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Ponnaganti et al., J Adv Sci Res, 2022; 13 (2): 142-148 142
Journal of Advanced Scientific Research, 2022; 13 (2): March-2022
Journal of Advanced Scientific Research
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FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF ACECLOFENAC
BY DIRECT COMPRESSION METHOD
Hyma Ponnaganti*, Kaveri Anke
Department of Pharmaceutics, Sarojini Naidu Vanita Pharmacy Mahavidyalaya, Hyderabad, Telangana, India
*Corresponding author: rk_hyma@yahoo.com
Received: 05-11-2021; Revised: 10-03-2022; Accepted: 12-03-2022; Published: 31-03-2022
© Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License
https://doi.org/10.55218/JASR.202213219
ABSTRACT
Nowadays, Oro dispersible tablets are gaining much importance because it is easily approachable and due to its patient
compliance. In this study, Formulation and evaluation of one such tablets of Aceclofenac by direct compression method
using super disintegrants like Cross carmellose sodium (CCS) was performed.
Due to low water soluble property of aceclofenac, it has poor dissolution and bioavailability. In order to minimize this
property OTD’s are prepared. ODT’s were prepared by direct compression method using super disintegrant i.e Cross
Carmellose Sodium (CCS) in different concentrations. The prepared powder blend was subjected to various evaluation
studies like pre compression parameters like angle of repose, tapped density, and bulk density. Post compression
parameters like weight variation, hardness, friability, drug content, wetting time, disintegration and dissolution studies
were performed. The drug excipients compatibility was verified by FTIR.
The precompression evaluation studies showed that the prepared powder blend has good flow property. The hardness
and friability revealed that it has good mechanical strength with acceptable disintegration time. The optimized
formulation indicated good in vitro drug dissolution profile with maximum drug being released at all the time intervals
indicates an ideal profile for the development of ODT’s. The results of pre compression studies and post compression
along with FTIR are presented.
Keywords: Oro dispersible tablets, Aceclofenac, FTIR, Super disintegrant, Cross carmellose sodium.
1. INTRODUCTION
Novel drug delivery system (NDDS) aims to improve
safety and efficacy of drug molecule by formulating a
convenient dosage form for administration and to
achieve better patient compliance; one such approach is
orodispersible tablets [1]. Oral medication delivery
methods, particularly tablets, are the most frequently
used dosage forms because they are small, provide a
consistent dose, and are painless to administer [2].
Dysphagia is more common in the elderly and children
due to physiological abnormalities associated with both
populations. Dysphagia affects approximately one-third
of the population and is linked to a variety of diseases
such as parkinsonism, diabetes mellitus (DM) [3],
mental impairments, motion sickness, unconsciousness,
and lack of water [4,5]. Because of benefits in dosage,
stability, storage, cost, and transportation, the World
Health Organization (WHO) now advises that
dispersible tablets be preferred over suspensions
wherever available. Patient compliance may be
enhanced using dispersible tablets and Orally
Disintegrating Tablets (ODTs), especially in juvenile,
geriatric, and institutionalised patients [6].
Orodispersible tablets (ORDs), sometimes known as
"mouth dissolving tablets," are solid dosage forms that
dissolve rapidly in the oral cavity in less than 1 minute
[7] and combine the benefits of both liquid and
traditional tablet formulations, making it easier to
consume the medicine in a liquid dose form. ORDs
breakdown quickly in the mouth with the assistance of
saliva [8] to create dispersion that may be readily
ingested without the need for water [9]. Other benefits
of ODTs that have been studied include their capacity to
improve the bioavailability of medicines that are poorly
water soluble by improving dissolution profiles [10].
An ideal ODT has a pleasing mouth feel, sufficient
hardness, and an appropriate friability limit, and is
manufactured using traditional methods [11].
ISSN
0976-9595
Research Article
Ponnaganti et al., J Adv Sci Res, 2022; 13 (2): 142-148 143
Journal of Advanced Scientific Research, 2022; 13 (2): March-2022
Superdisintegrants, which improve the disintegration
efficiency of tablets at low concentrations, have been
introduced because of advancements in tableting
technology. Superdisintegrants help ODTs generated by
direct compression disintegrate and dissolve better [12].
In addition, flavouring agents, sweetening agents may
also be added to provide an acceptable taste. Suitable
sweetening agents include sucrose, fructose, glucose,
sodium saccharin, aspartame. Colour is a vital means of
identification for many pharmaceutical tablets and is also
usually important for consumer acceptance [13].
Aceclofenac is a phenyl acetic acid-based Non-Steroidal
Anti-Inflammatory Drug (NSAID) with anti-inflam-
matory and analgesic effects that may be taken orally. It
is one of the most well-tolerated NSAIDs, having a
reduced rate of gastrointestinal side effects. Unfor-
tunately, because its limited water solubility (0.058g
/ml), it has poor dissolving and oral bioavailability.
It is a Biopharmaceutical Classification System (BCS)
class II drug, with oral bioavailability assessed by
gastrointestinal tract dissolution rate. As a result,
improving Aceclofenac solubility is critical to increasing
its bioavailability and therapeutic efficacy [14].
Oral fast dissolving tablets can be made using a variety
of ways. To produce quick tablet disintegration, direct
compression is one of the ways that requires the
addition of super disintegrant or highly water soluble
excipients to the formulation. Direct compression,
which does not utilize water or heat during the
formulation process, is the best technique for moisture
and heat-sensitive medications [14]. The goal of this
study was to develop and evaluate aceclofenac fast-
dissolving tablets using optimization approaches for drug
dissolution and absorption using a superdisintegrant,
cross carmellose sodium.
2. MATERIAL AND METHODS
Aceclofenac was a gift sample from Hetero Drugs Pvt.
Ltd (Hyderabad). Cross carmellose sodium, magnesium
stearate, talc, MCC, sodium saccharin and lactose were
obtained from SD Fine Chemicals. All the other used
were of analytical grade.
2.1. Estimation of Aceclofenac
Aceclofenac was estimated by Spectrophotometric
method at 276nm in phosphate buffer of. Accurately
weighed amount of Aceclofenac was dissolved in 3-4ml
of methanol and stirred until the drug was dissolved and
volume was made upto 100ml using phosphate buffer to
prepare 1mg/ml solution. 1ml of this solution is was
taken out and dissolved in 100ml of buffer solution
which forms secondary stock solution. From this
solution, dilutions were made with pH 6.8 phosphate
buffer to prepare a series of standard solutions
containing 2, 4, 6, 8 and 10 μg/ml of Aceclofenac. The
solutions were analyzed in the region 200-400nm using
UV spectrophotometer (Lab India UV) and the
absorbance was measured at 276nm using phosphate
buffer as blank. The calibration curve of aceclofenac was
plotted as shown in the graph.
Graph 1: Calibration curve of the drug
2.2. Formulation of Orodispersable tablets
The orodispersable tablets were prepared by direct
compression method according to the formula given in
Table 1.
Table 1: Formulation table of Aceclofenac orodispersable tablets
Ingredients (mg)
F1
F2
F3
F4
F5
Aceclofenac
100
100
100
100
100
Microcrystalline sodium
184
186
184
182
179
Cross carmellose sodium
5
10
15
20
25
Lactose
184
186
184
181
179
Sodium saccharin
10
10
10
10
10
Talc
2
2
2
2
2
Magnesium stearate
5
5
5
5
5
Total
500
500
500
500
500
Ponnaganti et al., J Adv Sci Res, 2022; 13 (2): 142-148 144
Journal of Advanced Scientific Research, 2022; 13 (2): March-2022
A total number of five formulations were prepared,
each formulation batch comprised of 30 tablets. Tablets
were formulated using cross carmellose sodium as
superdisintegrating agent at concentrations of 5%, 10%,
15%, 20% and 25%. Weighed quantities of
Aceclofenac, CCS, Lactose, sodium saccharin, MCC,
Talc and Mg stearate were taken. Drug along with the
other excipients were passed through sieve 60 except
talc and magnesium stearate, which were passed
through sieve 40. All the excipients along with drug
were taken in a mortar and pestle and triturated to form
a uniform mixture of the blend. The prepared blend was
compressed into 500mg tablets using 8mm round flat
punches on single station rotary tablet machine. The
composition of each formulation is given in Table 1.
2.3. Precompression evaluation of powder
blend
2.3.1. Angle of repose
Using the funnel method, the angle of repose of the
powder blend was calculated. The powder blend was
placed in a funnel and allowed to flow freely over the
surface after being precisely weighed. The angle of
repose was estimated by measuring the diameter of the
powder cone and repeating the process three times.
2.3.2. Bulk density
A measured quantity of powder blend was taken in a
measuring cylinder and volume occupied by the powder
was noted as bulk volume(vb) and mass as (m). The bulk
density was calculated as
Bulk density=mass of the powder(m)/tapped volume of
the powder(vt)
2.3.3. Tapped density
In a 25ml measuring cylinder, a weighed quantity of
powder was added. The cylinder was allowed to fall
under its own weight onto a hard surface from a height
of 2.5 cm at 2 sec intervals after the initial volume was
determined, mechanically for 50 times i.e 50 tappings.
The volume of powder retained in the cylinder is noted
as final volume (vt). Tapped density was calculated as
follows:
Tapped density=mass of the powder/ tapped volume of
powder (vt)
2.3.4. Compressibility index (Carr’s index)
Carr's granules' flow property features are determined
by the compressibility index. The potential powder arch
and stability are directly measured by the %
compressibility of granules. The following formula may
was used to compute the Carr's index.
% Carr’s index=et -eb /et ×100
Where, ‘et’ is the tapped density of granules and ‘eb’ is
bulk density of granules
2.4. Post compression evaluation of tablets
2.4.1. Weight variation
Each batch had twenty tablets chosen at random, and
the average weight was determined. The individual
weights of the tablets were then compared to the
average weight to determine the weight variance of the
tablets.
2.4.2. Friability
The Roche Friabilator was used to assess tablet friability
at 25 rpm for 4 minutes. The weight of twenty tablets
was recorded before and after the test, and friability was
estimated using the following formula:
% friability = [(initial weight-final weight) ÷ initial
weight] x 100
2.4.3. Hardness
Monsanto hardness Tester was used to determine the
breaking strength of the tablets. It was measured in
terms of kg/cm2. The tablet was placed in between the
two jaws of tester and rotated until the tablet was
broken. The hardness was measured by reading the scale
of the tester. The hardness limits for tablets should be
within the range of 4-6kg/cm2.
2.4.4. Wetting Time and absorption ratio
In a petri plate containing 10mL of water, round tissue
sheets were put. Six pills were then put on the tissue
paper's surface one after the other each time. The
wetting time was defined as the time it took for water
to reach the tablet's top surface. Time taken for wetting
of tablet was noted and wetted tablet was noted. Water
absorption ratio R was determined using the following
equation [15]:
R= Wa-Wb/Wb x 100[9]
Where Wb and Wa are the weights of the tablet before
and after water absorption, respectively.
2.4.5. Drug content
In this method, one tablet from each formulation was
taken in a mortar and pestle and crushed to fine
powder. From the crushed tablet take 5mg of
aceclofenac was taken and dissolved in 20ml of ethanol.
The solution was filtered and 0.1ml of the filtrate was
Ponnaganti et al., J Adv Sci Res, 2022; 13 (2): 142-148 145
Journal of Advanced Scientific Research, 2022; 13 (2): March-2022
taken and diluted in 10ml of ethanol. The absorbance of
resultant solution was measured by spectrophotometric
method at 276 nm in UV spectrometer (UV LAB
INDIA). The drug content was measured using the
standard calibration curve and the average percentage
drug content was calculated using the formula:
Drug content=concentration x dilution factor÷1000
2.4.6. Disintegration Time
Using an Electro lab disintegration device, an in vitro
disintegration test was performed on six tablets from
each batch. Each tablet was put in a disintegration
device with 900 mL of distilled water and kept at 37±2
°C. The disintegration time was calculated as the time it
took for the tablet to completely disintegrate with no
particle matter left in the mesh.
2.4.7. Dissolution Studies
An electro lab dissolution test device was used to
conduct an in vitro dissolution investigation of tablets at
a rotation speed of 100 rpm. The dissolution research
used six tablets from each batch at random. Each tablet
was put in a beaker with 900 mL of pH 6.8 phosphate
buffer. The temperature was kept constant at 37±0.5
C. For the single-point dissolving test on the
preliminary tablets, a sample of 5 mL was withdrawn at
30 minutes, and equivalent quantities of samples were
withdrawn at 5, 10, 15, 20, 25 and 30 minutes to
investigate the release profile of the optimised table.
2.4.8. Fourier transform infrared spectroscopy (FT-
IR)
FTIR was used to investigate the drug-polymer
interaction. The medication and polymer must be
compatible in order to create a stable result. As per the
technique, drug and polymer interactions were
investigated using FT-IR (Bruker Alpha Model).
Lactose, pure acyclofenac, Mg stearate, talc and
microcrystalline cellulose were analysed using infrared
spectroscopy. There is no difference in the peaks of the
combination when compared to the pure medication,
indicating that there are no interactions.
3. RESULTS AND DISCUSSIONS
3.1. Precompression Evaluation
All the precompression evaluation studies like Angle of
Repose, Bulk density, Tapped density, and Carr’s
compressibility index are given in table 2. Angle of
repose defines the flow property of powder blend.
Those with low angle of repose have good flow
property than those with high angle of repose values
[16]. All the formulation blends were shown good flow
property showing angle of repose within the range of
24.93°-30°. All the formulation powders were found
within the range of 0.41-0.43. All the formulation
powder blend were also found within the range of 0.59-
0.65. Carr’s index values were also found within the
range of 12.78-28.61 indicating all the formulation
blend were having acceptable flow property [17].
Table 2: Precompression parameters of powder blend
Formulation
Code
Bulk density
(gm/cc)
Tapped density
(gm/cc)
Angle of repose
(degrees)
Carr’s index
(%)
F1
0.4214
0.59
28.81
28.61
F2
0.4190
0.65
30.0
13.36
F3
0.4217
0.61
26.56
12.78
F4
0.4213
0.64
26.43
13.78
F5
0.4330
0.62
24.93
23.43
3.2. FT-IR Study
The use of spectroscopic methods such as FT-IR in Pre-
formulation has contributed significantly for the early
prediction and possibility of physical and chemical
interactions between the drug and excipient and to assist
in the rationalized selection of the most appropriate
excipients in the design of dosage forms. The drug
sample showed characteristic functional group peaks at
3442.23cm-1 due to N-H stretching, 3181.05cm-1 due
to O-H stretching, 1716.22 cm-1 due to C=O
stretching, 1547.60 cm-1 due to skeleton vibration of
aromatic C-C stretching, 1259.26 cm-1 C-N aromatic
amine, 1419.37 cm-1 O-H in plane bendin. Lactose
showed characteristic functional group peaks at
3460.12-3696.13 cm-1 due to stretching vibrations of C-
O-H bonds of lactose alcohol. Two sharp bands were
found at 3045-2958.84 cm-1 due to C-H stretching
vibrations [18]. Talc showed characteristic vibrations of
hydroxyl groups linked to Si(Si-OH) and Mg(Mg-OH)
at 3441-3671.54cm-1. Then bands with intense peaks at
1040 cm-1 are contributed by the siloxane group (Si-O-
Si) stretching vibrations while bands found at 669.16
cm-1 are due to Si-O-Mg bond [19]. Magnesium stearate
shows characteristic twin peaks at 1540.22 and 1463.55
Ponnaganti et al., J Adv Sci Res, 2022; 13 (2): 142-148 146
Journal of Advanced Scientific Research, 2022; 13 (2): March-2022
cm-1 that are attributed by asymmetric carboxylate
(COO) stretching vibration and symmetric vibrations of
carboxylate group respectively. The peaks at 2916.03
and 2840.34 cm-1 are due to the C-H stretching
vibrations [20]. The FT-IR spectrum of MCC shows
characteristic band of O-H stretching vibrations of
hydroxyl group at 3566.42cm-1. C=O bands of
aldehyde were found at 1771.27cm-1. Peaks at
1507.62cm-1 are associated with CH2 bending
vibrations. C-O stretching vibrations at 1362.80 were
associated with the CH2 -OH group. C-O-C bands were
focused at 1051.22cm-1 [21]. Sodium saccharin showed
characteristic peaks at 1647.40cm-1 due to C=O bonds.
C-C bond stretching vibrations were found at 1558.
40cm-1. Peaks found at 1251.48cm-1and 1145.93cm-1
were attributed to SO2-N- stretching vibrations.
All the characteristic peaks of aceclofenac were found in
their original range in the optimized formulation
indicating that there was no interaction between the
drug and other excipients.
Fig. 2: FTIR spectrum of Aceclofenac
Fig. 3: FTIR spectrum of optimised formulation
Ponnaganti et al., J Adv Sci Res, 2022; 13 (2): 142-148 147
Journal of Advanced Scientific Research, 2022; 13 (2): March-2022
3.3. Post compression parameters
All the post compression parameters results like
Hardness, Thickness, Friability and Weight variation are
given in following table 3.
Other parameters like disintegration, wetting time,
water absorption ratio, drug content are given in table 4.
3.3.1. The wetting time and water absorption ratio
It is one of the important parameter that determines the
ability of tablet to disintegrate and absorption capability
in the presence of small amount of water. The wetting
time was found to be within the range of 22-34 sec. The
gradual decrease in the wetting time is due to increase
in the concentration of super disintegrant that absorbs
water and swells resulting in dispersion of the tablet.
The results are tabulated in the table 5. Disintegrating
time is a very important factor which should be less than
60 sec. There was decrease in disintegrating time with
increase in the concentration of super disintegrator that
is from 54sec in F1 with 5% to 37sec in F5 with 25%
which shows that disintegration is inversely proportional
to the concentration of super disintegrator CCS. The
optimized formulation was found to be within the limits
that is 37 sec.
3.3.2. In vitro dissolution studies
Dissolution studies of the ODTs clearly indicate the
drug release as per specifications, optimized formulation
F5 showed best drug release of 100.8% in 30 min. The
results are shown in fig 4 [21].
Table 3: Post compression studies of aceclofenac tablets
Formulation code
Thickness (mm)
Hardness (kg/cm2)
Friability (%)
Weight variation
F1
2.38
4.0
0.42
480
F2
2.45
3.5
0.84
470
F3
2.34
3.0
0.41
470
F4
2.36
4.0
0.61
481
F5
2.42
3.5
0.42
475
Table 4: Post compression studies of aceclofenac tablets
Formulation code
Disintegration time (sec)
Wetting time (sec)
Water absorption ratio
Drug content
F1
54.8
34
58.69
92.75
F2
46.8
32
60.75
93.95
F3
45.8
29
63.65
95.67
F4
44
25
68.79
97.54
F5
37
22
74.65
99.93
Fig. 4: In vitro drug release studies of Aceclofenac formulations
Ponnaganti et al., J Adv Sci Res, 2022; 13 (2): 142-148 148
Journal of Advanced Scientific Research, 2022; 13 (2): March-2022
4. CONCLUSION
The oral dispersible tablets of aceclofenac were
successfully prepared by direct compression method.
The various evaluation tests like pre compression
studies, FTIR, post compression studies like weight
variation, hardness, drug content, disintegration,
dissolution were performed and results were found to
be within the limits. Formulation F5 with 25% of CCS
has shown the results that satisfies the acceptance
criteria for OTD’S. Hence, it is considered as optimized
formulation. From the above study, we can conclude
that Formulation F5 can be prepared as aceclofenac
ODT’s for better patient compliance than the
conventional forms that are available in the market.
Conflict of interest
The authors declare no conflict of interest.
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