TABLETS

RPh Saba Inayat Ali

Lecturer
DCOP
DUHS

13.10.2016
LEARNING OBJECTIVES
Describe the advantages and limitations of tablets as dosage forms
Describe the quality attributes of tablets
List and describe different types of tablets
List and describe different excipients used in tablets
Describe three methods of tablet preparation
CONTENTS
INTRODUCTION
ADVANTAGES/ DISADVANTAGES
CHARACTERISTICS
TYPES
FORMULATION ADDITIVES
METHOD OF PREPARATION
TABLETS (Latin tabuletta, Tab.)
Tablet is defined as a compressed solid dosage form
containing medicaments with or without excipients.

Pharmaceutical tablets are solid, flat or biconvex dishes, unit

dosage form, prepared by compressing a drugs or a mixture of
drugs, with or without diluents.
They vary in shape and differ greatly in size and weight, depending on amount of
medicinal substances and the intended mode of administration
 ADVANTAGES
 PRODUCTION ASPECTS
1. Large scale production at lowest cost
2. Easiest and cheapest to package and
ship
3. High stability (chemical, mechanical &
biological)
4. Lightest and most compact
 ADVANTAGES
 FORMULATION ASPECTS
1. Greatest dose precision with least content variability
2. provide special release profile products e.g. enteric or
delayed release tablets
3. Tablets may be formulated to release the therapeutic agent
at a particular site within the gastrointestinal tract to
reduce side effects, promote absorption at that site and
provide a local effect (e.g. ulcerative colitis).
4. Product identification is cheap – embossing or
monogrammed punch face
 ADVANTAGES
 PATIENT ASPECTS
1. Tablets are convenient to use and are an
elegant dosage form.
2. Ease of handling
3. Coating can mark unpleasant tastes &
improve patient acceptability
 DISADVANTAGES
Difficult to swallow in case of children and unconscious patients.
Some drugs resist compression into dense compacts,
owing to amorphous nature, low density character.
The main disadvantage of tablets as a dosage form is the problem of poor
bioavailability of drugs due to unfavorable drug properties, e.g. poor solubility, poor
absorption properties and instability in the gastrointestinal tract.
In addition, some drugs may cause local irritant effects or otherwise cause harm to
the gastrointestinal mucosa
DISADVANTAGES
Bitter tasting drugs, drugs with an objectionable odor or drugs that are sensitive to o
xygen may require encapsulation or coating. In such cases, capsule may offer
the best and lowest cost.
QUALITY ATTRIBUTE OF TABLET
DOSAGE FORM
The tablet should include the correct dose of the drug.
The appearance of the tablet should be elegant, and its weight,
size and appearance should be consistent.
The drug should be released from the tablet in a controlled and
reproducible way.
The tablet should be biocompatible, i.e. not include excipients,
contaminants and microorganisms that could cause harm to
patients.
QUALITY ATTRIBUTE OF TABLET
DOSAGE FORM
The tablet should be of sufficient mechanical strength to
withstand fracture and erosion during handling at all stages of its
lifetime.
The tablet should be chemically, physically and microbiologically
stable during the lifetime of the product.
The tablet should be formulated into a product acceptable to the
patient.
The tablet should be packed in a safe manner.
TYPES OF TABLETS
• Oral tablets
• Tablets used in oral cavity
• Tablets administered by other route
• Tablets used to prepare solution
ORAL TABLETS
Compressed Tablets
Multiple compressed tablets
 Layered Tablet
 Compression coated tablet or Repeat action tablets
Delayed action or enteric coated tablet
Film coated Tablet
Sugar coated tablet
Chewable tablets
TABLETS USED IN ORAL CAVITY
Buccal and sublingual tablets
Troches and Lozenges
Dental cones
TABLETS ADMINISTERED BY OTHER ROUTES
Implantation tablets or depot tablets
Vaginal Tablets
TABLETS USED TO PREPARE SOLUTION

1. Effervescent tablet
2. Hypodermic tablet
3. Dispensing tablet
4. Compressed tablet triturates
TYPES OF ORAL TABLETS
Compressed Tablets
Multiple compressed tablets
 Layered Tablet
 Compression coated tablet or Repeat action tablets

Delayed action or enteric coated tablet

Film coated Tablet
Sugar coated tablet
Chewable tablets
COMPRESSED TABLET
a tablet prepared, usually as a large-scale production, by means of great pressure;
most compressed tablets consist of the active ingredient and a diluent, binder,
disintegrator, and lubricant.
MULTIPLE COMPRESSED TABLETS
LAYERED TABLET
E.g. Admixture containing Phenylephedrin HCl
and Ascorbic Acid with Paracetamol.
Paracetamol + phenylephedrine Hydrochloride → one layer
Paracetamol + ascorbic acid → another layer
MULTIPLE COMPRESSED TABLETS
 COMPRESSION COATED TABLET OR REPEAT ACTION TABLETS

This type of tablet has two parts

internal core
surrounding coat (shell)
COMPRESSION COATED TABLETS
The core is small porous tablet and
prepared on one turret. For
preparing final tablet, a bigger die
cavity in another turret is used in
which first the coat material is filled
to half and then core tablet is
mechanically transferred, again the
remaining space is filled with coat
material and finally compression
force is applied.
This tablet readily lend itself in to a
repeat action tablet as the outer
layer provides the initial dose while
the inner core release the drug later
on.
24.10.2016
COATED TABLETS
SUGAR COATED TABLETS
Compressed tablets may be coated with a colored or an uncolored sugar layer.
The coating is water soluble and quickly dissolves after swallowing.
Time and expertise required in the coating process
Increase in cost
May add 50% to the weight and bulk of the uncoated tablets
SUGAR COATED TABLETS
FILM COATED TABLETS
A film coating is a thin polymer-based coat applied to a solid dosage form such as a
tablet.
The thickness of such a coating is usually between 20-100 µm.
The coating is designed to rupture and expose the core tablet at the desired location
in the GIT
FILM COATED TABLETS
The film is usually colored and has the advantage over sugar coatings in that it is;
more durable
less bulky
less time consuming to apply
ENTERIC COATED TABLETS
 An oral dosage form in which a tablet is coated with a material
to prevent or minimize dissolution in the stomach but allow
dissolution in the small intestine.
ENTERIC COATED TABLETS
This formulation is preferred when;
The API irritates gastric mucosa e.g., aspirin or
strong electrolytes
Drugs that produce nausea and vomiting
API is sensitive to low pH e.g., erythromycin
When it’s necessary to release the drug
undiluted. e.g., intestinal antibacterial,
antiseptic agents, intestinal vermifuge, etc.
ENTERIC COATED TABLETS
Enteric coated tablet is such an example of delayed action tablet.
The commonly used coating agents are:
Pharmaceutical Shellac
Hydroxypropyl methylcellulose phthalate
polyvinyl acetate phthalate
Diethyl phthalate
Cellulose acetate phthalate
CHEWABLE TABLETS
Have a smooth, rapid disintegration when chewed
or allowed to dissolve in the mouth
Antacid tablets
to obtain quick ingestion relief as well as the
antacid dose is too large to swallow and the
activity is related to particle size.
Multivitamin tablet
a patient can take as a daily dose.
BUCCAL TABLET
Flat oval tablets intended to
be dissolved in the buccal
pouch for absorption through
the oral mucosa
Buccal tablets are designed to
erode slowly
Fentanyl (Fentora) tablet for
cancer pain
SUBLINGUAL TABLET
They are to be placed under
the tongue and produce
immediate systemic effect by
enabling the drug absorbed
directly through
mucosal lining of the mouth
beneath the tongue
Isordil sublingual 5mg
for minor heart palpitation
attacks.
TROCHES AND LOZENGES
The tablet is a flat faced at least about 18mm in diameter and meant to suck and
dissolves in the mouth.
The compressed tablet is called troches and the tablets produced by fusion or candy
molding process are
called lozenges.
Flavours and sweeteners are added to make tablets palatable.
TROCHES AND LOZENGES
The tablet generally contains sucrose or lactose and gelatin solution to impart smooth
taste
Lozenges for local action in mouth/ throat are
Antiseptics, antibiotics, demulcents, antitussive agents or astringents
To produce systemic action
multivitamin tablet
DENTAL CONES
These tables are designed to be loosely packed
in the empty socket remaining following a
tooth extraction
to prevent multiplication of bacteria in the
socket by employing a slow releasing
antibacterial compound or
to reduce bleeding by an astringent or
coagulant containing tablet.
 IMPLANTATION TABLETS OR DEPOT
TABLETS
These tablets are inserted into subcutaneous
tissue by surgical procedures where they are
very slowly absorbed over a period of a month
or a year.
VAGINAL TABLETS
undergoes slow dissolution and drug release in vaginal cavity of women
The shape is kept ovoid or pear shaped to facilitate retention in vagina
The tablet should be made compatible with plastic tube inserters which are designed
to place the tablet in the upper region of vaginal tract.
These tablets generally release antibacterial, antiseptics or astringents to treat vaginal
infections or release steroids for systemic absorption.
e.g. Canesten tablet
VAGINAL TABLETS
Effervescent tablet
Due to liberation in CO2 gas, the
dissolution of API in water as well as taste
masking effect is enhanced.
The advantages of effervescent tablets
compared with other oral dosage forms
includes an opportunity for formulator to
improve taste
a more gentle action on patient’s stomach and
marketing aspects.
Hypodermic tablet
These tablets contain one or more readily water
soluble ingredients and are intended to be added in water for injection or sterile
water to form a clear solution which is to be injected by Parenteral route.
FORMULATION
ADDITIVES
 TABLET INGREDIENTS
In addition to active ingredients, tablet contains a number of inert materials
known as additives or excipients. Different excipients are:

Diluent
Binder and adhesive
Disintegrents
Lubricants and glidants
Colouring agents
Flavoring agents
Sweetening agents
DILUENTS
Diluents or fillers; used to increase the mass of tablet,
Anhydrous lactose
Lactose monohydrate
Spray dried lactose
Sucrose
Glucose
Starch
Sorbitol
Microcrystalline cellulose (Avicel)
Mannitol
Dibasic calcium phosphate, etc
Calcium carbonate
BINDER
Binders; used in case of wet granulation method,
added in the form of solution or as a solid in the
powder mix.
SOLUTION BINDER DRY BINDER
• Gelatin • Cellulose
• PVP • Methyl cellulose
• HPMC • PVP
• PEG • PEG
• Sucrose
• Starch
DISINTEGRANT
Disintegrants; facilitates breakdown of tablets when taken orally
Starch
MCC
Sodium starch glycolate
Sodium carboxymethyl cellulose
Crosslinked PVP
GLIDANTS
Glidants; enhance the flow property of the bulk powders within the
hopper and into the die in the tablet press
Silica
Avicel (colloidal silicon dioxide)
Talc
Magnesium stearate
LUBRICANTS
Lubricants; facilitates tablet ejection by reducing the friction between
the walls of machine and tablet surface
•Magnesium stearate
•Stearic acid
•PEG
•Sodium lauryl sulfate
•Sodium stearyl fumarate
•Liquid paraffin
ADSORBENTS
Kaolin
Magnesium oxide
COLORING AGENTS
Masking of off color drugs
Product Identification
Production of more elegant product
COLORING AGENTS
All coloring agents must be approved and certified by FDA
FD & C
D & C dyes
Two forms of colors are used in tablet preparation;
solution in the granulating agent or
Lake form of these dyes
Lakes are dyes absorbed on hydrous oxide and employed as dry powder coloring.
FLAVORING AGENTS
For chewable tablet‐flavor oil are used
SWEETENING AGENTS
For chewable tablets
Sugar
Mannitol
Saccharine (artificial): 500 time’s sweeter than sucrose
Disadvantage: Bitter after taste and carcinogenic
Aspartame (artificial)
Disadvantage: Lack of stability in presence of moisture.
METHOD OF
PREPARATION
25.10.2016
METHOD OF PREPARATION
 Direct compression
 Wet granulation
 Dry granulation
DIRECT COMPRESSION
Direct compression (DC) is by far the simplest means of production of a
pharmaceutical tablet
It requires only that the active ingredient is properly blended with appropriate
excipients before compression
reduced capital, labour and energy costs for manufacture
the avoidance of water for granulation for water sensitive drug substances
DRY GRANULATION METHOD
The ingredients in the formulation are intimately mixed and pre-compressed on
heavy duty tablet machines.
The slug which is formed is ground to a uniform size and compressed into the finished
tablet.
DRY GRANULATION METHOD
SLUGGING
Compression of powder or powder mixture into large tablets or slugs on a
compressing machine
8000-12000 pounds of pressure
Flat-faced
2.5cm (1 inch) in diameter
SLUGGING
ROLLER COMPACTION
WET GRANULATION METHOD
has more operational manipulations
more time-consuming
not suitable for drugs which are thermolabile or hydrolyzable by the presence of
water in the liquid binder
STEPS
1. The powdered ingredients are weighed and mixed intimately by geometric dilution
2. The granulating solution or binder is prepared
3. The powders and the granulation solution are kneaded to proper consistency
4. The wet mass is forced through a screen or wet granulator
5. The granules are dried in an oven or a fluidized bed dryer
6. The dried granules are screened to a suitable size for compression
7. A lubricant and a disintegrating agent are mixed with the granulation
8. The granulation is compressed into the finished tablet
SINGLE PUNCH TABLET PRESS
MULTIPLE STATION TABLET
ROTARY PRESS
CONCLUSION
Among the oral pharmaceutical dosage forms, tablets are
the most popular one, accounting for some 70% of all
ethical pharmaceutical preparations produced (Rubinstein,
2000).
REFERENCE
Ansel’s Pharmaceutical Dosage form and drug delivery systems, 8th edition, Ch# 8
Aulton’s Pharmaceutics, the design and manufacture of medicines, 3rd edition, Ch# 31