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1. FORMULATION AND EVALUATION OF FAST
DISSOLVING TABLET

2. SEMINAR REPORT ON
FAST DISSOLVING TABLET
DOMPERIDONE
BY
PAVULURI RAJA RAJESWARA RAO
MOHAMMED SUFIYAN AHMED
MOHAMMED MUDASSIR
KHAJA FAHEEMUDDIN
MOHAMMED ALTAF ALI
UNDER THE GUIDANCE OF
Mrs. K GOUTHAMI
(Assit. Proff in department of pharmaceutics)
DEPARTMENT OF
PHARMACEUTICS
SHADAN COLLEGE OF PHARMACY

3. CONTENTS
 INTRODUCTION
 LITERATURE
 OBJECTIVE
 PLAN OF WORK
 DRUG PROFILE
 EXCIPIENT PROFILE
 MATERIALS
 METHODOLOGY
 RESULTS AND DISCUSSION
 CONCLUSION
 REFERENCES

4. INTRODUCTION

5.  DEFINATION OF FAST DISSOLVING TABLETS :
A fast disintegrating tablet can be defined as a solid dosage form
that can disintegrate or dissolve within 30 seconds, in the oral
cavity resulting in a solution or suspension without
administration of water.
 REQUIREMENTS OF FAST DISINTEGRATING
TABLET:
 Require no water for oral administration
 Have a pleasing mouth feel.
 Have an acceptable taste masking property.
 Be optimum harder and less friable

6.  ADVANTAGES :
 Ease of administration to patients who refuse to swallow a
tablet, such as pediatric and geriatric patients and psychiatric
patients.
 No need of water to swallow the dosage form.
 Rapid dissolution and absorption of drug
 Convenience of administration and accurate dosing as
compared to liquids.
 Good mouth feel property helps to change the basic view of
medication as "bitter pill", particularly for pediatric patients.
 DISADVANTAGES:
 The disadvantage of most ODT is that they are fragile
and brittle.
 It needs special package for protection during storage
and transportation.

7.  CHARACTERISTICS OF FAST DISINTEGRATING
SYSTEMS
a) Ease of administration
b) Taste of the medicament
c) Hygroscopicity
d) Friability
e) Mouth feel
 PREPARATION METHODS OF FAST
DISSOLVING TABLETS
 Freeze drying
 Molding
 Sublimation
 Spray Drying
 Direct Compression
 Melt granulation
 Phase transition process ETC.

8. S.
NO.
TRADE NAME
ACTIVE
DRUG
MANUFACTURER
1.
Felden fast
melt
Piroxicam Pfiser Inc., NY, USA
2.
Claritin redi
Tab
Loratidine
Schering plough
Corp., USA
3.
Maxalt MLT Rizatriptan
Merck and Co., NJ,
USA
4.
Zyprexia Olanzapine
Eli lilly, Indianapolis,
USA
5.
Pepcid RPD Famotidine
Merck and Co., NJ,
USA
6.
Zofran ODT Ondansetron
Glaxo Wellcome,
Middlesex, UK
7.
Zoming-ZMT Zolmitriptan
AstraZeneca,
Wilmington, USA
8.
Zeplar TM Selegilline
Amarin Corp.,
London, UK
9.
Tempra
Quiclets
Acetaminoph
en
Bristol myers Squibb,
NY, USA
10.
Febrectol Paracetamol
Prographarm,
Chateauneuf, France
List of Marketed Fast Dissolving Tablets

9.  Mechanism of tablet disintegration:
 Capillary action (Wicking).
 Swelling.
 Due to disintegrating particle/particle repulsive
forces.
 Due to deformation.
 Due to release of gases.

10. LITERATURE
SURVEY

11. LITERATURE REVIEW
 Sharma Shailesh*, Singh Gurjeet and Gupta GD.,
developed mouth dissolve tablets of domperidone. Tablet
containing domperidone, camphor and crospovidone were
prepared by direct compression technique.
 Baria A.H et. al
develop a formulation for this drug which overcomes problems
such as difficulty in swallowing, inconvenience in administration
while traveling and better compliance.
 Vikas Sharma, vandana aurora, Chandra ray
developed the fast disintegrating tablets with improved
patient compliance and convenience.

12.  Himanshu Deshmkh et. al
development of numerous formulations with improved
performance and acceptability.
 SHAILESH SHARMA et. al., (2011)
prepared and evaluated the co processed superdisintegrant in
promoting tablet disintegration and having low friability.
 BIRAJU PATEL et. al., (2009)
fast dissolving tablets of glipizide were prepared by direct
compression method with a view to enhance patient compliance.
Two superdisintegrants via, crospovidone and croscarmellose
sodium (4%, 5%, 6%) with different binders viz, pvp k-30 and
pregelatinized starch (3%) were used.
 P.S.Kawtikwaret et al., (2009)
formulated, evaluated and optimized the fast dissolving tablets
containing tizanidine hydrochloride by using different
superdisintegrants like sodium starch glycolate, croscarmellose
sodium and crospovidone.

13. OBJECTIVE

14. OBJECTIVE OF THE STUDY
 The concept of Fast dissolving drug delivery system is to provide
patient with conventional means of taking their medication
 In some cases such as motion sickness, sudden episodes of
allergic attacks or coughing and unavailability of water, swallowing
conventional tablets may be difficult.
 Such problems can be resolved by means of Fast dissolving tablets
when put on tongue these tablets disintegrate and dissolve rapidly in
saliva without need of drinking water.
 Some drugs are absorbed from the mouth, pharynx and esophagus
as saliva passes down into the stomach.
 In such cases, bioavailability of drug is significantly greater than
those observed from conventional tablets dosage form.

15. PLAN OF
WORK

16. 1. Literature survey
2. Selection of drug and superdisintegrants
3. Determination of analytical methodology for Domperidone
a. Standard graph of Domperidone in 6.8 pH buffer
4. Preformulation studies
5. Preparation of Domperidone fast disintegrating tablets using direct
compression method
6. Evaluation of prepared tablets
a.Weight variation
b.Thickness
c. Hardness
d. Friability
e.Wetting time
f.Water absorption ratio
g. In-vitro disintegration test
h. Content uniformity
i. In-vitro release studies
8. Selection of optimized formulation based on evaluation parameters.

17. DRUG PROFILE

18. Name: Domperidone
Description: A specific blocker of dopamine receptors. It speeds
gastrointestinal peristalsis, causes prolactin release,
and is used as antiemetic and tool in the study of
dopaminergic mechanisms.
Structure:
IUPAC Name: 5-chloro-1-{1-[3-(2-oxo-2,3-dihydro-1H-1,3-
benzodiazol-1-yl)propyl]piperidin-4-yl}-2,3-dihydro-1H-1,3-
benzodiazol-2-one

19. Chemical Formula: C22H24ClN5O2
Molecular weight: 425.911
CLINICAL PHARMACOLOGY:
 Domperidone is a D2 dopamine receptor antagonist that blocks the
agonistic action of fescue alkaloids at the cellular level
 does not readily cross the blood-brain barrier
 In humans, domperidone is 91-93% bound to plasma proteins.
 undergoes rapid and extensive hepatic metabolism by hydroxylation
and N-dealkylation.
 Urinary and feacal excretions of domperidone in humans amount 31
and 66% of the oral dose,
 plasma half-life of domperidone administered orally is 6 hours with
low oral bioavailability
Pharmacodynamics:
 a specific blocker of dopamine receptors.
 speeds gastrointestinal peristalsis, causes prolactin release, used as
antiemetic

20. Mechanism of Action
 Domperidone acts as a gastrointestinal emptying (delayed) adjunct
and peristaltic stimulant.
 decreases small bowel transit time by increasing esophageal and
gastric peristalsis and by lowering esophageal sphincter pressure.
 generally related to its dopamine receptor blocking activity.
 It has strong affinities for the D2 and D3 dopamine
receptors, located just outside the blood brain barrier, that regulates
nausea & vomiting
Indications
 management of dyspepsia, heartburn, epigastric pain, nausea, and
vomiting.
 For oral dosage form (tablets):
 Treatment of GI motility disorder
• Adults—10 mg three to four times daily. Some patients may require
higher doses up to 20 mg three or four times daily.
 Nausea and vomiting:
• Adults—20 (mg) three to four times daily.

21. Uses of Domperidone :
 increases the contractions of stomach & bowel
 treat nausea and vomiting
 given only by or under the immediate supervision of your doctor.
Storage conditions:
• Store the medicine in a closed container at room temperature, away
from heat, moisture, and direct light. Keep from freezing.
• keep away from children
• don’t keep outdated medicine.

22. EXCIPIENTS PROFI

23. Croscarmellose sodium (CCS)
Chemical name: Cellulose, carboxymethyl ether, sodium salt, cross
linked.
Functional category: Tablet and capsule disintegrants
Structural formula:
Molecular weight: 90,000-700,000
Applications in pharmaceutical formulation or
technology:
 used in oral pharmaceutical formulations as a disintegrant
 used in both direct-compression and wet-granulation processes.
Description: odourless, white or grayish white powder.
Solubility: Insoluble in water,soluble in acetone, ethanol , toulene
Uses: used in oral pharmaceutical formulation as a disintegrants

24. Crospovidone
Chemical Name and CAS Registry Number
1-Ethenyl-2-pyrrolidinone homopolymer [9003-39-8]
Structural Formula
Functional Category : Tablet disintegrant.
Applications in Pharmaceutical Formulation or
Technology
 water-insoluble tablet disintegrant and dissolution agent
 solubility enhancer for poorly soluble drugs
Description: white to creamy-white, finely divided, free-flowing,
tasteless, odorless or nearly odorless, hygroscopic powder.
Stability and Storage Conditions: crospovidone is hygroscopic,
it should be stored in an airtight container in a cool, dry place.

25. Magnesium stearate
Chemical name: Octadecanoic acid magnesium salt.
Structural formula: [CH3 (CH2)16COO] 2Mg.
Functional category: Tablet and capsule lubricant.
Applications in pharmaceutical formulation or
technology:
 used in cosmetics, foods, and pharmaceutical formulations.
 primarily used as lubricant in tablets and capsule formation.
Description: very fine, light white, precipitated , faint odour of
steric acid & characteristic in taste.
Melting range: 117–1500C (commercial samples), 126–1300C (high
purity magnesium stearate).
Solubility: insoluble in ethanol, ether & slight soluble in warm
benzene

26. MATERIALS AND
EQUIPMENTS
SISCO

27. S.
NO
EQUIPMENT NAME
SOURCE
1
DIGITAL WEIGHING
MACHINE
SHIMADZU ATY 244
2
TABLET COMPRESSION
MACHINE
KARNAVATHI
MINI PRESS-I
3
MONSANTO HARDNESS
TESTER
CINTEX IND.
CORPORATION, MUMBAI
4 FRIABILITY TESTER
ELECTROLAB PVT LTD.
INDIA
5
USP DISSOLUTION
APPARATUS
LAB INDIA DS 8000
6
DISINTEGRATION
APPARATUS
LAB INDIA DT 1000
7 TRAY DRYER SISCO
8
UV-VIS DOUBLE BEAM
SPECTROPHOTOMETER
ELICO SL 164DOUBLE
BEAM
SPECTROPHOTOMETER
INSTRUMENTS DETAILS

28. S.NO DRUG/EXCIPIENTS NAME OF SUPPLIER
1 DOMPERIDONE TORRENT PHARMA
2
LACTOSE MONO
HYDRATE
SD FINE –CHEM PVT, MUMBAI
3 MANNITOL SD-200 SD FINE –CHEM PVT, MUMBAI
4
CROSCARMELLOSE
SODIUM
SD FINE –CHEM PVT, MUMBAI
5 CROSPOVIDON SD FINE –CHEM PVT, MUMBAI
6 ASPERTAME SD FINE –CHEM PVT, MUMBAI
7 MAGNESIUM STEARATE SD FINE –CHEM PVT, MUMBAI
8 TALC SD FINE –CHEM PVT, MUMBAI
INGREDIENT DETAILS

30. Colour, odour, taste and appearance:
The above terms were recorded by using descriptive terminology
Melting point determination:
determined by capillary method by using melting point apparatus
Determination of solubility:
determined by adding excess amount of drug in the solvent and
equilibrium solubility was determined by taking supernatant and
analyzing it on Lab India, double beam spectrophotometer.
% solubility = sample absorbance /standard absorbance × dilution factor
×100
Fourier Transformation Infra-red (FTIR) analysis:
Infra-red spectroscopy analysis was performed by Fourier
Transformation Infrared Spectrophotometer Alpha Brooker FTIR
(Tokyo, Japan).The instrument was calibrated by using polystyrene film.

31. Ultraviolet Visible (UV-visible) spectroscopy:
Construction of Calibration Curve:
Preparation of Stock Solution: 100 mg of Domperidone was taken in a
100 ml volumetric flask. 5 ml of methanol was added and shaken to
dissolve the drug. Add 7.4 ph phosphate to make upto level.
• From the above solution 1 ml is diluted to 10 ml with, 7.4 pH
phosphate buffer solutions to give 100 µg /ml concentration.
• The prepared solution i.e., 10 µg/ml concentration was scanned for
λmax from 200-400 nm in UV/Visible spectrophotometer.
Evaluation of API and Blend (Pre-compression
Parameters):
Angle of Repose: Flow property was determined by measuring the
Angle of Repose.
Angle of repose= tan-¹ (h/r)
Where, h = height r = radius

32. Procedure:
• 20gms of the sample was taken
• The sample was passed through the funnel slowly to form a
heap.
• The height of the powder heap formed was measured.
• The circumference formed was drawn with a pencil on the graph
paper . The radius was measured and the angle of repose was
determined. This was repeated three times for a sample.
Bulk density:
Bulk density is ratio of given mass of powder and its bulk volume.
Bulk density = M / V0
Where M= mass of the powder; V0=bulk
volume of the powder.
Tapped density: It is generally given by an equation
Tap density = M / Vr
Where M = mass of the powder,
Vr = final tapping volume of the powder.

33. Compressibility index and Hausner ratio:
to measure the unsettled apparent volume,(VO), and the final tapped
volume, (Vf), of the powder after tapping the material until no further
volume changes occur. Given by an expression as follows
Compressibility index = 100 × 1-( bulk density /tapped density)
Hausner ratio = tapped density / bulk density
Flow properties determination:
S.No Flow properties Angleof
repose(θ)
Compressibility
Index (%)or Carr’s
index
Hausner ratio
1 Excellent 25-30 <10 1.00-1.11
2 Good 31-35 11-15 1.12-1.18
3 Fair 36-40 16-20 1.19-1.25
4 Passable 41-45 21-25 1.26-1.34
5 Poor 46-55 26-31 1.35-1.45
6 Very poor 56-65 32-37 1.46-1.59
7 Very very poor > 66 >38 >1.6

34. EVALUATION OF TABLETS (Post Compression
Parameters):
Evaluation include the
diameter, size, shape, thickness, weight, hardness, disintegration &
dissolution characters. Physical Appearance: The general appearance of a tablet.
 Size & Shape: It can be dimensionally described & controlled.
Tablet thickness should be controlled within a ± 5% variation of
standard value.
 Weight variation test: comparison of the weight of the
individual tablets (xi) of a sample of tablets with an upper and lower
percentage limit of the observed sample average (x-mean).
Limits for Tablet Weight variation test:
Average weight of tablet (mg) % Difference allowed
130 or less 10 %
From 130 to 324 7.5 %
> 324 5 %
 Content Uniformity: used to ensure that every tablet contains
the amount of drug substance intended with little variation among
tablets within a batch.

35.  Friability: The friability test is closely related to tablet hardness &
designed to evaluate the ability of the tablet to withstand abrasion in
packaging, handling & shipping. The percentage friability was
determined by the formula:
% friability = (W1-W2) / W1 X 100
W1 = Weight of tablets before test andW2 = Weight of tablets after test
 Wetting time: time required for water to reach the upper
surface of the tablets was noted as the wetting time.
 Water absorption ratio: A tablet was put on the paper & the
time required for complete wetting was measured.
R = Wa – W b /Wb×100
Where Wa = weight of tablet after absorption
Wb = weight of tablet before absorption
Disintegration time: time required for a tablet to disintegrate.
 Disintegration test : The disintegration test is a measure of the
time required under a given set of conditions for a group of tablets to
disintegrate into particles

36.  Dissolution study of Domperidone of fast
disintegrating tablets:
Bath temperature : 37  0.5oC
Dissolution media : 7.4 pH buffer
Volume of dissolution media : 900 ml
Aliquot withdrawn : 5 ml
Dissolution apparatus : USP type II (paddle)
Revolutions per minute (Speed) : 50
FORMULATION DEVELOPMENT
List of used Excipients in the formulation:
Ingredients Purpose
Croscarmellose Sodium, Crospovidone Super disintegrants
Lactose monohydrate and Mannitol Diluents
Aspartame Sweetener
Magnesium stearate and Talc Glidant & Lubricant

37. Procedure for Formulation:
•Weigh all the ingredients (except Mg.Stearate) and sifted through # 44 mesh
separately.
•The ingredients after sifting through sieve no. 44 were thoroughly mixed by
geometrical order and mixed for 10 min.
•And finally add the Glidant (Magnesium Stearate) to the above blend mix it for 2min.
Compressed the above lubricated blend by using 6mm round
punches.
S.NO. Ingredients (mg) F1 F2 F3 F4 F5
1 Domperidone 20 20 20 20 20
2
Croscarmellose
sodium
10 20 10
3 Crospovidon --- --- 10 20 10
4 Lactose anhydrous 122 112 122 112 112
5 Mannitol 40 40 40 40 40
6 Aspertame 3 3 3 3 3
7 Magnesium stearate 3 3 3 3 3
8 Talc 2 2 2 2 2
Total weight(mg) 200 200 200 200 200
Composition of Domperidone Tablets:

39. PREFORMULATION:
S.N
O
API
CHARACTERISATIO
N
RESULTS
1 Physical Appearance Domperidone is a white powder
2 Melting point 242 °C
3 solubility
It is freely soluble in water, soluble in
alcohols, and slightly soluble in
common organic solvents, such as
acetonitrile and methyl ethyl ketone.
4 Bulk density 1.11 gm/ml
5 Tapped Density 1.42 gm/ml
6
Carr’s
index/Compressibility
index
27.92
7 Hausner’s Ratio 1.27
Conclusion:
The value of compressibility index above 25%, 15-25%, less than 15%
indicates poor flowability, optimum flowability & high flowability respectively.

40. PREPARATION OF STANDARD GRAPH FOR DOMPERIDONE
S. No Concentration (µ/ml) Absorbance (284nm)
1 0 0
2 2 0.072
3 4 0.162
4 6 0.249
5 8 0.329
6 10 0.422
Table for standard graph of domperidone
Standard graph Domperidone

41. Preformulation studies of blend of all formulation
Formulation
Bulk
density
(gm/cm3)
Tapped
density(gm/cm
3)
Angle of
repose(θ)
Carr’s Index(%) Hausner’s ratio
F1 0.40 0.47 21.5 14.8 1.17
F2 0.41 0.46 20.1 10.86 1.12
F3 0.41 0.47 19.6 12.7 1.14
F4 0.42 0.45 18.8 12.4 1.13
F5 0.43 0.48 17.8 10.4 1.11
FORMULATIO
N CODE
WEIGHT
VARIATIO
N
HARDNES
S
Kg/Cm2
THICKNESS
(mm)
FRIABILIT
Y
(%)
CONTENT
UNIFORMIT
Y
(%)
F1 Passes 4.5 2.08 0.15% 99.2
F2 Passes 5 1.98 0.12% 99.3
F3 Passes 4.3 1.99 0.13% 98.3
F4 Passes 4.4 2.02 0.14% 98.1
F5 Passes 4.8 2.01 0.12% 99.5
EVALUATION STUDIES OF TABLETS:

42. Disintegration time , Wetting time & Water absorption
ratio of all formulations
Formulation
Disintegration time
(sec)
Wetting time
(sec)
Water Absorption Ratio
F1 21 16 22.95
F2 18 15 24.29
F3 22 18 22.5
F4 20 17 21.5
F5 15 12 24.92
Invitro-Dissolution profiles:
Dissolution media pH 7.4 Phosphate buffer
Volume 900 ml
Apparatus Paddle
Speed 50 rpm
Time 2,4,6,8,10 min

43. Time
(Min)
F1 F2 F3 F4
F5
0 0 0 0 0 0
2 20.69 22.58 28.14 30.41 36.14
4 27.74 37.11 40.85 44.82 52.95
6 51.01 61.55 65.66 70.41 67.75
8 74.32 80.63 82.17 87.21 91.43
10 85.76 92.58 91.38 94.72 99.80
Dissolution profile of prepared formulations:
Conclusion:
Above graph indicates that %Drug release of F5 formulation shows better drug release when
compared with other formulations.

45. The objective of the present study is to develop a Domperidone
Fast dissolving tablets.
Finally it was concluded that:
Formulation 1&3: Drug and super disintegrant (i.e. Croscarmellose sodium and
Crospovidon) in the ratio of 1:1 which was prepared by direct compression
method have poor wetting property as it consist of less concentration of super
disintegrant.
Formulation 2, 4: consists Drug and superdisintegrants in the ratio of 1:2.
Formulation 5: consists Drug and combination of superdisintegrants in the ratio
of 1:2.
Formulation-5, has shown better dissolution profile and has shown maximum
%drug release within 10 minutes.
Among the all formulations (F1-F5), it was observed that formulation-5
has shown better dissolution profile with sufficient wetting capability. So
Formulation-5 was found to be the best formulation among others.
CONCLUSION

47. • S.S. Biradar, et al., “Fast dissolving drug delivery systems: a brief
overview” , The International Journal of Pharmacology.,2006;4(2).
• M.Slowson , et al ., “What to do when patients cannot swallow their
medications", Pharm. Times ., 1985; 51:90-96
• R.K. chang, et al., “Fast-dissolving tablets”, Pharma Technology.,
2000; 24(6):52-58.
• L.H.Reddy, et al., “Fast dissolving drug delivery systems:A review of
the literature” , International journal of pharmaceutical sciences.July
2002 :331-336.
• N.H. Indurwade , et al., “Novel approach – Fast dissolving tablets” ,
Indian drugs., August 2002; 39(8):405-409. etc
REFERENCES