formulation and evaluation of fast dissolving tablets …

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Sachin et al. World Journal of Pharmacy and Pharmaceutical Sciences

FORMULATION AND EVALUATION OF FAST DISSOLVING

TABLETS OF ETORICOXIB

Sachin Gholve1*, Ganesh Todkar

1 , Omprakash Bhusnure

1 , Atish Jadhav

1 , Ravi

Rajurkar2 and Sanjay Thonte

1

*1

Channabasweshwar Pharmacy College (Degree), Kava Road, Basweshwar Chowk,

Latur, Maharashtra, India-413512

2Channabasweshwar Pharmacy Polytechnic Kava Road, Basweshwar Chowk,

Latur, Maharashtra, India-413512

ABSTRACT

Fast dissolving tablet format is designed to allow administration of an

oral solid dose form in the absence of water or fluid intake. Such

tablets readily dissolve or disintegrate in the saliva. Currently it is

approved in more than 60 countries worldwide. Etoricoxib is a COX-2

selective inhibitor. Current therapeutic indications of Etoricoxib are

rheumatoid arthritis, psoriatic arthritis, osteo arthritis, ankylosing

spondylitis, chronic low back pain, acute pain and gout. Like any other

COX-2 selective inhibitor, so those to treat the above diseases and to

get quick action oral fast disintegrating tablets were prepared. The aim

of this research is the development of fast dissolving tablet of

Etoricoxib, to overcome solubility problem of Etoricoxib. Dissolution

of Etoricoxib enhanced by solid dispersion technique in which

Etoricoxib-carrier β-cyclodextrin solid dispersion were prepared by solvent evaporation

technique, in three molar rations (1:1, 1:2 and 1:3).In formulation Croscarmellose sodium and

Crospovidone used to maintain rapid disintegration. Preparation of tablet by direct

compression and evaluation were done. In vitro and In vivo taste evaluation was done.

Compatibility between drug and excipient examine by FTIR study.

KEYWORDS: Etoricoxib, Croscarmellose Sodium, Crospovidone, Microcrystalline

cellulose, Super disintegrants.

WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES

SJIF Impact Factor 5.210

Volume 4, Issue 10, 1357-1376. Research Article ISSN 2278 – 4357

Article Received on

03 Aug 2015,

Revised on 29 Aug 2015,

Accepted on 19 Sep 2015

*Correspondence for

Author

Sachin Gholve

Channabasweshwar

Pharmacy College

(Degree), Kava Road,

Basweshwar Chowk,

Latur, Maharashtra, India-

413512.


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1. INTRODUCTION

Oral delivery is currently the gold standard in the pharmaceutical industry where it is

regarded as the safest, most convenient and most economical method of drug delivery having

the highest patient compliance.[1]

Tablet is the most popular among all dosage forms

existingtoday because of its convenience of self-administration, compactness and easy

manufacturing; however in many cases immediate onset of action is required

thanconventional therapy.[2]

Oral routes of drug administration have wide acceptance up to

50-60% of total dosage forms.[4]

Also solid oral delivery systems do not require sterile

conditions and are therefore, less expensive to manufacture. Patient compliance, high-

precision dosing, and manufacturing efficiency make tablets the solid dosage form of

choice.[2]

Fast dissolving drug delivery systems (FDDD‟S) are a new generation of

formulations whichcombine the advantages of both liquid and conventional tablet

formulations and at the same time, offer added advantages over both the traditional dosage

forms.[3]

Clinically, nonsteroidal anti-inflammatory drugs (NSAIDs) are the most frequently

prescribed by physicians forinflammatory disorders. NSAIDs exert their effect through

inhibition of cyclooxygenase-II, the main form of isozyme associated with inflammation. But

the simultaneous inhibition of cyclooxygenase-I and the resulting gastric and renal

dysfunction limit their frequent uses. Etoricoxib is a cyclooxygenase-II (COX-II) selective

NSAID used in the treatment of rheumatoid arthritis, osteoarthritis, postoperative dental pain,

chronic low back pain, acute gout and primary dysmenorrhea. The COX-I to COX-II

selectivity ratio is higher than other COX-II inhibitors such as Rofecoxib, Valdecoxib and

Celecoxib. Etoricoxib is practically insoluble in water and peak blood level. The Center for

Drug Evaluation and Research (CDER), US FDA defined Oral Disintegrating Tablets (ODT)

as “A solid dosage form containing medicinal substances, which disintegrates rapidly, usually

within a matter of seconds, when placed upon the tongue.”[5]

The faster drug dissolve into solution, quicker the absorption and onset of clinical effect.

Some drugs area absorbed from the mouth, pharynx and esophagus as the saliva passes down

into the stomach. Insuch cases, bioavailability of drug is significantly greater than those

observed from conventionaltablets dosage form. The advantage of mouth dissolving dosage

forms are increasingly beingrecognized in both, industry and academics.[7]


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2. MATERIALS AND METHODS

2.1 MATERIALS

Etoricoxib procured from Glenmark Generics Limited, Gujarat,β-

cyclodextrin,Croscarmellose sodium,Crospovidone, Avicel(102), Talc, Magnesium Stearate

are procured from Research-Lab Fine chem. Industry, Mumbai.

2.2 METHODS

A. Preparation of standard curve of Etoricoxib in 0.1N HCl (pH 1.2)

100 mg Etoricoxib was dissolved in 100ml of water. 10ml of the resulting solution was

further diluted up to 100ml with 0.1 N HCL to make a stock solution of concentration

100μg/ml. Further serial dilutions were carried out with 0.1 N HCL to get drug concentration

between 1 to 12μg/ml. The absorbances of the dilutions were measured against water as a

blank at 235nm using Shimadzu double beam UV visible spectrophotometer. The plot of

absorbance vs. concentration was plotted and was found to obey Beers Lambert‟s law in the

range of 0 to 100 μg/ml. Data in this range was subjected to linear regression analysis. The

plot for standard calibration curve of drug in 0.1N HCL.

B. Drug- carrier interaction study

Pure Drug, Pure β-cyclodextrin and mixture of Drug+ β-cyclodextrin were analyzed for

interaction by Fourier Transform Infrared Spectroscopy (FTIR) using KBr disk method.

C. Preparation of Solid Dispersion

Accurately weighed quantity of Drug and all the carriers in various proportion, 1:1, 1:2, 1:3,

(drug : carrier) were carefully transferred in glass flask and dissolve suitable solvents like

Methanol, then solvent was removed by evaporation at400 C under reduced pressure by using

vacuum evaporator after that the obtained massis scraped, crushed, pulverized and shifted

through mesh No. 100.

D. Solubility Study of EtoricoxibSolid dispersion

Solubility studies of Etoricoxib in carrier solutions were carried out atroom temperature.

Excess amount of Etoricoxib was added to 0.1N HCL containing variousseries of stoppered

conical flasks and shaken for 48 hr. on a rotary flask shaker. The suspensions were filtered

through whatman filter paper and assayed for Etoricoxib using UV spectrophotometer at 235

nm against blank prepared using sameconcentration of the various carriers in 0.1N HCL. .

The solubility of Etoricoxib invarious solvents is calculated.


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E. Dissolution Study

All the ratios of Drug β-Cyclodextrin solid dispersions prepared were characterized by

dissolution studies. In-vitro dissolution study of the solid dispersions prepared wasperformed

using USP (Type-II) apparatus at a speed of 50 rpm. Dissolution study wascarried out using

900 ml of 1% 0.1N HCL as dissolution medium maintained at temperature of 37°C ±5ºC. At

appropriate intervals, 5 ml of the solution was takenand dissolution medium was replaced by

5 ml of fresh dissolution fluid to maintain constant volume. The samples were then analyzed

at 235 nm by UV/visiblespectrophotometer using 0.1N HCL as blank. The mean of three

determinations wasused to calculate the drug release from each of the solid dispersion.

2.3 Precompression parameter study

1. Physical appearance

It includes the visual inspection of solid dispersion.

2. Angle of repose

Angle of repose is defined as the maximum angle possible between the surfaceof pile of

powder and horizontal plane. The angle of repose was determined by thefunnel method. The

accurately weighed powder was taken in a funnel. The height ofthe funnel was adjusted in

such a way that the tip of the funnel just touched the apexof the heap of the powder. The

powder was allowed to flow through the funnel freelyonto the surface. The diameter of the

powder cone was measured. The angle of reposewas calculated by substituting the values of

the base radius „R‟ and pile height „H‟ inthe following equation (Aulton, 2003).

Tan θ= H / R ---------Equation I

Where, H = Pile height and R = Radius of Pile

Therefore; = tan –1 H / R

Table No. 2: Relationship between angle of repose (θ) and flow ability

Angle of repose (θ) Flowability

< 20 Excellent Excellent

20-30 Good

30-34 Acceptable

> 40 Very poor


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3. Bulk density

The sample equivalent to 25g was accurately weighed and filled in a 100 mlgraduated

cylinder and the powder was leveled and the unsettled volume, VOwasnoted. The bulk density

was calculated by the formula (Lachman et al, 1991)

Bulk density (ρo) = M/Vo--------Equation II

Where,

M = mass of powder taken, Vo = Apparent unstirred volume

4. Tapped density

The tapped density was determined by mechanically tapping the measuringcylinder and the

volume was noted (Lachman et al, 1991)

Tapped density (ρt) = M / Vt--------Equation III

Where,

ρt = tapped density, M = weight of granules, Vt = tapped volume of granules in cm3

5. Compressibility index

The bulk volume and tapped volume was measured and compressibility indexwas calculated

using the formula (Aulton, 2003).

Compressibility index =100 (Vo-Vf)/Vo--------Equation IV

Where,Vo = Bulk volume, Vf = Tapped volume

Table No.3: Relationship between % compressibility and flowability

6. Hausner’s ratio

Tapped volume and bulk volume were measured and the hausner‟s ratio was calculated using

the formula

Compressibility Flowability

5-15 Excellent

12-16 Good

18-21 Fairly

23-35 Poor

33-38 Very pure

>40 Extremely


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Hausner’s ratio = Vo/Vf--------Equation V

Where,

Vo = Bulk volume, Vf = Tapped volume

2.3.1 Preparation of fast dissolving tablets by direct compression technique:

Method: Fast dissolving tablets of Etoricoxib were prepared by direct compression method

according to the formula

Table No. 4: Formulations from F1 to F8

All the ingredients were passed through 60 # sieve separately, Magnesiumstearate & Talc

through 40 #. Then the ingredients were weighed and mixed in geometrical order and tablets

were compressed with 8 mm sizes flat round punch to get tablet using Rimek Compression

Machine.

2.4Post compression parameter study

1. Thickness

The thickness of the tablets was determined using a Vernier caliper. Five tablets from each

type of formulation were used and average values were calculated. It is expressed in mm.

(Lachman et al, 1991)

2. Hardness

The resistance of tablets to shipping, breakage, under conditions of storage, transportation

and handling before usage depends on its hardness. For each formulation, the hardness of 6

tablets was determined using the Monsanto hardness tester. The tablet was held along its

oblong axis in between the two jaws of the tester. At this point, reading should be zero

kg/cm2. Then constant force was applied by rotating the knob until the tablet fractured. The

value at this point was noted (Lachman et al, 1991).

Ingredients

Quantity in mg

SD1:1 SD1:3

F1 F2 F3 F4 F5 F6 F7 F8

Etoricoxib(equivalent to 30 mg) 60 60 60 60 120 120 120 120

Croscarmellose sodium 5.5 5.5 10.5 10.5 5.5 5.5 10.5 10.5

Crospovidone 4 8 4 8 4 8 4 8

Microcrystalline cellulose 123.5 119.5 118.5 114.5 63.5 59.5 58.5 54.5

Mg. Stearate 2 2 2 2 2 2 2 2

Talc 5 5 5 5 5 5 5 5


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3. Friability

Friability is the measure of tablet strength. Roche Friabilator was used for testing the

friability using the following procedure. This test subjects a number of tablets to the

combined effect of shock abrasion by utilizing a plastic chamber which revolves at a speed of

25 rpm, dropping the tablets to a distance of 6 inches in each revolution. A sample

ofpreweighed 6 tablets was placed in Roche Friabilator which was then operated for 100

revolutions i.e. 4 minutes. The tablets were then dusted and reweighed. A loss of less than 1

% in weight in generally considered acceptable.Percent friability (% F) was calculated as

follows (Lachman et al, 1991).

Initial weight - Final weight

% F = ------------------------------------------ × 100 -------------Equation VI

Initial weight

4. Weight variation test

To find out weight variation, 20 tablets of each type of formulation wereweighed individually

using an electronic balance, average weight was calculated andindividual tablet weight was

then compared with average value to find the deviation in weigh. (Indian pharmacopoeia,

1996).

Table No.5: Specifications for tablets as per Pharmacopoeia of India

Sr.No. Average Weight of Tablet % Deviation

1 80 mg or less 10

2 More than 80 mg but less that 250 mg 7.5

3 250 or more 5

5. Uniformity of drug content

Five tablets of each type of formulation were weighed and crushed in mortar and powder

equivalent to 50 mg of Etoricoxib was weighed and dissolved in 100 ml of 0.1N HCl (pH

1.2). This was the stock solution from which 0.2 ml sample was withdrawn and diluted to 10

ml with 0.1N HCl. The absorbance was measured at wavelength 235 nm using double beam

UV-Visible spectrophotometer. Content uniformity was calculated using formula.

% Purity = 10 C (Au / As) -------Equation VII

Where, C - Concentration,

Au and As - Absorbance‟s obtained from unknown preparation and standard Preparation.


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6. Wetting time

The method was applied to measure tablet wetting time. A piece of tissue paper folded twice

was placed in a small Petri dish (i.d. = 6.5 cm) containing 10 ml of water, a tablet was placed

on the paper, and the time for complete wetting was measured. Three trials for each batch

were performed and standard deviation was also determined.

7. In vitro disintegration time

The process of breakdown of a tablet into smaller particles is called as disintegration. The in-

vitro disintegration time of a tablet was determined using disintegration test apparatus as per

I.P. specifications. I.P. Specifications: Place one tablet in each of the 6 tubes of the basket.

Add a disc to each tube and run the apparatus using distilled water maintained at 37° ± 2°C as

the immersion liquid. The assembly should be raised and lowered between 30 cycles per

minute in the 0.1 N HCL maintained at 37° ± 2°C. The time in seconds taken for complete

disintegrationof the tablet with no palpable mass remaining in the apparatus was measured

and recorded.

2.5 In vitro drug release studies details

Apparatus used : USP XXIII dissolution test apparatus

Dissolution medium : 0.1 N HCL

Dissolution medium volume : 900 ml

Temperature : 37 ± 0.5°C

Speed of basket paddle : 50 rpm

Sampling intervals : 5 min

Sample withdraw : 10 ml

Absorbance measured : 235 nm

2.5.1 In vitro drug release kinetics

To analyze the mechanism of the drug release rate kinetics of the dosage form, the

Obtained were graphed as:

1. Cumulative percentage drug released Vs. Time (Zero order plots)

2. Cumulative percentage drug released Vs Square root of time (Higuchi plots)

3. Log cumulative percentage drug remaining Vs Time (First order plots)

4. Log percentage drug released Vs Log time (Peppas plots)


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1. Zero order release rate kinetics

To study the zero order release kinetics the release rate data are fitted to the following

equation

F= kt

Where F is the fraction of drug release, K is the release rate constant, t is the release time

When the data is plotted as cumulative percent drug release Vs time, if the plot is linear then

the data obeys zero order release kinetics with a slope equal to K. This model represents an

ideal release in order to achieve prolonged pharmacological action. This is applicable to

dosage forms like transdermal systems, coated forms, osmotic systems, as well as Matrix

tablets containing low soluble drugs.

2. First order rate kinetics

The equation for first order treatment is represented as

Log c = Logco- kt/2.303

Where, c is amount of drug remaining unreleased at time t,

Cois initial amount of drug in solution,

K is first order rate constant.

The model is applicable to hydrolysis kinetics and to study the release profiles of

pharmaceutical dosage forms such as those containing water soluble drugs in porous

matrices.

3. Higuchi release model

To study the Higuchi release kinetics, the release rate data were fitted to the following

equation:

F= K. t ½

Where F is the amount of drug release , K is the release rate constant, t is the release time

When the data is plotted as cumulative drug released Vs square root of time, Yields a straight

line, indicating that that the drug was released by diffusion mechanism. The slope is equal to

K This model is applicable to system with drug dispersed in uniform swellable polymer

matrix as in case of matrix tablets with water soluble drug.

4. Korsmeyer and Peppas release model

The release rate data were fitted to the following equation

Mt / M∞ = Ktn


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Where, Mt / M∞ is the fractional release of drug, „t‟ denotes the release time, „K‟ represents

a constant incorporating structural and geometrical characteristics of the device, „n‟ is the

diffusion exponent and characterize the type of release mechanism during the release process.

This model is used to analyze the release from polymeric dosage forms, when the release

mechanism is not well known or when there is a possibility of more than one type of release

phenomenon being involved.

Table No.6 Diffusional exponent standard values for Korsmeyer Peppas

Release Exponent ‘n’ Drug Transport Mechanism

0.5 Fickian diffusion

0.5<n<1.0 Anomalous transport

1.0 Case-II

>1.0 Super case-II transport

3. RESULTS

3.1 UV-Visible spectrophotometric study

λ max determination

Fig. 1: UV Spectra of Etoricoxib

a) Preparation of standard calibration curve of Etoricoxib

Table No.7: Standard calibration curve of Etoricoxib in 0.1N HCL

Sr. No. Concentration ( μg/ml) Absorbance at 235 nm

1 0 0

2 2 0.242

3 4 0.382

4 6 0.559

5 8 0.709

6 10 0.884

7 12 1.057


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Fig.2: Standard curve of Etoricoxib in 0.1 N HCL (Ph 1.2)

3.2 Infrared Spectroscopy

Fig.3: FT-IR Spectrum of Etoricoxib

Fig.4: FT-IR Spectrum of Etoricoxib: β-cyclodextrin


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Fig. 5: FT-IR Spectrum of Mixture

3.2.1 Infrared Spectroscopy Result

FTIR studies were conducted and the spectrum was recorded in the range of 4000-400 cm-1.

No significant interaction between the drug and excipients was observed. All the spectrum

i.e. drug and excipients were concordant with that of the standard IR spectra of pure drug

Etoricoxib.

3.3 Evaluation of Solid Dispersion

3.3.1 Solubility study of Etoricoxib solid dispersion

Table No. 8: Solubility study of solid dispersion

Sr. No. Drug : carrier ratio Solubility µg/ml

1 Pure drug 2.05

2 Etoricoxib+β-cyclodextrin (1:1) 19.22



Solubility of all solid dispersion can be increased as compared to pure drug by solid

dispersion. Solubility of at 1:1, 1: 2, 1:3 ratios gives respectively. Increasing the

concentration of polymer was 1:1 & 1:3 for SD1and SD2 respectively more soluble than pure

drug.


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Fig. 6: Solubility study of solid dispersion

% Drug release from solid dispersion

Table No. 9: % Drug release from solid dispersion

Sr. No. Time(min) Solid Dispersion

(1:1)

Solid Dispersion

(1:2)

Solid Dispersion

(1:3)

1 5 22.45 18.79 26.11

2 10 47.57 41.34 53.14

3 15 65.68 54.25 69.11

4 20 74.09 64.47 81.96

5 25 86.25 72.03 90.91

6 30 94.14 79.77 97.02

The drug release profile for all formulations shown in table. The drug release of β-

cyclodextrin at 1:1, 1:2, and 1:3 ratios gives 94.14, 79.77and 97.02% respectively. The

optimized batch sd1which contain β-cyclodextrin and Etoricoxib at 1:1 ratios which give

94.14 % drug release in 30 min and SD3 which contain β-cyclodextrin and Etoricoxib at 1:3

ratios which give 97.02% drug release in 30 min respectively.

Fig. 7: % Drug release from solid dispersion


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3.3.2 Precompression parameter study

Table No. 10: Precompression parameter study

Formulation

Code

Angle of

repose

Bulk

Density (wt/ml)

Taped

Density (wt/ml)

Hausner’s

ratio (%)

Compressibility

Index(%)

F1 26.10±0.56 0.41±0.02 0.49±0.04 1.17±0.01 13.47±0.23

F2 27.92±0.70 0.42±0.03 0.48±0.02 1.12±0.02 15.00±0.46

F3 25.74±0.45 0.42±0.03 0.49±0.04 1.14±0.02 12.82±0.45

F4 28.36±0.63 0.41±0.02 0.48±0.02 1.18±0.04 14.91±0.36

F5 27.40±0.69 0.42±0.03 0.48±0.02 1.13±0.03 11.86±0.17

F6 28.23±0.14 0.43±0.02 0.51±0.01 1.16±0.05 14.03±0.21

F7 26.56±0.60 0.42±0.03 0.49±0.04 1.15±0.06 13.67±0.11

F8 28.17±0.85 0.42±0.03 0.48±0.02 1.16±0.07 13.44±0.17

The values represents Mean±SD, n = 3

3.3.3 Post compression parameter study

Table No. 11: A-Post compression parameter study

Formulation

Code

Hardness

(kg/cm2)

Friability

(%)

Weight

variation (mg)

Thickness

(mm)

F1 4.5±0.12 0.34±0.08 202.1±0.05 3.20±0.02

F2 4.0±0.13 0.37±0.04 200.1±0.06 3.28±0.02

F3 4.3±0.11 0.33±0.03 202.0±0.03 3.35±0.02

F4 3.7±0.09 0.38±0.08 201.3±0.08 3.25±0.05

F5 3.5±0.10 0.39±0.03 200.0±0.03 3.30±0.02

F6 3.4±0.15 0.36±0.05 200.3±0.02 3.20±0.03

F7 3.5±0.10 0.35±0.06 200.0±0.03 3.30±0.02

F8 3.2±0.11 0.39±0.06 201.1±0.05 3.25±0.01


Table No.12: B Post compression parameter study

Formulation

Code Drug content (%) Wetting time (sec)

Disintegration

time (sec)

F1 95.23±1.26 38±1.25 67±1.35

F2 93.12±1.19 36±2.03 52±1.34

F3 94.01±1.46 38±1.56 59±1.56

F4 99.32±1.18 37±1.30 45±1.78

F5 98.10±1.95 24±1.86 47±1.86

F6 97.61±1.23 25±1.49 32±1.56

F7 97.21±1.43 24±1.15 44±1.56

F8 99.81±1.84 21±1.19 29±1.67



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3.4In-vitro dissolution study of F1 to F8 Formulation batches

Table No.13: In-vitro dissolution study of F1 to F8 batches.

Time

(min)

% Drug release

F1 F2 F3 F4 F5 F6 F7 F8

0 0.00 0.00 0.00 0.00 0.00 0.00 0.00 0.00

5 20.98 20.25 18.42 17.69 19.52 27.58 18.79 22.45

10 34.04 34.40 33.28 31.80 34.39 38.87 35.48 33.69

15 66.28 67.74 67.34 64.39 64.80 62.38 60.42 67.03

20 76.54 79.11 76.51 72.42 77.24 78.45 70.98 72.16

25 81.03 83.64 80.64 82.11 82.11 87.36 84.57 86.13

30 93.10 94.43 92.50 95.35 93.99 96.00 94.27 98.79

3.4.1 Percentage (%) Drug release

The In-vitro drug release from fast dissolving tablets prepared by direct compression method

were found to be in the range of 92.50 to 98.79

3.5 Release kinetics of Etoricoxib Tablets

3.5.1 Zero order release kinetic data

Fig.8: Zero order release kinetic of F1-F4

Fig.9: Zero order release kineticof F5-F8


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3.5.2 First order release kinetic data

Table No.14:First order release kinetic data

Sr.No. Time

(min)

Log% cumulative drug remain to be released

F1 F2 F3 F4 F5 F6 F7 F8

1 0 2 2 2 2 2 2 2 2

2 5 1.897 1.901 1.911 1.915 1.905 1.859 1.909 1.889

3 10 1.819 1.816 1.824 1.833 1.816 1.786 1.809 1.821

4 15 1.527 1.508 1.514 1.551 1.546 1.575 1.551 1.518

5 20 1.370 1.319 1.370 1.440 1.357 1.333 1.462 1.444

6 25 1.275 1.213 1.286 1.252 1.252 1.101 1.188 1.142

7 30 0.838 0.745 0.875 0.667 0.778 0.602 0.758 0.082

Fig.10: First order release kinetic of F1-F4

Fig.11: First order release kinetic of F5-F8


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3.5.3 Higuchi matrix release kinetic data

Table No. 15:Higuchi matrix release kinetic data

Sr. No

√T

% Cumulative drug release

F1 F2 F3 F4 F5 F6 F7 F8

1 0 0.00 0.00 0.00 0.00 0.00 0.00 0.00 0.00

2 2.236 20.98 20.25 18.42 17.69 19.52 27.58 18.79 22.45

3 3.162 34.04 34.40 33.28 31.80 34.39 38.87 35.48 33.69

4 3.872 66.28 67.74 67.34 64.39 64.80 62.38 60.42 67.03

5 4.472 76.54 79.11 76.51 72.42 77.24 78.45 70.98 72.16

6 5 81.03 83.64 80.64 82.11 82.11 87.36 84.57 86.13

7 5.477 93.10 94.43 92.50 95.35 93.99 96.00 94.27 98.79

Fig.12 : Higuchi matrix release kinetic of F1-F4

Fig.13: Higuchi matrix release kinetic of F5-F8


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3.5.4Peppas release kinetic data

Table No.16: Peppas release kinetic data

Sr. No. LogT(min) Log % drug release

F1 F2 F3 F4 F5 F6 F7 F8

1 0 0 0 0 0 0 0 0 0

2 0.6989 1.321 1.306 1.265 1.247 1.290 1.440 1.273 1.351

3 1 1.531 1.536 1.522 1.502 1.536 1.589 1.549 1.527

4 1.176 1.821 1.830 1.828 1.808 1.811 1.765 1.781 1.826

5 1.301 1.883 1.898 1.883 1.859 1.887 1.894 1.851 1.858

6 1.397 1.908 1.922 1.906 1.914 1.914 1.941 1.927 1.935

7 1.477 1.968 1.975 1.966 1.979 1.973 1.982 1.974 1.994

Fig.14: Peppas release kinetic of F1-F4

Fig.15: Peppas release kinetic of F5-F8


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Table No.17: Release kinetic of formulation F1-F8

Formulation Zero order

(R2)

First order

(R2)

Higuchi’s

(R2)

Peppas

R2 N

F1 0.953 0.9498 0.9388 0.9614 0.8971

F2 0.9505 0.9493 0.9343 0.9611 0.9248

F3 0.9468 0.9535 0.9284 0.9574 0.9549

F4 0.9692 0.9044 0.9268 0.9705 0.9896

F5 0.9604 0.9441 0.9375 0.9701 0.9301

F6 0.9695 0.9347 0.9644 0.9814 0.7581

F7 0.9823 0.9362 0.9435 0.9877 0.9395

F8 0.9705 0.8003 0.9369 0.9648 0.8813

4. CONCLUSION

In present work, a fast disintegrating Etoricoxib tablets were developed by direct

compression method using synthetic Superdisintegrants. In the preliminary part, FT-IR study

was carried out which suggested that there was no significant drug interaction between

Etoricoxib with β -cyclodextrin, Superdisintegrants and other excipients. UV scan of had

shown Etoricoxibabsorption at wavelength 235 nm in 0.1N HCL Physical parameters like

hardness, weight variation, thickness and friability were within pharmacopoeial limit.

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