CN105920000B - Nifedipine sustained-release preparation and preparation method thereof - Google Patents
Nifedipine sustained-release preparation and preparation method thereof Download PDFInfo
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
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- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
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- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
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- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
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Abstract
The invention discloses a kind of Nifedipine sustained-release preparations and preparation method thereof.The Nifedipine sustained-release preparation is prepared by Nifedipine Sustained-release Beads and pharmaceutically acceptable auxiliary material；The Nifedipine Sustained-release Beads include pastille slow-release capsule core and drug containing release layer, and the drug containing release layer, through fluidized bed for spraying, is wrapped in the outer layer of the pastille slow-release capsule core by nifedipine aqueous dispersion.Nifedipine sustained-release preparation of the present invention has ideal drug release feature, and preparation process is simple, efficient.
Description
Technical field
The present invention relates to a kind of medicament slow release preparations and preparation method thereof, more particularly to a kind of Nifedipine sustained-release preparation
And preparation method thereof.
Background technology
Nifedipine is dihydropyridine calcium ion channel antagonist, has very strong coronary artery dilator and peripheral arterial
Effect, inhibit vasopasm significant effect, be the choice drug of variant angina pectoris, be clinically widely used in treating high blood
Pressure and prevention angina pectoris.Its mechanism of action is mainly the Ca2+ influx by selective depression myocardial cell membrane, blocks cardiac muscle cell
Excitement-contraction coupling weakens myocardial contractive power, the consumption of cardiac energy and oxygen is reduced, by preventing calcium overload from directly protecting
Cardiac muscle cell.
But regrettably, there are still shortcomings during clinical application and formulation development for nifedipine, specific as follows：
A. nifedipine is short-acting calcium antagonist, and efficacy time is short, needs frequent drug administration；Unstable, the blood of ordinary preparation drug release
Concentration fluctuation is big, is susceptible to reflectivity increased heart rate, activation stomodaeal nervous system, is unfavorable for myocardial ischemia and heart failure
The adverse reactions such as the control exhausted.
B. nifedipine is insoluble in water, needs that release retarding agent is added in sustained release preparation preparation process, it is thus possible to cause
Drug is slow in release early period, is unable to quick acting and plays therapeutic effect.
C. existing nifedipine two-phase medicine-releasing system or controlled release system, although comparatively ideal drug release effect can be obtained,
Also there is the shortcomings of high complex process, manufacturing cost, low production efficiency.
Invention content
Based on this, the object of the present invention is to provide a kind of Nifedipine sustained-release preparations, have ideal drug release special
Property, and preparation process is simple, efficient.
It is a further object of the invention to provide the preparation methods of the Nifedipine sustained-release preparation.
A kind of Nifedipine Sustained-release Beads comprising pastille slow-release capsule core and drug containing release layer；The drug containing release layer
By nifedipine aqueous dispersion through fluidized bed for spraying, it is wrapped in the outer layer of the pastille slow-release capsule core.
The nifedipine aqueous dispersion includes by weight percentage in one of the embodiments,：Nifedipine is micro-
3 parts of powder, 9~15 parts of povidone, 1~2 part of lauryl sodium sulfate, 3~5 parts of hydroxypropyl methylcellulose, 0.5~1 part of talcum powder
With 100 parts of water.
The pastille slow-release capsule core includes by weight percentage in one of the embodiments,：It is 17 parts of nifedipine, micro-
50~60 parts of crystalline cellulose, 50~60 parts of lactose and 40~50 parts of framework material of sustained release.
The sustained-release matrix material is by hypotonicity acrylic copolymer aqueous dispersion in one of the embodiments,
(acrylic copolymer RS30D) is formed with high osmosis acrylic copolymer aqueous dispersion (acrylic copolymer RL30D).
The hypotonicity acrylic copolymer aqueous dispersion is ethyl acrylate, first in one of the embodiments,
Base methyl acrylate and methacrylic acid trimethyl ammonium chloride base ethyl ester in mass ratio 1:2:The aqueous copolymer dispersion of 0.1 composition,
Its mass concentration is 30%；The high osmosis acrylic copolymer aqueous dispersion is ethyl acrylate, methyl methacrylate
Ester and methacrylic acid trimethyl ammonium chloride base ethyl ester in mass ratio 1:2:The aqueous copolymer dispersion of 0.2 composition, mass concentration
It is 30%.
In one of the embodiments, the hypotonicity acrylic copolymer aqueous dispersion in the sustained-release matrix material with
The mass ratio of high osmosis acrylic copolymer aqueous dispersion is 9:1.
A kind of Nifedipine sustained-release preparation, by Nifedipine Sustained-release Beads of the present invention with it is pharmaceutically acceptable
Auxiliary material is prepared.
A kind of Nifedipine slow release tablet, by Nifedipine Sustained-release Beads of the present invention and disintegrant, glidant,
Lubricant is prepared through tabletting.
The Nifedipine slow release tablet in one of the embodiments, by Nifedipine sustained-release of the present invention
100 parts of pellet and 4~8 parts of disintegrant, 0.5~1 part of glidant, 0.5~1 part of lubricant, are prepared through tabletting.
The disintegrant can be selected from crosslinked polyvinylpyrrolidone in one of the embodiments, carboxymethyl starch is received,
Low-substituted hydroxypropyl cellulose or croscarmellose sodium；The glidant can be selected from silica or gas phase micro mist silicon
Glue；The lubricant can be selected from stearic acid, magnesium stearate, calcium stearate, talcum powder or Compritol 888 ATO.
The preparation method of Nifedipine Sustained-release Beads of the present invention, includes the following steps：
1) preparation of nifedipine aqueous dispersion：Take nifedipine bulk pharmaceutical chemicals to carry out micronization processes, size controlling 1~
5μm；Povidone, lauryl sodium sulfate, hydroxypropyl methylcellulose are added to the water, stirring and dissolving, and micro mist is added under stiring
The nifedipine and talcum powder of change continue stirring and form it into uniform aqueous suspension；
2) preparation of pastille slow-release capsule core：Nifedipine, microcrystalline cellulose and lactose are taken, is used as substrate after mixing,
It takes sustained-release matrix material as adhesive, whitewashing granulation is carried out using fluid bed, is dried after whitewashing；
3) preparation of Nifedipine Sustained-release Beads：Pastille slow-release capsule core obtained is taken, continues to use fluidized bed for spraying, will make
The nifedipine aqueous dispersion obtained is uniformly sprayed at the surface of pastille slow-release capsule core, is dried, whole grain, obtains after whitewashing
The Nifedipine Sustained-release Beads.
In one of the embodiments, in step 3), the nifedipine aqueous dispersion is uniform under stirring
It is sprayed at the surface of pastille slow-release capsule core；The spray press control of the fluidized bed for spraying is in 0.1~0.2MPa.
The preparation method of Nifedipine slow release tablet of the present invention, includes the following steps：Take nitre produced by the present invention
Benzene Horizon sustained release pellet, addition disintegrant, glidant and mix lubricant are uniform, then carry out tabletting, obtain the nitre benzene
Horizon sustained-release tablet.
Nifedipine Sustained-release Beads of the present invention have ideal drug release feature, and stability is good.Before drug release
The drug containing release layer of phase, pellet surface are rapidly dissolvable and reach effective blood concentration；In the drug release middle and later periods, drug can pass through
The corrosion slow release of diffusion and skeleton, to maintain stable blood concentration, to can more meet facing for hypertensive patient
Bed demand.In addition, Nifedipine Sustained-release Beads of the present invention, are prepared using one-step palletizing technique, preparation process letter
It is single, efficient.
The drug containing release layer of Nifedipine Sustained-release Beads of the present invention, be by the aqueous dispersion of micronizing nifedipine,
It is prepared through fluidized bed for spraying package pastille slow-release capsule core.Since nifedipine is multi-crystalline compounds, and it is insoluble in water, passed
Crystal phenomenon is easy to happen using organic solvent dissolving in system technique, influences the stability of drug.The present invention is by nitre benzene
It is flat to carry out micronization processes, and povidone and dodecyl sulphate are added in aqueous solution, the water-soluble of nifedipine can be improved
Property, nifedipine is effectively dispersed in the surface of sustained release capsule core, can avoid nifedipine that crystal phenomenon occurs, is improved
Medicine stability, and ensure that the drug of release layer being capable of Fast Stripping.In addition, by the way that hypromellose is added in aqueous solution
Element can avoid nifedipine from being precipitated during fluidized bed for spraying is coated；And by the way that talcum powder is added, it can avoid
There is a phenomenon where pellets to be adhered during fluidized bed for spraying is coated.
The pastille slow-release capsule core of Nifedipine Sustained-release Beads of the present invention, using microcrystalline cellulose and lactose as capsule core
Excipient be conducive to fluidized bed granulation with good mobility and mouldability, and can assign the good intensity of capsule core and
Porosity is conducive to the package absorption of drug containing release layer.And use hypotonicity acrylic copolymer aqueous dispersion and Thief zone
Property acrylic copolymer aqueous dispersion combines the sustained-release matrix material to be formed, can to the drug dissolution of pastille slow-release capsule core into
The predictable adjusting of row, to reach the stripping curve of target, moreover it is possible to which there is a phenomenon where pellets to bond when tabletting being avoided to make tablet
And it is unable to reach quick-release effect.
In Nifedipine slow release tablet of the present invention, preferably crosslinked polyvinylpyrrolidone etc. is used as disintegrant, energy
Enough ensure that tablet can be disintegrated into rapidly sustained release pellet in the solution, pellet is completed the drug release process being sustained after first quick-release, had good
Good drug release effect；It is preferred that silica or gas phase superfine silica gel powder be as glidant, by being attached to pellet surface, Neng Gougai
The surface nature of kind pellet particle, reduces the friction between pellet particle, avoids generating electrostatic；It is preferred that magnesium stearate etc. is as profit
Lubrication prescription can increase the mobility of pellet particle, reduce the frictional force between pellet particle and tableting die, ensure tablet surface
It is bright and clean.
The preparation method of Nifedipine Sustained-release Beads of the present invention, in step 3), the spray of the fluidized bed for spraying
Mist pressure is controlled in 0.1~0.2Mpa.If atomisation pressure is excessive, the drop that nifedipine aqueous dispersion is formed is too small, is fluidizing
It is easy rapid drying under the hot environment of bed whitewashing, can not be attached in capsule core；If atomisation pressure is too small, nifedipine is water-dispersed
Body be attached to after capsule core can not efficient drying, be easy to cause pellet adhesion.
Description of the drawings
Fig. 1 is the drug release profiles of Nifedipine slow release tablet in aqueous solution；
Fig. 2 is drug release profiles of the Nifedipine slow release tablet at pH 1.2；
Fig. 3 is drug release profiles of the Nifedipine slow release tablet at pH 4.0；
Fig. 4 is drug release profiles of the Nifedipine slow release tablet at pH 6.8.
Specific implementation mode
Embodiment one：The preparation of Nifedipine Sustained-release Beads
1, the preparation of nifedipine aqueous dispersion：
Each component is weighed respectively according to formula as below：
Nifedipine bulk pharmaceutical chemicals are subjected to micronization processes, size controlling is at 1~5 μm；By povidone, dodecyl sulphate
Sodium, hydroxypropyl methylcellulose are added to the water, stirring and dissolving, and the nifedipine and talcum powder of micronizing are added under stiring, continue
Stirring forms it into uniform aqueous suspension.
2, the preparation of pastille slow-release capsule core：
Each component is weighed respectively according to formula as below：
Take nifedipine, microcrystalline cellulose and lactose, be used as substrate after mixing, with acrylic copolymer RS30D and
The mixed liquor of acrylic copolymer RL30D is adhesive, carries out whitewashing granulation using fluid bed, is dried after whitewashing,
Obtain pastille slow-release capsule core.
3, the preparation of Nifedipine Sustained-release Beads：
Pastille slow-release capsule core obtained is taken, continues to use fluidized bed for spraying, nifedipine aqueous dispersion obtained is uniform
It is sprayed at the surface of pastille slow-release capsule core, is dried to pellet moisture after whitewashing and is less than 3%, then crossed 22 mesh sieves, obtain
To Nifedipine Sustained-release Beads.
Embodiment two：The preparation of Nifedipine slow release tablet
Each component is weighed respectively according to formula as below：
Crosslinked polyvinylpyrrolidone, silica and hard is added in Nifedipine Sustained-release Beads made from Example one
Fatty acid magnesium is uniformly mixed, and then carries out tabletting to get to Nifedipine slow release tablet.
Embodiment three：The drug release feature of Nifedipine slow release tablet is tested
1, chromatographic condition：
Mobile phase：0.1% phosphoric acid ﹣ methanol ﹣ acetonitriles (40:30:30)；Flow velocity：1.0mL/min；Chromatographic column：Octadecyl silicon
Alkane bonded silica gel chromatographic column (C18Column)；Sample size：20μL；Detection wavelength：235nm.
2, drug release determination method：It is protected from light operation
4 parts of Nifedipine slow release tablet made from Example two respectively, 6 every part, according to drug release determination method (China
2010 editions two annex X D of pharmacopeia) the first method, using dissolution method (two annex X C of Chinese Pharmacopoeia version in 2010)
The device of two methods (paddle method), respectively with the water of 900mL, the acetate buffer solution and pH6.8 of the hydrochloric acid solution of pH1.2, pH4.0
Phosphate buffer solution be dissolution medium (contain 0.3% Tween 80), rotating speed 75r/min is operated, is existed respectively in accordance with the law
0.25h, 0.5h, 1h, 2h, 4h, 6h, 8h, 12h take solution 10mL, filtering, discard primary filtrate 5mL, and supplement phase equality of temperature immediately
The dissolution medium of degree, same volume, takes subsequent filtrate as test solution.Nifedipine reference substance 10mg separately is taken, is placed in 50mL
In volumetric flask, add proper amount of methanol ultrasonic dissolution, then plus methanol dilution is to scale, shakes up, 3mL is taken to be placed in 4 100mL amounts respectively
In bottle, it is separately added into the phosphate buffer solution of water, the hydrochloric acid solution of pH1.2, the acetate buffer solution of pH4.0 and pH6.8,
It quantifies to scale, shakes up, as a contrast product solution.It is accurate respectively to measure test solution and each 20 μ L of reference substance solution, injection
Liquid chromatograph records its chromatogram respectively, and each sample group is calculated separately in the accumulative of different time with peak area by external standard method
Burst size, measurement result are as shown in Figures 1 to 4.
The experimental results showed that Nifedipine slow release tablet produced by the present invention has consistent body with nifedipine reference substance
Outer drug release feature.
Each technical characteristic of embodiment described above can be combined arbitrarily, to keep description succinct, not to above-mentioned reality
It applies all possible combination of each technical characteristic in example to be all described, as long as however, the combination of these technical characteristics is not deposited
In contradiction, it is all considered to be the range of this specification record.
Several embodiments of the invention above described embodiment only expresses, the description thereof is more specific and detailed, but simultaneously
It cannot therefore be construed as limiting the scope of the patent.It should be pointed out that coming for those of ordinary skill in the art
It says, without departing from the inventive concept of the premise, various modifications and improvements can be made, these belong to the protection of the present invention
Range.Therefore, the protection domain of patent of the present invention should be determined by the appended claims.
Claims (8)
1. a kind of Nifedipine Sustained-release Beads, which is characterized in that including pastille slow-release capsule core and drug containing release layer；Described contains
Medicine release layer, through fluidized bed for spraying, is wrapped in the outer layer of the pastille slow-release capsule core by nifedipine aqueous dispersion；
The nifedipine aqueous dispersion includes by weight percentage：3 parts of nifedipine powder body, 9~15 parts of povidone, ten
100 parts of 1~2 part of sodium dialkyl sulfate, 3~5 parts of hydroxypropyl methylcellulose, 0.5~1 part of talcum powder and water；
The pastille slow-release capsule core includes by weight percentage：17 parts of nifedipine, 50~60 parts of microcrystalline cellulose, lactose 50
~60 parts and 40~50 parts of framework material of sustained release.
2. Nifedipine Sustained-release Beads according to claim 1, which is characterized in that the sustained-release matrix material is by hypotonic
Permeability acrylic copolymer aqueous dispersion is formed with high osmosis acrylic copolymer aqueous dispersion.
3. Nifedipine Sustained-release Beads according to claim 2, which is characterized in that the hypotonicity acrylic acid copolymer
Object aqueous dispersion is ethyl acrylate, methyl methacrylate and methacrylic acid trimethyl ammonium chloride base ethyl ester in mass ratio 1:2:
The aqueous copolymer dispersion of 0.1 composition；The high osmosis acrylic copolymer aqueous dispersion is ethyl acrylate, methyl-prop
E pioic acid methyl ester and methacrylic acid trimethyl ammonium chloride base ethyl ester in mass ratio 1:2:The aqueous copolymer dispersion of 0.2 composition.
4. Nifedipine Sustained-release Beads according to claim 2, which is characterized in that hypotonic in the sustained-release matrix material
The mass ratio of permeability acrylic copolymer aqueous dispersion and high osmosis acrylic copolymer aqueous dispersion is 9:1.
5. a kind of Nifedipine sustained-release preparation, which is characterized in that by Nifedipine Sustained-release Beads described in claim 1 and pharmacy
Upper acceptable auxiliary material is prepared.
6. a kind of Nifedipine slow release tablet, which is characterized in that by Nifedipine Sustained-release Beads described in claim 1 and disintegration
Agent, glidant, lubricant, are prepared through tabletting.
7. Nifedipine slow release tablet according to claim 6, which is characterized in that the optional self-crosslinking of the disintegrant is poly-
Vinylpyrrolidone, carboxymethyl starch receive, low-substituted hydroxypropyl cellulose or croscarmellose sodium；The glidant
It can be selected from silica or gas phase superfine silica gel powder；The lubricant can be selected from stearic acid, magnesium stearate, calcium stearate, talcum
Powder or Compritol 888 ATO.
8. a kind of preparation method of Nifedipine Sustained-release Beads, includes the following steps：
1) preparation of nifedipine aqueous dispersion：Nifedipine bulk pharmaceutical chemicals are taken to carry out micronization processes, size controlling is at 1~5 μm；
Povidone, lauryl sodium sulfate, hydroxypropyl methylcellulose are added to the water, stirring and dissolving, and micronizing is added under stiring
Nifedipine and talcum powder continue stirring and form it into uniform aqueous suspension；
2) preparation of pastille slow-release capsule core：Nifedipine, microcrystalline cellulose and lactose are taken, substrate is used as after mixing, takes slow
Framework material is released as adhesive, whitewashing granulation is carried out using fluid bed, is dried after whitewashing；
3) preparation of Nifedipine Sustained-release Beads：Pastille slow-release capsule core obtained is taken, continues to use fluidized bed for spraying, it will be obtained
Nifedipine aqueous dispersion is uniformly sprayed at the surface of pastille slow-release capsule core, is dried after whitewashing, whole grain, obtains described
Nifedipine Sustained-release Beads.
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| CN109172534B (en) * | 2018-10-23 | 2020-08-07 | 迪沙药业集团有限公司 | Nifedipine sustained-release tablet composition |
| CN111643473B (en) * | 2020-07-28 | 2022-05-27 | 华润双鹤利民药业（济南）有限公司 | Nifedipine sustained release tablet and preparation method thereof |
| CN111643468B (en) * | 2020-07-28 | 2022-05-10 | 华润双鹤利民药业（济南）有限公司 | Nifedipine sustained release preparation and preparation thereof |
| CN117084992B (en) * | 2023-10-19 | 2023-12-26 | 华润双鹤利民药业（济南）有限公司 | Nifedipine controlled release tablet preparation and preparation method thereof |
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| CN105920000A (en) | 2016-09-07 |
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