Tablets: RPH Saba Inayat Ali Lecturer Dcop Duhs

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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  oxygen 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
Effervescent tablet
Hypodermic tablet
Dispensing tablet
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
The powdered ingredients are weighed and mixed intimately by
geometric dilution
The granulating solution or binder is prepared
The powders and the granulation solution are kneaded to proper
consistency
The wet mass is forced through a screen or wet granulator
The granules are dried in an oven or a fluidized bed dryer
The dried granules are screened to a suitable size for compression
A lubricant and a disintegrating agent are mixed with the
granulation
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

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