The document discusses gastroretentive drug delivery systems (GRDDS). It defines GRDDS as an approach to prolong gastric residence time to target drug release in the upper gastrointestinal tract. It notes that GRDDS are designed to overcome the short gastric residence time and unpredictable gastric emptying time. Potential candidates for GRDDS include drugs that act locally in the stomach, have a narrow absorption window, or have low solubility at high pH. Factors like density, size, and body posture can affect GRDDS. The benefits include improved drug absorption and bioavailability, while the challenges include drugs that may cause gastric lesions or undergo extensive first-pass metabolism. Examples of marketed GRDDS formulations are provided.

1. 10-04-2022 © R R INSTITUTIONS , BANGALORE 1
PRINCIPLE & CONCEPT OF GRDDS
RR COLLEGE OF PHARMACY
SUBMITTED BY: SUBMITTED TO:
PAWAN DHAMALA PROF. Dr. A. GEETHA LAKSHMI
1ST SEM , M.PHARMACY

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CONTENTS
INTRODUCTION
NEED FOR GRDDS
GASTROINTESTINE TRACT PHYSIOLOGY
POTENT CANDIDATES FOR GRDDS
VIDEO SHOWING GRDDS
FACTORS AFFECTING GRDDS
MERITS & DEMERITS
APPLICATION
MARKETED FORMULATION
CONCLUSION
REFERENCE

3. • Gastroretentive drug is an approach to prolong gastric residence time, there by
targeting site specific drugs release in the upper gastrointestinal tract (GIT) for
local or systemic effects.
• It is obtained by retaining dosage form into stomach & by releasing the in
controlled manner.
• Gastric residence time is time which a drug resides in stomach . Depending upon
fluid & food intake, GRDDS are designed to delay gastric emptying.
• GRDDS is designed to overcome physiological problems, such as short gastric
residence time(GRT) & unpredictable gastric emptying times (GET).
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INTRODUCTION

4. • GRDDS are locally active in the stomach (misoprostol, antacids, antibiotics
against H.pylori).
• Have an absorption window in stomach or in the upper small intestine (L-dopa ,
P- aminobenzoic acid, furosemide).
• Exhibit low solubility at high pH values (diazepam, verapamil).
• Alter normal flora of the colon (antibiotics).
• Absorbed by transport mechanism (paclitaxel).
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NEED FOR GRDDS

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GASTROINTESTINAL TRACT
PHYSIOLOGY

6. • Drugs acting locally in the stomach. E.g. Antacids & drugs for H. Pylori viz.,
Misoprolol.
• Drugs that are primarily absorbed in the stomach. E.g. Amoxicillin
• Drugs that is poorly soluble at alkaline pH. E.g. Furosemide, Diazepam, Verampil,
etc.
• Drugs with a narrow absorption window. E.g. Cyclosporine, Levodopa ,
Methotrexate etc.
• Drugs which are absorbed rapidly form the GI tract. E.g. Metronidazole,
tetracycline.
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POTENTIAL CANDIDATES FOR GRDDS

7. Continue…
• Drugs that degrade in the colon. E.g. Ranitidine, Metformin.
• Drugs that disturb normal colonic microbes. E.g. Antibiotics against H. Pylori.
• Drugs with less half life.
• Drugs that have very limited acid solubility. E.g. Phenytoin .
• Drugs that suffer instability in the gastric environment. E.g. Erythromycin.
• Drugs intended for selective release in the colon. E.g. corticosteroids.
• Drugs having extensive fast pass metabolism.
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DRUGS CANDIDATES NOT SUITABLE FOR GRDDS

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VIDEO SHOWING GRDDS

9. • Density
• Size & Shape of the dosage form
• Single or Multi unit formulation
• Age
• Gender
• Body posture
• Frequency of intake
• Diseased state of an individual.
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FACTORS AFFECTING THE GRDDS

10. • Improved drug absorption.
• Enhanced bioavilability.
• Reduced dose frequency.
• Controlled drug delivery of drugs.
• Minimized mucosal irritation.
• Local action.
• Better patient compliance.
• Site specific drug delivery.
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MERITS

11. • Drugs that causes gastric lesions. E.g. NSAIDs.
• Drugs that undergo first pass metabolism. E.g. Nifedipine.
• Drugs that have very limited acid solubility & stability. E.g. Phenytoin.
• Drugs that degrade in acidic environment.
• Drugs which are well absorbed along the entire GIT.
• Requires high levels of fluids in stomach.
• Requires presence of food to delay gastric emptying.
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DEMERITS

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GASTRIC RETENTIVE DRUG DELIVERY
SYSTEM

13. • Enhanced bioavailability.
• Sustained drug delivery.
• Site specific drug delivery system.
• Absorption enhancement.
• Minimized adverse activity at the colon.
• Reduced fluctuation of drug concentration.
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APPLICATIONS

14. S/N Brand name Drug Company
1 Cifran OD Ciprofloxacin Ranbaxy
2 Valrelease Diazepam Hoffman-LaRoche
USA
3 Oflin Ofloxacin Ranbaxy
4 Cytotec Misoprostol Pharmacia USA
5 Conviron Ferrous Sulphate Ranbaxy, India
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MARKETED FORMULATION

15. • The goal of any drug delivery system is to provide a therapeutic
amount of drug to the proper site of the body & also to achieve &
maintain the desired plasma concentration of the drug for a particular
period of time.
• However, incomplete release of the drug, shorter residence times of
dosage forms in the upper GIT leads to lower bioavailability.
• Such limitations of the conventional dosage forms have paved way to
an era of controlled & novel drug delivery system.
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CONCLUSION

16. • International Journal of Pharmaceutical and Chemical Science, 2012;1(2):859-866
• N.K. Jain, Controlled and Novel Drug Delivery, CBS Publishers & Distributors,
New Delhi, First edition 1997 (reprint in 2001).
• Encyclopedia of Controlled Delivery. Edith Mathiowitz, Published by Wiley
Interscience Publication, John Wiley and Sons, Inc, New York.
Chichester/Weinheim
• www.slideshare.com
• www.google.com
• www.Wikipedia.com
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REFERENCE

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