TABLETS
PHARM.D 4th SEMESTER
INTRODUCTION
According to the USP, tablets are solid dosage forms,
containing medicinal substances with or without
suitable diluents.
In the European Pharmacopoeia, tablets are defined as
‘solid preparations each containing a single dose of one
or more active substances
…
Tablets are available in a wide variety of shapes, sizes, colors, and
surface markings
They may differ greatly in size and weight, depending on the amount
of drug substance present and the intended method of administration
They may also vary in hardness, thickness, disintegration,
and dissolution, characteristics and in other aspects,
depending on their intended use and method of
manufacture.
Most tablets are used in the oral administration of drugs. Many of
these are prepared with colorants and coatings of various types.
Other tablets, such as those administered sublingually, buccally, or
vaginally, are prepared to have features most applicable to their
particular route of administration
Tablets are prepared primarily by compression, with a
limited number prepared by molding.
Compressed tablets are manufactured with tablet
machines capable of exerting great pressure in
compacting the powdered or granulated material (Fig.
8.1A and B).
Their shape and dimensions are determined by the use
of various shaped punches and dies
Molded tablets are prepared on a large scale by tablet
machinery or on a small scale by manually forcing
dampened powder material into a mold from which the
formed tablet is then ejected and allowed to dry.
…
Some tablets are scored, or grooved, which allows them to be
easily broken into two or more parts. This enables the patient to
swallow smaller portions as may be desired, or when prescribed,
it allows the tablet to be taken in reduced or divided dosage.
…
Some tablets that are not scored are not intended to be
broken or cut by the patient since they may have special
coatings and/or drug release features that would be
compromised by altering the tablet's physical integrity.
ADVANTAGES
(a) Precision and low content variability of the unit dose
(b) Low manufacturing cost
(c) Easy to package and ship
(d) Simple to identify
(e) Easy to swallow
(f) Appropriate for special-release forms
(g) Best suited to large-scale production
(h) Most stable of all oral dosage forms
(i) Essentially tamperproof
DISADVANTAGES
(a) Some drugs resist compression into tablets.
(b) poor bioavailability of drugs due to unfavourable drug
properties, e.g. poor solubility, poor absorption properties
and instability in the gastrointestinal tract.
(c) Some drugs (e.g., those with an objectionable taste or
odor, those sensitive to oxygen or atmospheric moisture)
require encapsulation or entrapment before compression.
These drugs are more appropriate in capsule form.
TYPES OF TABLETS
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Most commercial tablets can be divided into two general classes:
whether they are made by compression or molding.
1. Compressed tablets are manufactured with tablet machines
capable of exerting great pressure in compacting the powdered or
granulated material
2. Molded tablets are prepared on a large scale by tablet machinery
or on a small scale by manually forcing dampened powder
material into a mold from which the formed tablet is then ejected
and allowed to dry.
Tablets are used mainly for systemic drug delivery but may also
be used for local drug action
…
Tablets for oral ingestion are designed to be swallowed
intact, with the exception of chewable tablets.
Tablets may be coated for a number of reasons: to mask the
taste, color, or odor of the drug; to control drug release; to
protect the drug from the acid environment of the stomach;
to incorporate another drug and provide sequential release
or avoid incompatibility; or to improve appearance.
…
1. Compressed Tablet (CT)
Compressed tablets are formed by compression.
They are made from powdered, crystalline, or granular
materials, alone or in combination with binders,
disintegrants, controlled-release polymers, lubricants,
diluents, and, in many cases, colorants.
The vast majority of commercialized tablets today are
compressed tablets, either in an uncoated or coated state.
In addition to the medicinal agent or agents, compressed tablets usually contain a
number of pharmaceutical excipients, including the following:
Diluents or fillers, which add the necessary bulk to a formulation to prepare tablets of
the desired size
Binders or adhesives, which promote adhesion of the particles of the formulation,
allowing a granulation to be prepared and maintaining the integrity of the final tablet
Disintegrants or disintegrating agents, which promote breakup of the tablets after
administration to smaller particles for ready drug availability
Antiadherents, glidants, lubricants, or lubricating agents, which enhance the flow of
the material into the tablet dies, minimize wear of the punches and dies, prevent fill
material from sticking to the punches and dies, and produce tablets with a sheen
Miscellaneous adjuncts such as colorants and flavorants
After compression, tablets may be coated with various materials as described later.
Tablets for oral, buccal, sublingual, or vaginal administration may be prepared by
compression.
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2. Multiple Compressed Tablets
Multiple compressed tablets are prepared by subjecting the fill
material to more than a single compression
The result may be
a) a multiple-layer tablet or
b) a tablet within a tablet, the inner tablet being the core and the
outer portion being the shell
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Layered tablets are prepared by compressing a tablet
granulation around a previously compressed granulation. The
operation is repeated to produce multiple layers
Each layer may contain a different medicinal agent, separated for
reasons of chemical or physical incompatibility, staged drug release,
or simply the unique appearance of the layered tablet.
Usually, each portion of fill is a different color to produce a
distinctive-looking tablet.
In preparation of tablets within tablets, special machines are
required to place the preformed core tablet precisely within the die
for application of surrounding fill material
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3. Sugar-Coated Tablets (SCT)
Sugar-coated tablets are compressed tablets surrounded by a coloured or
uncoloured sugar coating
The coating may be added to
a) protect the drug from air and humidity,
b) to provide a barrier to a drug’s objectionable taste or smell, or
c) to improve the appearance of the tablet and permits imprinting of
identifying manufacturer’s information.
Among the disadvantages to sugarcoating tablets are the time and expertise
required in the coating process and the increase in size, weight, and shipping costs.
Sugarcoating may add 50% to the weight and bulk of the uncoated tablet
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4. Film-Coated Tablets
Film-coated tablets are compressed tablets coated with a thin
layer of a polymer capable of forming a skin-like film.
The film is usually colored and has the advantage over sugar
coatings in that it is more durable, less bulky, and less time-
consuming to apply.
The film typically increases tablet weight by only 2% to 3%
By its composition, the coating is designed to rupture and
expose the core tablet at the desired location in the
gastrointestinal tract
5. Gelatin-Coated Tablets
A recent innovation is the gelatin-coated tablet.
The innovator product, the gelcap, is a capsule- shaped
compressed tablet that allows the coated product to be
about one-third smaller than a capsule filled with an
equivalent amount of powder.
The gelatin coating facilitates swallowing, and gelatin-
coated tablets are more tamper evident (designed to provide
a visual indication if a package has been opened or
tampered with before reaching the consumer) than unsealed
capsules.
Examples include Tylenol Cold Multi- Symptom Daytime.
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6. Controlled-Release Tablets (CRT)
These tablets, as well as capsule versions, can be categorized into
three types:
1) those that respond to some physiological condition to release the
drug, such as enteric coatings;
2) those that release the drug in a relatively steady, controlled
manner; and
3) those that combine combinations of mechanisms to release pulses
of drug, such as repeat action tablet
Extended Release, Sustained Release, Prolonged Release, Delayed
Release, Repeat Action etc
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7. Enteric-Coated Tablets (ECT)
Enteric-coated tablets have delayed-release features.
Enteric-coated tablets are compressed tablets coated with substances that
resist solution in gastric fluid but disintegrate in the intestine.
Enteric coatings can be used for
a) tablets containing drug substances inactivated or destroyed in the
stomach,
b) for those that irritate the mucosa, or
c) as a means of delayed release of the medication.
Enteric-coated tablets are a form of delayed-action tablet. However, not
all delayed-action tablets are enteric or are intended to produce an
enteric effect.
They are designed to pass unchanged through the
stomach to the intestines, where the tablets
disintegrate and allow drug dissolution and
absorption and/or effect.
Enteric coatings are employed when the drug
substance is destroyed by gastric acid or is
particularly irritating to the gastric mucosa or
when bypass of the stomach substantially
enhances drug absorption.
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8. Repeat-action tablets
Repeat-action tablets are layered or compression-coated tablets in
which the outer layer or shell rapidly disintegrates in the stomach.
The components of the inner layer or inner tablet are insoluble in
gastric media but soluble in intestinal media
9. Extended-Release Tablets
Extended-release tablets (sometimes called controlled-release
tablets) are designed to release their medication in a
predetermined manner over an extended period
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10. Chewable Tablets
Chewable tablets, which have a smooth, rapid disintegration
when chewed or allowed to dissolve in the mouth, have a
creamy base, usually of specially flavored and colored
mannitol.
Chewable tablets are especially useful for administration of
large tablets to children and adults who have difficulty
swallowing solid dosage form
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11. Buccal and Sublingual Tablets
Buccal and sublingual tablets are flat, oval tablets intended to be
dissolved in the buccal pouch (buccal tablets) or beneath the
tongue (sublingual tablets) for absorption through the oral
mucosa.
They enable oral absorption of drugs that are destroyed by the
gastric juice and/or are poorly absorbed from the gastro intestinal
tract.
Buccal tablets are designed to dissolve slowly, whereas those for
sublingual use (such as nitroglycerin [NTG]) dissolve promptly
and provide rapid drug effects
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Lozenges or troches are disc-shaped solid dosage forms
containing a medicinal agent and generally a flavoring
substance in a hard candy or sugar base.
They are intended to be slowly dissolved in the oral
cavity, usually for local effects, although some are
formulated for systemic absorption.
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11. Effervescent Tablets
Effervescent tablets are prepared by compressing granular
effervescent salts that release gas when in contact with water.
These tablets generally contain medicinal substances that dissolve
rapidly when added to water.
The “bubble action” can assist in breaking up the tablets and
enhancing the dissolution of the active drug
Effervescent tablets are used to obtain rapid drug action, for
example for analgesic drugs or to facilitate the intake of the drug,
for example for vitamins.
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12.Tablet Triturates
Tablet triturates are small, usually cylindrical, molded, or compressed
tablets containing small amounts of usually potent drug
Tablet triturates are usually made from moist material, using a
triturate mold that gives them the shape of cut sections of a cylinder.
Such tablets must be completely and rapidly soluble.
Today, only a few tablet triturate products are available commercially,
with most of these produced by tablet compression.
Since tablet triturates must be readily and completely soluble in
water, only a minimal amount of pressure is applied during their
manufacture
A combination of sucrose and lactose is
usually the diluent. The few tablet triturates
that remain are used sublingually, such as
NTG tablets.
Pharmacists also employ tablet triturates in
compounding. For example, triturates are
inserted into capsules or dissolved in liquid
to provide accurate amounts of potent drug
substances.
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13. Hypodermic Tablets
Hypodermic tablets are soft, readily soluble tablets and were originally 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.
They were originally used by physicians in extemporaneous preparation of
parenteral solutions.
The required number of tablets was dissolved in a suitable vehicle, sterility
attained, and the injection performed.
The tablets were a convenience, since they could be easily carried in the
physician’s medicine bag and injections prepared to meet the needs of the
individual patients.
However, the difficulty in achieving sterility and the availability of prefabricated
injectable products, some in disposable syringes, have eliminated the need for
hypodermic tablets.
14. Dispensing Tablets
Dispensing tablets are no longer in use.
They might better have been termed compounding tablets
because the pharmacist used them to compound prescriptions;
they were not dispensed as such to the patient.
Dispensing tablets provide a convenient quantity of potent drug
that can be incorporated readily into powders and liquids, thus,
circumventing the necessity to weigh small quantities
The tablets contained large amounts of highly potent drug
substances, so the pharmacist could rapidly obtain premeasured
amounts for compounding multiple dosage units.
These tablets had the dangerous potential of being inadvertently
(without intention; accidentally.) dispensed as such to patients.
15. Molded Tablets
Certaintablets, such as tablet triturates, may be prepared
by molding rather than by compression.
The resultant tablets are very soft and soluble and are
designed for rapid dissolution.
16. Immediate-Release Tablets
Immediate-release tablets are designed to disintegrate
and release their medication with no special rate-
controlling features, such as special coatings and other
techniques.
17. Vaginal Tablets
Vaginal tablets, also called vaginal inserts, are
uncoated, bullet-shaped, or ovoid tablets inserted into
the vagina for local effects.
They are prepared by compression and shaped to fit
snugly on plastic inserter devices that accompany the
product.
They contain antibacterials for the treatment of
nonspecific vaginitis caused by Haemophilus
vaginalis or antifungals for the treatment of
vulvovaginitis candidiasis caused by Candida
albicans and related species.