154

ResearchArticle
FORMULATIONANDEVALUATIONOFFASTDISPERSIBLETABLETSOFACECLOFENACUSING
DIFFERENTSUPERDISINTEGRANT
MILINDPWAGH*,CHETANPYEWALE,SANTOSHUZATE,PARESHIKOTHAWADE,GANESHHMAHALE
DepartmentofPharmaceutics,MVPSsCollegeofPharmacy,Shivajinagar,GangapurRoad,Nashik422002,Maharashtra,India.
[email protected]
ABSTRACT
Convenience of administration and patient compliance are gaining significant importance in design of dosage form.
Fast dispersible tablets disintegrate either rapidly in water, to form a stabilized suspension, or disperse
instantaneouslyinthemouthtobeswallowedwithouttheaidofwater.Aceclofenac,anonsteroidalantiinflammatory
drug,isusedforposttraumaticpainandrheumatoidarthritis. Fastdissolvingtabletofaceclofenacwerepreparedby
directcompressionmethodafterincorporatingsuperdisintegrantscroscarmellosesodium,crospovidoneandsodium
starch glycolate. Nine formulation having superdisintegrant at different concentration (10, 15, 20 mg) level were
prepared. Effect of superdisintegrant on wetting time, dispersion time, drug content and in vitro release has been
studied. Tablet containing cross carmellose sodium showed excellent in vitro dispersion time and drug release as
comparedtootherformulation.AfterstudyofnineformulationsF3showsshortdispersiontimewithmaximumdrug
release in 30 min. It is concluded that fastdispersible aceclofenac tablets could be prepared by direct compression
usingsuperdisintegrants.
Keywords:Aceclofenac,Superdisintegrants,Fastdispersibletablets,Dissolutiontest

INTRODUCTION
Aceclofenac, a nonsteroidal antiinflammatory drug
(NSAID) has been indicated for various painful
indications and proved as effective as other NSAIDs
with lower indications of gastrointestinal adverse
effectsandthus,resultedinagreatercompliancewith
treatment
1,2
. Aceclofenac is practically insoluble. For
poorly soluble orally administered drugs, the rate of
absorption is often controlled by the rate of
dissolution
3
. The rate of dissolution can be increased
by increasing the surface area of available drug by
various methods (micronization, complexation, solid
dispersion)
4
.
Many patients find it difficult to swallow tablets and
hard gelatin capsules and thus do not comply with
prescription. This results in high incidence of
noncompliance and ineffective therapy
5
.

The proper
choice of superdisintegrant and its consistency of
performance are of critical importance to the
formulation development of fast dispersible tablets
6
.
The objective of the present study is to develop fast
dispersible tablets of aceclofenac and to study the
effectoffunctionalitydifferencesofsuperdisintegrants
on the tablet properties as well as to improve the
patient compliance without compromising the
therapeuticefficacy.
MATERIALSANDMETHODS
Materials
Aceclofenac (Glenmark Pharmaceuticals Ltd. Nasik,
India). Croscarmellose sodium, Sodium starch
glycolate, Crospovidone and Microcrystalline cellulose
(Intas Pharma, Ahmadabad, India), Aspartame
(Ranbaxy, New Delhi, India) were obtained. Other
materialsandsolventsusedwereofanalyticalgrade.
Preparationoftablets
Fast dispersible tablets containing 100 mg of
aceclofenac were prepared by direct compression
methodandthevariousformulaeusedinthestudyare
shown in [Table 1]. All the ingredients without
magnesium stearate and talc were mixed uniformly
followed by addition of magnesium stearate and talc.
Thepreparedpowderblendwasevaluatedforvarious
parameters like bulk density, tapped density, angle of
repose, compressibility indexand Hausner ratio. After
evaluation of powder blend the tablets were
compressed with a tenstation rotary punchtableting
machine (Rimek Mini Press1) using 7 mm flat
punchesset.
Evaluationofpowderblends
4,79
:

Bulkdensity
Apparentbulkdensity(b)wasdeterminedbyplacing
presieved drug excipients blend into a graduated
cylinder and measuring the volume (Vb) and weight
(M)asitis.
b=M/Vb
Tappeddensity
The measuring cylinder containing a known mass of
blend was tapped for a fixed number of taps. The
minimumvolume(Vt)occupiedinthecylinderandthe
weight (M) of the blend was measured. The tapped
density(t)wascalculatedusingfollowingformula.
t=M/Vt
International Journal of Pharmacy and Pharmaceutical Sciences
Vol 2, Suppl 1, 2010
155

TableNo1:TableshowsFormulationofFastDispersibleTabletofAceclofenac.
Ingredients(mg/tablet)
Formulations
F1 F2 F3 F4 F5 F6 F7 F8 F9
Aceclofenac 100 100 100 100 100 100 100 100 100
CroscarmelloseSodium 10 15 20
Crospovidone 10 15 20
SodiumStarchGlycolate 10 15 20
Microcrystallinecellulose 40 40 40 40 40 40 40 40 40
Mannitol 34 29 24 34 29 24 34 29 24
Aspartame 10 10 10 10 10 10 10 10 10
Talc 4 4 4 4 4 4 4 4 4
MagnesiumStearate 2 2 2 2 2 2 2 2 2
Total 200 200 200 200 200 200 200 200 200
Angleofrepose
Angle of repose () was determined using funnel
method. The blend was poured through a funnel that
can be raised vertically until a maximum cone height
(h) was obtained. The radius of the heap (r) was
measuredandangleofreposewascalculated.
=tan1(h/r)
Compressibilityindex
The simplest way of measurement of free flow
propertyofpowderiscompressibility,anindicationof
theeasewithwhicha materialcanbe inducedtoflow
is given by % compressibility which is calculated as
follows:
C=(tb)/t*100
tTappeddensity,bUntappedbulkdensity
Hausnersratio
Hausnersratioisanindexofeaseofpowderflow;itis
calculatedbyfollowingformula.
Hausnersratio=t\b
tTappeddensity,bUntappedbulkdensity
Table2:TableShowsEvaluationsPowderBlend
Parameters
Formulations
F1 F2 F3 F4 F5 F6 F7 F8 F9
Bulkdensity
(gm/cm
3
)
0.4340.04 0.4390.05 0.4490.04 0.4250.02 0.4160.03 0.4250.04 0.4210.05 0.4250.03 0.4300.04
Tappeddensity
(gm/cm
3
)
0.4700.05 0.4760.03 0.4870.04 0.4650.03 0.4590.05 0.4650.01 0.4590.02 0.4700.06 0.4810.03
Angleofrepose 24.330.03 24.150.02 24.090.03 25.670.01 26.340.02 25.780.04 24.130.01 25.820.02 24.490.03
%Compressibility 7.65 7.77 7.80 8.60 9.36 8.60 8.27 9.57 10.60
Hausnersratio 1.082 1.084 1.084 1.094 1.103 1.094 1.090 1.105 1.118
Evaluationoftablets
Allthetabletswereevaluatedfordifferentparameters
as hardness, friability, drug content, wetting time, In
vitrodispersiontime,andInvitrodissolutionstudy.
Hardness
8,10

For each formulation, the hardness of tablets was

determined usingthe Fizerhardnesstester(Cadmach,
India)
Friabilitytest
8,10
Twenty tablets were weight and placed in the Roche
friabilator (Electolab, Mumbai) and apparatus was
rotated at 25 rpm for 4 min. after revolution the
tablets were dusted and weighed. The friability is
givenbytheformula:
F=(1Wo/W)x100
Where,Woistheweightofthetabletsbeforethetest
andWistheweightofthetabletafterthetest.
Drugcontent
11

Two tablets were powdered and the blend equivalent

to200mgofaceclofenacwasweighedanddissolvedin
suitable quantity of phosphate buffer of pH (7.4). The
solution was filtered, suitably diluted and the drug
content was analyzed spectroscopically at 274 nm.
Eachsamplewasanalyzedintriplicate.
Wettingtime
12,13

A piece of tissue paper (10.7512 mm).folded twice

was placed in a culture dish (d=6.5 cm) containing 6
mlofwater.Atabletwasputonthepaperandthetime
forcompletewettingwasmeasured.
Invitrodispersiontime
14

Tablet was added to 10 ml of phosphate buffer

solution (pH 7.4) at 370.5C. Time required for
completedispersionofatabletwasmeasured.
Invitrodrugrelease
15,16
Invitrodrugreleaseofaceclofenacfromfastdissolving
tablets was determined using USP Dissolution Testing
Apparatus II (Paddle type) (Disso2000, Labindia).The
dissolution test was performed using 900 ml of
phosphate buffer (pH 7.4) at 37 0.5
0
C. The speed of
rotation of paddle was set at 100 rpm. At a
predetermined time interval (5 min); 5 ml samples
156

were withdrawn, filtered through Whatman filter

paper. Absorption of solution was checked by UV
spectrophotometer at 274 nm and drug release was
determinedfromstandardcurve.
Table3:TableShowsEvaluationsofTablets
Parameters
Formulations
F1 F2 F3 F4 F5 F6 F7 F8 F9
Hardness(kg/cm2) 3.81 3.89 3.92 3.42 3.48 3.50 3.66 3.68 3.71
Friability(%) 0.352 0.357 0.361 0.291 0.293 0.293 0.426 0.426 0.428
DrugContent(%) 99.31 99.42 99.60 98.86 99.23 99.56 99.43 99.34 99.12
WettingTime(sec) 57.43 57.56 56.23 54.46 55.56 54.54 59.35 59.45 56.37
DispersionTime(min) 28.31 24.10 23.34 31.56 33.47 35.42 33.35 29.25 29.41
%drugrelease
(min)
5 42.67 62.81 71.69 38.26 59.54 64.67 31.47 53.96 60.71
30 89.39 94.76 99.21 87.98 95.79 95.56 92.67 88.87 83.64
RESULTANDDISCUSSION
For each designed formulation, blend of drug and
excipients was prepared and evaluated for
micromeritic properties shown in Table2. Bulk
density was found to be between 0.4160.03 and
0.4490.04 gm/cm
3
and tapped density between
0.4590.05 and 0.4870.03 gm/cm
3
for all
Formulations. From density data % compressibility
was calculated and was found to be between 7.65%
and 10.60%. Angle of repose was found to be in the
range of 24.130.02 and 26.340.02. Hausner ratio
wasfoundbelow1.118. Alltheformulation showsthe
good blend properties for direct compression and
hence tablets were prepared by using direct
compressiontechnology.
Asthetabletpowdermixturewasfreeflowing,tablets
produced were of Hardness (3.50 3.92 kg/cm
2
) and
friability loss (0.2910.428 %) indicated that tablets
had a good mechanical resistance. Drug content was
found to be high (98.86%) in all the tablet
formulations. Thus wettingtimes of tablets was found
to be crospovidone croscarmellose sodium sodium
starch glycolate. While dispersion time was found
croscarmellose sodium sodium starch glycolate
crospovidone. The influence of superdisintegrants on
the dissolution of aceclofenac from the tablets is
shownasbelow.Thedrugreleasein5minand30min
increased with increase in the level of croscarmellose
sodium. However values decreased with increase in
the level of sodium starch glycolate. While values did
notchangeproportionallywithincreaseinthelevelof
crospovidone shown in fig 1, 2 and 3. Out of nine
formulations F3 formulation is best shows drug
release99.21in30minshowninfig3.
0 5 10 15 20 25 30
0
20
40
60
80
100
F1
F4
F7
Time (min)
%

D
r
u
g

c
u
m
u
l
a
t
i
v
e

r
e
l
e
a
s
e

Fig.1:FigureShows%CumulativeDrugReleaseof
FormulationF1,F4andF7
0 5 10 15 20 25 30
0
20
40
60
80
100
F2
F5
F8
Time (min)
%

D
r
u
g

c
u
m
u
l
a
t
i
v
e

r
e
l
e
a
s
e

Fig.2:FigureShows%CumulativeDrugReleaseof
FormulationF2,F5andF8
0 5 10 15 20 25 30
0
50
100
150
F3
F6
F9
Time (min)
%

D
r
u
g

c
u
m
u
l
a
t
i
v
e

r
e
l
e
a
s
e

Fig.3:FigureShows%CumulativeDrugReleaseof
FormulationF3,F6andF9
CONCLUSION
Inthepresentstudy,3disintegrantsrepresentingeach
of the 3 main classes of superdisintegrants differed in
their ability to disintegrate model tablets into their
primary particles when used at the same w/w
percentage concentration. Such a difference can
potentially affect drug dissolution. The dissolution
parameters were consistent with dispersion times of
croscarmellose sodium and sodium starch glycolate
containing tablets, while not consistent with
crospovidone.
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