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Asian Journal of Pharmaceutical Science & Technology

e-ISSN: 2248 – 9185 www.ajpst.com Print ISSN: 2248 – 9177

DEVELOPMENT AND EVALUATION OF FAST DISINTEGRATING

TABLETS OF GRANISETRON HCL WITH NATURAL AND

SYNTHETIC POLYMERS

*B. Sunil Kumar Reddy, Shubhrajit Mantry, S. Anil Kumar, E. Satheesh Kumar

*Department of Pharmaceutics, Kottam Institute of Pharmacy, Erravally-X-roads, Mahaboob Nagar Dist - 509125, A.P, India.

ABSTRACT

Granisetron HCl is a novel serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting

during cancer chemotherapy but its oral bioavailability is low due to extensive first-pass metabolism in liver which makes it an

ideal candidate for Fast dissolving drug delivery system. The present study aimed to develop fast disintegrating tablets of

Granisetron HCl using natural superdisintegrants like Plantago ovata, Gum Karaya and Agar & synthetic superdisintegrants like

Indion 234, Croscaramellose sodium, Sodium starch glycolate and crospovidone. Precompressional studies revealed good

micromeritic properties of powder blend. Various Formulations of were prepared by direct compression method and were

evaluated for their physico chemical properties, drug release and stability studies. FTIR and DSC show that there is no interaction

with drug and other excipients. The hardness, friability, drug content and disintegration time of fast dissolving tablets were

found uniform and reproducible. Dissolution test shows that 5 % w/w concentration was found optimum. Selected Formulation

F4 were subjected to FTIR and DSC that shows that is compatible and release was found superior to marketed conventional

tablets with respect to disintegration and dissolution and found to be stable. Stability studies shows that there is no much more

differences in their release.

Key words: Fast disintegrating tablets, Granisetron HCl, Superdisintegrants.

INTRODUCTION

Fast dissolving tablets disintegrates instantaneously

when placed on tongue, releasing the drug that dissolves or

disperses in the saliva. Cancer chemotherapy causes lot of

adverse effects, of which nausea and vomiting is prime

once. This can be clearly seen with model anticancer drug

cisplatin, which is first line drug in many types of cancers.

Hence anti-emetic drugs like ondansetron, granisetron are

administered one hour prior to the administration of

anticancer drug. Granisetron HCl is a novel serotonin 5-

HT3 receptor antagonist used as an antiemetic to treat

nausea and vomiting following chemotherapy. Its main

effect is to reduce the activity of the vagus nerve, which is a

nerve that activates the vomiting centre in medulla

oblongata. During chemotherapy - induced vomiting,

mucosal enterochromaffin cells release serotonin, which

stimulates 5-HT3 receptors [1-3]. The present study aimed

to develop fast dissolving tablets by using various of natural

and synthetic super disintegrants to increase the

bioavailability of drug. Identify drug-polymer compatibility

by FTIR and DSC studies. Prepare fast dissolving tablets by

using plain drug with different superdisintegrants by direct

compression method. Evaluate tablets for various physico-

chemical parameters such as hardness, friability, weight

variation, drug content, wetting time, in vitro disintegration

time. Subject the tablets for in vitro dissolution studies and

analyse with different kinetic models. Carryout stability

studies on selected fast dissolving tablets as per ICH

guidelines.

MATERIALS & METHODS

All the materials used in the formulation and

evaluation are listed below. Distilled water was used in the

present study.

The tablets were prepared by taking various

combinations of natural and synthetic polymers of plantago

ovata Gum karya, Agar, Indion 234, Crospovidone,

Croscaramellose sodium, SSG with various proportions

[4,5].

Corresponding Author: B. Sunil Kumar Reddy E-mail: manu28pharmacy@gmail.com

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S.No Material Supplier/ Manufacturer

1 Granisetron HCL Natco Pharma Ltd. Hyderabad

2 Plantago ovata Gift sample, Crystal colloid, Mumbai

3 Gum Karaya Krystal Colloid Ltd. Mumbai

4 Agar Hiedialabtrs Pvt Ltd, Mumbai

5 Crospovidone, Croscaramellose sodium, Sodium starch glycolate Maruti Chemicals, Ahmadabad

6 Iodine 234 Ion exchange ltd, Mumbai

7 Direct Compression mannitol Torrent Pharma Ltd, Ahmadabad

8 Microcrystalline Cellulose, Magnesium Stearate S.D.Fine Chemicals Pvt Ltd, Mumbai

9 Aerosil, Sodium Hydroxide, Potassium Di hydrogen Phosphate S.D.Fine Chemicals Pvt Ltd, Mumbai

Table 1. Composition of Granisetron HCl fast dissolving tablets containing Natural superdisintegrants

Ingredients(mg) Formulation code

F1 F2 F3 F4 F5 F6 F7 F8 F9 F10 F11 F12

Granisetron HCl 2 2 2 2 2 2 2 2 2 2 2 2

plantago ovata 4 6 8 10 … … … … … … … …

Gum karya … … … … 4 6 8 10 … … … …

Agar … … … … … … … … 4 6 8 10

MCC 136 134 132 130 136 134 132 130 136 134 132 130

SD Mannitol 50 50 50 50 50 50 50 50 50 50 50 50

Talc 2 2 2 2 2 2 2 2 2 2 2 2

Mg Stearate 2 2 2 2 2 2 2 2 2 2 2 2

Aerosil 2 2 2 2 2 2 2 2 2 2 2 2

Na. saccharin 2 2 2 2 2 2 2 2 2 2 2 2

TOTAL 200 200 200 200 200 200 200 200 200 200 200 200

Table 2. Composition of Granisetron HCl fast dissolving tablets containing synthetic superdisintegrants

Fig 1. UV absorbance spectra of Granisetron HCl in phosphate buffer of pH 6.8

Ingredients(mg) Formulation code

F13 F14 F15 F16 F17 F18 F19 F20

Granisetron HCl 2 2 2 2 2 2 2 2

Indion 234 4 6 8 10 … … … …

Crospovidone … … … … 4 6 8 10

Croscaramellose

sodium … … … … … … … …

SSG … … … … … … … …

MCC 136 134 132 130 136 134 132 130

SD Mannitol 50 50 50 50 50 50 50 50

Talc 2 2 2 2 2 2 2 2

Mg Stearate 2 2 2 2 2 2 2 2

Aerosil 2 2 2 2 2 2 2 2

Na. saccharin 2 2 2 2 2 2 2 2

TOTAL 200 200 200 200 200 200 200 200

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Table 3. Composition of Granisetron HCl fast dissolving tablets containing synthetic superdisintegrants

Ingredients(mg) Formulation code

F21 F22 F23 F24 F25 F26 F27 F28

Granisetron HCl 2 2 2 2 2 2 2 2

Crospovidone … … … … … … … …

Indion 234 … … … … … … … …

Croscaramellose Na 4 6 8 10 … … … …

SSG … … … … 4 6 8 10

MCC 136 134 132 130 136 132 128 124

SD Mannitol 50 50 50 50 50 50 50 50

Talc 2 2 2 2 2 2 2 2

Mg Stearate 2 2 2 2 2 2 2 2

Aerosil 2 2 2 2 2 2 2 2

Na. saccharin 2 2 2 2 2 2 2 2

TOTAL 200 200 200 200 200 200 200 200

Fig 2.UV absorbance spectra of Granisetron HCl in buffer of pH 1.2

Fig 3.Calibration curve for the estimation of Granisetron HCl in phosphate buffer of pH 6.8

Fig 4. FTIR spectrum of Granisetron HCl pure drug

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Fig 5. FTIR spectrum of formulation (F4)

Fig 6. DSC thermo gram of Granisetron HCl Pure drug

Fig 7. DSC thermo gram of formulation (F4) containing plantago ovata and Granisetron HCl

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Table 4. Micromeritic properties of Precompressional powder blend

Code Bulk density*

(gm/cm3)

Tapped density*

(gm/cm3)

Angle of repose*(θ) Carr’s Index*

(%)

Hausner’s

Ratio*

F1 0.44±0.15 0.51±0.63 15.08±0.23 13.72±0.18 1.15±0.01

F2 0.47±0.18 0.53± 0.42 14.31±0.17 11.32±0.12 1.12±0.03

F3 0.52±0.15 0.59±0.52 18.04±0.12 11.86±0.16 1.13±0.02

F4 0.55±0.17 0.49±0.35 16.13±0.19 14.28±0.28 1.16±0.01

F5 0.53±0.12 0.59±0.43 13.64±0.15 10.16± 0.31 1.11±0.02

F6 0.41 ± 0.11 0.47± 0.33 19.43±0.17 12.76± 0.25 1.14±0.03

F7 0.47 ± 0.13 0.55 ± 0.36 15.93±0.15 14.54± 0.13 1.17±0.01

F8 0.54 ± 0.12 0.63 ± 0.42 23.12±0.15 14.28± 0.11 1.16±0.03

F9 0.55 ± 0.10 0.62 ± 0.28 17.93±0.15 11.29 ± 0.28 1.12± 0.01

F10 0.53 ± 0.11 0.59±0.55 14.43±0.17 10.16±0.03 1.11 ± 0.02

F11 0.45 ± 0.13 0.52±0.35 24.54±0.18 13.46±0.01 1.15 ± 0.01

F12 0.46 ± 0.12 0.53±0.43 16.13±0.17 13.20±0.04 1.15 ± 0.03

F13 0.53 ± 0.15 0.60±0.28 20.59±0.21 11.66±0.01 1.13 ± 0.04

F14 0.46 ± 0.17 0.53±0.34 22.32±0.15 13.20±0.02 1.15 ± 0.01

F15 0.44±0.15 0.51±0.63 19.08±0.23 13.72±0.18 1.15±0.01

F16 0.47±0.18 0.53± 0.42 17.31±0.17 11.32±0.12 1.12±0.03

F17 0.52±0.15 0.59±0.52 16.04±0.12 11.86±0.16 1.13±0.02

F18 0.55±0.17 0.49±0.35 18.13±0.19 14.28±0.28 1.16±0.01

F19 0.53±0.12 0.59±0.43 23.64±0.15 10.16± 0.31 1.11±0.02

F20 0.41 ± 0.11 0.47± 0.33 14.43±0.17 12.76± 0.25 1.14±0.03

F21 0.47 ± 0.13 0.55 ± 0.36 19.93±0.15 14.54± 0.13 1.17±0.01

F22 0.54 ± 0.12 0.63 ± 0.42 21.12±0.15 14.28± 0.11 1.16±0.03

F23 0.55 ± 0.10 0.62 ± 0.28 15.93±0.15 11.29 ± 0.28 1.12± 0.01

F24 0.53 ± 0.11 0.59±0.55 21.43±0.17 10.16±0.03 1.11 ± 0.02

F25 0.45 ± 0.13 0.52±0.35 18.54±0.18 13.46±0.01 1.15 ± 0.01

F26 0.46 ± 0.12 0.53±0.43 17.13±0.17 13.20±0.04 1.15 ± 0.03

F27 0.53 ± 0.15 0.60±0.28 16.59±0.21 11.66±0.01 1.13 ± 0.04

F28 0.46 ± 0.17 0.53±0.34 22.32±0.15 13.20±0.02 1.15 ± 0.01

Table 5. Physico-chemical Evaluation fast dissolving tablets

Code Thickness (mm) Hardness

test(kg/cm2)

Weight variation

(%) Friability Drug content (%)

F1 4.28 ± 0.03 4.0±0.55 195.58±1.32 0.34±0.03 99.41 ± 0.39

F2 4.35 ± 0.01 3.8±0.35 200.64±1.46 0.36±0.01 99.18 ± 0.55

F3 4.25 ± 0.04 4.1±0.43 196.45±1.28 0.42±0.04 98.85 ± 0.63

F4 4.33 ± 0.06 4.2±0.28 201.68±1.53 0.33±0.01 99.28 ± 0.65

F5 4.32 ± 0.03 4.0±0.34 198.48±1.74 0.41±0.02 98.14 ± 0.73

F6 4.30 ± 0.05 3.9±0.30 200.64±1.43 0.44±0.01 99.24 ± 0.45

F7 4.31 ± 0.01 4.1±0.24 201.55±1.50 0.32±0.03 99.44 ± 0.65

F8 4.28 ± 0.02 4.2±0.28 198.48±1.56 0.49±0.01 99.81 ± 0.53

F9 4.35± 0.01 4.0±0.38 195.51±1.48 0.46±0.02 99.10± 0.46

F10 4.33± 0.03 3.8±0.41 200.66±1.52 0.45±0.04 98.46± 0.78

F11 4.30± 0.01 4.2±0.53 196.45±1.62 0.51±0.01 99.29± 0.83

F12 4.32± 0.03 4.1±0.23 198.68±1.32 0.49±0.02 98.17± 0.54

F13 4.31± 0.01 3.9±0.45 200.51±1.48 0.53±0.03 99.39± 0.68

F14 4.26 ± 0.03 4.0±0.53 201.66±1.53 0.42±0.01 98.58 ± 0.45

F15 4.28± 0.01 4.1±0.63 198.40±1.46 0.53±0.02 99.65± 0.72

F16 4.33± 0.03 4.2±0.42 196.64±1.53 0.38±0.03 99.45± 0.63

F17 4.31± 0.02 4.0±0.52 197.47±1.71 0.35±0.05 99.81± 0.38

F18 4.32± 0.01 3.8±0.35 195.60±1.54 0.49±0.01 99.32± 0.42

F19 4.28 ± 0.03 4.1±0.43 200.41±1.43 0.32±0.03 99.61± 0.53

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Code Thickness (mm) Hardness

test(kg/cm2)

Weight variation

(%) Friability Drug content (%)

F20 4.30 ± 0.01 4.2±0.33 196.56±1.52 0.52±0.05 99.17± 0.45

F21 4.31± 0.02 4.0±0.36 201.42±1.63 0.38±0.01 99.24± 0.43

F22 4.30± 0.03 3.8±0.42 197.70±1.35 0.52±0.03 98.39± 0.54

F23 4.28± 0.01 4.0±0.28 200.61±1.71 0.35±0.01 98.42± 0.63

F24 4.31 ± 0.01 3.8 ± 0.35 200.47±1.53 0.31 ± 0.01 97.75 ± 0.34

F25 4.28 ± 0.03 4.0 ± 0.43 197.64±1.34 0.45 ± 0.03 99.26 ± 0.54

F26 4.26 ± 0.01 4.1 ± 0.56 201.55±1.72 0.51 ± 0.03 97.09 ± 0.72

F27 4.28 ± 0.02 4.2 ± 0.63 199.60±1.65 0.34 ± 0.02 98.23 ± 0.36

F28 4.33 ± 0.03 3.9 ± 0.52 200.58±1.42 0.33 ± 0.05 99.03 ± 0.73

Table 6. Comparison of wetting time, water absorption ratio and disintegration time of tablets

Code Wetting time

(sec) Water absorption ratio

Disintegration time

(sec)

F1 24.23 ± 1.1 68.23.± 1.3 27.58 ± 1.5

F2 20.11 ± 1.2 71.50 ± 1.8 24.18 ± 1.3

F3 17.05 ± 1.6 78.51.± 1.2 22.12 ± 1.1

F4 13.18 ± 1.8 80.48 ± 1.6 17.10 ± 1.2

F5 29.16 ± 1.3 65.00 ± 1.1 32.05 ± 1.4

F6 25.08 ± 1.4 67.33 ± 1.3 29.14 ± 1.1

F7 22.28 ± 1.3 71.45 ± 1.1 27.14 ± 1.2

F8 18.10 ± 1.1 76.56 ± 1.0 22.35 ± 1.8

F9 40.31 ± 1.8 68.32 ± 1.3 43.08 ± 1.2

F10 33.17 ± 1.3 72.16 ± 1.4 37.11 ± 1.1

F11 28.25 ± 1.5 70.36 ± 1.3 33.18 ± 1.8

F12 23.21 ± 1.4 67.23 ± 1.1 27.18 ± 0.9

F13 41.18 ± 1.2 58.28 ± 1.5 45.18 ± 1.3

F14 37.12 ± 1.7 54.52 ± 1.3 41.12 ± 1.4

F15 32.15 ± 1.3 53.28± 1.5 35.15 ± 1.2

F16 27.32± 1.1 56.34± 1.0 31.32± 1.5

F17 49.15 ± 1.4 53.28.± 1.2 53.14 ± 1.6

F18 43.23± 1.5 51.63± 1.2 47.12 ± 1.3

F19 37.18± 1.2 71.48 ± 1.1 42.16 ± 1.2

F20 33.02± 1.1 70.24± 1.6 37.08 ± 1.0

F21 50.17± 1.3 68.56± 1.2 53.17 ± 1.4

F22 46.21± 1.6 70.21± 1.3 50.21 ± 1.5

F23 41.16 ± 1.2 69.44 ± 1.1 44.05 ± 1.1

F24 37.08 ± 1.0 67.33 ±1.5 41.12 ± 1.3

F25 58.17 ± 1.4 68.38 ±1.3 61.16 ± 1.4

F26 51.21 ± 1.5 66.21 ±1.1 55.36 ± 1.2

F27 46.16 ± 1.2 64.09 ±1.9 50.18 ± 1.3

F28 42.03 ± 1.7 80.76 ±1.7 46.08 ± 1.7

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Fig 8. Effect of concentration of superdisintegrants on disintegration time and wetting time of fast disintegrating tablet

Table 7. In vitro release data of Granisetron HCl from the tablets Containing Natural Superdisintegrants

Time

(min) F1 F2 F3 F4 F5 F6 F7 F8 F9 F10 F11 F12

0 0 0 0 0 0 0 0 0 0 0 0 0

0.5 4.01 9.37 13.39 20.08 2.67 5.35 10.71 14.73 1.33 4.01 6.696 12.05

1 15.34 20.70 26.06 34.09 12.67 16.68 22.04 30.08 9.99 14.01 19.36 24.72

1.5 27.48 32.87 39.59 50.35 22.11 27.49 34.21 43.63 18.08 23.45 31.52 38.25

2 39.68 47.78 57.22 66.70 31.60 39.69 49.13 61.28 27.55 34.30 41.07 51.85

2.5 50.61 60.09 69.59 83.13 39.81 50.62 60.11 76.35 34.39 42.52 49.33 62.84

3 61.60 73.81 87.38 99.66 52.08 61.61 72.49 88.82 42.61 50.78 58.97 71.22

3.5 72.65 86.27 99.91 --- 64.41 74.00 83.60 98.68 49.54 60.43 68.66 79.65

4 83.76 98.79 --- --- 76.82 85.11 97.45 --- 57.84 70.14 79.75 88.11

4.5 98.95 --- --- --- 87.95 96.29 --- --- 66.19 78.55 88.22 97.96

5 --- --- --- --- 97.80 --- --- --- 75.93 87.01 96.73 ---

5.5 --- --- --- --- --- --- --- --- 83.03 98.19 --- ---

6 --- --- --- --- --- --- --- --- 91.51 --- --- ---

6.5 --- --- --- --- --- --- --- --- 98.70 --- --- ---

Table 8. In vitro release data of Granisetron HCl from the tablets containing Synthetic Superdisintegrants

Cumulative release data (%)

Time(Min) F13 F14 F15 F16 F17 F18 F19 F20

0 0 0 0 0 0 0 0 0

0.5 9.37 10.71 12.05 13.39 6.69 8.03 9.37 10.71

1 16.68 20.70 23.38 26.06 12.67 15.34 18.02 20.70

1.5 24.81 27.51 30.20 34.24 19.43 23.46 27.49 31.53

2 31.64 35.69 38.40 42.46 24.89 30.29 34.34 37.06

2.5 37.17 42.58 45.31 48.05 31.72 35.81 41.22 43.95

3 44.06 48.17 52.25 53.66 35.91 41.36 46.80 49.55

3.5 48.32 52.45 56.55 60.65 40.12 45.60 52.41 55.17

4 52.60 56.75 60.87 64.99 45.69 49.86 56.71 59.49

4.5 56.90 61.07 65.22 69.36 49.96 55.49 61.04 63.83

5 61.22 65.42 70.93 75.09 55.58 59.80 65.38 69.53

5.5 65.57 71.13 76.66 80.85 59.90 64.14 71.09 75.26

6 71.27 76.86 82.43 86.64 65.58 71.18 76.83 81.01

6.5 77.01 82.63 88.22 92.46 71.28 75.58 81.25 88.14

7 82.78 88.43 92.71 99.65 75.68 81.33 87.04 93.97

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Time(Min) F13 F14 F15 F16 F17 F18 F19 F20

7.5 87.23 92.91 98.56 --- 81.44 87.12 92.86 98.48

8 91.71 97.42 --- --- 87.23 92.94 98.71 ---

8.5 97.55 --- --- --- 93.05 97.45 --- ---

9 --- --- --- --- 97.55 --- --- ---

9.5 --- --- --- --- --- --- --- ---

10 --- --- --- --- --- --- --- ---

Table 9. In vitro release data of Granisetron HCl from the tablets containing synthetic superdisintegrants

Cumulative release data (%)

Time(Min) F21 F22 F23 F24 F25 F26 F27 F28

0 0 0 0 0 0 0 0 0

0.5 4.017 5.35 6.69 8.03 1.33 2.67 4.017 5.35

1 8.65 11.33 14.01 18.02 7.31 8.65 9.99 12.67

1.5 12.71 16.74 19.44 24.82 12.70 14.05 16.74 19.43

2 19.47 23.53 27.58 32.99 18.13 20.82 24.86 26.23

2.5 26.27 30.35 34.42 38.52 20.90 26.29 30.35 33.07

3 31.77 35.87 39.97 44.09 26.37 30.45 34.53 37.26

3.5 37.30 41.42 45.54 49.68 29.19 34.63 40.08 42.82

4 42.86 47.00 51.14 55.31 33.37 38.83 45.65 48.41

4.5 47.11 52.61 56.77 60.96 38.90 45.74 49.91 54.03

5 52.72 58.25 61.10 65.31 44.47 50.00 55.54 59.68

5.5 58.36 62.58 65.44 69.68 48.72 54.29 59.85 64.01

6 62.69 66.94 69.81 75.40 55.68 59.94 65.53 68.37

6.5 67.04 71.31 75.54 81.16 61.33 66.95 72.58 75.43

7 71.42 75.71 81.30 86.95 67.02 72.67 76.98 79.85

7.5 77.15 81.47 88.43 92.77 72.73 78.41 82.75 86.97

8 82.92 87.26 94.25 99.96 78.48 84.18 89.88 92.79

8.5 88.72 93.08 98.77 --- 82.91 88.65 94.38 97.30

9 93.20 97.58 --- --- 87.37 94.47 98.89 ---

9.5 97.71 --- --- --- 91.85 98.99 --- ---

10 --- --- --- --- 97.69 --- --- ---

Fig 9. In-vitro release profile of fast disintegrating tablet of Granisetron HCl in phosphate buffer6.8pH

Effects of 2 %super disintegrants

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Fig 10. In-vitro release profile of fast disintegrating tablet of Granisetron HCl in phosphate buffer 6.8 pH (Effects of 3

%super disintegrants)

Fig 11. In-vitro release profile of fast disintegrating tablet of Granisetron HCl in phosphate buffer 6.8 pH (Effects of 4

%super disintegrants)

0

20

40

60

80

100

0 1 2 3 4 5 6 7 8 9 10

cum

mu

lati

ve

%re

lease

time(min)

plantago

ovata

gum

karaya

Fig 12. In-vitro release profile of fast disintegrating tablet of Granisetron HCl in phosphate buffer 6.8 pH (Effects of 5

%super disintegrants)

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Table 10. In vitro release of selected fast disintegrating tablets of Granisetron HCl (F4) and marketed product

Fig 13. In vitro release profile of selected fast dissolving tablet (F4) and marketed tablet

Table 11. Stability data of selected tablets (F4) after one month study

Tablet Drug content* (%) Disintegration time* (sec) T50% (min) * T90% (min)*

Before(F4) 99.28± 0.63 17.10 ± 1.2 1.5±0.1 2.7 ± 0.5

After (F4) 99.12± 0.16 16.10 ± 1.4 1.4± 1.4 2.6± 0.4

Fig 14. In vitro release profile of selected tablets after stability study

Formulation F4 Marketed tablet

Time

(min)

Conc. of drug

(mg) Cumulative Data

Conc. of drug

(mg) Cumulative Data

5ml 900 ml

Loss of

drug

(mg)

Release of

drug (mg)

% drug

released

*

5ml 900 ml Loss of

drug (mg)

Release of

drug (mg)

% drug

released*

0 0 0 0 0 0 0 0 0 0 0

0.5 0.0022 0.4017 0 0.4017 20.08 0.002 0.402 0 0.402 20.090

1 0.0037 0.6696 0.0123 0.6819 34.09 0.004 0.696 0.012 0.709 35.439

1.5 0.0055 0.9910 0.0160 1.0071 50.35 0.005 0.937 0.016 0.954 47.686

2 0.0072 1.3125 0.0215 1.3340 66.70 0.006 1.152 0.021 1.173 58.660

2.5 0.0090 1.6339 0.0288 1.6627 83.13 0.008 1.366 0.028 1.394 69.695

3 0.0108 1.9553 0.0379 1.9933 99.66 0.009 1.553 0.035 1.589 79.450

3.5 ------ ------ ------ ------ ------ 0.010 1.767 0.044 1.812 90.595

4 ------ ------ ------ ------ ------ 0.011 1.928 0.054 1.982 99.122

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RESULTS AND DISCUSSION

Weight variation test: It was determined as per B.P.

procedure & Complies with specification.

Friability test: Results complies with B.P. as the % losses

NMT 1.0% at both 100 revolutions.

Thickness: was found to be 4.33mm for F4, indicating that

tablets are suitable packing.

Hardness: it is in the range of 4.2 Kg/cm2 indicating that

the tablets are mechanically strong.

Disintegration test: the disintegration time of F4

formulation was found to be 17.10 sec.

Dissolution Studies: indicates that F4 was superior to other

formulations and shows drug relese of 99.66% in 3 min

time.

Drug- excipient compatibility studies: FTIR studies

indicated that there was no interaction with the excipients.

Stability studies: it was conducted for the F4 formulation at

specified temp for 60 days and found that all the parameters

were within the specification limit.

CONCLUSION From the results obtained, it can be concluded that

formulation F-4 has achieved the objective of drug release

when compared with marketed formulation containing

synthetic superdisintegrants. This shows that natural

superdisintegrants is more suitable than synthetic and

recommended for long term stability testing.

REFERENCES 1. Biradar SS, Bhagavati ST, Kuppasad IJ. Fast Dissolving Drug Delivery Systems. The Internet Journal of Pharmacology, 4,

2006, 2.

2. Doijad RC, Manvi FV, Dada Khalandar KS. A comparative study on mouth dissolving tablets of Granisetron with different

super disintegrants: Formulation and Evaluation. The Inter Journal of Pharmacology, 5, 2008, 2.

3. Kumar ND, Raju SA, Shrisand SB, Para MS. Formulation design of novel fast dissolving tablets using low and high

compressible saccharides. IJPRIF, 1(4), 2009, 1585-88.

4. Swamy PV et al. Design and evaluation of buccoadhesive bilayer tablets of granisetron hydrochloride. IJPSR, 1(8), 2010,

104-10.

5. Chakraborty S et al. Comparative study on effect of natural and synthetic superdisintegrants in the formulation of fast

dissolving tablets. International Journal of Green Pharmacy, 2(1), 2008, 25-5.