Principle & concept of GRDDS.pptx

Prepared By: Pawan Dhamala
M.Pharmacy(Pharmaceutics),
RR College Of Pharmacy.

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

2. 10-04-2022 © R R INSTITUTIONS , BANGALORE 2 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). 10-04-2022 © R R INSTITUTIONS , BANGALORE 3 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). 10-04-2022 © R R INSTITUTIONS , BANGALORE 4 NEED FOR GRDDS

5. 10-04-2022 © R R INSTITUTIONS , BANGALORE 5 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 . 10-04-2022 © R R INSTITUTIONS , BANGALORE 6 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. 10-04-2022 © R R INSTITUTIONS , BANGALORE 7 DRUGS CANDIDATES NOT SUITABLE FOR GRDDS

8. 10-04-2022 © R R INSTITUTIONS , BANGALORE 8 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. 10-04-2022 © R R INSTITUTIONS , BANGALORE 9 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 . 10-04-2022 © R R INSTITUTIONS , BANGALORE 10 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 . 10-04-2022 © R R INSTITUTIONS , BANGALORE 11 DEMERITS

12. 10-04-2022 © R R INSTITUTIONS , BANGALORE 12 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 . 10-04-2022 © R R INSTITUTIONS , BANGALORE 13 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 10-04-2022 © R R INSTITUTIONS , BANGALORE 14 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. 10-04-2022 © R R INSTITUTIONS , BANGALORE 15 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 10-04-2022 © R R INSTITUTIONS , BANGALORE 16 REFERENCE

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