Project seminar presentation
Partial Fulfillment of the requirements for the award of
“Degree of Bachelor of Pharmacy”
B.Pharm. (7th Semester)
Regd. No.: 1003254038
Under the guidance of
Dr. Prasanta Kumar Choudhury
Royal College of Pharmacy & Health Sciences, Berhampur ,
Affiliated to Biju patnaik University of Technology, Rourkela,
Aim and objectives
Plan of work
Targeted drug delivery systems:
The major goal of any drug delivery system is to supply a therapeutic
amount of drug to a target site in a body.
Targeted drug delivery implies selective and effective localization of
drug into the target at therapeutic concentrations with limited access
to non target sites.
A targeted drug delivery system is preferred in drugs having
instability, low solubility and short half life,
WHY COLON TARGETED DRUG DELIVERY IS NEEDED?
Rational for the Development of Oral Colon
Targeted Drug Delivery:
• Treatment of local pathologies
• Greater responsiveness to the absorption
• Site for delivery delicate drugs (Proteins and
Targeted drug delivery to the colon.
Decrease in dose administration.
Decrease side effects.
Improved drug utilization.
There are variations among individuals with respect to the pH level in the
small intestine and colon which may allow drug release at undesired site.
The pH level in the small intestine and caecum are similar which reduces
site specificity of formulation.
Diet and diseases can affect drug targeting to colon
DISORDERS OF COLON
•Crohn’s disease is a chronic inflammatory
disease of the gastrointestinal tract
•It is characterized by a granulomatous
inflammation affecting any part of the
tract, normally form fistulae.
•It is a chronic inflammatory disorder of
colon limited to the large intestine as against
the case with Crohn's Disease where any part
of the alimentary tract may be involved.
The various pharmaceutical approaches which have
been used for targeting drugs to the colon are
mainly based on:
Pressure dependent delivery system
Organ Transit time
Stomach <1(Fasting) , >3(Fed)
Small intestine 3-4
Large Intestine 20-30
Major metabolic processes occurring in the colon are hydrolysis and
Enzymes in Colon:
Reducing enzymes Hydrolytic enzymes
N-oxide reductase Glycosidases
Sulphoxide reductase Glucuronidase
Azoreductases, which reduces azo-bonds selectively and
Polysaccharidases which degrades the polysaccharides
AZO BOND CONJUGATES:
SAS on colon in presence of diazoreductase cleaves the azo bond to
form 5 ASA and Sulfapyridine.
Hydrolysis of sulphasalazine:
(i) 5-aminosalicylic acid .
(ii) And sulfapyridine.
Introduction of matrix tablet excludes complex production procedures
such as coating and pelletization
Drug release rate from the dosage form is controlled mainly by the type
and proportion of polymer used in the preparations
Advantages offered by matrix tablets:
Reduction in toxicity by slowing drug
Minimize the local and systemic
Improved patient compliance.
1. Cheng G.et al.,
Eudragit® L100 and S100 pH-
are able to achieve site-specific
drug delivery targeting at colon
following oral administration
2. Patil M.M. et
Compression coating layer was
adopted to delay the drug release
for about 2-3 hours and to allow
the tablet to pass intact through
the small intestine to the colon.
3. Aswar P.B. et
Matrix tablets containing guar
gum as a carrier and ethyl
cellulose as a binder was found
to be suitable for targeting
Diclofenac sodium for local
action in the colon
4. Shendge R.S. et
The matrix tablet containing binder
system of ethyl cellulose and dextrin
as a carrier was found to be suitable
for targeting the colon
5 Neekhra M. et
That cellulose acetate phthalate
coated capsules with 50% guar gum
may be useful for drug targeted to
the colon successfully.
S.M. et al.,
locust bean gum
Ratio 6:4 released only 2.24% of
drug in physiological environment of
stomach and small intestine and
released more than 90% of drug in
SL NO. AUTHOR/
7. Naikwade S. et
The formulation was
found to be working as
colon targeted drug
8. Badmapriya D.
Guar Gum, Matrix Tablets
Guar Gum colon
targeting coated with
two different polymeric
layers resulted in
the drug release in
range of 57.8 to
68.38%, due to the
3.0 DRUG PROFILE (Sulfasalazine)
Sulfasalazine was developed in the 1950s specifically to treat rheumatoid
Sulfasalazine is a sulfa drug, (a derivative of mesalazine)
It is formed by combining sulfapyridine and salicylate with an azo bond. It
may be abbreviated SSZ.
phenyl} diazen-1-yl] benzoic acid
Mechanism of action:
5-aminosalicylic acid (5-ASA) and sulfapyridine (SP), is still under
It may be related to the anti-inflammatory and/or immuno modulatory.
Clinical studies utilizing rectal administration of Sulfasalazine, SP and
5-ASA have indicated that the major therapeutic action may reside in the
Route of elimination:
The majority of 5-ASA stays within the colonic lumen and is excreted as
5-ASA and acetyl-5-ASA with the feces.
AIM AND OBJECTIVES
Present aim of the research work is based on Formulation
Design and Development of Colon Specific Matrix Tablets
of 5-Amino Salicylic Acid. Here the work is emphasized on
formulation of matrix tablets intended for colonic delivery.
The results are to be compared with marketed formulation to
see that whether any deviation occurred between the
marketed formulation and the prepared formulation.
PLAN OF WORK:
Selection of model drug and analytical studies.
Characterization of the drug:
UV spectral analysis
Preparation calibration curve of model drug
Preformulation Drug-Excipients compatibility study
Formulation of matrix tablets for colonic delivery.
Selection of final formulation and evaluation for potentiality to deliver the
drug to colonic region.
Comparison of the drug release data and fitting to different kinetic models.
Stability studies of the optimized formulations
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