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Research Article
Formulation and evaluation of topical gel of diclofenac sodium using different polymers
A Gupta1*, AK Mishra2, AK Singh1, V Gupta2, P Bansal 3
1
Babu Banarasi Das National Institute of Technology and Management, Lucknow, India
National Institute of Ayurvedic Pharmaceutical Research, CCRAS, Patiala, India
3
Baba Farid University of Health Sciences, Faridkot, India
2
Keywords: Topical drug delivery, Diclofenac sodium, HPMC, Carbapol 934P, Sodium alginate
INTRODUCTION
For topical treatment of dermatological disease as well as
skin care, a wide variety of vehicles ranging from solids to semisolids
and liquid preparations is available to clinicians and patients. Within
the major group of semisolid preparations, the use of transparent gels
has expanded both in cosmetics and in pharmaceutical preparations
[1]. A gel is colloid that is typically 99% wt liquid, which is immobilized
by surface tension between it and a macromolecular network of fibers
built from a small amount of a gelating substance present [2]. Topical
drug administration is a localized drug delivery system anywhere in
the body through ophthalmic, rectal, vaginal and skin as topical routes.
Skin is one of the most readily accessible organs of human body for
topical administration and main route of topical drug delivery system.
Numbers of medicated products are applied to the skin or mucous
membrane that either enhance or restore a fundamental function of a
skin or pharmacologically alter an action in the underlined tissues.
Such products are referred as topical or dermatological product [3].
Hydroxypropyl methylcellulose (HPMC), Carbapol 934P, Sodium alginate has been used as hydrophilic polymers topically in gel drug
delivery system [4, 5]. A series of grades based on molecular fractions
*Corresponding author.
A Gupta
Babu Banarasi Das National Institute of Technology
and Management,
Lucknow, India
Tel.: + 91-0902346846
E-mail: abhibbd2006@gmail.com,
vikas_4308@rediffmail.com
Viscosity
Viscosity was determined by using brookfield viscometer.
Viscosity measurements were carried out at room temperature (2527C) using a Brookfield viscometer (Model RVTDV II, Brookfield
Engineering Laboratories, Inc, Stoughton, MA). (Table 3)
Consistency
The measurement of consistency of the prepared gels was
done by dropping a cone attached to a holding rod from a fix distance
of 10cm in such way that it should fall on the centre of the glass cup
filled with the gel. The penetration by the cone was measured from
the surface of the gel to the tip of the cone inside the gel. The distance traveled by cone was noted down after 10sec. [9] (Table 3)
Homogeneity
F2
F5
F8
Drug content
Preformulation studies are needed to ensure the development of a stable as well as therapeutically effective & safe dosage
form. It is a stage of development during which characterizes the
physico-chemical properties of the drug substance and it interaction
with various formulation components. (Table 2)
pH
The pH of various gel formulations was determined by using digital pH meter (Table 3)
Spreadability
It was determined by wooden block and glass slide apparatus. Weights about 20g were added to the pan and the time were
noted for upper slide (movable) to separate completely from the fixed
slides. [8] (Table 3)
Spreadability was then calculated by using the formula:
S = M.L / T
Where,
S = Spreadability
M = Weight tide to upper slide
L = Length of glass slide
T = Time taken to separate the slide completely from each other
Drug Invention Today Vol.2.Issue 5.May 2010
Drug
(g)
F1
F2
F3
F4
F5
F6
F7
F8
F9
1
1
1
1
1
1
1
1
1
Polymer (g)
HPMC
Carbapol
(g)
934P (g)
3
3.5
4
-
0.25
0.5
0.75
-
Sodium
alginate (g)
8
8
8
10%
Glycerin
Methyl
Propyl
Distilled
NaOH
(ml)
paraben (ml)
paraben (ml)
Water (ml)
q.s.
q.s.
q.s.
15
15
15
15
15
15
15
15
15
0.1
0.2
0.3
0.05
0.1
0.15
Upto100
Upto100
Upto100
Upto100
Upto100
Upto100
Upto100
Upto100
Upto100
Solubility
Methanol
++++
Dissolution
Partition
Melting
Ethanol
(95%)
Water
& GAA
Ether,
chloroform
constant (PKa)
coefficient
point 0 C
+++
++
3.5
280
++++ Very soluble, +++ moderately soluble, ++ slightly soluble, + practically soluble
pH
Spreadability
Viscosity
Consistency Homogeneity
Skin
Drug
7.4
6.8
7.1
(g.cm/sec)
5.6
3.8
3.9
(dyns/cm 2)
0.94*10 -3
1.6*10 -3
1.7*10 -3
(60 sec)
6 mm
6 mm
5 mm
irritation
Nil
Nil
Nil
Content (%)
99.81
99.75
99.96
Very Good
Good
Good
Batches
Months
Appearance
pH
F2
F5
F8
0
1
2
3
0
1
2
3
0
1
2
3
Clear
Clear
Clear
Clear
Clear
Clear
Clear
Clear
Clear
Clear
Clear
Clear
7.4
7.4
7.3
7.3
6.8
6.8
6.7
6.6
7.1
7.1
7.1
7.0
Drug
Content (%)
99.81
98.27
97.54
96.91
99.75
98.87
96.05
95.33
99.96
97.12
96.43
95.65
1
2
3
4
Time
Interval
(min)
30
60
90
120
Medium pH
Batch F2
6.8
6.8
6.8
6.8
38.54
64.78
81.23
96.87
%Drug release
Batch F5
44.61
71.35
84.38
97.72
Batch F8
56.00
75.41
90.11
98.54
5.
6.
7.
8.
9.
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10.
1.
2.
3.
4.
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11.
12.
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Fried JR, Polymer Science and Technology. Prentice-Hall, New Jersey, 1998.
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