CN108014089A - A kind of Montelukast Sodium enteric-coated pellet capsule of stabilization and preparation method thereof - Google Patents
A kind of Montelukast Sodium enteric-coated pellet capsule of stabilization and preparation method thereof Download PDFInfo
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- CN108014089A CN108014089A CN201711328786.XA CN201711328786A CN108014089A CN 108014089 A CN108014089 A CN 108014089A CN 201711328786 A CN201711328786 A CN 201711328786A CN 108014089 A CN108014089 A CN 108014089A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
- A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K31/47—Quinolines; Isoquinolines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
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Abstract
The present invention relates to technical field of medicine, Montelukast Sodium enteric-coated pellet capsule more particularly to a kind of stabilization and preparation method thereof, the enteric-coated pellet capsule is made of the coating of pellet core, separation layer and enteric layer from the inside to the outside, wherein, pellet core accounts for the 50 65% of enteric-coated pellet capsule, separation layer accounts for the 10 20% of enteric-coated pellet capsule, and enteric layer coating accounts for the 25 30% of enteric-coated pellet capsule；Wherein, pellet core is made of Montelukast Sodium, sodium carboxymethylcellulose, filler, disintegrant and basifier；Separation layer is made of retarding agent, adhesive, antiplastering aid and opacifier；Enteric layer coating is made of enteric high molecular material, plasticizer, antiplastering aid and opacifier；Enteric-coated pellet capsule provided by the present invention simplifies preparation process, reduces production cost, improves product quality and stability, security and clinical efficacy are more preferable, is worth of widely use.
Description
Technical field
The present invention relates to technical field of medicine, and in particular to a kind of Montelukast Sodium enteric-coated pellet capsule of stabilization and
Its preparation method.
Background technology
Pellet is a kind of spherical or spherical preparation of diameter in 0.5-1.5mm, can improve medicine and be contacted in intestines and stomach
Area, improves bioavilability；Can be needed that slow-release controlled-release and compound preparation is made according to clinic；Drug release is stablized, drug release rule tool
There is reappearance；Medicine conveys the influence of the food rhythm and pace of moving things from alimentary canal；Good appearance, good fluidity are non-breakable；The system of pellet
Standby technology mainly have rolling pelletization method, extrusion spheronization method, Centrifugal fluidized pellet method, melted high speed shear method, congealing spray,
Pill etc. in spray drying process and liquid medium.
Preparation method directly prepares pellet core using extrusion spheronization in the present invention, by using bottom to spray after fluidized bed drying
Bag barrier gown, then bag enteric layer, simplify operating procedure compared with existing process, shorten man-hour, improve product yield, avoid
The shortcomings that time-consuming by existing preparation process, yield is low, substantially increases production efficiency.
Montelukast Sodium is suitable for the prevention and long-term treatment of adult and childhood asthma, includes the heavy breathing at prevention daytime and night
Asthma shape, is treated to bronchoconstriction caused by the asthmatic patient of aspirin sensitive and prevention movement.
Enteric-coated pellet capsule, which has listed ordinary tablet, chewable tablets and granule, has following advantage：1. domestic ordinary tablet and
Particle discharged in stomach easily lead to drug degradation lose it is amount of activated, that is to say, that：What patient may take be one it is invalid or
The medicine of partial failure；It is multicomponent system and enteric-coated pellet capsule every is made of more than 100 small pellets, the mistake of indivedual pellets
By mistake or defect will not have an impact the drug release behavior of preparation entirety, therefore the stability of medicine is improved.2. conventional capsule,
Tablet disperse limited area, drug absorption is slower, and blood concentration easily fluctuates, and bioavilability is relatively low, and local mucous membrane stimulates
Also it is big；And enteric-coated pellet capsule is big in intestines and stomach disperse area, good absorbing, bioavilability is high, and blood concentration is steady, mucous membrane thorn
It is small to swash property.3. due to there is enteric coating outside each pellet, enteric-coated pellet capsule can whole grain swallow or also open glue
Capsule directly takes pellet, and the patient for being very suitable for children and dysphagia takes.4. enteric coatel tablets or common capsulae enterosolubilis, due to grain
Footpath is big, not easily passs through pylorus, is easily influenced by food rhythmicity；Pellet is since particle diameter is small, in the case of the closing of such as pylorus
It can continue, uniformly across pylorus, be influenced by food rhythmicity small.
This product in an acidic solution with it is unstable under illumination condition, it is degradable to produce a large amount of impurity, after oral absorption
Also degradation impurity is also easy to produce in gastric juice, reduces curative effect.Be conducive to improve this product quality stability after making enteric coated pellets formulation
And clinical efficacy.Patent " a kind of montelukast sodium enteric-coated pellet of stabilization " (CN201610916676.4, Jiangsu Alpha is reported
Medicine company) using Blank Pellets coating, upper drug-loaded layer (this technique drug loss is larger), separation layer and enteric layer；This product prepares work
Skill flow is pellet core (extrusion spheronization), bag separation layer and enteric layer, and technical process reduction, reduces production cost, and medicine
Thing almost free of losses, has reported patent to have more advantage.Separately the Montelukast Sodium figuration coated in patent in blank capsule core is reported
Agent neutralizes contains the povidone incompatible with main ingredient and copolyvidone auxiliary material respectively in separation layer, supplementary material compatibility experiments are found
This two kinds of auxiliary materials easily make main ingredient produce a large amount of degradation impurities and make main ingredient yellowish.Auxiliary material and Meng Lusi used in this product prescription
Special sodium compatibility is preferable, and pellet core is non-discolouring under high temperature, high humidity and illumination condition, improves product quality and stabilization
Property.
The content of the invention
For the enteric-coated pellet capsule that the prior art is provided there are the problem of, the present invention propose a kind of Meng Lu of stabilization
Special sodium enteric-coated pellet capsule of department and preparation method thereof.The present invention provides enteric-coated pellet capsule cost existing for enteric-coated pellet capsule
It is low, security is good, drug effect is notable.
In order to realize above-mentioned purpose, it is achieved by the following technical programs：
A kind of Montelukast Sodium enteric-coated pellet capsule of stabilization, the enteric-coated pellet capsule from the inside to the outside by pellet core, every
Absciss layer and enteric layer coating composition, wherein, the pellet core accounts for the 50-65% of enteric-coated pellet capsule, and the separation layer accounts for intestines
The 10-20% of molten micro pill capsule, the enteric layer coating account for the 25-30% of enteric-coated pellet capsule；
The pellet core is made of Montelukast Sodium, sodium carboxymethylcellulose, filler, disintegrant and basifier, institute
The weight ratio for stating Montelukast Sodium is 7-10%, and the weight ratio of the sodium carboxymethylcellulose is 2-8%, the weight of the filler
It is 60-70% to measure ratio, and the weight ratio of the disintegrant is 5-8%, and the weight ratio of the basifier is 10-15%；
Preferably, the filler is selected from mannitol or lactose；The disintegrant is selected from crospovidone or crosslinking carboxylic first
Base sodium cellulosate；The one kind or more of the basifier in natrium carbonicum calcinatum, disodium hydrogen phosphate, zinc oxide and sodium hydroxide
Kind；
The separation layer is made of retarding agent, adhesive, antiplastering aid and opacifier, and the weight ratio of the retarding agent is 20-
35%, the weight ratio of described adhesive is 50-65%, and the weight ratio of the antiplastering aid is 6-11%, the weight of the opacifier
Than for 2-5%；
Preferably, the retarding agent is selected from ethyl cellulose, and described adhesive is selected from hypromellose, described anti-stick
Agent is selected from talcum powder or superfine silica gel powder, and the opacifier is selected from titanium dioxide or iron oxide red；
The enteric layer coating is made of enteric high molecular material, plasticizer, antiplastering aid and opacifier, the enteric high score
The weight ratio of sub- material is 70-75%, and the weight ratio of the plasticizer is 5-7%, and the weight ratio of the antiplastering aid is 15-
20%th, the weight ratio of the opacifier is 2-5%；
Preferably, the enteric high molecular material is selected from hypromellose phthalate, and the plasticizer is selected from
One or more in triethyl citrate, glycerine, Macrogol 6000, the antiplastering aid is selected from talcum powder or monostearate is sweet
Grease, the opacifier are selected from titanium dioxide or iron oxide red；
The preparation method of the enteric-coated pellet capsule includes the following steps：
(1) preparation of pellet core
Sodium carboxymethylcellulose, filler, disintegrant and the basifier for crossing 80 mesh sieves, montelukast sodium raw materials are taken respectively
200 mesh sieves are crossed, puts in mixer and is uniformly mixed altogether, dry powder in wet mixing pelletizer is put and mixes, are added with wetting agent using spraying
The mode softwood of liquid, puts pill in extrusion spheronization pellet processing machine, and mesh size is 24 mesh, collects wet ball and puts fluid bed in a constant temperature
It is dry under the conditions of degree, collect the drying capsule core of certain mesh sieve；
(2) preparation of separation layer
Retarding agent, adhesive are weighed, the ethanol that appropriate concentration is 85% is added, stirs evenly, add until completely dissolved
Antiplastering aid and opacifier, add the ethanol that remaining concentration is 85%, after stirring evenly, 80 mesh sieves are crossed, up to isolation coat
Liquid, dry capsule core is put in fluid bed, opens power supply, adjusting parameter carries out bag barrier gown；
(3) preparation of enteric layer
Retarding agent, adhesive are weighed, the ethanol that appropriate concentration is 85% is added, stirs evenly, add until completely dissolved
Antiplastering aid and opacifier, add the ethanol that remaining concentration is 85%, after stirring evenly, 80 mesh sieves are crossed, up to isolation coat
Liquid, dry capsule core is put in fluid bed, opens power supply, adjusting parameter carries out bag barrier gown.
Preferably, enteric-coated pellet capsule composition is as follows：60% pellet core, 10% separation layer, 30% enteric layer.
Preferably, temperature is 50~60 DEG C in fluid bed in step (1).
Preferably, dry capsule core particle diameter is 20~30 mesh in step (1).
Preferably, when standing time is small more than or equal to 12 in step (3).
It is as follows using above-mentioned technical solution, beneficial effects of the present invention：
1st, be made enteric-coated micro-pill solve existing formulation (tablet, chewable tablets, granule etc.) it is unstable in gastric acid environment,
Degradable situation；
2nd, this product is shown in that light easily decomposes, which improves stability of the product under illumination condition；
3rd, the present invention directly prepares pellet core using extrusion spheronization method, by using spray bag isolation in bottom after fluidized bed drying
Clothing, then bag enteric layer, simplify operating procedure compared with existing process, shorten man-hour, improve product yield, avoid existing system
The shortcomings that time-consuming, yield is low for technique, substantially increases production efficiency；
4th, this product preparation process flow is pellet core (extrusion spheronization), bag separation layer and enteric layer, and technical process is reduced,
And medicine almost free of losses, report patent to have more advantage, be conducive to industrialized production.
Brief description of the drawings：
Fig. 1 dissolution and the HPLC contrasts of degraded situation in pH1.2 and pH6.8 media for ordinary tablet, granule and embodiment
Figure, wherein：
Scheme a and detect HPLC collection of illustrative plates in simulate the gastric juice (pH1.2) solubility for granule, degrade 20.203%, tR=8.536
For acid degradation product；
Scheme b and detect HPLC collection of illustrative plates in simulate the gastric juice (pH1.2) solubility for ordinary tablet, degrade 16.995%, tR=8.540
For acid degradation product；
Figure c is 1 attached drawing of embodiment, represents enteric-coated micro-pill and dissolves detection HPLC collection of illustrative plates, degraded in simulated intestinal fluid (pH6.8)
0.754% (light degradation, anacidity catabolite)；
Figure d is 2 attached drawing of embodiment, represents enteric-coated micro-pill and dissolves detection HPLC collection of illustrative plates, degraded in simulated intestinal fluid (pH6.8)
0.812% (light degradation, anacidity catabolite)；
Figure e is 3 attached drawing of embodiment, represents enteric-coated micro-pill and dissolves detection HPLC collection of illustrative plates, degraded in simulated intestinal fluid (pH6.8)
0.521% (light degradation, anacidity catabolite)；
Fig. 2 places related material detection HPLC contrasts in 7 days for ordinary tablet, granule and embodiment are exposed under illumination condition
Figure, wherein：
It is that ordinary tablet exposed related material for placing 7 days under illumination condition detects HPLC figures to scheme a；
It is that granule exposed related material for placing 7 days under illumination condition detects HPLC figures to scheme b；
Figure c is 1 attached drawing of embodiment, represents enteric-coated micro-pill exposed related material detection for placing 7 days under illumination condition
HPLC schemes；
Figure d is 2 attached drawing of embodiment, represents enteric-coated micro-pill exposed related material detection for placing 7 days under illumination condition
HPLC schemes；
Figure e is 3 attached drawing of embodiment, and enteric-coated micro-pill exposed related material detection HPLC for placing 7 days under illumination condition schemes；
Embodiment
To make the purpose, technical scheme and advantage of the embodiment of the present invention clearer, below in conjunction with the embodiment of the present invention,
Technical solution in the embodiment of the present invention is clearly and completely described.Based on the embodiment of the present invention, the common skill in this area
Art personnel all other embodiments obtained without creative efforts, belong to the model that the present invention protects
Enclose.
Embodiment 1：
| Pellet core | |
| Montelukast Sodium | 100g |
| Mannitol | 800g |
| Crospovidone | 80g |
| Sodium carboxymethylcellulose | 35g |
| Natrium carbonicum calcinatum | 180g |
| 50% ethanol solution (contains 0.1MNaOH) | 1L |
| Spacer layer coating | |
| Ethyl cellulose | 85g |
| Hydroxypropyl methylcellulose (E5) | 160g |
| Talcum powder | 25g |
| Titanium dioxide | 20g |
| 85% ethanol | 5L |
| Enteric layer is coated | |
| Hypromellose phthalate | 500g |
| Triethyl citrate | 45g |
| Talcum powder | 125g |
| Titanium dioxide | 20g |
| 85% ethanol | 8L |
The preparation method of the enteric-coated pellet capsule includes the following steps：
(1) preparation of pellet core
Take respectively and cross the auxiliary materials such as natrium carbonicum calcinatum, mannitol, crospovidone and the sodium carboxymethylcellulose of 80 mesh sieves,
Montelukast sodium raw materials cross 200 mesh sieves, put in mixer and are uniformly mixed altogether, put dry powder in wet mixing pelletizer and mix, use
The wetting agent stated softwood processed by the way of liquid feeding of spraying, puts pill in extrusion spheronization pellet processing machine, and sieve screen apertures are collected through being 24 mesh
Wet ball puts fluid bed in 50~60 DEG C of dryings, collects the drying capsule core between 20~30 mesh；
(2) preparation of separation layer
Ethyl cellulose and hydroxypropyl methylcellulose are weighed, the ethanol that appropriate concentration is 85% is added, stirs evenly, treat completely
Talcum powder and titanium dioxide are added after dissolving, adds the ethanol that remaining concentration is 85%, after stirring evenly, crosses 80 mesh sieves,
Up to isolation coat liquid, dry capsule core is put in fluid bed, opens power supply, adjusting parameter carries out bag barrier gown；
(3) preparation of enteric layer
Hypromellose phthalate is weighed to be dissolved in appropriate 85% ethanol, place 12 it is small when more than treat completely
After dissolving, triethyl citrate, talcum powder and titanium dioxide are added, then adds 85% ethanol after stirring evenly, to cross 80 to full dose
Mesh sieve, up to enteric coating liquid, the base ball for wrapping barrier gown is put in fluid bed or coating pan, open power supply, adjusting parameter into
Row is enteric coated.
Embodiment 2：
Preparation method is the same as embodiment 1.
Embodiment 3：
| Pellet core | |
| Montelukast Sodium | 100g |
| Lactose | 790g |
| Crospovidone | 85g |
| Sodium carboxymethylcellulose | 30g |
| Natrium carbonicum calcinatum | 175g |
| 50% ethanol solution (contains 0.1MNaOH) | 1L |
| Spacer layer coating | |
| Methylcellulose | 90g |
| Hydroxypropyl methylcellulose (E5) | 150g |
| Superfine silica gel powder | 30g |
| Iron oxide red | 10g |
| 85% ethanol | 5L |
| Enteric layer is coated | |
| Hypromellose phthalate | 510g |
| Macrogol 6000 | 40g |
| Talcum powder | 130g |
| Titanium dioxide | 20g |
| 85% ethanol | 8L |
Preparation method is the same as embodiment 1.
1st, the related check data of enteric-coated pellet capsule
As can be seen from the above table, the Montelukast Sodium enteric-coated pellet capsule indices obtained by the present invention meet rule
It is fixed.
2nd, study on the stability
The montelukast sodium enteric-coated pellet of the present embodiment one~tri- is calculated into loading amount by intermediates content, is used after encapsulated
Aluminium-plastic sealing is packed, and in 40 DEG C ± 2 DEG C of high temperature, carries out accelerating the stability of 6 months to examine under conditions of relative humidity 75% ± 5%
Examine, as a result see the table below：
As can be seen from the above table, the Montelukast Sodium enteric-coated pellet capsule obtained by the present invention is in 40 DEG C of ± 2 DEG C of bars of high temperature
Investigated 6 months under part, every Index for examination meets regulation.
3rd, illumination condition stability inferior detects
The present invention obtains product compared with conventional tablet and granule, exposed under the conditions of illumination (4500LX ± 500LX)
The stability of 7 days is placed, it is as a result as follows：
Wherein, drug release determination method is as follows in buffer solution：
Lucifuge operates.This product is taken, according to dissolution method (four general rules of Chinese Pharmacopoeia version in 2015,0,931 second method), with
Phosphate buffer (0.5% lauryl sodium sulfate) 900ml of pH6.8 is dissolution medium, and rotating speed is 50 turns per minute, in accordance with the law
Measure, during through 30 minutes, takes solution about 10ml, filters, discards primary filtrate, take subsequent filtrate as test solution；Separately take Meng Lu
Department special dicyclohexylamine salt reference substance about 15mg, it is accurately weighed, to put in 50ml brown measuring bottles, add methanol about 40ml, ultrasound makes dissolving,
With methanol dilution to scale, shaking up, precision measures 1ml into 50ml brown measuring bottles, and solubilization goes out medium to scale, shakes up,
As reference substance solution.Tested according to high performance liquid chromatography (four general rules 0512 of Chinese Pharmacopoeia version in 2015).With octadecyl
Silane group silica gel is filler (150 × 4.6mm, 5 μm), and (6.8g di(2-ethylhexyl)phosphates are weighed with 0.05mol/L potassium dihydrogen phosphates
Hydrogen potassium, is dissolved in water to 1000ml, adds 1ml triethylamines, with phosphoric acid tune pH value to 5.6)-acetonitrile (25:75) it is mobile phase；
Detection wavelength：345nm；Column temperature：40℃；Flow velocity：1.0ml/min.Precision measures test solution and each 25 μ l of reference substance solution,
It is injected separately into chromatograph, records chromatogram, by external standard method with the stripping quantity of every bag of calculated by peak area, and result is multiplied by 0.764,
Limit is the 85% of labelled amount, should meet regulation.
Above example is only to illustrate the technical solution of type of the present invention, rather than its limitations；Although with reference to foregoing implementation
Type of the present invention is described in detail in example, it will be understood by those of ordinary skill in the art that：It still can be to foregoing each
Technical solution described in embodiment is modified, or carries out equivalent substitution to which part technical characteristic；And these are changed
Or replace, the essence of appropriate technical solution is departed from the spirit and scope of each embodiment technical solution of type of the present invention.
Claims (6)
- A kind of 1. Montelukast Sodium enteric-coated pellet capsule of stabilization, it is characterised in that the enteric-coated pellet capsule from the inside to the outside by containing Pill core, separation layer and enteric layer coating composition, wherein, the pellet core accounts for the 50-65% of enteric-coated pellet capsule, it is described every Absciss layer accounts for the 10-20% of enteric-coated pellet capsule, and the enteric layer coating accounts for the 25-30% of enteric-coated pellet capsule；Wherein, the pellet core is made of Montelukast Sodium, sodium carboxymethylcellulose, filler, disintegrant and basifier, institute The weight ratio for stating Montelukast Sodium is 7-10%, and the weight ratio of the sodium carboxymethylcellulose is 2-8%, the weight of the filler It is 60-70% to measure ratio, and the weight ratio of the disintegrant is 5-8%, and the weight ratio of the basifier is 10-15%；Wherein, the filler is selected from mannitol or lactose；The disintegrant is selected from crospovidone or cross-linked carboxymethyl fiber Plain sodium；One or more of the basifier in natrium carbonicum calcinatum, zinc oxide, sodium hydroxide and disodium hydrogen phosphate；Wherein, the separation layer is made of retarding agent, adhesive, antiplastering aid and opacifier, and the weight ratio of the retarding agent is 20- 35%, the weight ratio of described adhesive is 50-65%, and the weight ratio of the antiplastering aid is 6-11%, the weight of the opacifier Than for 2-5%；Wherein, the retarding agent is selected from ethyl cellulose or methylcellulose, described adhesive be selected from the third methylcellulose of carboxylic or PVP K30, the antiplastering aid are selected from talcum powder or superfine silica gel powder, and the opacifier is selected from titanium dioxide or iron oxide red；Wherein, the enteric layer coating is made of enteric high molecular material, plasticizer, antiplastering aid and opacifier, and the enteric is high The weight ratio of molecular material is 70-75%, and the weight ratio of the plasticizer is 5-7%, and the weight ratio of the antiplastering aid is 15- 20%th, the weight ratio of the opacifier is 2-5%；Wherein, the enteric high molecular material is selected from hypromellose phthalate, and the plasticizer is selected from citric acid One or more in triethyl, glycerine, Macrogol 6000, the antiplastering aid are selected from talcum powder or glycerin monostearate, The opacifier is selected from titanium dioxide or iron oxide red.
- 2. the Montelukast Sodium enteric-coated pellet capsule of stabilization according to claim 1, it is characterised in that the enteric-coated micro-pill glue The preparation method of capsule includes the following steps：(1) preparation of pellet coreSodium carboxymethylcellulose, filler, disintegrant and the basifier for crossing 80 mesh sieves, montelukast sodium raw materials mistake are taken respectively 200 mesh sieves, put in mixer and are uniformly mixed altogether, put dry powder in wet mixing pelletizer and mix, with wetting agent using spraying liquid feeding Mode softwood, put pill in extrusion spheronization pellet processing machine, mesh size is 24 mesh, collects wet ball and puts fluid bed in certain temperature Under the conditions of it is dry, collect the drying capsule core of certain sieve mesh number；(2) preparation of separation layerRetarding agent, adhesive are weighed, the ethanol that appropriate concentration is 85% is added, stirs evenly, add until completely dissolved anti-stick Agent and opacifier, add the ethanol that remaining concentration is 85%, after stirring evenly, cross 80 mesh sieves, will up to isolation coat liquid Dry capsule core is put in fluid bed, opens power supply, and adjusting parameter carries out bag barrier gown；(3) preparation of enteric layerWeigh enteric high molecular material to be dissolved in appropriate 85% ethanol, place a period of time until completely dissolved, add plasticising Agent, antiplastering aid and opacifier, then add 85% ethanol after stirring evenly, to cross 80 mesh sieves to full dose, will up to enteric coating liquid The base ball for wrapping barrier gown is put in fluid bed or coating pan, opens power supply, and adjusting parameter carries out enteric coated.
- 3. the Montelukast Sodium enteric-coated pellet capsule of stabilization according to claim 1, it is characterised in that the enteric-coated micro-pill glue Capsule composition is as follows：60% pellet core, 10% separation layer, 30% enteric layer.
- 4. the preparation method of the Montelukast Sodium enteric-coated pellet capsule of stabilization according to claim 2, it is characterised in that institute It is 50~60 DEG C to state in step (1) temperature in fluid bed.
- 5. the preparation method of the Montelukast Sodium enteric-coated pellet capsule of stabilization according to claim 2, it is characterised in that institute It is 20~30 mesh to state dry capsule core particle diameter in step (1).
- 6. the preparation method of the Montelukast Sodium enteric-coated pellet capsule of stabilization according to claim 2, it is characterised in that institute State in step (3) standing time be more than or equal to 12 it is small when.
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| CN201711328786.XA CN108014089A (en) | 2017-12-13 | 2017-12-13 | A kind of Montelukast Sodium enteric-coated pellet capsule of stabilization and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201711328786.XA CN108014089A (en) | 2017-12-13 | 2017-12-13 | A kind of Montelukast Sodium enteric-coated pellet capsule of stabilization and preparation method thereof |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103142541A (en) * | 2012-09-05 | 2013-06-12 | 北京万全阳光医学技术有限公司 | Stable montelukast sodium capsule |
| CN106491556A (en) * | 2016-10-21 | 2017-03-15 | 江苏阿尔法药业有限公司 | A kind of stable montelukast sodium enteric-coated pellet |
-
2017
- 2017-12-13 CN CN201711328786.XA patent/CN108014089A/en not_active Withdrawn
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103142541A (en) * | 2012-09-05 | 2013-06-12 | 北京万全阳光医学技术有限公司 | Stable montelukast sodium capsule |
| CN106491556A (en) * | 2016-10-21 | 2017-03-15 | 江苏阿尔法药业有限公司 | A kind of stable montelukast sodium enteric-coated pellet |
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