mouth dissolving tablets
TRANSCRIPT
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ScopeScopeIntroductionIntroductionAdvantages and disadvantagesAdvantages and disadvantagesof compressedof compressed
tabletstablets
Types of tabletsTypes of tablets
Tablet compression machineTablet compression machineTableting methodsTableting methods
Direct compressionDirect compression
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IntroductionIntroduction
18431843 a patent was granted toa patent was granted toThomas Brockedon (Englishman)Thomas Brockedon (Englishman)
for manufacturing pills andfor manufacturing pills and
lozengeslozenges
18741874both rotary and eccentricboth rotary and eccentric
pressespresses
No other tablet monographNo other tablet monograph
appeared until 1945appeared until 1945
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AdvantagesAdvantages
Production aspectProduction aspectLarge scale production at lowest costLarge scale production at lowest cost
Easiest and cheapest to package andEasiest and cheapest to package and
shipshipHigh stabilityHigh stability
User aspect (doctor, pharmacist,User aspect (doctor, pharmacist,
patient)patient)Easy to handlingEasy to handling
Lightest and most compactLightest and most compact
Greatest dose precision & least contentGreatest dose precision & least content
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DisadvantagesDisadvantagesSome drugs resist compression into dense compactsSome drugs resist compression into dense compacts
Drugs withDrugs withpoor wetting, slow dissolution, intermediate topoor wetting, slow dissolution, intermediate tolarge dosageslarge dosages may be difficult or impossible to formulatemay be difficult or impossible to formulateand manufacture as a tablet that provide adequate or fulland manufacture as a tablet that provide adequate or fulldrug bioavailabilitydrug bioavailability
Bitter taste drugs, drugs with an objectionable odor, orBitter taste drugs, drugs with an objectionable odor, orsensitive to oxygen or moisturesensitive to oxygen or moisture may require encapsulationmay require encapsulationor entrapment prior to compression or the tablets mayor entrapment prior to compression or the tablets may
require coatingrequire coating
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AbsorptioAbsorptio
n of drugn of drug
formform
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LubricantsLubricants
To reduce the friction during tabletTo reduce the friction during tabletejection between the walls of the tabletejection between the walls of the tabletand the walls of the die cavityand the walls of the die cavity
GlidantsGlidants
Reducing friction between the particlesReducing friction between the particles
To improve the flow properties of theTo improve the flow properties of thegranulationsgranulations
AntiadherantsAntiadherants
To prevent adherence of the granules toTo prevent adherence of the granules tothe punch faces and diesthe punch faces and dies
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Dissolution (enhancers andDissolution (enhancers andretardants)retardants)
Wetting agentsWetting agents
AntioxidantsAntioxidants
PreservativesPreservatives
Coloring agentsColoring agents
Flavoring agentsFlavoring agents
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Essential propertiesEssential properties
of tabletsof tabletsAccurate dosageAccurate dosage of medicament, uniform in weight,of medicament, uniform in weight,appearance and diameterappearance and diameterHave theHave the strengthstrength to withstand the rigors of mechanicalto withstand the rigors of mechanicalshocks encountered in its production, packaging,shocks encountered in its production, packaging,
shipping and dispensingshipping and dispensing
ReleaseRelease the medicinal agents in the body in a predictablethe medicinal agents in the body in a predictableand reproducible mannerand reproducible manner
Elegant product, acceptable size and shapeElegant product, acceptable size and shape
Chemical and physicalChemical and physical stabilitiesstabilities
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Types of tabletsTypes of tabletsRoute of administrationRoute of administration
Oral tabletsOral tablets
Sublingual or buccal tabletsSublingual or buccal tablets
Vaginal tabletsVaginal tabletsProduction processProduction process
Compressed tabletsCompressed tablets
Multiple compressed tabletsMultiple compressed tabletsTablet within a tablets: core and shellTablet within a tablets: core and shellMultilayer tabletMultilayer tablet
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Sugar coated tabletsSugar coated tablets
Film coated tabletsFilm coated tablets
Chewable tabletsChewable tablets
Effervescent tabletsEffervescent tablets
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Tablet productionTablet productionPowders intended for compression into tabletsPowders intended for compression into tabletsmust possess two essential propertiesmust possess two essential properties
Powder fluidityPowder fluidity
The material can be transported through the hopperThe material can be transported through the hopper
into the dieinto the dieTo produce tablets of a consistent weightTo produce tablets of a consistent weight
Powder flow can be improved mechanically by thePowder flow can be improved mechanically by the
use of vibrators, incorporate the glidantuse of vibrators, incorporate the glidant
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Powder compressibilityPowder compressibilityThe property of forming aThe property of forming a
stable, intact compact massstable, intact compact masswhen pressure is appliedwhen pressure is applied
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Tableting procedureTableting procedure
FillingFilling
CompressionCompression
EjectionEjection
bl iT bl i
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Tablet compressionTablet compression
machinesmachinesHopperHopper for holding and feeding granulation to befor holding and feeding granulation to becompressedcompressedDiesDies that define the size and shape of the tabletthat define the size and shape of the tablet
PunchesPunches for compressing the granulation within the diesfor compressing the granulation within the diesCam tracksCam tracks for guiding the movement of the punchesfor guiding the movement of the punches
Feeding mechanismsFeeding mechanisms for moving granulation from thefor moving granulation from the
hopper into the dieshopper into the dies
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http://upload.wikimedia.org/wikipedia/commons/7/72/Old_tablet_press.jpg -
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M l i i
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Multi-station rotaryMulti-station rotary
pressespressesThe head of the tablet machine that holds theThe head of the tablet machine that holds theupper punches, dies and lower punches inupper punches, dies and lower punches inplace rotatesplace rotates
As the head rotates, the punches are guidedAs the head rotates, the punches are guidedup and down by fixed cam tracks, whichup and down by fixed cam tracks, whichcontrol the sequence of filling, compressioncontrol the sequence of filling, compressionand ejection.and ejection.
The portions of the head that hold the upperThe portions of the head that hold the upperand lower punches are called theand lower punches are called theupper anupper anlower turretslower turrets
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The portion holding the dies is calledThe portion holding the dies is calledthethe die tabledie table
TheThepull down cam (C)pull down cam (C) guides theguides the
lower punches to the bottom, allowinglower punches to the bottom, allowingthe dies to overfillthe dies to overfill
The punches then pass over aThe punches then pass over aweight-weight-
control cam (E),control cam (E), which reduces the fillwhich reduces the fillin the dies to the desired amountin the dies to the desired amount
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AA swipe off blade (D)swipe off blade (D) at the end of theat the end of the
feed frame removes the excess granulationfeed frame removes the excess granulation
and directs it around the turret and back intoand directs it around the turret and back into
the front of the feed framethe front of the feed frame
The lower punches travel over theThe lower punches travel over the lowerlower
compression roll (F)compression roll (F) while simultaneouslywhile simultaneously
the upper punches ride beneath thethe upper punches ride beneath theupperuppercompression roll (G)compression roll (G)
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The upper punches enter a fixed distance into the dies, while theThe upper punches enter a fixed distance into the dies, while the
lower punches are raised to squeeze and compact the granulationlower punches are raised to squeeze and compact the granulation
within the dieswithin the dies
After the moment of compression, the upper punches areAfter the moment of compression, the upper punches are
withdrawn as they follow thewithdrawn as they follow theupper punch raising cam (H)upper punch raising cam (H)The lower punches ride up theThe lower punches ride up the cam (I)cam (I) which brings the tabletswhich brings the tablets
flush with or slightly above the surface of the diesflush with or slightly above the surface of the dies
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http://upload.wikimedia.org/wikipedia/commons/5/5a/Tablet_press_animation.gif -
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Although tablet compressing machinery hasAlthough tablet compressing machinery hasundergone numerous mechanical modificationsundergone numerous mechanical modifications
over the years, the compaction of materialsover the years, the compaction of materialsbetween a pair of moving punches within abetween a pair of moving punches within astationary die hasstationary die hasremained unchangedremained unchanged
The principle modification from earlierThe principle modification from earlier
equipment has been an increase in productionequipment has been an increase in productionrate which is regulated byrate which is regulated by
Number of tooling setsNumber of tooling sets
Number of compression stationsNumber of compression stations
Rotational speed of the pressRotational speed of the press
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Special adaptations of tablet machines allowSpecial adaptations of tablet machines allow
for the compression of layered tablets andfor the compression of layered tablets and
coated tabletscoated tablets
A device that chills the compressionA device that chills the compression
components to allow for the compression ofcomponents to allow for the compression of
low-melting point substances such as waxeslow-melting point substances such as waxes
i.e. suppositoriesi.e. suppositories
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Tableting methodsTableting methods
Dry methodsDry methods
Direct compressionDirect compression
Dry granulationDry granulation
Wet methodsWet methods
Wet granulationWet granulation
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Direct compressionDirect compression
Tablets are compressed directlyTablets are compressed directly
from powder blends of the activefrom powder blends of the active
ingredient and suitable excipientsingredient and suitable excipientsNo pretreatment of the powderNo pretreatment of the powder
blends by wet or dry granulationblends by wet or dry granulation
procedures is necessaryprocedures is necessary
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AdvantagesAdvantages
EconomyEconomyMachine: fewer manufacturingMachine: fewer manufacturing
steps and pieces of equipmentsteps and pieces of equipmentLabor: reduce labor costsLabor: reduce labor costs
Less process vallidationLess process vallidationLower consumption of powerLower consumption of power
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Elimination of granulationElimination of granulation
processprocessHeat (wet granulation)Heat (wet granulation)
Moisture (wet granulation)Moisture (wet granulation)High pressure (dry granulation)High pressure (dry granulation)
Processing without the need forProcessing without the need for
moisture and heat which ismoisture and heat which is
inherent in most wet granulationinherent in most wet granulation
proceduresprocedures
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Avoidance of high compactionAvoidance of high compactionpressures involves in producingpressures involves in producingtablets by slugging or rolltablets by slugging or rollcompactioncompaction
Elimination of variabilities inElimination of variabilities inwet granulation processingwet granulation processingBinders (temp, viscous, age)Binders (temp, viscous, age)
Viscosity of the granulatingViscosity of the granulatingsolution (depend on its temp),solution (depend on its temp),
How long it has been prepared,How long it has been prepared,
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Rate of binder addition and kneading canRate of binder addition and kneading can
affect the properties of the granules formedaffect the properties of the granules formed
The granulating solution, the type and lengthThe granulating solution, the type and length
of mixing and the method and rate of wet andof mixing and the method and rate of wet and
dry screening can change the density anddry screening can change the density and
particle size of the granules, which can have aparticle size of the granules, which can have amajor effect on fill weight and compactionmajor effect on fill weight and compaction
qualitiesqualities
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Type and rate of dryingType and rate of drying can lead not only to critical changes incan lead not only to critical changes in
equilibrium MC but also to unblending asequilibrium MC but also to unblending as
soluble active ingredients migrate to thesoluble active ingredients migrate to the
surfaces of the drying granulessurfaces of the drying granules
More unit processes are incorporated inMore unit processes are incorporated in
production, the chances of batch-to-batchproduction, the chances of batch-to-batch
variation are compoundedvariation are compounded
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Prime particle dissociationPrime particle dissociation
Each primary drug particle isEach primary drug particle is
liberated from the tablet massliberated from the tablet mass
and is available for dissolutionand is available for dissolutionDisintegrate rapidly to theDisintegrate rapidly to the
primary particle state primary particle state
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Uniformity of particle sizeUniformity of particle size
Greater stability of tablet on agingGreater stability of tablet on agingColorColorDissolution rateDissolution rate
Fewer chemical stability problemsFewer chemical stability problemswould be encountered as compared towould be encountered as compared tothose made by the wet granulationthose made by the wet granulation
processprocess
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ConcernsConcerns
Excipient available from onlyExcipient available from only
one supplier and often costone supplier and often cost
more than filler used inmore than filler used ingranulationgranulation
Procedure conservationProcedure conservation
Machine investmentsMachine investments
Lack of material knowledgeLack of material knowledge
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Physical limitation of drugPhysical limitation of drugNo compressibilityNo compressibilityNo flowabilityNo flowability
Physical characteristics ofPhysical characteristics ofmaterials (both drug andmaterials (both drug andexcipient)excipient)Size and size distributionSize and size distributionMoistureMoisture
Shape and surfaceShape and surface
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FlowabilityFlowabilityDensityDensity
Lot to lot variabilityLot to lot variability
Dusting problemDusting problem
ColoringColoring
Di t iDirect compression
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Direct compressionDirect compression
fillersfillersCommon materials that haveCommon materials that havebeen modified in the chemicalbeen modified in the chemical
manufacturing process tomanufacturing process toimprove fluidity andimprove fluidity and
compressibilitycompressibility