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____________________________________________Research Article
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(a)Drug characterization
Solubility analysis 4
The solubility studies were performed in phosphate
buffer solution, as the procedure described in USP.
Excess amount of drug was added to the phosphate
buffer pH 7.2 in each case and keeping it on a
water bath shaker for 24hrs at 32C. After 24hrs,
solutions were analyzed spectrophotometrically at
221nm, which was the absorption maxima
determined earlier.
Partition coefficient 5
50mg of ibuprofen is placed in a separating funnel.
50ml of purified water and 50ml of octanol were
added. The two phases were shaken
for 15min with intermittent release of pressure that
builds up within the separating funnel. The mixture
is set aside to allow the two phases to separate. The
concentration of drug in aqueous and organic phase
is determined by spectrophotometrically. The
absorbance of solution is measured at 221nm.
Partition coefficient = Conc of drug in organic
phase/ Conc of drug in aqueous phase
(b) Compatibility studies
In order to find out the possible interactions
between ibuprofen and the polymer, Fourier
transform infra red spectroscopy (FTIR) were
carried out on the pure substance, their physical
mixtures.10 mg of sample and 40 mg of KBr were
taken in a mortar and pestle and triturated. A small
amount of triturated sample was taken into a pellet
maker and was compressed at 10 kg/cm2 using a
hydraulic press. The pellet was kept on the sample
holder and scanned from 4000cm-1 to 400 cm-1 in
Spectrometer Model 2500. Samples were prepared
for pure polymer, pure drug and for physical
mixture of drug and polymer. The spectra obtained
through those samples were compared and
interpreted for shifting of major functional peaks
and disappearance of functional peaks.
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Chitosan
(%W/V)
F1
F2
F3
F4
F5
F6
F7
F8
F9
F10
F11
F12
F13
F14
F15
F16
F17
F18
F19
F20
F21
F22
F23
F24
F25
F26
F27
F28
F29
F30
F31
F32
F33
F34
F35
F36
1.5
1.5
1.5
1.5
2.0
2.0
2.0
2.0
2.5
2.5
2.5
2.5
-
Chitosan/
HPMC
(%W/V)
50:50
50:50
50:50
50:50
25:75
25:75
25:75
25:75
75:25
75:25
75:25
75:25
-
HPMC
(%W/V)
Glycerol
(%w/w)
1.5
1.5
1.5
1.5
2.0
2.0
2.0
2.0
2.5
2.5
2.5
2.5
10
20
30
10
20
30
10
20
30
10
20
30
10
20
30
10
20
30
10
20
30
10
20
30
10
20
30
Polymeric
solution
Polymer/s
Plasticizer
(glycerol)%
Drug
(mg)
D1
0.2
Plain Chitosan
20
40
D2
0.2
Plain Chitosan
30
40
D3
0.2
Plain Chitosan+HPMC
20
40
D4
0.2
Plain Chitosan+HPMC
30
40
D5
0.25
Plain HPMC
20
40
D6
0.25
PLAIN HPMC
30
40
EVALUATION TESTS
A. Physical Characterization
Physical appearance
All the transdermal films were visually inspected
for color, clarity, flexibility and smoothness.
Tensile strength 7
The films were evaluated using a texture analyzer
equipped with a 500 gm load cell. Film strip in 10
mm x 10 mm of dimension and free from air
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Swelling Index
Weighed pieces 1x1 cm2 of film were immersed in
distilled water; at 5, 10, 30, 60min. Soaked films
were removed from the medium at predetermined
time, blotted to remove excess liquid and weighed
immediately. The swelling index was calculated
from the weight increase, as follows.
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Concentration
(g/ml)
5
10
15
20
25
Absorbance
0.3124
0.5331
0.8074
1.0731
1.3306
A b so rb a n c e
10
15
20
25
30
concentration(g/ml)
Absorbance
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Appearance
Absence of film
Brittle
Thin, Brittle
Thin, Brittle
Absence of film
Thin, Sticky
Smooth, Flexible
Smooth, Flexible
Absence of film
Uneven, Thin, Sticky
Thin, Sticky
Thin, Sticky
Absence Of Film
Brittle, Rough
Rough
Rough, Brittle
Absence Of Film
Brittle, Thick
Rough, Thick
Thick, Sticky
Absence Of Film
Brittle, Thin
Smooth, Flexible
Smooth, Flexible
Absence Of Film
Brittle
Brittle
Brittle, Thick
Absence Of Film
Brittle
Thick, Rough
Thick, Rough
Absence Of Film
thick, brittle
Flexible, Smooth
Smooth, Flexible
Appearance
Avg.Thic-kness
(mm)
Smooth,
Flexible
Smooth,
Flexible
Smooth,
Flexible
Smooth,
Flexible
Smooth,
Flexible
Smooth,
Flexible
0.252
0.024
0.274
0.038
0.192
0.016
0.210
0.122
0.152
0.115
0.172
0.057
Tensile
Strength
(kg/cm2)
Folding
Edurance
Drug
Content
4.00.057
120
2.6
4.20.208
125
2.59
4.80.115
130
2.61
5.00.208
133
2.58
3.20.038
80
2.62
3.80.101
85
2.63
Weight
Uniformity
(gm)
0.468
0.03
0.47
0.06
0.45
0.03
0.45
0.02
0.441
0.019
0.429
0.021
Flatness
(%)
98
98.5
97.4
98
95.5
96
Moisture
Content
(%)
Moisture
Uptake
(%)
Water Vapor
Transmission Rate
(gm/cm. day)
D1
D2
D3
D4
D5
D6
5.9
6.8
16.2
17.7
12.7
13.6
13.5
14.8
19.5
20.2
15.5
16.3
8.57*10-3
16.03*10-3
18.5*10-3
20.1*10-3
12.7*10-3
14.0*10-3
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%Swelling Index
5min
73.5
75.9
66.5
67.1
60.5
62.2
10min
75.9
77.0
67.7
68.5
63.6
64.5
30min
77.1
78.7
70.4
72.5
64.2
66.2
60min
78.7
80.0
72.5
78.5
65.8
67.7
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% C u m u la tiv e re le a s e
100
90
80
70
60
50
40
30
20
10
0
0
10
15
20
25
30
Time(hrs)
D1
D2
D3
D4
D5
D6
% Cumulative
release
D4
86
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Higuchis
equation
R2
0.9398
Korsmeyers-peppas
equation
R2
n
0.9698
0.5072
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Higuchi plot
% C um ulative released
8
7
6
5
4
3
Actual
2
Matrix
1
0
0
200
400
600
800
1000
1200
1400
1600
peppas Plot
9
8
7
6
5
4
3
Actual
Peppas
1
0
0
200
400
600
800
1000
1200
1400
1600
log Time
Erythema
formation
Control
Test
0
0
0
0
0
0
0
0
0
0
0
0
0
0
CONCLUSION
Transdermal Drug Delivery Systems are ideally
suited for drugs that undergo hepatic first pass
metabolism along with a short elimination half life
of less than 4 hours. Ibuprofen Transdermal
patches were prepared by using plain Chitosan,
plain HPMC and Chitosan/HPMC. Among all the
patches D4 showed optimum sustained release
characteristics following Non-Fickian type of
diffusion.
Hence
it can
conclude the
Chitosan/HPMC (75:25) with 30% plasticizer may
be suitable for development of Transdermal Drug
Delivery System of Ibuprofen.
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Edema formation
Control
0
0
0
0
0
0
0
Test
0
0
0
0
0
0
0
ACKNOWLEDGEMENTS
The authors gratefully acknowledge the kind help
received from Aescul Pharma, Ongole, Andhra
Pradesh, for gift samples of ibuprofen and various
polymers like chitosan and HPMCE5LV. We also
acknowledge the cooperation provided by PRIST
UNIVERSITY for FTIR studies
REFERENCES
1. Finar I L.Organic Chemistry: The
fundamental principles, elbs, and 6th
edition, 1973: pp.759-61.
361
2.
3.
4.
5.
6.
7.
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