CN108853041A - A kind of oral quick disintegrating tablet - Google Patents
A kind of oral quick disintegrating tablet Download PDFInfo
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- CN108853041A CN108853041A CN201810949132.7A CN201810949132A CN108853041A CN 108853041 A CN108853041 A CN 108853041A CN 201810949132 A CN201810949132 A CN 201810949132A CN 108853041 A CN108853041 A CN 108853041A
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
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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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0007—Effervescent
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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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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Abstract
The present invention relates to a kind of oral quick disintegrating tablets, the oral quick disintegrating tablet is made of the lubricant of the microcapsules particle of 10-30 parts by weight, the instant sugar alcohol of 65-90 parts by weight, the disintegrating agent of 2-10 parts by weight, the flavoring agent of 1-5 parts by weight and 0.1-2 parts by weight, and the microcapsules particle is made of clad and the principal component being coated in clad.The specific gelatin dosage of the present invention can balance disintegration time and hardness well.Without using gelatin, then disintegration time is then greatly improved, while hardness then reduces.
Description
Technical field
The present invention relates to a kind of oral quick disintegrating tablets.
Background technique
Oral quick disintegrating tablet（Orally disintegrating tablets, abbreviation ODT）It is a kind of new oral dosage forms.
Such preparation can be under the conditions of anhydrous（Or only a small amount of water exists）The fater disintegration in oral cavity enters digestion with swallowing act
Road, without mucosa absorption in oral cavity, body absorption, metabolic process are consistent with conventional tablet.ODT has clothes compared with ordinary preparation
With the advantages that convenient, absorption is fast, bioavilability is high, small to alimentary canal mucous membrane irritation, receive significant attention.
In May, 2002 country's medicine is examined center and is provided as follows to the technical requirements of oral quick disintegrating tablet：It 1, should be in oral cavity rapidly
Disintegration, no grittiness, good mouthfeel is easy to swallow, nonirritant to mucous membrane of mouth, and orders character item 2 in quality standard, builds
Suitable disintegration time mensuration method and limit are found, and is ordered into standard.3, to slightly solubility, suitable dissolution determination side should be established
Method and limit, and order into quality standard.
With the raising of China's national health attainment and the development of nutrient and healthcare products industry, oral tablet had become main already
A kind of nutritional supplementation mode.It is estimated that there are about 50% people to have any problem to tablet is swallowed, the compliance of nutrient absorption is affected.
In paediatrics and old nutrition, medicine, to the solid that can be dissolved in water or can be chewed or can be dissolved rapidly in mouth
Preparation has very big demand, and the oral flash-dispersion formulations without that can be dispersed or dissolved rapidly with water and swallowing act can solve
Certainly this problem.This dosage form can be dispersed or dissolved in saliva rapidly after being put into mouth, nutrient can by oral cavity or
Mucosal absorption in esophagus, bioavilability is higher than ordinary preparation, and the side effect as caused by first-pass metabolism can also mitigate.
The ultimate challenge of the fast disintegrating tablet of exploitation is exactly the physical property of tablet and disintegrating property will be good.The purpose of the present invention
It is to develop a kind of oral quick disintegrating tablet with good physical behavior and disintegration.
Summary of the invention
In order to solve the above-mentioned technical problems, the present invention provides a kind of oral quick disintegrating tablet, the oral quick disintegrating tablet is by 10-30
The microcapsules particles of parts by weight, the instant sugar alcohol of 65-90 parts by weight, the disintegrating agent of 2-10 parts by weight, 1-5 parts by weight flavoring agent
And the lubricant composition of 0.1-2 parts by weight, the microcapsules particle is by clad and the principal component being coated in clad
Composition.
The mass ratio of the principal component and clad is 1：2-4.
The microcapsules particle is prepared by following preparation method：
100- is dispersed by the principal component of 5 parts by weight, the ethyl alcohol insoluble material of 1-8 parts by weight using magnetic stirring apparatus under room temperature
In the water of 500 parts by weight, the aqueous solution that is prepared.Particle is formed using test-type spray dryer spray drying soln；
The disintegrating agent of the particle of 5 parts by weight, the instant sugar alcohol of 0.1-3 parts by weight, 0.1-3 parts by weight is divided using magnetic stirring apparatus
It dissipates in the ethyl alcohol in temperature for 0-5 degrees Celsius of 100-500 parts by weight, dispersion solution is prepared.It is done by spraying using test-type
Dry device spray drying soln forms microcapsules particle.
The ethyl alcohol insoluble material is one or more of gelatin, yellow glue, gum arabic.
The instant sugar alcohol in mannitol, sorbierite, erythritol, xylitol, lactose, dextrose and saccharose one
Kind is several.
The disintegrating agent is selected from primojel, sodium carboxymethyl starch, croscarmellose sodium, crosslinking N- second
One or more of alkene -2-Pyrrolidone, calcium silicates, sodium carboxymethylcellulose.
The flavoring agent is selected from tree plum flavoring agent, mint flavor, chocolate flavor lotus, vanilla flavor, strawberry tune
One or more of taste agent, orange flavor.
The lubricant is in magnesium stearate, stearic acid, polyethylene glycol, polyox-yethylene-polyoxypropylene block copolymer
One or more.
A kind of preparation method of oral quick disintegrating tablet, the preparation method comprises the following steps：
Prepare microcapsules particle, the instant sugar alcohol of 65-90 parts by weight, the disintegrating agent of 2-10 parts by weight, 1-5 of 10-30 parts by weight
The flavoring agent of parts by weight；
Microcapsules particle is mixed with instant sugar alcohol, disintegrating agent and flavoring agent, 0.1-2 parts by weight are then added into mixture
Lubricant, then using flat face beveled edge tablet mould 5-30kN pressure and 10-30 piece/point speed under by mixture pressure
Piece.
The microcapsules particle is prepared by following preparation method：
100- is dispersed by the principal component of 5 parts by weight, the ethyl alcohol insoluble material of 1-8 parts by weight using magnetic stirring apparatus under room temperature
In the water of 500 parts by weight, the aqueous solution that is prepared.Particle is formed using test-type spray dryer spray drying soln；
The disintegrating agent of the particle of 5 parts by weight, the instant sugar alcohol of 0.1-3 parts by weight, 0.1-3 parts by weight is divided using magnetic stirring apparatus
It dissipates in the ethyl alcohol in temperature for 0-5 degrees Celsius of 100-500 parts by weight, dispersion solution is prepared.It is done by spraying using test-type
Dry device spray drying soln forms microcapsules particle.
The study found that after suitable water-insoluble inorganic auxiliary material and effervescent agent is added, even if in compression force and tablet hardness
In lower situation, fast disintegrating tablet can also have good physical property and disintegrating property simultaneously.Water-insoluble inorganic auxiliary material ratio
Common water-soluble saccharides or salt can more improve the disintegrating property of tablet.This is because be mainly made of water-soluble substances
The trend of tablet dissolved is greater than disintegration, after the water soluble ingredient dissolution of tablet outer layer, due to foring sticky solution, water to
The rate of piece heart diffusion reduces, so as to cause disintegration time extension.Microcapsules particle is introduced into oral quick disintegrating tablet by the present invention, is obtained
Obtained a kind of oral quick disintegrating tablet with good physical behavior and disintegration.
The above-mentioned of the application and other features, aspects and advantages are more readily understood with reference to following detailed description.
Detailed description of the invention
Fig. 1 is the flow chart of technique.
Specific embodiment
Unless otherwise defined, all technologies used herein and scientific term have and fields ordinary skill people of the present invention
The normally understood identical meaning of member.When there is a conflict, the definition in this specification shall prevail.
A kind of oral quick disintegrating tablet, the oral quick disintegrating tablet is by the microcapsules particles of 10-30 parts by weight, 65-90 parts by weight
Instant sugar alcohol, the disintegrating agent of 2-10 parts by weight, the flavoring agent of 1-5 parts by weight and 0.1-2 parts by weight lubricant composition, it is described
Microcapsules particle is made of clad and the principal component being coated in clad.
The mass ratio of the principal component and clad is 1：2-4.
Microcapsules particle of the invention has solid or liquid core and wraps up the solid coating of the core.This microcapsules
Particle can be formed by the method included the following steps：Core formation liquid stream is provided and coating forms liquid stream, two sprays are provided
The setting of pipe, wherein core is formed liquid stream addition core nozzle and will be coated by core nozzle surrounding concentric ring around the second jet pipe
It forms liquid stream and concentric tubes is added to produce microcapsules particle, once it is micro- that solidification microcapsules immediately are formed in suitable gas
Grain.
Therefore, the method for forming microcapsules particle consists essentially of the following steps：Liquid stream, which is sprayed, by jet pipe produces droplet,
Dry (such as in spray drying process) or hardening (such as in spray chilling method) droplet in air.In general, air is heat
, the microcapsules particle of jet pipe is left in drying.However, with regard to freeze-drying for, in this case liquid stream include lipid and/
Or wax and/or low melting point polymer, heating liquid stream melt these components, the microcapsules particle formed at jet pipe with hot-air
Solidify in opposite cold air.
In general, within the scope of conventional spray drying or spray chilling, the method be characterized in that jet pipe includes core nozzle
And the second jet pipe being concentrically formed around core nozzle, core is sprayed by core nozzle and forms liquid, second is sprayed by this
Pipe spray coating forms liquid stream.The coating that the droplet to be formed includes the core and second liquid of the first liquid is arranged in double venturi.
For spray drying, hot gas is usually the gas with various of air or such as inert gas, such as nitrogen, argon gas
Or other inert gases.For spray chilling, usually using 45 DEG C or the gas of lower room temperature.
In general, it is liquid or gas that core, which forms liquid,.When it have liquid property when, select free solution, suspension,
The group of dispersion liquid, colloidal solution or dispersion liquid, oil and emulsion composition.It includes reactive compound or substance that core, which forms liquid,
Optionally with one or more pharmaceutically acceptable auxiliary material combinations.Reactive compound or substance can be it is any kind of it is therapeutic,
Preventative, diagnosis or prognostic agent.Moreover, it can be the reagent for being imaged or marking.In a preferred embodiment
In, which can be the forms of pharmacologically active agents for needing to discharge with control mode；Therefore, coating in physiological environment for slowly dividing
Solution to discharge the core of package whithin a period of time.
The microcapsules particle is prepared by following preparation method：
100- is dispersed by the principal component of 5 parts by weight, the ethyl alcohol insoluble material of 1-8 parts by weight using magnetic stirring apparatus under room temperature
In the water of 500 parts by weight, the aqueous solution that is prepared.Particle is formed using test-type spray dryer spray drying soln；
The disintegrating agent of the particle of 5 parts by weight, the instant sugar alcohol of 0.1-3 parts by weight, 0.1-3 parts by weight is divided using magnetic stirring apparatus
It dissipates in the ethyl alcohol in temperature for 0-5 degrees Celsius of 100-500 parts by weight, dispersion solution is prepared.It is done by spraying using test-type
Dry device spray drying soln forms microcapsules particle.
As a preferred embodiment, the ethyl alcohol insoluble material is gelatin, yellow glue, one in gum arabic
Kind is several.
As a preferred embodiment, the instant sugar alcohol be selected from mannitol, sorbierite, erythritol, xylitol,
One or more of lactose, dextrose and saccharose.It is preferred that instant sugar alcohol is mannitol, more preferable mannitol 200.In a reality
It applies in scheme, instant sugar alcohol constitutes at least 50%, preferably at least 60% and more preferably at least 70% tablet (w/w).At one
In embodiment, instant sugar alcohol constitutes at least 80% tablet (w/w).In another embodiment, using two different sugar
Alcohol.
As a preferred embodiment, the disintegrating agent is selected from primojel, sodium carboxymethyl starch, crosslinking carboxylic
One or more of sodium carboxymethylcellulose pyce, cross-linked N-vinyl -2-Pyrrolidone, calcium silicates, sodium carboxymethylcellulose.At one
In preferred embodiment, using at least two disintegrating agents, for example, for example, croscarmellose sodium and calcium silicates, or
SSG and calcium silicates.Disintegrating agent (or a variety of disintegrating agents) constitutes 5-40%, the preferably tablet of 8-22% (w/w).In general, at least one
Kind disintegrating agent is super-disintegrant (i.e. EXPLOTAB).In another embodiment, disintegrating agent is Superporous hydrogels.Include
5% or smaller, preferably 2% or smaller and more preferably from about 1% Superporous hydrogels.The example of Superporous hydrogels is ability
Known to field technique personnel.
As a preferred embodiment, the flavoring agent is selected from tree plum flavoring agent, mint flavor, chocolate seasoning
One or more of agent lotus, vanilla flavor, strawberry-flavoured agent, orange flavor.
As a preferred embodiment, the lubricant is selected from magnesium stearate, stearic acid, polyethylene glycol, polyoxy second
One or more of alkene-polyoxypropylene block copolymers.
The tablet (w/w) of lubricant composition 0.1%-5.0%, preferably 0.2%-1.0%.In another embodiment,
Lubricant is not included in tablet formulation or other than being contained in tablet formulation, is coated on the surface of compression mold.
Bleeding agent is selected from the group being made of anhydrous organic acid and its salt.In one embodiment, bleeding agent is anhydrous lemon
Lemon acid or sodium citrate.Tablet (the w/ of bleeding agent (or reagent) composition 5-15%, preferably 8-12% and more preferable 9%-11%
w)。
Component mixture of the invention includes glidant, for example, for example, talcum powder or colloidal silicon dioxide, are constituted
The tablet (w/w) of 0.1%-3.0% and preferred 0.1%-0.5%.Component mixture optionally includes a kind of flavoring agent or flavoring agent
Mixture (for example, for example, Synthetic Oil, natural oil or plant extracts, other synthesis or natural perfume material), usually exist
The level of the tablet (w/w) of 0.5-5%.It is preferred that included flavoring agent is the combination of flavoring agent to enhance the taste of active constituent
Road masking.The mixture that the example of flavouring mixture includes, such as lemon and citrus.Component mixture also may include surface
Activating agent or wetting agent (such as Sodium Laurylsulfate, tween, sapn), the usually level in the tablet of 0.1-3% (w/w).
In one embodiment, component mixture includes penetration enhancer, selected from by cholate, such as sodium glycocholate；
Chitosan derivatives；Or the salt and derivative of short chain and medium chain fatty acid (C6-C12), such as the group of sodium caprate composition, it is used for
The cheek and/oral osmotic of the active constituent of raising poor permeability and absorption.
In another embodiment, component mixture includes surfactant or wetting agent, for example, for example, laurel sulphur
Sour sodium or poloxamer, the dissolution and absorption of the active constituent for improving dissolubility difference.
A kind of preparation method of oral quick disintegrating tablet, the preparation method comprises the following steps：
Prepare microcapsules particle, the instant sugar alcohol of 65-90 parts by weight, the disintegrating agent of 2-10 parts by weight, 1-5 of 10-30 parts by weight
The flavoring agent of parts by weight；
Microcapsules particle is mixed with mannitol, disintegrating agent and flavoring agent, the profit of 0.1-2 parts by weight is then added into mixture
Lubrication prescription, then using flat face beveled edge tablet mould 5-30kN pressure and 10-30 piece/point speed under by mixture tabletting.
Fig. 1 is preparation method flow chart of the invention.Tool has been prepared by selection ethyl alcohol insoluble material in the present invention
There are the microcapsules of multilayered structure, as the middle layer of cladding, using this microcapsules for the present invention, the tablet being prepared has
There are extremely excellent disintegration time and hardness.
Hereinafter, the present invention is explained in more detail by embodiment, it should be appreciated that these embodiments are only
Illustrate and not restrictive.If raw materials used to be all commercially available without other explanations.
Referring to several example the present invention is described in detail.
Embodiment 1
It is dispersed 5.0g vitamin C, 5.0g gelatin in 200ml water using magnetic stirring apparatus under room temperature, the dimension being prepared is raw
Plain C aqueous gelatin solution.Gelatin corpuscle is formed using test-type spray dryer spray drying soln.
5.0g gelatin corpuscle, 1.0g mannitol 200,1.0g crosslinked polyvinylpyrrolidone are dispersed using magnetic stirring apparatus
In the 200ml ethyl alcohol that temperature is 0-5 degrees Celsius, dispersion solution is prepared.It is spray-dried using test-type spray dryer
Solution forms microcapsules particle.
With following weight ratio 20g microcapsules particles, 70.5g mannitol 200,5g disintegrating agent, 4g flavoring agent, 2g crystallite
Cellulose.Microcapsules particle is mixed with mannitol, disintegrating agent and flavoring agent.Then 0.5g stearic acid is added into mixture
Magnesium.Then use 15mm flat face beveled edge tablet mould under the pressure of 10kN and the speed of 14 pieces/point by mixture tabletting.It obtains
Tablet have 37.13 ± 5.134 newton hardness, 14 ± 3 seconds disintegration times.
Embodiment 2
It is same as Example 1, using 2.0g gelatin.
It is dispersed 5.0g vitamin C, 2.0g gelatin in 200ml water using magnetic stirring apparatus under room temperature, is prepared
Vitamin C aqueous gelatin solution.Gelatin corpuscle is formed using test-type spray dryer spray drying soln.
5.0g gelatin corpuscle, 1.0g mannitol 200,1.0g crosslinked polyvinylpyrrolidone are dispersed using magnetic stirring apparatus
In the 200ml ethyl alcohol that temperature is 0-5 degrees Celsius, dispersion solution is prepared.It is spray-dried using test-type spray dryer
Solution forms microcapsules particle.
With following weight ratio 20g microcapsules particles, 70.5g mannitol 200,5g disintegrating agent, 4g flavoring agent, 2g crystallite
Cellulose.Microcapsules particle is mixed with mannitol, disintegrating agent and flavoring agent.Then 0.5g stearic acid is added into mixture
Magnesium.Then use 15mm flat face beveled edge tablet mould under the pressure of 10kN and the speed of 14 pieces/point by mixture tabletting.It obtains
Tablet have 38.44 ± 5.237 newton hardness, 14 ± 3 seconds disintegration times.
Embodiment 3
It is same as Example 1, using 1.2g gelatin.
It is dispersed 5.0g vitamin C, 1.2g gelatin in 200ml water using magnetic stirring apparatus under room temperature, is prepared
Vitamin C aqueous gelatin solution.Gelatin corpuscle is formed using test-type spray dryer spray drying soln.
5.0g gelatin corpuscle, 1.0g mannitol 200,1.0g crosslinked polyvinylpyrrolidone are dispersed using magnetic stirring apparatus
In the 200ml ethyl alcohol that temperature is 0-5 degrees Celsius, dispersion solution is prepared.It is spray-dried using test-type spray dryer
Solution forms microcapsules particle.
With following weight ratio 20g microcapsules particles, 70.5g mannitol 200,5g disintegrating agent, 4g flavoring agent, 2g crystallite
Cellulose.Microcapsules particle is mixed with mannitol, disintegrating agent and flavoring agent.Then 0.5g stearic acid is added into mixture
Magnesium.Then use 15mm flat face beveled edge tablet mould under the pressure of 10kN and the speed of 14 pieces/point by mixture tabletting.It obtains
Tablet have 39.44 ± 5.766 newton hardness, 15 ± 2 seconds disintegration times.
Comparative example 1
It is same as Example 1, using 0.2g gelatin.
It is dispersed 5.0g vitamin C, 0.2g gelatin in 200ml water using magnetic stirring apparatus under room temperature, is prepared
Vitamin C aqueous gelatin solution.Gelatin corpuscle is formed using test-type spray dryer spray drying soln.
5.0g gelatin corpuscle, 1.0g mannitol 200,1.0g crosslinked polyvinylpyrrolidone are dispersed using magnetic stirring apparatus
In the 200ml ethyl alcohol that temperature is 0-5 degrees Celsius, dispersion solution is prepared.It is spray-dried using test-type spray dryer
Solution forms microcapsules particle.
With following weight ratio 20g microcapsules particles, 70.5g mannitol 200,5g disintegrating agent, 4g flavoring agent, 2g crystallite
Cellulose.Microcapsules particle is mixed with mannitol, disintegrating agent and flavoring agent.Then 0.5g stearic acid is added into mixture
Magnesium.Then use 15mm flat face beveled edge tablet mould under the pressure of 10kN and the speed of 14 pieces/point by mixture tabletting.It obtains
Tablet have 20.39 ± 4.289 newton hardness, 14 ± 3 seconds disintegration times.
Comparative example 2
It is same as Example 1, using 15g gelatin.
It is dispersed 5.0g vitamin C, 15g gelatin in 200ml water using magnetic stirring apparatus under room temperature, the dimension being prepared
Raw element C aqueous gelatin solution.Gelatin corpuscle is formed using test-type spray dryer spray drying soln.
5.0g gelatin corpuscle, 1.0g mannitol 200,1.0g crosslinked polyvinylpyrrolidone are dispersed using magnetic stirring apparatus
In the 200ml ethyl alcohol that temperature is 0-5 degrees Celsius, dispersion solution is prepared.It is spray-dried using test-type spray dryer
Solution forms microcapsules particle.
With following weight ratio 20g microcapsules particles, 70.5g mannitol 200,5g disintegrating agent, 4g flavoring agent, 2g crystallite
Cellulose.Microcapsules particle is mixed with mannitol, disintegrating agent and flavoring agent.Then 0.5g stearic acid is added into mixture
Magnesium.Then use 15mm flat face beveled edge tablet mould under the pressure of 10kN and the speed of 14 pieces/point by mixture tabletting.It obtains
Tablet have 39.19 ± 5.150 newton hardness, 21 ± 4 seconds disintegration times.
Comparative example 3
It is same as Example 1, the step of not using gelatin to mix.
Using magnetic stirring apparatus by 5.0g vitamin C, 5.0g gelatin, 1.0g mannitol 200,1.0g crosslinked polyethylene pyrrole
Pyrrolidone is scattered in the 200ml ethyl alcohol that temperature is 0-5 degrees Celsius, and dispersion solution is prepared.It is spray-dried using test-type
Device spray drying soln forms microcapsules particle.
With following weight ratio 20g microcapsules particles, 70.5g mannitol 200,5g disintegrating agent, 4g flavoring agent, 2g crystallite
Cellulose.Microcapsules particle is mixed with mannitol, disintegrating agent and flavoring agent.Then 0.5g stearic acid is added into mixture
Magnesium.Then use 15mm flat face beveled edge tablet mould under the pressure of 10kN and the speed of 14 pieces/point by mixture tabletting.It obtains
Tablet have 21.34 ± 3.245 newton hardness, 17 ± 3 seconds disintegration times.
Comparative example 4
It is same as Example 1,1.0g mannitol 200 is not used.
It is dispersed 5.0g vitamin C, 5.0g gelatin in 200ml water using magnetic stirring apparatus under room temperature, is prepared
Vitamin C aqueous gelatin solution.Gelatin corpuscle is formed using test-type spray dryer spray drying soln.
Temperature is dispersed by 5.0g gelatin corpuscle, 1.0g crosslinked polyvinylpyrrolidone using magnetic stirring apparatus to take the photograph for 0-5
In the 200ml ethyl alcohol of family name's degree, dispersion solution is prepared.Microcapsules are formed using test-type spray dryer spray drying soln
Particle.
With following weight ratio 20g microcapsules particles, 70.5g mannitol 200,5g disintegrating agent, 4g flavoring agent, 2g crystallite
Cellulose.Microcapsules particle is mixed with mannitol, disintegrating agent and flavoring agent.Then 0.5g stearic acid is added into mixture
Magnesium.Then use 15mm flat face beveled edge tablet mould under the pressure of 10kN and the speed of 14 pieces/point by mixture tabletting.It obtains
Tablet have 37.51 ± 4.121 newton hardness, 25 ± 3 seconds disintegration times.
Comparative example 5
It is same as Example 1, the step of second of drying is not used.
It is dispersed 5.0g vitamin C, 5.0g gelatin in 200ml water using magnetic stirring apparatus under room temperature, is prepared
Vitamin C aqueous gelatin solution.Gelatin corpuscle is formed using test-type spray dryer spray drying soln.
It is fine with following weight ratio 20g gelatin corpuscles, 70.5g mannitol 200,5g disintegrating agent, 4g flavoring agent, 2g crystallite
Dimension element.Microcapsules particle is mixed with mannitol, disintegrating agent and flavoring agent.Then 0.5g magnesium stearate is added into mixture.
Then use 15mm flat face beveled edge tablet mould under the pressure of 10kN and the speed of 14 pieces/point by mixture tabletting.It obtains
Tablet has the hardness of 33.13 ± 5.003 newton, 29 ± 3 seconds disintegration times.
Comparative example 6
Same as Example 1,5.0g gelatin replaces with polyvinyl alcohol (weight average molecular weight 2000).
It is dispersed 5.0g vitamin C, 5.0g polyvinyl alcohol in 200ml water using magnetic stirring apparatus under room temperature, is prepared into
The vitamin C aqueous gelatin solution arrived.Gelatin corpuscle is formed using test-type spray dryer spray drying soln.
5.0g gelatin corpuscle, 1.0g mannitol 200,1.0g crosslinked polyvinylpyrrolidone are dispersed using magnetic stirring apparatus
In the 200ml ethyl alcohol that temperature is 0-5 degrees Celsius, dispersion solution is prepared.It is spray-dried using test-type spray dryer
Solution forms microcapsules particle.
With following weight ratio 20g microcapsules particles, 70.5g mannitol 200,5g disintegrating agent, 4g flavoring agent, 2g crystallite
Cellulose.Microcapsules particle is mixed with mannitol, disintegrating agent and flavoring agent.Then 0.5g stearic acid is added into mixture
Magnesium.Then use 15mm flat face beveled edge tablet mould under the pressure of 10kN and the speed of 14 pieces/point by mixture tabletting.It obtains
Tablet have 23.99 ± 4.569 newton hardness, 28 ± 3 seconds disintegration times.
The specific gelatin dosage of the present invention can balance disintegration time and hardness well.Without using gelatin then disintegration time
It then greatly improves, while hardness then reduces.And use similar substance polyvinyl alcohol, then it can not obtain the same technology effect of gelatin
Fruit.As can be seen that being set to kernel and clad can be well using this substance of gelatin and by gelatin and mannitol distribution
Balance disintegration time and hardness.
The foregoing is only a preferred embodiment of the present invention, is not intended to limit the scope of the present invention.It is all
The equivalent changes and modifications that content is done according to the present invention are encompassed by the scope of the patents of the invention.
Claims (10)
1. a kind of oral quick disintegrating tablet, which is characterized in that the oral quick disintegrating tablet is by the microcapsules particle of 10-30 parts by weight, 65-90
The instant sugar alcohol of parts by weight, the disintegrating agent of 2-10 parts by weight, the flavoring agent of 1-5 parts by weight and 0.1-2 parts by weight lubricant
Composition, the microcapsules particle are made of clad and the principal component being coated in clad.
2. a kind of oral quick disintegrating tablet according to claim 1, which is characterized in that the mass ratio of the principal component and clad
It is 1：2-4.
3. a kind of oral quick disintegrating tablet according to claim 1, which is characterized in that the microcapsules particle passes through following preparation
Method is prepared：
100- is dispersed by the principal component of 5 parts by weight, the ethyl alcohol insoluble material of 1-8 parts by weight using magnetic stirring apparatus under room temperature
In the water of 500 parts by weight, the aqueous solution that is prepared.Particle is formed using test-type spray dryer spray drying soln；
The disintegrating agent of the particle of 5 parts by weight, the instant sugar alcohol of 0.1-3 parts by weight, 0.1-3 parts by weight is divided using magnetic stirring apparatus
It dissipates in the ethyl alcohol in temperature for 0-5 degrees Celsius of 100-500 parts by weight, dispersion solution is prepared.It is done by spraying using test-type
Dry device spray drying soln forms microcapsules particle.
4. a kind of oral quick disintegrating tablet according to claim 1, which is characterized in that the ethyl alcohol insoluble material be gelatin,
One or more of yellow glue, gum arabic.
5. a kind of oral quick disintegrating tablet according to claim 1, which is characterized in that the instant sugar alcohol is selected from mannitol, mountain
One or more of pears alcohol, erythritol, xylitol, lactose, dextrose and saccharose.
6. a kind of oral quick disintegrating tablet according to claim 1, which is characterized in that the disintegrating agent is selected from starch glycolic acid
Sodium, sodium carboxymethyl starch, croscarmellose sodium, cross-linked N-vinyl -2-Pyrrolidone, calcium silicates, carboxymethyl cellulose
One or more of sodium.
7. a kind of oral quick disintegrating tablet according to claim 1, which is characterized in that the flavoring agent be selected from tree plum flavoring agent,
One or more of mint flavor, chocolate flavor lotus, vanilla flavor, strawberry-flavoured agent, orange flavor.
8. a kind of oral quick disintegrating tablet according to claim 1, which is characterized in that the lubricant is selected from magnesium stearate, hard
One or more of resin acid, polyethylene glycol, polyox-yethylene-polyoxypropylene block copolymer.
9. a kind of preparation method of oral quick disintegrating tablet, which is characterized in that the preparation method comprises the following steps：
Prepare microcapsules particle, the instant sugar alcohol of 65-90 parts by weight, the disintegrating agent of 2-10 parts by weight, 1-5 of 10-30 parts by weight
The flavoring agent of parts by weight；
Microcapsules particle is mixed with mannitol, disintegrating agent and flavoring agent, the profit of 0.1-2 parts by weight is then added into mixture
Lubrication prescription, then using flat face beveled edge tablet mould 5-30kN pressure and 10-30 piece/point speed under by mixture tabletting.
10. a kind of oral quick disintegrating tablet according to claim 9, which is characterized in that the microcapsules particle passes through following system
Preparation Method is prepared：
100- is dispersed by the principal component of 5 parts by weight, the ethyl alcohol insoluble material of 1-8 parts by weight using magnetic stirring apparatus under room temperature
In the water of 500 parts by weight, the aqueous solution that is prepared.Particle is formed using test-type spray dryer spray drying soln；
The disintegrating agent of the particle of 5 parts by weight, the instant sugar alcohol of 0.1-3 parts by weight, 0.1-3 parts by weight is divided using magnetic stirring apparatus
It dissipates in the ethyl alcohol in temperature for 0-5 degrees Celsius of 100-500 parts by weight, dispersion solution is prepared.It is done by spraying using test-type
Dry device spray drying soln forms microcapsules particle.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810949132.7A CN108853041A (en) | 2018-08-20 | 2018-08-20 | A kind of oral quick disintegrating tablet |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201810949132.7A CN108853041A (en) | 2018-08-20 | 2018-08-20 | A kind of oral quick disintegrating tablet |
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| CN201810949132.7A Pending CN108853041A (en) | 2018-08-20 | 2018-08-20 | A kind of oral quick disintegrating tablet |
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| CN (1) | CN108853041A (en) |
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| CN1568941A (en) * | 2003-07-22 | 2005-01-26 | 范敏华 | Mouth disaggregating tablet and preparation method thereof |
| TW200510003A (en) * | 2003-09-05 | 2005-03-16 | Pharmaceutical Ind Tech & Dev | Pharmaceutical composition of rapid disintegrating tablet and method of preparing the same |
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