Unit-II - TABLETS

HISTORY
 Pills are thought back to around 2400 BC. In earlier medical recipes were for liquid

preparation rather than solids.

 In ancient Egypt it was prepared by bread dough, honey as medicinal ingredients, such

as plant powder or spices were mixed in and formed by hand to make little balls.

 In ancient Greece, such medicines were known as ‘Katapotia’ (Which means-

“something to be shallowed”.

 Roman scholer Pliny in about 50-55AD, introduced first name it to ‘Pill’. At that time

it called ‘Pilula’.

 In 1843, british inventer William Brockedon was granted a patent for a machine

capable of shaping pills, lozenges etc.

 INTRODUCTION
• Tablets are compressed solid unit dosage form containing
medicament or medicaments with or without excipients.

• According to pharmacopoeia pharmaceutical tablets are solid unit

dosage form usually circular in shape and may be flat or biconvex,
prepared by compressing a drugs or a mixture of drugs, with or
without diluents.

• It is the most popular dosage form and 70% of the total medicines
are dispensed in the form of tablet.

• Maximum all medicaments are available in the tablet form except

where it is difficult to formulate or administer.
 General Properties Of Tablet
1. A tablet must be strong and hard to withstand mechanical shock
during manufacturing, packing, shipping, dispensing and use.

2. The drug content of the tablet must be bioavailable that is, the
tablet must be able to release its content uniformly.

3. The tablet must be able to release the medicinal agents in a

predictable and reproducible manner.

4. The tablet must be chemically and physically stable to maintain its

chemical and physical attributes during manufacture, storage, and use.

5. The tablet should have elegant product identity which is free from any
tablet defect like cracks, discoloration etc.

6. Tablets must be uniform in weight and in drug content.

 ADVANTAGES
• Easy to administered.
• Easy to dispense.
• Greatest chemical and microbial stability overall all oral
dosage form.
• Accuracy in dose.
• Bitter and nauseous substance can be easily dispensed by
the help of various coating techniques.
• Light and compact.
• Cost is lowest among all oral dosage form.
• Sustained release product is possible by enteric coating.
• Suitable for large scale production.
• Easiest and cheapest in packaging than the other oral dosage
form.
 DISADVANTAGES
• Problem with compression to crystalline drug.
• Hygroscopic drugs are not suitable for compressed
tablets.
• Drugs with low or poor water solubility, slow
dissolution, may be difficult to formulate.
• Cost of production may be increase because of coating
and encapsulation to remove bitter and unpleasant taste.
• Swallowing is difficult especially for children and ill
(unconscious) patients.
 TABLET
CLASSIFICATION
TABLET CLASSIFICATION
1. Ingested Orally
 Compressed Tablet
 Multiple Compressed Tablets
 Sugar-coated Tablets
 Film-coated Tablets
 Enteric-coated Tablets
 Sustained/Controlled Release Tablets

2. Used in Oral Cavity

 Chewable Tablets
 Buccal Tablets
 Sublingual Tablets

3. Used to prepare Solution

 Effervescent Tablets
 Hypodermic Tablets

4. Administered by other routes

 Implantable Tablets
 Vaginal Tablets
 TYPES OF TABLETS
• Compressed tablets
• Multiple Compressed Tablets
• Sugar-coated Tablets
• Film-Coated Tablets
• Immediate-Release Tablets
• Effervescent Tablets
• Enteric-coated Tablets
• Chewable Tablets
• Buccal and Sublingual Tablets
• Rapid-release Tablets
• Extended Release Tablets
• Sustained Release Tablets
• Layered Tablets
• Tablet Triturates
• Vaginal Tablets
 COMPRESSED TABLETS
• Compressed tablets represent a significant proportion of tablets that are
clinically used to provide systemic administration of therapeutic agents either in
an uncoated state or in a coated state.

• These tablets are designed to provide rapid disintegration in the gastric fluid
following ingestion hence, allowing rapid release of the drug and, ultimately,
systemic absorption of the dosage form.

• Compressed tablets are formed by compression of powdered, crystalline, or

granular materials into the required geometry by the application of high
pressures, utilizing steel punches and die.
 COMPRESSED TABLETS
• In addition to the Active Pharmaceutical Ingredient(s) (APIs), compressed
tablets usually contain a number of pharmaceutical excipients e.g., bulking
agents, disintegrants, binders, lubricants, controlled-release polymers and
other miscellaneous adjuncts such as colourants and flavourants which serve
different and specialized purpose during tablet manufacture, storage, and use.
Examples of compressed tablets include tablets for oral, buccal, sublingual, or
vaginal administration.
COMPRESSION OF TABLETS
COMPRESSION OF TABLETS
• Compressed tablets are prepared by compression techniques.
MULTIPLE COMPRESSED TABLETS/
MULTI-COMPRESSED TABLETS
• Multiple compressed tablets, also called multi-compressed tablets
are tablets that are composed of two or more layers. These tablets
are prepared by subjecting the fill material to more than one
compression cycle.
• The result may be a multiple-layer tablet or a tablet within a tablet,
the inner tablet being the core and the outer portion being the shell.
In other hand, it may be in different layers.
 MULTIPLE COMPRESSED TABLETS/
MULTI-COMPRESSED TABLETS
• Multiple compressed tablets can also be used when there is a need to mask
the bitter taste of a drug substance or where the drug substance in
question is irritant to the stomach. There are three sub-classes of multiple
compressed tablets and they include compression coated tablets, layered
tablets.
 SUGAR-COATED TABLETS
• These are compressed tablets that have been coated with concentrated sugar
solution to improve several types of factors, such as:
 Patient’s compliance

 Masking tastes or odours

 Increase stability and/or modify the release of therapeutic agents

 Increase appearance

• Sugar coating was once quite common but lost commercial appeal due to the
time and expertise required in the coating process, the increase in size and
weight of coated tablets, high cost of process validation and shipping.

• Examples of some API used in sugar-coated tablets are: Dried ferrous sulphate
BP 200mg, Ibuprofen tablet BP 200mg etc
 SUGAR-COATED TABLETS
Steps involved in sugar Coating of Tablets:
Sugar coating of tablets steps includes; waterproof or seal coating to sub-
coating, smooth coating for coloring finishing, polishing, and last Printing as
discussed below:
 Sealing (Seal Coat)
 Sub-Coating
 Smooth coating
 Color coating
 Polishing
 Printing
SUGAR-COATED TABLETS
SUGAR-COATED TABLETS
 FILM-COATED TABLETS
• Film-coated tablets are conventional tablets coated with a thin layer of
polymer (e.g., hydroxypropyl methylcellulose, hydroxypropyl cellulose) or
a mixture of polymers capable of forming a skin-like film.
• The film is usually coloured and also impacts the same general
characteristics as sugar coating with the added advantage of being more
durable, less bulky, and less time-consuming to apply.
• By its composition, the coating is designed to break and expose the core
tablet at the desired location in the gastrointestinal tract.
• Advances in material science and polymer chemistry have made these
coatings the first choice for formulation scientists.
FILM-COATED TABLETS
FILM-COATED TABLETS
Polymers for enteric film coating formulation
 FILM-COATED TABLETS
IDEAL CHARACTERISTICS OF FILM COATED TABLETS
 Film-coated tablets should have even coverage with uniform colour
coverage across the surface of each dosage unit within a batch, and
from batch to batch.

 Film-coated tablets must be free from defects. In any kind of defect which
affect functionality and stability of the finished product.

 Film-coated tablets must be compliant with finished product specifications

and any relevant consistent drug manufacturing requirements.
 IMMEDIATE-RELEASE TABLETS
• Immediate-release tablets are tablets designed to disintegrate and
release their medication with no special rate-controlling features, such
as special coatings and other techniques.
• Immediate release tablets are those which disintegrate swiftly and get
dissolved to release the medicaments.
• This type of tablets are able to provide advantages of liquid
medication in the form of solid preparation.
• This is the most common type of tablet and examples include,
chewable, effervescent, sublingual and buccal tablets.
 EFFERVESCENT TABLETS
• Effervescence is the evolution of bubbles of gas (carbon dioxide) from a
liquid as the result of a chemical reaction between acids and bases.
• Effervescent tablets are uncoated tablets that generally contain organic
acids (such as tartaric or citric acid) and sodium bicarbonate in addition
to the medicinal substance or API.
• They react rapidly in the presence of water by releasing carbon dioxide
which acts as a disintegrator to produce either a drug suspension or an
aqueous solution.
 EFFERVESCENT TABLETS
• These tablets are prepared by compressing granular effervescent salts
(organic acid and bicarbonate) with the medicinal substances.
• These tablets are to be protected from atmospheric moisture during
storage. So these tablets should be stored in well-closed air-tight
containers.
• Example: Dispirin tablet (Aspirin)
EFFERVESCENT TABLETS
 Effervescence reaction:

3NaHCO3 (aq) + H3C6H5O7 (aq) → 3H2O (aq) + 3CO2 (g) + 3Na3C6H5O7 (aq)
Sod. Bicarbonate Citric acid carbon dioxide

Effervescence is the evolution of bubbles of gas (carbon dioxide) from a

liquid as the result of a chemical reaction between acids and bases. The
reaction proceeds spontaneously when the acid and carbonate components
are mixed in water, even with a very small amount as a catalyzing agent.
Because water is one of the reaction products, it will accelerate the rate of
reaction, leading to difficulty in stopping the reaction.
 CHEWABLE TABLETS
• Chewable tablets are big sized tablets which are difficult to swallow and
thus, are chewed within the buccal cavity prior to swallowing.
• They are especially useful for administration of large tablets to children and
adults who have difficulty swallowing conventional tablets or antacid
formulations in which the size of the tablet is normally large and the
neutralisation efficacy of the tablet is related to particle size within the
stomach.
• Chewable tablets are not conventionally used if the drug has issues
regarding taste acceptability.
• Examples of chewable tablets: chewable antacid of magnesiumtrisilicate
tablet B.P.
 CHEWABLE TABLETS
• Chewable tablets are prepared in such a way that they can easily be crushed
by chewing. They are usually formulated for patients who have difficulty in
swallowing tablets.
• As soon as chewing starts in the mouth, the tablet is broken down into
smaller particles from where dissolution and subsequent absorption
occurs to effect the desired pharmacologic action. The increased
bioavailability from chewable tablets resulting from increased absorption
rate due to its dissolution or being chewed in the mouth into the
gastrointestinal tract in solution or granule form is the major advantage
over conventional solid tablets or capsules which are absorbed mainly after
disintegration and dissolution.
 CHEWABLE TABLETS
EXCIPIENTS USED IN THE FORMULATION OF CHEWABLE TABLETS
 Diluents: These are added to chewable tablet formulations to
increase the bulk volume of the tablet. When mixed with the
drug substance, the final product is given adequate weight and
size to assist in production and handling. Diluents commonly
used in chewable tablets include:
 Mannitol
 Sorbitol
 Dextrose
 Lactose
 Sucrose
 CHEWABLE TABLETS
 Flavouring agent: Flavourants are commonly used to impart pleasant
flavour and often odour to chewable tablets. Various group of
flavours for general baseline taste types are shown below.
 CHEWABLE TABLETS
 Sweetening agents: Sweeteners are added primarily to chewable tablets when the
commonly used carriers such as mannitol, lactose, sucrose, and dextrose do not
sufficiently mask the taste of the active substance or components. In these cases, the
sweetening agents are used to artificial enhance the overall sweetness impact.
Common sweeteners used in pharmaceutical products include:
 Aspartame
 Glycyrrhizin (Magnasweet)
 Saccharin
 CHEWABLE TABLETS
Colourants: Colourants are used in the manufacture of chewable
tablets for the following reasons:
1. Production of more elegant product.
2. To aid in product identification and differentiation
3. To mask unappealing or non-uniform colour of raw materials
4. To complement and match the flavour used in the formulation
 CHEWABLE TABLETS
ADVANTAGES
1. Patient convenience; can be taken at any required time and place when
water is not available.
2. Increased bioavailability resulting from increased absorption rate, due to
its dissolution or being chewed in the mouth into the gastrointestinal tract
(GIT) in solution or granule form.
3. Improved patient acceptance (especially pediatric) through pleasant taste.
4. Possible to use as a substitute for liquid dosage forms where immediate
pharmacological action is desired.
5. The large size of the dosage form is difficult to swallow. In such cases,
chewable tablet offers advantages over it.
6. Effectiveness of therapeutic agent is improved by the reduction in size
that occurs during mastication of tablets before swallowing.
 CHEWABLE TABLETS
DISADVANTAGES
1. Bitter or foul-tasting drugs are not good candidates for chewable tablet
formulation.
2. Chewable tablets contain sorbitol which may causes diarrhoea.
3. The presence use of flavouring agents in chewable tablet may cause ulcer
in the oral cavity.
4. Prolonged chewing of chewable tablet results in pain in facial muscles.
5. Chewable tablets are hygroscopic in nature, so must be kept in a dry
place.
6. They show the fragile, effervescence granules property.
7. Since these tablets have insufficient mechanical strength, so careful
handling is required.
BUCCAL AND SUBLINGUALTABLETS
• Buccal and sublingual tablets are small, flat, oval shaped tablets that
are intended to be dissolved in the buccal pouch (buccal tablets) or
beneath the tongue (sublingual tablets) for absorption through the
oral mucosa to produce a systemic effect.
BUCCAL AND SUBLINGUALTABLETS
• These tablets are employed to achieve either rapid absorption
into the systemic circulation e.g. glyceryl trinitrate sublingual
tablets or alternatively, to enable oral absorption of drugs that
are destroyed by the gastric juice and/or are poorly absorbed
from the gastrointestinal tract.
 ENTERIC-COATED TABLETS
• The term “enteric” refers to the small intestine; therefore, enteric
coatings resist breakdown of medication before it reaches the small
intestine.
• Enteric-coated tablets are compressed tablets that have delayed-
release properties. They are coated with polymeric substances (such
as cellulose acetate phthalate/cellulose acetate butyrate;
hydroxypropyl methyl-cellulose succinate; and methacrylic acid co-
polymers) that resist solution in gastric fluid but disintegrate and
allow drug dissolution and absorption in the intestine.
 ENTERIC-COATED TABLETS
• Enteric coatings are primarily employed when the drug substance is
inactivated or destroyed by gastric acid (e.g., erythromycin) or is
particularly irritating to the gastric mucosa (e.g., non-steroidal anti-
inflammatory drugs) or when bypass of the stomach substantially
enhances drug absorption.
• Example of enteric-coated tablets includes Diclofenac sodium
delayed-release tablet USP 100mg.
 GENERAL TIMEFRAME
 Gastric Emptying:
In a fasted state, the stomach can empty relatively quickly, with 90% emptied within
approximately 30 minutes.
However, with a meal, especially a high-fat one, gastric emptying can take several hours (e.g.,
more than 6 hours for a high-calorie, high-fat breakfast).
 Small Intestinal Transit:
Once in the small intestine, the transit time is typically more consistent, ranging from
approximately 3 to 7 hours.
It is essential to understand that the timing and nature of food intake can significantly impact
how quickly a tablet travels from the stomach to the small intestine, potentially affecting the
medication's absorption and effectiveness.
Why the small intestine is better at absorption than the
stomach?
i. Surface Area: The small intestine has circular folds, villi (finger-like projections), and
microvilli (even smaller projections on the villi). This increased surface area allows for
efficient contact with the digested food and maximizes nutrient uptake. In fact, the surface
area of the small intestinal mucosa is estimated to be around 30 square meters (320 sq ft),
compared to less than 1 square meter for the stomach.
ii. Specialized Cells: The small intestine contains various specialized cells, including enterocytes
(primary absorptive cells), goblet cells (secrete mucus), Paneth cells (secrete antimicrobial
peptides), and enteroendocrine cells (secrete hormones that regulate digestion and absorption).
iii. Enzyme Activity: The small intestine receives digestive juices and enzymes from the
pancreas, liver, and its own walls, which are crucial for breaking down food into absorbable
forms.
iv. Blood and Lymphatic Supply: The small intestine has a rich blood supply through arteries
branching from the celiac trunk and mesenteric arteries. This allows the rapid transport of
absorbed nutrients to the liver and other parts of the body for storage or use.
 ENTERIC-COATED TABLETS

Enteric coatings are employed when the drug substance is inactivated

or destroyed in the acid secretion of the stomach or is particularly
irritating to the gastric mucosa or when bypass of the stomach
substantially enhances drug absorption.
 ENTERIC-COATED TABLETS
 Reasons for the application of enteric coatings:
Enteric coatings are applied to dosage forms for the following
reasons:
i. To protect the acid-labile drug substances from the acidic pH of
gastric acid. Such drug substances include erythromycin,
pancreatin, omeprazole etc.
ii. To prevent gastric distress/ulceration or nausea due to irritation
caused by certain drugs such as aspirin and certain nonsteroidal
anti-inflammatory compounds.
iii. To deliver drugs that are optimally absorbed in the small intestine
to their primary absorption site in their most concentrated form.
iv. To provide a delayed release component to repeat action tablets.
 RAPID-RELEASE TABLETS
• Rapid-release tablets, also called rapidly dissolving tablets, rapidly
disintegrating tablets, orally-dispersible tablets, quick disintegrating tablets,
mouth dissolving tablets, fast disintegrating tablets, fast-dissolving tablets,
rapid-dissolving tablets, or porous tablets are characterized by disintegrating
or dissolving in the mouth within 1 minute, some within 10 seconds, leaving
an easy-to-swallow residue.
• Tablets of this type are prepared using very water-soluble excipients designed
to water into the tablet for rapid disintegration or dissolution without
chewing.
 RAPID-RELEASE TABLETS
• Rapid-release tablets offer increased convenience and ease of
administration with the potential to improve compliance, especially
when swallowing conventional solid oral-dosage forms presents
difficulties for the patient.
• Not with standing these advantages, there are a number of
disadvantages and difficulties associated with formulating rapid-
release tablets, including drug loading, taste masking, friability,
manufacturing costs, and stability of the product.
 EXTENDED-RELEASE TABLETS
• Extended-release tablets sometimes called controlled-release tablets,
prolonged-release, delayed release or sustained release tablets are
designed to release their medication in a predetermined manner over
a prolonged period of time. These tablet types are categorized into :
o Those that respond to some physiological condition to release the
drug, such as enteric coatings;
o Those that release the drug in a relatively steady, controlled
manner; and
o Those that combine combinations of mechanisms to release
pulses of drug such as repeat action tablets preparation.
EXTENDED-RELEASE TABLETS
 SUSTAINED RELEASE TABLET
 These tablets are used to get a sustained action of medicament. Sustained-
release dosage forms are dosage forms designed to release (liberate) a drug
at a predetermined rate in order to maintain a constant drug concentration
for a specific period of time with minimum side effects.
 These tablet when taken orally, release the medicament in a sufficient
quantity as and when required to maintain the maximum effective
concentration of the drug in the blood throughout the period of treatment.
 Sustained release of drug helps in getting the desired action in a sustained
way, thus these tablets are gaining popularity these days.
SUSTAINED RELEASE TABLET
 LAYERED TABLETS
• They are tablets composed of two or more layers of ingredients.
Layered tablets are prepared by compressing additional tablet
granulation on a previously compressed granulation to form two-
layered or three-layered tablets, depending on the number of
separate fills. Each layer may contain a different medicinal agent,
separated for reasons of physical or chemical incompatibility, staged
drug release, or simply the unique appearance of the layered tablet.
• Unlike conventional tablets where we have a single piece of
substance moulded to shape, layered tablets have the appearance of
a sandwich because the edges of each layer are exposed.
LAYERED TABLETS
LAYERED TABLETS
MANUFACTURING PROCESS
 TABLET TRITURATES
• Tablet triturates are small, usually cylindrical, moulded, or
compressed tablets containing small amounts of usually potent drugs
mixed with a combination of sucrose and lactose or any suitable
diluent. They are prepared from moist material, using a triturate
mould that gives them the shape of cut sections of a cylinder.
• Since tablet triturates must completely and rapidly dissolve in water,
only a minimal amount of pressure (sometimes use tablet triturate
mould) is applied during their manufacture.
• Several types of enzyme tablets are the example of tablet triturates/.
 VAGINAL TABLET
• These tablets are meant to dissolve slowly in vaginal cavity.
• These tablets are uncoated, bullet-shaped, or ovoid tablets designed for
vaginal administration, which are used to release steroids, antibacterial and
antiseptics etc to avoid infections.
• Following insertion, retention and slow dissolution of the tablet occur,
releasing the medicaments to provide the local pharmacological effect (e.g.
for the treatment of bacterial or fungal infection). E.g. Clotrimazole tablet.
• These type of tablets designed to be compatible with some type of plastic
tube inserter, which is usually employed to place the tablet in the upper
region of the vaginal tract.