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Tablets PDF
Tablets PDF
UNIT III
V.MANIMARAN
LECTURER
DEPARTMENT OF PHARMACEUTICS
SRM COLLEGE OF PHARMACY
Introduction
1.Theyareunitdosageformandofferthegreatestcapabilitiesofalloraldosageform
forthegreatestdoseprecisionandtheleastcontentvariability.
2.Costislowestofalloraldosageform.
3.Lighterandcompact.
4.Easiestandcheapesttopackageandstrip.
5.Easytoswallowingwithleasttendencyforhangup.
6.Sustainedreleaseproductispossiblebyentericcoating.
7.Objectionableodourandbittertastecanbemaskedbycoatingtechnique.
8.Suitableforlargescaleproduction.
9.Greatestchemicalandmicrobialstabilityoveralloraldosageform.
10.Productidentificationiseasyandrapidrequiringnoadditionalstepswhen
employinganembossedand/ormonogrammedpunchface.
DisadvantagesofTabletdosageformare:
1.Difficulttoswallowincaseofchildrenandunconsciouspatients.
2.Somedrugsresistcompressionintodensecompacts,owingtoamorphousnature,
lowdensitycharacter.
3.Drugswithpoorwetting,slowdissolutionproperties,optimumabsorptionhighinGIT
maybedifficulttoformulateormanufactureasatabletthatwillstillprovideadequateor
fulldrugbioavailability.
4.Bittertestingdrugs,drugswithanobjectionableodorordrugsthataresensitiveto
oxygenmayrequireencapsulationorcoating.Insuchcases,capsulemayofferthebest
andlowestcost.
2
GeneralpropertiesofTabletdosageforms:
1.Atabletshouldhaveelegantproductidentitywhilefreeofdefectslikechips,cracks,
discoloration,andcontamination.
2.Shouldhavesufficientstrengthtowithstandmechanicalshockduringits
productionpackaging,shippinganddispensing.
3.Shouldhavethechemicalandphysicalstabilitytomaintainitsphysicalattributes
overtime
4.Thetabletmustbeabletoreleasethemedicinalagentsinapredictableand
reproduciblemanner.
5.Musthaveachemicalstabilityovertimesoasnottofollowalterationofthe
medicinalagents.
DifferenttypesofTablets
(A)Tabletsingestedorally:
1.Compressedtablet,e.g.Paracetamoltablet
2.Multiplecompressedtablet
3.Repeatactiontablet
4.Delayedreleasetablet,e.g.EntericcoatedBisacodyltablet
5.Sugarcoatedtablet,e.g.Multivitamintablet
6.Filmcoatedtablet,e.g.Metronidazoletablet
7.Chewabletablet,e.g.Antacidtablet
(B)Tabletsusedinoralcavity:
1.Buccaltablet,e.g.Vitaminctablet
2.Sublingualtablet,e.g.VicksMentholtablet
3.Trochesorlozenges
4.Dentalcone
(c)Tabletsadministeredbyotherroute:
1.Implantationtablet
2.Vaginaltablet,e.g.Clotrimazoletablet
(D)Tabletsusedtopreparesolution:
1.Effervescenttablet,e.g.Dispirintablet(Aspirin)
2.Dispensingtablet,e.g.Enzymetablet(Digiplex)
3.Hypodermictablet
4.Tablettrituratese.g.Enzymetablet(Digiplex)
TabletIngredients
Inadditiontoactiveingredients,tabletcontainsanumberofinertmaterialsknown
asadditivesorexcipients.Differentexcipientsare:
1.Diluent
2.Binderandadhesive
3.Disintegrents
4.Lubricantsandglidants
5.Colouringagents
6.Flavoringagents
7.Sweeteningagents
1. Diluent: Diluents are fillers used to make required bulk of the tablet when the drug
dosage itself is inadequate to produce the bulk. Secondary reason is to provide better
tablet properties such as improve cohesion, to permit use of direct compression
manufacturing or to promote flow. A diluent should have following properties:
1.Theymustbenontoxic
2.Theymustbecommerciallyavailableinacceptablegrade
3.Therecostmustbelow
4.Theymustbephysiologicallyinert
5.Theymustbephysically&chemicallystablebythemselves&incombination
withthedrugs.
6.Theymustbefreefromallmicrobialcontamination.
7.Theydonotalterthebioavailabilityofdrug.
8.Theymustbecolorcompatible.
Commonlyusedtabletdiluents
1.Lactoseanhydrousandspraydriedlactose
2.DirectlycompressedstarchStaRx1500
3.HydrolyzedstarchEmdexandCelutab
4.MicrocrystallinecelluloseAvicel(PH101andPH102)
5.Dibasiccalciumphosphatedehydrate
6.Calciumsulphatedihydrate
7.Mannitol
8.Sorbitol
9.Sucrose Sugartab,DiPac,Nutab
10.Dextrose
2.BindersandAdhesives:Thesematerialsareaddedeitherdryorinwet
formtoformgranulesortoformcohesivecompactsfordirectlycompressed
tablet.
Example:Acacia,tragacanth Solutionfor1025%Conc.
Cellulosederivatives Methylcellulose,Hydroxypropylmethyl
cellulose,Hydroxypropylcellulose
Gelatin 1020%solution
Glucose 50%solution
Polyvinylpyrrolidone(PVP) 2%conc.
Starchpaste1020%solution
Sodiumalginate
Sorbitol
3.Disintegrants:Addedtoatabletformulationtofacilitateitsbreakingor
disintegrationwhenitcontactinwaterintheGIT.
Example:Starch 520%oftabletweight.
Starchderivative PrimogelandExplotab(18%)
Clays VeegumHV,bentonite10%levelincoloredtabletonly
Cellulose
Cellulosederivatives Ac DiSol(sodiumcarboxymethyl
cellulose)
Alginate
PVP(Polyvinylpyrrolidone),crosslinked
Superdisintegrants:Swellsuptotenfoldwithin30secondswhencontact
water.
7.Sweeteningagents:Forchewabletablets:Sugar,mannitol.
Saccharine(artificial):500timessweeterthansucrose
Disadvantage:Bitteraftertasteandcarcinogenic
Aspartame(artificial)
Disadvantage:Lackofstabilityinpresenceofmoisture.
Granulationtechnologyonlargescalebyvarioustechniques
TabletCompressionMachine
Tabletsaremadebycompressingaformulationcontainingadrugordrugswith
excipientsonstampingmachinecalledpresses.Tabletpressesaredesignedwith
followingbasiccomponents:
1)Hopperforholdingandfeedinggranulation
2)Diesthatdefinethesizeandshapeofthetablet.
3)Punchesforcompressingthegranulationwithinthedies.
4)Camtracksforguidingthemovementofthepunches.
5)Afeedingmechanismformovinggranulationfromhopperintothe
dies
EvaluationofTablet
1. General Appearance: The general appearance of a tablet, its identity and
general elegance is essential for consumer acceptance, for control of lottolot
uniformity and tablettotablet uniformity. The control of general appearance
involves the measurement of size, shape, color, presence or absence of odor, taste
etc.
2. Size & Shape: It can be dimensionally described & controlled. The thickness of
a tablet is only variables. Tablet thickness can be measured by micrometer or by
other device. Tablet thickness should be controlled within a 5% variation of
standard value.
3. Unique identification marking: These marking utilize some form of
embossing, engraving or printing. These markings include company name or
symbol, product code, product name etc.
4. Organoleptic properties: Color distribution must be uniform with no
mottling. For visual color comparison compare the color of sample against
standard color.
5. Hardness and Friability: Tablet requires a certain amount of strength or
hardness and resistance to friability to withstand mechanical shakes of handling
in manufacture, packaging and shipping. Hardness generally measures the tablet
crushing strength
6.Friability: Friability of a tablet can determine in laboratory by Roche friabilator.
This consist of a plastic chamber that revolves at 25 rpm, dropping the tablets
through a Distance of six inches in the friabilator, which is then operate for 100
revolutions. The tablets are reweighed. Compress tablet that lose less than 0.5 to 1.0
% of the Tablet weigh are consider acceptable.
2.DrugContentandRelease:
(I) Weight Variation test (U.S.P.): Take 20 tablet and weighed individually. Calculate
average weight and compare the individual tablet weight to the average. The tablet pass the
U.S.P. test if no more that 2 tablets are outside the percentage limit and if no tablet differs by
more than 2 times the percentage limit.
(II) Content Uniformity Test: Randomly select 30 tablets. 10 of these assayed individually.
The Tablet pass the test if 9 of the 10 tablets must contain not less than 85% and not more than
115% of the labeled drug content and the 10th tablet may not contain less than 75% and more
than 125% of the labeled content. If these conditions are not met, remaining 20 tablet assayed
individually and none may fall out side of the 85 to 115% range.
(III) Disintegration Test (U.S.P.): The U.S.P. device to test disintegration uses 6 glass
tubes that are 3 long; open at the top and 10 mesh screen at the bottom end. To test for
disintegration time, one tablet is placed in each tube and the basket rack is positioned in a 1L
beaker of water, simulated gastric fluid or simulated intestinal fluid at 37 20 C such that the
tablet remain 2.5 cm below the surface of liquid on their upward movement and not closer than
2.5 cm from the bottom of the beaker in their downward movement. Move the basket
containing the tablets up and down through a distance of 56 cm at a frequency of 28 to 32
cycles per minute. Floating of the tablets can be prevented by placing perforated plastic discs on
each tablet.
According to the test the tablet must disintegrate and all particles must pass through the 10
mesh screen in the time specified. If any residue remains, it must have a soft mass.
Disintegration time: Uncoated tablet: 530 minutes
Coatedtablet:12hours
3.DissolutionTest(U.S.P.):Twosetofapparatus:
Apparatus1: A single tablet is placed in a small wire mesh basket attached to the
bottom of the shaft connected to a variable speed motor. The basket is immersed in
a dissolution medium (as specified in monograph) contained in a 100 ml flask. The
flask is cylindrical with a hemispherical bottom. The flask is maintained at
370.50C by a constant temperature bath. The motor is adjusted to turn at the
specified speed and sample of the fluid are withdrawn at intervals to determine the
amount of drug in solutions.
Types of Coating
Different coating processes are: Pan coating, Fluid Bed Coating, Compression coating
A. Pan Coating
B.FluidBedCoating
CompressionCoatingMachines
Othermethodsofcoatingequipments:
PerforatedPanSystems
AccelaCota:Itisaprototypeofperforatedcylindricaldrumprovidinghigh
dryingaircapacity.Therefofeitispreferredforfilmcoating.
Hicoatersystem:Thedryingairisdirectedintothedrumispassedthroughthe
tabletbed,andisexhaustedthroughtheperforationsinthedrum.
SUPERCELLTabletCoater
Revolutionarytabletcoaterthataccuratelydepositscontrolledamountsofcoating
materialsontablets,eveniftheyareextremelyhygroscopicorfriable.
Problemsintableting
1Capping
2Lamination/Laminating
3Chipping
4Cracking
5Sticking/Filming
6Picking
7Binding
8Mottling
9Doubleimpression
Problemsandremediesfortabletcoating
1Blistering
2Chipping
3Cratering
4Picking
5Pitting
6Blooming
7Blushing
8Colourvariation
9Infilling
10Orangepeel/Roughness
11Cracking/Splitting
THECAUSESANDREMEDIESOFCAPPINGRELATEDTOFORMULATION(GRANULATION)
Removesomeorallfinesthrough100
1. Largeamountoffinesinthegranulation
to200meshscreen
Moistenthegranulessuitably.Add
Toodryorverylowmoisturecontent
2. hygroscopicsubstancee.g.:sorbitol,
(leadingtolossofproperbindingaction).
methyl celluloseorPEG4000
3. Notthoroughlydriedgranules. Drythegranulesproperly.
IncreasingthemountofbinderOR
Addingdrybindersuchaspre
Insufficientamountofbinderorimproper
4. gelatinizedstarch,gumacacia,
binder.
powderedsorbitol,PVP,hydrophilic
silicaorpowderedsugar.
Increasetheamountoflubricantor
5. Insufficientorimproperlubricant.
changethetypeoflubricant.
6. Granularmasstoocoldtocompressfirm. Compressatroomtemperature.
THECAUSESANDREMEDIESOFCAPPINGRELATEDTOMACHINE(DIES,PUNCHESANDTABLETPRESS)
Polishdiesproperly.Investigate
1.
Poorlyfinisheddies othersteelsorothermaterials.
Deepconcavepunchesor Deepconcavepunchesor
2.
bevelededgefacesofpunches. bevelededgefacesofpunches.
Lowerpunchremainsbelowthe Makepropersettingoflower
3.
faceofdieduringejection. punchduringejection.
Incorrectadjustmentofsweepoff Adjustsweepoffbladecorrectly
4.
blade. tofacilitateproperejection.
Reducespeedofturret(Increase
5. Highturretspeed.
dwelltime).
TheCausesandRemediesofLaminationrelatedtoMACHINE(Dies,PunchesandTabletPress)]
1. Rapid relaxation of the peripheral regions of a tablet, Use tapered dies, i.e. upper part of the die bore has an
on ejection from a die. outward taper of 3 to 5.
2 Rapid decompression Reduce turret speed and reduce the final compression
Use precompression step. pressure.
THECAUSESANDREMEDIESOFCHIPPINGRELATEDTOFORMULATION(GRANULATION)AREASFOLLOWS
CAUSES REMEDIES
Sr.No.
1. Stickingonpunchfaces Drythegranulesproperlyorincreaselubrication.
2. Toodrygranules. Moistenthegranulestoplasticize.Addhygroscopicsubstances.
3. Toomuchbindingcauseschippingatbottom. Optimizebinding,orusedrybinders.
THECAUSESANDREMEDIESOFCHIPPINGRELATEDTOMACHINE(DIES,PUNCHESANDTABLETPRESS)
1. Grooveofdiewornatcompressionpoint. Polishtoopenend,reverseorreplacethedie.
2. Barreleddie(centerofthediewiderthanends) Polishthedietomakeitcylindrical
3. Edgeofpunchfaceturnedinside/inward. Polishthepunchedges
4. Concavitytoodeeptocompressproperly. Reduceconcavityofpunchfaces.Useflatpunches.
THECAUSESANDREMEDIESOFCRACKINGRELATEDTOFORMULATION(GRANULATION)
2. Too dry granules. Moisten the granules properly and add proper amount of binder
1.
Tabletexpandsonejectionduetoairentrapment. Usetapereddie.
.
removingtablets
2. Deepconcavitiescausecrackingwhile
Usespecialtakeoff
THECAUSESANDREMEDIESOFSTICKINGRELATEDTOFORMULATION(GRANULATION)
CAUSES REMEDIES
Sr.No.
Drythegranulesproperly.Makemoistureanalysistodetermine
1. Granulesnotdriedproperly.
limits.
2. Toolittleorimproperlubrication Increaseorchangelubricant.
3. Toomuchbinder Reducetheamountofbinderoruseadifferenttypeofbinder.
4. Hygroscopicgranularmaterial. Modifygranulationandcompressundercontrolledhumidity.
5. Oilyorwaymaterials Modifymixingprocess.Addanabsorbent.
6. Toosoftorweakgranules. Optimizetheamountofbinderandgranulationtechnique.
THECAUSESANDREMEDIESOFSTICKINGRELATEDTOMACHINE(DIES,PUNCHESANDTABLETPRESS)
Sr.No. CAUSES REMEDIES
1. Concavitytoodeepforgranulation. Reduceconcavitytooptimum.
2. Toolittlepressure. Increasepressure.
3. Compressingtoofast. Reducespeed
THECAUSESANDREMEDIESOFPICKINGRELATEDTOFORMULATION(GRANULATION)
Sr.No. CAUSES REMEDIES
1. Excessivemoistureingranules. Dryproperlythegranules,determineoptimumlimit.
Increaselubrication;usecolloidalsilicaasapolishingagent,so
2. Toolittleorimproperlubrication.
thatmaterialdoesnotclingtopunchfaces.
Lowmeltingpointsubstances,maysoftenfromtheheatof Addhighmeltingpointmaterials.Usehighmetingpoint
3.
compressionandleadtopicking. lubricants.
4. Lowmeltingpointmedicamentinhighconcentration. Refrigerategranulesandtheentiretabletpress.
Compressatroomtemperature.Coolsufficientlybefore
5. Toowarmgranuleswhencompressing.
compression.
Reducetheamountofbinder,changethetypeorusedry
6. Toomuchamountofbinder.
binders.
THECAUSESANDREMEDIESOFPICKINGRELATEDTOMACHINE(DIES,PUNCHESANDTABLETPRESS)
1. Roughorscratchedpunchfaces. Polishfacestohighluster.
Designletteringaslargeaspossible.
EmbossingorengravinglettersonpunchfacessuchasB,A,O,R,P,
2. Platethepunchfaceswithchromiumtoproduceasmooth
Q,G.
andnonadherentface.
3. Bevelsordividinglinestoodeep. Reducedepthsandsharpness.
4. Pressureappliedisnotenough;toosofttablets. Increasepressuretooptimum.
THECAUSESANDREMEDIESOFBINDINGRELATEDTOFORMULATION(GRANULATION)
CAUSES REMEDIES
Sr.No.
1. Toomoistgranulesandextrudesaroundlowerpunch. Drythegranulesproperly.
2. Insufficientorimproperlubricant. Increasetheamountoflubricantoruseamoreeffectivelubricant
Reducegranularsize,addmorefines,andincreasethequantityof
3. Toocoarsegranules.
lubricant.
4. Toohardgranulesforthelubricanttobeeffective. Modifygranulation.Reducegranularsize.
5. Granularmaterialveryabrasiveandcuttingintodies. Ifcoarsegranules,reduceitssize.Usewearresistantdies.
6. Granularmaterialtoowarm,stickstothedie. Reducetemperature.
THECAUSESANDREMEDIESOFBINDINGRELATEDTOMACHINE(DIES,PUNCHESANDTABLETPRESS)
CAUSES REMEDIES
Sr.No.
1. Poorlyfinisheddies. Polishthediesproperly.
2. Roughdiesduetoabrasion,corrosion. Investigateothersteelsorothermaterialsormodifygranulation.
Reworktopropersize.
3. Undersizeddies.Toolittleclearance.
Increaseclearance.
Reducepressure.OR
4. Toomuchpressureinthetabletpress.
Modifygranulation.
THECAUSESANDREMEDIESOFMOTTLING
CAUSES REMEDIES
Sr. No.
1. A coloured drug used along with colourless or white Use appropriate colourants.
coloured excipients.
2. A dye migrates to the surface of granulation while drying. Change the solvent system,
Change the binder,
Reduce drying temperature and
Use a smaller particle size.
3. Improperly mixed dye, especially during Direct Mix properly and reduce size if it is of a larger size to prevent
Compression. segregation.
4. Improper mixing of a coloured binder solution. Incorporate dry colour additive during powder blending step, then add
fine powdered adhesives such as acacia and tragacanth and mix well
and finally add granulating liquid.
PROBLEMSANDREMEDIESFORTABLETCOATING
THECAUSEANDREMEDYOFBLISTERING
CAUSES REMEDIES
Sr.No.
Effectoftemperatureonthestrength,elasticityand
1. Usemilddryingcondition.
adhesionofthefilm
THECAUSEANDREMEDYOFCHIPPING
Highdegreeofattritionassociatedwiththecoating Increasehardnessofthefilmbyincreasingthemolecular
1. process. weightgradeofpolymer.
THECAUSESANDREMEDIESOFCRATERING
1. Inefficientdrying. Useefficientandoptimumdryingconditions.
Increaseviscosityofcoatingsolutiontodecreasespray
2. Higherrateofapplicationofcoatingsolution.
applicationrate.
THECAUSESANDREMEDIESOFPICKING
Useoptimumandefficientdryingconditionsorincreasethe
Inefficientdrying.
1. inletairtemperature.
Decreasetheraterofapplicationofcoatingsolutionby
2. Higherrateofapplicationofcoatingsolution
increasingviscosityofcoatingsolution.
THECAUSEANDREMEDYOFPITTING
Dispensingwithpreheatingproceduresattheinitiationof
coatingandmodifyingthedrying(inletair)temperaturesuch
1.
Inappropriatedrying(inletair)temperature thatthetemperatureofthetabletcoreisnotgreaterthanthe
meltingpointofthebatchofadditivesused.
THECAUSEANDREMEDYOFBLOOMING
Highconcentrationandlowmolecularweightof Decreaseplasticizerconcentrationandincreasemolecular
1.
plasticizer. weightofplasticizer
THECAUSESANDREMEDIESOFBLUSHING
1. Highcoatingtemperature Decreasethedryingairtemperatur
Useofsorbitolinformulationwhichcauseslargestfallin
AvoiduseofsorbitolwithHydroxyPropylCellulose,Hydroxy
thethermalgelationtemperatureoftheHydroxyPropyl
2. PropylMethylCellulose,MethylCelluloseandCellulose
Cellulose,HydroxyPropylMethylCellulose,Methyl
ethers.
CelluloseandCelluloseethers.
THECAUSEANDREMEDYOFCOLOURVARIATION
Impropermixing,unevenspraypattern,insufficient
Goforgeometricmixing,reformulationwithdifferent
1. coating,migrationofsolubledyesplasticizersandother
plasticizersandadditivesorusemilddryingconditions.
additivesduringdrying.
THECAUSEANDREMEDYOFINFILLING
Bubbleorfoamformationbecauseofairsprayingofa
1. Addalcoholorusespraynozzlecapableoffineratomization.
polymersolution
THECAUSESANDREMEDIESOFORANGEPEEL/ROUGHNESS
1. RapidDrying Usemilddryingconditions
2. Highsolutionviscosity Useadditionalsolventstodecreaseviscosityofsolution.
THECAUSEANDREMEDYOFCRACKING/SPLITTING
Uselowermolecularweightpolymersorpolymericblends.
1. Useofhighermolecularweightpolymersorpolymericblends.
Alsoadjustplasticizertypeandconcentration.
Thanku