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CHARACTERIZATION OF COPROCESSED EXCIPIENTS
FOR DISINTEGERANTS

Morphological Properties
Method
Co-processed
excipients
Aspect
ratio
Roundness Irregulariy ECD
Native
Pharmaburst

0.311 0.575 3.46 40.40
Pregelatinized
Starch
0.323 0.600 3.46 41.46
Crospovidone

0.399 0.598 4.26 22.56
Xanthan gum

0.296 0.541 4.48 57.91
Solvent
evaporatio
n method
Xanthan Gum:
pharmaburst
0.307 0.426 3.60 86.40
Xanthan Gum:
pregelatinized
starch
0.298 0.540 3.41 80.94
Xanthan gum :
Crospovidone
0.393 0.613 4.22 28.37
Ogunjimia
nd
Alebiowu's
methods

Xanthan gum :
pharmaburst
0.263 0.524 3.37 60.361
Xanthan gum :
pregelatinized
starch
0.287 0.629 3.25 94.230
Xanthan gum :
Crospovidone
0.389 0.625 4.23 17.74

Tableno.no presents the morphological characteristics, of the native and co-
processed excipients respectively.

Aspect ratio varies between 0 and 1, with a low value indicative of an
elongated particle and a perfect circle having an aspect ratio of 1.

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Roundness is a measure of how closely the projected area of the powder
resembles a circle; a perfect circle has a roundness value of 1.
Irregularity measures the surface area compared to the size of the
particle.

Equivalent circle diameter (ECD) is a measure of size, it is the diameter
of a sphere with the same cross-sectional area as the powder. The
higher the equivalent circle diameter, the larger is the mean particle size.

The results in the table no. showed that the aspect ratio, roundness,
irregularity and ECD were influenced by the co-processing of excipients in both
methods.
The aspect ratio of the co-processed excipients were lower than native
excipients but was higher than that of Xanthan gum. This implied that
inclusion of Xanthan gum and native excipient in the co-processed excipients
produced elongated excipients when compared to native excipients. but less
elongated when compared with native xanthan gum, In both methods.

In roundness measurement it was found that in solvent evaporation
method Co-processed Xantha Gum : pharmaburst and Xanthan Gum :
pregelatinized starch had roundness 0.426 and 0.540 respectively when it was
compared with their native Pharmaburst and Pregelatinized Starch having
roundness 0.575 and 0.600 respectively it indicates above co-processed
excipints were less circular than their native excipients, but in same method
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co-processed Xanthan gum : Crospovidone had roundness 0.613 and its
native Crospovidone had roundness 0.598 it implied co-processed Xanthan
gum : Crospovidone was more circular than the native Crospovidone. And same
results found in Ogunjimi and Alebiowu's method Xantha Gum : Pharmaburst
and Xanthan gum : pregelatinized starch were less circular than their native
excipients but Xanthan gum : Crospovidone was more circular than the native
Crospovidone it showed that more circular shape expose more surface area to
wet hence it will help to increase the disintegration property.
In the measurement of irregularity it was found that irregularity of the
xanthan gum is 4.48 which was more than each Co-processed excipients,
result implied that the co-processing produced less irregularly shaped particles
compared with xanthan gum and their respective native excipients. But in
Xanthan Gum : Pharmaburst by Solvent evaporation method was found to be
3.60 which was more than its native Pharmaburst had irregularity of 3.46 it
showed co-processed excipient was more irregular than its native excipient
hence it might have less flow property than the native excipient or it may create
space for air entrapment in tablet while compression which may lead to
lamination defect in tablet.
The ECD of the co-processed excipients were found to be large than
native excipients. Except in Xanthan gum : Crospovidone by Ogunjimi and
Alebiowu's methods the co-processed excipient was having ECD 17.74 and its
native Crospovidone had ECD 22.56 its indicated that co-processed excipient
had small surface area than the native excipient. Rest all the co-processed
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excipients had large ECD implied as a filler so they can minimize need of
bulking excipient in the tablets.
Evaluation of physical characteristics

Method
Co-processed
Excipient
Bulk
density
(gm/cm
3
)
Tapped
density
(gm/cm
3
)
Hausners
ratio
Carrs index
Native
Pharmaburst

0.4610.04 0.6280.02 1.350.2 25.780.03
Pregelatinized
Starch
0.7230.23 2.080.06
1.770.05

65.200.01
Crospovidone

0.2460.05 0.460.10
1.870.03

46.370.05
Xanthan gum

0.8350.03 1.250.13
1.500.09

33.360.06
Solvent
evaporat
ion
method
Xanthan
gum:pharmabur
st
0.3220.03 0.380.15
1.190.45

15.970.8
Xanthan
gum:pregelatiniz
ed starch
0.40.31 0.4890.09
1.190.65

15.890.11
Xanthan
gum:Crospovido
ne
0.2650.25 0.460.06
1.730.76

42.190.9
Ogunjim
i and
Alebiow
u's
methods

Xanthan
gum:pharmabur
st
0.3110.04 0.50.1
1.580.08

37.40.06
Xanthan
gum:pregelatiniz
ed starch
0.5660.14 0.6760.09
1.180.2

15.150.05
Xanthan gum :
Crospovidone
0.2550.23 0.3730.04 1.330.25 24.920.03
Mean sd

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The values for bulk density and tapped density were found to be in the
range of 0.2460.05 to 0.8350.03gm/cm
3
and 0.3730.04 to 2.080.06
gm/cm
3
indicating good packing capacity. These values may further influence
properties such as compressibility and Tablet.
Hausners ratio result was found in the range 1.180.2 to 1.870.03
implied medium flow property of the co-processed Excipients. Range of
hausners ratio of co-processed excipients was found to be slightly less than
their respective native excipients it showed increase in tablet compression flow
property.
Carrss Index in Solvent evaporation method of co-processed Xanthan
gum: Pharmaburst and Xanthan gum : pregelatinized starch were found to be
15.970.8 and 15.890.11 respectivly which indicates good flowability but the
compressibility of the Xanthan gum : Crospovidone was 42.190.9 which
showed very very poor flowability. In Ogunjimi and Alebiowu's method The
carrs index of Xanthan gum : pregelatinized starch was 15.150.05 which
showed good flow property Xanthan gum : pharmaburst showed carrs index
37.40.06 which indicated poor flow and Xanthan gum : Crospovidone has
carrs index 24.920.03 which also indicates poor flow and when all the co-
processed excipients were compared with native excipients each co-processed
excipient showed increased flowability.
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Evaluation of physical characteristics

Method
Co-processed
excipient
Angle of
repose in
degree
EMS % LOD %
Native
Pharmaburst

18.610.04 00 3.7
Pregelatinized
Starch
30.260.06 1.8 9.6
Crospovidone

26.150.3 16.8 8.95
Xanthan gum

24.080.09 33.3 11.2
Solvent
evaporation
method
Xanthan gum :
Pharmaburst
30.680.2 0.6 4
Xanthan gum :
pregelatinized
starch
16.190.08 1.9 11.6
Xanthan gum :
Crospovidone
48.900.6 17.1 15.5
Ogunjimi
and
Alebiowu's
methods

Xanthan gum :
Pharmaburst
26.040.09 10 5.5
Xanthan gum :
pregelatinized
starch
15.680.12 3.26 9.5
Xanthan gum :
Crospovidone
23.580.21 21.6 17.5

Angle of repose of co-processed Xanthan gum : pregelatinized starch by
both methods was found >20
0
it showed Excellent flow property and it was also
good when compared with their respective native excipients. In Solvent
evaporation method Xanthan gum : Pharmaburst, had angle of repose 30.68
0
it
showed acceptable flow property. And Xanthan gum: Crospovidone was have
angle of repose 48.90
0
indicated low flowability and it was also low flowable
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than the native excipient. The co-processed Xanthan gum : Pharmaburst
and Xanthan gum : Crospovidone by Ogunjimi and Alebiowu's methods were in
the range 20
0
-30
0
it showed good flow property .
Equillibrium moisture sorption the amount of water adsorbed dependent
on the affinity between the surface and water molecules, temperature and the
relative humidity as well as the surface area exposed. The difference in the
moisture sorption characteristics between the polymers could be due to the
differences in the polar groups available for inter-molecular interaction with
water molecules. The moisture absorption of Xanthan Gum is 33.3%. And
moisture absorption of co-processed excipient is more than their respective
native excipients it might be due to affinity of Xanthan Gum towards moisture
used in co-processing of excipients surface area increases with use of Xanthan
gum hence increase moisture was noticed it can be said that excess moisture
will help to bind the tablet hence it may reduces need of binder and the tablet
will be mechanically strong.

Loss on drying of co-processed excipients were more than the native
excipients it showed more content of water in co-processed excipient more
moisture will help to bind the particals within the tablets.



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Evaluation of Amlodipine Besylate Tablet

Method BATCH
Hardness
Kg/cm
2

Thickness
(mm)^
Friabiliy
(%)#
Drug
Content
(%)*
Weight
variation
(mg)*

Disint
egratio
n
In sec
STD F1. Std

3.430.03


2.270.09

0.651.0
6
991.95
1501.57

451.1
3
Solvent
Evaporati
on Method
F2.Xanthan
gum:pharmaburt

3.410.04

2.190.07

0.971.3
2
991.12
1500.06
5
470.5
6
F3.Xanthan
gum:pregelatinize
d starch

3.720.3

2.250.06
0.441.4
2
951.16 1501.18
570.9
8
F4. Xanthan
gum:Crospovidon

3.370.2

2.080.31

0.631.5
4
981.11
1500.02
3
410.2
1
Ogunjimi
and
Alebiowu's
methods

F5. Xanthan
gum:pharmaburt

3.240.09

2.26.005

1.081.3 1021.13
1500.07
8
460.8
5
F6. Xanthan
gum:pregelatinizd
starch

3.500.3

2.260.06

0.631.8 1001.19
1500.06
5
630.3
1
F7. Xanthan
gum:Crospovidon

3.450.2

2.20.04

0.781.8 991.18 1501.15
430.1
2

The hardness of tablets of each batch ranged 3.410.04 to 3.720.3
kg/cm2 (Table), which ensures good handling characteristics of all batches.
Thickness was shown in the range of 2.20.04 mm to 2.270.09 mm

Friability and disintegration parameters evaluated and studied
simultaneously it was found that. The disintegration time of std is 451.13 sec
and friability 0.651.06%. The disintegration time for tablet formulated by In
Solvent Evaporation Method co-processed Xanthan gum : Crospovidone co-
processed by was 410.21 sec which was less than that of standerd and
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friability was 0.631.54% which was good in comparision with standerd it
showed fast disintegration of tablet and have good mechanical strength as
compared with the standard .And disintegration time of tablets formulated by
using disintegrant co-processed by Ogunjimi and Alebiowu's method Xanthan
gum : Crospovidone was found 43 sec which is less than that of standard and
friability was 0.78% which showed good disintegration but more friable than
the standard. In evaluation of tablet formulated by co-processed Xanthan
gum : Pharmaburst by both methods disintegration time less than the
standard but tablets was more friable than the standard. And in Xanthan gum
: pregelatinized starch by both methods tablets disintegrates slow than the
standerd.
Drug content and weight variation was found in limit
Calibration curve for Amlodipine
The calibration curve was developed using a concentration range of 2,4,6,8,
and 10g/ml. The calibration curve obtained was linear.

y = 0.0103x
R = 0.997
0
0.02
0.04
0.06
0.08
0.1
0.12
0 2 4 6 8 10 12
Series1
Linear (Series1)
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Sr. No. Concentration (g/ml) Absorbance
0 0 0
1 2 0.0193
2 4 0.0398
3 6 0.0582
4 8 0.0850
5 10 0.1030



Dissolution studies

ti
m
e
STD Solvent Evaporation Method Ogunjimi and Alebiowu's methods

F1
F2.Xanthan
gum
:pharmabur
st
F3.
Xanthan
gum :
pregelatiniz
ed starch
F4
.Xanthan
gum :
Crospovido
n
F4.Xanthan
gum
:pharmaburs
t
F5.
Xanthan
gum :
pregelatiniz
ed starch
F6.
Xanthan
gum :
Crospovido
n
0 0 0


0 0 0 0 0
10 630.1
1
650.01 760.17 620.09 640.09 700.16 650.02
20 680.1
3
710.08 830.12 660.13 671.23 720.19 700.12
30 730.1
6
760.07 870.13 720.17 711.14 750.11 750.14
40 800.1
4
820.09 900.15 850.08 850.18 860.17 880.11
45 850.1
5
940.06 950.12 900.07 900.07 920.16 920.08
55 880.1
2
960.16 970.3 950.2 981.1 990.09 970.09
70 990.1
2
1010.1 1010.2 960.12 1000.1 1000.12 990.1
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