CN101428031A - Medicament preparation for preventing cardiovascular diseases - Google Patents
Medicament preparation for preventing cardiovascular diseases Download PDFInfo
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- CN101428031A CN101428031A CNA2008102096319A CN200810209631A CN101428031A CN 101428031 A CN101428031 A CN 101428031A CN A2008102096319 A CNA2008102096319 A CN A2008102096319A CN 200810209631 A CN200810209631 A CN 200810209631A CN 101428031 A CN101428031 A CN 101428031A
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- misoprostol
- aspirin
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Abstract
The invention discloses pharmaceutical preparation for preventing cardiovascular and cerebrovascular diseases. The pharmaceutical preparation is compound preparation which comprises aspirin and misoprostol; the dosage form of the compound preparation is pharmaceutical tablets, double-layer tablets or capsules which comprise aspirin and misoprostol. The preparation method of the pharmaceutical preparation comprises the following steps: preparing aspirin and misoprostol into micropills, and then preparing into tablets or capsules for taking. The drug is distributed uniformly in the gastrointestinal tracts, and belongs to a multi-unit administration system, the transport of the drug in the gastrointestinal tracts is hardly influenced by the food conveying rhythm, the difference of the drug in an individual and among individuals is small, the compliance of the patient is good, stimulation and untoward reaction which are caused by too high medicine concentration in local parts can be reduced, and injury of aspirin to the gastrointestinal tracts can be reduced or avoided; in the production process, the grain size of the two medicines is similar, and the misoprostol micropills are easy to uniformly blend with other micropills, so that the quality of the medicine is improved; the common tabletting technique and auxiliary material tabletting can be used, so as to reduce the production cost of the medicine.
Description
One, technical field
The medicine of being made up of aspirin and misoprostol that the present invention relates to specifically is a kind of pharmaceutical preparation of being made up of aspirin and misoprostol.
Two, background technology
Aspirin is antipyretic analgesic and the rheumatism treatment medicine of using always, and low-dosage aspirin has anti thrombotic action in addition, is used for prevention of stroke and coronary heart disease.But aspirin is the inhibitor of Cycloxygenase, can suppress the synthetic of prostaglandin, oral application, and particularly prolonged application has the ulcer function of causing.Aspirin caused ulcer has potential danger, because this ulcer is seldom or without any symptom, up to causing serious injury of gastrointestinal tract.As preventive usage and prolonged application is suffered denouncing of the doctor of Gastroenterology dept. always, the doctor of cardiology department then does one's utmost to advocate the use aspirin, thereby has formed a long-running argument difficult problem endlessly clinically.
Some prostaglandins medicine for example misoprostol can alleviate or prevent that aspirin is to this damage of gastrointestinal.Before the evidence aspirin discharges in vivo, use the prostaglandins medicine and can prevent the influence of aspirin gastrointestinal tract mucosa.Therefore aspirin and misoprostol are made a kind of compound preparation, and aspirin is carried out coating to delay its release, perhaps aspirin is packed casing it is discharged at intestinal, can reduce or avoid aspirin that gastrointestinal is damaged.Reached the purpose of not only prevention of stroke and coronary heart disease but also avoided to become a kind of pharmaceutical preparation that doctor of Gastroenterology dept. and the doctor of cardiology department can both accept the gastrointestinal damage.This outer coatings can also be as the screen layer between aspirin and the misoprostol, to prevent the influence of aspirin to misoprostol stability.
Three, summary of the invention
The purpose of this invention is to provide the pharmaceutical preparation that a kind of aspirin and misoprostol are formed, this pharmaceutical preparation is the compound preparation that aspirin and misoprostol are formed; The dosage form of compound preparation is medicinal tablet, bilayer tablet or the capsule of being made up of aspirin and misoprostol; The composition content of said preparation is that unit contains aspirin 40～50mg with every or every capsule; Contain misoprostol 0.2mg, when solving this medicine and being used to prevent cardiovascular and cerebrovascular disease, reduce or avoid aspirin gastrointestinal tract to be caused the problem of damage.
For achieving the above object, the technical solution used in the present invention is as follows:
1, the compound preparation of aspirin and misoprostol composition, the dosage form of compound preparation is medicinal tablet, bilayer tablet or the capsule of being made up of aspirin and misoprostol; It is formed content and contains with every or every capsule:
Aspirin 40～50mg
Misoprostol 0.200mg
2, contained aspirin is the aspirin coated micropill of making in the tablet in the such scheme, bilayer tablet or the capsule, and misoprostol is the misoprostol micropill of making.
1) preparation of aspirin casing micropill:
The preparation use of aspirin casing micropill is extruded spheronization and is prepared the ball core, fluidized bed process coating or coating pan coating.The purpose of coating is the release that is used to delay principal agent, in the process of preparation aspirin casing micropill, note suitably increasing the toughness of micropill coating, and fracture appears in coating in the tabletting process to avoid.For this reason, when giving the micropill coating, should in coating solution, add an amount of plasticizer and make the micropill of making have certain pliability, when pressurized, can produce slight distortion, break avoiding.But can not be too soft, produce to prevent excessive deformation and to break or damage.Aspirin is a kind of more highly acid medicine that has in addition, the long-time contact with enteric layer can make its acidproof ability drop, for this reason, the sealing coat that has designed one deck and with the hydroxypropyl emthylcellulose be major ingredient separates aspirin and enteric layer, has effectively avoided the destruction of aspirin to enteric layer.For prevent that further aspirin casing micropill from occurring breaking and set up screen layer at aspirin layer and misoprostol interlayer in the tabletting process, the present invention adds the blank micropill that the buffering micropill of being made by pharmaceutic adjuvant does not promptly contain aspirin and misoprostol component in technology, the buffering micropill is made up of pharmaceutic adjuvants such as microcrystalline Cellulose and stearic acid.This buffering micropill has triple role, prevents that promptly the aspirin coated micropill from breaking; Screen layer between aspirin layer and the misoprostol layer; Make the tablet smooth surface.
2) preparation of misoprostol micropill:
USP4 is adopted in the preparation of misoprostol powder among the present invention, and 301,146 method is dispersed in misoprostol in hydroxypropyl emthylcellulose or the polyethylene pyrrole network alkane ketone, and misoprostol concentration is 1%; Or misoprostol is dispersed in the mixture of hydroxypropyl emthylcellulose and polyethylene pyrrole network alkane ketone, the concentration of misoprostol is 1%.
A, will be dispersed in misoprostol powder and polyethylene pyrrole network alkane ketone and microcrystalline Cellulose mixing in the hydroxypropyl emthylcellulose, with the dehydrated alcohol is that spheronization is extruded in the wetting agent use or marumerization prepares the misoprostol micropill, and the concentration that contains misoprostol in the misoprostol powder is 1%.Misoprostol powder, polyethylene pyrrole network alkane ketone and the blended ratio of microcrystalline Cellulose are from 20:5:75 to 20:50:30, and the ratio of recommendation is 20:20:60.
B, with 1% misoprostol hydroxypropyl emthylcellulose powder and microcrystalline Cellulose mixing, polyethylene pyrrole network alkane ketone is dissolved in the dehydrated alcohol, make 20% polyethylene pyrrole network alkane ketone ethanol solution and make adhesive, spheronization is extruded in use or marumerization is made the misoprostol micropill.In the micropill ratio of 1% misoprostol hydroxypropyl emthylcellulose powder and microcrystalline Cellulose be 20:20 to 20:80, the ratio of recommendation is 20:60.
C, misoprostol is dispersed in the polyethylene pyrrole network alkane ketone, makes 1% misoprostol polyethylene pyrrole network alkane ketone powder.With 1% misoprostol polyethylene pyrrole network alkane ketone powder and microcrystalline Cellulose mixing, make wetting agent with ethanol solution, spheronization is extruded in use or marumerization is made the misoprostol micropill.In the micropill ratio of 1% misoprostol polyethylene pyrrole network alkane ketone powder and microcrystalline Cellulose be 20:20 to 20:100, the ratio of recommendation is 20:80.
The diameter of micropill generally between 0.25mm～1.5mm, is preferably between 0.8mm～1.2mm, in this diameter range, can avoid breaking because of tension force produces the coating of micropill.
3, contain the tablet or the capsular preparation of aspirin casing micropill and misoprostol micropill:
The tablet that contains aspirin casing micropill and misoprostol micropill is to use the process preparation of conventional preparation tablet, comprising:
A, promptly cushion tabletting behind micropill and other adjuvant mix homogeneously with aspirin casing micropill, misoprostol micropill and with the blank micropill that pharmaceutic adjuvants such as microcrystalline Cellulose are made.
B, will incapsulate behind aspirin casing micropill, misoprostol micropill and other adjuvant mix homogeneously.
The preparation of c, aspirin casing micropill and misoprostol micropill bilayer tablet: in aspirin casing micropill among the present invention and the misoprostol micropill bilayer tablet, to be the misoprostol micropill mix the tablet that is pressed into buffering micropill and suitable adjuvant to last synusia; Following synusia be aspirin casing micropill with buffering micropill and suitable adjuvant such as adhesive, filler, disintegrating agent, mix lubricant after the tablet that is pressed into.Proper auxiliary materials such as adhesive, filler, disintegrating agent, lubricant are meant the adjuvant commonly used that oral drug preparation allows.
According to the dosage of clinical prevention cardiovascular and cerebrovascular disease, determine that every or each capsular content are for containing aspirin 40～50mg; Contain misoprostol 200ug.
In the pharmaceutical preparation of reporting in the known patent documentation that contains misoprostol, in order to guarantee the stable of misoprostol, misoprostol is to be dispersed in the hydroxypropyl emthylcellulose, adopts direct powder compression when the preparation tablet, requires to use special process and adjuvant.USP6287600 mentions in example misoprostol is dissolved in the ethanol, is mixed and made into granule with hydroxypropyl emthylcellulose, makes tablet or capsule then.The granule proportion that this method of discovery is made in experiment is little, quality is light, and the edge is not neat.When the compacting double-layer tablet, this lamella is too loose, and is rough; With the aspirin mixed pressuring plate or when incapsulating, can not uniform mixing, influence end product quality.In addition, can not make micropill.The present invention makes micropill with misoprostol under the situation that does not influence misoprostol stability; Secondly after the misoprostol micropill was made tablet, this pellet tablet belonged to the multiple-unit drug-supplying system, helps improving curative effect, reduced untoward reaction; Its three, after misoprostol micropill and aspirin micropill and buffering micropill mix, available common tablet machine tabletting.At last, in process of production, aspirin micropill, misoprostol micropill proportion are approaching, and mix homogeneously easily helps improving the quality of product.
The good effect that the present invention has: the present invention makes the casing micropill with aspirin, and misoprostol is made micropill, then aspirin casing micropill and misoprostol micropill is made tablet or capsule with the micropill tablet forming technique; After taking, medicine is evenly distributed at gastrointestinal tract, belongs to the multiple-unit drug-supplying system, be subjected to food to carry the influence of the rhythm and pace of moving things few in the gastrointestinal transhipment, little with interindividual variation in the individuality of medicine, patient's compliance is good, can reduce the zest and the untoward reaction that cause because of local drug concentration is too high; In the production process, the granularity of two kinds of medicines is close, and misoprostol micropill and the easy mix homogeneously of other micropill are improved the quality of medicine, and can use common tablet forming technique and adjuvant tabletting, reduces the production cost of medicine.
Four, the specific embodiment
Embodiment 1: preparation aspirin/misoprostol sheet
1, the composition content of tablet
A, aspirin casing micropill contain aspirin 50mg
B, misoprostol micropill contain misoprostol 200ug
C, the buffering micropill an amount of
D, carboxymethyl starch sodium are an amount of
E, magnesium stearate are an amount of
2, the preparation of micropill
Aspirin and microcrystalline Cellulose are got in the preparation of a, aspirin casing micropill, the mixed of pressing 1:1 is even, make wetting agent with 5% ethyl cellulose ethanol solution, extrude spheronization and make micropill, the ball core that sieves and choose 0.8～1.2mm, put in the coating pan, wrap contagion gown and enteric coating respectively.
1% misoprostol hydroxypropyl emthylcellulose powder and the microcrystalline Cellulose weight ratio mixing by 20:60 is got in the preparation of b, misoprostol micropill, polyethylene pyrrole network alkane ketone is dissolved in the dehydrated alcohol, make 20% polyethylene pyrrole network alkane ketone ethanol solution and make adhesive, extrude spheronization and make the misoprostol micropill.
The preparation of c, buffering micropill is got microcrystalline Cellulose and stearic acid with the weight ratio mixing of 7:3, adds 2% sodium lauryl sulphate and makes wetting agent, extrudes spheronization and makes micropill.
3, make the tablet of heavy 0.5g by the conventional preparation method of tablet in the pharmaceutical preparation, every contains aspirin 50mg, misoprostol 200ug.
Embodiment 2: preparation aspirin/misoprostol double-layer tablet
1, constituent content
A, aspirin casing micropill contain aspirin 40mg
B, misoprostol micropill contain misoprostol 200ug
C, the buffering micropill an amount of
D, carboxymethyl starch sodium are an amount of
E, hydrogenated cottonseed oil are an amount of
2, the preparation of micropill, the preparation of aspirin micropill, buffering micropill is with embodiment 1.The preparation of misoprostol micropill: get 1% misoprostol hydroxypropyl emthylcellulose powder, polyethylene pyrrole network alkane ketone and microcrystalline Cellulose weight ratio mixing by 20:10:60, with the dehydrated alcohol is in the wetting agent, extrudes spheronization and makes the misoprostol micropill.
3, the preparation of double-layer tablet with aspirin casing micropill and an amount of c, d, e mixing, with misoprostol micropill and an amount of c, d, e mixing, uses bi-layer tablet press to be pressed into the tablet of heavy 0.5g.
Embodiment 3: preparation aspirin/misoprostol capsule
1, constituent content
A, aspirin casing micropill contain aspirin 50mg
B, misoprostol micropill contain misoprostol 200ug
2, the preparation of micropill is with embodiment 1.
3, the conventional preparation method of pressing capsule incapsulates said medicine and auxiliary materials and mixing, the heavy 0.4g of capsule.
Claims (6)
1, a kind of pharmaceutical preparation of being made up of aspirin and misoprostol is characterized in that: this pharmaceutical preparation is the compound preparation that aspirin and misoprostol are formed; The dosage form of compound preparation is medicinal tablet, bilayer tablet or the capsule of being made up of aspirin and misoprostol; The composition content of said preparation is that unit contains aspirin 40～50mg with every or every capsule, contains misoprostol 0.2mg.
2, the described pharmaceutical preparation of forming by aspirin and misoprostol of a kind of claim 1, it is characterized in that: contained aspirin is the aspirin coated micropill of making in described tablet, bilayer tablet or the capsule, and misoprostol is the misoprostol micropill of making.
3, the pharmaceutical preparation of being made up of aspirin and misoprostol according to claim 2 is characterized in that: the aspirin coated micropill is the casing micropill.
4, the pharmaceutical preparation of being made up of aspirin and misoprostol according to claim 2 is characterized in that: described tablet is to mix the back compacting in flakes by buffering micropill and other adjuvant that aspirin coated micropill, misoprostol micropill, pharmaceutic adjuvant are made.
5, the pharmaceutical preparation of being made up of aspirin and misoprostol according to claim 2 is characterized in that: the homogeneous mixture that contains aspirin coated micropill, misoprostol micropill and other pharmaceutic adjuvant in the described capsule.
6, the pharmaceutical preparation of being made up of aspirin and misoprostol according to claim 2 is characterized in that: described double-layer tablet on it synusia be that misoprostol micropill, buffering micropill mix the tablet that is pressed into the adjuvant that suits; Following synusia be the aspirin coated micropill with buffering micropill and suitable adjuvant such as adhesive, filler, disintegrating agent, mix lubricant after the tablet that is pressed into.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008102096319A CN101428031A (en) | 2008-12-03 | 2008-12-03 | Medicament preparation for preventing cardiovascular diseases |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008102096319A CN101428031A (en) | 2008-12-03 | 2008-12-03 | Medicament preparation for preventing cardiovascular diseases |
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| Publication Number | Publication Date |
|---|---|
| CN101428031A true CN101428031A (en) | 2009-05-13 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2008102096319A Pending CN101428031A (en) | 2008-12-03 | 2008-12-03 | Medicament preparation for preventing cardiovascular diseases |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102697746A (en) * | 2012-06-11 | 2012-10-03 | 广州朗圣药业有限公司 | Rapid melting misoprostol vaginal composition as well as preparation method and application of same |
| CN110538165A (en) * | 2019-09-27 | 2019-12-06 | 北京新领先医药科技发展有限公司 | Aspirin-containing enteric capsule and preparation method thereof |
-
2008
- 2008-12-03 CN CNA2008102096319A patent/CN101428031A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102697746A (en) * | 2012-06-11 | 2012-10-03 | 广州朗圣药业有限公司 | Rapid melting misoprostol vaginal composition as well as preparation method and application of same |
| CN110538165A (en) * | 2019-09-27 | 2019-12-06 | 北京新领先医药科技发展有限公司 | Aspirin-containing enteric capsule and preparation method thereof |
| CN110538165B (en) * | 2019-09-27 | 2023-03-14 | 北京新领先医药科技发展有限公司 | Aspirin-containing enteric capsule and preparation method thereof |
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| PB01 | Publication | ||
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Open date: 20090513 |