The relatively brief gastric emptying time (GET)

in humans which normally averages 2-3 hrs

through the major absorption zone i.e. stomach
and upper part of the intestine can result in
incomplete drug release from the drug delivery
system, leading to reduced efficacy of the
administered dose.
This has led to the development of oral gastro-
retentive dosage forms.
Gastro-retention is essential for –
1. Drugs that are absorbed from the stomach.
2. Drugs that are poorly soluble or degraded by the
higher pH of intestine.
3. Drugs with an absorption which can be modified by
changes in gastric emptying time.
4. Gastro-retention is useful for local as well as
sustained drug delivery for certain conditions, like H.
pylori infection which is the cause of peptic ulcers.
5. This dosage form also improves bioavailability,
therapeutic efficacy and may even allow a possible
reduction in the dose because of steady therapeutic
levels of drug.
High density approach
Low density approach
Principles of GRDDS
 A. FLOATING DRUG DELIVERY
SYSTEM
Floating drug delivery offers several
applications for drugs having poor
bioavailability because of the narrow
absorption window in the upper part of the
gastrointestinal tract.
It retains the dosage form at the site of
absorption and thus enhances the
bioavailability. It also implies the optimization
of the therapeutic effect of a drug in the body
with lower and less frequent dose.
On the basis of principles, floating delivery system can be developed:
1. Swelling system
2. Specific gravity
3. Gas generating system
 1. Effervescent system
2. Non-effervescent system
3. Hollow microspheres
4. Raft forming system
 1. Effervescent system
These delivery systems utilize effervescent
reactions between carbonate/bicarbonate
salts and citric/tartaric acid to liberate CO2,
which gets entrapped in the gellified
hydrocolloid layer of the systems thus
decreasing its specific gravity, making it to
float over GI fluid and release the drug
slowly at a desired rate for a prolonged
period of time.
Fig: Effervescent Floating Drug Delivery System
 2. Non effervescent system
This systems commonly use gel forming or
highly swell-able cellulose type hydro-colloids,
polysaccharides or matrix forming polymers
such as polycarbonate, polyacrylate,
polymethacrylate and poly styrene to cover
the core drugs.
In stomach, the polymer receives gastric fluid
to form gellified hydrocolloid layer and swell,
reduces specific gravity and floats over GF for
a prolong period of time and releasing drug in
desired rate.
Fig: Non-Effervescent Floating Drug Delivery System
 3. Hollow microspheres
Both natural and synthetic polymers have
been used to prepare floating microspheres.

4. Raft
R forming system
This systems have received much attention
for the drug delivery for GI infections and
disorders.
 SUSTAINED DRUG DELIVERY:
As mentioned earlier drug absorption from oral control release
(CR) dosage forms is often limited by the short gastro retention
time (GRT) available for absorption.
These special dosage forms are light, relatively large in size, and
do not easily pass through pylorus.

SITE SPECIFIC DRUG DELIVERY:

A floating dosage form is a feasible approach especially for drugs
which have limited absorption sits in upper small intestine.
The controlled, slow delivery of drug to the stomach provides
sufficient local therapeutic levels and limits the systemic
exposure to the drug.
This reduces side effects that are caused by the drug in the blood
circulation
Drugs that have poor bioavailability because their absorption is
limited to upper GI tract can be delivered efficiently thereby
maximizing their absorption and improving their absolute bio-
availabilities.
Floating dosage forms with SR characteristics can also be
expected to reduce the variability in transit performance.

Floating systems are not feasible for those drugs that have
solubility or stability problems in gastric fluid.
They require a sufficiently high level of fluids in the stomach for
the drug delivery, to float there in and to work efficiently.
Tablets Theophylline, Furosemide, Ciprofolxacin,
Pentoxyfillin, Captopril, Acetylsalicylic
acid
Capsules Nicardipine, Chlordiazepoxide HCl,
Diazepam, Propranlol
Granules Indomathacin, Prednisolone

Films Cinnarizine

Microspheres Verapamil, Aspirin, Ketoprofen, Iboprufen

 B. Mucoadhesive Gastrointestinal Drug
Delivery System
It is known that, the surface epithelium of the
stomach and intestine retains its integrity
throughout the course of its lifetime, even though it
is constantly exposed to a high concentration of
hydrochloric acid (as high as 0.16 N) and powerful
protein splitting enzymes, like pepsin.
This self-protective mechanism is due to the fact that,
the specialized goblet cells located in the stomach,
duodenum and transverse colon continuously
secrete a large amount of mucous that remains
closely applied to the surface epithelium.
The mucus contains mucin, an oligosaccharide
chain with terminal sialic acid (pKa = 2.6), which
is capable of neutralizing the hydrochloric acid
and withstanding the action of pepsin and thus
protects the epithelial cell membrane.
The surface epithelium adhesive properties of
mucin have been found out and recently applied
to the development of gastrointestinal drug
delivery devices based on bio (muco) adhesive
polymers.
The concept of using mucoadhesive polymer to
extend the GI transit time is elaborated in the
figure.
Fig: Interaction of mucoadhesive drug delivery system with mucus
layer on gastrointestinal surface epithelium
The drug delivery system coated with
mucoadhesive polymer binds to the mucin
molecules in the mucus lining of GI tract and is
therefore retained on the surface epithelium for
extended periods of time.

The drug molecules contained in the drug

delivery device coated with mucoadhesive
polymer are constantly released for absorption.
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