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Received: 05-02-2014
Accepted: 09-04-2014
Vol.3No.3.2014
OnlineAvailableatwww.thepharmajournal.com
The Oxford College of Pharmacy, 6/9 Ist cross Begur Road, Hongasandra, Bangalore 560068, India
[Email: sayanibh@hotmail.com, Tel: 447404237669]
The Oxford College of Pharmacy, 6/9 Ist cross Begur Road, Hongasandra, Bangalore 560068, India.
[Email: swethareddy555@gmail.com, Tel: 918030219831]
The present work is based on the formulation of effervescent granules of Fexofenadine hydrochloride unit dose.
Eight such formulations were prepared using different acids, salts, diluents and superdisintegrants by the wet
granulation method. The prepared granules were evaluated for flow property (like angle of repose, bulk density,
tapped density and Hausners ratio), particle size, moisture content, Effervescence time, in vitro dissolution studies
and stability studies. The formulated effervescent granules exhibited excellent flow properties and bulk density
suitable for a unit dose. The low moisture content of the formulations supported the stability of the formulations. All
the formulations exhibited effervescence time less than 20 sec and dissolution profile was found to be more than
95% in 5 mins. The stability studies revealed that the product was stable at variable temp and humidity conditions.
Keyword:
1. Introduction
Effervescent granules are popular delivery
systems for many pharmaceutical products such
as antacids, analgesics, and cough/cold
formulations. They are fast dissolving, highly
soluble, stable, convenient dosage forms. The
granules are added into a glass of water just
before administration and the drug solution or
dispersion is to be drunk immediately. The
granules are quickly dispersed by internal
liberation of Carbon dioxide in water due to
interaction between acid with alkali metal
carbonates or bicarbonates in the presence of
water. Due to liberation in Carbon dioxide gas,
the dissolution of the API in water as well as taste
masking effect is enhanced [1, 2]. The advantages
of effervescent granules compared with other oral
dosage forms includes an opportunity for the
formulator to improve taste, a more gentle action
on the patients stomach and marketing aspects.
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F1
120
24
18
44
1
5
3. Evaluation of granules
3.1 Particle size distribution
The size and size distribution of the granules
produced was determined by agitation for 10 min
with a sieve shaker fitted [8] with a progression of
standard sieves. From the weight retained on each
sieve, a particle size distribution graph was
plotted from which the median diameter was
determined.
F2
120
40
11
40
1
5
Formulation Code
F3
F4
F5
F6
120 120 120 120
45
46
51
45
39
43
45
45
1.5
1.5
1.5
1.5
1
1
1
1
5
5
5
5
F7
120
51
39
1.5
1
5
F8
120
45
45
1.5
1
5
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bulk= M / Vo..(1)
Where, bulk = Apparent bulk density, M =
Weight of the sample, Vo = Apparent volume of
powder.
3.3 Tapped density
A suitable amount of granules was placed in a
100 ml measuring cylinder. After absorbing its
initial volume, the sample was tapped 500 times
initially followed by an additional taps of 750
times until the difference between succeeding
measurement is less than 2% and then tapped
volume, was measured, to the nearest graduated
unit. Tapped density was calculated using
equation [9].
tab = M / Vf ....(2)
Where, tab = Tapped Density, M = Weight of
the sample, Vf = Tapped volume of powder
3.4 Hausners ratio
Hausners ratio is the ratio of tapped to bulk
density and was calculated by using the following
equation.
Hausners Ratio = tab/bulk(3)
Lower Hausners ratio (<1.25) indicates better
flow properties than higher ones, between 1.25 to
1.6 showing moderate flow properties, cohesive
powder and more than 1.5 poor flow [9].
3.5 Angle of repose
The angle of repose was determined by allowing
granules to flow through a funnel and fall freely
onto a graph paper on a horizontal surface. The
height and diameter of the resulting cone were
measured and the angle of repose is calculated
from this equation:
tan = h / r.(4)
Where, h is the height of the powder cone and r is
the radius of the powder cone.
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Formula
F1
F2
F3
F4
F5
F6
F7
F8
Angle of
repose SD
27.3 0.41
29.1 0.34
30.73 0.23
31.4 0.30
27.3 0.32
33.69 0.19
26.67 0.59
30.46 0.50
% Moisture
content SD
% Drug
Content SD
Effervescence
time(sec) SD
0.01 0.01
99.8 0.01
8 0.57
0.02 0.01
99.8 0.01
10 0.57
0.02 0.01
99.12 0.03
11 0. 1
0.04 0.02
96.81 0.01
15 0.57
0.02 0.01
99.44 0.01
9 0.57
0.02 0.01
97.2 0.04
12 0.1
0.03 0.01
98.1 0.01
13 0.57
0.06 0.01
97.8 0.01
18 0.57
SD=Standard deviation and no of replicates (n) =3.
% Drug
release at 5
mins SD
99.71.3
99.41.1
98.60.6
97.370.1
99.80.6
97.80.7
98.11.3
96.70.7
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and disintegration time as parameter yielded a Pvalue 1.34E-10, so it can be concluded all the
SS
df
MS
588.892
294.446
81.0069
76.33135
665.2234
21
23
3.634826
Pvalue
1.34E10
F crit
3.4668
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Fig 4: Drug content analysis after stability study for all formulations
6. Conclusion
The Granules were prepared by the wet
granulation technique that contains Citric acid,
Fumaric acid, Tartaric acid as acid components,
Sodium carbonate, Sodium bicarbonate, Calcium
carbonate, Potassium carbonate, Potassium
bicarbonate as salts, Spray dried lactose and
Mannitol
as
diluents,
Crospovidone,
Croscaramellose as Super disintegrants, Hydroxy
propyl methyl cellulose as a binder and alcohol as
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