TABLETS

Definition: Tablets are solid preparations consisting of one or

more active ingredient obtained by compressing uniform volumes
of particles into various shapes and sizes.
 official tablets are defined as circular discs with either flat or convex faces

 intended for oral administration

 used mainly for systemic drug delivery but also local action
 active ingredients + excipients
 some tablets are ----- swallowed whole
after being chewed
dissolved or dispersed in water
retained in the mouth where drug is liberated.
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
 Formulation aspects
1. Greatest dose precision with least content variability
2. Lend to give special release profile products e.g. enteric or
delayed release tablets
3. Product identification is cheap – embossing or monogrammed
punch face
 Patient aspects
1. Ease of handling
2. Coating can mark unpleasant tastes & improve patient
acceptability
DISAVDANTAGES

 Drugs with poor wetting, slow dissolution,

intermediate to large dosages may be difficult or
impossible to formulate and manufacture as a tablet
that provides 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
Tablets can be classified according to their drug-release
characteristics into:
I. According to drug release rate from the tablet
(USP classification):
a- Immediate-release tablet:
The tablet is intended to be released rapidly after administration, or the tablet is
dissolved and administered as solution. It is the most common type and includes
1- Disintegrating tablet (conventional or plain tablet)
2- Chewable tablets
3- Effervescent tablets
4- Sublingual and Buccal tablets
5- Lozenges

b- Modified-release tablet:
They have release features based on; time, course or location.
-They should normally be swallowed intact.
-Different excipients than immediate release tablets.
-The drug is released from an extended-release tablet slowly at a nearly constant rate.
Delayed-release tablets

The drug is liberated from the tablet some time after administration.
After this period has elapsed, the release is normally rapid.
e.g. Enteric tablet, for which the drug is released in the upper part of
the small intestine after the preparation has passed the stomach.

Multiple compressed tablets

- Tablet within a tablets: core and shell
- Multilayer tablet
Immediate-release tablet:
1- Disintegrating tablet (conventional or plain tablet)
- Disintegrating tablet is the most common type of tablets that is intended to be
swallowed and to release the drug in a relatively short time thereafter, by
disintegration and dissolution (fast and complete drug release in vivo).
- It includes normally the following type of excipients; filler
(with low dose drug), disintegrant, binder, glidant, lubricant and antiadherent.

- Tablet disintegration may be affected by;

1- Choice of the excipients.
2- Production conditions during manufacture.
- Conventional tablet may be single layer or multilayer.
Multilayer tablets are prepared by repeated compression of powders and are made
primarily to separate incompatible drugs from each other.
Steps of drug release from disintegrating tablets
2- Chewable tablets

Chewable tablets are to be chewed and thus mechanically disintegrated in the mouth,
so NO DISINTEGRANT IS INCLUDED IN ITS COMPOSITION.
Flavoring, sweetening and coloring agents are important.
Sorbitol and mannitol are common examples of fillers in chewable tablets, (mannitol
has negative heat of solution which results in cooling effect and also has sweetening
action)

Advantages of chewable tablets:

- Provide quick and complete disintegration of the tablet and thus obtain a rapid drug
effect after swallowing and dissolution.
- Easy administration, especially for infants and elderly people.
- Could be administered when water is not available.
Examples for chewable tablets are;
- Chewable Aspirin tablets (for children in the treatment of rheumatoid and to
prevent clot formations in adults)
-Chewable Antacid tablets
3- Effervescent tablets:

Effervescent tablets are uncoated tablets generally containing acid substances and
carbonates or hydrogen carbonates which react rapidly in the presence of water to
release carbon dioxide. They are intended to be dissolved or dispersed in water
before administration.

Effervescent tablets are dropped into a glass of water before administration during
which CO2 is liberated. This facilitates tablet disintegration and drug dissolution; the
tablet disintegration
should be complete within few minutes.
(Effervescence is a special mechanism for disintegration)
CO2 is created by the reaction between carbonate or bicarbonate and a weak acid
such as citric acid or tartaric acid.
Effervescent tablets are dropped into a glass of water before
administration, during which carbon dioxide is liberated.

facilitates tablet disintegration and drug

dissolution; the dissolution of the tablet
should be complete within a few
minutes.
 Uses of effervescent tablets:
1. Rapid drug action, e.g. analgesic drugs .
2. Facilitate the intake of the drug, e.g. vitamins.

After buffered water Temporarily

Dissolution of solution will increases the pH
tablets be obtained of the stomach

fast drug bioavailability (As drugs are

Rapid emptying of the stomach and
absorbed more effectively in the small
shortening the residence time
intestine than in the stomach)
e.g. analgesics

Drug-induced gastric irritation

can be avoided (short residence
time) e.g. aspirin tablets
As absorption of aspirin in the
stomach can cause irritation
Advantages of effervescent tablets:
1. To obtain rapid drug action, for example analgesics and antacids.
2. To facilitate drug intake, for example vitamins.
3. They are convenient, easy to use, premeasured dosage form as compared with the
powdered dosage forms.
4. They cannot spill as the powdered preparations can.
5. They can be individually packaged to exclude moisture, thereby avoiding the
problem of product instability of the unused contents during storage.

Effervescent tablets package

Effervescent tablets often include a flavor and a colorant.

Effervescent tablets are prepared by direct compression or dry granulation.
Effervescent tablets should be protected from moisture, so that a special package is needed;
each tablet is completely covered with aluminum foil and kept in a water-proof container,
often including a desiccant. Effervescent tablets may be packed in blister packs.
 Effervescent tablets usually contain

Carbonate or Flavor and a A water-soluble

bicarbonate and a colourant lubricant is
weak acid such as preferable in order
citric or tartaric N.B. Binder to avoid a film of
The amount of and hydrophobic
sodium bicarbonate disintegrant are lubricant on the
in an effervescent normally not surface of the water
tablet is often quit included in the after tablet
high (about 1 gram) composition dissolution
4- Sublingual and Buccal tablets:

 They are used for drug release in mouth followed by systemic

uptake of the drug.

 A rapid systemic drug effect can thus be obtained without first-

pass liver metabolism, because the drug diffuses into the blood,
directly through tissues under the tongue in case of sublingual tablets
and through oral mucosa in case of buccal tablets.

 They are often small and porous, the latter facilitating fast
disintegration and drug release.
 Sublingual tablets are placed under the tongue.

Ex. Nitroglycerin sublingual tablet; it exerts its action within two minutes for
rapid relief of "Angina pectoris" attack, because the sublingual area is rich in blood
supply. Nitroglycerine suffers from first-pass metabolism if taken orally. Also other
cardiovascular drug, barbiturates, and vitamins are prepared as sublingual tablet
dosage form.
Disadvantage

1) High dose can not be administered

2) Less area is available for absorption
3) Not suitable for bitter and irritating drugs
4) Less patient compliance
5) No eating, drinking and smoking is allowed
6) Highly ionic drugs can not be administered

19/20
Advantages

1) Rapid absorption
2) Dose reduction
3) Fast on set of action
4) Reduction in side effects
6) Suitable in disease like nausea, vomiting
7) Not required water
Buccal Tablets
 Buccal tablets are small, flat, and oval shaped dosage
form and unlike conventional tablets allow for drinking
and speaking without major discomfort.

 They soften, adhere to the mucosa and are retained in

position until dissolution and/or release is complete

 Can be used for both local and systemic drug delivery

21
Buccal tablets are placed in the side of the cheek for
absorption through oral mucosa.
N.B. Buccal tablets may be also prepared for their local
application.
5-Lozenges
They are tablets that dissolve slowly in the mouth and so release the drug
dissolved in the saliva.
Lozenges may be used for;
- Local medication for mouth or throat, e.g. local anesthetics,
antiseptics and antibiotics.
- Systemic drug uptake.

Compressed lozenges:
are made by using tablet machine with large and flat punches, with high
pressure is applied to produce hard tablets, so that they dissolve slowly in
mouth.

Bradoral® compressed loyenges

for treatment of sore throat
NO DISINTEGRANT IS INCLUDED IN
COMPRESSED LOZENGES COMPOSITION

Other additives (binder and filler) must have pleasant taste

or feeling during dissolution. High concentration of fillers which
are mainly sugars as glucose, sorbitol or mannitol.
High concentration of binder is used. Common binder used in
compressed lozenges is gelatin.
6-ODT
 Orally disintegrating tablets are defined as solid oral
preparations that disintegrate rapidly in the oral cavity
with an in vitro disintegration time of less than 30
seconds, according to FDA guidelines (guidance for
industry; 2008).
Allowing the reduction
in dosing frequency. Modified-release tablet

1-Extended-release tablet 2- Delayed-release tablet

Slowly release the drug in the GIT at a constant rate
Prolonged release and sustained release (12-24 hours) Drug release is delayed due to physiological
- The aim is to increase the time period conditions e.g. pH (a lag period followed by
during which a therapeutic concentration normal release).
level in the blood is maintained The best example is enteric coated tablets, the drug
- To increase the release time for drugs is released in the upper part of the small intestine
that can cause local irritation in the after which the preparation has passed the
stomach or intestine if they are released stomach.
quickly (iron salts) If the drug is sensitive to acid, or is irritant to the
stomach lining, an enteric coating can be used.
Immediate release
tablet

Extended release
Cumulative
tablet
amount of drug
released

Time
II. According to method of manufacturing:
a- Compressed tablet:

It is obtained by compressing uniform volume of particles using "Tablet compression

machine". It's used for large scale production.
b. Molded tablets:

Molding means shaping and hardening of semi- solid mixture of drug and
excipients.
It is obtained using ʺtablet mold“. It is restricted for small-dose tablet and for
small scale production.

Tablet mold
Tablets administered by other routes

These tablets are administered by other routes except for the

oral cavity and so the drugs avoided from passing
through the gastrointestinal tract.

These tablets may be inserted into other body cavities or

directly placed below the skin to be absorbed into
systemic circulation from the site of application.
 Vaginal tablets

 These tablets undergo slow dissolution and drug release

in the vaginal cavity of women. The shape kept ovoid or
pear shaped to facilitate retention in vagina.
 These tablets release generally antibacterial, antiseptics
or astringents to treat vaginal infections or release
steroids for systemic absorption.
 The tablet should be made compatible with plastic tube
inserters which are designed to place the tablet in the
upper region of vaginal tract.
 Implants
 These tablets are inserted into subcutaneous tissue by
surgical procedures where they are very slowly absorbed
over a period of one month or one year.
 A special injector with a hollow needle and plunger is
used to administer the rod shaped tablet for other shapes
surgery is required. The tablets may be pellets cylindrical
or rosette shaped with diameter not more than 8 mm.
They are sterile formulation without excipients and made
hard with large particle size to achieve gradual drug
release. Mainly, these tablets are prepared to deliver
growth hormones.
Coated tablets
Definition:

Coated tablets are defined as tablets covered with one or

more layers of mixtures of various substances with the
intention of (adding) conferring benefits and properties to
the dosage form over the uncoated one.

Press-coating (Enteric-coated tablets) Sugar-coated tablets Film-coated tablets

 Sugar coated tablets:
1- Protect tablets from moisture
2- Mask odor and flavor
3- Elegance

 Film coated tablets:

1- Thin film coat
2- Soluble or insoluble polymer film

 Enteric coated tablets:

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.