CN105663049A - Apixaban sustained-release pellet and preparation method thereof - Google Patents
Apixaban sustained-release pellet and preparation method thereof Download PDFInfo
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- CN105663049A CN105663049A CN201410671960.0A CN201410671960A CN105663049A CN 105663049 A CN105663049 A CN 105663049A CN 201410671960 A CN201410671960 A CN 201410671960A CN 105663049 A CN105663049 A CN 105663049A
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- eliquis
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- sustained
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Abstract
The invention discloses an apixaban sustained-release pellet and a preparation method thereof. The apixaban sustained-release pellet includes a coating layer and a drug-containing pellet, wherein the coating layer includes Eudragit NE30D, talcum powder, and lauryl sodium sulfate or polyethylene glycol; and the drug-containing pellet includes apixaban, a blank pellet core, a filling agent, a lubricant and a bonding agent. In the invention, the novel sustained-release preparation and the pellet preparation are employed, wherein the sustained release means that the drug release rate of the drug from the preparation is sustained to reduce the absorption rate of the drug in human body, thereby achieving more stable treatment effect. The pellet increases the distribution area of the drug on surface of gastrointestinal tract, reduces irritation, improves bioavailability, is free of the influence of the gastric emptying factor, enables the drug to be absorbed uniformly in body and is less in individual difference. The two advanced technologies are employed together to improve technical advantages of the drug. The sustained-release pellet, compared with an oral liquid, is good in stability, is convenient to package, transport and store, is simple in preparation method and is suitable for industrial production.
Description
Technical field
The invention belongs to chemical medicine slow releasing preparation field, be specifically related to a kind of Eliquis slow-release micro-pill and preparation method thereof.
Background technology
Eliquis is a kind of oral Selective activation Ⅹ factor inhibitors, the pre-preventing thrombosis of energy, but hemorrhage untoward reaction is lower than old medicine warfarin, for accepting buttocks or the thrombus prevention of knee replacement patient with operation.
At present, it is low to there is drug release stablizing effect in the existing product on market, and to gastrointestinal irritation greatly, bioavailability is low, packs, transports, preserves the deficiencies such as inconvenience, and preparation method complexity.
Summary of the invention
It is an object of the invention to provide one, to have drug release stablizing effect good, gastrointestinal irritation is little, bioavailability is high, packaging, transport, storage are conveniently, the advantages such as preparation method is simple, it is adaptable to a kind of Eliquis slow-release micro-pill of thrombus prevention accepting buttocks or knee replacement patient with operation and preparation method thereof.
In order to realize the purpose of the present invention, the present invention is achieved by the following technical solutions: a kind of Eliquis slow-release micro-pill, including coatings, pastille micropill; It is characterized in that: described coatings is wrapped in outside pastille micropill; Described coatings includes: 35-175mg is strange NE30D, 5-53mg Pulvis Talci especially; Described pastille micropill includes: 2.5mg Eliquis, 80mg celphere, 197.5-252.5mg filler, 10-50mg lubricant, 5-25mg binding agent.
Described coatings also includes the sodium lauryl sulphate of trace, Polyethylene Glycol therein one or both.
In described coatings, preferred weight proportion is: 132mg is strange NE30D, 7mg Pulvis Talci especially.
In described pastille micropill, preferred weight proportion is: 2.5mg Eliquis, 80mg celphere, 237.5mg filler, 20mg lubricant, 10mg binding agent.
Described filler is microcrystalline Cellulose, and lubricant is Pulvis Talci, and binding agent is hypromellose.
Its manufacture method comprises following operation:
Step 1: get the raw materials ready: by above-mentioned quality proportioning, use pulverizer to pulverize Eliquis, crosses 100 mesh sieves;
Step 2: mixing: weigh Eliquis according to above-mentioned quality proportioning, microcrystalline Cellulose is put in three-dimensional mixer and mixed 30 minutes, makes Drug Component, takes out standby;
Step 3: the preparation of binding agent: weigh appropriate hypromellose by above-mentioned quality proportioning, adds appropriate hot water and is configured to the binding agent that concentration is 2%, standby;
Step 4: pill: Drug Component is put in the charging spout of centrifugal pellet processing machine, binding agent is put in feed tank, and celphere is put in pot, opens machine, adjust parameter, start hydrojet, start when capsule core has damp for powder, after all having spread containing medicated powder, charging spout adds Pulvis Talci, continue for powder, after Pulvis Talci has all spread, discharging; Then using vulcanization bed drying machine to dry, first dry with cool breeze, after epidermis parches, open Hot-blast Heating, inlet temperature, at 50-55 degree Celsius, uses 14,24 mesh sieve after drying, the pastille micropill taking 14-24 order size is standby;
Step 5: the preparation of coating materials: weigh especially strange NE30D, Pulvis Talci, sodium lauryl sulphate, purified water by above-mentioned quality proportioning, first sodium lauryl sulphate is joined and purified water stirs evenly dissolving, add after especially strange NE30D stirs evenly, limit stirring just adds Pulvis Talci, standby after stirring 10 minutes;
Step 6: coating: by the pastille micropill of 14-24 order size, put in fluidized-bed coating machine, coating materials is put in feed tank, stir constantly, open machine, adjust parameter, start coating, to be coated dose be finished after, start to warm up maintenance temperature of charge more than 40 degree, dry 30 minutes, cooling, discharging, closing machine;
Step 7: fill: the pastille micropill after above-mentioned coating is used capsule filling machine, medicament pellet is loaded in 0# capsule;
Step 8: plastic-aluminum: above-mentioned capsule is used aluminium-plastic bubble plate packing machine, is packaged into aluminium-plastic panel, packed products.
Beneficial effects of the present invention: of the present invention be effective ingredient with Eliquis slow-release micro-pill, main accepted buttocks or the thrombus prevention of knee replacement patient with operation with being applicable to. The relatively new slow releasing preparation adopted and pellet preparations, slow release refers to by delaying medicine rate of releasing drug from this dosage form, reduces medicine and enters the absorption rate of body, thus playing more stable therapeutic effect; Micropill has medicine and increases at gastrointestinal tract surface distributed area, can reduce zest, improves bioavailability, is not affected by gastric emptying factor simultaneously, and drug absorption in vivo is uniform, and individual variation is little; Technology two kinds advanced applies the technical advantage more enhancing this medicine simultaneously. Compared with oral liquid, having medicine stability good, packaging, transport, the advantages such as storage is convenient, its preparation method is simple, it is adaptable to commercial production.
The present invention is through two groups of clinical verifications, and one of which is that treatment group uses the present invention, and every day uses once, within 7 days, being a course for the treatment of, another group comparison uses existing Eliquis controlled release tablet, every group selection outpatient 100 example, wherein male 60 examples, female 40 example, measure 70 years old big age, minimal ages 30 years old, every day uses once, within 7 days, is a course for the treatment of, clinical manifestation is that blood is thick, and arteriosclerosis, through stone-like pulse, thrombosis, table one is the contrasting data after taking a course for the treatment of:
Table 1 is taken front and back and is compared (unit: people) two groups of courses for the treatment of
There were significant differences for treatment group and matched group, it will thus be seen that the application that the present invention is clinically has significant curative effect.
The process characteristic of the present invention: 1, selecting raw material science, production technology is advanced, and its product is conveniently deposited and uses; 2, product Chinese medicine composition is easily absorbed by the body; 3, raw material sources are extensive, add process line short, the easy processing and manufacturing of product.
Detailed description of the invention:
Embodiment 1
A kind of Eliquis slow-release micro-pill, including coatings, pastille micropill; It is characterized in that: described coatings is wrapped in outside pastille micropill; Described coatings includes: 35-175mg is strange NE30D, 5-53mg Pulvis Talci especially; Described pastille micropill includes: 2.5mg Eliquis, 80mg celphere, 197.5-252.5mg filler, 10-50mg lubricant, 5-25mg binding agent.
Described coatings also includes the sodium lauryl sulphate of trace, Polyethylene Glycol therein one or both.
In described coatings, preferred weight proportion is: 132mg is strange NE30D, 7mg Pulvis Talci especially.
In described pastille micropill, preferred weight proportion is: 2.5mg Eliquis, 80mg celphere, 237.5mg filler, 20mg lubricant, 10mg binding agent.
Described filler is microcrystalline Cellulose, and lubricant is Pulvis Talci, and binding agent is hypromellose.
Embodiment 2
Its manufacture method comprises following operation:
Step 1: get the raw materials ready: by above-mentioned quality proportioning, use pulverizer to pulverize Eliquis, crosses 100 mesh sieves;
Step 2: mixing: weigh Eliquis according to above-mentioned quality proportioning, microcrystalline Cellulose is put in three-dimensional mixer and mixed 30 minutes, makes Drug Component, takes out standby;
Step 3: the preparation of binding agent: weigh appropriate hypromellose by above-mentioned quality proportioning, adds appropriate hot water and is configured to the binding agent that concentration is 2%, standby;
Step 4: pill: Drug Component is put in the charging spout of centrifugal pellet processing machine, binding agent is put in feed tank, and celphere is put in pot, opens machine, adjust parameter, start hydrojet, start when capsule core has damp for powder, after all having spread containing medicated powder, charging spout adds Pulvis Talci, continue for powder, after Pulvis Talci has all spread, discharging; Then using vulcanization bed drying machine to dry, first dry with cool breeze, after epidermis parches, open Hot-blast Heating, inlet temperature, at 50-55 degree Celsius, uses 14,24 mesh sieve after drying, the pastille micropill taking 14-24 order size is standby;
Step 5: the preparation of coating materials: weigh especially strange NE30D, Pulvis Talci, sodium lauryl sulphate, purified water by above-mentioned quality proportioning, first sodium lauryl sulphate is joined and purified water stirs evenly dissolving, add after especially strange NE30D stirs evenly, limit stirring just adds Pulvis Talci, standby after stirring 10 minutes;
Step 6: coating: by the pastille micropill of 14-24 order size, put in fluidized-bed coating machine, coating materials is put in feed tank, stir constantly, open machine, adjust parameter, start coating, to be coated dose be finished after, start to warm up maintenance temperature of charge more than 40 degree, dry 30 minutes, cooling, discharging, closing machine;
Step 7: fill: the pastille micropill after above-mentioned coating is used capsule filling machine, medicament pellet is loaded in 0# capsule;
Step 8: plastic-aluminum: above-mentioned capsule is used aluminium-plastic bubble plate packing machine, is packaged into aluminium-plastic panel, packed products.
Claims (6)
1. an Eliquis slow-release micro-pill, including coatings, pastille micropill; It is characterized in that: described coatings is wrapped in outside pastille micropill;Described coatings includes: 35-175mg is strange NE30D, 5-53mg Pulvis Talci especially; Described pastille micropill includes: 2.5mg Eliquis, 80mg celphere, 197.5-252.5mg filler, 10-50mg lubricant, 5-25mg binding agent.
2. a kind of Eliquis slow-release micro-pill according to claim 1, it is characterised in that: described coatings also includes the sodium lauryl sulphate of trace, Polyethylene Glycol therein one or both.
3. a kind of Eliquis slow-release micro-pill according to claim 1, it is characterised in that: in described coatings, preferred weight proportion is: 132mg is strange NE30D, 7mg Pulvis Talci especially.
4. a kind of Eliquis slow-release micro-pill according to claim 1, it is characterised in that: in described pastille micropill, preferred weight proportion is: 2.5mg Eliquis, 80mg celphere, 237.5mg filler, 20mg lubricant, 10mg binding agent.
5. a kind of Eliquis slow-release micro-pill according to claim 1,4, it is characterised in that: described filler is microcrystalline Cellulose, and lubricant is Pulvis Talci, and binding agent is hypromellose.
6. the preparation method of a kind of Eliquis slow-release micro-pill according to claim 1, it is characterised in that: comprise following operation:
Step 1: get the raw materials ready: by above-mentioned quality proportioning, use pulverizer to pulverize Eliquis, crosses 100 mesh sieves;
Step 2: mixing: weigh Eliquis according to above-mentioned quality proportioning, microcrystalline Cellulose is put in three-dimensional mixer and mixed 30 minutes, makes Drug Component, takes out standby;
Step 3: the preparation of binding agent: weigh appropriate hypromellose by above-mentioned quality proportioning, adds appropriate hot water and is configured to the binding agent that concentration is 2%, standby;
Step 4: pill: Drug Component is put in the charging spout of centrifugal pellet processing machine, binding agent is put in feed tank, and celphere is put in pot, opens machine, adjust parameter, start hydrojet, start when capsule core has damp for powder, after all having spread containing medicated powder, charging spout adds Pulvis Talci, continue for powder, after Pulvis Talci has all spread, discharging; Then using vulcanization bed drying machine to dry, first dry with cool breeze, after epidermis parches, open Hot-blast Heating, inlet temperature, at 50-55 degree Celsius, uses 14,24 mesh sieve after drying, the pastille micropill taking 14-24 order size is standby;
Step 5: the preparation of coating materials: weigh especially strange NE30D, Pulvis Talci, sodium lauryl sulphate, purified water by above-mentioned quality proportioning, first sodium lauryl sulphate is joined and purified water stirs evenly dissolving, add after especially strange NE30D stirs evenly, limit stirring just adds Pulvis Talci, standby after stirring 10 minutes;
Step 6: coating: by the pastille micropill of 14-24 order size, put in fluidized-bed coating machine, coating materials is put in feed tank, stir constantly, open machine, adjust parameter, start coating, to be coated dose be finished after, start to warm up maintenance temperature of charge more than 40 degree, dry 30 minutes, cooling, discharging, closing machine;
Step 7: fill: the pastille micropill after above-mentioned coating is used capsule filling machine, medicament pellet is loaded in 0# capsule;
Step 8: plastic-aluminum: above-mentioned capsule is used aluminium-plastic bubble plate packing machine, is packaged into aluminium-plastic panel, packed products.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410671960.0A CN105663049A (en) | 2014-11-22 | 2014-11-22 | Apixaban sustained-release pellet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410671960.0A CN105663049A (en) | 2014-11-22 | 2014-11-22 | Apixaban sustained-release pellet and preparation method thereof |
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| Publication Number | Publication Date |
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| CN105663049A true CN105663049A (en) | 2016-06-15 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201410671960.0A Pending CN105663049A (en) | 2014-11-22 | 2014-11-22 | Apixaban sustained-release pellet and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019204193A1 (en) * | 2018-04-16 | 2019-10-24 | Bristol-Myers Squibb Company | Apixaban formulations |
-
2014
- 2014-11-22 CN CN201410671960.0A patent/CN105663049A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019204193A1 (en) * | 2018-04-16 | 2019-10-24 | Bristol-Myers Squibb Company | Apixaban formulations |
| JP2021521242A (en) * | 2018-04-16 | 2021-08-26 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Apixaban preparation |
| JP7382957B2 (en) | 2018-04-16 | 2023-11-17 | ブリストル－マイヤーズ スクイブ カンパニー | Apixaban formulation |
| US11896586B2 (en) | 2018-04-16 | 2024-02-13 | Bristol-Myers Squibb Company | Apixaban formulations |
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Application publication date: 20160615 |
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| WD01 | Invention patent application deemed withdrawn after publication |