CN105596309A - Apixaban sustained-release tablet and preparation method thereof - Google Patents
Apixaban sustained-release tablet and preparation method thereof Download PDFInfo
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- CN105596309A CN105596309A CN201410671958.3A CN201410671958A CN105596309A CN 105596309 A CN105596309 A CN 105596309A CN 201410671958 A CN201410671958 A CN 201410671958A CN 105596309 A CN105596309 A CN 105596309A
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- eliquis
- sustained
- hydroxypropyl methylcellulose
- apixaban
- preparation
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Abstract
The invention discloses an apixaban sustained-release tablet and a preparation method thereof. The apixaban sustained-release tablet comprises the following components: apixaban, hydroxypropyl methylcellulose, and a lubricant. The apixaban sustained-release tablet employs a novel sustained-release preparation and a pellets preparation, sustained release means that by prolonging drug release rate of a drug in a dosage form, the absorption rate of the drug in human body is reduced, so that more stable treatment effect can be realized; the tablet has the advantage of large distribution area of the drug on surface of gastrointestinal tract, reduces irritation, increases bioavailability, and does not be influenced by gastric emptying influence, the drug can be uniformly absorbed by human body, individual difference is little; simultaneous application of two advanced technologies enhances the technical advantage of the apixaban sustained-release tablet; compared with oral liquid, the apixaban sustained-release tablet has the advantages of good drug stability, convenient package, transport and storage, the preparation method is simple and easy to operate, and is suitable for industrial production.
Description
Technical field
The invention belongs to chemical drug sustained release preparation field, be specifically related to a kind of Eliquis sustained release tablets and preparation method thereof.
Background technology
Eliquis is a kind of oral Selective activation X factor inhibitors, preventing thrombosis in advance, but hemorrhage bad reaction is lower than old medicine warfarin, for accepting the thrombus prevention of buttocks or knee replacement patient with operation.
At present, it is low that the existing product on market exists medicine to discharge stablizing effect, and large to GI irritation, bioavilability is low, packaging, transport, storage inconvenience, and the deficiency such as preparation method's complexity.
Summary of the invention
The object of this invention is to provide one have medicine discharge stablizing effect good, little to GI irritation, bioavilability is high, packaging, transport, storage are conveniently, the advantages such as preparation method is simple, be applicable to treat benign prostate hyperplasia, improve a kind of Eliquis sustained release tablets because of the relevant symptom of benign prostatic hyperplasis and preparation method thereof.
In order to realize object of the present invention, the present invention is achieved by the following technical solutions: a kind of Eliquis sustained release tablets, is characterized in that: be to be made up of the raw material of following weight: 5mg Eliquis, 50-95mg Hydroxypropyl methylcellulose, 3-20mg lubricant.
In described raw material, preferred weight proportion is: 5mg Eliquis, 93mg Hydroxypropyl methylcellulose, 5mg lubricant.
Described Hydroxypropyl methylcellulose can be one or both compositions of following model: 75hd100cr Hydroxypropyl methylcellulose, 75hd4000cr Hydroxypropyl methylcellulose, 75hd15000cr Hydroxypropyl methylcellulose, 100000cr Hydroxypropyl methylcellulose.
Described lubricant is one or both in dolomol, talcum powder, silica.
Its preparation method comprises following operation:
Step 1: get the raw materials ready: by above-mentioned quality proportioning, use pulverizer to pulverize Eliquis, cross 100 mesh sieves;
Step 2: mix: according to above-mentioned quality proportioning take Eliquis, Hydroxypropyl methylcellulose is put into three-dimensional mixer and is mixed 30 minutes, makes medicine segmentation, takes out for subsequent use;
Step 3: granulate: the supplementary material fine powder having mixed is put into wet granulator, and adhesive is put into feed tank, open machine, adjust parameter, start to add wetting agent, open simultaneously and shear fly cutter, 2-5 minute, discharging; Use oscillating granulator, with 20 order nylon screens granulations; Rear use fluid bed dryer is dried, first dry with cool breeze, after epidermis parches, opens Hot-blast Heating, and EAT, at 50-55 degree Celsius, uses the whole grain of the swing collator of 18 order nylon screen after drying, for subsequent use.
Step 4: always mixed: by the particle making, put into three-dimension type mixer, and add the lubricant of recipe quantity, always mixed 30 minutes, discharging was for subsequent use.
Step 5: compressing tablet: use 35 to rush high-speed rotary tablet press machine compressing tablet.
Step 6: plastic-aluminum: above-mentioned plain sheet is used to aluminium-plastic bubble plate packing machine, be packaged into aluminium-plastic panel, packed products.
In described step 3: granulation mode is replaceable is: the supplementary material fine powder mixing is put into fluidised bed granulator, adhesive is put into feed tank, open machine, adjust parameter, after goods fluid is in good condition, open spraying, adjust EAT, liquid supply speed, air inducing frequency, atomizing pressure, Real Time Observation stops spraying after granular size is moderate; Open Hot-blast Heating, EAT, at 50-55 degree Celsius, uses the whole grain of the swing collator of 18 order nylon screen after drying, for subsequent use.
Beneficial effect of the present invention: the sustained release pellet taking Eliquis as active ingredient of the present invention, the main thrombus prevention with being applicable to accept buttocks or knee replacement patient with operation. The more novel sustained release preparation and the pellet preparations that adopt, slowly-releasing refers to by delaying the rate of releasing drug of medicine from this formulation, reduces medicine and enters the absorption rate of body, thereby play more stable result for the treatment of; Micropill has medicine and increases at intestines and stomach surface distributed area, can reduce excitant, improves bioavilability, not affected by gastric emptying factor simultaneously, uniform absorption in medicine body, and individual difference is little; Two kinds of advanced technology are applied the technical advantage that has more strengthened this medicine simultaneously. Compared with oral liquid, there is medicine stability good, packaging, transport, preserves the advantages such as convenient, and its preparation method is simple, is applicable to industrial production.
The present invention is through two groups of clinical verifications, and wherein one group is that treatment group is used the present invention, and used once every day, within 7 days, be a course for the treatment of, another group contrast is used existing Eliquis controlled release tablet, every group selection outpatient 100 examples, wherein male 60 examples, female's 40 examples, measure 70 years old large age, minimal ages 30 years old, used once every day, within 7 days, is a course for the treatment of, clinical manifestation is that blood is thick, and artery sclerosis, through gangue, thrombus, table one is for taking a contrasting data after the course for the treatment of:
Table 1 is taken two groups of comparisons course for the treatment of in front and back (unit: people)
There were significant differences for treatment group and control group, thereby can find out that the present invention's application clinically has significant curative effect.
Process characteristic of the present invention: 1, select raw material science, production technology advanced person, its product is conveniently deposited and is used; 2, product Chinese traditional medicine composition is easily absorbed by the body; 3, raw material sources are extensive, add technique circuit short, the easy processing and manufacturing of product.
Detailed description of the invention:
Embodiment 1
A kind of Eliquis sustained release tablets, is characterized in that: be to be made up of the raw material of following weight: 5mg Eliquis, 50-95mg Hydroxypropyl methylcellulose, 3-20mg lubricant.
In described raw material, preferred weight proportion is: 5mg Eliquis, 93mg Hydroxypropyl methylcellulose, 5mg lubricant.
Described Hydroxypropyl methylcellulose can be one or both compositions of following model: 75hd100cr Hydroxypropyl methylcellulose, 75hd4000cr Hydroxypropyl methylcellulose, 75hd15000cr Hydroxypropyl methylcellulose, 100000cr Hydroxypropyl methylcellulose.
Described lubricant is one or both in dolomol, talcum powder, silica.
Its preparation method comprises following operation:
Step 1: get the raw materials ready: by above-mentioned quality proportioning, use pulverizer to pulverize Eliquis, cross 100 mesh sieves;
Step 2: mix: according to above-mentioned quality proportioning take Eliquis, Hydroxypropyl methylcellulose is put into three-dimensional mixer and is mixed 30 minutes, makes medicine segmentation, takes out for subsequent use;
Step 3: granulate: the supplementary material fine powder having mixed is put into wet granulator, and adhesive is put into feed tank, open machine, adjust parameter, start to add wetting agent, open simultaneously and shear fly cutter, 2-5 minute, discharging; Use oscillating granulator, with 20 order nylon screens granulations; Rear use fluid bed dryer is dried, first dry with cool breeze, after epidermis parches, opens Hot-blast Heating, and EAT, at 50-55 degree Celsius, uses the whole grain of the swing collator of 18 order nylon screen after drying, for subsequent use.
Step 4: always mixed: by the particle making, put into three-dimension type mixer, and add the lubricant of recipe quantity, always mixed 30 minutes, discharging was for subsequent use.
Step 5: compressing tablet: use 35 to rush high-speed rotary tablet press machine compressing tablet.
Step 6: plastic-aluminum: above-mentioned plain sheet is used to aluminium-plastic bubble plate packing machine, be packaged into aluminium-plastic panel, packed products.
In described step 3: granulation mode is replaceable is: the supplementary material fine powder mixing is put into fluidised bed granulator, adhesive is put into feed tank, open machine, adjust parameter, after goods fluid is in good condition, open spraying, adjust EAT, liquid supply speed, air inducing frequency, atomizing pressure, Real Time Observation stops spraying after granular size is moderate; Open Hot-blast Heating, EAT, at 50-55 degree Celsius, uses the whole grain of the swing collator of 18 order nylon screen after drying, for subsequent use.
Claims (9)
1. an Eliquis sustained release tablets, is characterized in that: be to be made up of the raw material of following weight: 5mg Eliquis, 50-95mg Hydroxypropyl methylcellulose, 3-20mg lubricant.
2. a kind of Eliquis sustained release tablets according to claim 1, is characterized in that: in described raw material, preferred weight proportion is: 5mg Eliquis, 93mg Hydroxypropyl methylcellulose, 5mg lubricant.
3. a kind of Eliquis sustained release tablets according to claim 1, is characterized in that: described Hydroxypropyl methylcellulose can be one or both compositions of following model: 75hd100cr Hydroxypropyl methylcellulose, 75hd4000cr Hydroxypropyl methylcellulose, 75hd15000cr Hydroxypropyl methylcellulose, 100000cr Hydroxypropyl methylcellulose.
4. according to a kind of Eliquis sustained release tablets described in claim 1-2, it is characterized in that: described lubricant is one or both in dolomol, talcum powder, silica.
5. according to the preparation method of a kind of Eliquis sustained release tablets described in claim 1-2, it is characterized in that: comprise following operation:
Step 1: get the raw materials ready: by above-mentioned quality proportioning, use pulverizer to pulverize Eliquis, cross 100 mesh sieves;
Step 2: mix: according to above-mentioned quality proportioning take Eliquis, Hydroxypropyl methylcellulose is put into three-dimensional mixer and is mixed 30 minutes, makes medicine segmentation, takes out for subsequent use;
Step 3: granulate: the supplementary material fine powder having mixed is put into wet granulator, and adhesive is put into feed tank, open machine, adjust parameter, start to add wetting agent, open simultaneously and shear fly cutter, 2-5 minute, discharging; Use oscillating granulator, with 20 order nylon screens granulations; Rear use fluid bed dryer is dried, first dry with cool breeze, after epidermis parches, opens Hot-blast Heating, and EAT, at 50-55 degree Celsius, uses the whole grain of the swing collator of 18 order nylon screen after drying, for subsequent use.
6. step 4: always mixed: by the particle making, put into three-dimension type mixer, and add the lubricant of recipe quantity, always mixed 30 minutes, discharging was for subsequent use.
7. step 5: compressing tablet: use 35 to rush high-speed rotary tablet press machine compressing tablet.
8. step 6: plastic-aluminum: above-mentioned plain sheet is used to aluminium-plastic bubble plate packing machine, be packaged into aluminium-plastic panel, packed products.
9. the preparation method of a kind of Eliquis sustained release tablets according to claim 5, it is characterized in that: in described step 3: granulation mode is replaceable is: the supplementary material fine powder mixing is put into fluidised bed granulator, adhesive is put into feed tank, open machine, adjust parameter, after goods fluid is in good condition, open spraying, adjust EAT, liquid supply speed, air inducing frequency, atomizing pressure, Real Time Observation stops spraying after granular size is moderate; Open Hot-blast Heating, EAT, at 50-55 degree Celsius, uses the whole grain of the swing collator of 18 order nylon screen after drying, for subsequent use.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410671958.3A CN105596309A (en) | 2014-11-22 | 2014-11-22 | Apixaban sustained-release tablet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410671958.3A CN105596309A (en) | 2014-11-22 | 2014-11-22 | Apixaban sustained-release tablet and preparation method thereof |
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| Publication Number | Publication Date |
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| CN105596309A true CN105596309A (en) | 2016-05-25 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410671958.3A Pending CN105596309A (en) | 2014-11-22 | 2014-11-22 | Apixaban sustained-release tablet and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109793715A (en) * | 2019-03-15 | 2019-05-24 | 南京卡文迪许生物工程技术有限公司 | A kind of Eliquis oral solid formulation and preparation method thereof |
| CN110302167A (en) * | 2019-06-27 | 2019-10-08 | 慧生医学科技(徐州)有限公司 | A kind of Eliquis sustained release tablets and preparation method thereof |
-
2014
- 2014-11-22 CN CN201410671958.3A patent/CN105596309A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109793715A (en) * | 2019-03-15 | 2019-05-24 | 南京卡文迪许生物工程技术有限公司 | A kind of Eliquis oral solid formulation and preparation method thereof |
| CN109793715B (en) * | 2019-03-15 | 2022-02-15 | 南京卡文迪许生物工程技术有限公司 | Apixaban oral solid preparation and preparation method thereof |
| CN110302167A (en) * | 2019-06-27 | 2019-10-08 | 慧生医学科技(徐州)有限公司 | A kind of Eliquis sustained release tablets and preparation method thereof |
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Application publication date: 20160525 |