Académique Documents
Professionnel Documents
Culture Documents
APPROACHES
EVALUATION
CONCLUSION
REFERENCES
The control of gastrointestinal transit of orally administered
dosage forms using gastroretentive drug delivery systems
(GRDDS) can improve the bioavailability of drugs that
exhibit site-specific absorption.
Floating systems are not feasible for those drugs that have
solubility or stability problems in gastric fluid.
Density
Food intake and nature of food-high meal is responsible
for GRT disturbance.
Age –elder people have significant larger GRT.
High density system
Floating systems
Expandable systems
Superporous hydrogels
Bioadhesive systems
Magnetic systems
Gastric contents have a density close to water (~1.004).
A density close to 2.5g/cm3 is necessary for significant
prolongation of gastric residence time.
The commonly used excipients in high density system
includes barium sulphate, zinc oxide, iron powder, and
titanium dioxide.
The major drawback with such systems is that it is
technically difficult to manufacture them with a large
amount of drug (>50%) and to achieve the required density
of 2.4-2.8g/cm3.
Single-unit floating dosage system
Non effervescent systems
Effervescent (gas-generating) systems
Raft-forming systems
Single-Unit Floating Dosage System
Noneffervescent Systems :
Hollow Microspheres :
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 gel in contact with gastric fluids, wherein each
portion of the liquid swells, forming a continuous layer called raft.
This raft floats in gastric fluids because of the low bulk density
created by the formation of CO2.
Usually the system contains a gel-forming agent and alkaline
bicarbonates or carbonates responsible for the formation of CO2 to
make the system less dense to float on the gastric fluids.
EXPANDABLE SYSTEM
Polymer
Mucus membrane
MAGNETIC SYSTEM :
The tests for floating ability and drug release are generally
performed in simulated gastric fluids at 37 C.
Methods to asses gastroretentivity of
GRDFs:
Radiology (X-Ray):
In this technique a radio-opaque material has to be
incorporated in the DF, and its location is tracked by X-ray
picture.
ɣ-Scintigraphy:
Gamma scintigraphy relies on the administration of a DF
containing a small amount of radioisotope,
e.g..,152Sm,which is a gamma ray emitter with a relatively
short half life.
Gastroscopy:
Gastroscopy is commonly used for the diagnosis and
monitoring of the GI tract.
This technique utilizes a fiberoptic or video system and can
be easily applied for monitoring and locating GRDFs in the
stomach.
Swelling studies:
Spray drying.
Modified methods.
Oil phase (polymer + solvent) is injected into the
aqueous phase (water + surfactant), the solvent dissolves
into the aqueous phase and evaporates at the air-liquid
interface.