Tablets.pptx

Tablet
s
By- Miss.Vaishali P.
Wasnik
Assistant Professor
P. R. Patil Institute of
Pharmacy Talegaon ( S.P.)

VPW, PRP, Talegaon (s.p.)
Tablets-
Tablets are unit dosage form in which one
usual dose of the drug has been accurately
placed.

Adavantages & Disadvantages
 Advantages
 Unit dosage form, greatest
dose precision and least
content variability.
 Lowest cost
 Lightest and most compact
form
 Easiest and cheapest to
package
 Product identification is
also cheap no additional
processing required
 Provide greatest ease of
swallowing.
 Special release profile can
formed
 Chemical, Mechanical and
microbiologic stability.
 Suitable for large scale
production
 Disadvantages
 Some drugs not suitable
for compression
(amorphous, flocculents ,
low density )
 Drugs with por wetting ,
slow disslution,
intermediate to large
dosage are difficult to
formulate into tablet.
 Bitter tasting, objectional
odor, drugs sensitive to
oxygen may require
coating
 ( capsule prefer at low
cost)

Tablets used for Ingestion
1. Compressed Tablets or Standard
compressed Tablets
- Standard uncoated tablets made by
compression- wet granulations,
double compaction or direct
compression.
- Rapid disintegration & drug release
- Most of tablets containing drugs
which gives local effect.( GIT- Water
insoluble drugs – Antacids and
adsorbents)
- Some drugs produced systemic effect
( aqueous solubility- Disintegrate and
dissolve in GI contents)

2. Multiple compressed Tablets
Tablets used for Ingestion
Layered
Tablet
Compression
coated
Tablet
- Either two components or three components
systems
- A tablet within a tablet
- Tablet within tablet within a tablet.

3. Chewable Tablets
- Chew in mouth prior to swallowing & not intended to
be swallowed intact.
- Infants and children or for elderly
- Bitter and foul tasting drugs not suitable.
- E.g.- Antacid tablets
- ( large dose of antacid can be given and better acid
neutralization)

4. Sugar and Chocolate coated
-

5. Film coated Tablets
- Polymers such as Hydroxypropyl
cellulose (HPC), Hydroxypropyl
methyl cellulose(HPMC), widely
used with suitable plasticizer.
- Advantages
• Better mechanical strength
• Avoid sugar for significant
segments of population
• Retain debossed markings
• Tasteless Tablet
• - Disadvantge
• Physical appearnce ( Elegancy) not
match with sugar coated tablets.

6. Repeat action Tablets
- The core of tablet is coated with shellac or an
enteric polymer so drug not releases into stomach.
- Second dose added into sugar coatings.
Immediate release
Delayed release

7. Delayed action And Enteric coated Tablets
- Enteric coated Tablets are a type of delayed action
tablet.
- But not all types of delayed type of tablets are
enteric.
- Why enteric coating?
 Some drugs irritate gastric mucosa (Aspirin)
 Some drugs destroyed in stomach (Erythromycin)
 For local effect in intestine( antibacterial,
Vermifuge)
- Cellulose acetate phthalate, polyvinyl acetate
phthalate, HPMC phthalate
- Acid esters ( insoluble in GI media)
- Esterases in intestinal fluid break down ester
linkages.

8. Controlled release Tablets

Tablets used for oral cavity
1. Buccal & Sublingual Tablets
- These tablets are small & somewhat flat
- Buccal tablets intended to be held between the
cheek and teeth or in the cheek pouch
- Sublingual tablets intended to held beneath the
tongue.
- Drugs administered by this route are intended to
produce systemic effects.
- The drugs used for this kind of tablets must have
good absorption properties through oral mucosa.
- By using this route of administration , first pass
metabolism of drugs are avoided.

Advantages
- The drugs which are
degraded in GI environment
like steroids, hormones,
may be avoided as the well
absorbed from mouth.
- More rapid onset of action
- First pass effect may be
avoided
- No disintegration required
- These tablets formulated by
excipients which do not
stimulate salivation.
- 15-30 min period slow
dissolution is required for
effective absorption.

2. Troches & Lozenges
- They are intended to exert local
effect in the mouth or throat.
- These tablets forms are
commonly used to treat sore
throat or to control coughing in
the common cold.
- They may contain local
Anesthetics, Antiseptics,
Antibacterial & Antitussives.
- Lozenges also called cough
drops
- Made with the drug and
flavored hard candy sugar by
compression or fusion or by a
candy moulding process.
- Troches made by compression.

3. Dental cones
- These are minor tablets
that are designed to be
placed in empty socket
after tooth extraction.
- Use- To avoid infection
- To reduce bleeding
- Tablet slowly dissolve or
erode for 20-40 min.

Tablets administered by other routes
1. Implantation Tablets
- Implantation or depot tablets are designed for
subcutaneous implantation in animals or man.
- To provide prolonged drug effect ( Months to Years)
- These tablets are small , cylindrical or rosette
shape & not more that 8 mm in length.
- Drawback- Needs surgical technique for
administration and Discontinue therapy.
- Tissue toxicity problem
- Special injecter ( Kern injecter) for rod shaped
tablets.

2. Vaginal Tablets
- Vaginal tablets are designed to undergo slow
dissolution and drug release in vaginal cavity.
- The tablet are oval or pear shaped to improve
retention into vagina.
- These tablets used to release antibacterial,
antiseptics or astringents to treat vaginal
infections.
- To release steroids for systemic absorption.
- Vehicle used for these tablets is slowly soluble
material .
- Plastic tube inserter is used to place the tablet in
upper vaginal tract.

Tablets used to prepare solutions
1. Effervescent Tablets
- Designed to produce solution rapidly with release
of CO2
- Prepared by compressing Organic Acids ( citric
acid, tartaric acid and sodium bicarbonate)
- When tablet comes in contact with water a
chemical reaction initiated.
- The reaction is rapid ( 1 Min)
- Such tablet produce flavored carbonated drink
which mask the taste of certain drug.
- Fro producing clear solution the drug must be
soluble in alkaline pH.
- Advantages- Preparing a solution containing an
accurate dose of drug
- Disadvantage
- Difficult to produce chemically stable product

2. Dispensing Tablets
- These tablets are intended to be added to a given
volume of water by the consumer to produce a
solution of a given drug concentration.
- Silver proteinate
- Bichloride of mercury
- Merbromin
- Quaternary ammonium compounds
- Buffering tablets and isotonicity tablets.

3. Hypodermic Tablets
- These tablets composed of one or more drug with
other readily water soluble ingredients and are
intended to be added to sterile water or water for
injection.
4. Tablets triturates
- These are small , cylindric, molded or compressed
tablets.

Excipients , Formulation of Tablet

Criteria for selection of excipients for tablet
1. They must be non toxic and acceptable to the
regulatory agencies in all countries where the
product is to be marketed.
2. They must be commercially available in an
acceptable grade in all countries where the product
is to be manufactured.
3. Their cost must be acceptably low.
4. They must not be contraindicated by themselves or
because of a component in any segment of
population.
5. They must be physiologically inert.

6. They must be physically and chemically stable by
themselves and in combination with drug and other
tablet components.
7. They must be free of any unacceptable microbiologic
“load”.
8. They must be color compatible.
9. If drug product is also classified as food , the diluent
and other excipients must be approved direct food
additives.
10. They must have no deleterious effect on the
bioavailability of the drugs in the product.

Formulation Components
Diluents
Binders and adhesive
Disintegrants
Lubricants,Antiadherents and Glidants
Colors
Flavours
Sweeteners

Diluents
Diluents are fillers designed to make up the
required bulk of the tablet when the drug
dosage itself is inadequate to produce this
bulk.
 Round tablets- 3/16 to 1/2 inch.
 Below 3/16 inch difficult to handle by
elderly.
 Larger than ½ inch become difficult to
swallow.

Tablet weight range- 120 to 700 mg
Diluents for secondary purpose
• To provide better tablet properties like cohesion
• To permit use of direct compression
manufacturing
• To promote flow
• Tablet formulator should remember that physical
and chemical interactions between formulation
components may be promoted by the intimate
contact between potential reactants that are
tightly compressed together in a tablet compact.
e. g.( Lactose + magnesium stearate)= Gradual
Discoloration of tablet
( Maillard reaction)

Lactose-
- Most widely used
- Have no reaction with most drugs
- Anhydrous lactose does not undergo Maillard
reaction
- For wet granulation Hydrous form of lactose is used.
- Two grade are available- Coarse(60-80 mesh)
- - Regular ( 80-100 mesh)
- Lactose granules show rapid drying , good drug
release and disintegration.
- Low cost diluent
- Spray dried lactose available for direct compression
with good flow property.
- Spray dried lactose prone to darkening in the
presence of excess moisture and amines- so
Neutral or acid lubricants should be used.

Strach-
- Corn, wheat, potato
- USP grade has poor flow property and
compression and have high moisture content 11-
14%.
- Directly compressible starches available
commercially
- Sta-Rx-1500- Binder, diluent and Disintegrating
agent
It contains 10% moisture and and prone to
softening when combined with excessive amount of
magnesium stearate.
- Emdex and Celutab – Hydrolysed starches ( 90-
92% dextrose + 3-5% maltose)
- They are free-flowing and directly compressible
- Replaces manitol in chewable tablet due to
sweet taste and smooth feeling in mouth.

Dextrose-
- Cerelose- Hadrate and anhydrous form
- Sometimes replace with spray dried lactose
Mannitol-
- Most expensive sugar
- Negative heat of solution
- Slow solubility
- Pleasant feeling in mouth
- Non hygroscopic
- Poor flow property so require high amount of
lubricants.
Chewable
tablet
Vitamins

Sorbitol-
- Optical isomer of mannitol
- Sometimes combine with mannitol formulations to
reduce cost
- It is hygroscopic at humidities above 65%.
Sucrose-
- Sugartab ( 90-93% sucrose + 7-10% invert sugar)
- DiPac ( 97% sucrose + 3% Modified dextrins)
- Nu Tab ( 95% sucrose + 4% invert sugar + Corn
starch and magnesium stearate)
- Directly compressible
- Used with mannitol for chewable tablet
- All grades hygroscopic at elevated moistures

-Microcrystalline cellulose-
- Avicel
- Directly compressible
- Two grades – pH 101 ( Powder)
- - pH 102 ( Granules)
- Good flow property
- Acts as disintegrating agent
- Expensive

Binders
Either added as dry or liquid
Wet granulation
To promote cohesive compacts.
Accacia & Tragacanth
- 10- 25% alone or in combination.
- More effective when used in solutions than dry
form.
- Heavily contaminated with bacteria.
- To reduce microbial proliferation – Wet granualation
masses quickly dried

Gelatin-
- Used in combination with accacia.
Starch Paste-
Starch +
Water
During heating , starch
hydrolysed to Dextrin and
Glucose
Translucent Paste is
Formed

-Liquid Glucose- 50 % solution in water is used as wet
granulating agent.
- Produce hard but somewhat brittle compacts.
- Low cost adhesive
- Bacterial proliferation may be a problem
- Modified natural plymers like alginates and cellulose
derivatives- ( MC, HPMC, HPC)
- Polyvinylpyrolidone is a synthetic polymer – used as
dry binder

Disintegrants
A disintegrant is added to most
tablet formulation to facilitate a
brekup or disintegrantion of the
tablet when it contacts water in
the GIT.
- It draws the water into the tablet
, swelling and causing the tablet
to burst apart.
- DA mixed at two stages
i) During the formation of
granules, prior to wetting the
granulating fluid.
(Intragranular)
ii) At the second mixing stage
during compaction of granules
into tablet (Extragranular)

- Starch USP and other starch derivatives
- Range 5-20% of tablet weight.
- Modified starches- Primogel and Explotab are used
in lower concentarion 1-8% - 4% is Optimum.
- Pregelatinised starches- used in 5% concentarion.
- Clays
- Veegum HV & Bentonite- 10%
- But produces offwhite color so limitedly used
- Microcrystalline cellulose
- Super disintegrants
 Sodium starch glycolate,
 Crospovidone,
 Croascarmellose and
 polacrilin poatassium

Lubricants , Antiadherents and
Glidants
A material that is primarily described as an
Antiadherents is typically a lubricant , with some
Glidant properties as well.
- Lubricants- these are intended to reduce the friction
during tablet ejection between the walls of the tablet
and the walls of the die cavity in which the tablet was
formed.
- Antiadherents- These are added for the purpose of
reducing sticking or adhesion of any of the tablet
granulataion or powder to the faces of the punches or
to the die wall.
- Glidants- These are intended to promote flow of the
tablet granulation or powder materials by reducing
friction between the particles.

-Most widely used Lubricants have been stearic acid and
various stearic acid salts and derivatives.
Calcium and magnesium salts of stearic acid are the
most common salts .
Talc-
Most of talc samples are found to contain trace
quantities of iron.
So talc is care fully added in those formulations
containing drug whose breakdown is catalysed by the
presence of iron.
Polyethylene glycols and some polymeric surfactants
used as water soluble lubricants. ( Less effective)

Talc, magnesium stearate and starch as well as starch
derivatives possess Antiadherents property.
Glidants
Talc- 5%
Corn starch- 5-10%
Colloidal silicas such as Cab-O-Sil, Syloid , Arrosil-
0.25-3% ( gives Drier environment)

Colors, Flavours and Sweeteners
Why colors are used?
- Disguising off color drugs
- Product identification
- Production of more elegant product.
Natural colors
- Availability is limited
- Unstable
- Two types of colors typically used in tablet
preperation
- 1) FD&C
- 2) D&C dyes
- Lakes & dyes use as a dry powder for coloring
- Water soluble dyes & pastel shades show least
mottling.

Flavours- Specially for chewable and other tablets that
dissolve in mouth.
- Water soluble flavours have found little acceptance
because of poor stability.
- Flavour oils are added to tablet granulation in
solvents, or dispersed on clays or emulsified in
aqueous granulating agents
Sweeteners
- Mannitol 72% as sweet as Sucrose
- Saccharin - Artificial sweetener- 500 time sweet
than sucrose
But it has bitter aftertaste and it is carcinogenic
- New artificial sweetener to replace the Saccharin is
Aspartame
- It lacks stability in the presence of moisture.

Tablet Manufacturing
Granulation Methods
and Compression of Tablet

The Manufacture of granulations for tablet compression
may follow one or combination of three established
methods
- Direct compression
- Compression granulation
- Wet granulation

Direct Compression-
Few crystalline substances like Sodium chloride,
sodium bromide and potassium chloride that may be
compressed directly.
Single substance
having good
compressibility
No Disintegration
Tablet
Drug
Disintegrant
May interfere
compressibility

Direct compression materials possessing good flow and
compressibility.
Inert, tasteless, reworkable. Able to disintegrate and
inexpensive.
Advantage of Direct compression
• Simple process
• Low labor input
• Economic
• Dry process so deterioration is decreased
• Tablet disintegrate into their primary particle rather
than granules
• Increased surface area for dissolution so faster drug
release.

Limitations
• Differences in particle size and bulk density between the
drug and diluent---------Stratification--------poor content
uniformity ( Low dose drug)
• Large dose drug having moderate compressibility may
create problem in direct compression process. ( diluent may
increase tablet weight and cost)
• Some times direct compression diluent may react with
drug.( Spray dried lactose + Amines= Yellow discoloration)
• Static charge build up during routine screening and mixing
which may prevent uniform distribution of drug .

Dry or Compression Granulation
When the effective dose of a drug is too high for direct
compaction
When drug is sensitive to heat , moisture or both .
e. g. Aspirin and Vitamins are prepared by compression
granulation.
Compaction of components of tablet by means of tablet
press or specially designed machinery, followed by
milling and screening prior to final compression of
tablet.
Slugging- large tablets ---------- Coarse milling-------
Screening --------Produce granular form with good flow
ability than previous powder form.

Equipment-
Large scale – Specially designed machine ------
Roller compactor

Wet granulation-
 Binding of powders together with an adhesive.
 Solution, suspension or slurry of binder which is added
to powder.
 At initial stages liquid film will be formed on powder
surface and may combine to produce discrete liquid
bridges at point of contact.
 Surface tension and negative capillary pressure in such
bridges provide the cohesive force and result in
condition called pendular state
 As the liquid content increases several bridges
produced giving rise funicular state
 More liquid added---mass kneaded to bring particles into
closer proximity-no void spaces -------bonding is affected
by interfacial forces at the granule surface and by
negative capillary pressure--------Capillary state

Further addition of liquid result in droplet formation
Particles are held together by surface tension but
without intergranular forces ------weak structures
Capillary state ------- Maximum strength of wet
granules

Wet screening
• To increase particle contact point and increase
surface area for drying
• Converting the moist mass into coarse , granular
aggregates by passage through a hammer mill or
oscillating granulator
• Drying --- to remove moisture
• After drying again screening

Tablet Compression Operation
Basic Components
1. Hopper- for holding and
feeding granulation to be
compressed.
2. Dies that define the size
and shape of the tablet
3. Punches for compressing
granulation within dies
4. Cam tracks for guiding the
movement of the punches.
5. A feeding mechanism for
moving granulation from
the hopper into dies

Multi station presses ------------Rotary
- Die table- rotate
- A) Feed frame –which has several interconnected
compartments
- B) Dies---- compartments spread the granulation
- C) The pull down cam- guides the lower punches
- D) Wipe off blade – At end of feed frame to remove
excess granulation
- E) Weight control cam– reduces the fill in dies to the
desired amount
- F) Lower compression roll- lower punches travel
over lower compression roll
- G ) Upper compression roll—Upper punches travel
over upper compression roll
- H) Upper punch raising cam-
- I) Lower punch ride up cam-

Compression machine Tooling
Each tooling set consist of A
die and upper and lower
punches.
BB tooling---
Length--2.5inch
Barrel diameter- 0.75 inches
Head diameter- 1 inch
B Tooling---
Lower punch length- 3 9/16
inch
D tolling--- for large tablets
Barrel diameter- 1 inch
Head diameter- 1 ¼ inch
Length- 5.25 inch

Dies for Above punches
 Outside diameter--- 0.945 inch
• 7/16 inch round tablet
• 9/16 inch capsule shaped tablet
 Outside diameter----1 3/16 inch
• 9/16 inch round tablet
• ¾ inch capsule shaped tablet
-Generally steel used to manufacture compression
tooling.
- Size , shape is unlimited
- Company names or symbols, trade names, dosage
strength or National drug code can be cut or
engraved into punch face.

Evaluation of Tablet
 General Appearance
 Size and Shape
 Unique identification markings
 Organoleptic Properties
 Hardness
 Friability
 Drug content and Release
 Content Uniformity
 Disintegration
 Dissolution

https://upload.wikimedia.org/wikipedia/com
mons/5/5a/Tablet_press_animation.gif
By Jeff Dahl - Own work, CC BY-SA 4.0,
https://commons.wikimedia.org/w/index.ph
p?curid=3606080
https://youtu.be/4xggZRckfTE

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Editor's Notes