ZAHID HUSAIN

M.Pharm (Pharmaceutics)
Faculty of Pharmacy, IU,
Lucknow
CONTENTS
◾ INTRODUCTION
◾ APPROPRIATE CANDIDATE DRUGS
FOR GRDDS
◾ ADVANTAGES
◾ LIMITATIONS
◾ APPROACHES
◾ CONCLUSION
◾ REFERENCES
◾ Oral drug delivery is widely used in
pharmaceutical field to treat the diseases.
◾ Some drugs are absorbed at specific site only
,these require release at that specific site.
◾ Gastro retentive drug delivery(GRDDS) is one of
the site specific drug delivery for the delivery of
the drugs at stomach.
◾ It is obtained by retaining dosage form into
stomach and drug is being released at controlled
manner at specific site.
◾ Drugs acting locally in the stomach.
E.g. Antacids and drugs for H. Pylori viz., Misoprostol.
◾ Drugs that are primarily absorbed in the stomach.
E.g. Amoxicillin
◾ Drugs that is poorly soluble at alkaline pH.
E.g. Furosamide, Diazepam, Verapamil, etc.
◾ Drugs with a narrow absorption window.
E.g. Cyclosporine, Levodopa, Methotrexate etc.
◾ Drugs which are absorbed rapidly from the
GI tract.
E.g. Metronidazole, tetracycline.

◾ Drugs that degrade in the colon.

E.g. Ranitidine, Metformin.

◾ Drugs that disturb normal colonic microbes

E.g. antibiotics against Helicobacter
pylori.
◾ Enhanced bioavailability
◾ Sustained drug delivery/reduced frequency of
Dosing
◾ Targeted therapy for local ailments in the
upper GIT
◾ Reduced fluctuations of drug concentration
◾ Improved selectivity in receptor activation
◾ Reduced counter-activity of the body
◾ Extended effective concentration.
◾ Minimized adverse activity at the colon.
◾ The drug substances that are unstable in the
acidic environment of the stomach are not
suitable candidates to be incorporated in the
systems.
◾ These systems require a high level of fluid in
the stomach for drug delivery to float and
work efficiently.
◾ Not suitable for drugs that have solubility or
stability problem in GIT.
◾ Drugs which are irritant to gastric mucosa are
also not suitable.
◾ These systems do not offer significant
advantages over the conventional dosage
forms for drugs, which are absorbed through
out GIT.
◾ High-density systems. (HDS)

◾ Floating systems. (FS)

◾ Swelling and expanding systems. (SS)

◾ Mucoadhesive & Bioadhesive systems.(AS)

◾ Gastric contents have a density close to water
(1.004 g cm−3). When the patient take high-
density pellets , they sink to the bottom of the
stomach where they become entrapped in the
folds of the antrum and withstand the peristaltic
waves of the stomach wall.
◾ A density close to 2.5 g cm−3 seems necessary
for significant prolongation of gastric residence
time.
◾ Barium sulphate , zinc oxide, iron powder, and
titanium dioxide are examples for excipients
used.
These have a bulk density lower than the gastric
content. They remain buoyant in the
stomach for a prolonged period of time, with
the potential for continuous release of drug.
They Include:
◾ Hydrodynamically balanced systems (HBS)
◾ Gas-generating systems
◾ Volatile liquid/ vacuum containing systems
◾ Raft-forming systems
◾ Low-density systems
◾ Carbonates or
bicarbonates, which react
with gastric acid or any
other acid (e.g., citric or
tartaric) present in the
formulation to produce
CO2
, are usually incorporated in
the dosage form, thus
reducing the density of the
system and making it float
on the media.
◾ Single layer matrix tablet is prepared by incorporating
bicarbonates in matrix forming hydrocolloid gelling
agent like HPMC, chitosin, alginate or other polymers
and drug.
◾ Bilayer tablet can also be prepared by gas generating
matrix in one layer and second layer with drug for its
SR effect.
◾ Triple layer tablet also prepared having first swellable
floating layer with bicarbonates, second sustained
release layer of drug and third rapid dissolving layer of
bismuth salt.
◾ System is incorporated with an inflatable
which
chambercontains liquid ether -gasifies at body
temperature to cause the chamber to inflate in
stomach.
◾ Inflatable chamber is loaded with a drug reservoir
which can be a drug, impregnated polymeric then
encapsulated in a gelatin capsule.
◾ Comprised of both an osmotic pressure controlled drug delivery device and an
inflatable floating support in a biodegradable capsule.
◾ In stomach, the capsule quickly disintegrates and release the
intragastric osmotically controlled drug delivery device .
◾ Inflatable support forms a deformable hollow polymeric bag containing liquid
that gasifies at body temperature to inflate the bag.
Consists of 2 compartments:
◾ Drug reservoir
◾ Osmotically active compartment.
◾ System can be float by flotation chamber,
which may be vacuum or filled with air or a
harmless gas.
◾ Drug reservoir is encapsulated inside a
microporous compartment.
◾ Prepared by incorporating a high level (2075%w/w) gel
forming hydrocolloids.
E.g.:- Hydroxy ethyl cellulose, hydroxy propyl cellulose, HPMC & Sod.
CMC into the formulation and then compressing these granules into
a tablets or capsules.
◾ It maintains the bulk density less than 1.
◾ This system is used for delivery
of antacids and drug delivery for
treatment of gastrointestinal
infections and disorders.
◾
The mechanism involved in
this system includes the
formation of a viscous cohesive
contact
gel in with gastric fluids,
forming a continuous layer
called raft.
◾ Polymers used commonly: Polycarbonates,
Cellulose acetate, Calcium alginate, Eudragit
S, agar and methoxylated pectin etc.
1. UNFOLDED The swelling is usually results
SYSTEMS
2. SWELLABLESYSTEMS from osmotic absorption of
water.
The device gradually
decreases in volume and
rigidity as a result depletion of
drug and expanding agent
and/or bioerosion of polymer
layer, enabling its elimination.
◾ The basis of mucoadhesion is that a dosage form can
stick to the mucosal surface by different mechanisms.
◾ Examples for Materials commonly used
for
bioadhesion are poly acrylic acid, chitosin, Polymethyl
vinyl ether, tragacanth, sodium alginate etc.
◾ N. K. Gastroretentive drug delivery
Jain,
systems: Garima Chawla, Piyush Gupta and
Aravind K. Bansal, editors. Progress in
controlled and novel drug delivery systems.
New delhi.
◾ S.P.vyas, roop K.khar controlled drug delivery
concepts and advances page no.196-217.