Based on the above information it may be concluded that gastro retentive drug delivery offers various potential advantages for drug with poor bioavailability due their absorption is restricted to the upper gastrointestinal tract (GIT) and they canbe delivered efficiently thereby maximizing their absorption and enhancing absolute bioavailability.Due to complexity of pharmacokinetics and pharmacodynamics parameters, in vivo studies are required to establish the optional dosage form for a specific drug.

1. SHREE MAHAVIR INSTITUTE
OF PHARMACY, NASHIK.
• BRANCH – B. PHARMACY.
• YEAR – 2022-2023.
.
.

2. COURSE STRUCTURE AND CONTENTS FOR
PRACTICE SCHOOL (BP507PS)
B. PHARMACY FINAL YEAR (SEM VII)
DOMAIN – 5
FORMULATION DEVELOPMENT
GASTRO RETENTIVE DRUG
DELIVERY SYSTEM
(REVIEW)

3. A REVIEW ARTICLE BY :
GHUGE KRISHNA TUKARAM
CLASS : FINAL YEAR B. PHARMACY
PRN : 1952811823048
ROLL NO. : 44
IN GUIDANCE OF :
PROF. MOHINI SHINDE (MADAM)

4. INDEX
• Abstract
• Introduction
• Approaches of GRDDs
• Appropriate drug candidates for GRDDs
• Factors affecting GRDDs
• Advantages Of GRDDs
• Disadvantages Of GRDDs
• Marketed preparations of GRDDs
• Conclusion
• References

5. 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. The purpose of this project was to
investigate, compile and present the recent as
well as past information in more concise way
with special focus on approaches which are currently utilized
in the prolongation of gastric residence time.
Abstract :

6. • Gastro retentive delivery systems are designed to be retained in the
stomach for a prolonged time and release their active ingredients and
thereby enable sustained and prolonged input of the drug to the upper
part of the gastrointestinal (GI) tract.
Introduction :
• Depends upon fluid and food intake.
• GRDDS are designed to delay gastric emptying .
• GRDDS obtained by retaining dosage form into stomach and by releasing
in controlled manner.

7. Approaches Of Gastric Retention :
• Floating System
• Swelling & Expandable System
• Mucoadhesive/Bioadhesive
System
• High-density System

9. Floating System :
One of the most essential techniques to achieving stomach
retention and appropriate drug bioavailability.
Dosage form should have less bulk density than that of the
gastric fluids (1.004–1.001 gm/cm3),
so that it can float on gastric fluid for entire duration of
therapy,
and the medicine is released slowly with a controlled rate.

10. Swellable & Expandable system:
In swellable and expandable type of system,
the dosage form is designed in such a way that its size is
small enough to administer through oral route but once it
reaches the stomach.
It goes in gastric fluid and swells; thus its size is expanded
and will be difficult to move on through the pyloric sphincter.
This improves the residence time of formulation in stomach.

11. Mucoadhesive System :
MDDSs are non-floating systems formulated to achieve gastric retention of
drugs, these are prepared with various mucoadhesive polymers to get attach
inside the lumen of the stomach wall and survive the gastrointestinal motility
for a longer period, these are also beneficial as site specific
drug absorption in infected area.
Examples of some mucoadhesive excipients are polycarbophil, lectins,
carbopol, chitosan, carboxymethylcellulose (CMC), pectin etc.
There are various types of mucoadhesion like:
• Hydration-Mediated Adhesion.
• Bonding-Mediated Adhesion.
• Receptor-Mediated Adhesion.

12. • Gastric contents have a density close to water.
• A density close to 2.5g/cm³ is necessary for
significant prolongation of gastricresidence 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.
High-density System :

13. • Drugs that acting locally in the stomach. E.g. Antacids.
• Drugs that primarily absorbed in the stomach.E.g. Amoxicillin.
• Drugs that poorly soluble at alkaline pH.E.g. Furosamide, Diazepam,
Verapamil, etc.
• Drugs with a narrow absorption window. E.g. Cyclosporine,, Levodopa,
Methotrexate etc.
• Drugs that absorbed rapidly from the GI tract.E.g. Metronidazole,
tetracycline.
• Drugs that degrade in the colon.E.g. Ranitidine, Metformin.
Appropriate Candidate Drugs For
GRDDS :

14. Advantages :
• Enhanced bioavailability.
• 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.

15. Disadvantages :
• Retention in the stomach is not desirable for drugs that cause gastric
lesions (e.g. Non- steroidal anti-inflammatory drugs NSAIDs).
• Can’t use drugs that are degraded in acidic environment of stomach
(e.g. Insulin).
• Can’t use drugs that undergo a significant first-pass metabolism (e.g.
Nifedipine).
• Can’t use drugs that have very limited acid solubility (e.g. Phenytoin).

16. Factors Affecting GRDDS :
• Gender
• Size and Shape of the dosage form
• Single or Multi unit formulation
• Age
• Density
• Body posture
• Frequency of intake
• Diseased state of an individual

17. Brand Name Active Ingredient(s)
Cifran OD ® Ciprofloxacin
Madopar ® L-DOPA and Benserazide
Valrelease ® Diazepam
Topalkan ® Aluminum –magnesium antacid
Almagate FlatCoat ® Aluminum –magnesium antacid
Liquid Gavison ® Ferrous sulfate
Conviron Ferrous sulfate
Cytotec® Misoprostal
Some Marketed Preparations
Of GRDDs :

18. BASED ON THE ABOVE INFORMATION IT MAY BE
CONCLUDED THAT GASTRO RETENTIVE DRUG DELIVERY
OFFERS
VARIOUS POTENTIAL ADVANTAGES FOR DRUG WITH POOR
BIOAVAILABILITY DUE THEIR ABSORPTION IS RESTRICTED
TO
THE UPPER GASTROINTESTINAL TRACT (GIT) AND THEY
CAN
BE DELIVERED EFFICIENTLY THEREBY MAXIMIZING THEIR
ABSORPTION AND ENHANCING ABSOLUTE
BIOAVAILABILITY.
DUE TO COMPLEXITY OF PHARMACOKINETICS AND
PHARMACODYNAMICS PARAMETERS, IN VIVO STUDIES ARE
REQUIRED TO ESTABLISH THE OPTIONAL DOSAGE FORM
FOR A
SPECIFIC DRUG.
Conclusion :

19. Article of Amit Kumar Nayak,
Gastroretentive drug delivery systems: a review,
Asian Journal of Pharmaceutical and Clinical Research,
March 2010, Page No. : 8.
Article Of Shivram Shinde, Imran Tadwee And Sadhana Shahi,
Gastroretentive drug delivery systems: a review, International Journal
of Pharmaceutical Research & Allied Sciences, J
anuary 2011, Page No. : 10.
Article of Meenakshi Jassal, Ujjwal Nautiyal, Jyotsana Kundlas,
A review : Gastroretentive drug delivery systems,
Indian Journal of Pharmaceutical and Biological Research (IJPBR),
March 2015, Page No. : 1.
References :

20. THANK YOU