Lab. 2 Industrial Pharmacy: Effervescent Granules

Lab.
2
Industrial pharmacy
Effervescent Granules
Granule dosage form
Small irregular particles ranging from 4-10
mesh size containing medicinal substances
Effervescent granules
Mixtures of medicinal agent with

citric acid, tartaric acid and
bicarbonate
Note: Granules may be non-medical: Deluse

granules (diatery supplements)
Dispensing
Dissolving granules in water and take during taken
during effervescence or immediately after.
Type of drugs used in effervescent

granules:
Usually water soluble drugs

1- Alka seltzer: (Aspirin) minor aches, pains, inflammation,
fever, headache.
2- Citrocarbonate: Urinary pH modifiers and to treat
gastric antiacid.
Important notes for using granules:
1- By using granules or coarse particles of mixed powders

rather than small powder particles
the rate of solution is decreased
violent and uncontrollable effervescence is prevented.
2- Sudden and rapid effervescence could overflow the

glass and leave little residual carbonation in the
solution.
3- Combination of citric
acid and tartaric acids
rather than either acid
alone to avoid certain
difficulties.
A-Thus when using

tartaric acid alone the
resulting granules loss
their firmness readily
and crumble (Chalky
and friable).
B- while using citric acid
alone result in a sticky
mixture difficult to
granulate.
Advantages:
1. Rapid onset of action
(prepared as solution)
rapid disintegration and dissolution.
2. Pleasant taste
chemical reaction between acid and base
lead to librate CO2 which act as local
anesthetic effect of oral cavity so mask the
undesirable taste.
3. Psychological effect, patient comfort to it.
4. Provide alkaline solution, neutralization of a

acidic drugs as aspirin (alkalinization of urine
and increase excretion of drug which is acidic).
Disadvantages:
It can be 1. Unstable (absorb the water
overcome by [moisture] from the
atmosphere).
packaging and
compressing
into tablet
2. Not accurate dose estimation
dosage form
because the one who estimate
and put them the dose is the patient himself.
in aluminum
foil
3. Sodium overload (these
(not in plastic granules are not suitable for
foil because it hypertensive patients)
allow the
absorption of
water from 4. Have many drug-drug
moisture). interaction.
Sources of acids
1.Natural (food) acids (citric acid, tartaric acid, malic
acid ,fumaric acid).
Highly soluble in water and thus widely use in
preparation of effervescent.
2. Anhydride acids (anhydrous citric acid and

anhydrous tartaric acid) .
when dissolved in water give hydrous acids.
3. Salts acids (disodium dihydrogen phosphate

used instead of
,and sodium disulfide).
but the last is
more effective soluble at pH 4.5 otherwise they are strong acids.
because it´s 4. Effervescent base: used mainly in the
more soluble in preparation of effervescent granules.
Ciric acid 1 part
water.
Tartaric acid 2 part
3.44 part
Total 6.44
Method of effervescent granules production
Method of effervescent granules production
1. Formulation:
a/ Amount of each material in the formula.
b/ Number of doses: usually we 1 tsp. as ordinary
dose which is equal to 5 gm of effervescent.
No. of doses =total amount /wt .of each dose

c/ The physic-chemical properties of each
component.
2. Mixing:
to get uniform distribution.
3.• Moistening
and granulation: use certain solvent to get paste through
wet granulator.
** In
In small
small amount
amount we
we use
use sieve
sieve with
with suitable
suitable particle
particle
size
size instead
instead of
of granulator.
granulator.
Methods of moistening and granulation
A- Dry method (heat fusion method):

Used in preparation of drugs which are not affected by heat (e.g. Mg
Sulfate).
During the heating process 60-80°C ,the heat causes the release of 1
molecule of water of crystallization from the citric acid, which in turn
dissolves a portion of powder mixture to prepare the moist mass and
granulation, and thus consequent release of some carbon dioxide.
3+ 3O + 3 +
Citric acid
2+ 2O + 2 +
Tartaric acid
B- Wet fusion method:
Used to
1- prepare small amount of effervescent granules.
2- prepare compounds which are affected by

heat.
1stst mix the powder together and then add

ethanol as moisture to get wet mass.
Water can´t be used as moisture because it

reacts directly and end the reaction.
4. Drying:
only for heat fusion method
By using tray dryer
5. Packaging and storage (cool and dry

place):
Stored in a wide mouth bottle with
colored glass, tightly closed and
sealed to exclude air , and kept in a
cool dry place.
Note: to get accurate dose

granules may be pressured into tablet dosage
form (e.g. Vit. C).
Experimental work:
Prepare 25 gm of effervescent granules using 1.5 gm of
Mg sulfate per dose as laxative.
As known that effervescent granules composed of
effervescent base and active ingredient (Mg sulfate).
The steps of calculation:

Find no. of doses
No. of doses =total amount of granules /wt. of each dose
=25/5
=5
Find the amount of active ingredient added to the total
amount of effervescent granules (25gm ):
5 × 1.5=7.5 gm of Mg sulfate should be added
3. Find the wt. of each active constituent of effervescent
base that should be added to the added to the formula.
25 -7.5=17.5 gm amount of the base.
For Citric acid, for Tartaric acid
and for NaHCO3:
Total gm of citric acid
6.4 1
17.5 x
x =2.7 gm
total gm of tartaric acid
6.4 2
17.5 x
X =5.4 gm or 2 x 2.7 = 5.4 gm

Total gm of NaHCO3
6.4 3.4
17.5 x
x = 9.3 gm or 2.7 x 3.4=9.3

Procedure
Heat fusion method:

1. Mix tartaric acid, NaHCO3, Mg sulfate
together.
2. Heat citric acid in water bath at 60-80 c°
to release water crystallization till it
becomes warm.
3. Immediately and directly add the above
mixture to dish of citric acid with rapid
mixing by hand till get the wet paste.
4. Sieving.
5. Drying.
wet fusion method:
1. Mix all ingredients
including Tartaric
acid, Citric acid,
NaHCO3, and the
active ingredient Mg
sulfate.
2. Add Alcohol (95%)
drop by drop with the
continuous mixing till
we get a wet paste.
3. Sieving.
4. Drying.

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Lab.

Mixtures of medicinal agent with

Note: Granules may be non-medical: Deluse

Type of drugs used in effervescent

Usually water soluble drugs

1- By using granules or coarse particles of mixed powders

the rate of solution is decreased

violent and uncontrollable effervescence is prevented.

2- Sudden and rapid effervescence could overflow the

A-Thus when using

3. Psychological effect, patient comfort to it.

4. Provide alkaline solution, neutralization of a

2. Anhydride acids (anhydrous citric acid and

3. Salts acids (disodium dihydrogen phosphate

No. of doses =total amount /wt .of each dose

Methods of moistening and granulation

A- Dry method (heat fusion method):

2- prepare compounds which are affected by

1stst mix the powder together and then add

Water can´t be used as moisture because it

5. Packaging and storage (cool and dry

Note: to get accurate dose

The steps of calculation:

X =5.4 gm or 2 x 2.7 = 5.4 gm

x = 9.3 gm or 2.7 x 3.4=9.3

Heat fusion method:

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