FORMULATION AND EVALUATION

2. 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.

3. 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 total medicines are
dispensed in the form of Tablet.

4. Tablets have less content uniformity
differences.
Easy to use and handle
Tablets are physically, chemically and
microbiologically stable dosage forms.
Manufacturing cost is less.
Shipping and transportation is easy and
cheap.

5. Drugs with high dose, low density and
hygroscopic in nature are difficult to
compress.
Drugs with bitter taste are difficult to
swallow.
Tablets are difficult to swallow for
paediatric and geriatric patient.

6. Tablets have the ability to be produced
with many different properties
including immediate, delayed or
sustained release of active drug
substance
They can be single or multiple
compression (double or triple layered,
tablet within a tablet)
They can also be coated with an active
drug substance, film or sugar coating

7. Physically Acceptable and Stable -
tablet print or imprint must be
legible, and tablets must be free
from chips, cracks, contamination,
uneven coloration
Tablets must remain whole during
manufacture, coating, packaging,
transport and dispensing

8. Tablets for oral ingestion
Compressed Tablets
•Multiple Compressed Tablets
•Delayed release Tablets
•Sugar coated Tablets
•Film coated Tablets
•Chewable Tablets

9. Buccal Tablets
Sublingual Tablets
Troches and lozenges
Dental cones

10. Implantable Tablets
Vaginal Tablets

11. Effervescent Tablets
Dispensible Tablets
Hypodermic Tablets
Tablets triturate

12. Compressed tablet
These are uncoated tablets made by
compression of granules.
These provides rapid disintegration and drug
release.
e.g. Paracetamol tablet.

13. 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.

14. 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.

15. 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.

16. 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

17. 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

18. 7. Chewable tablet:
These tablets are chewed in mouth and are
broken into small pieces.
Disintegration time is reduced and rate of
absorption increases.
Easily administered for elderly persons.
e.g. Antacid tablet

19. 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.

20. 2. Sublingual Tablet:
These tablets are to be placed under the
tongue.
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.

21. 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.

22. 3. Lozenge tablet & troches:
The tablets are usually used to such drug
as anaesthetic, antiseptic and antibacterial
agent, demulcent, astringent and
antitussive agent.

23. 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.

24. 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

25. 1. Effervescent tablet:
It 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)

26. 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.

27. 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.

28. 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)

29. A tablet is a combination of ingredients
that is compressed into a solid mass
The basic components of an immediate
release pharmaceutical tablet are
active drug substance
Diluents/ fillers
Binders
Disintegrants
Lubricants

30. Glidants
Anti-adherents
Anti-static agents
Colorants
Flavors
Sweeteners
Surfactants (Wetting agents)
Anti-oxidants
Film-coatings

32. BINDERS
PVP 0.5 – 4%
PREGELATIZED
STARCH
5-20% DIRECT
5-10% WET
MCC 5-25%
SUCROSE 50-70%
SOLUTION
HPC 4-6%
EC 5%
MC 1-6%

33. SR NO SOLVENTS
1 PURIFIED WATER
2 ETHANOL
3 PURIFIED WATER / ETHANOL
4 METHANOL+ISOPROPANOL

34. SR NO NAME QUANTITY
1 SODIUM STARCH GLYCOLATE 2-6%
2 CROSS CARMELLOSE SODIUM 1-6%
3 PREGELATIZED STARCH 5-10%
4 STARCH 5-10%
5 MCC 5-15%
6 CROSSPOVIDONE 2-5%

35. SR NO DISINTEGRATING AGENTS CONCENTRATION
(%W/W) IN
GRANULATION
1 STARCH USP 5-20
2 STARCH 1500 5-15
3 MCC (AVICEL) 5-15
4 ALGINIC ACID 5-15
5 GUAR GUM 2-8
6 MC, Sodium CMC 5-10

36. SR NO GLIDANTS, ANTIADHERENTS AND
LUBRICANTS
QUANTITY
1 FUMED SILICON DIOXIDE 0.1-0.5 %
2 MAGNESIUN STEARATE 0.25-2 %
3 STEARIC ACID 0.5-3 %
4 HYDROGENATED VEGETABLE OILS 2-5 %
5 SLS 1-3 %
6 MINERAL OIL 1-3 %
7 FUMED SILICON DIOXIDE 1-2 %

37. SR NO WETTING AGENTS QUANTITY
1 SLS 0.1-3%
2 POLYSORBATE 80 0.1-3%
ACIDIFYING AGENTS, BUFFERS,
STABILIZERS
3 CITRIC ACID 0.2-2%
4 SODIUM CITRATE 0.3-2%

38. The diluent is needed to increase the
bulk when quantity of medicament is
very small in each tablet.
e.g. Lactose, sucrose, sodium chloride,
dextrose and starch etc.

39. To break the tablet in smaller particles
when swallowed.
These acts by three ways:
swelling, by producing effervescence
and by melting at body temperature.

40. The disintegrating agent is divided into two
parts.
One part is mixed with other excipients before
granules formation and the other is mixed with
the dry granules before compression.
e.g. Potato, maize, wheat starch etc.

41. These provides moisture to convert the
fine powder into damp mass which after
passing through sieve forms granules.
e.g Starch paste, acacia, tragacanth,
gelatin solution, iso propyl alcohol etc.

42. To improve the flow properties
of granules.
e.g magnesium stearate & Talc

43. To reduce the interparticular friction
during compression and between tablet
and die wall during ejection of tablet.
e.g. Talc & magnesium stearate.

44. these provides strength to the
granules to keep the tablet intact and
selection of which depends on the
type of tablet
e.g. gum tragacanth, methyl cellulose
etc.

45. These are used to adsorb volatile
oil, liquid extracts and tincture
etc. Prevent sticking
e.g. Mg stearate, steraric acid etc.

46. 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.

47. SR NO DYES LAKES
1 Water soluble Water Insoluble
and colours by dispersion
2 May not mix with oils Not mix with oils but oil dispersible
3 Granular , dusty powder,
liquid dyes
Basically pigments
Soluble dye and metallic salt
causing precipitation to form lakes
4 D and C Certified Use in
drug and cosmetics but not in
food
FD and C Certified Use in drug and
cosmetics and in food
5 Migration of colours,
mottling
No Migration of colours and
mottling
6 Brilliant blue FCF, Acid Chocolate, red 40 aluminium lake

48. TABLET EXCIPIENTS EXAMPLES
DILUENTS Lactose USP, Mannitol USP, Sucrose,
Microcrystalline Cellulose NF, Sorbitol
BINDERS Acacia, Gelatin, Glucose, Starch
DISINTEGRANTS Starch, Starch Derivatives, Clays,
Cellulose, Alginates, PVP, Crosslinked
LUBRICANTS Stearic Acid, Talc, Surfactants, Waxes,
Polyethylene Glycol
ANTI-ADHERANTS AND
GLIDANTS
Silica Derivatives, Talc, Corn starch,
stearic acid and strearates
COLOURING AGENTS FD & C And D & C Dyes And Lakes
FLAVOURING AGENTS Mango, Pineapple, Rose
SWEETENING AGENTS Sucrose, Saccharin, glucose

49. Direct compression
Dry granulation
Wet granulation

50. Process Direct compression Dry granulation Wet granulation
Milling of drugs
and excipients
√ √ √
Mixing of milled
powders
√ √ √
Preparation of
binder solution
----- ----- √
Mixing of binder
solution milled
powders to form
wet mass
----- ----- √
Screening of wet
dough
----- ----- √

51. Process Direct
compression
Dry granulation Wet granulation
Drying of granules ----- ----- √
Compression of
slugs
----- √ -----
Screening of
granules
----- √ √
Mixing of
lubricant and
disintegrating
agent
√ √ √
Tablet
compression
√ √ √

52. Wet granulation is a widely employed
method for the production of compressed
tablets.
The steps required are:
1. Weighing and blending the ingredients
2. Preparing a dampened powder or a damp
mass
3. Screening the dampened powder or damp
mass into pellets or granules

53. 4. Drying the granulation
5. Sizing the granulation by dry
screening
6. Adding lubricant and blending
7. Forming tablets by compression.

54. 1. Reduced segregation of formulation
components during storage and/or
processing
2. Useful technique for the manufacture of
tablets containing low and or high
concentrations of therapeutic agent
3. Employs conventional excipients and
therefore is not dependent on the
inclusion of special grades of excipients

55. Tray drying
Concurrent drying
Vacuum drying
Fluid bed drying
Dielectric or microwave drying

56. 1. Often several processing steps are required
2. Solvents are required in the process: this leads
to a number of concerns:
• Drug degradation may occur in the presence of
the solvent.
• The drug may be soluble in the granulation
fluid
• Heat is required to remove the solvent

57. After weighing and mixing the ingredients, the
powder mixture is slugged, or compressed, into
large flat tablets or pellets about 1 inch in
diameter.
The slugs are broken up by hand or by a mill and
passed through a screen of desired mesh for sizing.
Lubricant is added in the usual manner, and
tablets are prepared by compression.
Aspirin, which is hydrolyzed on exposure to
moisture, may be prepared into tablets after
slugging.

58. By the dry granulation method, the powder
mixture is compacted in large pieces and
subsequently broken down or sized into
granules.
For this method, either the active ingredient or
the diluent must have cohesive properties
Dry granulation is especially applicable to
materials that cannot be prepared by wet
granulation because they degrade in moisture or
the elevated temperatures required for drying the
granules.

59. 1. These methods are not generally associated
with alterations in drug morphology during
processing.
2. No heat or solvents are required.
• Disadvantages 1. Specialist equipment is
required for granulation by roller compaction. 2.
Segregation of components may occur mixing. 3.
There may be issues regarding powder flow. 4.
The final tablets produced by dry granulation
tend to be softer than those produced by wet
granulation 5. Slugging and roller compaction

60. 1. Often several processing steps are required
2. Solvents are required in the process: this leads
to a number of concerns:
• Drug degradation may occur in the presence of
the solvent.
• The drug may be soluble in the granulation
fluid.
• Heat is required to remove the solvent.

61. 1. Often several processing steps are required
2. Solvents are required in the process: this leads
to a number of concerns:
• Drug degradation may occur in the presence of
the solvent.
• The drug may be soluble in the granulation
fluid.
• Heat is required to remove the solvent.

62. 1. Often several processing steps are required
2. Solvents are required in the process: this leads
to a number of concerns:
• Drug degradation may occur in the presence of
the solvent.
• The drug may be soluble in the granulation
fluid.
• Heat is required to remove the solvent.

63. PARAMETERS VARIABLES
Tablet Weight Limits on tablet weight are generally set as 3 to 5% of
a formulation specific target weight
Some issues that may cause weight variation are
powder flow problems, improper die fill, and
powder size distribution

64. PARAMETERS VARIABLES
Tablet Hardness Expresses as load required to crush a tablet
on end. Measured using a tablet hardness
tester.
Generally, the larger the tablet, the higher
the hardness. Smaller tablets (1/4" round)
usually have a hardness <5 kp. Larger
tablets usually have a hardness <20 kp
Some issues that may cause variations in
tablet hardness are inconsistent tablet
weight, particle size variations, poor
powder compressibility, insufficient binder
level

65. Tablet Thickness Uniform compression force and
volume of die fill, leads to uniform
thickness
Disintegration Time The time it takes for the tablet to break
up into individual granules or
particles.
Poor disintegration can come from
tablets which are compressed too
hard, insufficient disintegrant levels,
or too much binder.

66. Friability Friability is the tendency of a tablet to
crumble, chip or break.
It is measured by tablet weight loss
after rotation on a friabilator (i.e. 100
revolutions or 4 minutes at 25 RPM).
Typically % loss is <0.5%, but can be
up to 2% for very large tablets.
Friable tablets can be caused by low
moisture content, insufficient binder,
tablet configuration (e.g. sharp versus
beveled edges).

67. Chemically Acceptable and Stable - the
amount of active drug substance specified
on the label must be present in the tablet
at the time of manufacture and beyond the
expiration date.
Tablets must have acceptable drug content
uniformity.
Tablet must have acceptable drug release
characteristics (dissolution).

68. PARAMETERS DESCRIPTION
Identification Used to verify that
active drug substance in
the tablet is correct
Potency A measure of the amount of
active drug substance in the
tablet (i.e. mg/tablet or %
label claim)
Typically in the range of 90
or 95% to 105 or 110%

69. PARAMETERS DESCRIPTION
Related Substances Verifies the quantities
of other substances in
the product. Limits
should be set for other
known substances.
Unknown substances
should fall within ICH
guidelines.

70. PARAMETERS DESCRIPTION
Dissolution A measure of the rate and
extent of active drug
substance going into
solution.
Dissolution specifications
vary depending on the
type of tablet made.
Typically performed using
USP apparatus I (rotating
basket) or II (paddle), but
may also be done with
Apparatus III (Bio-dis) or
IV (Flow through cell)

71. PARAMETERS DESCRIPTION
Content Uniformity
A measure of the
consistency of tablet
potency, based on the
individual analysis of 10
tablets. Typically 85-115% of
label claim with a relative
standard deviation of <6%.

72. Dissolution Study
•USP Apparatus 1 (Basket
method)
•Apparatus 2 (Paddle method)
Tablet dissolution Apparatus are

73. of variable speed stirrer motor
cylindrical stainless steel basket on
stirrer shaft (Apparatus 1)
or a paddle as a stirring element
(Apparatus 2)
a 1000 ml glass vessel with cover

74. Apparatus
 Basket for capsules
 Paddle for tablets
Agitation
 Basket 100 rpm
 Paddle 50 and 75 rpm
Units to be tested
 6 to 12
Dissolution medium
 Usually 900 ml of aqueous media of various pH
Sampling
 Every 15 min for IR until 85 % is released
 1,2,4 hours and every hr thereafter for ER until 85% is
released.

75. In each test, a volume of the dissolution
medium as stated in monograph is placed in
the vessel and allowed to come to 370C +
0.50C.
The stirrer is rotated as the speed specified.

76. At the stated intervals of time samples of
the medium are withdrawn for analysis
of the proportion of drug dissolved.
The conventional tablets or capsule must
meet the stated monograph requirement
for rate of dissolution, “not less than 85%
of the labeled amount is dissolved in 30
minutes.”

77. Stage Number Tested Acceptance Criteria
S1 6 Each unit is not < Q+ 5%
S2 6 Average of 12 units (S1+S2) is >
D and no unit is < Q-15%
S3 12 Average of 24 units (S1+S2+S3)
is > Q and not more than 2 units
are < Q-15% and no unit is < Q-
25%

78. Time hr Amount of drug dissolved
1 Not more than 25%
4 Between 20% and 40%
8 Between 40% and 60%

79. It is the pressure required to fracture diametrically
placed tablets by applying the force.
Tablets require a certain amount strength or
hardness and resistance to friability to withstand
mechanical shock of handling in manufacturing,
packaging and shipping.
Hardness of individual of 10 tablets is determined
using Monsanto hardness tester.

80. Disintegration test apparatus contain
1000 ml beaker with basket rack
assembly.
Thermostatic arrangement for heating
fluid at 370C +20C is made in it.
Keep the dosage form in each rack and
start the apparatus.

81. Device raises and lowers the basket
containing dosage form for 29 to 32
cycles per minute
through the distance not less than
5.3 cm and not more than 5.7 cm. at
the end of time specified in the
monograph observe all the dosage
form disintegrated or not,
otherwise repeat the test

83. Place preweighed sample of 10 tablets in
the friabilator
tumble in a friabilator (model, Roche,
Bombay) for 4 min at 25 rpm
Dedust the tablets and record the loss in
weight caused by fracture or abrasion as
percentage friability
Compressed tablets should not lose more
than 1% of their weight

84. Percentage Friability = { ( W – Wo ) /
Wo } x 100
where,
Wo = initial weight of tablet
W = weight of tablet after friability
test

85. Select ten tablets randomly
from each batch
and measure the thickness
using screw gauge
Take the mean of three readings

86. Carry out weight variation test as per the
method described in the US
Pharmacopoeia-25 NF20, 2002.
Select twenty tablets randomly from each
batch.
Take weight of all twenty tablets. Calculate
the average weight of 20 tablets.

87. Calculate the Maximum % Deviation
Allowed.
Set the + limit of weight variation using the
average weight of the tablets.
eg. Say average weight of 20 tablets is 500
mg then ±5.0% deviation of 500 mg is +25
mg.
It means that the tablets should fall in the
weight limit of 475 mg to 525mg.

88. Then take weight of the same 20 tablets
individually.
The batch passes the test for weight
variation
if not more than two of the individual
tablet weight deviates from the average
weight by more than the percentage
shown in officials
and none deviate by more than twice

89. Average Weight
of Tablet (mg)
Maximum %
Deviation Allowed
130 mg or less ± 10.0 %
130 mg to 324 mg ± 7.5 %
More than 324 mg ± 5.0 %

90. Select at least 30 tablets randomly
Take 10 tablets out of 30 tablets and crush in
a glass mortar into fine powder.
Add the powdered tablet equivalent to dose
of drug in a 100ml of solvent mentioned in
official monograph of drug
and stir to dissolve the drug and finally
filter through sintered glass filter.

91. Dilute the filtrate suitably with the solvent
and analyze spectrophotometrically
against blank (solvent) for the
determination of drug content at particular
wavelength.
The tablet should be within + 15% of
labeled claim.

92. Single punch Machine
Rotary press

104. CAPPING
LAMINATION
CHIPPING
CRACKING
STIKING
BINDING
PICKING
MOLTTING
DOUBLE IMPRESSION