This document describes the formulation and evaluation of oral disintegrating tablets of sumatriptan succinate using superdisintegrants. Sumatriptan succinate tablets were prepared using different concentrations of Croscarmellose sodium and treated agar as superdisintegrants. The tablets were evaluated for various physical properties and drug release. Treated agar at 7.5% concentration showed the fastest disintegration time and wetting time compared to other formulations. The results indicate that treated agar provided better superdisintegrant properties than Croscarmellose sodium for formulating oral disintegrating tablets of sumatriptan succinate.

1. Formulation and Evaluation of Sumatriptan Succinate Oral
Disintegrating Tablets Using Super Disintegrants
In the partial fulfillment of the requirements for the award of the
degree of
BACHELOR OF PHARMACY
By
P.V.SIVA KRISHNA (Y15PH2056)
Under The Guidance of
Lakshmana Rao P M.Pharm(Ph.D)
Department of Pharmaceutics

2. CONTENTS
Introduction
Aim and Objectives
Drug and excipient Profiles
Methodology
Results and Discussion
Conclusion
Bibliography

3. INTRODUCTION
The oral route of administration continue to be the most
preferred route due to its manifold advantages including ease of
ingestion, pain avoidance, versatility and most importantly patient
compliance. The most popular dosage forms are tablets and capsules,
however geriatric patients may have difficulty in swallowing and/or
chewing resulting in non compliance and ineffective therapy.
To overcome these problems, oral disintegrating tablets (ODT) are a
good alternative since they disintegrate and dissolve rapidly in saliva
without need for drinking water. . Although the primary benefit of ODT
is to improve patient compliance, yet other benefits such as accuracy of
dosage, rapid onset of action and increase in bioavailability may be
accomplished.

4. AIM AND OBJECTIVES
In the present study an attempt will be made to design oral disintegrating
tablets of Sumatriptan succinate (anti migraine) by using treated agar and
Croscarmellose sodium as a superdisintigrants with a view to provide a
convenient means of administration to those patients suffering from
difficulties in swallowing such as pediatric and geriatric patients and
uncooperative mentally ill patients.
The objectives of the research work undertaken are as follows:
To formulate oral disintegrating tablets of Sumatriptan succinate using treated agar
and Croscarmellose sodium as a superdisintegrants in different ratios by direct
compression technique.
To study the physical characteristics of the individual drug by FTIR spectroscopy
and the optimized formulations by FTIR spectroscopy.
To evaluate various pre-compressional parameters of tablet blend
To evaluate various characteristics of the resulting tablets.
To evaluate the drug content and to perform in-vitro drug release study.

5. DRUG PROFILE
SUMATRIPTAN
Description: Sumatriptan is a white to almost white powder that is
readily soluble in water.
Molecular formula: C14H21N3O2S
Molecular weight: 295.401 g/mol
Class: Anti migraine
Structure:
Fig.No.5.1: structure of sumatriptan

6. IUPAC Name:
1-[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]-N-
methylmethanesulfonamide
Bio availability: Approximately 60%
Absorption: Mean absolute oral bioavailability is approximately 40%.
Food has no affect on the rate and extent of absorption.
Volume of distribution: 8.4±3.3 L/kg
Protein binding: 25%
Half life: The mean elimination half-life of Sumatriptan and of the active
N-desmethyl metabolite is 3 hours.
Mechanism of action:
Sumatriptan binds with high affinity to human 5-HT1B and 5-HT1D receptors leading to
cranial blood vessel constriction. The therapeutic activity of Sumatriptan for the
treatment of migraine headache can most likely be attributed to the agonist effects at the
5HT1B/1D receptors on intracranial blood vessels (including the arterio-venous
anastomoses) and sensory nerves of the trigeminal system which result in cranial vessel
constriction and inhibition of pro-inflammatory neuropeptide release.
Dose: 2.5mg, 10mg

7. Uses of Sumatriptan
• Vascular headaches
• Acute treatment of migraine attacks with or without aura.
• Not recommended for management of hemiplegic or basilar migraine
or for prophylaxis of migraine.
EXCIPIENT PROFLE
CELLULOSE, MICROCRYSTALLINE
Microcrystalline cellulose
JP: Microcrystalline cellulose
PhEur: Cellulosum microcristallinum
USPNF: Microcrystalline cellulose
LACTOSE, ANHYDROUS
BP: Anhydrous lactose
JP: Anhydrous lactose
PhEur: Lactosum anhydricum
USPNF: Anhydrous lactose

8. MATERIALS AND METHODS
Sumatriptan succinate was obtained as a gift sample from Pharmatrai, Hyderabad. Agar
was obtained from Merck specialties Pvt. Ltd, Mumbai. Croscaramellose sodium,
anhydrous Lactose and other excipients were obtained as a gift sample from Kawarlal
Exicipients limited, Chennai. All other materials used were of pharmacopoeial grade.
Methods
Preparation of Standard Graph:
Accurately weighed 100mg of drug was dissolved in small amount of 6.8 pH phosphate
buffer and volume was made up to the mark with phosphate buffer to get a
concentration of 1000 μg/ml (stock-I). The stock-I solution was further diluted to get a
solution of concentration 20 µg/ml (stock-II).From the stock-II, a series of dilutions
containing 2, 4, 6, 8& 10 µg/ml of drug. The absorbance of the above dilutions was
measured using a UV spectrophotometer at 226 nm using phosphate buffer as blank.
The method obeyed Beer,s Lamberts law in the concentration range of 0-10 µg/ml. No
interference by the excipients used in the study was observed.

9. Preparation of Sumatriptan succinate Tablets:
Sumatriptan Succinatetablets were prepared by direct compression method as per the
formula given in Table 2.
The required quantities of drug, Croscarmellose Sodium and Treated Agar as per the
formula in each case were blended thoroughly in a closed polyethene bag. Aerosil and
magnesium stearate were then added by passing through mesh no.80 and blended. The
blend of ingredients was then compressed directly into tablets using CADMACH 16
station tablet punching machine, equipped with round and flat punches of 8 mm
diameter.
Table 1: Calibration Curve of Sumatriptan succinate in 6.8 pH Phosphate Buffer
Concentration(µg/ ml) Absorbance
0 0
2 0.206
4 0.398
6 0.656
8 0.842
10 9.891

10. Table 2: Fomulae of Sumatriptan Succinate Tablets Prepared
employing Croscarmellose Sodium and Treated Agar as
Superdisintegrants
Ingredients CCS1 CCS2 CCS3 TA1 TA2 TA3
Sumatriptan Succinate 5 5 5 5 5 5
Lactose Anhydrous 86.5 84 81.5 86.5 84 81.5
Croscarmellose Sodium 2.5 5 7.5 --- --- ---
Treated Agar --- --- --- 2.5 5 7.5
Sodium Sacharin 1.5 1.5 1.5 1.5 1.5 1.5
Aerosil 3 3 3 3 3 3
Magnesium Stearate 1.5 1.5 1.5 1.5 1.5 1.5
Total Weight 100 100 100 100 100 100

11. RESULTS AND DISCUSSIONS
y = 0.105x
R² = 0.999
0
0.2
0.4
0.6
0.8
1
1.2
0 2 4 6 8 10 12
Absorbance
Conc. (µg/ml)
Calibration Curve of Sumatriptan Succinate with 6.8pH Phosphate
Buffer
Fig.No.1: Calibration Curve of Sumatriptan Succinate with 6.8pH
Phosphate Buffer Drug-excipients Compatibility studies

12. Formulations* Average Weight* Hardness *Kg/cm2 Friability *(%) Water
absorption ratio*
CCS1 98±0.12 3.6±0.11 0.481±0.16 39±0.14
CCS2 98±0.21 3.6±0.24 0.56±0.17 28±0.15
CCS3 99.8±1.8 3.5±0.49 0.57±0.17 34±0.24
TAG1 98±0.16 3.2±0.2 0.31±0.16 51±0.13
TAG 2 99±0.87 3.4±0.32 0.30±0.22 54±0.17
TAG 3 99±0.87 3.6±0.32 0.295±0.22 54±0.17
Table 4: Evaluation of ODT for formulations
* Data represent mean ±SD (n=3)

13. Formulations
Cumulative % drug dissolved (mins)
0 2.5 5 10 15 20
CCS1 0 38±0.26 61±0.35 75±0.92 88±0.24 94±0.31
CCS2 0 40±0.12 63±0.95 77±0.7 89±0.24 95±0.71
CCS3 0 52±0.21 72±0.31 80±0.12 90±0.21 96±0.11
Table 7: Dissolution profile of Sumatriptan succinate ODTs with
Croscarmellose Sodium
* Data represent mean ±SD (n=3)

14. Comparative dissolution profile of Sumatriptan succinate ODTs
containing different concentrations of Treated Agar as a natural
superdisintegrant.
0
20
40
60
80
100
120
0 5 10 15 20 25
%CumulativeDrugRelease
Time in mins
TAG1 TAG 2 TAG 3

15. DISCUSSIONS
The main objective of this research work was to formulate and evaluate the oral
disintegrating tablets of sumatriptan succinate using superdisintegrants. The FT-IR
represents the peaks of the sumatriptan succinate functional groups. These peaks were
not affected, they were prominently observed in IR-spectra of sumatriptan succinate
along with Croscarmellose Sodium, Treated agar etc.The spectral details of the drug
and the excipients shown in (Table.3) and (Figure.2-5).
For each formulation blend of drug and excipients were prepared and evaluated for
various precompression parameters like angle of repose, bulk density, tapped density,
carr’s index and Hausner’s ratio. The powder blend of all the formulations had
Hausner’s ratio of 1.12 indicating good flowability. The carr’s index was found to be
between 7.6-15.84% indicating fairly good flowability of the blend. The good
flowability of blend was also made evident with angle of repose values (31˚-37˚) which
is below 40˚ indicating good flowability. Since the powder material was free flowing
and used for the direct compression.
The tablets were prepared by direct compression technique and evaluated for
different post compression parameters. The hardness & Friability of the tablets
was found to be 3.2±0.2 to 3.6±0.32 and 0.295±0.22 to 0.57±0.17, all values
were found to be within the limits.

16. The wetting time of the formulations was found to be 10 ±0.12 to 20±0.13secand the
disintegration time was ranging from 12 ±0.55 to 24±0.45 seconds. The wetting time
and disintegration time both are less for the formulation containing treated agar (7.5%
w/w) as a modified superdisintegrant. The dissolution profile of all the formulations
was shown in the table 7.6 and in fig 7.5 & 7.6. The formulation with Treated Agar
(TAG3) shows faster disintegration and wetting time than formulation with
croscaramellose sodium. The order of enhancement of dissolution rate with various
superdisintegrants was found to be Treated Agar˃ croscaramellose sodium.

17. CONCLUSION
The above results suggest that the formulated oral disintegrating tablets
of sumatriptan succinate exhibited good physical parameters and rapidly
disintegrating without affecting the release profile and is very effective in
case of elderly and pediatric patients. The overall results indicated that
formulation with Treated Agar (7.5%) had a higher edge compared to
other formulations containing croscaramellose sodium. They satisfied all
the criteria for oral disintegrating tablets. This direct compression
process is simple, reproducible and robust to prepare orally
disintegrating tablets of sumatriptan succinate and other anti-migraine
drugs.

18. REFERENCES
Rangasamy Manivannan. Oral disintegrating tablets: A future Compaction Publication International Journal of
Pharmaceutical Research and Development 2009; 1: 1-10.
https://pubchem.ncbi.nlm.nih.gov/compound/sumatriptan
Mishra DN, Bindal M, Singh SK. Rapidly disintegrating oral tablet of valdecoxib. Indian drug. 2004; 41: 554.
Kaushik D, Dureja H, Saini TR. Mouth dissolving tablets: A review. Indian Drugs.2004; 41: 503-508.
Ansel HC, Popovich NG, Allen LV.Pharmaceutical dosage forms and drug delivery system. B.I. Waverly Pvt. Ltd,New
Delhi. 1995; 6:99-154.
Udaykumar.M, A.B.N.Nageswarao, T.V.S VinayKumar, Fast dissolving Tablets:
New-fangled DrugDelivery System A Comprehensive review, InternationalJournal
of Research in Drug Delivery, 2012, 2(3), Page:15-25.
Lachman L, Liberman H and Kanig J. In: The theory and practice of industrial pharmacy, 3rdedn. Varghese Publishing
House, Mumbai 1987.
Yunxia B, Sunada H, Yonezawz Y, DanjoK.Evaluation of rapidly disintegrating tablets prepared by direct compression
method. Drug Dev. Ind. Pharm. 1999; 25(5), Page: 571-581.
Patel D, Patel N. Studies in formulation of orodispersible tablets of rofecoxib. Indian J. Pharm. Sci. 2004, Vol.66, Issue
.5, Page: 621-625.
Khan S, Kataria P, Nakhat P, Yeole P. Taste masking of ondansetron hydrochloride by polymer carrier system and
formulation of rapid disintegrating tablets. AAPS PharmSciTech. 2007, 8(2), Article.46.
Late SG, Yi-Ying Y, Banga AK. Effect of disintegration promoting agent, lubricants and moisture treatment on
optimized fast disintegrating tablets. Int J Pharm 2009; 365(1-2), Page: 4-11.
Gohel MC, Bansal G, Bhatt N. Formulation and evaluation of orodispersible taste masked tablets of famotidine.
PharmaBiol World 2005; (3), Page: 75-80.
SudhirBharawaj, Vinay Jain, ShaileshShar, Orally Disintegrating Tablets: A Review, Drug Invention Today 2010,
Vol.2, Issue.1, Page: 81-88.