Tablets

Tablets
Is solid pharmaceutical dosage forms containing
drug substances and excipients and prepared
either by compression or molding methods
 Advantages
• Production aspect
– Large scale production at lowest cost
– Easiest and cheapest to package and ship
– High stability
• User aspect (doctor, pharmacist, patient)
– Easy to handle
– Lightest and most compact
– Greatest dose precision & least content variability
– Coating can mark unpleasant tastes & improve pt.
acceptability
– Ease of Administration
 Disadvantages
• Some drugs resist compression into dense
compacts
• Drugs with poor wetting, slow dissolution,
intermediate to large dosages may be difficult
or impossible to formulate and manufacture as a
tablet that provide adequate or full drug
bioavailability
• Bitter taste drugs, drugs with an objectionable
odor, or sensitive to oxygen or moisture may
require encapsulation or entrapment prior to
compression or the tablets may require coating
 Absorption
of drug
from tablets
Essential properties of tablets
• Accurate dosage of medicament, uniform in
weight, appearance and diameter
• Have the strength to withstand the rigors of
mechanical shocks encountered in its
production, packaging, shipping and
dispensing
• Release the medicinal agents in the body in a
predictable and reproducible manner
• Elegant product, acceptable size and shape
• Chemical and physical stabilities
 Types of tablets
• Route of administration
– Oral tablets
– Sublingual or buccal tablets
– Vaginal tablets
• Production process
– Compressed tablets
– Multiple compressed tablets
• Tablet within a tablets: core and shell
• Multilayer tablet
• Sugar-Coated Tablets (SCT)
• These are compressed tablets containing a sugar coating. Such
coatings may be colored and are beneficial in covering up drug
substances possessing objectionable tastes or odors, and in protecting
materials sensitive to oxidation.
• Film-Coated Tablets (FCT) –
• These are compressed tablets which are covered with a thin layer or
film of a water-soluble material. A number of polymeric substances
with film-forming properties may be used. Film coating imparts the
same general characteristics as sugar coating with the added advantage
of a greatly reduced time period required for the coating operation.
• Enteric-Coated Tablets (ECT)
• These are compressed tablets coated with substances that resist
solution in gastric fluid but disintegrate in the intestine. It can be used
for tablets containing drug substances which are inactivated or
destroyed in the stomach, for those which irritate the mucosa or as a
means of delayed release of the medication. 8
• Multiple Compressed Tablets (MCT)
• These are compressed tablets made by more than one compression
cycle.
• Layered Tablets - Such tablets are prepared by compressing
additional tablet granulation on a previously compressed
granulation. The operation may be repeated to produce multilayered
tablets of two or three layers. Special tablet presses are required to
make layered tablets
• Press-Coated Tablets - dry-coated, are prepared by feeding
previously compressed tablets into a special tableting machine and
compressing another granulation layer around the preformed tablets.
• They have all the advantages of compressed tablets, i.e,, speed of
disintegration, etc, while retaining the attributes of sugar-coated
tablets in masking the taste of the drug substance in the core
tablets...
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• Press-coated tablets also can be used to separate incompatible
drug substances
• In addition, they can provide a means to give an enteric
coating to the core tablets. Both types of multiple-compressed
tablets have been used widely in the design of prolonged-
action dosage forms.

• Modified Release Tablets –

• Compressed tablets can be formulated to release the drug
slowly over a prolonged period of time. Hence, referred to as
Prolonged-Release or Sustained-Release or controlled release
dosage forms as well.

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Tablets for Solution:
• Compressed tablets to be used for preparing solutions or imparting
given characteristics to solutions must be labeled to indicate that
they are not to be swallowed. Examples of these tablet: Potassium
Permanganate Tablets for Solution

Effervescent Tablets:
• In addition to the drug substance, these contain sodium bicarbonate
and an organic acid such as tartaric or citric.
• In the presence of water, these additives react liberating carbon
dioxide which acts as a distintegrator and produces effervescence.
• Except for small quantities of lubricants present, effervescent tablets
are soluble.
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• Buccal Tablets:
• These are small, flat, oval tablets.
• Tablets intended for buccal administration by inserting into the
buccal pouch may dissolve slowly; therefore, they are
formulated and compressed with sufficient pressure to give a
hard tablet.
Sublingual tablets:
* Asthose containing nitroglycerin, are placed under the tongue.
• Sublingual tablets dissolve rapidly and the drug substances
are absorbed readily by this form of administration.

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• Molded Tablets [Tablet Triturates (TT]
• Tablet triturates usually are made from moist material using a
triturate mold which gives them the shape of cut sections of a
cylinder. Such tablets must be completely and rapidly soluble.
The problem arising from compression of these tablets is the
failure to find a lubricant that is completely water soluble

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• Hypodermic Tablets (HT)
• Hypodermic tablets are soft, readily soluble tablets and
originally were used for the preparation of solutions to be
injected. Since stable parenteral solutions are now available
for most drug substances, there is no justification for the use
of hypodermic tablets for injection.
• Their use in this manner should be discouraged since the
resulting solutions are not sterile. Large quantities of these
tablets continue to be made, but for oral administration. No
hypodermic tablets ever have been recognized by the official
compendia

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• Dispersible Tablets
– dispersible tablets are designed to disintegrate quickly in the
mouth or disperse in a spoonful of water to become a
suspension.
• Troches (lozenges)
– Name based on shape (diamond). Cough tablets: Throat irritation
• Implant Tablets
• Pills
– pills include tablets, capsules, and variants thereof like caplets—
essentially anything with medication that can be digested, minus
the liquid forms, colloquially falls into the pill category.
• Caplets
– A smooth, coated, oval-shaped medicinal tablet in the shape of a
capsule
• Dental cones
• Chewable tablets
 Processing problems
• a. Capping is the partial or complete separation
of the top or bottom crowns of a tablet from the
main body of the tablet.
• Lamination is separation of a tablet into two or
more distinct layers. Both of these problems
usually result from air entrapment during
processing.

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• b. Picking is removal of a tablet’s surface material by a punch.

• Sticking is adhesion of tablet material to a die wall. These two

problems result from excessive moisture or substances with

low melting temperatures in the formulation

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• c. Mottling is an unequal color distribution on a
tablet, with light or dark areas standing on otherwise

uniform surface. This results from use of a drug with a

color different from that of the tablet excipients or

from a drug with colored degradation products.

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 Tablet Formulation

• Drug

• Diluents
• An inert substance is added to increase the bulk in order to make the
tablet of practical size for compression.
• Diluents used for this purpose include dicalcium phosphate, calcium
sulfate, lactose, cellulose, kaolin, mannitol, sodium chloride, dry
starch and powdered sugar.
• Certain diluents, such as mannitol, lactose, sorbitol, sucrose, when
present in sufficient quantity, can impart properties to some
compressed tablets that permit disintegration in the mouth by
chewing.
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• Selection of the diluent Is based partly on the experience of the
manufacturer as well as on diluent cost and compatibility with
other tablet ingredients
• However, in the formulation of new therapeutic agents, the
compatibility of the diluents with the drug must be considered, e.g:
• calcium salts used as diluents for the broad-spectrum antibiotic
tetracycline have been shown to interfere with the drug’s
absorption from the gastrointestinal tract.
• When drug substances have low water solubility, it is
recommended that water-soluble diluents be used to avoid possible
bioavailability problems.
• Many ingredients are used for several different purposes, even
within the same formulation; e.g, corn starch can be used in paste
form as binder, in dry form as disintegrant.

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• Binders
• Agents used to impart cohesive qualities to the powdered material to
insures the tablet remaining intact after compression, as well as
improving the free- flowing qualities by the formulation of granules of
desired hardness and size.
• Commonly used binders include: starch, gelatin and sugars as sucrose,
glucose, dextrose, and lactose.
• Natural and synthetic gums which have been used include acacia, sodium
alginate, carboxy- methylcellulose, methylcellulose, polyvinyl
pyrrolidone, Veegum. Other agents which may be considered binders
under certain circumstances are polyethylene glycol, ethylcelulose,
waxes, water and alcohol.
• The quantity of binder used has considerable influence on the
characteristics of the compressed tablets.
• The same amount of binder in solution will be more effective than if it
were in a dry form. So it is preferable to incorporate the binding agent in
solution. 22
• Lubricants
• Lubricant functions in tablet manufacture.
1. Prevent adhesion of the tablet material to the surface of the dies and
punches.
2. Decrease friction at particle dye interface
3. Facilitate the ejection of the tablets from the die cavity.
4. May improve the rate of flow of the tablet granulation.
• Most lubricants, with the exception of talc, are used in concentrations less
than 1%. When used alone, talc may require concentrations as high as 5%.
• Anti adherants:
• reduce sticking and adhesion of the tablet granulation or powder to the faces of
the punches or to the die walls.
• Glidants:
• promote the flow of the tablet granulation or powder materials by reducing
friction among particles
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• Disintegrants
• Is a substance, or a mixture of substances, added to a tablet to
facilitate its breakup or disintegration after administration.
• Materials serving as disintegrants have been classified chemically
as starches, clays, celluloses, algins, gums and cross-linked
polymers.
• The oldest and still the most popular disintegrants are corn and
potato starch which have been well-dried and powdered.
• Starch has a great affinity for water and swells when moistened,
thus facilitating the rupture of the tablet matrix.
• Starch 5%, is suggested, but if more rapid disintegration is desired,
this amount may be increased to 10 or 15%.
• Usually disintegration time would decrease as the percentage of
starch increased.

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• A group of materials known as super disintegrants
have gained in popularity. As Croscarmelose,
crospovidone and sodium starch glycolate
• The name comes from the low levels (2 to 4%) at
which they are completely effective.
• Sodium starch glycolate swells 7-12 fold in less than
30 seconds. Croscarmelose swells 4-8 fold in less
than 10 seconds.

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Colors and dyes serve to:
1. Disguise off-color drugs.
2. Provide product identification.
3. Produce a more elegant product.
Food, drug, and cosmetic dyes are applied as solutions;

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• Flavoring agents

Are usually limited to chewable tablets or tablets intended to dissolve

in the mouth.
• (a) Generally, water-soluble flavors have poor stability; hence,
flavor oils or dry powders usually are used.

• (b) Flavor oils may be added to tablet granulations in solvents,

dispersed on clays and other adsorbents, or emulsified in aqueous
granulating agents. Usually, the maximum amount of oil that can
be added to a granulation without influencing its tablet
characteristics is O.5%—O.75%.
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• Artificial sweeteners,
• like flavors, are usually used only with chewable tablets or
tablets dissolve in the mouth.
• (a) Some sweetness may come from the diluent (e.g.,
mannitol, lactose); agents, such as saccharin and aspartame,
can also be added.
• (b) Saccharin has an unpleasant after taste.
• (c) Aspartame is not stable in the presence of moisture.

• Adsorbents
(e.g., magnesium oxide, magnesium carbonate, bentonit, silicon
dioxide) are substances capable of holding quantities of fluid
in an apparently dry state.

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