CN102670531B - A kind of Loxoprofen sodium composition - Google Patents
A kind of Loxoprofen sodium composition Download PDFInfo
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- CN102670531B CN102670531B CN201210123938.3A CN201210123938A CN102670531B CN 102670531 B CN102670531 B CN 102670531B CN 201210123938 A CN201210123938 A CN 201210123938A CN 102670531 B CN102670531 B CN 102670531B
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- loxoprofen sodium
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- silicon dioxide
- polyvinylpolypyrrolidone
- magnesium stearate
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Abstract
The present invention relates to a kind of Loxoprofen sodium composition.Because loxoprofen sodium viscosity is comparatively large, its dispersible tablet one is after disintegrate, easy conglomeration, not easily all by No. two sieves; Two is easy moisture absorptions, and the slice, thin piece after moisture absorption is puffy, and drug content declines, and especially dissolution declines obviously.The present invention is by changing preparation process, and in being adopted by the silicon dioxide in prescription, addition adds, and obtains a kind of dispersing uniformity good, and highly stable compositions.
Description
Technical field the present invention relates to a kind of Loxoprofen sodium composition.
Background technology
Loxoprofen sodium, chemical name: 2-[4-(2-oxocyclopentyl methyl) phenyl] sodium propionate dihydrate.Belong to phenylpropionic acid non-steroid antiinflammatory drug.
Loxoprofen sodium is developed by Japanese Sankyo Co., Ltd.Loxoprofen sodium is compared with similar drugs clinically, and its feature is mainly reflected in: clinical effectiveness is good, and side effect is little.Another kind of feature is that indication is wide, the easing pain and diminishing inflammation after can being widely used in the anti-inflammatory and antalgic of rheumatoid arthritis, lumbago, scapulohumeral periarthritis, neck shoulder wrist syndrome etc., operation, wound clinically and after exodontia and the antipyretic-antalgic etc. of acute upper respiratory tract inflammation.Loxoprofen sodium dispersible tablets belongs to medical insurance Class B product.Because loxoprofen sodium viscosity is comparatively large, one be dispersible tablet composition after disintegrate, easy conglomeration, not easily all by No. two sieves; Two is easy moisture absorptions, and the slice, thin piece after moisture absorption is puffy, and drug content declines, and especially dissolution declines obviously.
The object of this invention is to provide a kind of loxoprofen sodium dispersive composition, said composition has good dispersing uniformity, and stable in properties.
Summary of the invention
The technical problem to be solved in the present invention is: solve the technical barrier that loxoprofen sodium dispersing uniformity is bad, provide a kind of loxoprofen sodium dispersive composition meeting States Pharmacopoeia specifications, and said composition stable in properties.
Technical scheme of the present invention is:
A kind of loxoprofen sodium dispersive composition, containing loxoprofen sodium and silicon dioxide, is characterized in that silicon dioxide adopts interior addition to add.
Silicon dioxide, as fluidizer, generally adds with outer addition, namely adds after granulation, to increase the mobility of granule, reduces the resistance of tabletting.The technical solution used in the present invention adds in being.
The preferred technical scheme of the present invention is 3 ~ 5% (percentage by weights) that the consumption of silicon dioxide accounts for prescription total amount.
The preferred technical scheme of the present invention is:
Loxoprofen sodium 2H
2o68.00g, microcrystalline Cellulose 199.0g, polyvinylpolypyrrolidone (XL-10) 15.00g, silica 1 5.00g, magnesium stearate 3.00g, 95% alcoholic solution is appropriate.Wherein silicon dioxide adopts interior addition to add.Make: 1000.
The preferred technical scheme of the present invention is:
Loxoprofen sodium 2H
2o68.00g, microcrystalline Cellulose 199.0g, polyvinylpolypyrrolidone (XL-10) 15.00g, silica 1 2.00g, magnesium stearate 3.00g, 95% alcoholic solution is appropriate.Wherein silicon dioxide adopts interior addition to add.Make: 1000.
The preparation method of the present composition is
The first step takes loxoprofen sodium and adjuvant, crosses 100 mesh sieves.
Second step takes the loxoprofen sodium dihydrate of recipe quantity, microcrystalline Cellulose, silicon dioxide, polyvinylpolypyrrolidone XL-10 in wet mixing pelletizer, is dry mixed 5min mix homogeneously, obtains mixture.
3rd step adds 95% ethanol (about 75g/1000 sheet) in mixture, soft material processed.
4th step is crossed 24 mesh sieves and is granulated.
5th step wet granular 60 DEG C forced air drying is less than 3% to weightlessness.
The dry granule of 6th step crosses 20 mesh sieve granulate, adds magnesium stearate, mix homogeneously.
Drug content in granule is determined in 7th pacing, determines sheet weight.
The Φ 10mm scrobicula stamping of 8th step, Hardness Control is within 50N.
9th step packaging.
The invention has the beneficial effects as follows:
Inside add silicon dioxide and can make principal agent and silicon dioxide Homogeneous phase mixing, effectively reduce the viscosity of loxoprofen sodium itself, can all by No. 2 sieves after dispersible tablet dispersion can be ensured.
Present composition hygroscopicity is little, and accelerated test six months indices are basicly stable, is convenient to store.And commercial dispersants sheet accelerates moisture expantion in six months causes packages in damaged condition, and dissolution obviously declines.
Embodiment 1 feature: add in silicon dioxide.
Loxoprofen sodium 2H
2o68.00g, microcrystalline Cellulose 199.0g, polyvinylpolypyrrolidone (XL-10) 15.00g, silica 1 5.00g, magnesium stearate 3.00g, 95% alcoholic solution is appropriate.Make: 1000.
The preparation method of the present composition is
The first step takes loxoprofen sodium and adjuvant, crosses 100 mesh sieves.
Second step takes the loxoprofen sodium dihydrate of recipe quantity, microcrystalline Cellulose, silicon dioxide, polyvinylpolypyrrolidone (XL-10) in wet mixing pelletizer, is dry mixed 5min mix homogeneously, obtains mixture.
3rd step adds 95% ethanol (about 75g/1000 sheet) in mixture, soft material processed.
4th step is crossed 24 mesh sieves and is granulated.
5th step wet granular 60 DEG C forced air drying is less than 3% to weightlessness.
The dry granule of 6th step crosses 20 mesh sieve granulate, adds magnesium stearate, mix homogeneously.
Drug content in granule is determined in 7th pacing, determines sheet weight.
The Φ 10mm scrobicula stamping of 8th step, Hardness Control is within 50N.
9th step packaging.Aluminum-plastic blister adds composite film packaging.Pack with commercially available prod.
Embodiment 2 feature: add in silicon dioxide.
Loxoprofen sodium 2H
2o68.00g, microcrystalline Cellulose 199.0g, polyvinylpolypyrrolidone (XL-10) 15.00g, silicon dioxide 9.00g, magnesium stearate 3.00g, 95% alcoholic solution is appropriate.1000 are made by the method for embodiment 1.
Embodiment 3 feature: add in silicon dioxide.
Loxoprofen sodium 2H
2o68.00g, microcrystalline Cellulose 199.0g, polyvinylpolypyrrolidone (XL-10) 15.00g, silica 1 2.00g, magnesium stearate 3.00g, 95% alcoholic solution is appropriate.1000 are made by the method for embodiment 1.
Reference examples 1: feature: silicon dioxide is additional.
Loxoprofen sodium 2H
2o68.00g, microcrystalline Cellulose 199.0g, polyvinylpolypyrrolidone (XL-10) 15.00g, magnesium stearate 3.00g, 95% alcoholic solution is appropriate.Make: 1000.Prepare by the preparation method of embodiment 1.Preparation method:
The first step takes loxoprofen sodium and adjuvant, crosses 100 mesh sieves.
Second step takes the loxoprofen sodium dihydrate of recipe quantity, microcrystalline Cellulose, polyvinylpolypyrrolidone (XL-10) in wet mixing pelletizer, is dry mixed 5min mix homogeneously, obtains mixture.
3rd step adds 95% ethanol (about 75g/1000 sheet) in mixture, soft material processed.
4th step is crossed 24 mesh sieves and is granulated.
5th step wet granular 60 DEG C forced air drying is less than 3% to weightlessness.
The dry granule of 6th step crosses 20 mesh sieve granulate, adds magnesium stearate, mix homogeneously.
Drug content in granule is determined in 7th pacing, determines sheet weight.
The Φ 10mm scrobicula stamping of 8th step, Hardness Control is within 50N.
9th step packaging.Aluminum-plastic blister adds composite film packaging.Pack with commercially available prod.
The inspection of test example 1 dispersing uniformity
According under version Chinese Pharmacopoeia annex IA tablet item in 2010:
[dispersing uniformity] dispersible tablet inspection method: get test sample 6, put in 250ml beaker, add
water 100ml, jolting 3 minutes, should all disintegrates by No. two sieves.
Each 6 of Example compositions, reference examples compositions, commercial dispersants sheet, carries out dispersing uniformity inspection by the method for States Pharmacopoeia specifications.
Table 1, dispersing uniformity check data
Test data shows: by No. 2 sieves in example composition 1min, and reference examples compositions 3.1min is by No. 2 sieves.Commercial dispersants sheet 1.5min is by No. 2 sieves.Namely the dispersion effect of the present composition is better than reference examples and commercial dispersants sheet.
Test example 2. stability comparative study data
Example composition, reference examples compositions and commercial composite are placed in climatic chamber, temperature 40 DEG C, humidity 75%, carries out accelerated test study on the stability.
Relevant data after table 2 example composition accelerated test
Note: dissolution adopts in slurry processes 50r/min, 900ml water, 37 DEG C, sampling in 30 minutes detects, detection method: high phase liquid chromatography.
Test data shows: the present composition through accelerated test after 6 months indices change not obvious.Present composition stable in properties is described.
Relevant data after table 3 reference examples and commercial dispersants sheet accelerated test
Note: dissolution adopts in slurry processes 50r/min, 900ml water, 37 DEG C, sampling in 30 minutes detects, detection method: high phase liquid chromatography.
Test data shows: reference examples and enforcement sample are after accelerated test, and sheet moisture absorption is serious, and sheet is puffy, and packaging is by distending; Drug content obviously declines; Related substance obviously raises; Dissolution obviously declines.
It is good that above test data illustrates that the present composition has dispersing uniformity, stable feature.In other words, technical scheme of the present invention obtains a kind of dispersing uniformity and good stability in the product of prior art.Tool has an unexpected effect.
Claims (4)
1.
a kind of loxoprofen sodium dispersive composition, it is characterized in that, containing loxoprofen sodium 2H2O68.00mg in the compositions of unit dose, microcrystalline Cellulose 199.0mg, model is the polyvinylpolypyrrolidone 15.00mg of XL-10, silica 1 5.00mg, magnesium stearate 3.00mg, wherein, described dispersive composition is tablet, and in silicon dioxide adopts, addition adds.
2.
a kind of loxoprofen sodium dispersive composition, it is characterized in that, containing loxoprofen sodium 2H2O68.00g, microcrystalline Cellulose 199.0g in every 1000, model is the polyvinylpolypyrrolidone 15.00g of XL-10, silicon dioxide 9.00g, magnesium stearate 3.00g, 95% alcoholic solution is appropriate, wherein, in silicon dioxide adopts, addition adds, and preparation method is:
the first step takes loxoprofen sodium and adjuvant, crosses 100 mesh sieves;
second step takes the loxoprofen sodium dihydrate of recipe quantity, microcrystalline Cellulose, silicon dioxide, polyvinylpolypyrrolidone in wet mixing pelletizer, is dry mixed 5min mix homogeneously, obtains mixture;
3rd step adds 95% ethanol in mixture, measures as 75g/1000 sheet, soft material processed;
4th step is crossed 24 mesh sieves and is granulated;
5th step wet granular 60 DEG C forced air drying is less than 3% to weightlessness;
the dry granule of 6th step crosses 20 mesh sieve granulate, adds magnesium stearate, mix homogeneously;
drug content in granule is determined in 7th pacing, determines sheet weight;
the Φ 10mm scrobicula stamping of 8th step, Hardness Control is within 50N;
9th step packaging; Aluminum-plastic blister adds composite film packaging.
3.
a kind of loxoprofen sodium dispersive composition, it is characterized in that, containing loxoprofen sodium 2H2O68.00g, microcrystalline Cellulose 199.0g in every 1000, model is the polyvinylpolypyrrolidone 15.00g of XL-10, silica 1 2.00g, magnesium stearate 3.00g, 95% alcoholic solution is appropriate, wherein, in silicon dioxide adopts, addition adds, and preparation method is:
the first step takes loxoprofen sodium and adjuvant, crosses 100 mesh sieves;
second step takes the loxoprofen sodium dihydrate of recipe quantity, microcrystalline Cellulose, silicon dioxide, polyvinylpolypyrrolidone in wet mixing pelletizer, is dry mixed 5min mix homogeneously, obtains mixture;
3rd step adds 95% ethanol in mixture, measures as 75g/1000 sheet, soft material processed;
4th step is crossed 24 mesh sieves and is granulated;
5th step wet granular 60 DEG C forced air drying is less than 3% to weightlessness;
the dry granule of 6th step crosses 20 mesh sieve granulate, adds magnesium stearate, mix homogeneously;
drug content in granule is determined in 7th pacing, determines sheet weight;
the Φ 10mm scrobicula stamping of 8th step, Hardness Control is within 50N;
9th step packaging; Aluminum-plastic blister adds composite film packaging.
4.
the preparation method of compositions described in claim 1, is characterized in that,
the first step takes loxoprofen sodium and adjuvant, crosses 100 mesh sieves;
second step takes the loxoprofen sodium dihydrate of recipe quantity, microcrystalline Cellulose, silicon dioxide, polyvinylpolypyrrolidone XL-10 in wet mixing pelletizer, is dry mixed 5min mix homogeneously, obtains mixture;
3rd step adds 95% ethanol in mixture, measures as 75g/1000 sheet, soft material processed;
4th step is crossed 24 mesh sieves and is granulated;
5th step wet granular 60 DEG C forced air drying is less than 3% to weightlessness;
the dry granule of 6th step crosses 20 mesh sieve granulate, adds magnesium stearate, mix homogeneously;
drug content in granule is determined in 7th pacing, determines sheet weight;
the Φ 10mm scrobicula stamping of 8th step, Hardness Control is within 50N;
9th step packaging.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201210123938.3A CN102670531B (en) | 2012-04-19 | 2012-04-19 | A kind of Loxoprofen sodium composition |
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| CN201210123938.3A CN102670531B (en) | 2012-04-19 | 2012-04-19 | A kind of Loxoprofen sodium composition |
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| CN102670531B true CN102670531B (en) | 2015-11-11 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN104644665A (en) * | 2014-06-26 | 2015-05-27 | 黄心诚 | Medicine for treating arthritis |
| CN111700868B (en) * | 2020-06-23 | 2021-04-20 | 福建东瑞制药有限公司 | Loxoprofen sodium tablet and preparation process thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1628648A (en) * | 2004-08-26 | 2005-06-22 | 复旦大学 | Loxoprofen sodium sustained release preparation |
| CN1771973A (en) * | 2005-10-25 | 2006-05-17 | 张哲峰 | Composite medicine containing nonsteroidal anti-inflammatory analgetic and its prepn |
| CN101342147A (en) * | 2008-08-28 | 2009-01-14 | 复旦大学 | Loxoprofen sodium framework tablet |
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2012
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1628648A (en) * | 2004-08-26 | 2005-06-22 | 复旦大学 | Loxoprofen sodium sustained release preparation |
| CN1771973A (en) * | 2005-10-25 | 2006-05-17 | 张哲峰 | Composite medicine containing nonsteroidal anti-inflammatory analgetic and its prepn |
| CN101342147A (en) * | 2008-08-28 | 2009-01-14 | 复旦大学 | Loxoprofen sodium framework tablet |
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Effective date of registration: 20160822 Address after: 264205 No. 1 South Qingdao Road, Weihai economic and technological development, Shandong Patentee after: DISHA PHARMACEUTICAL GROUP Co.,Ltd. Patentee after: WEIHAI DISU PHARMACEUTICAL Co.,Ltd. Address before: 264205 No. 1 South Qingdao Road, Weihai economic and technological development, Shandong Patentee before: DISHA PHARMACEUTICAL GROUP Co.,Ltd. Patentee before: Shandong Disha Pharmaceutical Co.,Ltd., Disha Phamaceutical Group Patentee before: WEIHAI DISU PHARMACEUTICAL Co.,Ltd. Patentee before: Weihai Weitai Pharmaceutical Technology Development Co.,Ltd. |
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Effective date of registration: 20210623 Address after: No.1 Qingdao South Road, Weihai Economic and Technological Development Zone, Shandong Province Patentee after: DISHA PHARMACEUTICAL GROUP Co.,Ltd. Address before: No.1 Qingdao South Road, Weihai Economic and Technological Development Zone, Shandong Province Patentee before: DISHA PHARMACEUTICAL GROUP Co.,Ltd. Patentee before: Dijia Pharmaceutical Group Co.,Ltd. Effective date of registration: 20210623 Address after: No.1 Qingdao South Road, Weihai Economic and Technological Development Zone, Shandong Province Patentee after: DISHA PHARMACEUTICAL GROUP Co.,Ltd. Patentee after: Dijia Pharmaceutical Group Co.,Ltd. Address before: No.261 economic and Technological Development Road, Weinan, Qingdao, Shandong Province Patentee before: DISHA PHARMACEUTICAL GROUP Co.,Ltd. Patentee before: WEIHAI DISU PHARMACEUTICAL Co.,Ltd. |