FORMULATION AND EVALUATION OF ORO-DISPERSIBLE ANTI-
M.PHARM DISSERTATION PROTOCOL
RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES
UNDER THE GUIDANCE OF
DEPARTMENT OF PHARMACEUTICAL TECHNOLOGY
KARNATAKA COLLEGE OF PHARMACY
RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES
PROFORMA FOR REGISTRATION OF SUBJECTS FOR DISSERTATION
1. Name of the candidate and J.PURNACHANDER
address Karnataka College of Pharmacy
Hegdenagar Main Road
S/O SANJEEVA RAO
2. Name of the institute KARNATAKA COLLEGE OF
Hegde nagar main road
3. Course of the study and subject MASTER OF PHARMACY IN
4. Date of admission to the course
28TH JULY 2011
5. Title of the topic:
FORMULATION AND EVALUATION OF ORO DISPERSIBLE ANTI-
6. Brief resume of the intended work:
6.1 Need for the Study:
Among the different routes of administration, the oral route of administration continues
to be the most preferred route due to various advantages including ease of ingestion,
avoidance of pain, versatility, most importantly patient compliance and self
administration. The different dosage forms include tablets, capsules, syrups,
suspensions. However, pediatric and geriatric patients experience difficulty in
swallowing conventional tablets, which leads to poor patient compliance. Pediatric,
geriatric, institutionalized patients and people commonly suffering from dysphasia,
clinical conditions where water intake is limited, situations where water is not available
and for drugs undergoing high first pass metabolism.
Oral dispersible tablets are solid single-unit dosage forms that are placed in mouth and
allowed to disperse/dissolve in the saliva without the need of water and provide a quick
onset of action. Rapid disintegration of tablet results in quick dissolution and rapid
absorption which provide rapid onset of action. Some drugs are absorbed from mouth,
pharynx and oesophagus as the saliva passes down into the stomach. In such cases,
bioavailability of drug is significantly greater than those observe from convectional
tablet dosage form.
Oral dispersible tablets are prepared by various techniques; mainly direct compression,
wet granulation, sublimation, lyophilisation and moulding. The simplicity and cost
effectiveness of the direct compression process have positioned this technique as an
attractive alternate to traditional granulation technologies.The superdisintegrants have
an vital role for preparation of oro dispersible tablets and are highly effective and
Antiemetics class of drug that is effective against vomiting and nausea.Antiemetics are
typically used to treat motion sickness and the side effects of opiod analgesic general
anaesthetics and chemotherapy directed against cancer.
Conventional tablet as antiemetic’s, ingestion, absorption and onset of action is
difficult during emetic condition which results in delayed bioavailability. So the current
work is to focus on formulate and evaluate oro-dispersible Anti-emetic tablets with
faster onset of action by using suitable methods and different superdisintegrants with its
physicochemical characters and stability study may be the tool to improve the anti
emitics patient compliance and therapy.
6.2 Review of Literature:
Developed rapidly disintegrating oramucosal drug delivery systems are the focus of
extensive research due to their rapidly and efficiently deliver drugs. These drug delivery
systems are able to release the drug as soon as they come into contact with saliva and
highly attractive for patient groups such as infants, pediatrics and geriatrics. The
challenges posed by accurate in vitro disintegration and dissolution testing of rapidly
disintegrating drug delivery system employing conventional and the most recent novel
methodologies and including the use of ex-vivo permeation studies and in vivo model.1
Developed fast dissolving tablets of valsartan were prepared using different
superdisintegrants by direct compression method. FDTs were evaluated for
physicochemical properties and in vitro dissolution. Effect of disintegrant on
disintegration behaviour of tablet in artificial saliva, pH 5.8 was evaluated. Wetting time
of formulations containing Crospovidone was least and tablets showed fastest
disintegration. The drug release from FDTs increased with increasing concentration of
superdisintegrants and was found to be highest with formulations containing
Crospovidone. The release of valsartan from FDTs was found to follow non-Fickian
Developed In the present work, fast dissolving phenobarbitone tablets were prepared by
direct compression method with a view to enhance patient compliance. The
methodology worked out was by using three
superdisintegrants (2-8%w/w) i.e., L-hydroxypropyl cellulose , pregelatinized starch,
Crospovidone with varying concentration of microcrystalline cellulose(5-15%w/w)
were used and directly compressible mannitol was used as a diluent to enhance the
mouth feel. The prepared batches of tablets were evaluated for hardness, friability, drug
content uniformity and In-vitro dispersion time. Three promising formulations were
tested for drug release pattern (in pH 6.8 phosphate buffer), short term stability (at
40°/75% RH for three months) and drug-excipient interaction (IR spectroscopy). Short-
term stability studies on the formulations indicated that there are no significant changes
in drug content and In-vitro dispersion time.3
Developed FDTs disintegrate either rapidly in water, to form a stabilized suspension, or
disperse instantaneously in the mouth to be swallowed without the aid of water. A direct
compression method was used to prepare these two types of tablets containing coated
ibuprofen as a high dosed model drug. The selected tablet formulation, containing 26%
galactomannan and 5% crospovidone, disintegrates before the galactomannan starts to
swell. These tablets disperse in water within 40 s and show a crushing strength of 95 N.
An optimum tablet formulation, containing 34% mannitol and 13% crospovidone,
provides a short wetting time of 17 s and a sufficient crushing strength of 40 N. In
conclusion, fast dispersible tablets with acceptable hardness and desirable taste could be
prepared within the optimum region.4
Prepared fast-disintegrating tablets of diclofenac potassium with sufficiently integrity
as well as a pleasant taste using two different fillers and binders. Tablets were made
with direct compression method. Porosity, hardness and disintegration time were
determined. It carried out using a validated spectrophotometric method for the analysis
of drug. Fast disintegration tablet of diclofenac potassium with durable structure and
desirable taste can be prepared using both fillers and binders. Single dose of fast
disintegration tablet was effective in relieving the pain.5
Prepared fast disintegrating ondasetron hydrochloride tablets by masking the bitter
taste of ondansetron hydrochloride by polymer carrier system. Taste
masking was done by complexing ondansetron hydrochloride with amino alkyl
mithacrylate co polymer in different ratio by the precipitation method. Tablets of batch
containing 1:1 of mannitol and micro crystalline cellulose and 7% w/w polyplasdone
XL-10 showed faster disintigrtion within 12.5 sec then marketed conventional
Formulated and evaluated grnisetron hydro chloride orodispersible tablets AC-Di-Sol.
The mix powder blends of verifying compostion were prepared and granulated for
micromeritic properties and then subjected to tablet preparation by direct compression.
The physical parameters were found satisfactory. Tablets prepared with cross povidone
at 5% was found to best formulation as it exihibited satisfactory physical parameters
least disintegration ,wetting time and highest percent drugs release.(99.45%) at 10min
and good stability at accelerated condition.7
Examined effect of calcium silicate and various lubricants on an optimized B-
cyclodextrin-based fast-disintegrating tablet formulation were also evaluated at 75, 85
and 95% relatives humidities. Magnesium stearate, being commonly used lubricant was
used to optimize lubricant concentration in optimization study. Concentration of
lubricant was found to be important for tablet disintegration and hardness. An optimized
value of 1.5% of magnesium stearate gave disintegration and hardness of 1.42kg.
Hardness was not affected at 75% moisture treatment.8
Prepared a rapidly disintegration tablet in the oral cavity using a glycine as a
disintegrant. Effect disintegrant on the disintegration of the tablet in the oral cavity was
evaluated. Wetting time prepared from carboxymethylcellulose having the hardness of 4
kg was 3s. Result suggested that NS-300 possessed wetting nature and resulted in the
rapid disintegration of tablet. Tablet formulation containing NS-300 and glycine was
highly applicable to water-insoluble drug.9
Developed fast-disintegrating tablets using a progressive three-stage approach. A series
of hardness, fracturability and disintegration time tests were formulated performed on
the formulation. During stages 1, tablets were prepared in concentration between 2%
and 5% w/w and combination bloom strength gelatin using 75 and 225 BSG. Stage 2,
addition of the sacchrides sorbitol, mannitol and sucrose in concentration of 10 and 80%
w/w. next stage, the addition of viscosity-modifying polymers to improve mouth-feel
and aid pre- gastric retention.10
Formulated directly compressed RDS of fenoverine with sufficient mechanical
integrity, content uniformity and acceptable palatability to assist patients of any age
group for easy administration. Tablets were evaluated for weight variation, thickness,
hardness, friability, taste, drug content, in vitro drug release and in vitro and in vivo
disintegration time. Superdisintegrants such as crospovidone, croscarmellose sodium
and sodium starch glycolate. DSC studied did not indicate any excipient incompatibility
either during mixing.11
6.3 Objective of the Study:
The objective of the present study is as follows:
1. To carry out Pre-formulation studies
2. Development of ideal oro dispersible anti-emetic tablets
3. Evaluation of formulated products
4. To finalize product
5. To carry out stability studies as per ICH Guidelines
Materials & Methods:
Drug: The Anti-emetic drug will be procured from suitable pharma grade manufacturer.
Polymer: The natural biodegradable polymers and superdisintegrants will be used.
All other chemicals will be used of Analytical grade.
Preliminary Morphological Studies
2. Preparation of solid dispersion:
Disintegration time in oral cavity
Water absorption ratio
In-vitro release studies
7.1 Source of Data:
The data was obtained from the literature survey and Internet source.
Digital Library RGUHS Library, Bangalore.
Library, Karnataka College of Pharmacy, Bangalore.
The data was obtained on experimental work.
7.2 Method of Collection of Data (including sampling procedure, if any) :
Data will be collected from the prepared formulations; in-vitro dissolution
studies and stability studies as per ICH Guidelines.
7.3 Does the study require any investigations or interventions to be conducted
On patients or other human or animals? If so please describe briefly
DOES NOT REQUIRE
7.4 Has the Ethical Clearance been obtained from your Institution in case of 7.3?
8. LIST OF REFERENCES:-
1. Deshika R, Viness P, Yahya EC, Lisa CT. Rapidly disintegrating oramucosal
drug delivery technologies. Pharm Dev Tech 2009;14(6):588-601.
2. CP Jain, PS Naruka formulation and evaluation of fast dissolving tablets of
valsartan, I J Pharma and pharma sci 2009;1;219-26.
3. Mahadevappa VR,Basawaraj B, Appalaraju S, Raghunandan D, Swamy PV.
Formulation and design of rapidly disintigrating phenobarbiton tablets by direct
compression method. I J Pharm and Biosci 2010;1:62-8.
4. Peter CS, Simone S, Fast dispersible ibuprofen tablets. Eur J Pharm Sci
5. Tansel C, Aysegul D, Selcuk C, Nursabah B. Formulation and evaluation of
diclofenac potassium disintegrating tablets and their clinical application
migraine patients. Drug Dev Ind Pharm 2010;early online:1-9.
6. Shagufta K,Prashant K,Premchand N,Pramod Y.Taste masking of ondransetron
hydrochloride by polymer carrier system and formulation of rapid disintegrating
tablets.AAPS pharma sci tech 2010;8;E1-8.
7. Sunitha B, Sachin A, Vivek M. Formulation and evaluation of granisetron
hydrochloride orodispersible tablets. Bulletin of pharma res 2011;1(2);41-6.
8. Sameer GL, Yi-ying Y, Ajay KB. Effects of disintegration-promoting agent,
lubricants and moisture treatment on optimized fast disintegrating tablets. Int J
9. Jinichi F, Etsue Y, Yasuo Y, Katsuhide T. Evaluation of rapidly disintegrating
tablets containing glycine and carboxymethylcellulose. Int J Pharm 2006;
10. Rahul C, Zahra H, Farhan A, Alan MS, Afzal RM. The role of formulation
excipients in the development of lyophilized fast-disintegrating tablets. Eur J
Pharm Biopharm 2009;72:119-129.
11. Sunil KB, Michael AR, Soumyajit M, Madhusudan RY. Formulation and
evaluation of rapidly disintegrating fenoverine tablets: effects of
superdisintegrants. Drug Dev Ind Pharm 2007;33:1225-32.
9. Signature of the Candidate
10. Remarks of the Guide:
The topic selected for dissertation is satisfactory. Adequate equipment & chemicals are
available to carry out the project work.
11. Name & Designation (in BLOCK LETTERS)
11.2 Signature of Guide
Mrs. ROHINI R. M.)
11.4 Signature of Co-Guide
11.5 Head of the Department DR.B PRAKASH RAO
Professor and Head
Department of Pharmaceutical
Karnataka College of Pharmacy.
11.6 Signature of HOD:
12. 12.1 Remark of the Principal:
All the required facilities will be provided to carry out dissertation work under the
supervision of the guide.
12.2 Signature of the Principal
(Prof. Dr K.RAMESH )
Karnataka College of Pharmacy
Hegdenagar Main Road