Subject:

Pharmaceutics-II (Dosage form Science)

Topic:

Tablets

Compiled by:

 Urooj Fatima
 Aalia Mehboob
 Hadia Khalid
 Aliza Shahid
 Maryam Qasim
 Aneesa Ejaz
 Faria Maqsood
 Anvisha Fatima

Session: 2020-2025

Department of Pharmacy

The Islamia University of Bahawalpur

Composed by: Haider Irshad & M. Tanveer Ashfaq

Proofread by: Yashfa Rashid

 Tablets

Definition:

Tablets are solid dosage forms usually prepared with the aid of suitable
pharmaceutical excipients. A tablet is a small disc or cylinder of compressed solid substances
that contains a measured amount of medicine or drug.

 They may vary in size, shape, weight, hardness, thickness, disintegration and
dissolution characteristic 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 coating of various types.
 Other tablets such as those administrated sublingually, buccally, or vaginally, are
prepared to have features most applicable to their particular route of administration.

Excipients used in tablet formulation:

Excipients used in tablet formulation may be classified into two groups:

1- Those that help to impart satisfactory processing and compression characteristics to

the formulation. e.g. bulking agents/diluents, binders, glidants, and lubricants.
2- Those that help to give additional desirable physical characteristics to the compressed
tablets e.g. disintegrates, surface active agents/surfactants, colours, flavours,
sweetening agents (as in the case of chewable tablets), polymers or hydrophobic
materials (as in the case of controlled release tablets).

The following excipients are used:

 Diluents or fillers  Disintegrants
 Binders or adhesives  Anti-adherants
 Glidants  Lubricants
 Colorants  Flavourants
 Binders or Adhesives
 Binders or adhesives promote the adhesion of particles of the formulation and add the
necessary bulk to the formulation, allowing a granulation to be prepared, and
maintaining the integrity of the final tablet.
 Diluents or fillers:

Diluents or fillers add the necessary bulk to a formulation to prepare tablets of

the desired size.

 Anti-adherents, glidants, lubricants or lubricating agents:

Enhance the flow of 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.

 Disintegrants or Disintegrating agents:

These promote the breakup of the tablets into smaller particles after administration to
make the drug readily available.

 Miscellaneous adjuncts:

Includes colorants and flavourants.

 Absorbents:

In addition to the drug substance, compressed tablets also contain adsorbents; they are
used whenever there is a need to include a liquid or semisolid drug substance or
excipients within the tablet formulation. Adsorbents adsorb moisture that may attack
tablets or cause cohesiveness of the tablet powder/granular material from the liquid or
semi-solid components, thus allowing proper tablet compression. Examples include
silicon dioxide, magnesium oxide, starch etc.

Types of Tablets:

1) Compressed tablets
2) Multiple compressed tablets
3) Uncoated tablets
 Soluble tablets
 Dispersible tablets effervescent tablets
  Chewable tablets
 Tablets for use in mouth
i- Buccal tablet
ii- Sub lingual tablet
iii- Troches & lozenges
iv- Dental cone
4) Coated tablets
 Sugar coated tablets
 Film coated tablets
 Gelatin coated tablets
 Enteric coated tables
5) Hypodermic tablets
6) Immediate release tablets
7) Rapid release tablets
8) Extended release tablets
9) Vaginal tablets
10) Implantation tablets
11) Dispensing tablets
12) molded tablets

Classification of Tablets:

1. Compressed tablets:

It imprints a significant proportion of tablets that are clinically used to provide

systemic administration of therapeutic agents either in an uncoated state or in coated
state. These are formed by the compression of powders, crystalline materials, or
granular materials into the required geometry by the application of high pressures,
using steel punches & dies. In addition to active pharmaceutical ingredient (API),
compressed tablets usually contain a number of excipients.

Excipients:
 In addition to the medicinal agent or agents, compressed tablets usually contain a
number of pharmaceutical adjuncts, including the following:

1) Diluents or Fillers: they are added to increase the size of tablets to get a significant
tablet weight that can be handed or compressed, thereby rendering the manufacturing
process more reliable & reproducible. e.g. Anhydrous lactose, spray dry lactose,
microcrystalline cellulose, etc.
2) Binders or Adhesives: they are also referred to as granulators or granulating fluid.
They are polymeric, natural or synthetic materials that impart cohesive qualities to
powdered materials used in tablet manufacture. They ensure that the tablets remain
intact after compression, and improve the free flowing qualities of the powder
materials without retarding disintegration or dissolution. e.g. acacia gum, tragacanth,
methyl cellulose etc.
3) Disintegrates: they are added to formulation to overcome the cohesive strength
imparted during compression thus facilitating the breakdown of the tablet into
granules for ready drug availability once they come into contact with moisture e.g.
starch dyes, cellulose etc.
4) Glidants: glidants are fine powders that enhance the movement of powders or
granules within the hopper and into the die cavity prior to compaction, compression or
encapsulation. By enhancing flow rates of powders of granules, there is less
variability of the tablets manufactured, resulting in more consistent dosing of the drug
substance e.g. colloidal silicon dioxide, talc etc.
5) Lubricants: lubricants, as the name suggests, reduce friction between the powder mix
& the die walls during compression & ejection. They also prevent the mixed
powder/granules from sticking to the processing zone of the tablet press especially the
punches and die. In some cases, lubricants reduce inter-particulate friction & thus
improve flow rates of powders or granules. e.g. magnesium stearate, boric acid etc.

Examples:

Paracetamol tablet, Acetaminophen, Calpol etc.

Advantages:

 Accurate dosages can be administered simply.

 Easy to transport in bulk.
  More stable than liquid preparations.
 Release rate of drug can be tailored
 Tablets are versatile.
 Tablets can be man produced quickly.

Uses:

The compressed tablets that have been coated with concentrated sugar solution to
improve patients compliance, increase aesthetic appeal, mask objectionable taste or
odour, increase stability and/or modify the release of the therapeutic agents.

2. Multiple Compressed tablets:

These tablets are prepared by subjecting the fill material to more than a single
compression. The result may be a multiple compressed tablet, a multiple layered
tablet, or a tablet within a tablet: the inner tablet being the core and the outer layer a
shell. Each layer may contain a different medicinal agent, separated for reasons of
chemical or physical incompatibility staged during release.

Excipients:

1) Disintegrates: these are added to the formulation to promote the breakup of tablets
into small granules and their constituent particles. e.g.: Crospovidone
2) Lubricants: Lubricants reduce the friction between the powder mix & the die walls
during compression & ejection. They also prevent the mined powder/granules from
sticking to the processing zone of the tablet press, especially the punches & die. e.g
talc & magnesium stearate.

Example: Norgesic tablets

Significance/Purpose:

 It is employed as a means of administering more than one API in a single dosage from
to achieve controlled drug delivery.
  It is appropriate for chronological release of two drugs in combination and also for
sustained release of the tablet in which one layer is for immediate release and the
second layer is maintenance dose.

Uses:

These are used in anti-hypersensitive, diabetic, anti-hypersensitive and analgesic

drugs, where combination therapy is often used.

Reason:

So that
ingredients do
not combine
and remained in layered form.

A core of one drug and a shell of another A layered tablet of two drugs

3. Uncoated tablets:
 These are made in such a way that the release of active ingredients is unmodified
 When examined under a lens, these show either a relatively uniform texture (single
layer) or stratified texture (multi layer), but no signs of coating.

Examples:

Betnisol, Aspirin, CeCon (Vitamin C) , Strepsils (dry cough lozenges), Fentora etc.

Types:

 Soluble tablets
 Dispersible tablets
  Effervescent tablets
 Chewable tablets
 Tablets for use in mouth
i. Buccal tablet
ii. Sublingual tablet
iii. Troches & lozenges
iv. Dental cone
 Soluble tablets:
These are uncoated or film coated tablets that are intended to be dissolved in water
giving a clear or slightly opalescent solution.
Examples:
Betnisol, Erythromycin, Amitriptylidine, Valsartan, Pidofenac potassium etc.

Advantages:

The film is usually colored & has the advantage over sugar coating in that it is more
durable, less bulky & less time consuming to apply.

Excipients:

1) Polymers: the main role of polymer is to protect drug from physiological

environment & prolong the release of the drug to improve its stability. E.g. cellulose
ethers, glycols, other carbohydrates, vinyl derivatives, acrylic polymers etc.
2) Colourants: they help to give additional desirable physical characteristics to the
tablets.
Eg. Water soluble dyes (FD and C yellow 5 Lake)
 Water insoluble (FD and C yellow 5 Lake)
 Inorganic pigments (iron oxide titanium dioxide)
3) Plasticizers: they are used mainly for oral solid dosage forms. They are added to the
polymers used as film forming agents in order to make the polymer pliable and soft,
enhancing the flexibility and plasticity of the films.
E.g. Polwls , organic esters, oils/glycerides.
4) Solvents/vehicle: they are used as solvents in which the medicinally active agent is
formulated or administrated.
 E.g. water, alcohols, chlorinated hydrocarbons, ketones, esters

Uses:

 They are used for the relief of headache, migraine, backache, rheumatic pain,
toothache and body pains.
 They also relive sore throat and fevers, & aches and pains of colds & flu

 Dispersible tablets:
These are uncoated tablets or film coated tablets intended to be dispersed in water
before administration, giving a homogenous dispersion.

Example: Aspirin

Excipients:

1) Fillers: they add the necessary bulk to the formulation to prepare tablets of the
desired size.
Eg. DiSPERZiSTA (dispersible filler for supplement tablets)
2) Lubricants: they reduce the friction between the powder mix & the die walls during
compression & ejection. They also prevent the mixed powder/granules from sticking
to the processing zone of the tablet press, especially the punches & die.
E.g. talc & magnesium stearate
3) Disintegrant: they are added to the formulation to promote the breakup of tablets
into small granules & their constituent particles
E.g. croscarmellose sodium, crospovidone, sodium starch glycolate, microcrystalline
cellulose.
4) Sweeteners: they are added to pharmaceutical dosage form to mask biller taske of the
partially dissolved drug and to improve palatability in general.
E.g. saccharin, sodium, aspartame, citric acid, menthol, lemon flavor
5) Dispersion Aids: they helps in giving a homogenous dispersion.
6) Multiple flavorings

Advantages:
  It can be administered easily to patients having difficulty in swallowing like the
elderly, stroke victims and pediatrics
 Cost effective as minimum number of ingredients are required
 Improved safety by prevention from the choking or obstruction as in case of
conventional dosage forms during swallowing

Uses:

 They are used for the secondary prevention of thrombotic cerebrovascular or

cardiovascular disease, following by-pass surgery.
 They are also used to reduce fever and mild to moderate pain.
 They also provide relief of symptoms of seasonal and allergic nasal conditions.
 May also be used to treat hives.

 Effervescent tablets:

Effervescent tablets or carbon tablets are tablets which are designed to dissolve in
water and release carbon dioxide (bubble action). They are products of compression
of component ingredients in the form of powders into a dense mass, which is packed
in a blister pack (bubble pack).

Active ingredients:

Vitamin tablets may be sold as effervescent tablets. There are several categories of
active ingredients that may be best administered in the form of effervescent
preparations:

 Those that are difficult to digest and are disruptive to the stomach or esophagus.
 Those that are pH-sensitive, such as amino acids & antibiotics.
 Those that are susceptible to light, oxygen or moisture.

Excipients:

1) Acid components: they are most commonly used being readily abundant & relatively
inexpensive
 E.g. citric acid, tartaric acid, ascorbic acid, malic acid, other sources of acid
components, including formic acid, nicotinic, acid etc.
2) Alkali components:
Sodium bicarbonate, sodium carbonate, sodium glycine carbonate, potassium
bicarbonate, potassium carbonate, acid, nicotinic acid etc.
3) Binders: they are necessary in effervescent tablets in order to bring the tablets
hardness to a point where handling is possible.
E.g. PEG 6000
4) Lubricants: without lubricants, production of effervescent tablets on high speed
equipment would not be possible. A perfect lubricant for effervescent products must
be water soluble, non-toxic and tasteless.
E.g. magnesium stearate, stearic acid, sodium chloride, sodium acetate.
5) Sweeteners: water soluble flavors may be added to mask the unpleasant taste of the
tablet and make the product palatable.
E.g. Sorbitol, Sucrose, Aspartame, Sodium saccharin, other natural sweeteners.
6) Colorants: colorants may be added to the formulation to produce colored solutions or
products.
E.g. dyes or lake pigments, dried flower buds, herbs and chamomile extracts may be
used for this purpose.
7) Antifoaming agents: Anti-foaming agents may be included in the formulation to
reduce foam formation and consequently reduce the tendency of drugs to stick to the
wall of the glass above the water level.
E.g. Polydimethyl slioxane

Example:

 Alka Seltzer
 Zantac Efferdose

Advantages:

 Better and quicker absorption

 Optimal compatibility
 Increase in liquid intake
 Simple measuring into exact doses
 Simple handling
Disadvantages:

 Most excipients used are relatively expensive.

 It requires special production facilities.
 Its high sodium or potassium content makes it unsuitable for administration to patients
with heart failure or cardiac insufficiency.
 Some are bulky in relation to tablets or capsules.
 It is sometimes difficult to make drugs with unpleasant taste sufficiently palatable as
an effervescent product.

Reason: Bubble action can assist in breaking up the tablets and enhancing the dissolution of
the active drug.

Uses:

 It is used in soft drinks, fruit juices, sweets, jams and juices.

 It also acts as an anti-oxidant in prepared meats and in tinned vegetables and fruit.

 Chewable Tablets:
Chewable tablets are an oral dosage form intended to be chewed and then swallowed
by the patient rather than swallowed as a whole. It may be defined as a solid dosage form
containing medicinal substances with or without suitable diluents that is intended to be
chewed, producing a pleasant tasting residue in the oral cavity, that is easily swallowed and
does not have a bitter or unpleasant taste.

Excipients:
Diluents:
These are added to chewable tablet formulation to increase the bulk volume of the
tablet. Diluents commonly used in chewable tablets include:
Mannitol:
It is a white odourless, crystalline powder, or free flowing granules that is essentially
inert and non-hygroscopic. It is commonly used as a diluent because of its negative heat of
solution, sweetness and ‘mouth feel’.
Sorbitol:
 Sorbitol is a polyol that occurs as an odourless, white or almost colourless, crystalline,
hygroscopic powder. It is used as diluent owing to its pleasant, sweet taste and cooling
sensation.
Dextrose:
This is an odourless, sweet-tasting , colourless or white crystalline or granular powder
obtained through acid or enzymatic hydrolysis of starch. It acts as diluent and binder.
Lactose:
Lactose, also known as milk sugar is a disaccharide commercially produced from the
whey of cow’s milk. It is the oldest and most widely used pharmaceutical excipient in the
history of tablet making.
Sucrose:
Sucrose has been extensively used in tablets in tablets both as filler and as a binder.
Sucrose as a diluent is used in formulations, particularly where artificial sweeteners are to be
avoided.
Flavouring Agents:

Flavorants are commonly used to impart pleasant flavor, and often odour to chewable
tablets.
Flavor Groups for taste types
Sweet Vanilla, grape, maple, honey, stone fruit, berries
Sour Citrus, raspberry, anise, cherry, strawberry, root beer
Salty Mixed fruit, mixed citrus, butterscotch, nutly, spice
Bitter Liquorice, coffee, mint, grape fruit, wine, fennel, peach
Metallic Grape, lemon-lime, burgundy
Alkaline Mint, chocolate, cream, vanilla.

3. Sweetening Agents:
Sweeteners are added primarily to chewable tablets when commonly used carriers
such as mannitol, lactose, sucrose and dextrose do not sufficiently mask the taste of the active
substance or components. Common sweeteners used in pharmaceutical products include:
Aspartame (Nutrasweet), a nondrug approved artificial sweetener
Glycyrrhizin (magnasweet):
It is a liquorice derivative with an intense, late, long-lasting sweetness:
Saccharin:
It is FDA approved and 500 times sweeter than sucrose. It has a bitter after taste.
Colourants:
The Food Drug and Cosmetic Act of 1938 created three categories of coal tar dyes, of
which only FD&C colours and D&C colours are used in manufacture of chewable tablets.
The third category (External D&C) is not certifiable for use in products intended for
ingestion.

Advantages:
The advantages of chewable tablets include:
 Palatability
 Stability
 Ease of delivery
 Portability
 Precise dosing
Uses:
The chewable tablets having calcium or Vitamin D are used:
 To help in growth and good health
 To prevent or treat soft, brittle bones (osteoporosis)
 To treat or prevent low calcium levels
Examples:
Chewable tablets include antacids, antibiotics, anticonvulsants, analgesics, anti-
asthmatics, vitamins and cold preparations.
 Carbamazepine  Montelukast
 Motrin  Fluoride
 Angina  Didanosine

1) Buccal and 2) 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 poorly absorbed from GIT.
Excipients:
1 Microcrystalline cellulose; diluent, absorbent
2 Lactose monohydrate; diluent, binder
3 Cross povidone; super disintegrant
4 Cross carmellose sodium; super disintegrant
5 Sodium starch glycolate; super disintegrant
Advantages:
1) These drugs do not go through the digestive system so they are not metabolized
through the liver. This means you may be able to take a lower dose and still get the same
result.
2) Another advantage is that you do not have to swallow the drug. Drugs that are
absorbed under the tongue or betweem the cheek and gum can be easier to take for people
who have problems swallowing pills.
Examples:
Buccal tablets
1. Fentora
2. Belbuca
3. Bunavail
Sublingual Tablets
1. Nitroglycerin
2. Loratadine
iii. Lozenges or Troches
Lozenges are solid dosage forms that are intended to be dissolved or disintegrated
slowly in the mouth. A lozenge is a solid preparation consisting of sugar and gum, giving
strength and cohesiveness to the lozenge.
Excipients:
Candy base
Sugar
Sugar free vehicles
 Binders
 Lubricants
  Flavouring agents
 Colouring agents
 Whipping agent
 Humectants
Advantages:
- It is use to medicate the mouth and throat for the slow administration in digestion or
cough remedies.
- Lozenges provide a pleasant dosage form for patients who are unable to swallow
other types of solid dosage forms.
- This product is used to temporarily relieve pain from minor mouth problems (such as
cankers sores, sore gums/ throat, mouth/gum injury)
Examples:
 Clotrimazole troches
 Strepsils
iv. Dental Cones
A tablet form intended to be placed in the empty socket, following a tooth extraction for
preventing the local multiplication of pathogenic bacteria associated with tooth extractions.
The cones may contain an antibiotic or an antiseptic.
Advantages:
- They prevent the multiplication of bacteria in the socket following such extraction by
using slow releasing antibacterial compounds or to reduce bleeding by containing the
astringent
- These cones generally get dissolved in 20-40 minutes
Excipients:
- Lactose
- Sodium bicarbonate
- Sodium chloride
Examples:
Parasorb cone (collagen)

Coated Tablets:
 These are the tablets covered with one or more layers of mixtures of substances such as
resins, gums, fillers, sugar, plasticizers, waxes, colouring matter etc.

 Sugar coated tablets:

These are compressed tablets that have been coated with concentrated sugar solution
order to improve patient’s compliance and mask objectionable taste or odour.
The sugar layer may be coloured or uncolored. Sugar coating may add 50% to the
weight and bulk of uncoated tablets.

Examples:

Reasulf tablets, Advil-ibuprofen tablet, Baclofen-Ibuprofen 400mg (Mylan products ltd.)

Advantage:

1. Coating is water soluble and quickly dissolves after swallowing.

2. Sugarcoat protects the drug from the environment and provides a barrier to
objectionable taste or odour
3. The sugarcoat also enhances the appearance of the compressed tablet and permits
imprinting of the identifying, manufacturer’s information

Disadvantage:

Time and expertise are required for the coating process and there is an increase in size
of tablet, weight of tablet, and shipping costs.

Excipients used in sugar coated tablets:

Because sugar coated process consists of various steps, a variety of additives may be
incorporated into each type of formulation to achieve a particular function. These
include:

1. Sugar and its substituents:

The major ingredients used in sugar-coating process is sugar (primarily sucrose),
although this may be substituted by other sugars and sugar alcohols such as glucose,
lactose, maltitol, isomaltose, sugar alcohols.
 2. Binders:
Binders increase the strength and elasticity of the coating by forming bands and thus a
coherent matrix.
E.g. polyvinyl acetate (PVA) , polyvinyl pyrrolidone (PVP)
3. Fillers:
Fillers build up the structure and add mass to the coatings e.g. dextrin, cornstarch, and
calcium sulfate
4. Colorants:
Colorants add colour to the coating and cover imperfections, which may appear in the
tablet core e.g. dyes, pigments.
5. Anti-adhesives, lubricants and glidants:
These materials reduce friction between coated tablets and also prevent dust
formation during drying e.g. talc and colloidal silicon dioxide.
6. Flavoring agents:
Flavors improve and enhance the acceptability and palatability of the dosage form in
order to maximize patient compliance e.g. fruit flavors etc.
7. Suspension stabilizers:
They prevent phase separation or sedimentation of the coating suspension while it is
being applied during the coating process e.g. surface active agents or thickening
agents.
8. Smoothing agents:
These materials smoothen out the surface of the coating by lubricating and binding
the fines that may be created during the coating process e.g. combination of syrup and
acacia gum.
9. Polishing agents:
Polishing agents enhance the reflectivity and intensity of colour of coating e.g.
beeswax and carnauba
Colour of sugar coated tablets: Red, orange, yellow, blue, purple, brown.
Is sugar days sticky? No
Is sugar syrup itself binder? No
Is colour is poisonous? No

Advantages/ideal characteristics of sugar coated tablets:

  Sugar coated tablets have smooth, rounded contour, with an even colour coverage and
a high degree of gloss.
 These tablets must meet the requirements as specified in official compendia.
 Those tablets that have been imprinted should show distinct print with no smudging
or broken print.

Film coated tablets:

These are compressed tablets covered with a thin layer of resins, polymers or
plasticizers capable of forming a film. The film is usually coloured. By its
composition, the coating is designed to rupture and expose the core tablet at the
desired location in the gastrointestinal tract.

Examples:

Erythromycin, Amitriptyline.

Excipients of film coated formulations:

Film coating formulations typically contain the following components:

1. Polymer:
A polymer is a substance consisting of very large molecular, composed of many
repeating units. Their consequently large molecular mass produces unique physical
properties including toughness, high elasticity, viscoelasticity and a tendency to form
amorphous and semi-crystalline structures e.g. cellulose ethers, glycols, other
carbohydrates, vinyl derivatives.
2. Plasticizer:
Plasticizer is a substance that is added to a material to make it softer and more
gullible, to increase its plasticity, to decrease its viscosity and to decrease friction
during its handling in manufacture. eg. polycol, organic esters, oils/glycerides.
3. Colorants:
It is a substance that is added or applied in order to change the colour of a material or
surface. E.g.
 Water soluble dyes (FD&C yellow 5)
  Water insoluble (FD&C yellow 5 lake)
 Inorganic pigments (iron oxide titanium dioxide)
4. Opacifier:
An opacifier is a substance added to a material in order to make the ensuing system
opaque. Opacifiers must have a refractive index substantially different from the
system.
5. Solvent:
A solvent is a substance that dissolves in a solute, resulting in a solution. The quantity
of solute that can dissolve in a specific volume of solvent varies with temperature.
E.g. water, alcohols, ketones, esters, chlorinated hydrocarbon etc.
6. Vehicle:
A component for internal or external use, that is used as a carrier or diluent in which
liquids, semisolids, or solids are dissolved or suspended.
Advantages:
 Reduce pressing times
 Increases process efficiency and output
 Exhibits formulation flexibility
 Expands opportunities for branding and identification
 Less bulky
Disadvantages:
Flammability hazards
Toxicity herds
Concerns over environmental pollution on
Commonly used coating film: The most widely used polymers in non-functional film
coating are cellulose derivatives, such as hypermellose.

Gelatin coated tablets:

These are 1/3rd smaller than a capsule filled with an equivalent amount of powder. The
gelatin coating facilitates swallowing and gelatin coated tablets are more tamper evident
than unseated capsules.

Examples:
 Hydrochlorothiazide tablet, Tylenol cold multi-symptom daytime

Advantages:

 The gelatin coating facilitates swallowing, enables custom branding, and prevents
counterfeit since they are more tramper-evident than unsealed capsules.
 These are also ideal for double-blind clinical studies, or for drug substances that can
irritate the esophageal mucosa when they are incorporated in an immediate release
tablet.

Reason for coating:

For consumers, gelatin dissolves in the human body at normal body temperature,
making it the ideal ingredient in softgels, while protecting the precious actives inside against
oxygen, light, moisture and dust.

Excipients of gelatin coated tablets:

1. Lubricants:
Lubricants, as the name suggests, reduce friction between the powder mix & die walls
during compression & ejection. They also present the mixed powder/granules from
sticking to the processing zone of the tablet press especially the punches & die. In
some cases, lubricants reduce inter-particular friction & thus improve flow sates of
powders or granules.
E.g. stearic acid- as lubricants in tablets, or hard gelatin capsules because they
improve certain characteristics of capsules.

2. Diluents or fillers:
They are added to increase the size of tablets to get a significant tablet weight that can
be handed or compressed, thereby rendering the manufacturing process more reliable
and reproducible.
E.g. Microcrystalline cellulose (MCC) is used as a filler for capsule filling.

Uses of gelatin coated tablets:

1. Gelatin coated tablets are easy to swallow, have custom branding, prevent
counterfeit.
2. These are tamper-evident and mask unpleasant odour or taste/flavors,
 3. They improve stability of photosensitive active pharmaceutical ingredients (API)
and they look life softgels.

Enteric Coated Tablets:

An enteric coated is a polymer barrier applied to oral medication that prevents its
dissolution or disintegration in the gastric environment. It is also an effective, method to
obtain drug targeting such as gastro-resistant drugs.
Excipients:
The substances used in enteric coating are :
- Hydro propyl methylcellulose phthalate (HPMCP)
- Polyvinyl acetate phthalate
- Diethyl phthalate
- Cellulose acetate phthalate
In general, tablets can be coated using either a fluid-bed dryer or air-suspension coating.
Advantages:
- Enteric-release coating applied to nutritional tablets or soft gels improve consumer
appeal.
- They help reduce unpleasant flavors and odors because the food additive is not
released in the stomach; If is released in small intestine instead .
- They have delayed released features.
- They are designed to pass unchanged through the stomach to the intestine,where the
tablet disintegrate and allow drug dissolution and absorption or effected .
- It can reduce frequent dosing of tablets or capsules by releasing sequential medication
which can improve patient compliance.
- It is also used in capsules preparing enteric-coated granules.
Examples:
- Alophen-Bisacodyl 5mg USP
- Arthrotec-Diclofenac sodium and misoprostol
- Azulfidine EN-Sulfasalazine
- Bayer EC- Aspirin 81mg
5) Hypodermic tablets
These tablets are soft, readily soluble tablets that 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.
Excipients:
- Disintegrates .e.g. Starch
- Glidants .e.g. colloidal anhydrous silicon
- Lubricants .e.g. Stearic acid
Advantages & Disadvantages:
- Hypodermic tablets are no longer in the US.
- These tablets were a convenience, since they could be easily carried in physicians
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 of
hypodermic tablets.
Example:
- Dilaudid – Dihydromorphinone HCl

6) Immediate Release Tablets

These are the tablets which disintegrate rapidly and get dissolved to release the
medicaments with no special rate controlling features such as special coatings and other
techniques.
Excipients:
- Super disintegrants:
 Carmellose
 Sodium starch glycolate
 Crosspovidone
Advantages:
- These provide instantaneous disintegration of the tablet after administration in the
stomach thus decreasing the disintegration time, which in turn enhances drug
dissolution rate
 - These tablets start working quickly
Examples:
- Percocet
- Norco

7) Rapid Release Tablets

These are also called rapidly dissolving tablets, rapidly disintegrating tablets, orally
disintegrating tablets, quick disintegrating tablets, mouth dissolving tablets, or porous tablets
and are characterized by disintegrating or dissolving in the mouth with in 1 minute, some
within 10 sec, leaving an easy to swallow residue.
Excipients:
- Collidal silicon dioxide
- Carmellose
- Celluloe Filling
- Disintegrate
- Dissolution Accelerator
- Rapid Release agent
Advantages:
- No need of water to swallow the tablet.
- Accurate dosing as compared to liquids.
- Dissolution and absorption of drug is fast offering rapid onset of action.
- Bioavailability of drug is increased.
- It helps to reduce fever and/or mild to moderate pain (headache, backache)
Examples:
 Tizanidine
 Griseofulvin
 Prednisone

8) Extended-release Tablets:
These are sometimes called contoured-release tablets, prolonged release, delayed
release or sustained release tablet, designed to release their medication in a pure determined
manner over a prolonged period of time.
Example:
Dolophine, Duragesic
Benefits:
 Simplification of dosing regimens
 Reduction in pill burden
 Reduction in the peak to trough fluctuating in serum drug concentration that may be
associated with a decreased risk of adverse effects & of seizures.
Disadvantages:
 Manufacturing costs
 Dose limitations
 Forgiveness period

9) 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 non-specific Vaginitis caused by
Haemophilus Vaginalis antifungals for the treatment of vulvovaginits candidiasis caused by
Candida Albicans and related species.
Excipients:
- Methyl cellulose
- Sodium carboxymethylcellulose
- Sodium aginate
- Carbopol 974
Advantages:
- It is an ideal route for drug administration because it allows for the administration of
lower doses, steady drug levels and less frequent administration than the oral route.
- Avoid first pass metabolism
- Used before surgery since oral therapy
- Is restricted
- Introduce drugs into body
Examples:
Vagistat (Tiocona zole)
 Vandazole (metronidazole)

10) Implantation Tablets:

These are long-acting sterile tablets designed to provide continuous release of drug
often over a period of months or a year.
- These are mainly used for the administration of hormones such as testosterone
steroids for conception e.g.
- Implanon-etongestrel (organon)
- Disulfiram Tablet for implantation

11) Dispensing Tablets:

 Also known as compounding tablets. It is used for compounding prescription not
dispensed as such to patients.
 The tablets have the dangerous potential of being inadvertently dispensed as such to
patients e.g.
 Silver Potentiate
 Bichloride of mercury merbromin and quaternary ammonium compounds.
Disadvantages:-
 These tablets contain large amounts of highly potent drug substances, so the
pharmacist can rapidly obtain premeasured amount for compounding multiple dosage
units.
 These tablets have the dangerous potential of being inadvertently dispensed as such to
the patients.
Excipients:-
Glidants – Magnesium Silicate
Lubricants – Stearic Acid

12) Molded Tablets

 Certain tablets such as tablet triturates may be prepared by molding rather than by
compression.
 They are very soft & soluble, rapid dissolution.
Excipients:
  Lactose – an hydrous and spray dried lactose
 Directly compressed starch
 Hydrolyzed Starch
 Microcrystalline cellulose – Avicel
 Dibasic calcium phosphate dehydrate
 Calcium sulphate dehydrate
 Mannitol
 Sorbitol
 Sucrose
 Dextrose

Advantages:-
These are very soft and soluble and are designed for rapid dissolution.

Manufacturing of tablets
Tablet manufacturing process is dependent on several factors including the
compression properties of therapeutic agents, particle size of therapeutic agents, excipients
and chemical stability of therapeutic agents during manufacturing process.

Methods:

There are three methods by which tablets are manufactured:

1) Wet Granulation
2) Dry Granulation
3) Direct compression

Steps:

1) Mixing of therapeutic agents with excipients

2) Granulation of mixed powders

(This is performed in direct compression)

3) Mixing of powders or granules with excipients. ( Mostly lubricants)

4) Compression
 The details of each of these steps will vary depending on manufacturing method used

Wet Granulation:

Most frequently used method in the manufacturing of tablets. Water is frequently used
as granulation fluid. Heat is employed to dry formed granules. It is important to ensure that
the therapeutic agent is chemically stable during the granulation process. The wet granulation
exhibits sufficient mechanical properties to be subsequently exposed to other unit operations.
E.g. film coating

 The manufacturing of tablets by wet granulation is not as efficient as other methods

e.g. direct compression

Dry Granulation:

When tablet ingredients are sensitive to moisture and unable to with stand elevated
temperature during drying, and when the tablet ingredients have insufficient cohesive
properties (slugging). This technique is used in preparation of aspirin, aspirin combinations
etc.

Direct Compression:

Wet granulation and dry granulation methods having series of unit operations, both time
consuming and potentially costly. Potentially more attractive option for manufacturing of
tablets involves powder mixing and subsequent compression of powder mix, thereby
obviating the need for granulation. This process is known as direct compression. The
mechanism of particle-particle interactions in tablets produced by direct compression are
similar to that in dry granulation and roller-compaction.

Quality Control tests for tablets

 Pharmacopoeial or Official Tests.

They are called official tests because the test methods are described in the official
compendia such as the British Pharmacopoeia, American Pharmacopoeia etc.
These tests include

 Content of active ingredient

 Uniformity of weight / weight variation test

 Disintegration Time Test:

This test determines whether dosage forms such as tablets, capsules, boluses, pessaries and
suppositories disintegrate within a prescribed time, when placed in a liquid medium under
prescribed experimental conditions.

 Dissolution test:

Evaluates the rate and extant that a c compound forms a solutions under carefully
controlled conditions.

 Content of active ingredient:

The tablets are weighed together and are crushed in a mortar with a pestle. An amount
equivalent to the theoretical content of each tablet is weighed out on an analytical
balance.

 Uniformity of weight / weight variation tests.

British pharmacopoeia includes a test for the uniformity of weight which requires that
when the tablets in a sample of 20 are weighed singly, not more than 2 deviate from the
average weight by a percentage greater than that specified and no tablet derviates by
more than double that.

 Uniformity of content:

Pharmacopoeial analysis parameter for the quality control of capsules or tablets.

 Non –official tests

They are called non-official tests because the test methods are not described in the
official compendia these tests include:
 Tablet hardness or crushing strength test
 Friability test
 Tablet thickness

 Tablet Hardness Test.

 To determine the breaking point and structural integrity of a tablet and finding out how
it changes under conditions.

Friability Test:

To test the durability of tablets during transit

Tablet Defects

Tablet defects are deficiencies that are usually encountered in tablet formulation.

1. Capping
2. Lamination
3. Chipping
4. Sticking
5. Picking
6. Cracking
7. Binding/binding in the die
8. Edging/flashing of tablet
9. Mottling
10. High friability
11. Weight variation
12. Hardness variation
13. Aging of tablets/loss of harness.
14. Protracted hardness (hardness increase with time)
15. Disintegration time too long.
16. Uneven breakage
17. Black spot/stain
18. Double impression
19. Bisected/score line/breakline or imprint or logo, not sharp or well-defined
20. Splitting of layered tablets or layer separation
21. Layers not sharply defined bilayer tablet

Capping:
 Capping is a term used to describe the partial or complete separation of the top or
bottom crowns of a tablet from the main body of the tablet.

Lamination:

Lamination is the separation of a tablet into two or more

distinct horizontal layers. It is a tablet defect in which a
tablet splits or separates into layers.

Chipping:

Chipping is the breaking of tablet edges during the

pressing process or during the subsequent handling and
coating.

Sticking:
 Sticking is a defect of the tablet where the tablet surface sticks to the punch face or
adhesion of tablet material to the die wall during compression.

Picking:

Picking is the term used when a small amount of material from a tablet is sticking to
and being removed from the tablet surface by a punch.

Cracking:

Cracking is a defect of tablets where small, fine cracks are observed on the upper or
very rarely on the sidewall. Easily visible in the tablet that contains a pigment or dye.

Binding / binding in the die:

 Binding is the tablet defect where tablets adhere, seize or tear in the die. A film is
formed in the die and ejection of the tablet is hindered. The tablet splits during the
molding/pressing process and the powder adheres to punch edges.

Mottling:

Mottling is the term used to describe an unequal distribution of colour on a tablet,

with light or dark spots standing out on an otherwise uniform surface.

Double impression:

Double impression is machine related tablet defect where a monogram or engraving

shape or break line/score line or imprint or logo appears twice on the tablet surface.

Weight variation:
 Weight variation of the tablets produced is a relatively common problem of the
tableting process. Hence weight variations to a limited extent are quite normal due to
variations in the density of the powder material and due to partial/incomplete filling of the
dies.

Low tensile strength:

Since radial tensile strength measurement considers the thickness of a tablet, and only
tensile stress and axial tensile strength express the strength in the direction in which capping
may occur, the tensile strength characterizes the strength of a tablet more completely than
hardness.
Embossing:

Embossed means imprinted with a mark raised above the dosage form surface.
Embossing is the imprint or spur line on the tablet not being clear. Causes of embossing
include faulty punch design, use of too coarse granules, and picking and sticking of granules
on punches.

Tablet thickness:

Tablet thickness is measured with a vernier caliper, thickness gauge or automated

equipment. The thickness of a tablet should be controlled within 5% variation, a standard
value depending on the size of the tablet.