TABLETS

-BY IQRA RAHAT

M.PHARM(PHARMACEUTICS)
 TABLET
o Tablet is defined as a compressed solid dosage
form containing medicaments with or without
excipients.

 According to I.P. “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.

 70% of the total medicines are dispensed in the

form of tablets
 ADVANTAGES OF TABLET DOSAGE
FORM

o They are unit dosage form which

offers greatest dose precision and least
content variability .

o Cost is lowest of all oral dosage form.

o Easiest and cheapest to package and

strip.

o Easy to swallow .
o Lighter and compact.

o Sustained release product is possible by enteric coating.

o Objectionable odour and bitter taste can be masked by

coating technique.

o Greatest chemical and microbial stability over all oral

dosage form.
DISADVANTAGES OF TABLET DOSAGE FORM

 Difficult to swallow in case of children and unconscious

patients.

 Some drugs resist compression into dense compacts,

owing to amorphous nature, low density character.
 Drugs with poor wetting, slow dissolution properties, optimum
absorption high in GIT may be difficult to formulate or
manufacture as a tablet that will still provide adequate or full
drug bioavailability.

 Bitter tasting drugs, drugs with an objectionable odour or drugs

that are sensitive to oxygen may require encapsulation or
coating. In such cases, capsule may offer the best and lowest
cost.
 DIFFERENT TYPES OF TABLETS
(A) Tablets ingested orally:
 1. Compressed tablet, e.g. Paracetamol tablet

 2. Multiple compressed tablet

 3. Repeat action tablet

 4. Delayed release tablet, e.g. Enteric coated

 5. Sugar coated tablet, e.g. Multivitamin

tablet
 6. Film coated tablet, e.g. Metronidazole tablet .

 7. Chewable tablet, e.g. Antacid tablet

(B) Tablets used in oral cavity:

 1. Buccal tablet, e.g. Vitamin-c tablet

 2. Sublingual tablet, e.g. Vicks Menthol tablet

 3. Troches or lozenges

 4. Dental cone
(c) Tablets administered by other route:

 1. Implantation tablet

 2. Vaginal tablet, e.g. Clotrimazole tablet

(D) Tablets used to prepare solution:

 1. Effervescent tablet, e.g. Dispirin tablet (Aspirin)

 2. Dispensing tablet, e.g. Enzyme tablet (Digiplex)

 3. Hypodermic tablet
 Compressed tablets:
These tablets are prepared by compression
technique in which tablets are not coated with
any materials.

Multiple compressed tablets: Multiple

compressed tablets are formulated when two
or more active pharmaceutical ingredients are
needed to be administered simultaneously and
if they are incompatible.
1. To separate physically or chemically
incompatible ingredients.
2. 2. To produce repeat action or prolong
action product.
 Repeat action
Sugar coated or multiple compressed tablets are used for this
purpose .The core tablet is usually coated with shellac or an
enteric polymer so that it will not release its drug in stomach but
intestine.

 Delayed action and enteric-coated tablet:

This dosage form is intended to release the drug after some time
delay or after the tablet has passed one part of the GIT into
another. E.g. enteric coated tablets to avoid release drug in
stomach but to release in intestine.
 Sugar coated tablet: These are
compressed tablets which are coated with
sugar, in order to mask the bitter taste or
odor of the drug.

 Film coated tablet:

These are compressed tablets covered with
a thin layer or film of a water soluble
material. A number of polymeric
substances may be used for film coating.
Film coating imparts the same general
characteristics as sugar coating , in
addition it offers reduced time period
required for the coating operation.
 Chewable tablet: These are intended to be
chewed in the mouth before swallowing. Used for
the patients who have difficulty in swallowing
tablets whole or for children who have not yet
learn to swallow.
 Buccal and sublingual tablet: These tablets are
small, flat and are intended to be held between
the cheek and teeth or in cheek pouch (buccal
tablet) or below the tongue (sublingual tablet).
Drugs used by this route are for quick systematic
action. The tablets are designed not to be
disintegrate but slowly dissolve.
 Troches and lozenges: Used in the oral cavity to
exert local effect in mouth and throat. They are
commonly used to treat sore throat or to control
coughing in common cold. They may contain
local anesthetics, antiseptic, antibacterial agents
and can dissolved in 30min.
 Dental cone: These tablets are designed
to be placed in the empty socket
remaining after tooth extraction. Main
purpose is to prevent microbial growth
in the socket or to reduce bleeding.

 Implantation tablets: These tablets are

inserted into subcutaneous tissue by
surgical procedures or by using a
special injector where they are very
slowly absorbed over a period of a
month or a year.

 Vaginal tablets: These are designed to

undergo slow dissolution and drug
release in vaginal cavity. Tablets are ,
used to treat vaginal infection.
 Effervescent tablets: Tablets produce a solution
rapidly with the release of carbon dioxide. The
tablets are prepared by compressing the active
ingredient with mixture of organic acid such as
citric acid or tartaric acid and sodium bicarbonate.

 Dispersible tablets: Tablets are intended to be

added to a given volume of water to produce a
solution of a given drug concentration.

 Hypodermic tablets: These tablets are composed

of one or more drugs with water soluble
ingredients. Drug is added to sterile water to
prepare sterile solution, which is injectable.

 Tablet triturates: Usually are made from moist

materials using a triturate mold, which gives them
the shape of cylinder. Such tablet must be
completely and rapidly soluble.
 TABLET PREPARATION
 Tablets are usually prepared by compression technique which
includes various ingredients,
like-:
 Diluents

 Binder and adhesive

 Disintegrents

 Lubricants and glidants

 Colouring agents

 Flavoring agents

 Sweetening agents
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.They must be non toxic

2. They must be commercially available in acceptable grade

3. They must be physiologically inert

4. They must be physically & chemically stable by themselves & in

combination with the drugs.

5. They must be free from all microbial contamination.

6. They do not alter the bioavailability of drug.

7. They must be color compatible.

Some commonly used Diluents are:

Lactose
Calcium sulphate dihydrate
Mannitol
Sorbitol
Directly Compressed Starch
Sucrose
Dextrose
2. Binders and Adhesives:
Binders are either added in wet form or dry form, which
serves as a binding agent in the formulation. Commonly used
binders includes starch, carboxy methyl cellulose, acacia.The
type of the binders added vary with the formulation. The
amount of binder added and type of binder influences the
tablet properties.

3. Disintegrants: Added to a tablet formulation to facilitate its

breaking or disintegration when it comes to contact in water
in the GIT. Disintegrants like starch, clays, cellulose are used.
 Superdisintegrants: Swells up to ten fold within 30 seconds
when contact water.
Example: Crosscarmellose- cross-linked cellulose,
Crosspovidone- cross-linked povidone (polymer), Sodium starch
glycolate- cross-linked starch.

 Lubricant and Glidants: Lubricants are intended to prevent

adhesion of the tablet materials to the surface of dies and
punches, reduce inter particle friction and may improve the rate
of flow of the tablet granulation. For ex- Stearic acid,Magnesium
Stearate.
Glidants are intended to promote flow of granules
or powder material by reducing the friction between the
particles. Ex- Starch and Talc .
 Coloring agent: The use of colors and dyes in a tablet has three
purposes:
(1) Masking of off color drugs
(2) Product Identification
(3) Production of more elegant product All coloring agents must be
approved and certified by FDA. Example: FD & C yellow 6-
sunset yellow FD & C yellow 5- Tartrazine FD & C green 3- Fast
Green
 Flavoring agents: For chewable tablet- flavor oil are used in
order to impart flavour or odour to the tablet formulation
 Sweetening agents: Sweetining agents are added in order to
mask the bitter taste of the drug. Ex: aspartame, mannitol, lactose.
 METHODS OF TABLET
MANUFACTURING
There are three methods by which tablets are manufactured;
1.Wet granulation
2. Dry granulation
3. Direct compression
Manufacturing process is dependent on several factors,
including the compression properties of the therapeutic agents,
the particle size of the therapeutic agent, excipients and the
chemical stability of the therapeutic agent during the
manufacturing process.
 STEPS IN MANUFACTURE OF
TABLETS
 1. Mixing of the therapeutic agents with the excipients.

 2. Granulation of the mixed powders(this is not performed in

direct compression)

 3. Mixing of the powders or granules with other

excipients(mostly lubricants)

 4. Compression into tablets

 5. The details of each of these steps will vary depending on the

manufacturing method used.
 WET GRANULATION
 It is most commonly used method for the manufacturing of
tablets.
 Water is frequently used as the granulation fluid (and heat is
employed to dry the formed granules), it is important to ensure that
the therapeutic agent is chemically stable during the granulation
process.
 The wet granulation exhibit sufficient mechanical properties to be
subsequently exposed to other unit operations, Eg: film coating.
 Tablet quality is directly affected by the choice and concentration of
binder and the type and volume of granulation fluid. Due to the
number of unit operations
to the required, the manufacture of tablets by wet granulation is not as
efficient as other methods. eg:
direct compression
 ADVANTAGES & DISADVANTAGES
Advantages:-

 1. Reduced segregation of formulation components during

storage and processing. Leading to reduced intra and inter batch
variability.

 2. It uses low concentration of therapeutic agent.

 3. It is not dependent on the inclusion of special grades of

excipients (is spray dried excipients used in direct compression
method).
4. Tablets produced by wet granulation are amenable to post
processing unit operations, eg: tablet coating techniques.

Disadvantages:

1.It has several processing steps

2.Heat is required to remove the solvent. This may result in the

degradation of thermo labile therapeutic agents.
 DRY GRANULATION
 When tablet ingredients are sensitive to moisture and
unable to withstand elevated temperature during drying
and when the tablet ingredient have insufficient cohesive
properties, in that case dry granulation is carried out
 This technique is used in preparation of aspirin, aspirin
combination, acetophenetidin.
Excipients used in this method:
 1. Diluents/ filler: anhydrous lactose/ lactose
monohydrate, starch, dibasic calcium phosphate, and
MCC
 2. Disintegrants: Starch, MCC, Sodium starch glycolate,
Croscarmellose sodium, Crospovidone.

 3. Lubricants: Stearates (Mg. stearate, steric acid), Glyceryl fatty

acid esters, polyoxyethylene stearates, SLS.

 4. Glidants: Talc, Colloidal silicon dioxide.

 5. Miscellaneous Excipients: Colours, sweetening agents, etc

 ADVANTAGES & DISADVANTAGES
This technique popularity has decreased in recent years,
having been superseded by direct compression. However
both slugging and roller compaction are still employed in
tablet manufacture.
Advantages:
 1. Both roller compaction and slugging require
conventional grades of excipients.
 2. These methods are not generally associated with
alterations in drug morphology during processing.
 3. No heat or solvent are required so no effect on
thermoliable drugs.
 Disadvantages:
 1. Specialist equipment is required for granulation by roller
compaction.
 2. Seggregation of components may occur during post mixing.

 3. There may be issues regarding powder flow.

 4. The final tablets produced by dry granulation tend to be softer

than those produced by wet granulation, rendering them more
difficult to process using post tabletting techniques, eg: film
coating.
 5. Slugging and roller compaction lead to the generation of
considerable dust. Therefore there may be a reduction in the yield
of tablets.
 DIRECT COMPRESSION
 Direct compression is a process by which tablets are compressed
from powder mixture of API and suitable excipients.No
pretreatment of the powder blend by wet or dry granulation
procedure is required. Directly compressible Excipients:
1. Diluents/filler: Dicalcium phosphate, Mannitol, Sorbitol, MCC.
2. Disintegrants: MCC (eg: Avicel) pregelatinised starch
(starch1500), Sodium starch glycolate, Croscarmellose and
Sodium Crospovidone.
3. Lubricants: Magnesium stearate, stearic acid, Sodium stearyl
fumarate. 4. Glidants: Talc, Colloidal Silicon dioxide.
 ADVANTAGES:
 1. There are fewer processing steps and therefore the method is
potentially more cost effective than other methods.

 2. Direct compression does not require the use of water or other

solvents. Therefore negates potential problems regarding the
stability of therapeutic agents in the presence of the solvents. In
addition heating is not required in direct compression.

 3. Lubrication is performed in the same vessel as powder mixing,

thereby reducing both transfer losses and contamination of
equipment.
 DISADVANTAGES:
1. Special grade excipients are required.
2. The quality and uniformity of the final dosage form depends on
the excipients.
3. There may be issues regarding powder flow into the tableting
machine.
4. The final tablets produced by direct compression tend to be
softer than those produced by wet granulation, rendering them
more difficult to process using post tableting techniques, eg: film
coating
5. It is not used if a colourent is required in the formulation due to
the mottled appearance of the resulting dosage form.
 EVALUATION OF TABLET
 General Appearance: The general appearance of a tablet, its
identity and general elegance is essential for consumer
acceptance, for control of lot-to-lot uniformity and tablet-to-
tablet uniformity. The control of general appearance involves
the measurement of size, shape, color, presence or absence of
odor, taste etc.
 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.
 2. 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.
 Organoleptic properties: Color distribution must be uniform with
no mottling. For visual color comparison compare the color of
sample against standard color.

Mottling of Tablets
 Hardness and Friability:

(b) Tablet hardness can be defined as the force required breaking a

tablet in a diametric compression. In this test the tablet is placed
between two anvils, force is applied to the anvils, and the crushing
strength that just causes the tablet to break is recorded. Generally
used Hardness testers are:
 Monsanto Tester

 Pfizer Tester

 Erweka Tester
Monsanto Hardness Tester
 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.
 (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.
wt.variation= initial wt-final wt/initial wt*100

< 80mg- deviation upto 10% is allowed

80-250mg - deviation upto 7.5% is allowed
>250 mg- deviation upto 5% is allowed
 (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.
 Disintegration Test (U.S.P.): The U.S.P. device to test
disintegration uses 6 glass tubes that are 3 inch 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 1-L 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 5-6 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: 5-30 minutes

 Coated tablet: 1-2 hours

 Disintegration Test (U.S.P.):
 Dissolution can be defined as the amount of drug
substance that goes into solution per unit time under
standardized conditions of liquid/solid interface,
temperature and solvent composition.
 Ensuring the sufficient bioavailability is the key aspect
during the development of a new per oral dosage form.
 For the solid dosage forms, the bioavailability can be given
by the release rate of an active pharmaceutical ingredient
(API) from the dosage form. The release rate can be
determined in vitro by the dissolution test.
 This test is provided to determine compliance with the
dissolution requirements where stated in the individual
monograph for dosage forms administered orally
Dissolution Medium—A suitable dissolution medium is used. Use
the solvent specified in the individual monograph. The volume
specified refers to measurements made between 20° and 25°.
If the Dissolution Medium is a buffered solution, adjust the
solution so that its pH is within 0.05 unit of the specified pH
given in the individual monograph.

Time—Where a single time specification is given, the test may

be concluded in a shorter period if the requirement for
Procedure minimum amount dissolved is met. Specimens are
to be withdrawn only at the stated times within a tolerance of
±2%.