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Granules

(Dr.) Mirza Salman Baig


Assistant Professor (Pharmaceutics)
AIKTC, School of Pharmacy,New Panvel
Affiliated to University of Mumbai (INDIA)

Granules

"Granules are prepared agglomerates


of smaller particles of powders"

Why Granules?
To avoid powder segregation.
To enhance the flow of powder.
To produce uniform mixtures.
To produce dust free formulations.
To eliminate poor content uniformity.
To improve compaction
characteristics of mix.

Granules
Advantages
Granules are more flowable

compared to powder.
Segregation of the
constituents of the powder
mixture could be avoided by
granulation.
Granules are more stable
against humidity and
atmosphere.
Granules are more easily
wetted by liquids than light
and fluffy powders.

Disadvantages

.The masking of bitter

tastes may be a problem


with this type of
preparation.
Granules are not a good
method of administering
potent drug with low dose.
Instability in presence of
moisture.
Problems in packaging
and storage.

To avoid powder segregation.

To enhance the flow of


powders
To produce uniform mixtures.
(Mixtures of various particles tend to
segregate in transport or handling
because of differences in particle size,
shape and density)

TYPES

1:Effervescent granules
Effervescent granules are uncoated
granules generally containing acid
substances and carbonates or
hydrogen carbonates which react
rapidly in the presence of water to
release carbon dioxide.
They are intended to be dissolved or
dispersed in water before
administration.

Formula
Sodium bicarbonate
Citric acid
Tartaric acid

Contd...
Effervescent salts are granules or coarse
to very coarse powder containing a
medicinal agent in a dry mixture usually
composed of sodium bicarbonate, citric
acid and tartaric acid .
When added to water the acid and base
react to liberate carbon dioxide
resulting in effervescence.
The resulting carbonated solution mask
the undesirable taste of medicinal agent.

Effervescent granules

2:Coated granules
Coated granules are usually multidose preparations consist of granules
coated with one or more layers of
mixtures of various excipients.
The substances used as coatings are
usually applied as solution or
suspension in conditions in which
evaporation of the vehicle occur.

Coated granules

3:Gastroresistant granules
These are delayed release granules
that are intended to resist the gastric
fluid and to release the active
substance in intestinal fluid
These properties are achieved by
covering the granules with the
gastro-resistant material or by other
suitable means.

Gastro-resistant granules

4:Modified release granules


They are coated or uncoated granules
which contain special excipients or which
are prepared by special procedure are
both , designed to modified the rate , the
place or the time at which the active
substance or substances are released.
Modified release granules include
prolonged release granules and delayed
release granules.

Modified release granules

Methods of Granulation
Dry Granulation
WET GRANULATION

When To Choose DRY method?


Drug dose is too high.
Do not compress well after wet
granulation.
Heat sensitive drugs.
Moisture sensitive drugs.
e.g. Aspirin , Vitamins

Dry granulation
Dry granulation is performed by
two ways.
a) Roll compactor
b) Slugging

a) Roll compactor
Dry powder is passed through a roll
compactor and then through a granulating
machine.
A roll compactor, also called a roll press
or roller compactor, processes a fine
powder into dense sheets or forms by
forcing it through two mechanically
rotating metal rolls running counter to
each other .
The surface of the compacting rolls may
be smooth or may have pocket
indentations or corrugations that allow
compaction of different forms and textures

b)Slugging:
Slugging, is the compression of a

powder or powder mixture into large


tablets or slugs on a compressing
machine under 8,000 to 12,000 lb of
pressure, depending on the physical
characteristics of the powder.
The slugs are generally flat-faced
and are about 2.5 cm (1 inch) in
diameter.

b)Slugging:
The slugs are granulated into the
desired particle size, generally for
use in the production of tablets.
The dry process often results in the
production of fines, that is, powder
that has not agglomerated into
granules.
These fines are separated, collected,
and reprocessed.

Wet granulation
In this, powdered medicament and
other excipients are moistened with
granulating agent.

Contd...

This is the most used method to


prepare granules.

The main disadvantage of this


method is the higher number of steps
present in this process when
compared with the other two
methods.

Steps of Wet Granulation:

1. The 1st step is the wetting of the powder


with a liquid or solution to form a paste.

Characteristics of the granulating liquid:


It should have all required characteristics of
pharmaceutical excipient, &
It should dissolve the powder only within a
certain limit (mild solvent):

From another side, if the solvent cannot


absolutely dissolve the powder, we
cannot obtain the liquid forces, which
stick together the powder particles.

The fraction of powder, which dissolves in


the solvent, & then re-crystallizes, after
the drying, will form bridges between the
particles of the powder.

When two particles become in contact


between each other by certain forces,
they institute:
forces of electrostatic nature (week
forces) &
forces of viscous or/and adhesive natures
(which are the most important) so the
particles remain attached to each others.
Thus the used liquid in the wet
granulation must be mild solvent for the
powder.

Other methods

Rapid Mixer Granulator

FBG
Fluidization is the operation by
which fine solids are transformed into
a fluid like state through contact with
a gas.
Granulating and drying can be
completed in one step inside the
machine.

Other granulation techniques


Steam Granulation
Melt Granulation
Moisture Activated Dry Granulation (MADG)
Moist Granulation Technique (MGT)
Thermal Adhesion Granulation Process (TAGP)
Foam Granulation
Pneumatic Dry Granulation (PDG)

contd...
Freeze granulation Technology
Steam Granulation
Melt Extrusion Technology
Liquisolid Technique
TOPO Technology
Continuous Flow Technology

Granulation Characterization

Powders

Granules

Comparatively poor flow properties

Flow well compared to tablets, good


choice for compressing tabs

Relatively less stable (physically and


Chemically) due to inc. S.A & Atm.
Effect

Has less surface area, more stable to


atm. effect

More likely to hardening / cake


formation on long storage

Less likely

For some powders, drugs float on the


surface, difficult to make solution

More easily wetted by the solvents,


good choice reconstitution liquids

Relatively poor compressibility

Good compressibility

Chances of non uniform dosing are


more

Relatively more uniformity of


contents in case of granules

More dust due to small particle size

Generate less dust on handling

Comparatively less appealing

Have a more elegant appearance

Relatively simple method of


processing/formulation

It involves more processing,


exposure to heat and contact with
solvents

Effervescent Granules
Definition: Mixture of organic acid and alkali
effervesces when subjected to water due to
reaction between the acid and the base with
evolution of co2
Examples: Citric or tartaric acids with
sodium carbonate or bicarbonate
Uses: The liberated carbon dioxide has
the following advantages:
It masks the bitter and nauseous taste.
It promotes gastric secretions.
It acts as a carminative.
psychological impression at the patient..

Effervescent Granules
Formulation:
- Bulk powders or divided powders
- Packed in separate packages of
contrasting colors.
- The contents are mixed in a quantity of
water at the time of dosing.
- The liquid is consumed just after the
reaction begin to subside.

Effervescent Granules
Definition: Sweetened effervescent
powders formulated as granules.
Granulation:
1- Wet method: By the addition of a
binding liquid (Alcohol is frequently used).
2- Dry method: Heating effloresced powder
to liberate the water of crystallization
which then acts as the binding agent

Effervescent Granules
Wet Granulation
Procedure:
1- The powders are mixed without pressure in a
suitable container.
2- Alcohol is added in portions with stirring until a
dough like mass is formed.
3- The materials are then passed through sieve # 6.
4- The resulted granules are dried at a temperature
not exceeding 50C.
5- The granules are packed in air tight containers