CN1241572C - Slow and control release aspirin capsule formulation and method for making same - Google Patents
Slow and control release aspirin capsule formulation and method for making same Download PDFInfo
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- CN1241572C CN1241572C CN 03144249 CN03144249A CN1241572C CN 1241572 C CN1241572 C CN 1241572C CN 03144249 CN03144249 CN 03144249 CN 03144249 A CN03144249 A CN 03144249A CN 1241572 C CN1241572 C CN 1241572C
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- aspirin
- micropill
- polyethylene glycol
- hydroxypropyl methylcellulose
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Abstract
The present invention relates to an aspirin slow-controlled-release capsule preparation and a preparing method thereof, which mainly comprises aspirin, sucrose, starch, alcohol, Tween-80, acrylic resin and talcum powder. 1000 capsules comprise 100 to 350 g of micro pills containing the medicines of 50, 75 or 150 g of the aspirin and 0 to 200 g of hollow micro pills. The ingredients of the prescription are prepared by the following method: the aspirin is wrapped on hollow pill cores to produce the micro pills containing the aspirin; the micro pills containing the medicines and having required particle diameters are obtained by sieving operation; release-control films are wrapped; finished products are obtained by loading the micro pills wrapped by the films into capsules. The present invention does not release the aspirin in the stomach, and releases little aspirin (lower than 0.1%) in stomach juice so as to reduce the side effect of the aspirin on the stomach. The aspirin release degree in intestinal liquid is good (close to 100%) so as to reduce the side effect. Thus, the treating effect is improved.
Description
Technical field
The present invention relates to the sustained and controlled release capsule preparation preparation, particularly aspirin sustained and controlled release capsule preparation and preparation method thereof of aspirin.
Background technology
Aspirin is a kind of medicine that uses last 100 years, and main pharmacological was analgesic paroxysmal pain antiinflammatory when it was heavy dose of, and clear and definite blood coagulation resisting function is arranged during 50-150g, thereby as all kinds of thrombotic common drugs of a kind of prevention.But the side effect of aspirin mainly is a GI irritation, also clearly.Heavy dose of or especially obvious when taking for a long time.The existing case history report that much causes gastric ulcer, gastrorrhagia about a large amount of use aspirin.The Aspirin Enteric-coated Tablets production and sales were once arranged, reduced gastrointestinal stimulation, but it is very big that tablet is influenced by musculus sphincter pyloricus, report that its time from the stomach to the small intestinal is to cause blood drug level very unstable in 15 minutes to 7 hours thereby have, and cause the small intestinal local concentration too high easily, the aggravation side effect.Be badly in need of a kind of pre-preventing thrombosis effect that can bring into play aspirin clinically, reduce its gastrointestinal side effect again, and the metastable preparation of blood drug level.The slow controlled-release technology of micropill is to develop a very fast technology recently, existing successful application on a lot of kinds, and effect is obvious.Based on this, if, just can reach the reduction side effect, the purpose that heightens the effect of a treatment with the aspirin that is applied to of this technology success.
Summary of the invention
The object of the invention provides a kind of aspirin sustained and controlled release capsule preparation and preparation method thereof, reduces the side effect of aspirin by the sustained and controlled release capsule preparation preparation of making aspirin.The aspirin sustained and controlled release capsule preparation preparation that the present invention makes is subjected to the influence of sphincter of pylorus hardly, and discharges aspirin under one's belt hardly, thereby has reduced side effect, has improved curative effect.
Capsule of the present invention is the micropill that contains the aspirin of effective dose, or also contains an amount of blank micropill, and described micropill contains medical controlled release, extended release agent.
The aspirin of described effective dose is 50-150g; Described capsule grain diameter is 450 μ m-1700 μ m; Described blank micropill diameter is 450 μ m-1700 μ m.
Described aspirin micropill comprises that ball core, medicated layer and coatings constitute.
Described blank micropill comprises that ball core and coatings constitute.
The weight of described ball core is formed and is comprised:
Sucrose or lactose 50-150g
Starch or microcrystalline Cellulose 50-150g
Hydroxypropyl methylcellulose or polyvidone or Polyethylene Glycol 2-10g
The weight of described medicated layer is formed and is comprised (per 1000 capsules consumptions):
Aspirin 50g-150g
Sucrose or lactose 50-150g
Starch or microcrystalline Cellulose 50-150g
Hydroxypropyl methylcellulose or polyvidone or Polyethylene Glycol 2-10g
The described weight that contains aspirin micropill coatings is formed (every 1000g micropill consumption):
Acrylic resin or hydroxypropyl methylcellulose phthalate 30-100g
Plasticizer: tween 80 or Polyethylene Glycol or Oleum Ricini 5-15g
95% ethanol 1000-1500g
Destaticizer Pulvis Talci 15-30g
Described blank micropill coatings is formed the coatings of stating that can be same as, and also can be made of hydroxypropyl methylcellulose, polyvidone or Polyethylene Glycol:
Blank micropill 1000g
Hydroxypropyl methylcellulose, polyvidone or Polyethylene Glycol constitute 2-10g
95% ethanol 1000-1500g
Destaticizer Pulvis Talci 15-30g
Can adorn capsule (per 1000 capsules consumptions) in following composition and ratio according to selected capsule model:
Pastille micropill 100-350g, wherein, aspirin 50g, 75g or 150g;
Blank micropill 0-200g.
The preparation method of aspirin sustained and controlled release capsule preparation comprises the steps: earlier with ball core (preferred 450 μ m-780 μ m) binding agent (as syrup, hydroxypropyl methylcellulose, polyvidone or Polyethylene Glycol etc.) moistening, in wetting state aspirin medicated powder (or mixed powder of aspirin and suitable dressing) is spread on the ball core uniformly then, wrap one deck coatings (as crylic acid resin or hydroxypropyl methylcellulose phthalate) after drying again, pack corresponding capsule into promptly by specification (or adding blank micropill) at last.Device therefor is general core type coating machine far away, fluidized-bed coating machine or through improved coating pan.
The aspirin sustained and controlled release capsule preparation preparation that the present invention makes is subjected to the influence of sphincter of pylorus hardly, and discharges aspirin under one's belt hardly, discharges seldom (less than 0.1%) in gastric juice, has reduced the side effect of aspirin to stomach; Release fine (nearly 100%) in intestinal juice, thus side effect reduced, so improved curative effect.
Description of drawings
Fig. 1 is the release of the present invention at gastric juice).
Fig. 2 is the release of the present invention at intestinal juice.
Fig. 3 is the comparison that the present invention and aspirin intestinal hold the intestinal juice release of tablet.
The specific embodiment
Embodiment 1: the preparation of ball core
The ball core that uses among the present invention can adopt commercially available celphere, also can adopt core type coating machine far away, fluidized-bed coating machine or prepares by following prescription oneself through improved Corm Eleocharitis type coating pan.Preferred diameter is 450 μ m-780 μ m, and bulk density is best with 0.75-0.95g/ml.
Self-control celphere prescription:
Sucrose (or lactose) 1-4Kg
Starch (or microcrystalline Cellulose) 1-4Kg
30-66% sucrose slurry sucrose 3-5Kg
(or 1-4% hydroxypropyl methylcellulose, 3-10% polyvidone or 3-10% Polyethylene Glycol) 0.1-0.5Kg
Preparation method:
Sucrose (or lactose) was pulverized 150 μ m sieve, and starch (or microcrystalline Cellulose) is crossed 150 μ m sieve, is mixed with mixed powder in the prescription ratio.The sucrose slurry adds recipe quantity purified water heating for dissolving (or by concentration preparation hydroxypropyl methylcellulose, polyvidone, Polyethylene Glycol) with sucrose and crosses 150 μ m sieve.Mixed powder added core type coating machine far away, fluidized-bed coating machine or in improved coating pan, adjust parameters such as turnover air quantity, temperature, rotating speed, make mixed powder be in suitable kinestate, then adhesive is sprayed into through spray gun, make micropill, the micropill that uses the screening plant sieve to get suitable diameter more after drying promptly gets celphere.
Embodiment 2: the preparation and the coating that contain the aspirin micropill
Containing the aspirin micropill and can use core type coating machine far away or prepare by following prescription among the present invention through improved coating pan.
Contain aspirin micropill prescription:
Celphere 13-18Kg
Aspirin 6-10Kg
Starch (or microcrystalline Cellulose) 1-4Kg
Sucrose (or lactose) 1-4Kg
30-66% sucrose slurry sucrose 5-7Kg
(or 1-3% hydroxypropyl methylcellulose, 3-10% polyvidone or 3-10% Polyethylene Glycol) 0.1-0.5Kg
Aspirin was pulverized 150 μ m, and starch (microcrystalline Cellulose) is crossed 150 μ m, and sucrose (lactose) was pulverized 150 μ m, made mixed powder in the prescription ratio.The sucrose slurry is added recipe quantity purified water heating for dissolving (or by concentration preparation hydroxypropyl methylcellulose, polyvidone, Polyethylene Glycol) with sucrose cross 150 μ m sieve.Celphere added core type coating machine far away or in improved coating pan, adjust parameters such as turnover air quantity, temperature, rotating speed, make celphere be in suitable kinestate, then adhesive is sprayed into through spray gun, after treating the celphere moistening, use powder feeder unit to be disseminated to uniformly mixed powder and make micropill on the celphere.The micropill of the suitable diameter of screening promptly gets the desired aspirin micropill that contains among the present invention after drying.Carry out coating by following coating prescription then.
Contain aspirin micropill coating prescription:
Contain aspirin micropill 30Kg
Acrylic resin (or hydroxypropyl methylcellulose phthalate) 0.9-3Kg
Tween 80 (or Polyethylene Glycol) 0.15-0.45Kg
75-100% ethanol 35-45Kg
Pulvis Talci 0.45-0.9Kg
With recipe quantity acrylic resin (or hydroxypropyl methylcellulose phthalate), tween 80 (or Polyethylene Glycol or Oleum Ricini) is used the 75-100% dissolve with ethanol, places and crosses 150 μ m sieve after 24 hours.To contain that the aspirin micropill adds core type coating machine far away, fluidized-bed coating machine or in improved coating pan, adjust parameters such as turnover air quantity, temperature, rotating speed, make and contain the aspirin micropill and be in suitable kinestate, then coating solution is sprayed into through spray gun, control hydrojet speed simultaneously with the control response rate and outward appearance.Dry after screen promptly.Through quality analysis, the stomach release of this product very little (see Fig. 1, Fig. 1 is the release of the present invention at gastric juice), the intestinal juice release is (see Fig. 2, Fig. 2 is the release of the present invention at intestinal juice) better.Fig. 3 is the comparison that the present invention and aspirin intestinal hold the intestinal juice release of tablet.
Embodiment 3: the preparation of blank micropill and coating
Blank micropill among the present invention can use core type coating machine far away or prepare by following prescription through improved coating pan.
Celphere 10-15Kg
Starch (or microcrystalline Cellulose) 4-8Kg
Sucrose (or lactose) 4-8Kg
30-66% sucrose slurry sucrose 4-6Kg
(or 1-3% hydroxypropyl methylcellulose, 3-10% polyvidone or 3-10% Polyethylene Glycol) 0.25-1.25Kg
Starch (microcrystalline Cellulose) is crossed 150 μ m, and sucrose (lactose) was pulverized 150 μ m, made mixed powder in the prescription ratio.The sucrose slurry is added recipe quantity purified water heating for dissolving (or by concentration preparation hydroxypropyl methylcellulose, polyvidone, Polyethylene Glycol) with sucrose cross 150 μ m sieve.Celphere added core type coating machine far away or in improved coating pan, adjust parameters such as turnover air quantity, temperature, rotating speed, make celphere be in suitable kinestate, then adhesive is sprayed into through spray gun, after treating the celphere moistening, use powder feeder unit to be disseminated to uniformly mixed powder and make micropill on the celphere.The micropill of the suitable diameter of screening promptly gets desired blank micropill among the present invention after drying.Except that being undertaken the coating, also can carry out coating then by following coating prescription by the coating method among the embodiment two.
Blank micropill 10-15Kg
1-4% hydroxypropyl methylcellulose (or 3-10% polyvidone, 3-10% Polyethylene Glycol) 0.3-1.0Kg
Can carry out coating by the coating method among the embodiment 2.
Claims (2)
1, a kind of aspirin sustained and controlled release capsule preparation comprises ball core, medicated layer and coatings, or also comprises the pastille micropill that blank micropill constitutes, and the micropill diameter of said preparation is 450 μ m-1700 μ m;
The weight of described ball core or blank micropill is formed, and contains in per 1000 capsules:
Sucrose or lactose 50-150g
Starch or microcrystalline Cellulose 50-150g
Hydroxypropyl methylcellulose or polyvidone or Polyethylene Glycol 2-10g
Weight contained in per 1000 capsules of described medicated layer is formed:
Aspirin 50g-150g
Sucrose or lactose 50-150g
Starch or microcrystalline Cellulose 50-150g
Hydroxypropyl methylcellulose or polyvidone or Polyethylene Glycol 2-10g;
The prescription that it is characterized in that the every 1000g pastille of described coatings micropill is formed:
Hydroxypropyl methylcellulose phthalate 30-100g
Tween 80, Polyethylene Glycol or Oleum Ricini 5-15g
95% ethanol 1000-1500g
Destaticizer Pulvis Talci 15-30g.
2, according to the described aspirin sustained and controlled release capsule of claim 1 preparation, it is characterized in that the coating of described blank micropill,
The prescription of the blank micropill of every 1000g is formed:
Hydroxypropyl methylcellulose phthalate 30-100g
Tween 80, Polyethylene Glycol or Oleum Ricini 5-15g
95% ethanol 1000-1500g
Destaticizer Pulvis Talci 15-30g; Or
Press following prescription coating:
Blank micropill 1000g
Hydroxypropyl methylcellulose, polyvidone or Polyethylene Glycol 2-10g
95% ethanol 1000-1500g
Destaticizer Pulvis Talci 15-30g.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03144249 CN1241572C (en) | 2003-09-08 | 2003-09-08 | Slow and control release aspirin capsule formulation and method for making same |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03144249 CN1241572C (en) | 2003-09-08 | 2003-09-08 | Slow and control release aspirin capsule formulation and method for making same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1522702A CN1522702A (en) | 2004-08-25 |
| CN1241572C true CN1241572C (en) | 2006-02-15 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03144249 Expired - Fee Related CN1241572C (en) | 2003-09-08 | 2003-09-08 | Slow and control release aspirin capsule formulation and method for making same |
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Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101491508B (en) * | 2009-01-23 | 2011-04-20 | 上海微丸医药开发有限公司 | Preparation method of aspirin Intestine-soluble micro-pill capsules |
| CN115414333A (en) * | 2022-05-31 | 2022-12-02 | 湖北中古生物制药有限公司 | Policosanol aspirin compound preparation and preparation method thereof |
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- 2003-09-08 CN CN 03144249 patent/CN1241572C/en not_active Expired - Fee Related
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| Publication number | Publication date |
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| CN1522702A (en) | 2004-08-25 |
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Granted publication date: 20060215 Termination date: 20120908 |