CN1245163C - Puerarin dispersing tablet composition and its preparation method - Google Patents
Puerarin dispersing tablet composition and its preparation method Download PDFInfo
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- CN1245163C CN1245163C CN 03141615 CN03141615A CN1245163C CN 1245163 C CN1245163 C CN 1245163C CN 03141615 CN03141615 CN 03141615 CN 03141615 A CN03141615 A CN 03141615A CN 1245163 C CN1245163 C CN 1245163C
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Abstract
The present invention relates to a dispersive table composition of puerarin and a preparation method thereof. The composition adopts puerarin as a main component, and also contains proper excipient and an auxiliary agent, wherein the excipient and the auxiliary agent are selected from a disintegrating agent, a diluting agent, a lubricating agent, an antisticking agent, edulcorant, etc. The composition is suitable for preparing dispersible tablets which can be disintegrated within less than three minutes in water of 19 DEG C to 21 DEG C, and thus, the composition provides convenience for patients with difficulty in swallowing. In addition, bioavailability is enhanced. The composition can be used for treating apoplexy, coronary disease and angina pectoris.
Description
Technical field
The invention belongs to medical technical field, be specifically related to a kind of puerarin pharmaceutical preparation,, the invention still further relates to the preparation method of said preparation simultaneously more specifically to a kind of dispersible tablet of puerarin agent.
Background technology
Puerarin has pharmacological action comparatively widely; experimental results show that puerarin has dilating effect to coronary artery; can protect global ischemia cardiac muscle and myocardial ischemia reperfusion injury; reduce the acute myocardial infarction area; reduce myocardial oxygen consumption; prevent platelet adhesion, gathering and thrombosis, puerarin has significant protective effect to acute cerebral ischemia, and B-adrenergic receptor is had blocking effect.Clinically, puerarin is mainly used in the treatment of diseases such as coronary heart disease, angina pectoris, myocardial infarction, ischemic cerebrovascular, sudden deafness, retina artery and vein obstruction.
The preparation of puerarin is widely used in clinical, and wherein injection accounts for very big proportion.As everyone knows, for the cardiovascular and cerebrovascular vessel patient that needs are taken medicine for a long time, need take during except that first aid the intravenous injection, keeping treatment should be more convenient with oral formulations, therefore should develop the oral formulations that absorbs the puerarin fast, that bioavailability is high.The oral formulations of puerarin is mainly tablet in the market, because the dissolubility of puerarin is bad, the effective ingredient stripping of tablet is slow, onset in time; Though drop pill is rapid-action, the curative effect height, producing needs the special installation cost higher.
Summary of the invention
The object of the present invention is to provide a kind of steady quality, convenient drug administration, rapid-action, dispersible tablet of puerarin and production method thereof that curative effect is high, product is an oral administered dosage form.
Dispersible tablet is a solid medicinal form for oral administration, and they must disintegrate in 3 minutes in 19 ℃～21 ℃ water, and is dispersed in the water.2000 editions two radicals by which characters are arranged in traditional Chinese dictionaries of Chinese Pharmacopoeia have recorded this dosage form, and dispersing uniformity has been done requirement: 2 dispersible tablets are put into the extremely complete disintegrate of 100ml water jolting and can be passed through sieve No. 2.
The parameter of definition dispersible tablet is as follows: 1. the particulate uniform distribution of its disintegration rate high in water 2. disintegrates.Disintegration rate and dispersed homogeneous degree also depend on adjuvant and active component.The character of finished tablet and quality depend on adjuvant blended with it to a great extent, are very important so correctly select adjuvant.The new medicinal formula of the puerarin of suitable preparation dispersible tablet provided by the invention has been considered these problems, the active component puerarin accounts for the 7-15% of composition total weight in this prescription, and all the other are excipient and adjuvant: disintegrating agent, diluent, lubricant, antitack agent.In addition, also can add sweeting agent etc.
Because the key parameter of dispersible tablet is their disintegration rates in water, so the disintegrating agent of selecting is one of most crucial steps.The effect of disintegrating agent is to make surface area to increase so that the active component of this tablet very rapidly discharges.The consumption of the disintegrating agent in the present invention's prescription is the 5-10% of composition total weight, and this disintegrating agent can be sodium starch glycol, acroleic acid polymerization derivant or crospolyvinylpyrrolidone.Diluent includes and helps pressed powder shape material and make tablet have the excipient of certain intensity.Microcrystalline Cellulose, lactose, hydroxypropyl cellulose, mannitol and their mixture are suitable diluent, and its consumption is the 60-90% of composition total weight.Microcrystalline Cellulose is a kind of most suitable flowability and the powder mixture of compressibility.It also can be used as adhesive, form the tool suitable stiffness, the tablet of certain intensity is arranged, and its absorbability causes very short disintegration time.Usually the mixture that can adopt microcrystalline Cellulose and lactose is as diluent, and the microcrystalline Cellulose of particle mean size between 50～90 microns is proper, and its content accounts for 40～50% of composition total weight.Lactose is a kind of disaccharide, can make tablet produce very big hardness, and its content accounts for 20～40% of composition total weight.
The lubricant of mentioning among the present invention comprises can reduce frictional force between the tablet endoparticle, reduces the excipient of the recoil strength on the nib wall.Lubricant can adopt magnesium stearate or micronized sodium lauryl sulphate, makes the easier release of downtrodden preparation, even can guarantee to fill up the nib space, thereby reduces the weight differential of tablet.Its content accounts for 1～2.5% of composition total weight in the present invention." antitack agent " among the present invention comprises the adhesion of prevention granule, thereby avoids or reduce the excipient of their frictional force.Polyvidone is suitable antitack agent, and its content accounts for 3～6% of composition total weight.Among the present invention, sweeting agent can be synthetic or natural, or its mixture.
The present invention adopts the wet granule compression tablet technology to prepare above-mentioned dispersible tablet through testing repeatedly, and concrete steps are as follows:
Progressively increase method with principal agent and the various auxiliary materials and mixing except that lubricant by equivalent, cross 80 mesh sieves; Material behind the mixing is put in the appropriate containers, and the adding dehydrated alcohol is an amount of, makes soft material; 20 orders pushed the sieve series wet granular; Place thermostatic drying chamber 65-85 ℃ to descend dry 100-150 minute wet granular, take by weighing granule by prescription, add the lubricant of recipe quantity, tabletting promptly behind the mixing.
Dispersible tablet of puerarin to commercially available puerarin sheet and development carries out dissolution relatively, under identical leaching condition, and 45 minutes stripping less thaies 15% of puerarin sheet, and dispersible tablet of puerarin stripping fully in 15 minutes.
The more known dosage form of the dispersible tablet of puerarin has series of advantages, comprises;
1, good dispersing state, disintegration time are short, the medicine stripping is fast;
2, absorption is fast, bioavailability is high,
3, taking convenience can be swallowed, chew to contain and suck or with taking after the aqueous dispersion, especially is fit to old man, paralytic and the patient of the difficulty of swallowing takes.
The specific embodiment
The invention is further illustrated by the following examples.
Embodiment 1:
The prescription of dispersible tablet composition is as follows:
Puerarin 25.13g
Lactose 45.00g
Microcrystalline Cellulose 70.00g
Crospolyvinylpyrrolidone 7.50g
Aspartame 3.00g
Polyvidone 7.00g
Dehydrated alcohol is an amount of
Magnesium stearate is an amount of
Be pressed into 1000 altogether
Its preparation technology is as follows:
All cross 80 mesh sieves before the supplementary material weighing.Precision takes by weighing the puerarin of recipe quantity and lactose, microcrystalline Cellulose, crospolyvinylpyrrolidone (4.5g), aspartame, polyvidone, progressively increases method with principal agent and various adjuvant manual mix homogeneously earlier by equivalent.Cross twice of 80 mesh sieve.
Material behind the mixing is put in the appropriate containers, and the adding dehydrated alcohol is an amount of, the system soft material.20 orders pushed the sieve series wet granular.
Wet granular is divided in enamel tray, puts in the air blast thermostatic drying chamber 70 ℃ of dry 2h.Precision takes by weighing the weight of dried particles, and the amount by 1% adds magnesium stearate, adds the residue crospolyvinylpyrrolidone of 3.0g again, and behind the mixing, the circular punch die of 7mm is pressed into 1000.Promptly.
Embodiment 2:
The prescription of dispersible tablet composition is as follows:
Puerarin 25.00g
Lactose 50.00g
Microcrystalline Cellulose 65.00g
Crospolyvinylpyrrolidone 7.50g
Aspartame 1.00g
Polyvidone 9.00g
Dehydrated alcohol is an amount of
Sodium lauryl sulphate is an amount of
Be pressed into 1000 altogether
Its preparation technology is as follows:
All cross 80 mesh sieves before the supplementary material weighing.Precision takes by weighing the puerarin of recipe quantity and lactose, microcrystalline Cellulose, crospolyvinylpyrrolidone (4.5g), aspartame, polyvidone, progressively increases method with principal agent and various adjuvant manual mix homogeneously earlier by equivalent.Cross twice of 80 mesh sieve.
Material behind the mixing is put in the appropriate containers, and the adding dehydrated alcohol is an amount of, the system soft material.20 orders pushed the sieve series wet granular.
Wet granular is divided in enamel tray, puts in the air blast thermostatic drying chamber 70 ℃ of dry 2h.Precision takes by weighing the weight of dried particles, and the amount by 2% adds micronized sodium lauryl sulphate, adds the residue crospolyvinylpyrrolidone of 3.0g again, and behind the mixing, the circular punch die of 7mm is pressed into 1000.Promptly.
Embodiment 3:
The prescription of dispersible tablet composition is as follows:
Puerarin 25.00g
Mannitol 100.00g
Sodium starch glycol 10.00g
Aspartame 3.00g
Polyvidone 8.00g
Dehydrated alcohol is an amount of
Sodium lauryl sulphate is an amount of
Be pressed into 1000 altogether
Preparation technology is with example 2.
The dispersible tablet of puerarin that is made by above-mentioned component prescription and technology has all that dispersity is good, disintegration time short, the medicine stripping is fast, the bioavailability advantages of higher.
Claims (2)
1, a kind of dispersible tablet of puerarin compositions, it is characterized in that by active component puerarin and excipient and auxiliary the composition, wherein puerarin accounts for 7～15% of composition total weight, and all the other are that excipient and adjuvant are formed: disintegrating agent, diluent, lubricant, antitack agent; Wherein, disintegrating agent is sodium starch glycol or crospolyvinylpyrrolidone, and the content of disintegrating agent is 5～10% of composition total weight; Diluent is the complex of microcrystalline Cellulose and lactose, and wherein the content of microcrystalline Cellulose accounts for 40～50% of composition total weight, and lactose accounts for 20～40% of composition total weight; Lubricant is micronized sodium lauryl sulphate or magnesium stearate, and its content is the 1-2.5% of composition total weight; Antitack agent is a polyvidone, and its content is 3～6% of composition total weight.
2, a kind of dispersible tablet of puerarin preparation of compositions method as claimed in claim 1 is characterized in that concrete steps are as follows: progressively increase method with principal agent and the various auxiliary materials and mixing except that lubricant by equivalent, cross 80 mesh sieves; Material behind the mixing is put in the appropriate containers, and the adding dehydrated alcohol is an amount of, makes soft material; 20 orders pushed the sieve series wet granular; Place thermostatic drying chamber 65-85 ℃ to descend dry 100-150 minute wet granular, take by weighing granule by prescription, add the lubricant of recipe quantity, tabletting promptly behind the mixing.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03141615 CN1245163C (en) | 2003-07-15 | 2003-07-15 | Puerarin dispersing tablet composition and its preparation method |
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| Application Number | Priority Date | Filing Date | Title |
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| CN 03141615 CN1245163C (en) | 2003-07-15 | 2003-07-15 | Puerarin dispersing tablet composition and its preparation method |
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| CN1476841A CN1476841A (en) | 2004-02-25 |
| CN1245163C true CN1245163C (en) | 2006-03-15 |
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| CN 03141615 Expired - Fee Related CN1245163C (en) | 2003-07-15 | 2003-07-15 | Puerarin dispersing tablet composition and its preparation method |
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Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1326527C (en) * | 2005-07-28 | 2007-07-18 | 南京中山制药有限公司 | Dispersible tablet of puerarin and its preparation process |
| CN102266051B (en) * | 2011-06-14 | 2012-11-21 | 北京康比特体育科技股份有限公司 | Antifatigue composition and preparation method thereof |
| CN110800907A (en) * | 2019-12-18 | 2020-02-18 | 武汉有明汉方医药科技有限责任公司 | Beauty-maintaining and young-keeping instant solid beverage and preparation method thereof |
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Assignee: Yanzhou Hill Kangtai Pharmaceutical Co., Ltd. Assignor: Botai Medicine Science and Technology Co., Ltd., Shanghai Contract fulfillment period: 2008.12.29 to 2023.4.15 contract change Contract record no.: 2009370000077 Denomination of invention: Puerarin dispersing tablet composition and its preparation method Granted publication date: 20060315 License type: Exclusive license Record date: 2009.4.24 |
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Free format text: EXCLUSIVE LICENSE; TIME LIMIT OF IMPLEMENTING CONTACT: 2008.12.29 TO 2023.4.15; CHANGE OF CONTRACT Name of requester: YANZHOU HILL KANGTAI PHARMACEUTICAL CO., LTD. Effective date: 20090424 |
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Owner name: YANZHOU HILL KANGTAI PHARMACEUTICAL CO., LTD. Free format text: FORMER OWNER: SHANGHAI BOTAI PHARMACEUTICAL TECHNOLOGY CO., LTD. Effective date: 20091023 |
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Effective date of registration: 20091023 Address after: Xin Yan Zhen private industrial park in Shandong city of Yanzhou Province Patentee after: Yanzhou Hill Kangtai Pharmaceutical Co., Ltd. Address before: Room 335, No. 3021, National Road, Shanghai, China Patentee before: Botai Medicine Science and Technology Co., Ltd., Shanghai |
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Owner name: SHANDONG XI ER KANGTAI PHARMACEUTICAL CO., LTD. Free format text: FORMER NAME: YANZHOU XI ER KANGTAI PHARMACEUTICAL CO., LTD. |
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| CP01 | Change in the name or title of a patent holder |
Address after: Xin Yan Zhen Private Industrial Park 272100 Shandong city of Yanzhou Province Patentee after: SHANDONG XIER KANGTAI PHARMACEUTICAL CO., LTD. Address before: Xin Yan Zhen Private Industrial Park 272100 Shandong city of Yanzhou Province Patentee before: Yanzhou Hill Kangtai Pharmaceutical Co., Ltd. |
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