PRASANNA COLLEGE OF PHARMACY

LAILA,BELTHANGADY
ASSIGNMENT

Subject : Novel Drug Delivery System

Topic : Gastro Retentive Drug Delivery System

Presented by : Disha .D
21P8652
VII Semester, B. Pharmacy
Prasanna College Of Pharmacy

Presented to : Ms.Sindhura Pallavi

Lecturer, B. Pharmacy
Prasanna College Of Pharmacy
Submission Date : 07- March -2025
Gastro Retentive Drug Delivery System :
 Dosage forms that can be retained in the stomach are called Gastro retentive drug delivery system
(GRDDS).
 GRDDSs can improve the controlled delivery of drugs that have an absorption window by continuously
releasing the drug for a prolonged period of time before it reaches its absorption site.
 Prolonging the gastric retention of the drugs is sometimes desirable for achieving therapeutic benefits of
drugs that are absorbed from the proximal part of the GIT(gastro intestinal tract) or those are less soluble in
or are degraded by alkaline pH.
Factors Controlling Gastric Retention of Dosage Forms :
(a) Density of Dosage Form:
 Dosage forms having a density lower than that of gastric fluid experience floating behaviour and hence
gastric retention.
 A density of <1.0 gm/ml is required to exhibit floating property.
 However, the floating tendency of the dosage form usually decreases as a function of time, as the dosage
form gets immersed into the fluid, as a result of the development of hydrodynamic equilibrium.
(b) Shape and Size of the Dosage Form:
 The mean gastric residence times of non-floating dosage forms are highly variable and greatly dependent on
their size, which may be large, medium and small units.
 In most cases, the larger the dosage form the greater will be the gastric retention time (GRT) due to the
larger size of the dosage form would not allow this to quickly pass through the pyloric antrum into the
intestine.
 Ring-shaped and tetrahedron-shaped devices have a better gastric residence time as compared with other
shapes.
(c) Food Intake and Nature of Food:
 Food intake, the nature of the food, caloric content, and frequency of feeding have a profound effect on the
gastric retention of dosage forms.
 The presence or absence of food in the stomach influences the GRT of the dosage form.
 Usually, the presence of food increases the GRT of the dosage form and increases drug absorption by
allowing it to stay at the absorption site for a longer time.
(d) Effect of Gender, Posture and Age:
 Generally, females have slower gastric emptying rates than male.
 The effect of posture does not have any significant difference in the mean gastric retention time (GRT) for
individuals in upright, ambulatory and supine state.
 In the case of elderly persons, gastric emptying is slowed down.
Advantages of GRDDS :
1. Enhanced bio-availability.
2. Reduced frequency of dosing.
3. Targeted therapy for local ailments in the upper GIT.
4. Patient compliance.

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 5. Improved therapeutic efficacy.

Disadvantages of GRDDS :
1. Requirement of high levels of fluids in the stomach for the delivery system to float and work efficiently.
2. Requires the presence of food to delay gastric emptying.
3. Drugs, which undergo significant first pass metabolism, may not be desirable candidates for floating drug
delivery system since the slow gastric emptying.
4. May lead to altering systemic bioavailability.
5. Drugs having solubility or stability problems in the highly acidic gastric environment or which are irritants to
gastric mucosa cannot be formulated as GRDDs.
Approaches for GRDDs :
1. Floating drug delivery systems.
2. Mucoadhesive systems.
3. Swellable systems.
4. High density systems.
1. Floating Drug Delivery System
 Floating drug delivery systems (FDDS) have a bulk density lower than gastric fluids and thus remain
buoyant in stomach for a prolonged period of time, without affecting the gastric emptying rate.
 While the system floats on gastric contents, the drug is released slowly at a desired rate from the system.
After the release of drug, the residual system is emptied from the stomach.
 This results in an increase in gastric retention time and a better control of fluctuations in plasma drug
concentrations.
Floating systems can be classified into two distinct categories,
i. Effervescent system and
ii. Non-effervescent systems

Effervescent systems:
a) Gas generating systems.
b)Volatile liquid containing systems.
c) Inflatable gastrointestinal delivery systems.
d)Intragastric osmotically controlled drug delivery system.

Non-Effervescent systems:
a) Colloidal gel barrier systems.
b)Alginate beads.
c) Hollow microspheres.
d)Microporous compartment system.

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Effervescent system
(a) Gas Generating Systems:
 These are formulated by intimately mixing the CO2 generating agents and the drug within the matrix.
 These have a bulk density lower than gastric fluids and therefore remain floating in the stomach unflattering
the gastric emptying rate for a prolonged period.
 The drug is slowly released at a desired rate from the floating system and after the complete release, the
residual system is expelled from the stomach.
 This leads to an increase in the gastric retention time and a better control over fluctuations in plasma drug
concentration.
Dividend into two types:
 Intra Gastric Single Layer Floating Tablets
 Intra Gastric Bilayer Floating Tablets
i. Immediate release layer
ii. Sustained release layer

(b) Volatile Liquid / Vacuum Containing Systems:

 These systems can be made to float in the stomach because of the floatation chamber, which may be a
vacuum or filled with air or a harmless gas, while the drug reservoir is encapsulated inside a microporous
compartment.

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 (c) Inflatable Gastrointestinal Delivery Systems:
 In these systems, an inflatable chamber is incorporated, which contains liquid ether that evaporates at body
temperature to cause the chamber to inflate in the stomach.
 These systems are fabricated by loading the inflatable chamber with a drug reservoir, which can be a drug,
impregnated polymeric matrix, then encapsulated in a gelatin capsule.
 After oral administration, the capsule dissolves to release the drug reservoir together with the inflatable
chamber.
 The inflatable chamber automatically inflates and retains the drug reservoir compartment in the stomach.
 The drug continuously released from the reservoir into the gastric fluid.

d) Intragastric Osmotically Controlled Drug Delivery System:

 It is comprised of an osmotic pressure-controlled drug delivery device and an inflatable floating support in a
biodegradable capsule.

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 In the stomach, the capsule quickly disintegrates to release the intragastric osmotically controlled drug
delivery device.
 The inflatable support inside forms a deformable hollow polymeric bag that contains a liquid that vaporizes
at body temperature to inflate the bag.
 The osmotic pressure-controlled drug delivery device consists of two components drug reservoir
compartment and an osmotically active compartment.
 The drug reservoir compartment is enclosed by a pressure responsive collapsible bag, which is
impermeable to vapour and liquid and has a drug delivery orifice.
 The osmotically active compartment contains an osmotically active salt and is enclosed within a semi-
permeable housing.
 In the stomach, the water in the gastro-intestinal fluid is continuously absorbed through the semi-permeable
membrane into osmotically active compartment to dissolve the osmotically active salt.
 An osmotic pressure is thus created which acts on the collapsible bag which forces the drug reservoir
compartment to reduce its volume and which in turn activate the drug release from the drug solution
compartment through delivery orifice.
 The floating support is also made to contain a bio-erodible plug that erodes after a predetermined time to
deflate the support.
 The deflated drug delivery system is then emptied from the stomach.

Non-Effervescent system
(a) Colloidal Gel Barrier Systems:
 Such systems contain drugs with gel forming hydrocolloids meant to remain buoyant on stomach contents.
 These systems incorporate a high level of one or more gel forming highly swellable cellulose type
hydrocolloids. For e.g. HPMC, NaCMC.
 On coming in contact with gastric fluids forms a viscous core.Incorporates H₂O and entraps air.Density of
system falls below 1 gm/cm³. Then it starts floating.

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b) Microporous Membrane System:
 Based on the encapsulation of drug reservoir inside a Microporous compartment, The peripheral walls of the
drug reservoir compartment are completely sealed to prevent any direct contact of the gastric mucosal
surface with the undissolved drug.
 In stomach, the floatation chamber containing entrapped air causes the delivery system to float over the
gastric contents.
 Gastric fluid enters through the apertures, dissolves the drug and carries the dissolved drug for absorption.
c) Alginate Beads:
 Spherical beads of approximately 2.5 mm in diameter can be prepared by dropping a sodium alginate
solution into aqueous solutions of calcium chloride, causing precipitation of calcium alginate.
Sodium alginate + Calcium chloride, Calcium alginate + NaCl.
 The beads are then separated and frozen in liquid nitrogen, and freeze dried at -40°C for 24 hours, leading to
the formation of porous system.Maintain a floating force of over 12 hours.
d) Hollow Microspheres:
 Microballoons / hollow microspheres loaded with drugs are prepared by simple solvent evaporation
method.Commonly used polymers to develop these systems are polycarbonate, cellulose acetate, calcium
alginate, Eudragit S, agar and pectin, etc.
 These systems have capacity to float on acidic dissolution media containing surfactant for about 12 hours in
vitro.