CN107625741A - A kind of taste masking coated preparation and preparation method thereof - Google Patents
A kind of taste masking coated preparation and preparation method thereof Download PDFInfo
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- CN107625741A CN107625741A CN201610565347.XA CN201610565347A CN107625741A CN 107625741 A CN107625741 A CN 107625741A CN 201610565347 A CN201610565347 A CN 201610565347A CN 107625741 A CN107625741 A CN 107625741A
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Abstract
The invention belongs to oral solid formulation field, and in particular to a kind of patient of suitable dysphagia takes, and taste masking coated preparation without bitter taste and preparation method thereof.Pass through packaging technique carry out taste masking direct to drug core; three layers of coating are comprised at least outside the active constituents of medicine of preparation; respectively protected acidic layer, separation layer and taste mask layer; enable medicine quick release while; with good mouthfeel; taste masking effect is good, will not be discharged into during taking in oral cavity, so as to there is the disagreeable tastes such as bitterness.Preparation enters in gastric environment, and clothing film is quickly dissolved, and medicine is released in gastric acid environment, and therapeutic action is played so as to be absorbed by organisms.
Description
Technical field
The invention belongs to oral solid formulation field, and in particular to a kind of patient of suitable dysphagia takes, and does not have
Taste masking coated preparation of bitter taste and preparation method thereof.
Background technology
Oral administration is the most frequently used administering mode, the advantage is that drug safety, conveniently, easily receives and adopt for patient
With disadvantage is however that absorption is slower, general oral half an hour is just effective, and is easily destroyed by intestines and stomach, has to intestines and stomach strongly
Stimulate or have bad smell or the medicine for the treatment of concentration is not suitable for being prepared into mouth needed for can not reaching in intestines and stomach absorption difference
Formulation.Wherein oral formulations include the formulations such as tablet, capsule, granule, oral liquid, have been swallowed for children, old man etc.
Difficult patient, preceding 2 and improper.
Research shows, dysphagia be not only refer to the autonomous swallow such as children, old man not yet develop completely/move back
The crowd of change, in addition to may temporary caused by congenital development imperfection, disease, physical damnification etc. or chronicity gulp down
Pharynx is difficult, for example, the imperfection that a minority is developed due to belch, causes when swallowing, medicine is easily accessible tracheae rather than oesophagus,
Also it is one kind of dysphagia.
Compared to liquid dosage forms such as oral liquids, granule (including granula subtilis), dry suspensoid agent etc. are used as non-aqueous solid system
Agent, the conventional substitute products of piece agent, capsule etc. are prepared, there is its unique advantage, such as to prepare cost cheap, easily stored
Carry etc..At present, for the patient of dysphagia, 2 kinds nothing more than of such oral solid formulation is taken, that is, is dissolved in point
Take after dissipating/dissolving, or directly swallow, however, which kind of mode no matter taken, because such preparation specific surface area is (relative to piece
The solid pharmaceutical preparations such as agent) increase, easily exposure medicine bad smell, made troubles to taking.In addition, investigation display, relatively
Mode is taken in former, many patients are more willing to directly swallow such preparation, rather than are taken after adding water dispersed/dissolved,
This is probably directly to take more convenient, and the bad smell of preparation is smaller.Also, particularly closed for unconscious crisis patient
It is suitable.
However, the non-aqueous solid pharmaceutical preparation prepared using prior art, is directly swallowed existing greatest problem and is, particle
Or particulate can produce certain astringent sense in mouth, the time for causing preparation to rest in mouth increases rather than quickly entered esophagus.Lose
Regret, this shortcoming, for dysphagia patients, further amplification.
Further, since most drug has the bad smells such as bitter taste, excitant, not relaxing for patient is brought when directly swallowing
Taking sensation can allow it to limit the application of such preparation significantly, therefore, taste masking is also directly to swallow system to taking generation mental handicape
One of problem that agent must solve.
Coating method is the most frequently used masking methods of solid pharmaceutical preparation, and coating refers to using Utech (Eudragit), ethyl cellulose
The coating material such as plain (EC), hydroxypropyl methyl cellulose (HPMC), to drug powder or a certain size, the medicine core (micropill of hardness
Or particle) be coated, reach the purpose of taste masking, including 3 kinds of film-coating, enteric coating and sugar-coat.Can be reduced after coating medicine with
The contact of taste bud, so as to taste masking.Protection against the tide, lucifuge, isolation air, raising medicine stability and control medicine can also be played simultaneously
Thing rate of release and the effect at position.
Coating material ethyl cellulose (EC), hydroxypropyl methyl cellulose (HPMC) clothing film are not influenceed by pH, in vivo respectively
Discharged in kind of environment in certain speed, for bitter taste than stronger medicine, taste masking clothing film can reach taste masking function but very
Difficulty makes medicine quick and completely discharged.WO1999/026608 provides a kind of coated granule of granulated crystalline ibuprofen, and it is adopted
With directly by the mode of drug coating, by insoluble polymer ethyl cellulose, the hydrophilic polymer of certain weight ratio
The coating membrane of hydroxypropyl methylcellulose and silica composition is coated on the drug core with certain particle diameter in water-alcohol dispersion liquid
On, make up to taste masking, stable ibuprofen granule.But employ the ethyl cellulose of water-insoluble, its discharge still by
Influence is arrived.
Utech dissolves in acid, is swelled in water and neutrality, alkaline environment, although overcoming ethyl to a certain extent
The shortcomings that cellulose, but influenceed by vivo environment excessive, and excessively rely on gastric acid environment.When different crowd is taken medicine
When, the difference of gastric acid environment also influences whether the release of medicine.
For bitter taste than more serious insoluble drug, how while excellent taste masking effect is provided, can protect again
The quick release of medicine is demonstrate,proved, ensures the validity of medicine, turns into a urgent problem to be solved in the prior art.
The content of the invention
The present invention provides a kind of taste masking coated preparation for being easy to swallow and preparation method thereof, by packaging technique to medicine core
The heart directly carries out taste masking so that medicine can quick release while, there is good mouthfeel, taste masking effect is good, is taking
During will not be discharged into oral cavity, so as to will not have the disagreeable tastes such as bitterness.Preparation enters in gastric environment, and clothing film is instant soon
Solution, medicine are released in gastric acid environment, and therapeutic action is played so as to be absorbed by organisms.
Taste masking coated preparation of the present invention, it is characterised in that three layers of coating are comprised at least outside active constituents of medicine, point
Not Wei protected acidic layer, separation layer and taste mask layer, wherein the taste masking ingredients in the taste mask layer are Utech, the protected acidic
The acidic ph modifier that can make formulation ingredients quick release is included in layer.
Taste masking coated preparation in the present invention comprises at least three layers of coating structure：Protected acidic layer, separation layer and taste mask layer,
Three layers of coating structure can play a part of covering active constituents of medicine peculiar smell, but the structure for wherein mainly playing taste masking is
Taste mask layer, comprising coating framework ingredient it is taste masking ingredients Utech in the taste mask layer, such as Utech E100, Utech is in acid
Dissolving, be swelled in water and neutrality, alkaline environment, its influenceed by vivo environment it is excessive, such as the different time of before or after meals
Point medication, the rate of release of medicine is different, and also Utech excessively relies on gastric acid environment, and the change of gastric acid environment also influences whether
The release of medicine.Based on it is above-mentioned some, design protected acidic layer increases the release of taste mask layer, increases the rate of release of medicine,
Acidic ph modifier is included in wherein described protected acidic layer, the acidic ph modifier can provide sour environment so that outstanding
Special strange taste masking clothing film can also obtain dashing forward in neutral and alkaline buffer to be released, vivo environment and its hydrochloric acid in gastric juice ring when eliminating medication
The influence in border.In order to prevent the direct contact of taste masking coatings and acid coatings, the stability of preparation is improved, is coated in taste masking
Separation layer is added among layer and acid coatings.
The protected acidic layer includes the acidic ph modifier selected from one or more of：Citric acid, lactic acid, winestone
Acid, malic acid, adipic acid, fumaric acid, phosphoric acid, metatartaric acid, gluconic acid, acetic acid, ascorbic acid, butanedioic acid, fumaric acid.
Acidic ph modifier dosage in the protected acidic layer does not limit strictly, as long as can achieve the goal, even if
Taste mask layer can dash forward release under circumstances, and it can be 15%~50% in the weight/mass percentage composition in protected acidic layer, excellent
Elect 15%~45%, more preferably 20%~40%, most preferably 25%~30% as.
Also include the composition selected from one or more of in the protected acidic layer：Adhesive, antitackiness agent, plasticizer,
Surfactant, filler, flavouring, lubricant, disintegrant.One embodiment of the present of invention includes adhesive and resisted glutinous
Agent.
Described adhesive, antitackiness agent, plasticizer, surfactant, filler, flavouring, lubricant, disintegrant do not have
Especially limitation, as long as the composition of stable acidic protective layer can be formed.Such as adhesive can be selected from：Icing Sugar, syrup, shallow lake
Slurry, polyvinylpyrrolidone, methylcellulose, hydroxypropyl methylcellulose, sodium carboxymethylcellulose, rubber cement, dextrin, alginic acid
One or more in sodium, polyvinyl alcohol etc.；The antitackiness agent can be selected from：Talcum powder, superfine silica gel powder, cornstarch, tristearin
One or more in sour magnesium, glycerin monostearate etc.；The plasticizer can be selected from：Triethyl citrate, decanedioic acid two
One kind or more in butyl ester, dibutyl phthalate, glycerol triacetate, castor oil, glycerine, propane diols, polyethylene glycol etc.
Kind；The surfactant may be selected from：One kind or more in TWEEN Series, Span series, lecithin, lauryl sodium sulfate etc.
Kind；The filler can be selected from：Starch, sucrose, dextrin, calcium sulfate, calcium monohydrogen phosphate, calcium carbonate, microcrystalline cellulose, sweet dew
One or more in alcohol, lactose, pregelatinized starch；The flavouring can be selected from：Lactose, sucrose, glucose, mannitol,
One or more in citric acid, peppermint oil etc.；The lubricant can be selected from：Magnesium stearate, calcium stearate, talcum powder, ten
One or more in sodium dialkyl sulfate, Stepanol MG, superfine silica gel powder etc.；The disintegrant can be selected from：Starch,
One or more in avicel cellulose, calcium carbonate, CMC-Na, sodium alginate etc..
Taste masking coated preparation in the present invention, wherein quality hundred of the Utech in the taste mask layer in taste mask layer
It is 30%~80% to divide content, preferably 35%~75%, more preferably 40%~65%, most preferably 45%~60%.
Also include the composition selected from one or more of in the taste mask layer：Adhesive, antitackiness agent, plasticizer, surface
Activating agent, filler, flavouring, lubricant, disintegrant.Such as one embodiment in the present invention includes pore-foaming agent and resisted glutinous
Agent.
Described adhesive, antitackiness agent, plasticizer, surfactant, filler, flavouring, lubricant, disintegrant do not have
Especially limitation, as long as the composition of stable acidic protective layer can be formed.Such as adhesive can be selected from：Icing Sugar, syrup, shallow lake
Slurry, polyvinylpyrrolidone, methylcellulose, hydroxypropyl methylcellulose, sodium carboxymethylcellulose, rubber cement, dextrin, alginic acid
One or more in sodium, polyvinyl alcohol etc.；The antitackiness agent can be selected from：Talcum powder, superfine silica gel powder, cornstarch, tristearin
One or more in sour magnesium, glycerin monostearate etc.；The plasticizer can be selected from：Triethyl citrate, decanedioic acid two
One kind or more in butyl ester, dibutyl phthalate, glycerol triacetate, castor oil, glycerine, propane diols, polyethylene glycol etc.
Kind；The surfactant may be selected from：One kind or more in TWEEN Series, Span series, lecithin, lauryl sodium sulfate etc.
Kind；The filler can be selected from：Starch, sucrose, dextrin, calcium sulfate, calcium monohydrogen phosphate, calcium carbonate, microcrystalline cellulose, sweet dew
One or more in alcohol, lactose, pregelatinized starch；The flavouring can be selected from：Lactose, sucrose, glucose, mannitol,
One or more in citric acid, peppermint oil etc.；The lubricant can be selected from：Magnesium stearate, calcium stearate, talcum powder, ten
One or more in sodium dialkyl sulfate, Stepanol MG, superfine silica gel powder；The disintegrant can be selected from：Starch, knot
One or more in crystalline cellulose, calcium carbonate, CMC-Na, sodium alginate etc..
Taste masking coated preparation in the present invention, wherein the separation layer is clipped between protected acidic layer and taste mask layer,
Play a part of strengthening medicine stability.Conventional spacer layer coating material includes hydroxypropyl methyl cellulose, hydroxy propyl cellulose
Element, polyvinylpyrrolidone, polyethylene glycol, talcum powder, the film-forming coating materials such as stearic acid.
Had no particular limits in the present invention for the active component, refer to have pharmacological activity is selected from following list
The combinations of one compound or two kinds and its above compound, including the chemical medicine of synthesis, bio-pharmaceutical, extracted from plant
Active working substance, effective active single component etc., such as can be：It is antihypertensive, anxiolytic, antithrombotic, anticonvulsion
Medicine, hypoglycemic agent, decongestant, resistance amine medicine, antitussive, antineoplastic, beta-Blocking agent, anti-inflammatory agent, antipsychotic drug, cognition
Function promoter, antiatherosclerotic, gemfibrozil, antiadipositas drug, autoimmune disease medicine, Alibra, antibacterial
Medicine and antifungal, somnifacient, antibiotic, antidepressants, antiviral agent etc..Active component is in one embodiment of the present of invention
Active component includes Loratadine, Cefixime etc. in metacortandracin, other embodiments.
When carrying out the coating such as protected acidic layer, separation layer, taste mask layer to active component, may be selected directly to drug powder
Be coated, can also select by active component according to this area customary preparation methods be prepared as carrying medicine micropill, carry medicine granule,
The forms such as medicine microplate are carried, are then coated.
The taste masking coated preparation of the present invention can also include the 4th layer of smooth layer, and the 4th layer of smooth layer is included into fractional condensation
Jelly, the gel can select：Gelatin, carragheen, xanthans, konjaku flour, carbomer, agar etc., preferably carbomer, example
Such as Carbomer971.The dosage of gel can be 10~50%, preferably 12%~45%, more preferably 15%~40%.The present invention
Taste masking coated preparation coat the 4th layer of smooth layer, on the one hand can reach more preferable taste masking effect, another aspect gel is met
Gel can be formed after water, makes micropill surface very smooth, can reach and preferably swallow effect, realize it is anhydrous swallow, greatly improve
The compliance of medication.
The taste masking coated preparation of the present invention can also be mixed with flavoring material and that taste masking effect is prepared is more preferable
Taste masking preparation.The flavoring material can further enhance the taste masking effect of the taste masking coated preparation, and increase patient is especially
The mouthfeel and compliance of child patient medication, the flavoring material constituent can be any drug flavors and easy of can covering
In the pharmaceutic adjuvant or its mixture that are received by patient, particularly child patient, such as include one kind in following composition or more
Kind：Aromatic, sweetener, acid, diluent, gel, lubricant；Can be directly direct by the composition with flavoring function
Mix with taste masking coated preparation of the present invention, used as flavoring material, can also be by this area conventional method by fragrance
The flavoring composition such as agent, sweetener, acid uses after being prepared as flavoring particle as flavoring material.One embodiment of the present of invention
Middle flavoring material includes diluent, adhesive, sweetener, acid and aromatic simultaneously.
One or more of the aromatic in artificial essence or natural essence, natural perfume material include lemon oil, fennel
Sesame oil, peppermint oil etc., artificial essence include orange flavor, strawberry essence, vanilla, Mint Essence, lemon extract, banana incense
Essence etc.；One kind in aspa sweet tea, Sucralose, acesulfame potassium, honey element, mannitol, sorbierite of the sweetener or
It is a variety of；The one kind of the acid in citric acid, sodium citrate, potassium citrate, sodium dihydrogen citrate, malic acid, tartaric acid
It is or a variety of；One or more of the diluent in sorbierite, mannitol, sucrose；It is fine that described adhesive is selected from carboxymethyl
Tie up one kind in plain sodium, polyvinylpyrrolidone, methylcellulose, ethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose
It is or a variety of；The lubricant is not particularly limited, and can be pharmaceutically conventional lubricant, be selected from talcum powder, stearic acid
It is more than one or both of magnesium, stearic acid, superfine silica gel powder, titanium dioxide, magnesia.
Wherein sweetener, aromatic, the content of acid can not be 0 simultaneously；The amount of diluent can be 50%~
95%, preferably 55%~90%, more preferably 60%~85%；Binder content can be 1%~15%, preferably 2%~
14%, more preferably 5%~11%；Lubricant content can be 0~10%, preferably 0.2%~8%, more preferably 0.5%~
6%；Levels of sweetener can be 0~10%, preferably 0.2%~8%, more preferably 0.5%~6%；Fragrance level can be 0
~10%, preferably 0.2%~8%, more preferably 0.3%~6%；Tart flavour agent content can be 0~10%, preferably 0.5%
~8%, more preferably 2%~5.5%.
The present invention also provides a kind of method for preparing above-mentioned taste masking coated preparation, including：
1. protected acidic layer is coated：PH adjusting agent and other coating constituents are prepared with water turns into suspension, to activity into
The load medicine micropill, particle, microplate of drug powder or carrying active composition is divided to carry out fluidized bed coating.Coating continues drying after terminating
And sieved.
2. spacer layer coating：Spacer layer coating composition is prepared with water turns into suspension, fluidized bed coating is selected, to the 1st
Product made from step carries out spacer layer coating.Coating continues to dry and sieved after terminating.
3. taste mask layer is coated：Utech and the other coating constituents of taste mask layer are configured to suspension, select fluidized bed coating,
The product obtained to the 2nd step carries out taste masking coating.Coating continues drying and sieved after terminating.
The present invention taste masking coated preparation can also carry out other functional coatings, such as in order to obtain more preferable taste masking and
It lubricates mouthfeel, can also include the 4th layer of smooth layer, the 4th layer of smooth layer includes component gel agent, after gel meets water
Gel can be formed, make micropill surface very smooth, can reach and preferably swallow effect, realize it is anhydrous swallow, greatly improve medication
Compliance, the gel can select：Gelatin, carragheen, xanthans, konjaku flour, carbomer, agar etc., preferably card ripple
Nurse, such as Carbomer971.Smooth layer coating method can select method commonly used in the art, such as fluidized bed coating.
The taste masking coated preparation of the present invention can also be mixed with flavoring particle and that taste masking effect is prepared is more preferable
Taste masked particle agent.The flavoring particle can further enhance the taste masking effect of the taste masking coated preparation, and increase patient is especially
The mouthfeel and compliance of child patient medication, the flavoring particle can by conventional method of granulating, by flavoring material and/or its
Its composition, such as aromatic, sweetener, acid, diluent, gel and/or lubricant etc., are compressed to after granule,
Mixed with taste masking coated preparation, can also directly by flavoring material and/or other component powders it is well mixed after directly with it is described
Taste masking coated preparation mixes.
Embodiment
It is further explained and described present invention by the following examples.Described embodiment understands only for help
Present invention, it is understood not to the restriction to present subject matter and protection domain.
The metacortandracin taste masking coating micro-pill of embodiment 1.
Active medicine metacortandracin is carried in the form of medicine micropill is carried, metacortandracin carries medicine micropill and coats protected acidic successively
Layer, separation layer, taste mask layer, each layer raw material and its dosage are as follows：
Carry medicine micropill：
| Composition | Unit formulation dosage |
| 0.5~0.6mm sucrose capsule cores | 190mg |
| Metacortandracin | 5mg |
| Hydroxypropyl methylcellulose E5LV | 5mg |
| Tween 80 | 1mg |
| Citric acid | 1mg |
Protected acidic layer：
| Citric acid | 5mg |
| Hydroxypropyl methylcellulose E5LV | 1mg |
| Talcum powder | 15mg |
Separation layer：
| Hydroxypropyl methylcellulose E5LV | 11.2mg |
| Talcum powder | 5mg |
Taste mask layer：
| Utech E100 | 12mg |
| Macrogol 6000 | 1.2mg |
| Talcum powder | 6mg |
Preparation method is：
1. carry the preparation of medicine micropill：
Solution is made in metacortandracin, citric acid, hydroxypropyl methylcellulose, the dissolving of Tween 80 water, selects fluidized bed coating, it is right
Sucrose capsule core carries out medicine-feeding coating.35~45 DEG C of coating process control material temperature, coating continue to dry 30 minutes after terminating.And
Sieved, collect the micropill between 25~50 mesh.
2. protected acidic clothing film coating：
Citric acid, hydroxypropyl methylcellulose, talcum powder are turned into suspension with water preparation, fluidized bed coating is selected, to carrying medicine
Ball carries out protected acidic coating.30~35 DEG C of coating process control material temperature, coating continue to dry 30 minutes after terminating.Go forward side by side
Row screening, collects the micropill between 25~50 mesh.
3. spacer layer coating：
Hydroxypropyl methylcellulose, talcum powder are turned into suspension with water preparation, fluidized bed coating is selected, to made from the 2nd step
Micropill carries out spacer layer coating.40~50 DEG C of coating process control material temperature, coating continue to dry 30 minutes after terminating.Go forward side by side
Row screening, collects the micropill between 25~50 mesh.
4. taste mask layer is coated：
Utech E100, talcum powder, polyethylene glycol are configured to suspension with ethanol, fluidized bed coating is selected, to isolation
Micropill carries out taste masking coating.30~35 DEG C of coating process control material temperature, coating continue to dry 30 minutes after terminating.And to micro-
Ball is sieved, and collects the micropill between 25~50 mesh.
Metacortandracin taste masking coated preparation micropill control group：Formula material, dosage and preparation method thereof reference implementation example 1, no
The coating for removing protected acidic layer is only that with part.
The metacortandracin taste masking coating micro-pill prepared respectively in terms of mouthfeel and dissolution rate two is taken to embodiment 1 is commented
Valency,
Take mouthfeel：10 volunteers, in the case of the difference of embodiment 1 and control group is not informed, swallow after taking
The mouthfeel of preparation is counted, 10 people think that the taste masking coating micro-pill of embodiment 1 and control group takes process free from extraneous odour, 9
People thinks that the product of embodiment 1 receives compared with the products taste of control group compared to more preferable.
Dissolution rate：According to dissolution rate and drug release determination method (《Chinese Pharmacopoeia》Version four in 2015, the method for general rule 0,931 second)
Determination method, using 500ml water as dissolution medium, rotating speed is 50 turns per minute.Sampling is measured at 30 minutes, and dissolution rate must not
Less than 80%.
Dissolution determination method：
The taste masking coated preparation of the present invention is evaluated in terms of mouthfeel and dissolution rate two is taken, illustrates to compare for bitter taste
Serious medicine, especially insoluble drug, the present invention can ensure medicine again while excellent taste masking effect is provided
The quick release of thing, ensure the validity of medicine.
The Loratadine taste masking coated granule of embodiment 2.
Directly carry out powder coating using Loratadine drug powder, successively drug overcoats cladding protected acidic layer, every
Absciss layer, taste mask layer, each layer raw material and its dosage are as follows：
Protected acidic layer：
| Composition | Unit formulation dosage |
| Tartaric acid | 5.5mg |
| Hydroxypropyl methylcellulose E5LV | 1.2mg |
| Stearic acid | 13mg |
Separation layer：
| Hydroxypropyl methylcellulose E5LV | 12.0mg |
| Magnesium stearate | 5mg |
Taste mask layer：
| Utech E100 | 11.7mg |
| Macrogol 6000 | 1.4mg |
| Magnesium stearate | 5.5mg |
Preparation method is：
1. protected acidic clothing film coating：
Tartaric acid, hydroxypropyl methylcellulose, stearic acid are turned into suspension with water preparation, fluidized bed coating is selected, to chlorine thunder
He determines dried powder and carries out protected acidic coating.30~35 DEG C of coating process control material temperature, coating continue drying after terminating
30 minutes.And sieved, collect the particle between 25~50 mesh.
2. spacer layer coating：
Hydroxypropyl methylcellulose, magnesium stearate are turned into suspension with water preparation, fluidized bed coating is selected, the 1st step is made
Particle carry out spacer layer coating.40~50 DEG C of coating process control material temperature, coating continue to dry 30 minutes after terminating.And
Sieved, collect the particle between 25~50 mesh.
3. taste mask layer is coated：
Utech E100, magnesium stearate, polyethylene glycol are configured to suspension with ethanol, fluidized bed coating is selected, to the 2nd
Walk obtained particle and carry out taste masking coating.30~35 DEG C of coating process control material temperature, coating continue to dry 30 points after terminating
Clock.And particle is sieved, collect the particle between 25~50 mesh.
Take mouthfeel：Method is taken with the people of embodiment 1,10, represents to take process without bitter taste, acceptance level height.
Dissolution rate：Method with 1,10 minutes dissolution rates of embodiment be within 50%, 30 minute 92%, 45 minute be 95%, medicine
Thing release is quick.
The Cefixime taste masking coated granule of embodiment 3.
Directly carry out powder coating using Cefixime drug powder, successively drug overcoats cladding protected acidic layer, every
Absciss layer, taste mask layer, each layer raw material and its dosage are as follows：
Protected acidic layer：
| Composition | Unit formulation dosage |
| Malic acid | 6.5mg |
| Hydroxypropyl methylcellulose E5LV | 1.2mg |
| Magnesium stearate | 15mg |
Separation layer：
| Hydroxypropyl methylcellulose E5LV | 12.5mg |
| Talcum powder | 5mg |
Taste mask layer：
| Utech E100 | 12.5mg |
| Macrogol 6000 | 1.1mg |
| Talcum powder | 5.5mg |
Preparation method is：
1. protected acidic clothing film coating：
Malic acid, hydroxypropyl methylcellulose, magnesium stearate are turned into suspension with water preparation, select fluidized bed coating, it is correct
Spore gram oxime dried powder carries out protected acidic coating.30~35 DEG C of coating process control material temperature, coating continue to do after terminating
Dry 30 minutes.And sieved, collect the particle between 25~50 mesh.
2. spacer layer coating：
Hydroxypropyl methylcellulose, talcum powder are turned into suspension with water preparation, fluidized bed coating is selected, to made from the 1st step
Particle carries out spacer layer coating.40~50 DEG C of coating process control material temperature, coating continue to dry 30 minutes after terminating.Go forward side by side
Row screening, collects the particle between 25~50 mesh.
3. taste mask layer is coated：
Utech E100, talcum powder, polyethylene glycol are configured to suspension with ethanol, fluidized bed coating is selected, to the 2nd step
Obtained particle carries out taste masking coating.30~35 DEG C of coating process control material temperature, coating continue to dry 30 minutes after terminating.
And particle is sieved, collect the particle between 25~50 mesh.
Take mouthfeel：Method is taken with the people of embodiment 1,10, represents to take process without bitter taste, acceptance level height.
Dissolution rate：Method with 1,10 minutes dissolution rates of embodiment be within 52%, 30 minute 91%, 45 minute be 95%, medicine
Thing release is quick.
The metacortandracin taste masking coating micro-pill of embodiment 4.
The metacortandracin taste masking coating micro-pill finished product obtained in embodiment 1 is carried out to the cladding of smooth layer, smooth layer prescription again
It is as follows：
| Composition | Unit formulation dosage |
| PVPK29/32 | 18mg |
| Carbomer971 | 54mg |
| Talcum powder | 18mg |
| Stearic acid 50 | 9mg |
| Sodium acid carbonate | 36mg |
Preparation method：By PVPK29/32, Carbomer971, talcum powder, stearic acid 50, sodium acid carbonate prepared with ethanol
As suspension, fluidized bed coating is selected, smooth coating is carried out to taste masking coating micro-pill.Coating process control material 30~35
DEG C, coating continues to dry 30 minutes after terminating.And micropill is sieved, collect the micropill between 25~50 mesh.
Take mouthfeel：Method is taken with the people of embodiment 1,10, and it is more real without bitter taste, mouthfeel acceptance level to take process for expression
It is high to apply example 1.
Dissolution rate：Method with 1,10 minutes dissolution rates of embodiment be within 49%, 30 minute 90%, 45 minute be 95%, medicine
Thing release is quick, and smooth layer coating has little to no effect to the release of medicine.
The flavoring material of embodiment 5.
Mouthfeel is taken in order to further be lifted, the taste masking coated preparation in the present invention can mix flavoring material, weigh mountain
Pears alcohol, citric acid, Aspartame, sodium carboxymethylcellulose, orange essence mix 5~10 minutes.
To being prepared after flavoring material is uniformly mixed with the metacortandracin taste masking coated preparation of embodiment 1 and embodiment 4
Taste masking preparation take mouthfeel and dissolution rate is measured：
Take mouthfeel：Method is taken with the people of embodiment 1,10, and it is more real without bitter taste, mouthfeel acceptance level to take process for expression
Apply example 1 and embodiment 4 is more preferable.
Dissolution rate：Method with embodiment 1,10 minutes dissolution rates of embodiment 1 and the mixed preparation of flavoring material are 52%,
30 minutes were 96% for 92%, 45 minute, and 10 minutes dissolution rates of embodiment 4 and the mixed preparation of flavoring material are 49%, 30
Minute was 95% for 90%, 45 minute, and flavoring material has little to no effect to the release of medicine.
Claims (14)
1. a kind of taste masking coated preparation, it is characterised in that three layers of coating are comprised at least outside active constituents of medicine, are respectively acid protect
Sheath, separation layer and taste mask layer, wherein the taste masking ingredients in the taste mask layer are Utech, being included in the protected acidic layer can
So that the acidic ph modifier of formulation ingredients quick release.
2. taste masking coated preparation as claimed in claim 1, it is characterised in that the protected acidic layer includes being selected from next
Kind or a variety of acidic ph modifiers：Citric acid, lactic acid, tartaric acid, malic acid, adipic acid, fumaric acid, phosphoric acid, metatartaric acid,
Gluconic acid, acetic acid, ascorbic acid, butanedioic acid, fumaric acid.
3. the taste masking coated preparation as described in any one of claim 1~2, it is characterised in that the acid in the protected acidic layer
Property weight/mass percentage composition of the pH adjusting agent in protected acidic layer be 15%~50%, preferably 15%~45%, more preferably
20%~40%, most preferably 25%~30%.
4. the taste masking coated preparation as described in any one of claims 1 to 3, it is characterised in that also wrapped in the protected acidic layer
Include the composition selected from one or more of：Adhesive, antitackiness agent, plasticizer, surfactant, filler, flavouring, lubrication
Agent, disintegrant.
5. the taste masking coated preparation as described in any one of Claims 1 to 4, it is characterised in that the protected acidic composition of layer removes
Also include adhesive and antitackiness agent outside acidic ph modifier.
6. the taste masking coated preparation as described in any one of Claims 1 to 5, it is characterised in that the Utech in the taste mask layer
Weight/mass percentage composition in taste mask layer is 30%~80%, and preferably 35%~75%, more preferably 40%~65% are optimal
Elect 45%~60% as.
7. the taste masking coated preparation as described in any one of claim 1~6, it is characterised in that also include choosing in the taste mask layer
From the composition of one or more of：Adhesive, antitackiness agent, plasticizer, surfactant, filler, flavouring, lubricant,
Disintegrant.
8. the taste masking coated preparation as described in any one of claim 1~7, it is characterised in that the taste masking composition of layer is except especially
Also include pore-foaming agent and antitackiness agent outside strange.
9. the taste masking coated preparation as described in any one of claim 1~8, it is characterised in that the separation layer is by protected acidic
Layer separates with taste mask layer, and it includes the composition selected from one or more of：Adhesive, antitackiness agent, plasticizer, surface-active
Agent, filler, flavouring, lubricant, disintegrant.
10. the taste masking coated preparation as described in any one of claim 1~9, it is characterised in that the active component refers to have
The combination selected from following single compound or two kinds and its above compound of pharmacological activity：Antihypertensive, anxiolytic,
Antithrombotic, anticonvulsive drug, hypoglycemic agent, decongestant, resistance amine medicine, antitussive, antineoplastic, beta-Blocking agent, anti-inflammatory
Medicine, antipsychotic drug, cognitive function accelerator, antiatherosclerotic, gemfibrozil, antiadipositas drug, autoimmunity disease
Sick medicine, Alibra, antimicrobial and antifungal, somnifacient, antibiotic, antidepressants, antiviral agent.
11. the taste masking coated preparation as described in claim 1~10, it is characterised in that also including the 4th layer of smooth layer, described
Four layers of smooth layer include component gel agent.
12. the taste masking coated preparation as described in any one of claim 1~11, it is characterised in that also added with further increase
The flavoring material of taste masking effect.
13. the taste masking coated preparation as described in any one of claim 1~12, it is characterised in that the taste masking coated preparation is
Granule, micropill or microplate.
14. a kind of method for the taste masking coated preparation for preparing any one of claim 1~13, including：
Protected acidic layer is coated：PH adjusting agent and other coating constituents are prepared with water turns into suspension, to active ingredient medicine
The load medicine micropill of powder or carrying active composition, particle, microplate carry out fluidized bed coating, and coating continues to dry and carried out after terminating
Screening；
Spacer layer coating：Spacer layer coating composition is prepared with water turns into suspension, selects fluidized bed coating, the 1st step is made
Product carry out spacer layer coating, coating continues to dry and sieved after terminating；
Taste mask layer is coated：Utech and the other coating constituents of taste mask layer are configured to suspension, fluidized bed coating is selected, to the 2nd
Walk obtained product and carry out taste masking coating, coating continues drying and sieved after terminating.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610565347.XA CN107625741A (en) | 2016-07-18 | 2016-07-18 | A kind of taste masking coated preparation and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610565347.XA CN107625741A (en) | 2016-07-18 | 2016-07-18 | A kind of taste masking coated preparation and preparation method thereof |
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| CN107625741A true CN107625741A (en) | 2018-01-26 |
Family
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610565347.XA Pending CN107625741A (en) | 2016-07-18 | 2016-07-18 | A kind of taste masking coated preparation and preparation method thereof |
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| Country | Link |
|---|---|
| CN (1) | CN107625741A (en) |
Cited By (4)
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| CN107625742A (en) * | 2016-07-19 | 2018-01-26 | 北京科信必成医药科技发展有限公司 | One kind is anhydrous to swallow taste masking preparation and preparation method thereof |
| CN110755404A (en) * | 2019-12-04 | 2020-02-07 | 长春雷允上药业有限公司 | Azithromycin pharmaceutical composition and preparation method thereof |
| CN111214456A (en) * | 2020-03-10 | 2020-06-02 | 浙江普利药业有限公司 | Voriconazole dry suspension and preparation method thereof |
| CN118340736A (en) * | 2024-04-23 | 2024-07-16 | 海南恒诚三叶制药有限公司 | Cefpodoxime proxetil tablet and preparation method thereof |
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| CN111214456A (en) * | 2020-03-10 | 2020-06-02 | 浙江普利药业有限公司 | Voriconazole dry suspension and preparation method thereof |
| CN118340736A (en) * | 2024-04-23 | 2024-07-16 | 海南恒诚三叶制药有限公司 | Cefpodoxime proxetil tablet and preparation method thereof |
| CN118340736B (en) * | 2024-04-23 | 2024-10-18 | 海南恒诚三叶制药有限公司 | Cefpodoxime proxetil tablet and preparation method thereof |
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Effective date of registration: 20230421 Address after: 8639, Floor 6, Building 3, No. 3, Yongchang North Road, Daxing District, Beijing, 100176 Applicant after: Beijing Kexin Jurun Pharmaceutical Technology Co.,Ltd. Address before: 100083 room 15, 15 / F, block a, Tiangong building, 30 Xueyuan Road, Haidian District, Beijing Applicant before: COSCI MED-TECH Co.,Ltd. |