Research Article [Jain
et al
., 2(4): April, 2011]
ISSN: 0976-7126
Int. J. of Pharm. & Life Sci. (IJPLS), Vol. 2, Issue 4: April: 2011, 681-686
681
INTERNATIONAL JOURNAL OF PHARMACY & LIFE SCIENCES
Formulation and evaluation of aceclofenac fast dissolving tablets
Ankur Sharma, Abhishek Jain*, Anuj Purohit, Rakesh Jatav and R. V. Sheorey
Department of Pharmaceutics, Central India Institute of Pharmacy, Indore, (M.P.) - India
Abstract
The present investigation deals with development of fast dissolving tablets of aceclofenac to produce the intended
benefits. Fast dissolving tablets of aceclofenac were prepared using superdisintegrants crospovidone, croscarmellose
sodium and sodium starch glycolate and surfactant sodium lauryl sulfate, using the direct compression method. The
tablets prepared were evaluated for thickness, uniformity of weight, hardness, friability, wetting time, in vitro
disintegration time and in vitro dissolution time. The tablets disintegrated within 18 to 49 seconds. Almost 90% of
drug was released from all formulations within 15 min. Stability studies of the tablets at 40±2°/75%±5% RH for 3
months showed non significant drug loss. The formulation containing 6% of croscarmellose sodium was found to
give the best results. Apart from fulfilling all official and other specifications, the tablets exhibited higher rate of
release.
Key-Words: Direct compression, In vitro dissolution and In vitro disintegration time, Fast dissolving, Aceclofenac,
Wetting time
Introduction
Oral routes of drug administration have wide
acceptance up to 50-60% of total dosage forms. Solid
dosage forms are popular because of ease of
administration, accurate dosage, self medication, pain
avoidance and most importantly the patient
compliance. The most popular solid dosage forms are
being tablets and capsules; one important drawback of
this dosage forms for some patients, is the difficulty to
swallow. Drinking water plays an important role in the
swallowing of oral dosage forms. Often times people
experience inconvenience in swallowing conventional
dosage forms such as tablet when water is not
available, in the case of the motion sickness (kinetosis)
and sudden episodes of coughing during the common
cold, allergic condition and bronchitis. For these
reason, tablets that can rapidly dissolve or disintegrate
in the oral cavity have attracted a great deal of
attention
1
.
Fast dissolving tablets are those when put on tongue
disintegrate instantaneously releasing the drug which
dissolve or disperses in the saliva. Some drugs are
absorbed from the mouth, pharynx and esophagus as
the saliva passes down into the stomach. In such cases,
bioavailability of drug is significantly greater than
those observed from conventional tablets dosage form.
* Corresponding Author:
E-mail: abhishek0684@gmail.com
Their growing importance was underlined recently
when European pharmacopoeia adopted the term
“Orodispersible tablet” as a tablet that to be placed in
the mouth where it disperses rapidly before
swallowing
2
. The bioavailability of some drugs may be
increased due to absorption of drug in oral cavity and
also due to pregastric absorption of saliva containing
dispersed drugs that pass down into the stomach
3
.
Aceclofenac (2-[(2,6-dichlorophenyl) amine]
phenylacetoxyacetic acid) is an orally effective non-
steroidal anti-inflammatory drug (NSAID) of the
phenyl acetic acid group, which possesses remarkable
anti-inflammatory, analgesic and antipyretic properties.
The analgesic efficacy of aceclofenac 100 mg is more
prolonged than that of acetaminophen 650 mg.
Aceclofenac appears to be particularly well-tolerated
among the NSAIDs, with a lower incidence of
gastrointestinal adverse effects
4
. Aceclofenac is
practically insoluble in water. For poorly soluble orally
administered drugs, the rate of absorption is often
controlled by the rate of dissolution. The rate of
dissolution can be increased by increasing the surface
area of available drug by various methods
5
. The
dissolution of a drug can also be influenced by
disintegration time of the tablets. Faster disintegration
of tablets delivers a fine suspension of drug particles
resulting in a higher surface area and faster
dissolution
6
.
Research Article [Jain
et al
., 2(4): April, 2011]
ISSN: 0976-7126
Int. J. of Pharm. & Life Sci. (IJPLS), Vol. 2, Issue 4: April: 2011, 681-686
682
Objective of my study to formulate and evaluate
Aceclofenac fast dissolving tablets by direct
compression method and to increase the drug release
profile in short duration of time. Evaluation of
formulated tablets was done using various quality
parameters like hardness, friability, wetting time, DT,
in vitro dissolution study. Finally, stability study of
optimized batches was performed.
Material and Methods
Materials
Aceclofenac, aspartame and croscarmellose were
received as a gift sample from Stallion Lab. Pvt. Ltd.,
bawla, Gujarat. Sodium Starch Glycolate,
crospovidone, mannitol, sodium lauryl sulfate and
microcrystalline cellulose were gifted from Aura
Nutraceuticals Ltd., Budasan, Gujarat.
Preparation of Fast Dissolving Tablets of
Aceclofenac
7
Different tablets formulations were prepared by direct
compression technique. Drug, diluent,
superdisintegrants, surfactant and sweetener were
passed though sieve # 40 and magnesium stearate was
passed through # 80 sieve. Required quantity of drug,
and surfactant was mixed first than other excipients
were mixed thoroughly. The powder was compressed
using cadmach compression machine equipped with
10/32 round biconvex punches by direct compression
technique. The compositions of various batches are
shown in table 1.
Evaluation of Aceclofenac Fast Dissolving Tablets
Weight variation test
8
Weight variation test was done by weighing 20 tablets
individually, by using Sartorious balance (Model CP-
224 S). Calculating the average weight and comparing
the individual tablet weight to the average weight.
Tablet thickness
8
The thickness was measured by placing tablet between
two arms of the Varnier calipers. 5 tablets were taken
and their thickness was measured.
Tablet hardness
8
The tablet hardness, which is the force required to
break a tablet in a diametric compression force. The
hardness tester used in the study was Monsanto
hardness tester, which applies force to the tablet
diametrically with the help of an inbuilt spring.
Tablet friability
8
The friability of the tablets was measured in a Roche
friabilator (Camp-bell Electronics, Mumbai). Tablets of
a known weight (W
0
) or a sample of 20 tablets are
dedusted in a drum for a fixed time (100 revolutions)
and weighed (W) again. Percentage friability was
calculated from the loss in weight as given in equation
as below. The weight loss should not be more than 1
%. Determination was made in triplicate.
W
0
-W
% Friability = --------------- × 100
W
0
Drug content
9-10
Twenty tablets were taken and amount of drug present
in each tablet was determined. The tablet was crushed
in a mortar and the powder equivalent to 100mg of
drug was transferred to 100ml standard flask. The
powdered was dissolved in 5ml of methanol and made
upto volume with phosphate buffer pH 6.8. The sample
was mixed thoroughly and filtered through a 0.45
membrane filter. The filtered solution was diluted
suitably and analyzed for drug content by UV
spectrophotometer at 274nm using phosphate buffer
pH 6.8 as blank.
Wetting time
11
A piece of tissue paper (12cmx10.75cm) folded twice
was placed in a Petri dish (Internal Diameter = 9cm).
10ml of water containing Eosin, a water soluble dye , is
added to petridish. A tablet is placed carefully on the
surface of tissue paper. The time required for water to
each upper surface of the tablet is noted as a wetting
time. Determination was made in triplicate.
In- vitro Disintegration test
12
The disintegration time was measured using
disintegration test apparatus. One tablet was placed in
each tube of the basket. The basket with the bottom
surface made of a stainless steel screen (mesh no. 10)
was immersed in water bath at 37 ± 20C. The time
required for complete disintegration of the tablet in
each tube was determined using a stop watch. To be
complied with the Pharmacopoeial standards,
dispersible tablets must disintegrate within 3 min when
examined by the disintegration test for tablets.
In- Vitro dissolution studies
12
In vitro dissolution studies for Aceclofenac fast
dissolving tablets was carried out using USP paddle
method at 50 rpm in 900 ml of phosphate buffer pH 6.8
as dissolution media, maintained at 37±0.5°C. 5 ml
aliquot of the solution was withdrawn from the
dissolution apparatus after suitable time intervals, and
the samples were replaced with fresh dissolution
medium. Absorbance of these solutions was measured
at 274 nm using a shimadzu UV-1700UV/VIS
spectrophotometer.
Stability study
12
The stability study of optimized formulation (batch F9)
was carried out as per ICH (International Conference
on Harmonization) guidelines at 400 ºC and 75% RH
using stability chamber for three month. The effects of
temperature and time on the physical characteristics of
tablets were evaluated for assessing the stability of
prepared formulations. The samples were collected
monthly and different parameters like hardness,
Research Article [Jain
et al
., 2(4): April, 2011]
ISSN: 0976-7126
Int. J. of Pharm. & Life Sci. (IJPLS), Vol. 2, Issue 4: April: 2011, 681-686
683
uniformity of weight, friability, drug content and
disintegration time were studied.
Results and Conclusion
Attempt was made in the present investigation to make
a fast dissolving tablet of Aceclofenac by direct
compression method. Formulation was carried out
using different three types of super disintegrants and
optimized the concentration and hardness of the tablet
to give the minimum disintegration time and get
maximum drug release. To improve the in-vitro
dissolution optimized the concentration of surfactant.
1.5 % concentration of surfactant used to get maximum
drug release with minimum time. Since the flow
properties of the powder mixture are important for the
uniformity of the mass of the tablets, the flow of the
powder mixture was analyzed before compression of
the tablets. The results of angle of repose and
compressibility index (%) ranged from (24.23±0.04º to
28.75±0.01º) and (15.22±0.04 to 23.52±0.02),
respectively. The results of loose bulk density and
tapped bulk density ranged from (0.36±0.04 gm/cm
3
to
0.39±0.03 gm/cm
3
) and (0.46±0.01 gm/cm
3
to
0.56±0.03 gm/cm
3
), respectively. The results of angle
of repose (<30) and compressibility index indicates
good flow properties of powder blend (Table 2).
The results of physical properties of different batches
of aceclofenac fast dissolving tablets are given in
(Table 3). Tablet mean thickness was almost uniform
in all the formulations. The thickness varies between
3.69±0.2 mm to 3.80±0.02 mm. The prepared tablets in
all the formulations possessed good mechanical
strength with sufficient hardness in the range of
3.0±0.15 kg/cm
2
to 3.6±0.1 kg/cm
2
. Friability values
below 1% were an indication of good mechanical
resistance of the tablets. All the tablets from each
formulation passed weight variation test, as the %
weight variation was within the Pharmacopoeial limits
of ±7.5% of the weight. The weight variation in all the
formulations was found to be 198.4±0.89 mg to
201.0±1.0 mg. The percentage drug content of all the
tablets was found to be between 99.23±0.53 to
101.56±1.34 percent of aceclofenac which was within
the acceptable limits.
The wetting time for all the formulations was
performed in triplicate. The time for all formulations
varied between 18±0.97 to 86±2.11 sec (Table 3). The
wetting time of the tablets were also considerably
reduced in tablets containing croscarmellose which
may be attributed due to the wicking and swelling type
of disintegrants thus facilitating the faster
disintegration. The in vitro dissolution profile indicated
faster and maximum drug release from formulation F-9
(Fig. 2).
Formulation F-9 which showed promising results, were
subjected to stability studies at ambient room
conditions for 3 months. After 3 months, aceclofenac
fast dissolving tablets did not show any change in
physical appearance or drug content. In the formulation
using superdisintigrant with the concentration of 6%
and hardness range of 3-4 kg/cm2, disintegration time
and drug release found to be 18±0.97 seconds and
99.07±0.10% respectively within 15 minutes.
Percentage friability and % drug content were found
0.64±0.01% and 99.57±0.26%, respectively and were
within the acceptable limit.
In the present study, the effects of different
concentrations of superdisintegrants on FDT of
Aceclofenac were studies. It was found that
aceclofenac tablets passes for hardness, friability,
wetting time, DT, and in vitro dissolution profile. It
was observed that when croscarmellose sodium used at
6% concentration (formulation F9) with surfactant (3
mg) % drug release was maximum in 15 minutes and
disintegration time was least (18 seconds). And in
stability testing of batch F9, tablets did not show any
change in physical appearance or drug content.
Therefore it is concluded that croscarmellose sodium
can be effectively used as superdisintegrant in
aceclofenac fast dissolving tablets.
Acknowledgments
Authors thank the Principal for providing the facilities
and in the institute.
References
1. Bhowmik D., Chiranjib B., Krishnakanth,
Pankaj, Chandira R.M. (2009). Fast dissolving
tablet: An overview. Journal of Chemical and
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2. Bhandari S., Mittapalli R.K., Ganu R., Rao Y.M.
(2008). Orodispersible tablets: An overview.
Asian J. Pharm., 2(1):2-11.
3. Swamy P.V., Gada S.N., Shirsand S.B., Kinagi
M.B. and Shilpa H. (2010). Design and
evaluation of cost effective orodispersible tablets
of diethylcarbamazine citrate by effervescent
method. International Journal of Pharma
Sciences and Research, 1(6): 258-264.
4. Srinivas M., Parambil A., Krishnan M., Achutha
N.U. (2008). Enhancement of dissolution rate
and bioavailability of aceclofenac. International
Journal of Pharmaceutics, 350: 279– 290.
5. Indian Pharmacopoeia (2007). Ministry of
Health and Welfare; Controller of Publication;
63.
6. Wagh M.P., Yewale C.P., Zate S.U., Kothawade
P.I. and Mahale G.H. (2010). Formulation and
evaluation of fast dispersible tablets of
aceclofenac using different superdisintegrants.
Research Article [Jain
et al
., 2(4): April, 2011]
ISSN: 0976-7126
Int. J. of Pharm. & Life Sci. (IJPLS), Vol. 2, Issue 4: April: 2011, 681-686
684
International Journal of Pharmacy and
Pharmaceutical Sciences, 2: 154-157.
7. Malakar S., Rao S.B., Kumar A.P. and Kulkarni
S.V. (2010). Formulation and evaluation of fast
dispersible aceclofenac tablets: effect of
functionality of super disintegrants. Journal of
Global Pharma Technology; 2(5): 90-96.
8. Banker G.S. and Anderson N. R. (1987). In:
Lachman L., Lieberman H.A. and Kanig J.L. The
Theory and Practice of Industrial Pharmacy. 3rd
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399.
9. Ravikumar, Patil S.R., Patil M.B., Paschapur
M.S. and Mahalaxmi R. (2010). Design and
characterization of aceclofenac mouth dissolving
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Der Pharmacia Lettre, 2(1) :220-236.
10. Chakraborthy S., Khandai M., Singh S.P. and
Patra N. (2008). Comparative study on effect of
natural and synthetic superdisintegrant in the
formulation of fast dissolving tablets.
International Journal of Green Pharmacy, 22-
25.
11. Patel H.A., Patel J.K., Patel K.N. and Patel R.R.
(2010). Studies on formulation and in-vitro
evaluation of fast dissolving tablets of
domperidone. Int. J. Ph. Sci., 2(1): 470-476.
12. Shah D.P., Jain V.C., Sonani N.G., Dalvadi H.P.
and Patel N.J. (2010). Influence of various
excipients on quality control parameter of
aceclofenac tablets containing SSG.
International Journal OF Pharmaceutical
Sciences, (1):113-121.
Table 1: Composition of Fast Dissolving Tablets of Aceclofenac
Ingredients
(mgs)
Formulation Code (in mg)
T
F1
F2
F3
F4
F5
F6
F7
F8
F9
Aceclofenac
100
100
100
100
100
100
100
100
100
100
Mannitol
77
74
70
66
74
70
66
74
70
66
Crospovidone
-
4
8
12
-
-
-
-
-
-
Sodium starch
glycolate
-
-
-
-
4
8
12
-
-
-
Croscarmellose
Sodium
-
-
-
-
-
-
-
4
8
12
Microcrystalline
Cellulose
7
7
7
7
7
7
7
7
7
7
Aspartame
10
10
10
10
10
10
10
10
10
10
Magnesium
stearate
2
2
2
2
2
2
2
2
2
2
Surfactant
-
3
3
3
3
3
3
3
3
3
Total
200
200
200
200
200
200
200
200
200
200
Research Article [Jain
et al
., 2(4): April, 2011]
ISSN: 0976-7126
Int. J. of Pharm. & Life Sci. (IJPLS), Vol. 2, Issue 4: April: 2011, 681-686
685
Table 2: Angle of Repose, Loose Bulk Density, Tapped Density and % Compressibility Index
Each data represents Mean ±SD (n=3)
Table 4: Stability Study of Optimized Batch of Aceclofenac Fast Dissolving Tablets
Sr.
No.
Time
Parameters
Hardness
(Kg/cm
2
)
Uniformity of
weight
Disintegration
time(sec)
Drug content
(%)
1
0 week
3.6±0.57
200.2±0.32
18±1.02
99.57±0.09
2
4 week
3.4±0.15
200.3±0.28
17±1.59
98.83±0.11
3
8 week
3.3±0.10
200.6±0.34
17±0.83
97.49±0.12
4
12 week
3.1±0.15
200.8±0.33
16±0.93
96.71±0.15
Each data represents Mean ±SD (n=3)
0 sec. 9 sec. 22 sec. 34 sec.
Fig. 1: Wetting time of Fast Dissolving tablet ( batch F9)
Formulation
Code
Angle of
Repose (θ)
Loose Bulk
Density
(gm/cm
3
)
Tapped Bulk
Density
(gm/cm
3
)
% Compressibility
T
25.67±0.02
0.36±0.04
0.56±0.03
23.52±0.02
F1
26.43±0.02
0.37±0.01
0.47±0.01
21.27±0.04
F2
27.35±0.02
0.39±0.02
0.49±0.02
20.40±0.03
F3
28.75±0.01
0.38±0.01
0.46±0.01
17.39±0.05
F4
26.98±0.01
0.37±0.01
0.47±0.01
21.21±0.02
F5
25.12±0.03
0.39±0.03
0.49±0.02
20.40±0.03
F6
24.53±0.04
0.37±0.03
0.50±0.02
22.91±0.02
F7
25.65±0.02
0.38±0.02
0.48±0.03
20.83±0.01
F8
24.63±0.03
0.39±0.02
0.48±0.01
18.75±0.03
F9
24.23±0.04
0.39±0.01
0.46±0.03
15.22±0.04
Research Article [Jain
et al
., 2(4): April, 2011]
ISSN: 0976-7126
Int. J. of Pharm. & Life Sci. (IJPLS), Vol. 2, Issue 4: April: 2011, 681-686
686
In-vitro Release of Aceclofenac Fast Dissolving Tablets
0
20
40
60
80
100
120
0 5 10 15 20
Time (min)
% Cummulative drug release
T
F1
F2
F3
F4
F5
F6
F7
F8
F9
Fig. 2: Drug release study of aceclofenac Fast Dissolving tablets of different batches in pH 6.8
phosphate buffer
Table 3: Result of Evaluation Parameters of Aceclofenac Fast Dissolving Tablets
Each data represents Mean ±SD (n=3)
Formulation
code
Parameters
Average
weight (mg)
Thickness
(mm)
Hardness
%
Friability
% drug
content
Wetting
time (sec)
Disintegration
time (sec)
T (Trial
Batch)
201.0±1.0
3.79±0.03
3.3±0.05
0.76±0.03
99.69±0.54
86±2.11
82±2.5
F1
200.0±0.81
3.69±0.2
3.3±0.1
0.75±0.01
99.23±0.53
52±2.18
26±2.03
F2
200.1±0.26
3.70±0.2
3.2±0.1
0.78±0.01
99.34±0.44
51±2.33
34±1.75
F3
200.1±0.39
3.69±0.2
3.0±0.15
0.81±0.02
99.64±1.24
47±1.24
49±1.5
F4
198.4±0.89
3.80±0.02
3.3±0.15
0.76±0.01
101.56±1.34
46±1.36
29±1.23
F5
198.6±0.93
3.80±0.02
3.6±0.1
0.64±0.02
99.85±0.65
42±1.33
24±1.89
F6
200.1±0.32
3.79±0.02
3.2±0.15
0.79±0.01
98.62±0.61
39±1.28
20±1.13
F7
200.1±0.29
3.78±0.2
3.3±0.1
0.75±0.02
99.23±0.40
40±2.31
19±1.73
F8
199.4±0.43
3.79±0.2
3.2±0.05
0.71±0.01
99.41±0.56
37±1.58
19±1.25
F9
199.6±0.28
3.80±0.2
3.5±0.05
0.64±0.01
99.57±0.26
34±1.52
18±0.97