Research J. Pharm. and Tech.

10(9): September 2017

ISSN 0974-3618 (Print) www.rjptonline.org

0974-360X (Online)

RESEARCH ARTICLE

Formulation and Evaluation of Aspirin Tablets by Using Different

Lubricants in Combination for better Kinetic Drug Release Study by PCP
Pawan Singh*, Prevesh Kumar, Dr. Neelkant Prasad
Asst. Professor, IFTM University Moradabad-244001
*Corresponding Author E-mail: Pawansinghh690@gmail.com

ABSTRACT:
Aspirin tablet is prepared by wet granulation method. Aspirin belonging to the class of NSAID having analgesic,
antipyretic, anti-inflammatory and antiplatelet activity at systematic standard doses. In this Lubricants in
combination leads to better drug release kinetic. The Prepared Tablet is Evaluated In terms of bulk density,
tapped density, the angle of repose, Carr’s Index and, hardness test, weight variation test, friability test and in
vitro study. The result associated with optimized batch is good satisfactory and having better drug release
kinetic. The in-vitro dissolution studies we got result our formulation follow Zero Order Kinetics with the effect
of lubricants using in combination for better kinetic drug release.

KEYWORDS: Aspirin, Wet granulation compression method and Release Kinetic.

INTRODUCTION: Conventional oral dosage forms often produce

Aspirin also has an antiplatelet effect by inhibiting the fluctuations of drug plasma level that either exceeds safe
creation of thromboxane, which binds platelet molecules therapeutic level or quickly fall below the minimum
together to generate a patch over damaged walls of blood effective level; this effect is usually totally dependent on
vessels. Aspirin is used for long-term, at low doses, to the agent’s biologic half-life, the frequency of
prevent heart attacks. Aspirin tablets are obtained by wetadministration, and especially the releaserate[2]. For this
Compression Method. The particles to be compressed purpose, aspirin which is analgesic and antipyretic was
consist of one or more medicaments, with or without selected as a model drug. They are intended for oral
excipients substance such as diluents, binders, and administration. Some tablets are swallowed whole or
disintegration agents, lubricant, glidants and substances after being chewed, some are dissolved or dispersion in
capable of modifying the behavior of the medicaments in water before administration and some are retained in the
the digestive tracts. Such substances must be innocuous mouth where the active ingredient is liberated.
and therapeutically inert in the quantities present. Preparation intended for administration by other routes,
for example, in the form of implants and passerines may
Many strategies are available for the design and also be presented in the form of tablets but because they
development of modified-release drug delivery may require special formulations, methods of
formulations. [1] manufacture or from of presentation appropriate to the
use they may not comply with all the requirement of this
monograph. Because of their composition, a method of
manufacture or intended use, tablets present variety of
characteristics and consequently there are several
Received on 09.06.2017 Modified on 07.07.2017 categories of tablets. Useless otherwise stated in the
Accepted on 20.07.2017 © RJPT All right reserved individual monograph, tablets are uncoated. Where the
Research J. Pharm. and Tech. 2017; 10(9): 2934-2938.
DOI: 10.5958/0974-360X.2017.00519.4 coating is permitted the monograph directs coating the
statement reads “The tablets are coated “Unless
otherwise directed, tablets may be coated in one of the
2934
 Research J. Pharm. and Tech. 10(9): September 2017

different ways. Tablets are the most widely used unit MATERIALS AND METHODS:
solid dosage form of the drug (s) administered by oral Materials:
route. These are administered into the body to produce Aspirin, HPMC, PVP, Sodium Stearate, Talc were
systemic effects of the drug to cure, prevent or suppress procured from Research Lab, IFTM University,
the disease condition. More than 90% of the marketed Moradabad. All the chemicals and reagents were of
drugs are formulated in the form of tablet dosage form as analytical grade.
they produce several advantages in comparison to other
dosage forms such as lack of physical and chemical CALIBRATION CURVE:
stability of the drug in the form of liquids, easy to A standard calibration curve of aspirin was constructed
handle, self-medication can be possible etc. There are in phosphate buffer (pH 7.2) and assayed spectrophoto
different classes of tablets available in the market, in that metrically at 265 nm. the data obtained are given below:
uncoated and coated tablets are one class. Some of the
drugs may be damaged in gastric environment and some Concentration X (µg/ml) Absorbance Y (nm)
0 0
may irritate the gastric mucosa. Drugs that produce this
0.5 0.122
effect are NSAIDS, potent antibiotics like erythromycin, 1 0.241
azithromycin etc. For these type of drugs, layers of 1.5 0.331
coating solution are applied to form a thick coat around 2 0.432
the tablet which may prevent the drug exposure to the 2.5 0.542
acidic environment and moreover prevents gastric
irritation.
Binder:
Binders hold the ingredients in a tablet together. Binders
ensure that tablets and granules can be formed with
required mechanical strength, and give volume to low
active dose tablets. Binders are usually:

Observation Table: List of Binder used in the Tablet Formulation

S.NO. BINDER EXAMPLE
1 Saccharides Sucrose, lactose
2 Polysaccharid Starches, cellulose as microcrystalline
es cellulosehydroxypropyl cellulose
3 Sugar alcohols Xylitol, sorbitol or maltitol
3 Protein: gelatin Equation for the standard curve: Conc. = 4.68
5 Synthetic poly Polyvinylpyrrolidone (PVP), polyethyle Abs. + -0.051 R = 0.9989
mers: ne glycol (PEG).
6 Solution Polyvinylpyrrolidone, starch, sucrose
binders and polyethylene glycol, Method of Preparationof Aspirin tablet:
water or alcohol Four different batches of the tablet were prepared using
7 Dry binders Methylcellulose, Polyvinylpyrrolidone, wet granulation technique. The composition of a tablet
and Polyethylene glycol. per batch is given in Table 1.
LUBRICANTS:
These are preventing ingredients from clumping together The calculated amount which was required to prepare
and from sticking to the tablet punches or capsule filling 400 mg aspirin tablets, containing 250 mg drug, HPMC
machine. Lubricants also ensure that tablet formation polymer, and PVP as abinderwere mixed uniformly[3].
and ejection can occur with low resistance between the
solid and die wall. lubricants in tablets or hard gelatin
capsules. Lubricants are agents added in small quantities An enough granulating agent (water) was added slowly
to tablet and capsule formulations to improve certain to prepare wet mass. Granules were prepared by sieving
processing characteristics. method using a20# sieve. [4]
Table 2: Lubricants Used in the Tablet Formulation
S.NO. LUBRICANTS EXAMPLE
1 Minerals talc or silica, Further, granules were dried at 35-45ºC for six hours.
2 fats stearin, magnesium tearate or stearic The dried granules were stored in desiccators until
acid compression of tablets. Prior to compression, the dried
granules were subjected to study and evaluated for their
flow characteristics. [5]

2935
 Research J. Pharm. and Tech. 10(9): September 2017

shakes during handling in the manufacture, packaging,

and shipping. Hardness generally measures the tablet
The required amounts of granules were weighed and crushing strength. The hardness of tablets was
compressed using automaticallyoperated tablet punching determined using Pfizer hardness tester. [10].
machine having 12mm flat faced punch diameter. and
during the tablet preparation to maintain the Thickness:
low resistance between the solid and die wall, lubricants The thickness of the sustained release tablets was
added in granules. Lubricant combinations are agents determined using Vernier caliper. and the results were
added in small quantities to the tablet during the tablet expressed as mean values of 10 determinations, with
preparation. standard deviations[11].

Disintegration Test (U.S.P.):

The compressed tablets of each batch were stored in The U.S.P. device to test disintegration consists of 6
airtight container at room temperature for further study. glass tubes that are 3inch long; open at the top and 10
[6]
mesh screens at the bottom end. During the
disintegration test, one tablet is placed in each tube and
Table 1: Formula Used to Prepare Tablet.
S. No Ingredients (mg) F1 F2 the basket rack is positioned in a 1-L beaker of either
1 Aspirin 250 250 water, simulated gastric fluid or simulated intestinal fluid
2 HPMC 50 50 at 37 ± 2 °C such that the tablet remains 2.5 cm below
3 Microcrystalline cellulose 70 70 the surface of liquid on their upward movement and not
4 Polyvinyl Pyrrolidone Q. S. Q.S. closer than 2.5 cm from the bottom of the beaker in their
5 Sodium Stearate+ Talc 1+5 0.5+10
downward movement. Move the basket containing the
Evaluation of granules: tablets up and down through 5-6 cm at a frequency of 28
Granules were evaluated for all pre-compression to 32 cycles per minute.
parameters like angle of repose, bulk density, tapped
density, bulkiness, Hauser's ratio and compressibility Drug content:
index. The evaluation was done using all the methods as The tablets were powdered, and 250 mg equivalent
per specified in pharmacopeias[7]. weight of aspirin in tablet powder was accurately
weighed and transferred to a 100-ml volumetric flask.
Table 2: Pre-Compression Properties of Granules. Initially, 10 ml of phosphate buffer (pH 7.2) was added
Properties Batch F1 Batch F2 and shaken for 10 min. [12]Thereafter, the volume was
Bulk density (g/cm3) 0.376(0.017) 0.372(0.016) made up to 100 ml with buffer. Subsequently, the
Tapped density (g/cm3) 0.437(0.022) 0.435(0.022) solution in the volumetric flask was filtered, and 1 ml of
Bulkiness (cm3/g) 2.66(0.031) 2.63(0.031)
the filtrate was diluted and analyzed at 265 nm using
Carr’s index 11.857(0.31) 11.853(0.31)
Hausner’s ratio 1.130(0.30) 1.133(0.30) UV-visible spectrophotometer (Shimadzu UV-1800,
Angle of repose (degrees) 28.37(0.028) 28.33(0.028) Japan). The drug content of each sample was estimated
from their previously prepared standard curve[13].
Evaluation of Tablets:
Weight variation: Table 3: Result-Evaluation parameters of tablets.
Parameters Batch F1 Batch F2
Tablets were evaluated for weight variation as per USP Weight variation (mg) 0.072(±0.025) 0.074(±0.022)
XXIV monograph using digital electronic balance. Hardness (kg) 8.8(±0.023) 8.7(±0.022)
Twenty tablets of each batch were used to evaluate Thickness (mm) 2.76(±0.011) 2.75(±0.012)
weight variation among tablets and mean and the Friability(w/w%) 0.26 ± 0.12 0.30 ± 0.18
standard deviation was calculated[8]. Disintegration Time 27±2 32±1
(min)
Drug content (mg) 248.0(±0.12) 249.0(±0.19)
Friability:
Friability of a tablet can determine in the laboratory byKinetics of Drug Release:
Roche Friabilator. This consists of a plastic chamber that
Kinetics drug release was studied, in 900 ml phosphate
revolves at 25 rpm. Tablets were used to evaluate buffer pH 7.2, maintained at 37±2°C for 6 h, at 100 rpm.
friability as per USP XXIV monograph. Friability testing 5ml of the sample was withdrawn after a specified time
was done by Roche Friabilator with readings in interval and was replaced by an equal volume of fresh
triplicate[9]. dissolution medium.20 Collected samples were analyzed
spectrophotometrically at a measured wavelength of 265
Hardness: nm, and cumulative percent drug release was
Tablet requires a certain amount of strength or hardness calculated[10-11]. The test was performed in triplicate to
and resistance to friability to withstand mechanical
2936
 Research J. Pharm. and Tech. 10(9): September 2017

assure significance of results. Drug release profile was
studied using percentage drug release Vs time (h)
plot.[14]the kinetic study was done F2batch,Various
models such as Zero order kinetics (cumulative
percentage amount of drug release versus time), First
order kinetics (log cumulative percentage of drug
remaining to release versus time), Higuchi (fraction of
drug release, Mt/Mi, versus square root of time) and
Korsermeyer-Peppas (log fraction of drug released, were
applied to assess the kinetics of drug release from
prepared tablets. Most suited model for drug release was
predicted based on regression coefficient i.e. nearer the
value of regression coefficient towards 1, greater the
suitability of best-fitted release mechanism.[15]

% Release (Average) with model fitting, Q(t) and t(x%)

Name of the Drug = Aspirin Batch = none Date = 12/04/2017
Loading Dose in mg = 250
Total no. of Readings, including 'Zero-time' reading =
6 Done by = pawan singh
Dissolution Medium = Phosphate buffer 7.2
RPM = 100
Volume of Dissolution Medium (ml) = 900
Volume of Sample removed (ml) = 5
Dilution Factor = 1
Slope of Calibration curve = 4.5240
Constant of Calibration curve = -0.1371
R of Calibration curve = 0.9972
Mode l Fitting (Ave ra ge )- Be st fit mode l- Zero order
R k Pa ra me te rs ca lcula te d by- Hix.Crow.
Zero order 0.9807 0.1230 Tim e Q (t) %Releas ed t (x %)
T-test 10.043 (Passes) hr hr

1st order 0.9806 -0.0012 1 0.1 0.011 0.1

T-test 10.001 (Passes) 2 0.2 0.012 0.1
Matrix 0.8799 0.2267 3 0.4 0.012 0.1
T-test 3.704 (Passes) 5 0.6 0.012 0.1
Peppas 0.9784 0.0843 6 0.7 0.013 0.1
T-test 9.473 (Passes) Pa ra me te rs for
Hix.Crow. 0.9806 -0.0004 Korsme ye r-Pe ppa s Equa tion-
T-test 10.015 (Passes) n = 1.2509
t-Table at P0.05 (Tw o Tails), DF=n-2:- 2.776 k = 0.0843
MODEL FITTING: Residual Sum of Squares
RESULTS Ze ro 1st orde r Ma trix Pe ppa s Hix .Crow .
Sr.No. Time Avg. %R SD 0 0 0 0 0
1 0 0.000 0.000 0.000 0.000 - 0.000
2 1 0.097 0.001 0.001 0.017 0.000 0.001
3 2 0.150 0.009 0.009 0.029 0.003 0.009
4 3 0.349 0.000 0.000 0.002 0.000 0.000
5 4 0.504 0.000 0.000 0.003 0.001 0.000
6 5 0.660 0.002 0.002 0.024 0.001 0.002

CONCLUSION: reference batch, do not show much difference in

The Tablet of the Aspirin is Prepared by the Direct
Compression Process. the maximum drug release in four
hours was found to be in batch F1, which is far less than
the release of drug in reference tablet All these values
have been tabulated below in Table 3. The in-
vitrorelease profile of the drug from the tablets was
major governing criteria to decide the commercially used
binder (starch as in reference batch) is a good binding
agent. The release profile for the drug was taken for a
period of four hours which can best be depicted by graph
between percentage drug release and time Batch
F2contain.
DISCUSSION:
Physical properties of granules: Parameters studied
were the angle of repose, carr’s index, Hauser's ratio,
bulk density, tapped density, and bulkiness. Lesser
bulkiness showed the ease of compaction into tablet 3.
dosage form over conventional dosage forms containing
binders such as starch. As per the results of physical
characterization batch from F1 and F2. especially the 4.
micromeritics studies and granule flow property. By
adding the lubricant in the combination.
Kinetic profile of drug release:
By the using the lubricant in the combination in this
formulation. F2 Formulation was found to be best under
the all pharmaceutical parameters and our F2
formulation follows Zero Order Kinetics Mechanism.
REFERENCES:
1. al Gohary OM, el Din K, el Tahir H. Formulation of aspirin-
magaldrate double-layer tablets: in vitro evaluation and
cytoprotective activity in rats. Bollettino Chimicopharmaceutics.
1996;135(7):421-8.
2. Abe T, Yanagihara Y, Uchino T, Oriyama T, Komatsu M,
Nakajima K, et al. Evaluation of the pharmaceutical characteristics
of various enteric-coated aspirin tablets under different storage
conditions. Chemical & Pharmaceutical Bulletin. 2014;62(7):617-
26.
Bird HA, Dixon JS, Finney PL, Leatham PA, Lowe JR, Pickup
ME, et al. A clinical and biochemical evaluation of Clozic, a novel
disease modifying drug in rheumatoid arthritis. Clinical and
Experimental Rheumatology. 1983;1(2):93-9.
Blythe RH, Grass GM, Macdonnell DR. The formulation and
evaluation of enteric coated aspirin tablets. American Journal of

2937
 Research J. Pharm. and Tech. 10(9): September 2017

Pharmacy and the Sciences Supporting Public Health.

1959;131(6):206-16.
5. Colombo P, Conte U, Caramella C, Geddo M, La Manna A.
Disintegrating force as a new formulation parameter. Journal of
Pharmaceutical Sciences. 1984;73(5):701-5.
6. Cooper SA, Voelker M. Evaluation of onset of pain relief from
micronized aspirin in a dental pain model.
Inflammopharmacology. 2012;20(4):233-42.
7. Dhaliwal HS, Sloan P, Arkinstall WW, Thirlwell MP, Babul N,
Harsanyi Z, et al. Randomized evaluation of controlled-release
codeine and placebo in chronic cancer pain. Journal of Pain and
Symptom Management. 1995;10(8):612-23.
8. Gordin A, Karppinen I, Holttinen K. Comparison of slow-release
indomethacin and diflunisal in patients with arthrosis. Current
Medical Research and Opinion. 1984;9(4):275-9.
9. Hawkey C, Burnett I, Gold MS, Garsed K, Stevenson D, Mannath
J, et al. Endoscopic evaluation of the gastro-duodenal tolerance of
short-term analgesic treatment with 25 mg diclofenac-K liquid
capsules. Alimentary Pharmacology & Therapeutics.
2012;35(7):819-27.
10. Taday PF. Applications of terahertz spectroscopy to
pharmaceutical sciences. Philosophical transactions Series A,
Mathematical, physical, and engineering sciences.
2004;362(1815):351-63; Discussion 63-4.
11. Taylor M, Elhissi AM. Predicting the physical properties of tablets
from ATR-FTIR spectra using partial least squares regression.
Pharmaceutical Development and Technology. 2011;16(2):110-7.
12. Gamal W, Fahmy RH, Mohamed MI. Development of novel
amisulpride-loaded solid self-nanoemulsifying tablets: preparation
and pharmacokinetic evaluation in rabbits. Drug Development and
Industrial Pharmacy. 2017:1-29.
13. Tawfeek HM, Faisal W, Soliman GM. Enalapril maleate orally
disintegrating tablets: Tableting and in vivo evaluation in
hypertensive rats. Pharmaceutical Development and Technology.
2017:1-25.
14. Jaffary SR, Ahmed SW, Shakeel S, Asif HM, Usmanghani K. In
vitro antioxidant and reducing capability of weight loss tablet
formulation. Pakistan Journal of Pharmaceutical Sciences.
2016;29(5(Suppl)):1749-53.
15. Mori D, Makwana J, Parmar R, Patel K, Chavda J. Formulation,
evaluation and optimization of the felodipine nanosuspension to be
used for direct compression to tablet for in vitro dissolution
enhancement. Pakistan Journal of Pharmaceutical Sciences.
2016;29(6):1927-36.

2938