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Priyanka D et al. Int J Trends in Pharm & Life Sci. 2017: 3(4); 55-66. 55

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International Journal of Trends in Pharmacy and Life Sciences Vol. 3, Issue: 4, 2017: 55-66.

FORMULATION AND IN VITRO EVALUATION OF LIQUI SOLID 5

COMPACT OF FELODIPINE Donthula Priyanka*, L. Matsyagiri, K.Pavan Kumar

Department of Pharmaceutics, RBVRR Women’s College of Pharmacy, Affiliated to Osmania University- Hyd, Barkatpura, Hyderabad. Telangana, India

E.Mail: [email protected]

ABSTRACT

The main aim of present work, Formulation and in vitro evaluation of liquid solid compact of

Felodipine is to increase Bio-availability using different ratios of co solvents. In this technique actual

mechanism of increasing solubility is the wetting of drug particle by using cosolvent and increase in surface

area of the drug particle by preparing in the form of Liquisolid compact. The study shows that the solubility

of Felodipine is very less in water and hence the various non-volatile solvents having more solubility than

the water are used among them tween-80, PEG, glycerol, propylene glycol have shows good solubility of

Felodipine in water.among them propylene glycol have shown increased solubility of Felodipine, Hence

propylene glycol is selected for the preparation of liquisolid compacts. Microcrystalline cellulose and

aerosil was selected as carrier and coating material. Then Cros-caramellose sodium was added as the

superdisintegrant and magnesium sterate acts as Glidant in the formulation. The FTIR and DSC spectral

studies showed no interaction of drug with polymer and excipients. F5 formulation has been selected as the

optimized formulation among all the other formulation and percentage drug release for F5 Formulation was

98.36 % at the end of 60 mins. The Optimized formulation F5 was kept in Kinetic release models; it follows

Higuchi model and its regression value R2 Was 0.987. Finally the optimized formulation (F5) was kept for

stability studies For 15 days, 30 days, 45 days. There is no significant difference in the values obtained

before and after stability of final optimized formulation.

Key Words: Cosolvents, Felodipine, Free flowing, Liquisolid technique, Wetting

*Corresponding Author:

D. Priyanka,

RBVRR Women’s College of Pharmacy,

Affiliated to Osmania University-Hyd, Barkatpura,

Hyderabad. Telangana, India.

Tel.: +91-9966463776;

INTRODUCTION

The solubility is defined as a maximum quantity of solute that can dissolve in a certain quantity of

solvent or quantity of solution at a specified temperature. Almost More than 90% drugs are orally

administered and their Drug absorption, bioavailability, pharmacokinetic profile highly dependent on

solubility of that compound in aqueous medium. More than 90 % of drugs are approved since 1995 have

poor solubility. It is estimated that 40 % of active new chemical entities (NCEs) identified in combinatorial

screening programs employed by many pharmaceutical companies are poorly water soluble. Low aqueous

solubility is the major problem encountered in formulation development of new chemical entities as well a, s

for the generic development. The insufficient dissolution rate of the drug is the limiting factor in the oral

bioavailability of poorly water soluble compounds. These poorly water soluble drugs are allied with slow

drug absorption leading to inadequate and variable bioavailability and gastrointestinal mucosal toxicity of

drugs. Poor water soluble drugs belong to BCS class II and class IV. [1-9].

Advantages

• Increased bioavailability of poorly water soluble drugs.

• Less production cost compared to soft gelatin capsules.

Received: 20/04/2017

Revised: 18/0/5/2017

Accepted: 25/05/2017

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• Suitable for industrial production.

• Drug release can be modified by changing suitable ingredients.

• Rapid release liquisolid tablets (or) capsules exhibit enhanced in vitro & in vivo drug release compared to

their commercial products.

• Sustained released tablets (or) capsules of water insoluble drugs exhibit zero order release.

• It can be used to formulate liquid medications.

• Used in controlled drug delivery.

Disadvantages

• Liquisolid system requires low drug loading capacities.

• Requires more efficient excipients and it should provide faster drug release with smaller tablet size.

• Higher amounts of carrier and coating materials are required [10].

Limitations

• Not suitable for formulation of high dose water insoluble drugs.

• If more amounts of carrier is added it increase the flow properties of powder, it may increases the tablet

weight too, hence it is difficult to swallow.

• It does not require chemical modification of drugs.

• Acceptable compression may not be achieved because the liquid drug may be squeezed out during

compression resulting in unsatisfactory tablet weight

Applications

This technology is powerful tool to improve the bioavailability of poorly water soluble drugs

Rapid release rate

Suitable for controlled release

Applicable in probiotics.

The technique of liquisolid preparation is used to formulate a drug solution in solid dosage forms.

Drug solution is generally, prepared by dissolving the drug in non-volatile water-

MATERIALS AND METHODS

Materials: Felodipine was a gift sample from Dr. Reddy’s Lab., Tween 80, PEG 400, Aerosil, Micro

crystalline cellulose, cross Carmellose sodium, magnesium Stearate provided by S.D fine chemicals

Mumbai.

Method of preparation: Preparation of liquicompact tablets prepared by direct compression method. The

Felodipine was dissolved in Propylene glycol and a homogenous drug solution was prepared. Next, the

calculated Weights (W) of the resulting liquid medicaments were incorporated into the calculated quantities

of the carrier material and mixed thoroughly. The resulting wet mixture was then blended with the

calculated amount of the coating material using a standard mixing process to forms simple admixture. The

prepared Liquisolid powder systems were manually compressed into multi stationary punching machine.

Evaluation of tablets: To design tablets and later monitor tablet production quality, quantitative evaluation

and assessment of tablet chemical, physical and bioavailability properties must be made.[11-19]

Weight variation test: It is desirable that all the tablets of a particular batch should be uniform in weight. If

any weight variation is there, that should fall within the prescribed limits:

±10 % for tablets weighing 300 mg or less; ±7.5 % for tablets weighing 300 - 315 mg; ±5 % for tablets

weighing more than 315 mg; Twenty tablets were taken randomly and weighed accurately and the average

weight calculated

Hardness test: This is the force required to break a tablet in a diametric compression. Hardness of the tablet

is determined by Stock’s Monsanto hardness tester which consists of a barrel with a compressible spring.

The tablet hardness of 4-6 kg/cm2 is considered as suitable for handing the tablet.

Size and Thickness: Control of physical dimensions of the tablets such as size and thickness is essential for

consumer acceptance and tablet-tablet uniformity. The thickness of tablet is measured by Vernier Calipers



scale. Tablet thickness should be controlled within a ±5%. In addition thickness must be controlled to

facilitate packaging.

Friability test: It is performed to evaluate the ability of tablets to withstand abrasion in packing, handling

and transporting. Initial weight of 20 tablets is taken and these are placed in the roche friabilator, rotating at

25 rpm for 4min. The difference in the weight is noted and expressed as percentage. It should be preferably

between 0.5 to 1.0 %.

In vitro Disintegration test: For most tablets the first important step toward solution is break down of tablet

into smaller particles or granules, a process known as disintegration. This is one of the important quality

control tests for disintegrating type tablets. Six tablets are tested for disintegration time using USP XXII

apparatus. Disintegration type conventional release tablets are tested for disintegrating time.

Drug – excipients compatibility study

FTIR: Completely dried potassium bromide was transferred into a mortar. About 2 % of pure drug or with

excipients was weighed in digital balance, mixed and grinded to a fine powder. Two stainless steel disks

were taken out of the desiccators. A piece of the pre-cut cardboard (in the tin can next to the oven) on top of

one disk was placed and cut out hole was filled with the finely ground mixture. The second stainless steel

disk was kept on top and transfers the sandwich onto the pistil in the hydraulic press. With a pumping

movement, hydraulic pump handle moved downward. The pistil will start to move upward until it reaches

the top of the pump chamber. Then, the pump handle moved upwards and continued pumping until the

pressure reaches 20,000 prf. Rest for a few seconds and with the small lever on the left side, the pressure

was released. Removing of the disks and pulling apart. Obtained film was homogenous and transparent in

appearance. Than inserted into the IR sample holder and attach with scotch tape and run the spectrum.[20]

Differential scanning calorimeter: The physical nature of the prepared LS optimized mixture and SD

optimized mixture was studied by DSC. The conversion of crystalline drug into amorphous form was

studied. DSC analysis was performed using TA Instruments Perkin-Elmer pyris differential scanning

calorimeter (DSC). The instrument was calibrated with indium standard. 3-5 mg samples were weighed and

placed in a closed, hermetic sample pans with pin hole. Thermograms were obtained by heating the sample

at a constant rate 10°C /min. A dry purge of nitrogen gas (50 ml/min) was used for all runs. Samples were

heated from 0°C to 250.0°C. The melting point, heat of fusion, disappearance of the crystalline sharp peak

of the drug and appearance of any new peak and peak shape were noted. The pure drug and Aerosil were

analyzed by DSC in same manner and the melting point and heat of fusion values were noted. The

thermogram of the LS optimized formulation was superimposed with that of pure drug and Aerosil.[21]

In-vitro dissolution study: Dissolution studies were carried out for all the formulations combinations in

triplicate, employing USP XXVII paddle method and 900ml of pH 6.8 phosphate buffer as the dissolution

medium. The medium was allowed to equilibrate to temp of 37+ 0.5°C. Tablet was placed in the vessel and

the vessel was covered the apparatus was operated for 1 hr in pH 6.8 phosphate buffer at 50 rpm. At definite

time intervals of 5 ml of the aliquot of sample was withdrawn periodically and the volume replaced with

equivalent amount of the fresh dissolution medium. The samples were analyzed spectrophotometrically at

230 nm using UV-Spectrophotometer. [22]

Release Kinetics [23-26]

The analysis of drug release mechanism from a pharmaceutical dosage form is an important. As a model-

dependent approach, the dissolution data was fitted to five popular release models such as zero-order, first-

order, diffusion and exponential equations.

Zero Order Release Kinetics: It defines a linear relationship between the fraction of drug released versus

time. Q = kot

Where, Q is the fraction of drug released at time t and kois the zero order release rate constant.

A plot of the % of drug released against time will be linear if the release obeys zero order release kinetics.

First Order Release Kinetics: Wagner assuming that the exposed surface area of a tablet decreased

exponentially with time during dissolution process suggested that drug release from most of the slow release



tablets could be described adequately by apparent first-order kinetics. The equation that describes first order

kinetics is

In (1-Q) = - K1t

Where, Q is the fraction of drug released at time t and k1 is the first order release rate constant.

Thus, a plot of the logarithm of the fraction of drug remained against time will be linear if the release obeys

first order release kinetics.

Higuchi’s equation: It defines a linear dependence of the active fraction released per unit of surface (Q) on

the square root of time.

Q=K2t½

Where, K2 is the release rate constant. A plot of the fraction of drug released against square root of time will

be linear if the release obeys Higuchi equation. This equation describes drug release as a diffusion process

based on the Fick’s law, square root time dependant.

Power Law: In order to define a model, which would represent a better fit for the formulation, dissolution

data was further analyzed by Peppas and Korsemeyer equation (Power Law).

Mt/M = K.tn

Where, Mt is the amount of drug released at time t and M is the amount released at time , thus the

Mt/Mis the fraction of drug released at time t,k is the kinetic constant and n is the diffusional exponent. A

plot between log of Mt/M against log of time will be linear if the release obeys Peppas and Korsemeyer

equation and the slope of this plot represents “n” value.

Table 1: Diffusion exponent and solute release mechanism for cylindrical shape

Sl. No Diffusion Exponent Overall solute diffusion mechanism

01 0.45 Fickian diffusion

02 0.45<n<0.89 Anomalous (non-fickian) diffusion

03 0.89 Case II transport

04 n>0.89 Super Case II transport

Stability studies: The purpose of stability testing is to provide evidence on how the quality of an active substance or

pharmaceutical product varies with time under the influence of a variety of environmental factors such as temperature,

humidity, and light. Also, the stability of excipients that may contain or form reactive degradation products, have to be

considered. [27-30]

Table 2: Objectives of Stability Testing

Objective Type of study Use

To select adequate (from the viewpoint

of stability) formulations and container- closure systems

Accelerated

Development of the product

To determine shelf-life and storage

conditions

Accelerated and real-

time

Development of the product and of

the registration dossier

To substantiate the claimed shelf-life Real-time Registration dossier

To verify that no changes have been

introduced in the formulation or

manufacturing process that can

adversely affect the stability of the

product

Accelerated and real-

time

Quality assurance in general,

including quality control.



1477.61

RESULTS AND DISCUSSION

Table 3: Standard calibration curve of Felodipine in ph 6.8 phosphate solution

Sl. No Concentration (µg/ml) Absorbance

0 00 0

1 10 0.0575

2 20 0.1222

3 30 0.1756

4 40 0.2356

5 50 0.2948

Fig.1: Standard calibration curve of Felodipine

1.0

0.9

2475.95

1991.00

1891.04

934.34 1316.29 1080.01 4065.39

698.48

0.8

3925.37

3565.24 3300.74

2599.44 2857.38

1944.481794.16

1166.69 857.46

Singl0e.7channel

3894.25

3699.97

2927.10

1867.97

1726.18

1284.81

977.44 1046.01

781.16868.40 617.07

3809.97 1917.18 1626.52

0.6

0.5

3844.51367386.2806.47

3874.28

183157.8710.55

1676.34 1426.56 1706.40

1614.95 1740.86

1243.03

645.09 572.83

3829.05 3648.97 1646.719532.518395.91 0.4 3743.64 1694.07 1464.98

3861.02 1564.15

0.3 1515.85

1548.29

2362.99

3500 3000 2500

Wave number

cm-1

2000 1500 1000

Fig. 2: Infrared spectrum of pure Felodipine

Linear (Series1)

0 10 20 30 40 50 60

Concentration ( mcg/ml)

y = 0.0059x + 0.00S0e4ries1 R² = 0.9996

0.5

Standard graph of felodipine

Ab

oso

rban

ce



[%]

874.48

1138.03

670.36

629. 1090.19

601

1069.13

898.15 1166.14

1.22

2897.24 2977.94 ttance

3643.93 2312.36

1200.27

1649.014511.89

3522.79

2350.17

01

.36

350

300

250

200

150

100

0 0 0Wavenumber cm0 - 0 0

1

Fig. 3: Infrared spectrum of pure felodipine drug with tween 80

3500 3000 2500 2000 1500 1000

Wavenumber cm-1

Fig. 4: Infrared spectrum of pure felodipine drug with propylene glycol

From the above figure2-6, it can be seen that, the major functional group peaks observed in spectras of Drug

with all the polymers remains unchanged as compared with spectra of Felodipine. So from the above IR

spectra it can be observed that there is no interaction between Felodipine and Polymers used in the

formulations.

90 2312.12

85

2956.62 934.60

T s tt [ ] 3396.62 1492.90

1169.18 893.16

75 1223.88 731.79

1460.20

70

1421.87 65

1283.82

60

1642.59



Loading Factor: “ Liquid load factor’’ and is defined as the Weight ratio of the liquid formulation(W) and

the Carrier material (q) in the system Lf = W/Q,,R`` represents the ratio between the Weights of the Carrier

(Q) and Coating (q) material present in the formulation R= Q/q The liquid load factor that ensures

acceptable flowability (Lf) can be determined by Lf= Φ + Ψ (1/R. Loading factor was calculated for the

formulations.

Table 5: Loading Factor

Ingredients (mg) F1 F2 F3 F4 F5 F6 F7

Felodipine 5 5 5 5 5 5 5

Propylene glycol 40 80

PEG-400 40 80

Tween- 80 40 80

Micro crystalline cellulose 300 400 300 400 300 400 440

Aerosil (Coating material) 60 80 60 80 60 80 60

Cros Caramellose sodium 30 30 30 30 30 30 30

Magnesium Stearate 5 5 5 5 5 5 5

Fig. 5: Differential Scanning Calorimetry of Felodipine Liquisolid compact formulation

Formulation design

Table 4: Formulation of Felodipine tablets (F1-F7)

Sl. No Formulation Loading Factor R Value

1 F1 0.15 5

2 F2 0.21 5

3 F3 0.15 5

4 F4 0.21 5

5 F5 0.15 5

6 F6 0.21 5

7 F7 0.01 7.3

Factor: =Liquid medication (W)/ Carrier material (Q)

Ratio (R):- Q/q

Where, Q- Carrier material, q- Coating material



Evaluation of felodipine tablets

Table 6: Bulk density, Compressibility index, Hauser’s ratio, Angle of repose of

Batch Bulk density

(gm/cm3)*

Tapped density

(gm/cm3)*

Compressibility

Index

(%)*

Hausner

Ratio* Angle of repose

(θ°)*

F1 0.4130 0.4738 12.8205 1.1470 26.33

F2 0.4027 0.4149 2.9411 1.0302 22.29

F3 0.4027 0.4149 2.9411 1.0302 24.15

F4 0.4972 0.5424 8.3333 1.0.909 23.48

F5 0.5704 0.6560 13.0434 1.1500 25.26

F6 0.5943 0.6538 9.0909 1.1000 28.78

F7 0.5418 0.5587 3.0303 1.0312 22.48

Discussion: Evaluation of Felodipine tablets is given in table 6.The pure drug Felodipine pre-formulation

was found to be limits. The bulk density of various powder mixed blends prepared with different super

disintegrates. Effervescent was measured by graduated cylinder. The bulk density was found in the range

0.4027– 0.5943kg/cm3. The tapped density was found in the range 0.4149– 0.6560 gm/cm

3. The

compressibility index was found in the range 2.9411-13.0434%. The Hausner ratio was found in the range

1.03-1.15. The angle of repose was found in the range 22.29-28.78. The variation of results is due to

different concentration of excipients with drug in each formulation.

Table 7: Evaluation tests for Felodipine liquid solid compact tablets

Batch Hardness

(kg/m3)

Thickness (mm) Friability (%)

Disintegration time (min)

F1 4.18 3.45 0.28 19

F2 4.28 3.24 0.06 21

F3 4.35 3.44 0.11 13

F4 4.42 3.27 0.20 16

F5 4.90 3.44 0.16 17

F6 5.76 3.69 0.44 09

F7 6.48 3.05 0.18 12

Table 8: Evaluation tests for Felodipine liquid solid compact tablets

Batch Weight Variation (mg) Drug Content (%) Wetting time (min)

F1 460±0.2 99 1.3

F2 584±0.4 98 2.3

F3 485±0.1 100 1.4

F4 610±0.3 99 1.6

F5 430±0.5 100 2.1

F6 658±1.0 100 1.3

F7 553±1.4 99 1.4

Discussion: Tablets were prepared using direct compression technique. Since the material was free flowing,

tablets were obtained of uniform weight due to uniform die fill tablets were obtained in the range with

acceptable weight variations as per pharmacopoeia specifications. The Hardness of the tablets was found in

the range 4.18-6.48 Kg/cm2 The thickness of the tablets was found in the range 3.05 – 3.53 mother

friability of tablets was observed in the range 0.06-0.44. The disintegration time was found in the

range 09-23mins.The wetting time was found in the range 1.3-2.6mins. Tablets are evaluated for the content

uniformity test all the formulations are under the IP specifications.

Table 9: In vitro dissolution profile of different formulations in pH 6.8 phosphate buffer

Time (Min) F1 F2 F3 F4 F5 F6 F7 (C.T)

0 0 0 0 0 0 0 0

10 35.62 32.41 38.14 37.26 38.27 35.13 32.08



Log %

dru

g

rem

eain

ing

Fig. 6: In-vitro Dissolution profile of Felodipine Liquisolid compact formulations F1-F7

Discussion: In vitro drug release studies were conducted for the formulation using USP dissolution

apparatus type- II (paddle), at 50 rpm. The percentage drug release at the end of 60mins was found in the

range 80.17-98-36%.

Kinetic analysis of dissolution data

Table 10: Drug Release Kinetics of Batch (F5) Liquisolid compact

Time

(min)

Square root of

time Log time

% drug

released

Log % drug

released

% drug

remaining

Log % drug

remaining

0 0 - 0 - 100 2

10 3.162278 1 38.27 1.5828585 61.73 1.790496277

20 4.472136 1.30103 48.26 1.6835873 51.74 1.713826424

30 5.477226 1.477121 65.23 1.8144474 34.77 1.541204691

40 6.324555 1.60206 77.45 1.8890214 22.55 1.353146546

50 7.071068 1.69897 88.64 1.9476297 11.36 1.055378331

60 7.745967 1.778151 98.36 1.9928185 1.64 0.214843848

2

1.5

1

0.5

0

First order plot

0 20 40 60 80

Time (min)

Fig. 7: Zero order kinetics of optimized batch (F5) Fig. 8: First order kinetics of optimized batch (F5)

R² = 0.8563

f6

f7 10 20 30 40 50 60

Time in (mins)

f1

100

50

Dissolution Profile 150

Zero order plot

150

10²0= 0.9443

50

0

0 50 time(min)

100

% d

rug r

elea

se

% o

f D

rug

Re

leas

e

2)0 48.16 46.17 46.31 44.25 48.26 46.40 44.21

30 57.85 61.68 62.45 60.46 65.23 61.24 59.18

40 68.70 67.09 70.73 69.13 77.45 74.07 65.37

50 79.19 78.32 85.56 78.81 88.64 82.46 79.28

60 82.45 80.17 92.14 88.05 98.36 93.24 91.38



R² = 0.9874

% d

rug r

elea

se

Log %

dru

g

rele

ase

120 100 80 60 40 20 0

Higuchi plot

0 5 10

Square root time

Korsemeyer peppa's plot 2

1

0 0 1 2

Log time

Fig. 9: HIGUCHI model of optimized batch (F5) Fig. 10: Korsemeyer peppa’s model of optimized

batch (F5)

Discussion: The release rate kinetic data for the F5 was given in table 9. The Optimized formulation F5 was

kept in Kinetic release models; it follows Higuchi model and its regression value R2 Was 0.987

Stability results:

Table 11: Percentage Cumulative release of stability studies of optimized Studies

Parameters After 15 days After 30 days After 45 days

Physical appearance No change No change No change

Weight variation (mg) 435.0±0.34 434.0±0.55 433.0±0.23

Thickness (mm) 3.69 3.53 3.74

Hardness (kg/cm3) 5.76 5.55 5.45

Friability (%) 0.44 0.43 0.43

Drug content (%/ tablet) 100 99.81 99.0

Wetting time (min) 1.3 2 2

Disintegration time (min) 09 19.13 21.05

Percentage drug release 98.32 97.97 97.73

Discussion: According to ICH guidelines, 45 days stability study at 40C ±2

0C, 27

0C ±2

0C and 45

0C ±2

0C

for 45 days at RH 75±5% of optimized formulation (F5) was carried out. It showed negligible change over

time for parameters like appearance, drug content, dissolution and assay etc., No significant difference in the

drug content between initial and formulations stored at 40C ±2

0C, 27

0C ±2

0C and 45

0C ±2

0C for 45 days at

RH 75±5% for 45 days.

CONCLUSIONS

In this technique actual mechanism of increasing in solubility is the wetting of drug particle and increase in

surface area of the drug due to that the solubility of drug get increased. The study shows that the solubility

of Felodipine is very less in water and hence the various non-volatile solvents having more solubility than

the water hence among tween-80, PEG, glycerol, propylene glycol shows more solubility of Felodipine.

Hence propylene glycol is selected for the preparation of liquisolid compacts. The microcrystalline cellulose

and aerosil was selected as carrier and coating material, Cros-caramellose sodium as the superdisintegrant

and magnesium sterate acts as Glidant in the formulation. The evaluation of the liquisolid compacts was

done pre-compression study like flow properties bulk density, tap density, angle of repose, Hausner’s ratio

and Carr’s index was performed and shows the significant results. In post compression evaluation like size

and thickness, hardness test, weight variation test, in vitro disintegration time, friability was done. The FTIR

and DSC spectral studies show no interaction of drug with polymer and excipients. F5 formulation has been

selected as the optimized formulation among all the other formulation and percentage drug release was

98.36 % at the end of 60 mins. Optimized formulation The Optimized formulation F5 was kept in Kinetic

release models; it follows Higuchi model and its regression value R2 Was 0.987. Finally the optimized

formulation .was compared with marketed formulations the results was satisfactory. Optimized formulation

(F5) was kept for stability studies For 15 days, 30 days, 45 days. There is no significant difference in the

values obtained before and after stability of final optimized formulation.

R² = 0.9817



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ACKNOWLEDGEMENT

The authors wish to thank our respectful Prof. Mrs. Sumakanth, Principal, RBVRR Women’s College of

Pharmacy, Affiliated to Osmania University-Hyd, Barkatpura, Hyderabad, Telangana, India, for providing

constant support to write this research article.

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