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Preparation and Evaluation of oral dispersible cetirizine tablets

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 Rajani et.al IJPPA, 2017;VOl -01(03):44-52 Original Research Article
ISSN:2394-1618

INTERNATIONAL JOURNAL OF PHARMACY

AND PHARMACEUTICAL ANALYSIS
Journal Home Page: www.ijppa.com

“PREPARATION AND EVALUATION OF ORAL DISPERSIBLE

CETIRIZINE TABLETS”
Rajani* V, Lavanya B and Parthiban P

Nova College of Pharmaceutical Education and Research, Vijayawada-521456,

Andhra Pradesh, India
E-mail id: rajani.vaddeswarapu@gmail.com
ABSTRACT
Cetirizine is a second generation Anti- histamine used in the treatment of allergies,
hayfever, angioedema, urticaria. Oral dispersible Cetirizine tablets are necessary for
immediate pharmacological action to decrease the allergic reaction to relieve the patient
from suffering. It is a major metabolite of hydroxyzine and a racemic selective H1 receptor
inverse agonist.This dissertation work was done with an aim to design an immediate
release oral dosage of Cetirizineand evaluation of the tablets for various parameters
including in vitro drug release studies. Cetirizine tablets were formulated by using
microcrystalline cellulose and mannitol as fillers, croscarmellosesodium (CCS),
crospovidone (CP)as super disintegrant and magnesium stearate as lubricant. The
powdered blend were compressed into tablets and were analyzed for the parameters such
as average weight, disintegration time, friability, thickness, weight variation, hardness,
moisture content and drug content.The formulation F1 with low mannitol concentration
and 48% of croscarmellose sodium as super disintegrant showed satisfactory results than
other formulations.

INTRODUCTION Tablets remain popular as a dosage form

because of the advantages afforded both
to the manufacturer and the patient.
Tablets may be defined as the solid
pharmaceutical dosage forms containing
Properties of tablets
drug substances with or without suitable
diluents and prepared either by
The attributes of an acceptable tablet are
compression or moulding methods. They
as follows:
have been in wide spread use since the
latter part of the 19th century and their
➢ The tablet must be sufficiently
popularity continues. The term
strong and resistant to shock,
compressed tablet is believed to have
abrasion, should withstand
been first used by “JOHN WYETH”.
 Rajani et.al IJPPA, 2017;VOl -01(03):44-52
handling during manufacturing,
packing, shipping, and use.
Hardness and friability tests
measure this property.
➢ Tablet must be uniform in weight
and in drug content of the
individual tablet. This is
measured by the weight variation
and content uniformity tests.
➢ The drug content of the tablet
must be bioavailable. This
property is measured by the
dissolution test. Accurate
bioavailability can be obtained
from the drug levels in the blood
after its administration.
➢ Tablets must be elegant in
appearance, characteristic shape,
color and other markings
necessary to identify the product.
➢ Tablets must retain all these
functional attributes which
include drug stability and efficacy.
MATERIALS AND METHODOS
Cetirizine HCl, croscarmellose sodium
(CCS), crospovidone (CP), sodium
starch glycolate (SSG),Hydroxy propyl
cellulose. Formula for the Cetirizine HCl
porous tablet tabulated in the Table No.1
Precompression characteristics: Before
going to the formulation the powder
flowproperties like Bulk density, Tapped
density, Truedensity, Angle of Repose,
Compressibility index andHausner’s ratio
were performed and the results
weretabulated in the Table No.2.
i.Bulk density: Bulk density of a
compound varies substantially with the
method of crystallization, milling or
formulation. Bulk density is determined
by pouring pre sieved blend into a
graduated cylinder via a large funnel and
measure the volume and weight.
Original Research Article
ISSN:2394-1618
Bulk density = Weight of blend/Bulk
volume of blend
Bulk density was expressed in g/cc.
ii. Tapped density: Tapped density is
determined by placing a graduated
cylinder containing a known mass of
blend and mechanical tapper apparatus,
which is operated for a fixed number of
taps until the powder bed volume has
reached a minimum volume. using the
weight of the drug in the cylinder and this
minimum volume, the taped density may
be computed.
Dt =M/Vt
Dt = Tapped density
M = weight of blend
Vt = Tapped volume of blend
iii. Carr’s Index (CI): Carr’s index is
measured using the values of bulk density
and tapped density. The following
equation is used to find the Carr’s index.
CI = (TD-BD) x100/TD
Where TD = Tapped density
BD = Bulk density
iv.Hausner’s Ratio: It indicates the flow
properties of the powder and ratio of
Tapped density to the Bulk density of the
powder or blend.
Hausner’s Ratio = Tapped
density/Bulk density
v.Angle of repose: The manner in which
stresses are transmitted through a bead
and the beads response to applied stress
are reflected in the various angles of
friction and response. The method used to
find the angle of repose is to pour the
powder ion a conical heat on a level, flat
surface and measure the included angle
with the horizontal.
Tanθ = h/r
Where, h= height of the heap
r= Radius of the heap
 Rajani et.al IJPPA, 2017;VOl -01(03):44-52
POST COMPRESSION STUDIES
i.Tablet Thickness Test: Randomly 10
tablets were taken from each formulation
trial batch and their thickness was
measured using a Venire caliperse.
ii. Weight Variation Test: The weight
variation test is carried out in order to
ensure uniformity in the weight of tablets
in a batch. The total weight of 20 tablets
from each formulation was determined
and the average was calculated. The
individual weights of the tablets were also
determined accurately and the weight
variation was calculated.
iii.Measurement of Tablet Hardness:
The hardness of tablet is an indication of
its strength. The force is measured in kg
and the hardness of about 3-5 kg/cm2 is
considered to be satisfactory for uncoated
Dissolution parameters
Medium: 0.1N HCL, 900ml.
Apparatus: USP Type 2 (paddle).
Rotation speed: 50 RPM
Temperature: 37±5oC.
Time: 30sec, 1, 1.5,2,4,6,8,10, and15min.
RESULTS AND DISCUSSIONS
Immediate release tablets of Cetirizine
were formulated by direct compression
method by using microcrystalline
cellulose and mannitol as fillers,
croscarmellose sodium (CCS),
crospovidone (CP)as super disintegrated
magnesium stearate as lubricant.
Compatibility studies were performed
using IR spectrophotometer. The IR
spectrum of pure drug and physical
mixture of drug and excipients were
studied. The peaks obtained in the
spectra’s of each formulation correlates
with the peaks of drug spectrum. This
Original Research Article
ISSN:2394-1618
tablets. Hardness of 10 tablets from each
formulation was determined by Monsanto
hardness tester.
iv.Friability Test: It is measured of
mechanical strength of tablets. Roche
Friabilator is used to determine the
friability by following procedure. Twenty
tablets were weighed and placed in Roche
Friabilator where the tablets were
exposed to rolling and repeated shocks
resulting from free falls within the
apparatus. After 100 revolutions, tablets
are removed, degusted and weighed
again. The friability was determined as
the percentage loss in weight of the
tablets.
% Friability = (loss in weight / Initial
weight) X 100
Post compression results were showed in
the Table No.4.
indicates that the drug is compatible with
the formulation components.
The blends were analyzed for parameters
such as Sieve analysis, Bulk density,
Tapped density, Compressibility index
and Hausner’s ratio and the results were
found to be within limits.
Bulk density and tapped density values
were found to be within limits.
Compressibility index has been proposed
as an indirect measure of bulk density,
size and shape, surface area and
cohesiveness of material. The powdered
blend has required flow property.
After compression, all the tablets were
dried at 60oC for 12hrs and were
evaluated for various parameters like
weight variation, hardness, thickness,
friability, disintegration and in-vitro drug
release.
All formulations were found to have good
hardness so they were taken for further
 Rajani et.al IJPPA, 2017;VOl -01(03):44-52
studies. The measured hardness of tablets
of each batch are in the range of 5.1 to 5.4
kg/cm2. Tablets mean thickness were
almost uniform in all formulations and
were found to be in the range of 3.61 to
3.64 mm. Friability values are found to be
less than 1% in all the cases and
considered to be satisfactory. The total
weight of each formulation was
maintained constant and the weight
variation of the tablets was within limits
of 5%. All the tablets passed the
pharmacopoeial specifications for
disintegration of Cetirizine Dispersible
tablets within less than 20 sec.
All 10 formulations were subjected for
the invitro dissolution studies using tablet
dissolution tester USP XXIII. The samples
were withdrawn at different time
intervals and analysed at 231.78nm.
cumulative drug release and cumulative
% drug retained were calculated on the
basis of mean amount of cetirizine
hydrochloride present in the respective
CONCLUSION
Oral dispersible Cetirizine tablets are
necessary for immediate pharmacological
action to decrease the allergic reaction to
relieve the patient from suffering.
In this formulation Croscarmellose
sodium, Crospovidone, Sodium starch
glycolate, L-Hydroxy propyl cellulose with
varying concentrations are formulated
and found that F1 formulation with
Cetirizine Hydrochloride -10mg,
Microcrystalline cellulose-86mg,
Croscarmellose sodium-5mg, was
Mannitol-78mg,Magnesium stearate-
0.5mg, Talc-0.5mg was showing
satisfactory results i.e., tablet
disintegrated in 05sec and its wetting
ability was 28sec.It attained 99.76%in a
time of 8min and dispersion in 20sec
Original Research Article
ISSN:2394-1618
tablet. The results obtained in the in vitro
drug release for the 10 formulations are
tabulated and graph was plotted between
%cumulative drug release vs time.
Formulation
F1,F2,F3,F4,F5,F6,F7,F8,F9,F10 releases
above 85 % respectively at the end of
8min, 10min,12 min and 15 min.
This rapid dissolution might be due to fast
breakdown of particles and rapid
absorption of drugs. The drug release was
completely achieved in a shorter duration
of time. In all the formulations the drug
release was near to 100% within 15
minutes. High dissolution may also occur
due to faster breakdown. F3 showed
release variation probably due to slow
breakdown of particles. Cumulative %
drug retained as a function of time were
calculated for all the formulations.
Cumulative % drug retained as a function
of time for F1-F10 shown in table no4.
when compared to the other
formulations. Formulations with
Crospovidone as superdisintegrant
showed unsatisfactory results. Physically
the tablet shows color change and
kinematically the drug release was
unsatisfied. So it is suggested
crospovidone is not suitable for the
formulation of oral dispersible Cetirizine
Hydrochloride tablets. Formulations with
Sodium starch glycolate with varying
ratios of mannitol showed change in the
drug release with the increase of mannitol
concentration keeping Sodium starch
glycolateconstant,the drug release was
found to be increasing with a decrease in
the concentration of mannitol. So when
compared F1 with F2, F1 showed greater
release of drug with decrease of mannitol
concentration. Similar results was
 Rajani et.al IJPPA, 2017;VOl -01(03):44-52 Original Research Article
ISSN:2394-1618

observed in Hydroxy propyl cellulose as among all the formulations F1

superdisintegrant i.e., with the increase of
mannitol concentration the drug release
was decreased,whenF9 and F10 are
compared keeping Hydroxy propyl
cellulose as constant.F9 showed greater
drug release than F10.As F10 is having
greater concentration of mannitol than
F9. When formulations are made with
Croscarmellose sodium with the increase
of mannitol concentration drug release
was decreased. Also with an increase of
Croscarmellose sodium drug release was
increased. In F2,F3, andF4 formulations
mannitol concentrations are kept
constant and croscarmellose sodium was
varied, it was observed that with an
increase of Superdisintegrants greater
drug release was obtained. But when
compared with mannitol concentration
the drug release was more in low
concentration mannitol formulations. So
formulation with low mannitol
concentration and croscarmellose sodium
as super disintegrated showed
satisfactory results than other
formulations. So it is finally concluded
that in any formulation with increase in
mannitol concentration the drug release
was decreased. The dissolution profiles
and drug content of the tablets were
found to be satisfactory even after
subjecting the tablets to stability studies
at 40oC and 75%RH for 1 month and 3
months respectively.
The formulation F1 and process can be
easily scaled up and can be easily
employed in large scale production
because the process is simple, cost
effective and precise and also yields
reproducible good result that involves
complex process for manufacturing the
tablets.

ACKNOWLEDGEMENT
The authors are sincerely thanks to the Nova college of Pharmaceutical education and
Research, Jupudi, Ibrahimpatnam, Krishna(Dt), AP, India for providing the facilities to
Complete this research work.

Table No.2: Pre-compression parameters for formulation batches

Bulk Tapped
Angle Of Hausner’s
S.No Density Density Compressibility index
Repose Ratio
g/cc3 g/cc3
F1 29.89 0.588 0.666 11.71 1.13
F2 30.12 0.476 0.555 14.23 1.16
F3 30.01 0.50 0.625 20 1.25
F4 30.67 0.555 0.666 20 1.25
F5 29.24 0.454 0.526 13.68 1.15
F6 30.11 0.476 0.540 11.85 1.13
F7 28.15 0.512 0.592 13.15 1.15
F8 29.25 0.492 0.564 12.76 1.14
F9 30.09 0.532 0.623 14.60 1.17
F10 29.52 0.55 0.654 15.90 1.18
 Rajani et.al IJPPA, 2017;VOl -01(03):44-52 Original Research Article
ISSN:2394-1618

Fig: 1 Flow chart representing the process involved in the preparation of tablets

THODOLOGY

Raw material

Study of drug- excipient

compatibility

PreCompression
Dry mixing Evaluation
Bulk density
Compressed into tablets Tapped density
Thickness Compressibility index

Hardness Hausner’s ratio

Release studies and kinetics

Friability
Selection of best formulation
Drug content

Disintegration Stability studies

Dissolution

Table No.1: COMPOSITION OF FORMULATIONS

Ingredients
F1 F2 F3 F4 F5 F6 F7 F8 F9 F10
(mg)
Cetirizine
10 10 10 10 10 10 10 10 10 10
Hydrochloride
MCC 86 65 70 81 65 75 65 65 81 81
Cross
5 10 5 10 - - - - - -
Carmellose
Crospovidone - - - - 10 10 - - - -
Sodium
starch _ _ _ _ -- _ 10 10 - --
glycolate
 Rajani et.al IJPPA, 2017;VOl -01(03):44-52 Original Research Article
ISSN:2394-1618

Hydroxy
propyl _ _ - _ _ - _ - 10 10
cellulose
Mannitol 78 94 94 78 94 84 94 84 78 84
Talc 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5
Magnesium
0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5
stearate
Total 180 180 180 180 180 180 180 180 180 180

Table No.3: Post compression parameters for formulation batches

Thickness Hardness Uniformity Content
S.No Friability
Mm Kg/cm 2 of weight uniformity
F1 3.61 5.4 0.06 181.5 4.95
F2 3.64 5.1 0.18 180.05 4.80
F3 3.65 5.3 0.26 179.6 4.79
F4 3.66 5.3 0.22 180.59 4.87
F5 3.63 5.2 0.28 181.12 4.90
F6 3.62 5.4 0.13 179.98 4.82
F7 3.63 5.1 0.17 180.04 4.85
F8 3.65 5.5 0.24 181.06 4.77
F9 3.64 5.4 O.18 179.92 4.90
F10 3.62 5.3 0.26 180.54 4.89
Table No.4: In-Vitro Release Profile of Cetirizine from formulations F1-F10

Cumulative % drug release

S.No Time
(min) F1 F2 F3 F4 F5 F6 F7 F8 F9 F10

1 1 23 15.4 24.39 20.6 11.72 28.41 20.6 9.26 7.4 9.26

2 1.5 40.1 31.46 34.27 29.91 18.1 43.84 41.9 14.8 13.27 16.67

3 2 55.54 33.01 47.27 37.64 26.05 52.5 52.8 23.15 20.99 24.39

4 4 71.87 52.47 55.25 57.5 30.06 56.52 59.9 43.84 27.48 41.68

5 6 91.09 74.66 60.27 80.55 40.13 61.46 67.9 58.36 41.06 51.88

6 8 99.7 89.19 66.47 90.11 52.49 67.02 79 69.79 51.57 58.37

7 10 99.77 98.75 75.05 99.13 68.87 72.89 87.4 83.07 60.22 67.33

8 12 99.86 98.89 89.86 99.35 72.87 79.89 89.4 91.73 69.18 77.21

9 15 99.96 99.05 90.86 99.89 88.78 89.07 91.4 92.73 86.9 84.32
 Rajani et.al IJPPA, 2017;VOl -01(03):44-52 Original Research Article
ISSN:2394-1618

Fig No:2 In-Vitro Release Profile of Cetirizine from formulations F1 to F10

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