of disintegrating agents, 0.5～5 part of binding agent, 1～10 part of correctives.
Wherein:
Filler comprises one or more in microcrystalline Cellulose, starch, lactose, dextrin or the mannitol, but is not limited to above-mentioned filler.
Disintegrating agent includes but not limited to one or more in polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium or the pregelatinized Starch.
Correctives includes but not limited to one or more in aspartame, stevioside, saccharin sodium, protein sugar, sweet close element, flavoring orange essence or the Fructus Citri Limoniae essence.
Employed binding agent is a hypromellose.
A kind of preferred supplementary material of the present invention forms and proportioning is: 0.5～5 part of 40～150 parts of Febuxostats, 50～200 parts of microcrystalline Cellulose, 5～20 parts of cross-linking sodium carboxymethyl celluloses, 10～30 parts of polyvinylpolypyrrolidone, 50～200 parts of lactose, 1～10 part of aspartame, 0.5～5 part of magnesium stearate and hypromellose.
The present invention is by principal agent---Febuxostat, and filler, disintegrating agent, correctives mix, granulate, total mixing, tabletting makes Febuxostat dispersing tablet preparation.Specifically be that supplementary material is crossed 100 mesh sieves, take by weighing recipe quantity Febuxostat, microcrystalline Cellulose, aspartame, hypromellose, lactose, cross-linking sodium carboxymethyl cellulose and polyvinylpolypyrrolidone, mix homogeneously, the compacting thin slice is pulverized 24 order granulate, add the recipe quantity magnesium stearate, total mixed, tabletting.
The present invention's preparation method more specifically is as follows, becomes example with preferred group:
(1) gets the raw materials ready
According to the composition and the proportioning of product get the raw materials ready (parts by weight)
40～150 parts of Febuxostats
50～200 parts of microcrystalline Cellulose
5～20 parts of cross-linking sodium carboxymethyl celluloses
10～30 parts of polyvinylpolypyrrolidone
50～200 parts of lactose
1～10 part of aspartame
0.5～5 part of magnesium stearate
0.5～5 part of hypromellose
(2) granulation, tabletting
Supplementary material is crossed 100 mesh sieves, takes by weighing recipe quantity Febuxostat, microcrystalline Cellulose, aspartame, hypromellose, lactose, cross-linking sodium carboxymethyl cellulose and polyvinylpolypyrrolidone, mix homogeneously, the compacting thin slice is pulverized 24 order granulate, add the recipe quantity magnesium stearate, total mixed, tabletting.
Febuxostat dispersing tablet preparation of the present invention and preparation method thereof has following beneficial effect:
(1) Febuxostat dispersing tablet preparation of the present invention is to improve by dosage form to form on the basis of Febuxostat sheet, is mixed with by principal agent and specific disintegrating agent and correctives to form, and mouthfeel is good, steady quality.
(2) Febuxostat dispersing tablet preparation good absorbing of the present invention.It is compared with conventional tablet, and disintegrate becomes homodisperse granule rapidly in water, and the stripping that helps medicine absorbs, and therefore, oral post-absorption is fast, the bioavailability height.
(3) the Febuxostat dispersing tablet preparation of the present invention patient that is specially adapted to child, old man and can not swallows solid preparation can effectively improve this part patient's medication compliance.
The specific embodiment
Further clearly understand the present invention by the following specific embodiment that provides.But they are not limitation of the invention.
Embodiment 1 (most preferred embodiment):
By 1000 calculating of preparation, the composition of supplementary material and proportioning are:
Febuxostat 80g
Microcrystalline Cellulose 100g
Polyvinylpolypyrrolidone 10g
Aspartame 8.5g
Cross-linking sodium carboxymethyl cellulose 8.5g
Lactose 100g
Hypromellose 4g
Magnesium stearate 1g
???????????????????????????????????????????????????????
Make 1000
Preparation method:
1. supplementary material is crossed 100 mesh sieves.
2. take by weighing recipe quantity Febuxostat, microcrystalline Cellulose, aspartame, hypromellose, lactose, cross-linking sodium carboxymethyl cellulose and polyvinylpolypyrrolidone, mix homogeneously, the compacting thin slice is pulverized, and 24 order granulate add the recipe quantity magnesium stearate, and are total mixed, tabletting.
3. sampling, intermediate detects.
4. tabletting is packed.
Every of this product contains Febuxostat 0.08g, the heavily about 0.22g of sheet.
This product and conventional tablet dissolution curve are seen Fig. 1.As seen the dispersible tablet stripping is better than ordinary tablet.
Embodiment 2: the Febuxostat dispersing tablet preparation accelerated test of embodiment 1 preparation (concrete data see the following form)
Carry out accelerated test according to Chinese Pharmacopoeia, this product placed under 40 ℃, the condition of RH75% investigate 6 months, respectively at 0,1,2,3, the sampling in June detects, leading indicators such as the dispersing uniformity before and after investigation is placed, dissolution, related substance, content the results are shown in following table (data of this preparation are continuous three batch data averages).The result shows that this product investigates 6 months under the accelerated test condition, and significant change does not all take place every index of examining.
The Febuxostat dispersing tablet preparation accelerated test is investigated the result
| Time (moon) | Dispersing uniformity | Dissolution | Related substance | Content |
| ??0 | Up to specification | ??96.8％ | ??0.12％ | ??99.3％ |
| ??1 | Up to specification | ??97.6％ | ??0.10％ | ??99.8％ |
| ??2 | Up to specification | ??96.8％ | ??0.11％ | ??100.5％ |
| ??3 | Up to specification | ??98.6％ | ??0.12％ | ??98.9％ |
| ??6 | Up to specification | ??98.7％ | ??0.10％ | ??99.7％ |
Embodiment 3:
By 1000 calculating of preparation, the composition of supplementary material and proportioning are:
Febuxostat 40g
Microcrystalline Cellulose 50g
Polyvinylpolypyrrolidone 10g
Aspartame 3g
Cross-linking sodium carboxymethyl cellulose 5g
Lactose 50g
Hypromellose 0.5g
Magnesium stearate 0.5g
?????????????????????????????????????????????
Make 1000
The Febuxostat dispersing tablet preparation accelerated test is investigated the result
| Time (moon) | Dispersing uniformity | Dissolution | Related substance | Content |
| ??0 | Up to specification | ??95.2％ | ??0.10％ | ??99.1％ |
| ??1 | Up to specification | ??97.1％ | ??0.10％ | ??99.6％ |
| ??2 | Up to specification | ??96.3％ | ??0.12％ | ??99.5％ |
| ??3 | Up to specification | ??97.9％ | ??0.12％ | ??98.1％ |
| ??6 | Up to specification | ??96.7％ | ??0.10％ | ??98.7％ |
Embodiment 4:
By 1000 calculating of preparation, the composition of supplementary material and proportioning are:
Febuxostat 150g
Microcrystalline Cellulose 200g
Polyvinylpolypyrrolidone 30g
Aspartame 10g
Cross-linking sodium carboxymethyl cellulose 20g
Lactose 200g
Hypromellose 5g
Magnesium stearate 5g
??????????????????????????????????????????????????
Make 1000
The Febuxostat dispersing tablet preparation accelerated test is investigated the result
| Time (moon) | Dispersing uniformity | Dissolution | Related substance | Content |
| ??0 | Up to specification | ??96.3％ | ??0.11％ | ??99.2％ |
| ??1 | Up to specification | ??97.4％ | ??0.10％ | ??99.4％ |
| ??2 | Up to specification | ??96.2％ | ??0.11％ | ??98.8％ |
| ??3 | Up to specification | ??98.1％ | ??0.11％ | ??98.1％ |
| ??6 | Up to specification | ??97.8％ | ??0.10％ | ??99.1％ |
Embodiment 5:
By 1000 calculating of preparation, the composition of supplementary material and proportioning are:
Febuxostat 80g
Microcrystalline Cellulose 100g
Low-substituted hydroxypropyl cellulose 10g
Stevioside 8.5g
Cross-linking sodium carboxymethyl cellulose 8.5g
Mannitol 100g
Hypromellose 4g
Magnesium stearate 1g
?????????????????????????????????????
Make 1000
The Febuxostat dispersing tablet preparation accelerated test is investigated the result
| Time (moon) | Dispersing uniformity | Dissolution | Related substance | Content |
| ??0 | Up to specification | ??96.7％ | ??0.12％ | ??99.4％ |
| ??1 | Up to specification | ??97.3％ | ??0.10％ | ??99.6％ |
| ??2 | Up to specification | ??96.6％ | ??0.11％ | ??100.1％ |
| ??3 | Up to specification | ??98.2％ | ??0.11％ | ??98.2％ |
| ??6 | Up to specification | ??98.5％ | ??0.10％ | ??99.1％ |
Claims (7)
1. Febuxostat dispersing tablet preparation, it is characterized in that by the principal agent Febuxostat, add filler, disintegrating agent, binding agent, correctives and mix lubricant are formed, and the composition of supplementary material and proportioning are: 1～10 part of 40～150 parts of Febuxostats, 100～400 parts of filleies, 15～50 parts of disintegrating agents, 0.5～5 part of binding agent and correctives.
2. Febuxostat dispersing tablet preparation according to claim 1 is characterized in that described filler selects one or more in microcrystalline Cellulose, starch, lactose, dextrin, the mannitol.
3. Febuxostat dispersing tablet preparation according to claim 1 is characterized in that described disintegrating agent selects one or more in polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium, the pregelatinized Starch.
4. Febuxostat dispersing tablet preparation according to claim 1 is characterized in that described correctives comprises one or more in aspartame, stevioside, saccharin sodium, protein sugar, sweet close element, flavoring orange essence, the Fructus Citri Limoniae essence.
5. Febuxostat dispersing tablet preparation according to claim 1 is characterized in that described binding agent adopts hypromellose.
6. Febuxostat dispersing tablet preparation according to claim 1 is characterized in that the composition of supplementary material and proportioning are: 0.5～5 part of 40～150 parts of Febuxostats, 50～200 parts of microcrystalline Cellulose, 5～20 parts of cross-linking sodium carboxymethyl celluloses, 10～30 parts of polyvinylpolypyrrolidone, 50～200 parts of lactose, 1～10 part of aspartame, 0.5～5 part of magnesium stearate and hypromellose.
7. the preparation method of the described Febuxostat dispersing tablet preparation of one of claim 1～6, it is characterized in that described supplementary material crosses 100 mesh sieves, take by weighing the supplementary material except that lubricant of recipe quantity, mix homogeneously, the compacting thin slice is pulverized, 24 order granulate, the lubricant that adds recipe quantity again, total mixed, tabletting.
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| CN200910231562A CN101711751A (en) | 2009-12-04 | 2009-12-04 | Febuxostat dispersing tablet preparation and preparation method thereof |
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102078308A (en) * | 2010-12-29 | 2011-06-01 | 蚌埠丰原涂山制药有限公司 | Aspirin lysine dispersible tablet and preparation method thereof |
| CN102552197A (en) * | 2011-12-28 | 2012-07-11 | 辰欣药业股份有限公司 | Tablet containing febuxostat and preparation method of the tablet |
| CN102614146A (en) * | 2012-04-28 | 2012-08-01 | 杭州朱养心药业有限公司 | Method for preparing febuxostat tablet and febuxostat tablet |
| CN102614145A (en) * | 2012-04-28 | 2012-08-01 | 杭州朱养心药业有限公司 | Stable febuxostat tablet and preparation method thereof |
| CN103393617A (en) * | 2013-08-16 | 2013-11-20 | 成都蓉药集团四川长威制药有限公司 | Febuxostat tablet and preparation method thereof |
| US9248119B2 (en) | 2010-06-16 | 2016-02-02 | Takeda Pharmaceuticals U.S.A., Inc. | Modified release dosage forms of xanthine oxidoreductase inhibitor or xanthine oxidase inhibitors |
| CN106176738A (en) * | 2016-08-31 | 2016-12-07 | 辰欣药业股份有限公司 | A kind of Febustat pharmaceutical composition and tablet producing technology thereof |
-
2009
- 2009-12-04 CN CN200910231562A patent/CN101711751A/en active Pending
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9248119B2 (en) | 2010-06-16 | 2016-02-02 | Takeda Pharmaceuticals U.S.A., Inc. | Modified release dosage forms of xanthine oxidoreductase inhibitor or xanthine oxidase inhibitors |
| US9937157B2 (en) | 2010-06-16 | 2018-04-10 | Takeda Pharmaceuticals U.S.A., Inc. | Modified release dosage forms of xanthine oxidoreductase inhibitor or xanthine oxidase inhibitors |
| CN102078308A (en) * | 2010-12-29 | 2011-06-01 | 蚌埠丰原涂山制药有限公司 | Aspirin lysine dispersible tablet and preparation method thereof |
| CN102552197A (en) * | 2011-12-28 | 2012-07-11 | 辰欣药业股份有限公司 | Tablet containing febuxostat and preparation method of the tablet |
| CN102614146A (en) * | 2012-04-28 | 2012-08-01 | 杭州朱养心药业有限公司 | Method for preparing febuxostat tablet and febuxostat tablet |
| CN102614145A (en) * | 2012-04-28 | 2012-08-01 | 杭州朱养心药业有限公司 | Stable febuxostat tablet and preparation method thereof |
| CN102614145B (en) * | 2012-04-28 | 2013-05-01 | 杭州朱养心药业有限公司 | Stable febuxostat tablet and preparation method thereof |
| CN103393617A (en) * | 2013-08-16 | 2013-11-20 | 成都蓉药集团四川长威制药有限公司 | Febuxostat tablet and preparation method thereof |
| CN103393617B (en) * | 2013-08-16 | 2015-11-04 | 四川峨嵋山药业股份有限公司 | Febustat tablet and preparation method thereof |
| CN106176738A (en) * | 2016-08-31 | 2016-12-07 | 辰欣药业股份有限公司 | A kind of Febustat pharmaceutical composition and tablet producing technology thereof |
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Open date: 20100526 |