CN101467985B - Bisoprolol fumarate dispersible tablet and preparation method thereof - Google Patents
Bisoprolol fumarate dispersible tablet and preparation method thereof Download PDFInfo
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- CN101467985B CN101467985B CN2007103042970A CN200710304297A CN101467985B CN 101467985 B CN101467985 B CN 101467985B CN 2007103042970 A CN2007103042970 A CN 2007103042970A CN 200710304297 A CN200710304297 A CN 200710304297A CN 101467985 B CN101467985 B CN 101467985B
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Abstract
The invention discloses a bisoprolol fumarate dispersible tablet for the treatment of essential hypertension and angina pectoris diseases and preparation process for same. The tablet is obtained by pelletizing at least part of accessories by wet method, mixing the accessories with bisoprolol fumarate, and tabletting the mixture. Inventive medicament has high bioavailability, good stability, quick disintegration and dissolution, quick action, and good compliance for patient.
Description
Technical field
The present invention relates to a kind of dispersible tablet and preparation method thereof, particularly a kind of dispersible tablet that contains the bisoprolol fumarate and preparation method thereof.
Background technology
Hypertension and angina pectoris are the modal cardiovascular disease in the world today, are the dead and wounded or disabled primary causes of disease of adult.In recent years, along with progress and the raising day by day of living standards of the people and the continuous quickening of work rhythm of society, the hypertension number of patients increases greatly.China's hypertension and angina pectoris prevalence also obviously rise, and have become one of the most serious country of these two kinds of disease harm in the world.And the damage of organs such as the heart that hypertension causes, brain, kidney, serious threat human beings'health and life.
The bisoprolol fumarate is a β with heart selectivity
1Receptor blocking agent, in the therapeutic dose scope, this product does not have tangible membrane stabilizing action or inherent sympatheticomimetic action.Long action time, it is good and do not have the tolerance phenomenon to take the control symptom continuously, minimum to the respiratory system side effect.The bisoprolol fumarate is used for essential hypertension, anginal treatment clinically.
Bisoprolol fumarate's in the market oral formulations mainly is tablet and capsule, it is inconvenient that the subject matter that these ordinary preparations exist is that patient uses when falling ill, poor compliance, and onset is slow, so these ordinary preparations exist significantly not enough in this type of disease for the treatment of.Chinese patent 200610050157.0 discloses a kind of bisoprolol Fumarate drop pills and preparation method thereof, drop pill bioavailability height, disintegrate be molten loose fast, dissolution is high, release fast, produce effects are fast.But the relative tablet complexity of drop pill preparation technology, the cost height.
The bisoprolol fumarate is to damp and hot instability, general method is wet method granule processed tabletting then when preparing tablet or capsule, in pelletization, need in baking oven, dry, make that the tablet or the capsule related substance that make are higher, have a strong impact on the quality of preparation.
Summary of the invention
The present invention be intended to overcome existing bisoprolol fumarate's preparation patient compliance is poor, onset slow and the preparation process Chinese medicine be under the hygrothermal environment unstable and cause the defective that related substance is bigger, for clinical treatment provide a kind of disintegrate molten loose fast, stripping is fast, the bisoprolol fumarate dispersible tablet and preparation method thereof of produce effects and good stability fast.
The invention provides a kind of bisoprolol fumarate dispersible tablet, contain bisoprolol fumarate and adjuvant, adjuvant comprises disintegrating agent, filler and lubricant.
The invention provides a kind of bisoprolol fumarate dispersible tablet, disintegrating agent is selected one or more the mixture in microcrystalline Cellulose, polyvinylpolypyrrolidone, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, sodium carboxymethyl cellulose, the carboxymethyl starch sodium for use, and the percentage by weight of disintegrating agent is 33%-82%.
The invention provides a kind of bisoprolol fumarate dispersible tablet, filler is selected one or more in calcium hydrogen phosphate, starch, lactose, sucrose, the calcium sulfate for use, and the percentage by weight of filler is 15%-65%.
The invention provides a kind of bisoprolol fumarate dispersible tablet, lubricant is selected one or more in micropowder silica gel, Pulvis Talci, the magnesium stearate for use, and the percentage by weight of lubricant is 0.5%-3%.
The invention provides a kind of bisoprolol fumarate dispersible tablet, can prepare by following steps: take by weighing a certain amount of adjuvant, prepare soft material with binding agent, in 50 ℃ of baking ovens, dry, add bisoprolol fumarate and residue adjuvant behind the granulate, tabletting behind the mixing.
The specific embodiment
The present invention is described in further detail below in conjunction with embodiment, but be not limited to following embodiment.Wherein " % " refers to " percentage by weight ".
The comparative example 1
(this embodiment is ordinary tablet)
| Component | Percentage ratio (%) |
| Bisoprolol fumarate's starch phosphate hydrogen calcium polyvinylpolypyrrolidone micropowder silica gel magnesium stearate total amount | 2.50 50.0 40.0 5.50 1.00 1.00 100.0 |
Preparation method:
Take by weighing bisoprolol fumarate, starch, calcium hydrogen phosphate, the polyvinylpolypyrrolidone of recipe quantity, water soft material processed behind the mixing, granulate with 18 mesh sieves, baking is 2 hours in 50 ℃ of baking ovens, take out with 30 mesh sieve granulate, after the micropowder silica gel and magnesium stearate mixing with gained granule and recipe quantity, with the stamping of 6mm scrobicula namely.
The comparative example 2
(dispersible tablet of this embodiment for making with common process)
| Component | Percentage ratio (%) |
| Bisoprolol fumarate's microcrystalline Cellulose PH101 calcium hydrogen phosphate polyvinylpolypyrrolidone micropowder silica gel magnesium stearate total amount | 2.50 50.0 37.5 8.00 1.00 1.00 100.0 |
Preparation method:
Take by weighing bisoprolol fumarate, microcrystalline Cellulose PH101, calcium hydrogen phosphate, the polyvinylpolypyrrolidone of recipe quantity, water soft material processed behind the mixing, granulate with 18 mesh sieves, baking is 2 hours in 50 ℃ of baking ovens, take out with 30 mesh sieve granulate, after the micropowder silica gel and magnesium stearate mixing with gained granule and recipe quantity, with the stamping of 6mm scrobicula namely.
Embodiment 1
| Component | Percentage ratio (%) |
| Bisoprolol fumarate's microcrystalline Cellulose PH101 calcium hydrogen phosphate polyvinylpolypyrrolidone micropowder silica gel magnesium stearate total amount | 2.50 50.0 37.5 8.00 1.00 1.00 100.0 |
Preparation method:
Take by weighing the microcrystalline Cellulose PH101 of half recipe quantity and the calcium hydrogen phosphate of polyvinylpolypyrrolidone and recipe quantity; Water soft material processed behind the mixing, granulate with 18 mesh sieves, baking is 2 hours in 50 ℃ of baking ovens, take out with 30 mesh sieve granulate, behind bisoprolol fumarate, micropowder silica gel, magnesium stearate and remaining microcrystalline Cellulose PH101 and the polyvinylpolypyrrolidone mixing with gained granule and recipe quantity, with the stamping of 6mm scrobicula namely.
Embodiment 2
| Component | Percentage ratio (%) |
| Bisoprolol fumarate's microcrystalline Cellulose PH101 calcium hydrogen phosphate polyvinylpolypyrrolidone micropowder silica gel magnesium stearate total amount | 2.50 30.0 55.5 10.0 1.00 1.00 100.0 |
Preparation method:
Take by weighing the microcrystalline Cellulose PH101 of half recipe quantity and the calcium hydrogen phosphate of polyvinylpolypyrrolidone and recipe quantity; Water soft material processed behind the mixing, granulate with 18 mesh sieves, baking is 2 hours in 50 ℃ of baking ovens, take out with 30 mesh sieve granulate, behind bisoprolol fumarate, micropowder silica gel, magnesium stearate and remaining microcrystalline Cellulose PH101 and the polyvinylpolypyrrolidone mixing with gained granule and recipe quantity, with the stamping of 6mm scrobicula namely.
Embodiment 3
| Component | Percentage ratio (%) |
| Bisoprolol fumarate's microcrystalline Cellulose PH101 calcium hydrogen phosphate polyvinylpolypyrrolidone micropowder silica gel magnesium stearate total amount | 2.50 70.0 19.5 6.00 1.00 1.00 100.0 |
Preparation method:
Take by weighing the microcrystalline Cellulose PH101 of half recipe quantity and the calcium hydrogen phosphate of polyvinylpolypyrrolidone and recipe quantity; Water soft material processed behind the mixing, granulate with 18 mesh sieves, baking is 2 hours in 50 ℃ of baking ovens, take out with 30 mesh sieve granulate, behind bisoprolol fumarate, micropowder silica gel, magnesium stearate and remaining microcrystalline Cellulose PH101 and the polyvinylpolypyrrolidone mixing with gained granule and recipe quantity, with the stamping of 6mm scrobicula namely.
Comparative example 1 and embodiment 1,2,3 and the dissolution of marketed tablet in the time of 5 minutes relatively:
Dissolution when measuring 5 minutes by 2005 editions Chinese Pharmacopoeia appendix XC dissolution methods, the result is as follows:
| Embodiment | Dissolution (%) |
| Marketed tablet comparative example 1 embodiment 1 embodiment 2 embodiment 3 | 42 36 81 76 85 |
As can be known from the results: can obviously improve the dissolution rate of pharmaceutical preparation after medicine made dispersible tablet.Comparative example 2 and embodiment 1,2,3 and the related substance of marketed tablet relatively
With the related substance in the liquid chromatography detection respective tablets, the result is as follows:
| Embodiment | Related substance (%) |
| Marketed tablet comparative example 2 embodiment 1 embodiment 2 embodiment 3 | 1.62 1.85 0.83 0.79 0.91 |
As can be known from the results; Be starkly lower than the tablet of common process preparation and commercially available with the dispersible tablet related substance of prescription of the present invention and prepared.
Claims (1)
1. a bisoprolol fumarate dispersible tablet is characterized in that, each component composed as follows:
Its preparation method is as follows:
Take by weighing the microcrystalline Cellulose PH101 of half recipe quantity and the calcium hydrogen phosphate of polyvinylpolypyrrolidone and recipe quantity; Water soft material processed behind the mixing, granulate with 18 mesh sieves, baking is 2 hours in 50 ℃ of baking ovens, take out with 30 mesh sieve granulate, behind bisoprolol fumarate, micropowder silica gel, magnesium stearate and remaining microcrystalline Cellulose PH101 and the polyvinylpolypyrrolidone mixing with gained granule and recipe quantity, with the stamping of 6mm scrobicula namely.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2007103042970A CN101467985B (en) | 2007-12-27 | 2007-12-27 | Bisoprolol fumarate dispersible tablet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2007103042970A CN101467985B (en) | 2007-12-27 | 2007-12-27 | Bisoprolol fumarate dispersible tablet and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN101467985A CN101467985A (en) | 2009-07-01 |
| CN101467985B true CN101467985B (en) | 2013-08-14 |
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|---|---|---|---|
| CN2007103042970A Active CN101467985B (en) | 2007-12-27 | 2007-12-27 | Bisoprolol fumarate dispersible tablet and preparation method thereof |
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN112245401A (en) * | 2020-11-09 | 2021-01-22 | 郑州卓峰制药有限公司 | A pharmaceutical tablet for treating hypertension and coronary heart disease, and its preparation method |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1600313A (en) * | 2003-09-28 | 2005-03-30 | 东北制药总厂 | Cefetamet pivoxil hydrochloride dispersion dispersion tablets and preparation method |
| CN1799543A (en) * | 2005-03-11 | 2006-07-12 | 浙江泰利森药业有限公司 | Telmisartan dispersible tablet and its preparation method |
| CN1823767A (en) * | 2006-03-20 | 2006-08-30 | 杨军 | Medicinal composition for treating cerebrovascular disease |
-
2007
- 2007-12-27 CN CN2007103042970A patent/CN101467985B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1600313A (en) * | 2003-09-28 | 2005-03-30 | 东北制药总厂 | Cefetamet pivoxil hydrochloride dispersion dispersion tablets and preparation method |
| CN1799543A (en) * | 2005-03-11 | 2006-07-12 | 浙江泰利森药业有限公司 | Telmisartan dispersible tablet and its preparation method |
| CN1823767A (en) * | 2006-03-20 | 2006-08-30 | 杨军 | Medicinal composition for treating cerebrovascular disease |
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| CN101467985A (en) | 2009-07-01 |
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Owner name: AVENTIS PHARMA (HAINAN) CO., LTD. Free format text: FORMER OWNER: BEIJING D-VENTURE PHARM. T. CORP. Effective date: 20110811 |
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Effective date of registration: 20110811 Address after: 570314 No. 279 Nanhai Road, Hainan, Haikou Applicant after: Beijing D-Venturepharm Technology Development Co., Ltd. Address before: 100097 Beijing city Haidian District Sijiqing Wanquan Zhuang 3 Building Applicant before: Beijing D-Venture Pharm. T. Corp. |
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