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TABLE

TS
PREPARED BY:
ASHWINI JOSHI
ASSISTANT PROFESSOR
SVCP,HYD
CONTENTS
INTRODUCTION
• Tablets are compressed solid unit dosage
form containing medicament or medicaments
usually circular in shape and may be flat or
biconvex.
• Tablet is defined as a compressed solid dosage
form containing medicaments with or without
excipients.
• 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.
• It is the most popular dosage form and 70% of the
ADVANTAGES & DISADVANTAGES
• Advantages of tablets:
✔ Easy to administered.
✔ Easy to dispense.
✔ More stable.
✔ Accuracy in dose.
✔ Bitter and nauseous substance can be easily dispensed.
✔ Light and compact.
✔ Economical.
✔ Sustained release product is possible by enteric coating.
• Disadvantages of tablets:
✔ 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.
TYPES OF TABLET
1. Compressed 2. Sublingual
2. Multiple 1. Buccal tablet, e.
tablet, e.g. tablet,
compressed g.
Paracetamol e.g. Vicks
tablets, Vitamin-c tablet
tablet Menthol
(A) Tablets (B) Tablets
ingested used in oral tablet
orally cavity
3. Delayed
release tablet, 4. Sugar
3. Troches 4. Dental
e.g. Enteric coated
or cone
coated tablet, e.g.
Bisacodyl lozenges
1. Implantation Multivitamin
2. Vaginal 1. 2. Dispensing
tablet tablet
tablet, e.g. tablet, Effervescent tablet, e.g.
Testosterone e.g. tablet, e.g. Enzyme
tablet (c) Tablets Clotrimaz Disprin (D) Tablets tablet (Digiplex)
administered used to
by ole tablet tablet (Aspirin)prepare
other route solution:
4. Tablet
3.
triturates
Hypoder
e.g. Enzyme
mic
tablet
tablet
(Digiplex)
TABLETS INGESTED ORALLY
1. Compressed tablet: These are uncoated tablets made by compression of granules.
These provides rapid disintegration and drug release. e.g. Paracetamol tablet.
2. Multiple compressed tablet: These tablets are prepared to separate physically or
chemically incompatible ingredients or to produce repeat action or prolonged action
products. The ingredients of formulation are compressed into a core tablet and the
incompatible substance with other excipients are compressed over the previously
compressed core tablet.
3. Sustained action tablet: These tablets when taken orally release the medicament in a
sufficient quantity as and when required to maintain maximum effective concentration of
drug in the blood.
4. Enteric coated tablet: These tablets are coated with the material which does not
disintegrate in stomach but passes through as it is i.e. enteric polymer e.g.:
Hydroxypropyl methyl cellulose phthalate etc. These tablets dissolve in intestine and are
site specific.
5. Sugar coated tablet: The compressed tablets with sugar coating are called sugar coated
tablets. It is done to mask the bitter and unpleasant taste and odour of the medicament. It
enhances the appearance and protects the drug from atmospheric effects. e.g.
Multivitamin tablet
6. Film coated tablet: These are the compressed tablets having a film coating of film
coating polymer like hydroxy propyl cellulose, ethyl cellulose , HPMC. It also protects the
formulation from atmospheric effects. These are tasteless, have increase in tablet weight
and have less elegance. e.g. Metronidazole tablet
7. Chewable tablet: These tablets are chewed in mouth and are broken into small pieces.
ORAL CAVITY TABLETS
1. Buccal Tablets:
These tablets are to be placed in buccal pouch or between the gum & lip or cheek.
Tablet dissolve & disintegrated slowly & absorb directly.
2. Sublingual Tablet:
These tablets are to be placed under the longue. They dissolve & disintegrated
quickly & absorbed directly without passing into G.I.T. Buccal and sublingual tablet
should be formulated with bland excipients, which do not stimulate salivation.
3. Lozenge tablet & troches:
These tablets are designed to exert a local effect on mouth or throat. These tablets
are usually used in treatment of sore throat or control coughing. The tablets are
usually used to such drug as anaesthetic, antiseptic and antibacterial agent,
demulcent, astringent and antitussive agent. Lozenges were earlier called pastilles.
4. Dental cones:
These are relatively minor compressed tablet meant for placing them in the empty
socket after tooth extraction. Usually, these tablets contain an antibacterial,
compound which is released slowly. Prevent the growth of bacteria. These tablets
may contain an astringent or coagulant to reduce bleeding. The base for these
types is sodium bicarbonate, sodium chloride or it may be amines acid. These
cones generally get dissolved in 20 to 40 min time.
TABLETS ADMINISTERED BY OTHER ROUTE
1. Implantation tablet:
These tablets are placed below the skin or inserted subcutaneously by
means of a minor surgical operation and are slowly absorbed. These
must be sterile and are made by heavy compression and fusion. e.g.
Testosterone tablet.
2. Vaginal tablet:
These tablets are meant to dissolve slowly in vaginal cavity. These are
ovoid or pear shaped and are used to release steroids, antibacterial and
antiseptics etc to avoid infections. e.g. Clotrimazole tablet.
TABLETS USED TO PREPARE SOLUTIONS
1. Effervescent tablet:
These tablets when added in water produce effervescence. So they
dissolved rapidly in water due to the chemical reaction which takes place
between alkali bicarbonate and citric acid or tartaric acid. These tablets
are to be protected from atmospheric moisture during storage (in well
closed container). e.g. Disprin tablet (Aspirin)
2. Dispensing tablet:
These are intended to be added to a given volume of water to produce a
solution of a given concentration. The medicaments given are silver
proteinate and quaternary ammonium compounds. These are highly
toxic if taken orally and great care must be taken in packaging and
labelling. e.g. Enzyme tablet (Digiplex)
3. Hypodermic tablet:
These are compressed tablets which are composed of one or more drugs.
These tablets are dissolved in sterile water and administered parenterally.
4. Tablet triturates:
These are small cylindrical, moulded or compressed tablets which
contains a potent medicament with a diluent. On small scale hand
operated whereas for bulk production automated machines are used. e.g.
Enzyme tablet (Digiplex)
TABLET TYPES AND
EXCIPIENTS
PREPARED BY:
ASHWINI JOSHI
ASSISTANT PROFESSOR
SVCP, HYDERABAD
TYPES & CLASSES
OF TABLETS
1.ORALLY INGESTED TABLETS:

Over 90% of
tablets
manufactured
are ingested
orally.
These are
designed to
be swallowed
intact, with
exception of
chewable tablets.
COMPRESSED TABLETS OR STANDARD
COMPRESSED TABLETS:

- These are standard uncoated tablets made by


compression using wet granulation, direct compression or
double compression.
- Provide rapid disintegration & drug release.
- Mostly intended to exert local action in GIT.
- Typically include water insoluble drugs such as antacids
and adsorbents.
- Other drugs having systemic effect have some aqueous
solubility, dissolve from tablet and disintntegrate tablet
MULTIPLE COMPRESSED TABLETS:

There are 2 classes of multiple compressed tablets:


1. layered tablets
2. compression coated tablets

-Both types may be either two component or three component


systems: two or three layer tablets, a tablet within a tablet or a
tablet within a tablet within a tablet.
-Both types usually undergo a light compression as each
component is laid down, with the main compression being the
final one.
-The layered tablet is preferred to the compression
coated tablet because surface contact between
layers is lessened and production is simpler and
more rapid.

ADVANTAGES:
-Separate physically or chemically incompatible
ingredients.
DELAYED ACTION AND ENTERIC COATED TABLETS:
- Delayed action tablets are intended
to release a drug after some delay or
after the tablet has passed through
one part of GI tract into other.
- The enteric coated tablet is the most
common example of a delayed action
type product.
- The polymers used in enteric coating
are acid esters, are insoluble in gastric
media that have a pH of about 4 and
begin dissolving as the tablets enter
duodenum (pH of 4 to 6).
- Cellulose acetate phthalate
- Polyvinylacetate phthalate
- Hydroxypropylmethyl cellulose phthalate
Advantages:
Enteric coated tablets are used for drugs such as:
- Drugs irritating to gastric mucosa which include aspirin and
strong electrolytes such as NH4CL.
- Drugs that are destroyed by low pH of stomach
- Drugs that cause nausea and vomiting if released in
stomach
- Drugs that are to be released undiluted and in highest
possible concentration within intestine
SUGAR-COATED TABLETS:

an elegant, glossy, easy-to-swallow tablet


dosage form.
they permit separation of incompatible
ingredients between coating and core, and
utilized in preparing many multivitamin and
multivitamin mineral combinations.

Disadvantages:
The process is time consuming and require
skilled coating artisans.
The use of water soluble
polymers, automated-spray
coating equipment, and high-
drying- efficiency sidevented
coating pans have greatly
reduced some of these
disadvantages, resulting in:
more elastic and
mechanically stable coatings
coat weight may be 50% or
less of the core weight
the process may be completed
in a day or less.
These are an alternative to sugar coated tablets in which
drug is not required in the coating.
The film coating composition consists of one or more
polymers, a plasticizer for the polymer and a surfactant, all
delivered to the tablets in solution from an organic or
aqueous solvent.
Polymers used: hydroxypropyl cellulose, hydroxypropyl,
methylcellulose, 30% ethylcellulose dispersion (Aquacoat),
Advantages:
tasteless.
tablet coating operation takes only one or two hours.
better mechanical strength of the coating based on
elasticity & flexibility of polymer coating.
little increase in tablet weight than sugar-coated
ability to retain debossed markings on the tablet
avoidance of sugar, which is contraindicated in diet of
some people.
Disadvantages:
less attractive and elegant in physical appearance than
CHEWABLE TABLETS:

Intended to be chewed in the mouth prior to swallowing and


are not intended to be swallowed intact.

Examples:
-Chewable aspirin tablet for children use.
-Antacid tablet

Advantage:
provide a unit dosage form of medication which
can be easily administered to infants and children
or to the elderly, who may have difficulty swallowing a tablet
intact.
Disadvantage:
Bitter or foul tasting drugs can not be given by this dosage
form
2.
TABLE
TS
USED
IN
THE
ORAL
BUCCAL AND SUBLINGUAL TABLETS:
• Small, flat tablets, intended to be held between cheek
and teeth or in the cheek pouch (buccal tablets) or
beneath the tongue (sublingual tablets).
• Release drug contents for absorption directly through
oral mucosa.
• Designed not to disintegrate but to slowly dissolve,
over a 15 to 30 min
period.
• Produce systemic drug effects as the drug is absorbed
from oral mucosa to blood stream leading directly to
general circulation.
• Shoud be formulated with bland excipients.

Advantages:
• More rapid onset of action.
• It avoids 1 st pass metabolism of drugs.
• Protects the drug from extensive decomposition of the
gastric
environment.
TROCHES AND LOZENGES:

Disc shaped solid dosage forms containing


medicinal agent
& flavoring substance in a hard candy or sugar base.
Intended to exert a local effect in the mouth or
throat.
Commonly used to treat sore throat or to control
coughing in normal cold.
May contain local anesthetics, antiseptics,
antibacterials,
demulcents, astringents and antitussives.
Designed not to disintegrate but to dissolve or slowly
erode over a period of 30 min or less in mouth.
Lozenges: also called pastilles or cough drops. They
may be made by compression but are usually
formed by fusion or by a candy-molding machine.
Troches: are made by compression.
DENTAL CONES:

- Designed to be placed in the


empty socket remaining following
a tooth extraction.
- It is formulated to dissolve slowly
in presence of a small volume of
serum/ fluid over a 20 or
40 min period.

Uses:
- To prevent multiplication of
bacteria in the socket by
employing a slow releasing
antibacterial.
- To reduce bleeding by containing
an astringent or amino acid.
3. TABLETS ADMINISTERED BY OTHER ROUTES

Vaginal tablets / Inserts:


Uncoated bullet shaped or ovoid tablets.
Designed to undergo slow dissolution
and drug release in vaginal cavity.
It may contain antibacterials, antiseptics or astringents to treat
vaginal infections such as vaginitis or antifungals to treat
fungal infections such as candidiasis or to release steroids for
systemic absorption.
often buffered to promote pH favorable
to action of an antiseptic agent.
Placed in the upper region of vaginal tract by plastic tube
inserter.
IMPLANTATION/DEPOT TABLETS:

Small, cylindric or rossete shaped forms,


not more than 8mm in length.
Designed for subcutaneous implantation.
Provide as constant a drug delivery rate
as possible.
Provide prolonged drug effects ranging
from one month to a year.

Disadvantages:
It has safety problems
Tissue toxicity problems in the area of
implantation site.
4.TABLETS USED TO PREPARE SOLUTIONS:

Effervescent Tablets:
Designed to produce a solution rapidly with the
simultaneous release of CO2.
prepared by compressing the active
ingredients with mixtures of organic acids
such as citric acid or tartaric acid and
NaHCO3.
When such a tablet is dropped into a glass of
water, a chemical reaction is initiated
between the acid and NaHCO3 to form
sodium salt of the acid and to produce CO2
in water. The reaction is quite rapid and is
usually completed within in one minute or
less.
The are packed in hermetic-type foil pouches
Advantages:
Provide a mean of extemporaneously
preparing a solution containing
accurate drug dose.
They produce pleasantly flavored
carbonated drink which assists in
masking the taste of certain drugs.
Disadvantages:
Difficulty of producing a chemically
stable product.
Moisture in air during product
preparation may be adequate to
initiate effervescent reactivity.
During the course of reaction, water is
liberated which autocatalyzes the
reaction.
Compression of tablet in the hands of
DISPENSING
TABLETS:

Intended to be added to a given volume of


water by the pharmacist or the consumer, to
produce a solution of a given drug
concentration.
Materials incorporated in dispensing tablets
include mild silver proteinate, bichloride of
mercury and quarternary ammonium
compounds.

Disadvantages:
Difficuty with dispensing tablets is that some of
the components previously used in this
dosage form are highly toxic and extremely
hazardous and even lethal if mistakenly
swallowed.
HYPODERMIC TABLETS:

They are composed of one or more


drugs with other readily soluble water
soluble ingredients and are intended
to be added to sterile water or WFI.
Advantage:
The physician can carry many vials of
tablets in his bag with only one bottle
of sterile WFI.
Disadvantage:
The likelihood of administering a
nonsterile solution, even though
portable sterile filteration equipment
exists to help assure sterility.
TABLET
TRITURATES:
Small, usually cylindric molded or compressed tablets.
Provide extemporaneous method of preparation by the pharmacist.
The drugs used were potent and mixed with lactose and a binder
such as powdered acaia, after which the mixture was moistened to
produce a moldable, compactable mass. This mass was forced
into holes of a mold board wood or plastic, after which tablets were
ejected using a peg board, whose pegs matched the holes in the
mold, dried and dispensed.
Disadvantages:
Unreliable bioavailability.
Poor content uniformity of tablets containing potent drugs.
TABLET EXCIPIENTS
THESE ARE THE SUBSTANCES
ADDED IN THE
MANUFACTURING OF TABLET
AND PERFORM FOLLOWING
FUNCTIONS:
• IMPART WEIGHT, ACCURACY, &
VOLUME
• IMPROVE SOLUBILITY
• INCREASE STABILITY
• ENHANCE BIOAVAILABILITY
• MODIFY DRUG RELEASE
• ASSIST PRODUCT IDENTIFICATION
• INCREASE PATIENT ACCEPTABILITY
• FACILITATE DOSAGE FORMDESIGN
EXCIEPIENTS-
FUNCTIONS
❑ Impart weight, accuracy, & volume(its allow acccuracy of
dose)
❑ Improve solubility
❑ Increase stability
❑ Enhance bioavailability
❑ Modifying drug release
❑ Assist pdt identification
❑ Increase patient acceptability
❑ Facilitate dosage form design

12-07-201 Sagar Kishor 37


6 Savale
EXCIPIENT FUNCTIONS
1. DILUENTS

Diluents are fillers used to make up required bulk


of the tablet when the drug dosage itself is
inadequate to produce the bulk.
Provide better tablet properties such as improved
cohesion or to promote flow.
PROPERTIES OF DILUENTS

1. They must be non toxic


2. They must be commercially available in acceptable
grade.
3. Their cost must be low
4. They must be physiologically inert
5. They must be physically & chemically stable by
themselves & in
combination with the drugs.
6. They must be free from any unacceptable microbial
contamination.
7. They must not be contraindicated by themselves and in
comibation with the drug and other tablet components.
8. They must be color compatible.
9. They must have no deleterious effect on the
bioavailability of drugs.
COMMONLY USED:
1. Lactose-anhydrous and spray dried
lactose
2. Directly compressed starch
3. Hydrolyzed starch
4. Microcrystalline cellulose-Avicel (2
grades: pH 101 and pH 102)
5. Dibasic calcium phosphate dehydrate
6. Calcium sulphate dihydrate
7. Mannitol
8. Sorbitol
9. Sucrose
10. Dextrose
2. BINDERS AND ADHESIVES:
These materials are added either dry or in liquid form to form
granules or to promote cohesive compacts for directly
compressed tablet.

• EXAMPLES:
Natural gums:
Acacia, tragacanth - 10-25% Conc solution
Disadvantages:
variable in composition and performance, based on their
natural origin
heavily contaminated with bacteria
Solution: When these materials are used, wet granulation
masses should be quickly died at 37C to reduce microbial
proliferation
• Cellulose derivatives: Methyl cellulose, Hydroxy propyl methyl
cellulose, Hydroxy propyl cellulose
Dry: binder properties
Aqueous solutions: adhesive properties.

•Natural protein: Gelatin- 10-20% solution


Advantage: more consistent material & easier to prepare in
solution form.
• Glucose: 50% soln in
Advantage: water low cost
Disadvantag bacterial proliferation
e:
•Synthetic polymer: Polyvinylpyrrolidone (PVP)- 2%
conc.

• Starch paste: 10-20% soln

• Sodium alginate
3.
DISINTEGRANTS

facilitate the breaking or disintegration of tablet when


it contacts water in the GIT.
draw water into the tablet resulting in swelling and
cause the tablet to burst apart.
help in dissolution of the drug and attainment of high
drug bioavailability.
They can increase in volume in the presence of
water by 200 to 500%.
• Examples:
• Starch- 5-20% of tablet weight.

• Starch derivatives – low substituted carboxymethyl starches


(used in
1-8% concentration. 4% usually optimum)

• Pre-gelatinized starches (5%)

• Clays- Veegum HV and bentonite (10%)

• Microcrystalline cellulose

• Cellulose derivatives- Ac- Di-Sol (internally cross linked


sodium
carboxymethylcellulose)
SUPERDISINTEGRANTS:

Swells up to ten folds within 30 seconds when


contact water.

• Examples:
Crosscarmellose- cross-linked cellulose
Crosspovidone- cross-linked povidone
(polymer) Sodium starch glycolate- cross-
linked starch.
4. LUBRICANTS, ANTIADHERENTS AND
GLIDANTS:

Lubricants are intended to reduce the friction


during tablet ejection between the walls of the
tablet and the walls of the die cavity in which the
tablet was formed.

Antiadherents are intended to reduce sticking or


adhersion of tablet granulation or powder to the
faces of the punches or to the die walls.

Glidants are intended to promote flow of granules


or powder material by reducing the friction
Lubricants:
-Stearic acid salts – Calcium and Magnesium stearate
- Stearic acid – it is less effective lubricant than stearic acid salts and also has a
lower melting point.
-Talc – it contains trace quantities of iron, therefore it should be considered carefully.
-PEG-- The finer the particle size of the lubricant, the more effective the lubricant
action.

• Antiadherents:
Starch, talc , magnesium
stearate

• Glidants:
Corn Starch – 5-10% conc
Talc- 5% conc
Silica derivatives - Colloidal silicas such as Cab-O- Sil in
0.25-3% conc.
5. COLORING AGENTS:
PURPOSE:
(1) Masking of color drugs
(2) Product Identification
(3) Production of more elegant product
• All coloring agents must be approved and certified by FDA. Two
forms of colors are used in tablet preparation –
FD &C and D & C dyes.
These dyes are applied as solution in the granulating agent or
Lake form of these dyes.
Lakes are dyes absorbed on hydrous oxide and employed as dry
powders for coloring.

• Example:
FD & C blue 2 - Indigo carmine
In any colored tablet, the formulation should be checked for
resistance to color changes on exposure to light.
6. FLAVORING AGENTS:

Used in chewable tablets or


tablets intended to dissolve in
mouth.
Flavor oils are used and are
added to tablet granulations in
solvents, are dispersed on clays
and other absorbents or
emulsified in aqueous
granulating agent.
The maximum amount of oil that
can be added is 0.5 -0.75%.
7. SWEETENING AGENTS:

Used only in chewable tablets to


exclude or limit the use of sugar
in the tablets.
Examples:
• Saccharine (artificial): 500 times
sweeter than sucrose
Disadvantage: Bitter after taste
and carcinogenic
• Aspartame (artificial):
Disadvantage: Lack of stability
in presence of moisture.
•Mannitol
8. WETTING AGENTS
• Water molecules attract each other equally in all directions. Water
molecules on the surface, however, can only be pulled into the bulk
water by water molecules underneath, since there are no water
molecules to pull in the opposite direction. The surface tension of water
is strong enough to support the weight of tiny insects such as water
striders.

• The surface tension in action can be visualized by placing a small drop of


alcohol on a thin layer of water. Alcohol with lower surface tension mixes
with water causing reduction in the surface tension in the local region.
Owing to the higher surface tension of water in the neighbor, water is
pulled
in from
th12e-07 m-20ithe alcohol
1 d6 dle of thedropped region into the neighbor, and this leads
water layer.
to the formation of a dry spot
FLOW
CHART
API
Filler Mixing of
screening
granulation blend

Preparation of Granulation
Binder(s) binder solution

Drying LOD

Milling

Disintegrant screening Initial Blending

lubricant screening
Final Blending

Weight
Compression Hardness
Friability

Film Coating of Tablets

Solvent
Preparation Packaging and
Film coating agent
Labelling

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