CN101721380A - Method for preparing sustained-release preparation - Google Patents
Method for preparing sustained-release preparation Download PDFInfo
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- CN101721380A CN101721380A CN200810218419A CN200810218419A CN101721380A CN 101721380 A CN101721380 A CN 101721380A CN 200810218419 A CN200810218419 A CN 200810218419A CN 200810218419 A CN200810218419 A CN 200810218419A CN 101721380 A CN101721380 A CN 101721380A
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Abstract
The invention discloses a method for preparing sustained-release preparation, which comprises the steps of: step 1, according to the mass percent of 1:0.1-100, mixing raw material with bioactivity and ethyl vitamin, PEGs or HPMCs, and preparing solution or mixed suspension liquid for standby application; step 2, preparing the needed granules or pellets for standby application in advance; and step 3, according to the mass percent of 1:1-20, spraying the liquid prepared in the step 1 into the granules or pellets prepared in the step 2 to be mixed together, and tabletting or filling into capsules. The preparation method overcomes the defects of complexity and hard industrialization of the original technique, and is simple in technique and easy to control; furthermore, the sustained-release preparation prepared by the method can obviously reduce the adverse reaction of medicine, enhances the compliance of patients and improves the clinical curative effect.
Description
Technical field
The invention belongs to medicament preparation method field, especially relate to a kind of method for preparing sustained-release preparation.
Background technology
Sustained-release preparation means the preparation that can continue to discharge medicine after the medication in a long time.Medicine in the sustained-release preparation slowly discharges and absorbs by suitable speed, and blood drug level " peak valley " fluctuation is less, can avoid surpassing the toxic and side effects of treatment blood drug level scope, can remain on the long period within the valid density scope to keep curative effect again.Compare with ordinary preparation, but sustained-release preparation extended treatment acting duration reduces toxic and side effects, reduces the medication number of times, makes things convenient for patient's medication, improves the compliance of medication.As far back as early 1970s, the research and development of slow release and controlled release preparation have just been begun abroad, so far the history in year surplus in the of existing 40.Advantages such as administration number of times is few, blood concentration fluctuation is less, route of administration is diversified, zest is little and curative effect lasting because such medicine has, safety more and more are subjected to clinical attention.Sustained-release and controlled release preparation research development in recent years is very rapid, and the trend that continues rising is arranged.With in the past regular dosage form such as tablet, capsule, injection relatively, the major advantage of slow release, controlled release preparation is 1. can reduce administration number of times, the compliance of improvement; 2. reduce the peak valley phenomenon of blood drug level, reduce toxic and side effects, improve curative effect; 3. increase the stability of Drug therapy.Overcome sustained-release preparation in addition and can also avoid some drugs, avoid the administration at night the gastrointestinal zest.Because these advantages, sustained-release preparation is called as the second filial generation and the third generation pharmaceutical preparation behind conventional formulation.Be with fastest developing speed, the new medicinal preparation that industrialization level is the highest.But the preparation method of existing slow release, controlled release preparation still has the following disadvantages: traditional sustained-release preparation preparation method, and its technological operation relative complex, the cost height, and wayward, restricted its suitability for industrialized production.
Summary of the invention
The object of the invention is to overcome the deficiency that above-mentioned prior art exists, and provide that a kind of technology is simple, cost is low, easy to control, can be suitable for the method for preparing sustained-release preparation of suitability for industrialized production.
The technical scheme that solves the problems of the technologies described above is:
A kind of method for preparing sustained-release preparation comprises the steps:
Step 1,1: 0.1 by mass percentage～100 ratio is mixed the raw material of biologically active and ethyl vitamin or PEG class or HPMC class, makes solution or suspension, and is standby;
Step 2 prepares required granule or piller in advance, and is standby;
Step 3,1: 1 by mass percentage～20 ratio, the liquid that above-mentioned steps one is made sprays in granule that step 2 makes or the piller and mixes, and compacting is in flakes or filling capsule.
The granule of above-mentioned steps two or piller can have two kinds of preferred versions, and a kind of is 1: 0.1 by mass percentage～100 ratio, and raw material and lactose, starch, dextrin, the cellulose family of biologically active is mixed and made into; Another kind is that granule or piller be matters of containing biological activities not.
Above-mentioned steps three can be 1: 1 by mass percentage～10 ratio, and the liquid that above-mentioned steps one is made sprays in granule that step 2 makes or the piller and mixes, and compacting in flakes or filling capsule.
As preferred scheme, above-mentioned steps one also needs to add entry or ethanol or isopropyl alcohol or propylene glycol or acetone after in proportion the raw material of biologically active and ethyl vitamin or PEG class or HPMC class being mixed, and makes needed solution or suspension; Therefore, when step 3,, the granule for preparing or piller sprayed into to add in solution that entry or ethanol or isopropyl alcohol or propylene glycol or acetone make or the suspension mix according to the ratio of mass percent 1: 1～20; As further improving; above-mentioned granule or piller spray into and add in solution that entry or ethanol or isopropyl alcohol or propylene glycol or acetone make or the suspension and be mixed in proportion; the mixture that adds magnesium stearate lubricant and/or Pulvis Talci and/or micropowder silica gel is again made granule; or piller, or oral administration solution, last; in blocks or the filling capsule of compacting; wherein, described lubricant can be a kind of in magnesium stearate, Pulvis Talci, the micropowder silica gel, or its mixture.
The above-mentioned method for preparing sustained-release preparation, described bioactive raw material can be a kind of of nifedipine, captopril, diclofenac sodium, ketoprofen, naproxen, tiopronin, aspirin, acetaminophen, methadone hydrochloride, pseudoephedrine hydrochloride, pseudoephedrine sulfate, caffeine, chlorphenamine maleate, potassium chloride, ambroxol hydrochloride, or multiple, or the compositions of slow controlled release component and other active ingredient.
Above-mentioned PEG class is a kind of in PEG4000～20000, or its combination; Described solution is water or ethanol or isopropyl alcohol or propylene glycol or acetone.
The preparation method of sustained-release preparation of the present invention, wherein the principal agent bearing capacity is the 1～500mg of each preparation unit.
In the beneficial effect of the present invention:
The preparation method of sustained-release preparation of the present invention, by adopting advanced film controlled release preparation technology, bioactive substance is made the granule that discharges by certain speed, and then compacting in flakes, capsule, piller, granule, oral administration solution, the sustained-release preparation of this method preparation is rapid-action, strong drug action, action time, prolongation and toxic and side effects were low, can obviously reduce the untoward reaction of medicine, increase patient's compliance, improve clinical efficacy; And the preparation method of sustained-release preparation of the present invention, it is simple to have a technological operation, and cost is low, is easy to control and the advantage that is easy to suitability for industrialized production.
The specific embodiment
The present invention utilizes the film control techniques; bioactive substance and ethyl vitamin or PEG class or HPMC class are mixed in proportion, are prepared into and discharge uniform hybrid particles or piller, more in flakes the granule compacting; or make granule, piller, oral administration solution, capsule, reach the slow release purpose.
Below be several concrete embodiments:
Embodiment 1:
The preparation method of the described sustained-release preparation of present embodiment, its preparation process is as follows:
At first,, and add entry or ethanol or isopropyl alcohol or propylene glycol or acetone, make solution or suspension bioactive substance and 1: 1 by mass percentage mixed of ethyl vitamin; Certainly, the ethyl vitamin can be by the PEG class, or the HPMC class replaces, bioactive raw material can be a nifedipine, captopril, diclofenac sodium, ketoprofen, naproxen, tiopronin, aspirin, acetaminophen, methadone hydrochloride, pseudoephedrine hydrochloride, pseudoephedrine sulfate, caffeine, chlorphenamine maleate, potassium chloride, ambroxol hydrochloride a kind of, or it is multiple, or the compositions of slow controlled release component and other active ingredient, and above-mentioned mass percent, can be according to different needs, proportion can be selected between 1: 0.1～100;
Secondly, bioactive substance is made granule or piller; Certainly, according to using needs, granule or piller also can be to be made by the material that does not contain active substance; During matters of containing biological activities, be 1: 0.1 by mass percentage～100 ratio, raw material and lactose, starch, dextrin, the cellulose family of biologically active is mixed and made into granule or piller;
At last, 1: 1 by mass percentage～20 ratio sprays into liquid in granule or the piller, adds or do not add lubricant, and compacting is in blocks, or filled capsules.Lubricant can be one or more a mixture in magnesium stearate, Pulvis Talci, the micropowder silica gel.Here need explanation, if make solution or suspension, do not add water or ethanol or isopropyl alcohol or propylene glycol or acetone, then 1: 1 by mass percentage～10 ratio sprays into liquid in granule or the piller.
Embodiment 2
Its implementation method is similar to embodiment 1, and difference is: at first, bioactive substance and ethyl vitamin in 1: 10 ratio and add entry or ethanol or isopropyl alcohol or propylene glycol or acetone, are made solution or suspension; Secondly, liquid is sprayed in the blank piller; At last, with above-mentioned piller filled capsules or make oral administration solution.
Embodiment 3
Its embodiment is also similar to embodiment 1, and difference is: at first, bioactive substance and ethyl vitamin in 1: 80 ratio and add entry or ethanol or isopropyl alcohol or propylene glycol or acetone, are made solution or suspension; Secondly, bioactive substance is made granule or piller, spray into aforesaid liquid; At last, granule or piller are mixed the granule or the piller of other active substance by different proportion, add or do not add lubricant and be in magnesium stearate, Pulvis Talci, the micropowder silica gel one or more mixture, compacting in flakes, or filled capsules.
Claims (10)
1. a method for preparing sustained-release preparation is characterized in that, comprises the steps:
Step 1,1: 0.1 by mass percentage～100 ratio is mixed the raw material of biologically active and ethyl vitamin or PEG class or HPMC class, makes solution or suspension, and is standby;
Step 2 prepares required granule or piller in advance, and is standby;
Step 3,1: 1 by mass percentage～20 ratio, the liquid that above-mentioned steps one is made sprays in granule that step 2 makes or the piller and mixes, and compacting is in flakes or filling capsule.
2. according to the described method for preparing sustained-release preparation of claim 1; it is characterized in that; the granule of above-mentioned steps two or piller are 1: 0.1 by mass percentage～100 ratios, and raw material and lactose, starch, dextrin, the cellulose family of biologically active is mixed and made into.
3. according to the described method for preparing sustained-release preparation of claim 1, it is characterized in that the granule of above-mentioned steps two or piller be matters of containing biological activities not.
4. according to the described method for preparing sustained-release preparation of claim 1; it is characterized in that above-mentioned steps three, 1: 1 by mass percentage～10 ratio; the liquid that above-mentioned steps one is made sprays in granule that step 2 makes or the piller and mixes, and compacting in flakes or filling capsule.
5. according to the right 1 described method for preparing sustained-release preparation, it is characterized in that, after above-mentioned steps one is mixed the raw material of biologically active and ethyl vitamin or PEG class or HPMC class in proportion, also need to add entry or ethanol or isopropyl alcohol or propylene glycol or acetone, make needed solution or suspension.
6. according to the right 5 described methods that prepare sustained-release preparation; it is characterized in that; above-mentionedly add solution or the suspension that entry or ethanol or isopropyl alcohol or propylene glycol or acetone are made; when step 3; according to the ratio of mass percent 1: 1～20, the granule for preparing or piller sprayed into to add in solution that entry or ethanol or isopropyl alcohol or propylene glycol or acetone make or the suspension mix.
7. according to the right 6 described methods that prepare sustained-release preparation; it is characterized in that; above-mentioned granule or piller spray into and add in solution that entry or ethanol or isopropyl alcohol or propylene glycol or acetone make or the suspension and be mixed in proportion; the mixture that adds magnesium stearate lubricant and/or Pulvis Talci and/or micropowder silica gel is again made granule; or piller; or oral administration solution, last, the in blocks or filling capsule of compacting.
8. according to the right 7 described methods that prepare sustained-release preparation, it is characterized in that described lubricant is a kind of in magnesium stearate, Pulvis Talci, the micropowder silica gel, or its mixture.
9. according to the right 1 described method for preparing sustained-release preparation, it is characterized in that, described bioactive raw material is a kind of of nifedipine, captopril, diclofenac sodium, ketoprofen, naproxen, tiopronin, aspirin, acetaminophen, methadone hydrochloride, pseudoephedrine hydrochloride, pseudoephedrine sulfate, caffeine, chlorphenamine maleate, potassium chloride, ambroxol hydrochloride, or multiple, or the compositions of slow controlled release component and other active ingredient.
10. according to the right 1 described method for preparing sustained-release preparation, it is characterized in that described PEG class is a kind of in PEG4000～20000, or its combination; Solution is water or ethanol or isopropyl alcohol or propylene glycol or acetone.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810218419A CN101721380A (en) | 2008-10-17 | 2008-10-17 | Method for preparing sustained-release preparation |
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| CN200810218419A CN101721380A (en) | 2008-10-17 | 2008-10-17 | Method for preparing sustained-release preparation |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102349915A (en) * | 2011-08-16 | 2012-02-15 | 石药集团中诺药业（石家庄）有限公司 | Acetaminophen, caffeine, chlorphenamine maleate, and vitamin C preparation and preparation method thereof |
| JP2012214465A (en) * | 2011-03-30 | 2012-11-08 | Kowa Co | Caffeine-containing liquid composition and capsule formulation filled with the composition |
| CN105267152A (en) * | 2015-11-12 | 2016-01-27 | 上海智同医药科技有限公司 | Controlled-release pellet preparation |
-
2008
- 2008-10-17 CN CN200810218419A patent/CN101721380A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2012214465A (en) * | 2011-03-30 | 2012-11-08 | Kowa Co | Caffeine-containing liquid composition and capsule formulation filled with the composition |
| CN102349915A (en) * | 2011-08-16 | 2012-02-15 | 石药集团中诺药业（石家庄）有限公司 | Acetaminophen, caffeine, chlorphenamine maleate, and vitamin C preparation and preparation method thereof |
| CN102349915B (en) * | 2011-08-16 | 2014-02-26 | 石药集团中诺药业（石家庄）有限公司 | Acetaminophen, caffeine, chlorphenamine maleate, and vitamin C preparation and preparation method thereof |
| CN105267152A (en) * | 2015-11-12 | 2016-01-27 | 上海智同医药科技有限公司 | Controlled-release pellet preparation |
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Application publication date: 20100609 |