TABLET

A Project report submitted in partial fulfillment for the award of degree of

Bachelor of Pharmacy
2020-2024

Submitted By
GAURAV VATS
B. Pharmacy 8th Semester
Registration No. 19-VIR-
University Roll No. 2
Supervisor
Miss PRITI
Assistant Professor,
PHARMACEUTICS

VAISH INSTITUTE OF PHARMACEUTICAL EDUCATION

AND RESEARCH, ROHTAK
Pt. B. D. Sharma University of Health Sciences, Rohtak
2024

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 CERTIFICATE

I certify that literature survey independently carried out with proper care. I hereby
recommended that this project being accepted in the partial fulfillment of
requirement for the degree of Bachelor of Pharmacy. I am pleased to forward this
project for evaluation. This is to certify that the project entitled “Menthol: An
important phytoconstituents with diverse biological activities” is a bonafide
literature survey done by Mr. Atul Sharma in partial fulfillment of the
requirement for the degree of Bachelor of Pharmacy under the guidance of Miss
Vandana, Assistant Professor in Pharmaceutical Biotechnology, VIPER, Rohtak.

Principal Supervisor
Dr. Rakesh Gupta
Professor,
Pharmaceutical Chemistry
VIPER, Rohtak

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 ACKNOWLEDGEMENT

It is a moment of great pleasure to express my sincere gratitude and indebtedness

to my guide Miss PRITI, Assistant Professor in Pharmaceutics, VIPER, Rohtak;
for her proficient guidance, patience, constant encouragement, valuable
suggestions and moral support that she bestowed on me during the entire period of
my project work on “TABLETS”. I acknowledge my deepest gratitude to my
family for supporting me spiritually throughout the project and my life in general.
Above all, I owe to Almighty God for granting me the wisdom and strength to
undertake this study and enabling me to complete the project work.

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 INTRODUCTION
A tablet (also known as a pill) is a pharmaceutical oral dosage form(oral solid dosage, or OSD)
or solid unit dosage form. Tablets may be defined as the solid unit dosage form of medication
with suitable excipients. It comprises a mixture of active substances andexcipients, usually in
powder form, that are pressed or compactedinto a solid dose. The main advantages of tablets
are that they ensure a consistent dose of medicine that is easy to consume.
Tablets are prepared either by moulding or by compression. The excipients can include diluents,
binders or granulating agents,glidants (flow aids) and lubricants to ensure efficient
tabletting;disintegrants to promote tablet break-up in the digestive tract; sweeteners or
flavours to enhance taste; andpigments to make the tablets visual attractive or aid in visual
identification of an unknown tablet. A polymer coating is often applied to make the tablet
smoother and easier to swallow, to control the release rate of the active ingredient, to make it
more resistant to the environment (extending its shelf life), or to enhance the tablet's
appearance.
The compressed tablet is the most commonly seen dosage form in use today. About two-thirds
of all prescriptions are dispensed as solid dosage forms, and half of these are compressed
tablets. A tablet can be formulated to deliver an accurate dosage to a specific site in the body; it
is usually taken orally, but can be administered sublingually, buccally, rectally or intravaginally.
The tablet is just one of the many forms that an oral drug can take such as syrups, elixirs,
suspensions, and emulsions.

Definition
According to the Indian Pharmacopoeia Pharmaceutical tablets are solid, flat or biconvex
dishes, unit dosage form, prepared by compressing a drugs or a mixture of drugs, with or
without diluents. Tablet is defined as a compressed solid dosage form containing
medicaments with or without excipients. They vary in shape and differ greatly in size and
weight, depending on amount of medicinal substances and the intended mode of
administration.

Properties
1) Should be elegant product having its own identity while being free of defects such as chips,
cracks, discoloration and contamination.
2) Should have strength to withstand the rigors of shocks encountered in its production,
packaging, shipping and dispensing.
3) Should have the physical stability to maintain its physical attributes over time.
4)Must be able to release the medicament agent(s) in the body in a predictable and
reproducible manner.
5)Must have a suitable chemical stability over time so as not to allow alteration of the
medicinal agent(s).

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Advantages
1) Tablets are unit dosage form and offer the greatest capabilities of all oral dosage form for
the greatest dose precision and the least content variability.
2) They are easiest and cheapest to package and strip.
3) Low in cost.
4) Lighter and compact.
5) Having greatest chemical and microbial stability over all oral dosage forms.
6) Suitable for large scale production.
7) Easy to swallow with least tendency for hang-up.
8) Objectionable odour and bitter taste can be masked by coating technique.
9) Sustained release product is possible by enteric coating.
10) Easy to handling.

Disadvantages
1) Difficult to swallow in case of children and unconscious patients.
2) Some drugs resist compression into dense compacts, owing to amorphous nature, low
density character.
3) Drugs with poor wetting, slow dissolution properties, optimum absorption high in GIT
may be difficult to formulate or manufacture as a tablet that will still provide adequate
or full drug bioavailability.
4) Bitter testing drugs, drugs with an objectionable odor or drugs that are sensitive to
oxygen may require encapsulation or coating. In such cases, capsule may offer the best
and lowest cost.
5) Irritant effects on the GI mucosa by some solids (e.g., aspirin).

INGREDIENTS
In addition to active ingredients, tablet contains a number of inert materials known as
additives or excipients. Different excipients are:

S.no. Ingredients Examples

1. Diluents Calcium Phosphate; Carboxymethylcellulose Calcium; Cellulose;
Dextrin; Lactose; Microcrystalline Cellulose; PR gelatinized Starch;
Sorbitol; Starch
2. Binders Acacia; Alginic Acid; Carboxymethylcellulose; Cellulose; Dextrin;
Gelatin; Liquid Glucose; Magnesium Aluminum Silicate;
Maltodextrin; Methylcellulose; Povidone; Sodium Alginate;
Starch; Zein.

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3. Lubricants Calcium Stearate; Glyceryl Palmitostearate; Magnesium Oxide;
Poloxamer; Polyvinyl Alcohol; Sodium Benzoate; Sodium Lauryl
Sulfate; Sodium Stearyl Sulfate; Stearic Acid; Talc; Zinc Stearate
4. Glidants Magnesium Trisilicate; Cellulose; Starch; Talc; Tribasic Calcium
Phosphate
5. Anti – Corn Starch; Metallic Stearate; Talc
adherents
6. Disinteg Alginic Acid; Carboxymethylcellulose; Cellulose; Colloidal
rants Silicon Dioxide; Croscarmellose Sodium; Crospovidone;
Potassium Polacrilin; Povidone
7. Coloring FD&C or D&C Dyes or Lake Pigments
agents
8. Flavoring Ethyl Maltol; Ethyl Vanillin; Menthol; Vanillin
agents
9. Absorbents Kaolin; Magnesium Aluminum Silicate; Tricalcium Phosphate

1) Diluents: Diluents are fillers used to make required bulk of the tablet when the drug
dosage itself is inadequate to produce the bulk. Also used to improve cohesion, to permit
use of direct compression.
2) Binders: to form cohesive compacts for directly compressed tablet.
3) Lubricants: Lubricants are intended to prevent adhesion of the tablet materials to the
surface of dies and punches, reduce inter particle friction and may improve the rate of
flow of the tablet granulation.
4) Glidants: Glidants are intended to promote flow of granules or powder material by
reducing the friction between the particles.
5) Anti–adherents: Anti-adherents are added to the tablet formulations to prevent the
material from sticking to the walls of the tablet press.
6) Disintegrates: Added to a tablet formulation to facilitate its breaking or disintegration
when it contact in water in the GIT.
7) Coloring Agents: The use of colors and dyes in a tablet has three purposes:
(A) Masking of off color drugs (B) Product Identification (C) Production of more elegant
product.
8) Flavoring Agents: Flavoring oils are needed for chewable tablets. The oil is generally
added in a dry form such as spray-dried beadlets.
9) Absorbents: The inclusion of absorbents in a tablet formulation is necessary if the
product contains asubstance with a high affinity to water. Hygroscopic materials, if
present, render the blend wet and difficult to handle during manufacture

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Types of Tablets
Oral Tablets for Ingestion
1) Standard Compressed Tablets
2)Multiple Compressed Tablets
3)Compression Coated Tablets – a) sugar coated, b) film coated tablets, c) gelatin coated tablets, d)
enteric coated tablets ---
Layered tablet
Inlay tablet
4)Targeted Tablets – a) Floating Tablet ,b) Colon Targeting Tablet
4) Chewable tablets
5)Dispersible tablets

Tablets used in the Oral Cavity

1) Lozenges and troches
2)Sublingual tablet
3)Buccal tablet
4)Dental cones
5)Mouth dissolved / rapidly dissolving tablets

Tablets Administered by other Routes

1) Vaginal tablet
2)Rectal tablet
3) Implants

Action Wise
1) Modified Release Tablet

Oral Tablet for Ingestion

Over 90% of tablets manufactured are ingested orally. These are designed to swallow intact,
with exception of chewable tablets.

1) Standard Compressed Tablets: These are standard uncoated tablets made by

compression using wet granulation, direct compression or double compression. It provides
rapid disintegration and drug release. They are mostly intended to exert local action in GIT. It
typically includes water insoluble drugs such as antacid and adsorbents. In addition to

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medicinal agents compressed tables usually contains a number of pharmaceutical adjuvants
such as diluents, binders, disintegrants, etc.

2) Multiple Compressed Tablets: Multiple compressed tablets are prepared by more

than one compression cycle. This process is best suited when separation of active ingredient
is needed for stability purposes, or if the mixing process is inadequate to guarantee uniform
distribution of two or more active ingredients. There are three categories under this class:
Compression coated tablets, Layered tablets and Inlay tablets.

3) Compression Coated tablets: This tablet readily lends itself into a repeat action.
Outer layer provides the initial dose while the inner core releases the drug later on. Hence, it
is useful for releases of two active pharmaceutical ingredients (APIs), one immediate release
formulation which is entrapped in coat and the other sustained release formulation
entrapped in the core. It is also possible to provide loading dose and maintenance dose for
one drug using this concept. Colton 232, Stock 538 and Manesty Drycota 900 are
equipment’s utilized for preparing compression coated tablets.

a) Sugar Coated Tablets: The sugar coat protect the enclosed drug from the environment and
provide a barrier toobjectionable taste or odour. It also produces an elegant, glossy
appearance. The patient acceptability also increases due to the sweet taste of tablet. Widely
utilized in preparing multivitamin and multivitamin mineral combination.

b) Film Coated Tablets: It is the type of coated tablets in which drug is not required to
coating. In case to provide more strength to the tablet, film coating is used as alternative to
sugar coating. The polymers such as HPC (Hydroxypropyl cellulose), HPMC
(Hydroxypropylmethyl cellulose), and Ethyl cellulose are used for this technique. It is also a fast
process than the sugar coating technique. It has the advantages over sugar coating in that it is
more durable, less bulky and less time consuming to apply, but it is less attractive and elegant
in physical appearance than sugar coating. The coating is designed to rupture and expose the
core tablet at the desire location in the gastrointestinal tract.

c) Gelatin Coated Tablets: The innovator product, the gel cap 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 facilities swallowing, and gelatin–coated
tablets are more tamper evident than unsealed capsule.

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d) Enteric Coated Tablets: The enteric coated tablets are coated with the material resistant to
acidic medium (stomach environment) and hence are not able to release drug in stomach.
Whereas, it easily releases drug in intestine (alkaline) media. Hence, drugs have to pass
through stomach and the time of release of drug is delayed and hence called delayed action
tablet.

-Layered Tablets: Layered tablets are composed of two or three layers of granulation
compressed together. Theyhave the appearance of a sandwich because the edges of each
layer are exposed. When two or more active pharmaceutical ingredients are needed to be
administered simultaneously and they are incompatible, the best option for the formulation
pharmacist would be to formulate multilayered tablet. A single tablet composed of two or
more layers and usually each layer is of different color to produce a distinctive looking tablet
Equipment-Versa press [7].

-Inlay Tablets: A variation of the compression coated tablet is the inlay, dot, or bull's-eye
tablet. Instead of the core tablet being completely surrounded by the coating, its top surface
is completely exposed. This form can be useful in sustained release preparations to reduce
the size and weight of the tablet. Two drugs are incorporated in tablet, one in core and one in
coat. Release of both drugs starts immediately but coating is responsible for slow release
and core is responsible for immediate release of incorporated drugs. Inlay tablet are
prepared with the Stokes, Colton, or Kilian machines. No alterations in equipment are needed
only the feed frame and hopper, which normally provide the top coating, are not installed.

3) Targeted Tablets:

Under this category there are two types of tablets.

a. Floating tablets: These are designed to prolong the residence time of the dosage form
within the GI tract. This not only prolongs GI residence time but also does so in an area of
the GI tract that would maximize drug reaching its absorption site in solution and hence,
ready for absorption. These are low density tablets. It can expand in gastric environment.
Floating in diarrhoea to keep the drug in floating condition in stomach to get a relatively
better response. Controlled delivery of drugs. It minimizes the mucosal irritation by releasing
drug slowly. Used in treatment of gastrointestinal disorders such as gastro esophageal reflux.
Ease of administration and better patient compliance.

b. Colon Targeting Tablets: It provides a desired drug concentration in the body by delivering
a therapeutic amount of drug to a target site i.e. colon. It is suitable and required for the drugs
having instability, low solubility, and short half-life, a large volume of distribution, poor
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absorption, low specificity, and therapeutic index. The pH in this region (colon) varies from 6.4-
7 and presence of microbial flora plays an important role in drug release. Various mechanisms
adopted for drug release in this area are: Coating with pH sensitive polymer e.g., Eudragit S100
and L100; Biodegradable polymer which are sensitive to colonic bacteria; Bio- adhesive
polymer e.g., poly carbophils. Redox sensitive polymers. It provides delivery of drugs accurately
into the lower GI tract (by avoiding the drug release in upper GIT), which occurs primarily in the
large intestine.

4)Chewable Tablets: Chewable tablets which are required to be broken and chewed in
between the teeth before ingestion. These tablets are given to the children who have
difficulty in swallowing and to the adults who dislike swallowing. These tablets are intended
to disintegrate smoothly in mouth at a moderate rate either with or without actual chewing.
Chewable tablet are often employed when the active ingredient is intended to act in a
localized manner rather than systemically the composition of chewable tablet consists of
gum core, which may or may not be coated. The core is composed of an insoluble gum base
like fillers, waxes, antioxidants, sweeteners, flavoring agents. The percentage of gum base
varies from 30-60%. Mannitol is widely used as an excipient in chewable tablet for its non-
hygroscopic nature for moisture sensitive drugs.

5) Dispersible Tablets: Dispersible tablets as defined in European Pharmacopoeia are

uncoated or film coated tablets intended to be dispersed in water before administration
giving a homogeneous dispersion. Typically a dispersible tablet is dispersed in about 5 to
15 ml of water (e.g. in a tablespoonful or a glass of water) and the resulting dispersion is
administered to the patient. Dispersible tablets are required to disintegrate within 3 min in
water at 15 to25. Also the dispersion produced from a dispersible tablet should pass through
a sieve screen with a nominal mesh aperture of 710 µm .

B) TABLETS USED IN ORAL CAVITY

1) Lozenges and Torches: Lozenges are flavored medicated dosage forms intended to be
sucked and held in mouth or pharynx. Two lozenge forms include hard (or boiled) candy
lozenges and compressed tablet lozenges (TROUCHES). Lozenges may be used for; Local
medications in the mouth or throat, Systemic drug uptake. Soft variety of lozenge, called a
pastille, consists of medicament in a gelatin or glycero- gelatin or in a base of acacia, sucrose
and water. No disintegrant is included in compressed lozenges composition. Other additives
(binder and filler) must have pleasant taste or feeling during dissolution. Common binder used
in compressed lozenges is gelatin; common fillers are (Sorbitol, mannitol and glucose)

2) Sublingual Tablets: They are to be placed under the tongue and produce immediate
systemic effect by enabling the drug absorbed directly through mucosal lining of the mouth
beneath the tongue. The tablets are usually small and flat, compressed lightly to keep them
soft. The tablet must dissolve quickly allowing the drugs to be absorbed quickly It is designed to
dissolve in small quantity of saliva. Sublingual, meaning literally 'under the tongue' refers to a
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method of administering substances via the mouth in such a way that the substances are
rapidly absorbed via the blood vessels under the tongue rather than via the digestive tract .

3) Buccal Tablets: These drugs are intended to be dissolved in buccal pouch. Tablets are
designed not to disintegrate. It is placed near the opening of parotid duct to provide the
medium to dissolve the tablet. Buccal tablets are most often used when replacement hormonal
therapy is the goal. Long–Acting Buccal Tablets include use of viscous natural or synthetic gums
or mixtures of gums can be compressed to form a hydrated surface layer from which the
medicament slowly diffuses and is available for absorption through buccal mucosa.
Mucoadhesive polymers like PANA and carbopol 934 are used.

4) Dental Cones: These tables are designed to be loosely packed in the empty socket
remaining following a tooth extraction. Main purpose behind the use of this tablet is either to
prevent multiplication of bacteria in the socket by employing a slow releasing antibacterial
compound or to reduce bleeding by an astringent or coagulant containing tablet. It’s
formulated to dissolve or erode slowly in presence ofa small volume of serum or fluid over
20-40 minutes period. Usually used vehicles are sodium chloride, sodium bicarbonate or
amino acid.

5) Mouth Dissolved or Rapid Dissolving Tablets: Mouth dissolving tablets can define
as "A solid dosage form containing medicinal substances, which disintegrates rapidly, usually
within a matter of seconds, when placed under the tongue. Mouth Dissolving Tablet has a
pleasing mouth feel, and it not required water to swallow. MDT easily dissolved or
disintegrates in saliva within a few seconds (15 s to 3 min). .Some MDT tablets are designed
to dissolve in saliva remarkably fast, within a few seconds, and are called true fast- dissolving
tablets. Others contain agents to enhance the rate of tablet disintegration in the oral cavity
and are more appropriately termed as fast- disintegrating tablets, as they may take about
one minute to disintegrate completely. Having good hardness, dose uniformity, easy
administration and serves as the first choice of dosage form for pediatrics, geriatrics and
travelling patients .

C) Tablets Administered by Other Routes

1) Vaginal Tablets: Designed for vaginal administration in treatment of local vaginal
infections, for systemic absorption and absorption into vaginal tissue can be inserted with aid
of an applicator. In the treatment of localized vaginal infections such as, Candida albicans,
yeast and Haemophilus vaginalis. These are uncoated bullet shape or ovoid tablets. Designed

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to under go slow dissolution and drug release in vaginal cavity. Pleased in an upper region of
vaginal tract by plastic tube inserter. Itmay contain antibacterial, antiseptic, or astringents .

2) Rectal tables: It is old and acceptable means of treatment. The volume and nature of
rectal fluid, its buffer capacity, pH and surface tension play a large part in this but are subject to
wide variation, even within single subject, resulting in variability of absorption by this route.
Rectal tables not required refrigeration. Better product stability even at room temperature.

3) Implants: These tablets are implanted in the body cavities for a prolonged effect from
several days to months up to year. These tablets are small in size and cylinder like in shape.
They are designed for subcutaneous implantation by surgical procedure where they are slowly
absorbed over a period of month or a year. Special injector with a hollow needle and plunger
is used to administer the rod shaped tablet. For other shapes surgery is used. They are sterile
formulations without excipients. Mainly these tablets are prepared to deliver growth
hormones to food producing animals. Ear is preferred site for administration of drug

ACTION WISE
Modified Release Tablet: Release the medicament slowly for long time duration after
administration of a single tablet. Used to target the site specific releases. Comparison of blood
concentration vs. time any adjuvant that can alter water uptake rate, swelling, and gelling
characteristics can alter the release rate of API.The drug release can be modified by providing
suitable micro environment pH in the tablet .Inclusion of alkaline polymers results in desirable
drug release of acidic drugs.

TABLET COATING:
Coating is a process by which an essentially dry,outer layer of coating material is applied to the
surface of a dosage form in order to conferspecific benefits over uncoated varietyCoating may
be applied to a wide range of oral solid dosage form, such as particles, powders,granules,
crystals, pellets and tablets. Whencoating composition is applied to a batch oftablets in a
coating pan, the tablet surfaces become covered with a tacky polymeric film.Before the tablet
surface dries, the applied coating changes from a sticky liquid to tacky semisolid, and eventually
to a nonsticky dry Surface pans. The entire coating process is conducted in a series of
mechanically operated acorn-shaped coating pans of galvanized iron stainless steel or copper.
The smaller pans are used for experimental, developmental, and pilot plant operations, the
larger pans for industrial production.

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Objectives to coat a tablet
THERAPY
• To avoid irritation of oesophagus and stomach
• To avoid inactivation of drug in the stomach
• To modify the drug release

• To improve patient compliance

• To mask the bitter taste

TECHNOLOGY
• To decrease the influence of moisture and atmosphere.
• Reduces the risk of interaction between incompatible material
• Improve the drug stability
• To prolong the shelf life of the drug

MARKETING
• To avoid bitter taste
• To improve product identity
• To improve the appearance and acceptability
• In improving product robustness

Disadvantages of tablet coating

• Disadvantages of sugar coating such as relatively high cost, long coating time and high bulk
have led to the use of other coating materials.
• However the process of coating is tedious and time-consuming and it requires the expertise of
highly skilled technician.

COATING PROCESS
Equipment
A. Conventional Pan Systems

B. Perforated Pans Systems

C. Fluid Bed Systems

A. Conventional pan systems: The standard coating pan system consists of a circular metal
pan mounted somewhat angularly on a stand. The pan is 8-60 inches diameter and is rotated on
its horizontal axis by a motor. Heated air is directed into the pan and onto the tablet bed
surface, and is exhausted by means of ducts positioned through the front of the pan.

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B. Perforated pan system: It consists of a Perforated or partially perforated drum that
rotates on its horizontal axis in an enclosed housing.

Driacoater:
• Introduces drying air through hollow perforated ribs located inside periphery of the drum.
• As the coating pan rotates, ribs dip into tablet bed
• Drying air passes up through and fluidizes the tablet bed
• Exhaust is from the back of the pan

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C. Fluidized bed (Air suspension system):
• These are highly efficient drying systems
• Fluidization of tablet bed is achieved in a columnar chamber by the upward flow of drying air.
• The airflow is controlled so that more air enters the center of the column, causing the tablets
to rise in the center.
• The movement of tablets is upward through the center of the chamber. They then fall
towards the chamber wall and move downward to re-enter the air stream at the bottom of the
chamber.
• Coating solutions are continuously applied from a spray nozzle located at the bottom of the
chamber or are sprayed onto the top of the cascading tablet bed by nozzles located in the
upper region of the chamber.

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TYPES OF COATING PROCESSES
Three main types of coatings used in the
pharmaceutical industry are
• Sugar coating
• Compression coating
• Film coating

1. SUGAR COATING:
• It involves successive application of sucrose based coating formulations to tablet core, in
suitable coating equipment.
• Water evaporates from the syrup leaving a thick sugar layer around each tablet.
• Sugar coats are often shiny and highly colored.
• Typically, tablets are sugar coated by panning technique, using traditional rotating sugar-
coating pan with a supply of drying air (thermostatically controlled).
• The pan is automatically rotated, allowing tablets to tumble over each other while making
contact with the coating solutions which are gently poured or sprayed, portion wise onto the
tablets with warm air blown to hasten drying. Each coat is applied only after the previous coat
is dried.

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2. COMPRESSION COATING
• Although less popular, it gained increased interest in recent years for creating
modifiedreleased
products involves the compaction of granular materials around preformed tablet core using
specially designed tableting equipment.
• Compression coating is a dry process.
• After tablet / core manufacture, it is transferred ( centrally positioned) to a slightly larger die
that is partially filled with a coating powder. More coating powder is filled on the top of the
core and compressed again resulting in tablet with in tablet.
• Mechanically, it a complex process, as a tablet may be tilted when transferred to a secondary
die cavity.
Need for compression coating
• Traditionally, to separate incompatible material (one in core and other in coat). There is an
interface between two layers and thus compromise product stability. It is possible to apply an
inert placebo coating layer first, to separate core from the final coat.
• Used to create modified release product.

3. Film Coating
Film coating and sugar coating shares the same equipments and process parameters.
Two methods,
1) Pan-Pour method:
• Same as that of pan-pour sugar coating
• Method is relatively slow and relies heavily on skill and technique of operator
• Aqueous based film coating is not suitable due to localized over-wetting.
2) Pan-Spray method:
• Use of automated spraying system
Types of film coating
• Immediate release

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• Modified release

COATING COMPOSITION
• Polymers
• Solvents
• Plasticizers
•Colorants

1. POLYMER / FILM FORMER: A film former capable of producing smooth thin films
reproducible under the prescribed coating conditions.
Classified as
1. Non enteric materials
E.g. HPMC, MHEC, EC, HPC, Povidone, SCMC
2. Enteric materials
E.g. CAP, Acrylate Polymers, HPMCP, PVAP

POLYMERS FOR FILM COATING

-Immediate release coating polymer
1.Cellulose derivatives:
The mostly widely used of cellulosic polymers is
HPMC
- It is readily soluble in aqueous media
2. Vinyl derivative
A copolymer of PVP and vinyl acetate forms better films.

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Modified release coating polymers
-Extended release Enteric coating
They are dissolved inOrganic solvent or dispersed in aqueous medium (why for enteric
coating?)
Cellulosic derivatives:
Highly substituted cellulosic ether, thus rendering the polymer water-insoluble.
E.g. Ethyl cellulose

Enteric coating
1.Methacrylic acid copolymers:
The presence of carboxylic acid groups renders this class to be insoluble in water at low PH
(stomach) but gradually becomes soluble as the PH rises. E.g. Ethyl cellulose towards neutrality
(upperpart of the small intestine).
2. Phthalate esters:
e.g.celluloseacetatephthalate

2. PLASTICIZER:
These afford flexibility and elasticity to the coa and thus provide durability.
They are of two types:
• Internal plasticizers: Chemical modification of the polymer that alters the physical properties.
o Degree of substitution
o Type of substitution
o Chain length.
• External plasticizers : They are non-volatile or the other polymer, which when include with
primary polymeric film former, changes the flexibility.
Tensile strength, or
o Adhesion properties of the resulting film.
Concentration of Plasticizer Expressed as the
amount of polymer being plasticized.
Recommended Level of Plasticizer: 1 to 50% by
weight of the film former.
EXAMPLES
• Castor oil; propylene glycol of 200 and 400
series; and surfactants eg; Tweens; Spans;
and organic acid esters.
• Water- soluble plasticizer: PEG, propylene
glycol.
• Organic- soluble plasticizer : castor-oil and

3. COLORANTS
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• Colorants may be soluble in the solvent system or suspended as insoluble powders.
• Used to provide distinctive color and elegance to a dosage form.
• To achieve proper distribution of suspended colorants in the coating solutions requires the
use of finepowdered.
colorants (< 10 microns ).
• Most of colorants are synthetic DYES or LAKES OF DYES approved by the FD&C and D&C.
LAKES: derived from dyes by precipitating with carriers. Eg; alumina or talc.
• Lakes contains 10 to 30 % of the pure dye content.
• For very light shade, concentration: less than 0.01 %.
• For dark shade, concentration : more than 2.0 %
• Examples
– Inorganic materials: iron oxides
– Natural coloring materials: Anthocyanins, caramel, carotenoids, chlorophyll, indigo, flavones,
turmeric, and carminic acid

4. SOLVENTS
Volatile organic solvents may be used to allow good spreadability of the coat components over
the tablet and allowing rapid evaporation, but they are expensive and show environmental
hazards. Aqueous vehicles are safer, but they show slower evaporation and may affect drug
stability.

Ideal characters of coating material

1)Solubility in the coating solution.
2) Capacity to produce elegant looking product.
3 ) Stability in presence of water, heat, moisture, air, and substrate being coated and no
change in properties with aging.
4) Essentially no odor or taste.
5) Compatibility with common coating solution additives.
6) Nontoxic and ease of application.
7) Resistance to cracking and should act as barrier.
8) No bridging or filling of the debossed tablet surfaces by the film former.
9) Ease of printing procedure on highspeed equipment.
10) Low cost & Ease of application without specialized equipment.

PREPARATION OF TABLETS
Tablets are prepared by three methods
1) Wet granulation method
2)Dry granulation method
3)Direct compression

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1) Wet Granulation Method - It is the most common and widely used method. This
method involves various steps like weighing of ingredients, mixing, granulation, and screening
of damp pass, drying, lubrication and compression of tablets. The main active ingredient,
diluent, disintegrant are blended together, and then it is allowed to pass through the sieve
(sifting). Solutions of the binding agent are added to the initial mixture with stirring. The
amount of binding agent added should be sufficient, in order to avoid over wetting of the tablet
[46- 60]. If the powder is not wetted properly, the granules will be too soft and can be broken

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down during lubrication, which is difficult during compression of tablet. Tray drying is most
common method of drying the tablet granules, Tray drying was the most widely used method
of drying properly, the granules will be too soft and can be broken down during lubrication,
which is difficult during compression of tablet. Tray drying is most common method of drying
the tablet granules, Tray drying was the most widely used method of drying through the screen;
usually 60-100 mesh nylon cloth is used. After dry granulation, lubricant is added as fine
powder, which is required for proper filling of the die cavity .

2) Dry Granulation Method: This method is used for tablet preparation, in case tablet
ingredients are highly sensitive to moisture, or unable to with stand elevated temperatures
during drying, slugging may be used to form the granules. Dry granulation or double
compression, usually eliminates various steps, which involves slugging of the powder mass.The
active ingredient, diluent and lubricant are blended together, to form the slug. Thus, the
compressed slug is passed through the mesh or through the mill and the remaining lubricant
is added to the granulation, blended properly and compressed to form the tablets.

3) Direct Compression: Direct compression involves direct compressing the powdered

Material into tablets. Direct compression is adopted, if drug constitutes major portion of
tablet [86-90] total weight (Figure 1). Tablets containing 25% or less of drug substances can
be formulated, with a suitable diluent which acts as a carrier or vehicle for the drug. Tablets
prepared by above method are subjected to compression machine which may be single
station or multiple station.

Tablet presses
Tablet presses, also called tableting machines, range from small, inexpensive bench-top models
that make one tablet at a time (single-station presses), with only around a half-ton pressure, to
large, computerized, industrial models (multi-station rotary presses)
that can make hundreds of thousands to millions of tablets an hour with much greater
pressure. The tablet press is an essential piece of machinery for any pharmaceutical and
nutraceutical manufacturer. Tablet presses must allow the operator to adjust the position of
the lower and upper punches accurately, so that the tablet weight, thickness and
density/hardness can each be controlled. This is achieved using a series of cams, rollers, or
tracks that act on the tablet tooling (punches). Mechanical systems are also incorporated for
die filling, and for ejecting and removing the tablets from the press after compression.
Pharmaceutical tablet presses are required to be easy to clean and quick to reconfigure with

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different tooling, because they are usually used to manufacture many different products. There
are two main standards of tablet tooling used in pharmaceutical industry:
American standard TSM and European standard EU. TSM and EU configurations are similar to
each other but cannot be interchanged.
Modern tablet presses reach output volumes of up to 1,700,000 tablets per hour. These huge
volumes require frequent in-process quality control for the tablet weight, thickness and
hardness. Due to reduce rejects rates and machine down-time, automated tablet testing
devices are used on-line with the tablet press or off-line in the IPC labs

The tablet pressing operation

24
New marketed formulation
Brand Active Ingredient (Salt) Primary Use
Name
Erleada Apalutamide Non-metastatic castration-resistant prostate cancer
Orilissa Elagolix Endometriosis pain
Aimovig Erenumab Prevention of migraine headaches
Nerlynx Neratinib Early-stage HER2-positive breast cancer
Tavalisse Fostamatinib Chronic immune thrombocytopenia
Xpovio Selinexor Relapsed or refractory multiple myeloma
Xofluza Baloxavir marboxil Acute uncomplicated influenza
Rybelsus Semaglutide Type 2 diabetes
Reyvow Lasmiditan Acute treatment of migraine
Nubeqa Darolutamide Non-metastatic castration-resistant prostate cancer
Tukysa Tucatinib HER2-positive breast cancer
Oxlumo Lumasiran Primary hyperoxaluria type 1
Jelmyto Mitomycin Low-grade upper tract urothelial cancer
Cabenuva Cabotegravir/Rilpivirine HIV treatment (long-acting injectable)
Evrysdi Risdiplam Spinal muscular atrophy
Zynlonta Loncastuximab tesirine- Relapsed or refractory large B-cell lymphoma
lpyl
Amondys 45 Casimersen Duchenne muscular dystrophy with exon 45
skipping
Truseltiq Infigratinib Cholangiocarcinoma
Rezurock Evrysdi Tuberous sclerosis complex (TSC)-associated
seizures
Ponvory Ponesimod Relapsing forms of multiple sclerosis

25