Mouth Dissolving Tablets

8/14/2019 Mouth Dissolving Tablets

1/41


2/41

ScopeScopeIntroductionIntroductionAdvantages and disadvantagesAdvantages and disadvantagesof compressedof compressed

tabletstablets

Types of tabletsTypes of tablets

Tablet compression machineTablet compression machineTableting methodsTableting methods

Direct compressionDirect compression


3/41

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


4/41

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


5/41

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


6/41

AbsorptioAbsorptio

n of drugn of drug

formform


7/41


8/41

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


9/41

Dissolution (enhancers andDissolution (enhancers andretardants)retardants)

Wetting agentsWetting agents

AntioxidantsAntioxidants

PreservativesPreservatives

Coloring agentsColoring agents

Flavoring agentsFlavoring agents


10/41

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


11/41

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


12/41

Sugar coated tabletsSugar coated tablets

Film coated tabletsFilm coated tablets

Chewable tabletsChewable tablets

Effervescent tabletsEffervescent tablets


13/41

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


14/41

Powder compressibilityPowder compressibilityThe property of forming aThe property of forming a

stable, intact compact massstable, intact compact masswhen pressure is appliedwhen pressure is applied


15/41

Tableting procedureTableting procedure

FillingFilling

CompressionCompression

EjectionEjection

bl iT bl i


16/41

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


17/41
http://upload.wikimedia.org/wikipedia/commons/7/72/Old_tablet_press.jpg


18/41


19/41

M l i i


20/41

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


21/41

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


22/41

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)


23/41

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


24/41


25/41
http://upload.wikimedia.org/wikipedia/commons/5/5a/Tablet_press_animation.gif


26/41


27/41

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


28/41

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


29/41

Tableting methodsTableting methods

Dry methodsDry methods


Dry granulationDry granulation

Wet methodsWet methods

Wet granulationWet granulation


30/41


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


31/41

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


32/41

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


33/41

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,


34/41

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


35/41

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


36/41

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


37/41

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


38/41

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


39/41

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


40/41

FlowabilityFlowabilityDensityDensity

Lot to lot variabilityLot to lot variability

Dusting problemDusting problem

ColoringColoring

Di t iDirect compression


41/41


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

Mouth Dissolving Tablets

Documents

Transcript of Mouth Dissolving Tablets