CN104069085A - Aspirin enteric sustained-release capsule and preparation method thereof - Google Patents
Aspirin enteric sustained-release capsule and preparation method thereof Download PDFInfo
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- CN104069085A CN104069085A CN201410310585.7A CN201410310585A CN104069085A CN 104069085 A CN104069085 A CN 104069085A CN 201410310585 A CN201410310585 A CN 201410310585A CN 104069085 A CN104069085 A CN 104069085A
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- aspirin
- slow releasing
- coated slow
- releasing capsule
- aspirin enteric
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Abstract
The invention provides an aspirin enteric sustained-release capsule and a preparation method thereof, and relates to the technical field of medicament production. The formula of the capsule comprises the following components: 30-60 percent of aspirin, 30-60 percent of packing, 1-10 percent of release regulating agent and 2-20 percent of a frame material, wherein the packing is one or more of mannitol, sorbitol, xylitol, lactose, saccharose, glucose, starch, dextrin, pregelatinized starch and microcrystalline cellulose; the release regulating agent is one or more of sodium carboxymethyl starch, polyvinylpolypyrrolidone, hydroxypropylcellulose and microcrystalline cellulose; the frame material is one or more of hydroxypropyl methyl cellulose, ethyecellulose, carbomer, sodium alginate and stearic acid. About 100mg of the aspirin enteric sustained-release capsule is taken once a day conventionally, irritation of the capsule to gastric mucosa is avoided due to existence of the enteric capsule after a patient takes the aspirin enteric sustained-release capsule, the capsule is dissolved after entering the intestinal tract, and the content micro-tablet of the capsule slowly release aspirin, so that the aspirin enteric sustained-release capsule is very convenient for patients who have cardiovascular diseases and need to take medicines for a long time.
Description
Technical field
The present invention relates to medicament production technical field, relate in particular to a kind of aspirin enteric-coated slow releasing capsule and preparation method thereof.
Background technology
Aspirin claims again aspirin, belongs to NSAID (non-steroidal anti-inflammatory drug).As the non-selective inhibitors of cyclooxygenases of synthetic the earliest, aspirin is mainly used in treating flu, heating, headache, rheumatism etc., has applied clinically so far more than 100 year, and aspirin remains most widely used antipyretic analgesic so far.Along with going deep into of studying, the clinical practice field of aspirin is constantly expanded in recent years, comprises control cardiovascular and cerebrovascular disease and prophylaxis of cancer etc.Can antiinflammatory as large dose oral administration, middle dosage is taken and can be eased pain, and low dose is taken and can be prevented the platelet initiation blood vessel blockage of condensing, cardiovascular disease that simultaneously can anti-tampon causes effectively.Aspirin has stronger stimulation to gastric mucosa, and long-term, high-dose is taken and can be caused gastric ulcer and gastrorrhagia.The half-life of another A Silin only has 15 minutes, for the patient who needs the cardiovascular disease of Long-term taking medicine, needs multiple dosing every day, very inconvenient.
Summary of the invention
The object of the invention is to overcome the defect of prior art, a kind of aspirin enteric-coated slow releasing capsule and preparation method thereof is provided, this aspirin enteric-coated slow releasing capsule can not have stimulation to gastric mucosa, for the patient of cardiovascular disease, does not need again multiple dosing every day.
Technical problem to be solved by this invention realizes by the following technical solutions.
Aspirin enteric-coated slow releasing capsule formula of the present invention contains 30%-60% aspirin, 30%-60% filler, 1%-10% release regulator and 2%-20% framework material, described percentage ratio accounts for the mass percent of aspirin tablet total amount for each composition, and described filler is one or more in mannitol, sorbitol, xylitol, lactose, sucrose, glucose, starch, dextrin, pregelatinized Starch and microcrystalline Cellulose; Described release regulator is one or more in carboxymethyl starch sodium, polyvinylpolypyrrolidone, hyprolose and microcrystalline Cellulose; Described framework material is one or more in hydroxypropyl emthylcellulose (HPMC), ethyl cellulose, carbomer, sodium alginate and stearic acid.
In the present invention, described aspirin is the aspirin described in the routine of this area, and the content of described aspirin is preferably 30%-50%,, the mass percent of described percentage ratio aspirin enteric-coated slow releasing capsule content total amount for each composition accounts for.
In the present invention, described filler is preferably one or more in lactose, starch, dextrin and pregelatinized Starch.The content of described filler is preferably 40%-50%, the mass percent of described percentage ratio aspirin enteric-coated slow releasing capsule content total amount for each composition accounts for.
In the present invention, described release regulator is preferably carboxymethyl starch sodium and/or polyvinylpolypyrrolidone, and better is carboxymethyl starch sodium.The content of described release regulator is preferably 2%-5%, the mass percent of described percentage ratio aspirin enteric-coated slow releasing capsule content total amount for each composition accounts for.
In the present invention, described framework material is preferably hydroxypropyl emthylcellulose (HPMC) and/or ethyl cellulose, and better is hydroxypropyl emthylcellulose.The content of described framework material is preferably 5%-15%, the mass percent of described percentage ratio aspirin enteric-coated slow releasing capsule content total amount for each composition accounts for.
In the present invention, described aspirin enteric-coated slow releasing capsule preferably also contains binding agent.The kind of described binding agent and content are that this area routine is used.Described binding agent is preferably hydroxypropyl emthylcellulose and/or PVP K30 (PVP K30), and better is PVP K30; The content of described binding agent is preferably 2.0%-2.5%, and described percentage ratio accounts for the mass percent of aspirin enteric-coated slow releasing capsule total amount for each composition.
In aspirin enteric-coated slow releasing capsule of the present invention, also can contain conventional various active component or other additives adding in this area, as long as no antagonism or the aspirin enteric-coated slow releasing capsule effect of not appreciable impact the present invention.
Aspirin enteric-coated slow releasing capsule formula of the present invention is preferably comprised of 30%-60% aspirin, 30%-60% filler, 1%-10% release regulator, 2%-20% framework material and lubricant; Described filler is one or more in mannitol, sorbitol, xylitol, lactose, sucrose, glucose, starch, dextrin, pregelatinized Starch and microcrystalline Cellulose; Described release regulator is one or more in carboxymethyl starch sodium, polyvinylpolypyrrolidone, hyprolose and microcrystalline Cellulose; Described framework material is one or more in hydroxypropyl emthylcellulose (HPMC), ethyl cellulose, carbomer, sodium alginate and stearic acid.
Aspirin enteric-coated slow releasing capsule one preferred embodiments formula of the present invention is comprised of 30%-50% aspirin, 40%-55% filler, 2%-5% release regulator, 5%-15% framework material and 0.5%-2% lubricant, and described percentage ratio accounts for the mass percent of aspirin enteric-coated slow releasing capsule total amount for each composition.The concrete kind of each composition all as previously mentioned.
Aspirin enteric-coated slow releasing capsule of the present invention, first by this area conventional tablet preparation method, make little slice, thin piece, preferably, as wet granule compression tablet method or direct powder compression, when described preparation method is wet granule compression tablet method, the formula of described aspirin tablet preferably contains binding agent.Described binding agent as previously mentioned.Then microplate is poured into enteric coated capsule.
Wherein, described wet granule compression tablet method preferably comprises the steps:, by filling a prescription after aspirin, filler, release regulator and framework material mix homogeneously, to add the alcoholic solution soft material processed containing binding agent, the granulation of sieving, dry, granulate, add lubricant, tabletting.Wherein, in the alcoholic solution of described binding agent, ethanol content is preferably 50%-100%, and that better is 70%-85%, and percentage ratio is percent by volume.
Wherein, described direct powder compression preferably comprises the steps:, by filling a prescription after aspirin, filler, release regulator and framework material mix homogeneously, to add lubricant, tabletting, fill.
In the present invention, the specification of described aspirin enteric-coated slow releasing capsule is generally conventional by this area, makes the capsule containing aspirin 25-300mg.
Agents useful for same of the present invention and raw material be commercially available obtaining all.
Meeting on the basis of this area general knowledge, in the present invention, the optimum condition of each above-mentioned technical characterictic can combination in any obtain preferred embodiments of the present invention.
Positive progressive effect of the present invention is: aspirin enteric-coated slow releasing capsule of the present invention is used about 100mg time/every day routinely, after patient takes, existence due to enteric coated capsule, avoided the stimulation to gastric mucosa, enter after intestinal, capsule dissolves, the content microplate of capsule slowly discharges aspirin.For the patient of the cardiovascular disease of Long-term taking medicine, quite convenient.
The specific embodiment
For technological means, creation characteristic that the present invention is realized, reach object and effect is easy to understand, below in conjunction with specific embodiment, further set forth the present invention.
Each component equal commercially available obtaining except specified otherwise in following embodiment; Wherein, concrete model K4M, K15M, K100M and the E4M of described hydroxypropyl emthylcellulose are the conventional model of ability.
Embodiment 1
Preparation method: aspirin, hydroxypropyl emthylcellulose, carboxymethyl starch sodium, starch are sieved respectively, be dry mixed 10 minutes, add binding agent polyvidone alcoholic solution soft material processed, granulate, dry, granulate, adds magnesium stearate mix homogeneously, be pressed into microplate, fill, obtains.
Embodiment 2
Preparation method: aspirin, hydroxypropyl emthylcellulose, carboxymethyl starch sodium, pregelatinized Starch, microcrystalline Cellulose are sieved respectively, be dry mixed 20 minutes, add magnesium stearate mix homogeneously, be directly pressed into microplate, fill, obtains.
Embodiment 3
Preparation method: aspirin, hydroxypropyl emthylcellulose, carboxymethyl starch sodium, dextrin are sieved respectively, be dry mixed 10 minutes, add binding agent polyvidone alcoholic solution soft material processed, granulate, dry, granulate, adds magnesium stearate mix homogeneously, be pressed into microplate, fill, obtains.
Embodiment 4
| Component | Gram |
| Aspirin | 80 |
| Hydroxypropyl emthylcellulose | 20 |
| Carboxymethyl starch sodium | 4 |
| Lactose | 74 |
| Magnesium stearate | 2 |
| Gross weight | 180 |
Preparation method: aspirin, hydroxypropyl emthylcellulose, carboxymethyl starch sodium, lactose are sieved respectively, be dry mixed 20 minutes, add magnesium stearate mix homogeneously, be directly pressed into microplate, fill, obtains.
Embodiment 5
Preparation method: aspirin, hydroxypropyl emthylcellulose, polyvinylpolypyrrolidone, starch are sieved respectively, be dry mixed 10 minutes, add binding agent polyvidone alcoholic solution soft material processed, granulate, dry, granulate, adds magnesium stearate mix homogeneously, be pressed into microplate, fill, obtains.
Embodiment 6
Preparation method: aspirin, hydroxypropyl emthylcellulose, polyvinylpolypyrrolidone, pregelatinized Starch are sieved respectively, be dry mixed 20 minutes, add magnesium stearate mix homogeneously, be directly pressed into microplate, fill, obtains.
Embodiment 7
Preparation method: aspirin, hydroxypropyl emthylcellulose, polyvinylpolypyrrolidone, dextrin are sieved respectively, be dry mixed 10 minutes, add binding agent polyvidone alcoholic solution soft material processed, granulate, dry, granulate, adds magnesium stearate mix homogeneously, be pressed into microplate, fill, obtains.
Embodiment 8
| Component | Gram |
| Aspirin | 300 |
| Hydroxypropyl methyl fiber (K4M) | 75 |
| Carboxymethyl starch sodium | 10 |
| Lactose | 110 |
| Magnesium stearate | 5 |
| Gross weight | 500 |
Preparation method: aspirin, hydroxypropyl emthylcellulose, polyvinylpolypyrrolidone, lactose are sieved respectively, be dry mixed 20 minutes, add magnesium stearate mix homogeneously, be directly pressed into microplate, fill, obtains.
Embodiment 9
| Component | Gram |
| Aspirin | 80 |
| Hydrochlorothiazide | 12.5 |
| Hydroxypropyl emthylcellulose | 20 |
| Carboxymethyl starch sodium | 4 |
| Lactose | 61.5 |
| Magnesium stearate | 2 |
| Gross weight | 180 |
Preparation method: aspirin, hydrochlorothiazide, hydroxypropyl emthylcellulose, polyvinylpolypyrrolidone, lactose are sieved respectively, be dry mixed 20 minutes, add magnesium stearate mix homogeneously, be directly pressed into microplate, fill, obtains.
Table 1 is that the oral rear drug disposition of embodiment 4 medicine discharges result.Data are as follows:
| Time (hour) | Discharge the accumulative total percent of medicine |
| 1 | 39.7％ |
| 2 | 63.8％ |
| 3 | 83.9％ |
| 4 | 90.2％ |
| 5 | 94.7％ |
| 6 | 99.6％ |
Table 1
The mensuration product that table 2 is embodiment 1 is taken rear blood drug level result.Data are as follows:
Table 2
More than show and described ultimate principle of the present invention, principal character and advantage of the present invention.The technical staff of the industry should understand; the present invention is not restricted to the described embodiments; that in above-described embodiment and description, describes just illustrates principle of the present invention; without departing from the spirit and scope of the present invention; the present invention also has various changes and modifications, and these changes and improvements all fall in the claimed scope of the invention.The claimed scope of the present invention is defined by appending claims and equivalent thereof.
Claims (9)
1. an aspirin enteric-coated slow releasing capsule, it is characterized in that, its formula contains 30%-60% aspirin, 30%-60% filler, 1%-10% release regulator and 2%-20% framework material, the mass percent of the percentage ratio of each composition aspirin enteric-coated slow releasing capsule content total amount for each composition accounts for, described filler is one or more in mannitol, sorbitol, xylitol, lactose, sucrose, glucose, starch, dextrin, pregelatinized Starch and microcrystalline Cellulose; Described release regulator is one or more in carboxymethyl starch sodium, polyvinylpolypyrrolidone, hyprolose and microcrystalline Cellulose; Described framework material is one or more in hydroxypropyl emthylcellulose, ethyl cellulose, carbomer, sodium alginate and stearic acid.
2. aspirin enteric-coated slow releasing capsule according to claim 1, is characterized in that: the content of described aspirin is 30%-50%, the mass percent of described percentage ratio aspirin enteric-coated slow releasing capsule content total amount for each composition accounts for.
3. aspirin enteric-coated slow releasing capsule according to claim 1, is characterized in that: the content of described filler is 40%-50%, the mass percent of described percentage ratio aspirin enteric-coated slow releasing capsule content total amount for each composition accounts for.
4. aspirin enteric-coated slow releasing capsule according to claim 1, is characterized in that: the content of described release regulator is 2%-5%, the mass percent of described percentage ratio aspirin enteric-coated slow releasing capsule content total amount for each composition accounts for.
5. aspirin enteric-coated slow releasing capsule according to claim 1, is characterized in that: the content of described framework material is 5%-15%, the mass percent of described percentage ratio aspirin enteric-coated slow releasing capsule content total amount for each composition accounts for.
6. aspirin enteric-coated slow releasing capsule according to claim 1, is characterized in that: in aspirin enteric-coated slow releasing capsule, also contain lubricant, described lubricant is one or more in Pulvis Talci, micropowder silica gel and magnesium stearate; The content of described lubricant is 0.5%-2%, the mass percent of described percentage ratio aspirin enteric-coated slow releasing capsule content total amount for each composition accounts for.
7. the preparation method of aspirin enteric-coated slow releasing capsule described in any one in a claim 1～6, it is characterized in that, described preparation method is for first adopting wet granule compression tablet method or powder to be directly pressed into microplate, described preparation method is wet granulation while being pressed into microplate, and described formula contains binding agent; Then pack enteric coated capsule into and get final product.
8. the preparation method of aspirin enteric-coated slow releasing capsule according to claim 7, it is characterized in that: described wet granulation is pressed into microplate and comprises the steps: by formula after aspirin, filler, release regulator and framework material mix homogeneously, add the alcoholic solution soft material processed containing binding agent, the granulation of sieving, dry, granulate, add lubricant, be pressed into microplate, fill; Wherein, in the alcoholic solution of described binding agent, ethanol content is 50%-100%, is preferably 70%-85%, and percentage ratio is percent by volume.
9. the preparation method of aspirin enteric-coated slow releasing capsule according to claim 7, it is characterized in that: described powder is directly pressed into microplate and comprises the steps: by formula after aspirin, filler, release regulator and framework material mix homogeneously, add lubricant, be pressed into microplate, fill.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410310585.7A CN104069085A (en) | 2014-06-26 | 2014-06-26 | Aspirin enteric sustained-release capsule and preparation method thereof |
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| CN201410310585.7A CN104069085A (en) | 2014-06-26 | 2014-06-26 | Aspirin enteric sustained-release capsule and preparation method thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105796524A (en) * | 2016-03-29 | 2016-07-27 | 南京多宝生物科技有限公司 | Aspirin enteric-coated tablet |
| CN108434109A (en) * | 2018-04-25 | 2018-08-24 | 首都医科大学附属北京儿童医院 | Miniature mercaptopurine tablets, miniature mercaptopurine enteric-coated sustained-release tablet, and preparation method thereof |
| CN112587506A (en) * | 2020-12-09 | 2021-04-02 | 南京森博医药研发有限公司 | Method for preparing mesalazine enteric sustained-release capsule |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101502517A (en) * | 2008-09-04 | 2009-08-12 | 山东淄博新达制药有限公司 | Glipizide enteric sustained-release preparation composition and method for preparing the same |
| CN101874786A (en) * | 2010-06-05 | 2010-11-03 | 浙江金华康恩贝生物制药有限公司 | Aspirin enteric-coated preparation prepared by solvent-free extrusion spheronization method |
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2014
- 2014-06-26 CN CN201410310585.7A patent/CN104069085A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101502517A (en) * | 2008-09-04 | 2009-08-12 | 山东淄博新达制药有限公司 | Glipizide enteric sustained-release preparation composition and method for preparing the same |
| CN101874786A (en) * | 2010-06-05 | 2010-11-03 | 浙江金华康恩贝生物制药有限公司 | Aspirin enteric-coated preparation prepared by solvent-free extrusion spheronization method |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105796524A (en) * | 2016-03-29 | 2016-07-27 | 南京多宝生物科技有限公司 | Aspirin enteric-coated tablet |
| CN105796524B (en) * | 2016-03-29 | 2019-01-01 | 山西兰花药业股份有限公司 | A kind of aspirin enteric coated tablet |
| CN108434109A (en) * | 2018-04-25 | 2018-08-24 | 首都医科大学附属北京儿童医院 | Miniature mercaptopurine tablets, miniature mercaptopurine enteric-coated sustained-release tablet, and preparation method thereof |
| CN112587506A (en) * | 2020-12-09 | 2021-04-02 | 南京森博医药研发有限公司 | Method for preparing mesalazine enteric sustained-release capsule |
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