This powerpoint presentation consists of the brief introduction of Tablets and introduction the granulation methods as well.further topics will be covered in the next part of this presentation.

1. TABLETS
“JUST READING MCQ’s FROM BOOKS DOESN’T ENSURE SUCCESS IN GPAT”
“Take Care in Corona
Stay Safe Ladke/
Ladki”
Take- Talc
Care in- Colloidal silica
Corona- Corn Starch
Stay- Stearates
Safe- Sodium Lauryl
Sulfate
Ladke/ Ladki- Leucine
VIVEK SINGH

2. 2
TABLETS
“According to IP, Tablets are solid, flat or biconvex dishes, unit dosage form,
prepared by compressing a drug or a mixture of drugs, with or without
diluents”.
“As per USP, tablets are solid dosage form each containing a unit dose of one or
more medicament”.
VIVEK SINGH

3. A tablet should have elegant product identity
Free from defects such as cracks, discoloration & contamination
Should have chemical & physical stability for longer duration
Should be pharmacologically stable
Should have high bioavailability
Should withstand the mechanical shocks encountered during production,
packaging, transportation and dispensing
IDEAL PROPERTIES OF TABLETS
VIVEK SINGH

4. Provide accurate, stable with great precision of dose
Easy to handle, use & carry and patient compliant
Least microbial contamination
Packaging & shipping is easy & cheap
Low manufacturing cost, high manufacturing speed
Targeted drug delivery is possible
ADVANTAGES OF TABLETS
VIVEK SINGH

5. Hygroscopic drugs are not suitable for tablets
Slow dissolution drugs are not suitable for tablets
High dose drugs are not suitable for tablets
Drugs degraded in GIT are not suitable
Liquid & volatile drugs are difficult to formulate as tablet
Swallowing of tablet is difficult for children & unconscious patients
DISADVANTAGES OF TABLETS
VIVEK SINGH

6. CLASSIFICATION OF TABLETS
TABLETS INGESTED
ORALLY
• Compressed tablet
• Controlled release
tablet
• Chewable tablet
• Sugar coated tablet
• Film coated tablet
• Enteric coated tablet
• Compressed coated
tablet
TABLETS USED IN
ORAL CAVIETIES
Buccal tablets
Sublingual tablets
Lozenges
Dental cone
TABLETS
ADMINISTERED BY
OTHER ROUTES
•Implantation tablets
•Vaginal tablets
TABLETS USED TO
PREPARE
SOLUTIONS
•Effervescent tablets
•Dispensing tablets
•Hypodermic tablets
•Tablet triturates
VIVEK SINGH

7. TABLET EXCIPIENTS
Pharmaceutical excipients are substances other than the pharmacologically active
drug or prodrug which are included in the manufacturing process or are contained
in a finished pharmaceutical product dosage form.
VIVEK SINGH

8. TABLET EXCIPENTS
1) DILUENTS/ FILLERS
Why?
They are used to produce tablet of reasonable size i.e. minimum diameter of 3 mm.
A) Lactose:
▪ Disaccharide
▪ Alpha- lactose monohydrate (wet granulation) is most widely used.
▪ Hydrous lactose- causes MAILLARD REACTION- interaction of amine drugs with hydrous
lactose in presence of lubricant like Magnesium Stearate causes yellowish discoloration.
▪ Spray dried lactose: contains 3% moisture, used for direct compression
▪ But it is prone to darkening in presence of excess of moisture, amines, furaldehyde.
▪ Anhydrous lactose- No MAILLARD REACTION
✓ Are added to
provide
improved
cohesion
✓ To allow direct
compression
manufacturing
✓ To enhance flow
✓ To adjust weight
of tablet as per
die capacity
VIVEK SINGH

9. TABLET EXCIPENTS
1) DILUENTS/ FILLERS
Why?
They are used to produce tablet of reasonable size i.e. minimum diameter of 3 mm.
B) STARCH:
▪ It may give rise to softer tablets.
▪ Moisture content- 11-14%
▪ Sta-Rx-1500: free flowing & directly compressible, may act as diluent, binder, disintegrating
agent and self lubricating agent, glidant (0.25%)
▪ Emdex & Celutab: contains 90-92% dextrose, 3-5% maltose. These are hydrolysed starches &
are free flowing & directly compressible.
▪ They are sweet in taste & can be used in place of mannitol.
VIVEK SINGH

10. TABLET EXCIPENTS
1) DILUENTS/ FILLERS
Why?
They are used to produce tablet of reasonable size i.e. minimum diameter of 3 mm.
C) DEXTROSE:
▪ It is used to replace the spray dried lactose to reduce the tablet to darken.
D) MANNITOL:
▪ It has negative heat of solution.
▪ Its slow solubility & pleasant feeling in mouth, used mainly in Chewable tablets.
▪ Non-hygroscopic so can be used in vitamin formulation which are moisture sensitive.
▪ It has poor flow so require higher amount of lubricants.
VIVEK SINGH

11. TABLET EXCIPENTS
1) DILUENTS/ FILLERS
Why?
They are used to produce tablet of reasonable size i.e. minimum diameter of 3 mm.
E) SORBITOL:
▪ It is optical isomer of Mannitol but it is hygroscopic above humilities 65%.
F) SUGAR BASED DILUENTS:
▪ Sugar tab: 90-92% sucrose + 7-10% invert sugar
▪ Dipac: 97% sucrose + 3% dextrins
▪ Nutab: 95% sucrose + 4% invert sugar with small amount of corn starch & magnesium stearate
G) MICROCRYSTALLINE CELLULOSE (AVICEL):
▪ Directly compressible
▪ Avicel 101- Powder form Avicel – 102- Granular form
VIVEK SINGH

12. TABLET EXCIPENTS
1) DILUENTS/ FILLERS
Why?
They are used to produce tablet of reasonable size i.e. minimum diameter of 3 mm.
H) CALCIUM SLATS:
▪ DCP (Dibasic Calcium Phosphate) & Calcium sulphate have low concentration of unbound
moisture.
▪ The bound water of calcium sulphate is not released up to 80 degree Celsius.
▪ DCP is virtually insoluble in water and hence used in conjunction with disintegrating agent.
▪ Calcium based diluents can cause interaction with tetracyclines API.
ACRONYM: Love
MSD
Love- LACTOSE
M- Microcrystalline
cellulose
S- STARCH
D- DICALCIUM
PHOSPHATE
VIVEK SINGH

13. BINDERS & ADHESIVES
SUGARS
NATURAL
SYNTHETIC/
SEMISYNTHETIC
Sucrose,
Glucose
Starch
paste,
Acacia,
Tragacant
h,
Gelatin,
AlginatesHPMC,
PEG,
Polyvinyl
alcohol
GPS versus SCAM
G- GELATIN
P- POVIDONE
S- SUCROSE
Versus
S-STARCH
C- CARBOXYMETHYL
CELLULOSE
A- ACACIA
M- METHYL CELLULOSE
VIVEK SINGH

14. FUNCTIONS OF BINDERS
They give adhesiveness to the powder during preliminary granulation & to
the compressed tablet.
It is utilized for converting powder into granules through a process known as
granulation.
They add to the cohesive strength already available in the diluent.
They are more effective when added out of solution.
Most effective dry binder (used in direct compression): Microcrystalline
cellulose
VIVEK SINGH

15. BINDERS & ADHESIVES
✓ Acacia & Tragacanth- (10-25%): natural origin, so variable in composition easily attacked by
microorganism.
✓ Starch paste- (5-10%) prepared by dispersing starch into water when heated. The paste must
be translucent. On heating starch hydrolysed to dextrin & glucose. While clear paste indicates
complete conversion to glucose.
✓ Cellulose derivatives: used for both alcoholic & aqueous solution, common binder for direct
compression & their aqueous solution is adhesive.
✓ Polyvinyl pyrrolidone (PVP): adhesive in both aqueous or alcoholic solution. Its concentration
used is 0.5- 3%.
✓ Ethyl cellulose- used only with alcoholic solution & can retard the disintegration & dissolution
of drugs.
VIVEK SINGH

16. DISINTEGRANTS
✓ Addition of disintegrants are to increase surface area of the tablet fragments
✓ Addition of disintegrants to overcome cohesive forces that keep particles together in a tablet.
✓ Helps in the fragmentation of the tablet after administration.
✓ Starch- Most commonly used (5-20 %)
✓ Modified starch PRIMOGEL & EXPLOTAB are low substituted carboxy methyl starches (1-8%).
✓ Clays & Bentonite- (10%) it can give off white appearance.
✓ Ac-Di-Sol : internally cross linked sodium carboxymethyl cellulose i.e. Na CMC.
✓ Cross linked Polyvinyl pyrrolidone (PVP): also known as Super Disintegrants. Example- Sodium
Starch glycolate, cross carmellose (cross linked CMC), Cross Povidone, PALACRILLIN K+ - it is a
cation exchange resin.
✓ Sodium glycine carbonate- source of carbon dioxide for effervescent tablets.
VIVEK SINGH

17. MECHANISM OF TABLET DISINTEGRATION
✓ Capillary action
✓ Swelling
✓ Heat of wetting
✓ Particle repulsive forces
✓ Deformation
✓ Release of gases
✓ Enzymatic reactions
“Shriram College of
Commerce A Milestone
for Commerce students”
Shriram- Starch
College of- Chemically
modified starches
Commerce- Cellulose
A- Alginic acid
Milestone for-
Microcrystalline cellulose
Career- Crosslinked
povidone
VIVEK SINGH

18. LUBRICANTS, ANTIADHERENTS & GLIDANTS
✓ Lubricants- they are intended to reduce the friction during tablet ejection between walls of the
tablet and walls of the die cavity in which tablet was formed. Example- Magnesium stearate
✓ Antiadherents- they are used to reduce the sticking & adhesion of tablet powder to the
punches of die wall.
✓ Glidants- they are used to promote the flow of the tablet granules from hopper & reducing the
friction between the particles. Example- Colloidal Silicon dioxide (0.25-5%), calcium &
magnesium stearates (0.25-1%), talc (5%)
✓ NOTE: Talc possess both glidant & lubricant activity (contains iron, so carefully used if any
formula contains drug which breakdown is catalysed by iron)
✓ Lubricants based upon fatty acids are insoluble in water & hence can retard the disintegration
& dissolution time.
VIVEK SINGH

19. LUBRICANTS, ANTIADHERENTS & GLIDANTS
✓ Water soluble lubricants: PEG 6000 (Macrogol 6000 or carbowax), magnesium lauryl sulphate,
fumaric acid.
✓ Microcrystalline cellulose/ Avicel: low coefficient of friction, when compressed MCC particles
deform physically & surfaces from H- bonding. MCC is hygroscopic & water causing the
weakening of interparticulate hydrogen bonds.
❖ MECHANISM OF DISINTEGRANTS:
❖ Those that enhance the action of capillary forces in producing rapid intake of aqueous liquids.
So disintegrant have porous structure & show low interfacial tension towards aqueous fluids.
Rapid penetration by water in the tablet matrix resulting in breakdown of tablet. Example-
starch, MCC, cationic resins, sodium starch glycolate.
❖ Those which swells on contact with water e.g. acacia, Tragacanth. But they produce sticky/
gelatinous mass that resists break up of tablet.
VIVEK SINGH

20. LUBRICANTS, ANTIADHERENTS & GLIDANTS
✓ Glidants: they get absorbed or interposing their particles between those of other compounds
which results in reduction of adhesive tendencies or lower the interparticulate friction system.
So they are also called as flow promoters. Example- Colloidal Silicon dioxide, Starch, Talc
✓ Calcium stearates (Lubricant) can cause Maillard reaction with amine drugs like aminophylline
with lactose.
✓ A common mistake during tablet granulation is adding both disintegrant & lubricant in one
mixing step. This results in disintegrant to be coated with lubricant & often results in both
decrease in disintegrants porosity & decrease in the efficiency of disintegrants.
“Mean Standard Time OR Monthly Season Ticket”
Mean/ Monthly- Metallic stearates
Standard/ Season- Stearic Acid
Time/ Ticket- Talc
FOR LUBRICANTS
VIVEK SINGH

21. COLORS, FLAVORS & SWEETENERS
✓ Lakes: They are dyes that has been absorbed on hydrous {Al(OH)3} oxide and usually employed
as dry powders for coloring. They contain 10-30% of pure dye & maximum up to 50%.
▪ During the wet granulation, care must be taken to prevent colour migration during drying
(mottling) [mainly with soluble dyes]. Colorant should not be more than 2% , flavour oil
maximum up to 0.5- 0.75%.
✓ Mannitol is 72% solvent as sucrose.
✓ Saccharin 500 times sweeter than sucrose but it is carcinogenic in nature.
✓ Aspartame (dipeptide aspartic acid + Phenylalanine) replace saccharin but this aspartame lack
stability in the presence of moisture and it is hygroscopic.
❖ WETTING AGENTS: they are used to increase water uptake & enhancing disintegration &
assisting dissolutions. Example- SLS or Docusate sodium known to enhance the dissolution as it
is anionic in nature which causes destruction of intestinal membranes. These are added when
the drug is hydrophobic in nature.
VIVEK SINGH

22. GRANULATION
❖ Granulation is the process of collecting particles together by creating bonds between them.
Bonds are formed by compression or by using a binding agent.
❖ To improve flow by increasing particle size since larger particles flow more readily than smaller
ones.
❖ To prevent the segregation which is mainly due to differences in the particle size of API and
excipients because granulation produces a homogenous mixture, as in granulation particles
stuck together and cannot separate.
❖ Improves the compressive characteristics.
❖ It reduces the dust.
VIVEK SINGH

23. NEED OF GRANULATION
❖ To avoid powder segregation.
❖ To enhance flow of powders.
❖ To produce uniform mixture.
❖ To produce dust free formulations.
❖ To eliminate poor content uniformity.
❖ To improve compression characteristics.
VIVEK SINGH

24. VIVEK SINGH

25. DIRECT COMPRESSION
API
Diluent
Lubricant
Glidant
Disintegrating agent
Weighing and mixing
Compression
Granulation
Techniques
Direct
Compression
Dry
Granulation
Wet
Granulation
VIVEK SINGH

26. 2
6
Direct Compression: some crystalline substances which can be compressed directly. A directly
compressible diluents are added e.g. microcrystalline cellulose
Disadvantages:
❖ Differences in particle size & bulk density between drug & diluents leads to stratification within
granulation resulting in poor content of uniformity of drug in compressed tablet.
❖ In direct compression, diluents may interact with the drug e.g. Maillard’s reaction (yellow
discoloration between amine groups and hydrous lactose).
❖ Because of dry nature of direct compression a static charge develops which prevents uniform
distribution of drug in the granulation.
❖ The maximum % of non compressible content in direct compression can be up to 30%.
DIRECT COMPRESSION
VIVEK SINGH

27. DIRECT COMPRESSION
❖ No drying stage/ heating, no moisture involvement.
❖ Tablet disintegrates into primary particles rather than granular aggregates, which results
in increase in surface area available for dissolution resulting in faster drug release.
❖ Limitation of direct compression is that it depends upon fluidity & compressibility of
tablet diluents. So it cannot be used for the drug which have low potency i.e. high dose of
active ingredients, in such cases the incorporation of diluents (at least 30%) required for
direct compression leads to larger tablets which are unacceptable.
❖ Most widely used diluents in directly compressible tablets is Avicel/ microcrystalline
cellulose due to its excellent flow property & superior compressibility.
VIVEK SINGH

28. Compression (Dry) Granulation: used when drug is sensitive to heat, moisture e.g. vitamins,
aspirin etc.
➢ Powder blend slugs Screened or milled to produce granular form
Equipments:
❖ Roller Compactor
❖ Chilsonator
❖ Hut’s compactor
Wet Granulation: forms the granules by binding the powder together with an adhesive, instead
of by compaction.
Equipments:
Sigma blade (mixture)
Nauta mixer
Fluidised bed dryer
Littleford lodige mixer/ granulator
Diosna mixer/ granulator
VIVEK SINGH

29. VIVEK SINGH

30. API+ Diluent/ filler
mixing
wetting
granulation
drying
sieving
mixing
compression
Binding agent
+ Water
Lubricant, glidant and
disintegrating agent addition
WET GRANULATION
VIVEK SINGH

31. VIVEK SINGH

32. VIVEK SINGH
Wetting involves the
initial wetting of powder
bed and existing granules
by the granulating fluid to
form nuclei.
At this stage, formed
granules break into
fragments which bind to
other granules forming a
layer of material over the
surviving granule
In coalescence or ball
growth stage, partially
wetted primary particles
& larger nuclei come
together to form granules.
As granules increase in size,
they are consolidated by
compaction forces due to bed
agitation. This phase controls
internal granule porosity & final
granule properties such as
hardness & dissolution

33. ANYQUESTIONS?
VIVEK SINGH