International Journal of Trend in Scientific Research and Development (IJTSRD)

Volume 4 Issue 1, December 2019 Available Online: www.ijtsrd.com e-ISSN: 2456 – 6470

Formulation and Evaluation of

Amlodipine Fast Dissolving Tablets
Aparna. P,
P Dr. Subash Chandran M. P, Remya S B
Department off Pharmaceutics, Sree Krishna College of Pharmacy and Research Centre,
Parassala, Thiruvananthapuram, Kerla, India

ABSTRACT paper Aparna. P | Dr.

How to cite this paper:
Fast dissolving tablet is a new era for successful development of controlled Subash Chandran M. P | Remya S B
release formulation along with various features to provide successful drug "Formulation and Evaluation of
delivery. In the present study, an attempt was made to design and evaluate Amlodipine Fast Dissolving Tablets"
fast dissolving tablets
lets of Amlodipine besylate, which is used commonly for Published in
the treatment of angina pectoris. The tablets were prepared by direct International
compression method followed by sublimation method using super Journal of Trend in
disintegrants sodium starch glycolate, crosspovidone and croscarmellose
croscarmell Scientific Research
sodium. The prepared powder blends were evaluated for preformulation and Development
parameters. The tablets were evaluated for thickness, hardness, weight (ijtsrd), ISSN: 2456-
2456
variation, drug content uniformity, friability and in vitro drug release 6470, Volume-4
Volume | IJTSRD29563
studies. In vitro drug release studies were performed by using USP type II Issue-1,
1, December
apparatus (paddle method) at 50 rpm in 900 ml of 0.1N HCl as dissolution 2019,
019, pp.428
pp.428-436, URL:
medium for 30 minutes at 37±0.5°C. The formulation F9 containing https://www.ijtsrd.com/papers/ijtsrd2
Croscarmellose sodium (7%) showed better disintegration and dissolution 9563.pdf
up to 30 minutes.
inutes. Hence, formulation F9 was considered as optimized
formulation which showed the best drug release profile up to 30 minutes. Copyright © 2019 by author(s) and
The results of mathematical model fitting of data obtained indicated that, International Journal of Trend in
the best fit model in all the cases the release was
wa found to be by diffusion Scientific Research and Development
and fickian release. The results of FTIR analysis showed that there was no Journal. This is an Open Access
A article
physical and chemical interaction between drug and other excipients. The distributed under
study indicates that the fast dissolving tablets of Amlodipine besylate can the terms of the
effectively
tively reduce the adverse effects and frequency of administration of Creative Commons
the drug. Attribution License (CC BY 4.0)
(http://creativecommons.org/licenses/
http://creativecommons.org/licenses/
KEYWORDS: Amlodipine besylate; Superdisintegrants; Crospovidone; Sodium by/4.0)
starch glycolate; Cross carmellose sodium; Direct compression; Sublimation
method; FDT; Evaluation parameters.
INRODUCTION
Tablet is still most popular conventional dosage forms bioavailability of drug is significantly more than those
existing today because of ease of self administration, observed from conventional tablets dosage form. The time
compact in nature, easy to manufacture and it can be for disintegration of fast disintegrating tablets is generally
deliver in accurate dose. One important drawback of considered to be less than one minute. The fast dissolving
conventional dosage forms is the difficulty in swallowing solid dosage
age form turns into a soft paste or liquid form for
(dysphagia) or chewing in some patients particularly
partic easy swallowing, and thus it is free of risk of choking2.
pediatric and geriatric patients. United States Food and
drug administration (FDA) defined fast dissolving tablet Angina pectoris, commonly known as angina, is chest pain
(FDT) as “a solid dosage form containing medicinal due to ischemia of the heart muscle. Amlodipine besylate
substance or active ingredient which disintegrate rapidly is a calcium channel blocker, chemically it is 3-Ethyl-5-
usually within a matter of seconds when placed upon the methyl (±) -2-[(2-aminoethoxy)
aminoethoxy) methyl] -4-(2-
tongue.” Fast dissolving tablets are also known as mouth-
mouth chlorophenyl) -1,4 dihydro-6-methyl-3,5-
dissolving tablets, melt-in
in mouth tablets, orodispersible pyridinedicarboxylate, monobenzene sulphonate3.
tablets, rapimelts, porous tablets, quick dissolving tablet.
tablet Amlodipine besylate is a white crystalline powder with a
Fast dissolving tablets dissolve or disintegrate in
i the oral molecularr weight of 567.1. Its empirical formula is
cavity without the need of water1. Most fast dissolving C20H25CIN2O5.C6H6O3S. Amlodipine is a dihydropyridine
tablets must include substances to mask the bitter taste of calcium antagonist (calcium ion antagonist or slow- slow
the active ingredient. This masked active ingredient is channel blocker) that inhibits the transmembrane influx of
then swallowed by the patient's saliva along with the calcium ions into vascular smooth muscle and cardiaccar
soluble and insoluble excipients. It has been concluded muscle. Like other calcium channel blockers, amlodipine
that faster the dissolution, faster the absorption (only the acts by relaxing the smooth muscle in the arterial wall,
unionized form of drug) and onset of action. Some drugs decreasing total peripheral resistance and hence reducing
are absorbed from the oral cavity, pharynx and esophagus blood pressure; in angina it increases blood flow to the
as the saliva passes down into the stomach. Thus T the heart muscle4.

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29563 | Volume – 4 | Issue – 1 | November--December 2019 Page 428
 International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470
The basic approach in development of FDT is the use of compressed, and with tablet weight, while with a constant
super disintegrants like cross povidone (2-5%), sodium die fill, thickness varies with variations in compressive
starch glycolate (2-8%), crosscarmellose sodium which load. Tablet thickness should be controlled within ± 5 %
provide instantaneous disintegration of tablet after variation of a standard value. Any variation in tablet
putting on tongue their by release the drug in saliva5. thickness within a particular lot of tablets or between
manufacture’s lots should not be apparent to the unaided
The other ingredients are micro crystalline cellulose as eye of consumer acceptance of the product. In addition,
tablet disintegrant, mannitol as diluent, talc and thickness must be controlled to facilitate packing.
magnesium stearate as lubricant, and camphor as Thickness of tablets indicates the strength to withstand
sublimating agent which increases the porosity of the compression force applied during manufacturing process.
tablet6. Direct compression was used for the preparation Thickness of tablets was measured by verniercalliper. It is
of FDT7. The technologies used for manufacturing fast expressed in millimetre.
dissolving tablets are freeze-drying, spray-drying, tablet
moulding, sublimation, sugar-based excipients, tablet Weight variation10
compression, and disintegration addition8. With a tablet designed to contain a specific amount of drug
in a specific amount of tablet formula, the weight of the
MATERIALS AND METHODS tablet being made is routinely measured to ensure that a
Materials tablet contains the proper amount of drug. The weight
Amlodipine Besylate was purchased from Yarrowchem variation test is done by weighing 10 tablets individually
Products, Mumbai, India. Crosspovidone, Sodium starch and calculating the average weight, and comparing the
glycolate, Crosscarmellose sodium, Mannitol, Micro individual tablet’s weight to the average. The limits for
crystalline cellulose, Camphor, Magnesium stearate and weight variation are given in the table 1.
talc all of them are purchased from Yarrowchem Products, Maximum percentage
Mumbai, India. All the excipient and reagents used are S1. No Average Weight
difference allowed
analytical grade. 1 130 or less 10
2 130-324 7.5
Methods
3 More than 324 5
Preparation of FDT of Amlodipine besylate
Table1: Weight variation range
Amlodipine besylate FDTs were prepared by direct
compression method followed by sublimation method. Hardness/Crushing strength11
The superdisintegrants such as Crosspovidone,Sodium Tablet requires a certain amount of strength or hardness
starch glycolate,Cros carmellose sodium used in varying and resistance to friability, to withstand mechanical
concentrations (3,5,7%). In this study camphor is used as shocks of handling in manufacture, packaging and
a sublimating agent. All the ingredients were passed shipping. The hardness can be tested using Monsanto
through the sieve no 60. The drug/polymer mixture was hardness tester or Pfizer. Here Monsanto was used. The
prepared by homogeneously mixing the Croscarmellose tablet to be tested was held between a fixed and a moving
sodium, crospovidone, sodium starch glycolate, jaw of Monsanto Hardness Tester. The force applied to the
microcrystalline cellulose, mannitol and Amlodipine. All edge of the tablet was gradually increased by moving the
the ingredients of the fast dissolving tablet of amlodipine screw knob forward until the tablet breaks. The reading
were weighed, sifted and mixed in mortar with the help of was noted from the scale which indicates the pressure
pestel, and finally magnesium stearate and talc were required to break the tablet. The hardness of a tablet
added as lubricating agent and camphor were added as depends on the weight of the material used, space
sublimating agent. The 150 mg mixture was then between the upper and lower punches at the time of
compressed using an 8 mm punch in a single stroke on compression and pressure applied during compression.
single punch tablet machine. Each tablet weighed 150 mg. The hardness also depends on the nature and quantity of
The force of compression was adjusted so that hardness of recipients used during formulation. If the finished tablet is
all the prepared tablets ranges from 2-4 kg/cm2. Camphor too hard, it may not disintegrate in the required period of
was sublimated in vacuum at 80°c for 30 minutes after time and if the tablet is too soft it may not withstand the
preparation of tablets (Fig: 1). handing during packing and transporting.
EVALUATION OF FAST DISSOLVING TABLET Friability9
General Appearance Tablet’s hardness is not an absolute indicator of strength
The general appearance of a tablet, its visual identity and since in some formulations, when compressed into very
overall elegance, is essential for consumer acceptance. The hard tablets, tend to cap on attrition, losing their crown
control of the general appearance of a tablet includes the portions. Friability test can be performed to evaluate the
measurements of a number of attributes such as a tablets ability of the tablets to withstand abrasion in packing,
size, shape, colour, presence or absence of an odour, taste, handling and transporting. The Friabulator consists of a
of any identifying markings. The prepared tablet was plastic chamber divided into two parts and revolves at 25
evaluated for its colour, shape, odor, taste, surface etc. rpm. A fixed number of tablets are weighed, placed in the
tumbling chamber and rotated for four minutes of 100
Thickness9 revolutions. During each revolution the tablets fall from a
The thickness of a tablet is the only dimensional variable distance of six inches to undergo shock. After 100
related to the process. At a constant compressive load, revolutions the tablets are again weighed. The loss in
tablet thickness varies with change in die fill, with particle weight indicates the friability. The acceptable limits of
size distribution and packing of the particle mix being weight loss should not be more than 0.8% t.

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 International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470
The friability (f) is given by of the solid dosage form into granules, deaggregation of

 granules to yield fine particles and dissolution of drug
f = 1- X 100

from the fine particles into solution.
Where, Drug dissolution is a multistep process involving
wo = initial weight of the sample before friability test heterogenous reactions at solid-liquid phase boundaries.
w = weight of the samples after friability test The heterogenous reactions that constitute the overall
mass transfer process are considered to take place in two
Drug content9 steps
The potency of tablet is expressed in terms of grams, 1. Convective transport of the soluble solid through
milligrams or micrograms of drug per tablet and is given hydrodynamic boundary layers surrounding solid-
as the label strength of the product. So to evaluate the liquid interphase to the bulk phase
tablet’s potency, the amount of drug per tablet needs to be 2. A reaction at the solid –liquid interphase(Interfacial
monitored from tablet to tablet, and batch to batch. For transport)
the drug content uniformity test ten tablets were weighed
and pulverised to a fine powder.A quantity of powder Procedure
equivalent to 5 mg of amlodipine was taken and dissolved Apparatus : USP Type 2 (paddle)
in suitable quantity of pH 1.2 solutions and liquid was Agitation speed (rpm) : 50
filtered using whatman filter paper and diluted. The Medium : 0.1 N HCl
amlodipine content was determined by measuring the Temperature : 37 ± 0.5 ̊ C
absorbance at 239 nm using UV spectrophotometer. Time : 5, 10, 15, 20, 25, 30 minutes
Wavelength : 239 nm
Wetting Time12
The wetting time of the tablets can be measured by using Steps
five circular tissue papers of 10 cm diameter are placed in 900 ml of 0.1 N HCl was taken in the basket. Temperature
a petridish with a 10 cm diameter. 10 mL of water- was maintained at 37 ± 5 ̊ C. One tablet was placed in the
containing amaranth a water soluble dye is added to basket. The basket was rotated at 50 rpm. 1 ml of sample
petridish. A tablet is carefully placed on the surface of the from each basket was withdrawn at the intervals of 5, 10,
tissue paper. The time required for water to reach upper 15, 20, 25, 30 minutes. Replace the basket with equal
surface of the tablet is noted as a wetting time. volume of 0.1 N HCl .The samples withdrawn was filtered
and diluted to 10 ml with 0.1 N HCl. The absorbance of
Water Absorption Ratio12 these solutions is measured at 239 nm. The amount and
A piece of tissue paper folded twice was placed in a small percentage of drug release can be calculated from the
petri dish containing 6 ml of water. A tablet was put on the given formula.
tissue paper and allowed to completely wet. The wetted
tablet was then weighted. Water absorption ratio, R was  
 
determined using following equation.  × ℎ  × 

R = 100 × Wa – Wb/Wa =
1000
 
 
Where, Wa = Weight of tablet after water absorption % 
  = × 100
 
Wb = Weight of tablet before water absorption.
Kinetic study14
Disintegration9
Dissolution profile modeling
A generally accepted fact is that for a drug to be readily
There are several linear and non-linear kinetic models to
available in the body it must be in solution form. For most
describe release mechanisms and to compare test and
tablets, the first important step towards dissolution is the
reference dissolution profiles are as follows:
breakdown of tablet into smaller particles or granules.
This process is known as disintegration. Disintegration is
Zero order kinetics
still be used as a tool of quality control of tablets and
Drug dissolution from pharmaceutical dosage forms that
capsules.
do not disaggregate and release the drug slowly (assuming
that area does not change and no equilibrium conditions
Procedure
are obtained) can be represented by the following
The test was carried out on 6 tablets using Tablet
equation:
disintegration tester. Distilled water at 37°C ± 2°C was
W0 – Wt = K0t
used as a disintegration media and the time in second
taken for complete disintegration of the tablet with no
Where W0 is the initial amount of drug in the
palable mass remaining in the apparatus was measured in
pharmaceutical dosage form, Wt is the amount of drug in
seconds.
the pharmaceutical dosage form at time t and k is
Dissolution13 proportionality constant.
Dissolution is a physiochemical process by which a solid
substance enters the solvent phase to yield a solution. Dividing this equation by W0 and simplifying:
Dissolution (release of drug from the dosage form) is a key ft = k0t
prerequisite for any orally administered drug to be Where ft = 1 – (Wt / W0 ) and ft represents the fraction of
systemically effective .In case of oral drug products, the drug dissolved in time t and k0 the apparent dissolution
release properties are mainly influenced by disintegration rate constant or zero order release constant

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 International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470
First order kinetics
This type of model to analyze drug dissolution study was first proposed by Gibaldi and Feldman and later by Wagner. The
relation expressing this model:
Log Qt = Log Q0 + K1t/2.303

Where Qt is the amount of drug released in time t, Q0 is initial amount of drug in the solution and K1 is the first order
release rate constant.

Korsmeyer Peppas model

Korsmeyer developed a simple semi empirical model, relating exponentially the drug release to the elapsed time (t).
Qt/Qα = Kktn

Where Kk is a constant incorporating structural and geometric characteristic of the drug dosage form and n is the release
exponent, indicative of the drug release mechanism as shown in the table 2:

Table2: Drug transport mechanism

Sl. No Release exponent(n) Drug transport mechanism Rate as a function of time
1 0.5 Fickian diffusion t-.0.5
2 0.5 ˂n ˂ 1.0 Anomalous transport tn-1
3 1.0 Case II transport Zero order release
4 Higher than 1.0 Super case II transport tn-1

The Release exponent can be obtained from the slope and the Constant (Kk) obtained from the intercept of the graphical
relation between logarithmic versions of left side of the equation versus log t.

Higuchi Model
Qt = KHt1/2
Where Qt = the amount of drug released at time t and
KH = the Higuchi release rate;
This is the most widely used model to describe drug release from pharmaceutical matrices. A linear relationship with the
square root of time versus the concentration indicates that the drug release follows strict Fickian diffusion.

RESULTS AND DISCUSSION

The powder blend for all formulation containing various concentration of Crossspovidone (3,5,7%), Sodium starch
glycolate (3,5,7%) and cross carmellose sodium (3,5,7%) as superdisintegrant was prepared shown in the Table 3, and
then the FTIR studies were carried out on the basis of as the method specified(Fig.7-10), FTIR spectrum of drug shows the
prominent peaks with respect to the functional groups. The FTIR spectrum of physical mixture of drug with polymer and
drug with excipient concludes that there is no significant interaction between the drug, polymer and excipients. In the
spectrum of drug-polymer mixture, the characteristic peak of drug was not altered. The soluble diluents, such as mannitol
and microcrystalline cellulose were selected as diluents considering its advantages in terms of easy availability and
negative heat of dissolution. Post formulation studies of the formulated batches are shown in the Table 5 and 6. From the
physical evaluation of all the batches formulated shown in Table 4, it was concluded that the tablets of all the batches had
desirable physical properties. Hardness varies from 2.8 -3.7 Kg/cm2. The thickness varies from 2.9-3.3 mm. The friability
was varies from 0.40 -0.72 %, which indicates that all the batches had sufficient mechanical strength to withstand
mechanical abrasion. All batches of formulation passes the weight variation test as per the limits prescribed in IP. The
wetting time (Fig: 2) of all the batches were also considerably reduced in tablets. A tablet is carefully placed on the surface
of the tissue paper. The time required for water to reach upper surface of the tablet is noted as a wetting time. It is clear
that the wetting time varies depend on the concentration of the superdisintegrants used for the study. The drug content
uniformity of all the batches was in the limit of 95 - 98 %. The water absorption ratio of all the batches were tested by the
method it is clear that the order of swelling observed in these polymers could indicate the rates at which the preparation
are able to absorbed water and swell. Maximum liquid uptake and swelling polymers were achieved after 2 -8 minutes.
The swelling index was calculated with respect to time .As the time increases, the swelling index was increased because
weight gain by the tablet was increased proportionally with rate of hydration. Later it decreased due to the dissolution of
outer most gelled layer of tablet into dissolution medium. Batches F1 to F9 showed good mechanical integrity, but the
disintegration time was in the range of 15 to 40 seconds. The results shown that sublimation of camphor from tablets
resulted in faster disintegration. In vitro release studies were carried out using USP Type 2 tablet dissolution test
apparatus paddle method at 37±0.5 °C, taking 900 ml of pH-1.2 dissolution medium. Speed of rotation of the paddle was
set at 50 rpm. Aliquots of 1 ml were withdrawn after 5, 10, 15, 20, 25, 30 min and analyzed spectrophotometrically at 239
nm. The percentage drug release of formulations F1-F3 formulated with different concentrations of same superdisintegrant
crosspovidone showed the drug release 79.09 %, 81.90 % and 82.09 % respectively at the end of 30 minutes(Fig:3). From
formulations F4-F6 with another superdisintegrant sodium starch glycolate were showed 82.29 %, 83.60 % and 86.29 %
respectively at the end of 30 minutes(Fig:4). From formulations F7- F9 formulated with superdisintegrant croscarmellose
sodium were showed the results as 89.10 %, 91.19 % and 92.29 % respectively at the end of 30 minutes(Fig:5). F9 shows
the percentage drug release of 92.29 % at the end of 30 minutes. So F9 selected as the optimized formulation in this study.

@ IJTSRD | Unique Paper ID – IJTSRD29563 | Volume – 4 | Issue – 1 | November-December 2019 Page 431
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The dissolution profile of most satisfactory formulation F9 was fitted to zero order, first order, Higuchi model, Korsmeyer-
Peppas model and Hixson-Crowell model to ascertain the kinetic modeling of the drug release(Fig:6). The kinetic
treatment of the drug release data of F9 followed first order drug release and Korsmeyer-Peppas profile with R2 values
0.989 and 0.993 respectively(Table:7&8). It indicated that drug release was dissolution controlled and directly
proportional to log cumulative percentage drug release.

Fig:1: Fast dissolving tablets of Amlodipine.

Fig:2: Before and after wetting time of FDTs

F1-F3 F4-F6
100 100
Percentage drug release(%)

Percentage drug release(%)

80 80
60 60
F1 F4
40 40
F2 F5
20 20
F3 F6
0 0
0 10 20 30 40 0 10 20 30 40
Time(min) Time(min)

Fig: 3: Dissolution profile of Formulations F1-F3. Fig: 4: Dissolution profile of Formulations F4-F6.

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 International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470

F7-F9
100

Percentage drug release(%)

80
60
F7
40
F8
20
F9
0
0 10 20 30 40
Time(min)

Fig: 5: Dissolution profile of Formulations F7-F9.

F7

Zero order First order y = -0.0356x +

Log Cumulative % drug

120 y = 2.6784x + 23.875 2.500 1.9464
cumulative %drug release

100 R² = 0.8186 R² = 0.9892

2.000

remaining
80
1.500
60 Zero order First order
1.000
40
20 Linear (Zero 0.500 Linear (First
order) order)
0 0.000
0 20 40 0 20 40
Time (hrs.) time (hrs.)

Kors-peppas
peppas
100 y = 61.773x + 150
y = 16.835x + 5.7992
cumulative %drug released
log cumulative %drug release

80 1.8272 R² = 0.9792
60 R² = 0.9939 100
Kors-peppas Higuchi
40
50
20 Linear (Kors- Linear
0 peppas) 0 (Higuchi)
0.000 1.000 2.000 0.000 2.000 4.000 6.000
log time SQRT of Time Higuchi

Hixson Crowell
3.000
2.500 y = 0.0833x + 0.3207
CBR(Wo)-CBR(Wt)

R² = 0.96
2.000
1.500 hixson
1.000 Linear (hixson)
0.500
0.000
0 20 40
Time (hrs.)
Fig: 6: Kinetic study of formulation F9

@ IJTSRD | Unique Paper ID – IJTSRD29563

29563 | Volume – 4 | Issue – 1 | November--December 2019 Page 433
 20
40
60
80

0
100
120

%T

@ IJTSRD
-20
0
100
120

20
40
60
80
%T
20
40
60
80

-20
0
100
120

%T
0
15
30
45
60
75
90
105

%T

|
4000
A2
4000
4000
4000

3750
3750
3750
3750

AMLO+ ssg
AMLO+ ssg
3595.31
3595.31

AMLO+ CCS
3552.88
3552.88
3512.37
3512.37

3500
3500
3500
3500
3
367
.71
3367.71
3367.71 3367.71

3
240
.41
3230.77
3230.77 3234.62

3250
3250
3250
3250
3
061
.03
305
9.10
3059.10 3057.17
2987.74
2987.74 2987.74
2
947
.23
2949.16

3000
2949.16 2947.23

3000
2
916
.37

3000
3000

2910.58
2910.58 2910.58
2
850
.79

Unique Paper ID – IJTSRD29563

2750
2750
2750

2750
2
648
.26

|
2644.41

2
513
.25 2507.4
6 2509.39
2507.46

2500

2500
2500

2500

2250
2250

2250
2250

2000
2000

2000

2000

Volume – 4 | Issue – 1
1
689
.64 1689.64
1
689.64 1689.64
1
637
.56 1637.56

Fig:10: FTIR of Drug + Excipients

|
1633.7
1
1750

1750
1750
1633.71

1750
1
602
.85 1602.85
1604.77 1604.77
1
575
.84 1575.84
1577.77 1577.77

Fig:8 FTIR of Amlodipine +Crosspovidone

1
537
.27 1529.55
1539.20 1539.20
1
475
.54
1481.33
1479.40 1479.40
1500

1500
1500
1458.18

1500
1
463
.97 1379.10 1379.10
Fig:7: FTIR of Amlodipine +Croscarmellose sodium

Fig:9: FTIR of Amlodipine +Sodium starch glycolate

1377.17
1
379
.10 1346.3
1 1346.31
1344.38
1
344
.38 1296.1
6 1296.16
1288.45
1
307
.74 1288.45 1288.45
1250

1250
1199.72
1250

1
286
.52

1250
1199.72 1199.72
1111.00
1
236
.37 1111.0
0 1111.00
1039.63
1
201
.65
100
4.91 1004.91 1008.77
1
107
.14
1000

923.90

1000
1000

1
039
.63 873
.75 873.75

1000
898.83
840
.96 840.96
1
012
.63
875.68
750.31 750.31
9
33.5
5
833.25
7
34.88 734.88
8
75.6
8
750

736.81

750
750

6
94.37 694.37
7
58.0
2

750

November-December 2019
698.23
6
59.66 659.66
7
38.7
4
678.94
615.29 615.29
6
94.3
7
659.66
563.21 563.21
6
65.4
4
500

613.36
500

500
6
17.2
2 408.91 408.91
567.07

500
1/cm

5
69.0
0
1/cm

1/cm

1/cm
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 International Journal of Trend in Scientific Research and Development (IJTSRD) @ www.ijtsrd.com eISSN: 2456-6470
Composition of Fast dissolving tablet
INGREDIENTS F1 F2 F3 F4 F5 F6 F7 F8 F9
Amlodipine besylate 10 10 10 10 10 10 10 10 10
Crosspovidone 3 5 7 - - - - - -
Sodium starch glycolate - - - 3 5 7 - - -
Cross carmellose sodium - - - - - - 3 5 7
Mannitol 100 100 100 100 100 100 100 100 100
Microcrystalline cellulose 25 23 21 25 23 21 25 23 21
Camphor 10 10 10 10 10 10 10 10 10
Magnesium stearate 1 1 1 1 1 1 1 1 1
Talc 1 1 1 1 1 1 1 1 1
Total weight(mg) 150 150 150 150 150 150 150 150 150
Table: 3 Formulation ingredients

Physical evaluation
Sl. No Formulation Weight variation (mg) Thickness (mm)* Hardness (Kg/cm2)* Friability (%)*
1 F1 149±0.042 3.2±0.042 3.5±0.021 0.46±0.021
2 F2 149±0.034 2.95±0.015 3.2±0.042 0.48±0.042
3 F3 151±0.042 3.1±0.041 2.8±0.031 0.66±0.026
4 F4 149±0.026 3.0±0.036 3.6±0.052 0.67±0.042
5 F5 151±0.029 3.3±0.021 2.9±0.012 0.58±0.042
6 F6 152±0.021 3.1±0.042 3.3±0.030 0.72±0.034
7 F7 149±0.036 2.9±0.052 3.1±0.016 0.51±0.036
8 F8 148±0.042 3.0±0.021 3.5±0.040 0.40±0.021
9 F9 151±0.021 3.15±0.034 3.7±0.038 0.65±0.029
Table4: Physical evaluation of tablet
*Average of three determinations
Sl. No Formulation Wetting Time (Sec) Drug content (%) Disintegration Time(sec)
1 F1 20 96.28 27
2 F2 19 97.41 23
3 F3 23 96.85 19
4 F4 18 97.12 33
5 F5 17 96.30 25
6 F6 20 96.78 28
7 F7 21 97.14 19
8 F8 18 97.12 18
9 F9 15 97.88 15
Table5: Wetting time, drug content and disintegration time of tablets

Sl. No Formulation % swelling (Time in Min)

2 4 6 8
1 F1 92.06 94.52 95.56 93.61
2 F2 65.28 73.75 84.26 83.40
3 F3 67.58 75.89 94.56 92.43
4 F4 67.19 76.05 99.65 93.42
5 F5 69.12 87.79 108.32 103.85
6 F6 75.89 98.34 101.65 95.41
7 F7 75.98 89.31 109.36 105.45
8 F8 97.15 104.67 112.26 105.28
9 F9 96.06 101.45 107.35 102.19
Table6: Water absorption study of tablet

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log
cumulative Square log Cumu % Cube Root
Time % drug log Cumu % % Drug Wo-
% drug root drug of % drug
(Hr) remaining time drug released Wt
released time remainining RemainingWt
released
0 0 100 0.000 2.000 0.000 0.000 100 4.642 0.000
5 50.09 49.91 2.236 1.698 0.699 1.700 50.09 3.682 0.960
10 61.20 38.8 3.162 1.589 1.000 1.787 11.11 3.385 1.257
15 74.39 25.61 3.873 1.408 1.176 1.872 13.19 2.948 1.694
20 81.29 18.71 4.472 1.272 1.301 1.910 6.9 2.655 1.987
25 89.10 10.9 5.000 1.037 1.398 1.950 7.81 2.217 2.425
30 92.29 7.71 5.477 0.887 1.477 1.965 3.19 1.976 2.666
Table 7: Kinetic analysis data of F9

FORMULATION Kinetic Models

F9 Zero order First order Kors Peppas Plot Hixon crowell Higuchi
R2 value 0.818 0.989 0.993 0.960 0.979
Table8: Regression values of kinetic models

CONCLUSION
Fast dissolving tablets of Amlodipine besylate was [7] Amborn J, Tiger V. Apparatus for handling and
prepared by direct compression and followed by packaging friable tablets. US Patent; 2001: 6,311,462.
sublimation method using three different
[8] Ujjwal Nautiyal, Satinderjeet Singh, Ramandeep
superdisintegrants such as Croscarmellose Sodium,
Singh, Gopal, Satinder Kakar. Fast Dissolving Tablets
Crospovidone and Sodium Starch Glycolate with other
as A Novel Boon, A Review. J of Pharma Chemical and
standard excipients. FTIR studies showed that there was
Biological Sci. 2014; 2(1): 05-26.
no marked interaction between fast dissolving tablets and
superdisintegrants. In vitro drug release from the tablets [9] United States Pharmacopeia 30,NF,Asian
shows significantly improved drug dissolution. Optimized edition.(1174);(2007) :643
formulation F9 showed a drug release of 92.29 % and
[10] L. Lachman, H A. Liberman and J. l. kaing, The Theory
showed the minimum disintegration time was 15 seconds.
and practice of Industrial Pharmacy,3rd Edition,
Varghese Publishing House. 1987: 297-299.
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[4] Product monograph. Amlodipine besylate. Pfizer
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Cosmetology.2011 ;( 1): 4.
[5] Rowe RC, Sheskey PJ, Owen SC. Hand book of
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