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Gastro-Intestinal Retentive Drug Delivery System.
- 1. PRESENTED BY DUSANE SHANTANUSANTOSH (PH03) M.PHARMACY (PHARMACEUTICS) UNDER THE GUIDANCE OF MRS. GANGOTRI YADAV DEPT: PHARMACEUTICS SHRI D.D. VISPUTE COLLEGE OF PHARMACYAND RESEARCH CENTRE, PANVEL, NEW MUMBAI. 2025-2026 PRESENTATION ON TOPIC ENTITLED GASTRO RETENTIVE DRUG DELIVERTY SYSTEM
- 2. CONTENT • INTRODCUTION • GITPHYSIOLOGY • POTENTIAL CANDIDATES FOR GRDDS • FACTORS AFFECTING GRDDS • MERIT AND DEMERIT • APPROACHES TO GI TRANSIT • EVALUATION PARAMETERS • APPLICATIONS • MARKETED FORMULATION • CONCLUSION • REFERENCE
- 3. INTRODUCTION Gastroretentive drug deliveryis an innovative approach designed to extend gastric residence time, enabling targeted, site-specific drug release in the upper gastrointestinal tract (GIT) for either local or systemic effects. This method ensures the dosage form stays in the stomach, releasing the drug in a controlled and precise manner.
- 4. The GI tractis a nine-meter tube running from the mouth to the anus, including the throat, esophagus, stomach, small intestine (duodenum, jejunum, ileum), and large intestine (cecum, appendix, colon, rectum). GI Physiology involves – 1) Gastric Emptying Time 2) Gastric Motility 3) Gastrointestinal Transit Time GIT PHYSIOLOGY
- 5. • Start →Gastric Emptying (Occurs in Fasting & Fed States) • Gastric Contractions → Influence Emptying Based on Stomach Contents • Types of Emptying: • Liquids: Emptied by intra-gastric pressure (first-order process) • Digestible Solids: Converted into chyme before emptying • Indigestible Solids: Emptied during fasting via IMMC Gastric Emptying Time:
- 6. Gastric Motility: The InterdigestiveMyoelectric Cycle (MMC) is divided into four phases: Phase I – Basal Phase Last for 30-60 mins (Rare Contraction) Phase II – Preburst Phase Lasts 20-40 minutes, with intermittent action potentials and contractions. Phase IV Lasts 0-5 minutes, occurring between phases III and I. Gradually increasing intensity and frequency Phase III (Burst Phase) Lasts 10-20 minutes, regular contractions also known as housekeeper phase
- 7. Gastrointestinal Transit Time: Theresidence time of liquid & solid foods in each segment of the GI tract is different. Since most drugs are absorbed from the upper intestine (duodenum, jejunum, and ileum), the total effective time for drug absorption is 3-8 hrs. This is why one has to take most drugs 3-6 times a day. Segment Type of food Solid Liquid Stomach 10-30mins 1-3hrs Duodenum 60secs 60secs Jejunum & ileum 3hr±1.5hr 4hr±105hr Colon - 20-50hr
- 8. POTENTIAL CANDIDATES FORGRDDS Drug acting Locally in Stomach Drugs that are poorly soluble at alkaline pH E.g. Furosemide, Diazepam, Verampil Drugs that are primarily absorbed in Stomach E.g. Amoicillin Drugs with narrow absorption window E.g. Cyclosporine, Levodopa, Methotrexate E.g. Antacid and drugs for H. Pylori viz., Misoprolol Drugs which are absorbed rapidly in Stomach E.g. Metronidazole Drugs that have very limited acid solubility E.g. Phenytoin
- 9. FACTORS AFFECTING GRDDS 1)Density. 2) Size and shape of dosage form. 3) Single and Multi unit formulation. 4) Age. 5) Gender. 6) Body Posture. 7) Frequency of intake. 8) Disease state of an individual.
- 10. MERITS DEMERITS o Drugsthat causes gastric lesions. o Drugs that undergoes first pass metabolism. o Drugs that have limited acid solubility and stability. o Drugs that degrade in acidic environment. o Drugs which are well absorbed along with entire GIT. o Required high levels of fluid in stomach. o Required presence of food to delay gastric emptying. o Improved drug absorption. o Enhanced bioavailability. o Reduced dose frequency. o Controlled drug delivery of drug. o Minimized mucosal irritation. o Local action. o Better patient compliance. o Site specific drug delivery. MERITS AND DEMERITS OF GRDDS
- 11. APPROCHES TO GITRANSIT o Floating Systems. o Bio Adhesive Systems. o Swelling System. o High Density Systems.
- 12. Floating systems inGRDDS prolong the residence time of a dosage form in the stomach by making it buoyant. They float on gastric fluid, reducing rapid drug emptying into the small intestine, improving absorption and ensuring sustained release. These systems are especially useful for drugs with a narrow absorption window in the stomach. • Types of FDDS: 1) Effervescent systems. 3) Non effervescent systems. 2) Micro-porous floating system. 4) Alginate bead • Example of marketed formulation: 1) Brand name: Cifran OD 2) Drug: Ciprofloxacin 3) Remark: Gas generating floating tablet Floating System
- 13. Effervescent systems 1. VOLATILELIQUID CONTAINING SYSTEM: INTRAGASTRIC OSMOTICALLY CONTROLLED • These systems have a floating support with a liquid that gasifies at body temperature. A semipermeable coating surrounds the drug reservoir. Upon administration, the liquid volatilizes, the system floats, and water is absorbed, generating osmotic pressure to release the drug.
- 14. 2. Gas-Generating System: Thesesystems use an effervescent reaction between carbonate/bicarbonate salts and citric/tartaric acid to release CO2. The gas is trapped in the gellified hydrocolloid layer, decreasing the system's specific gravity and making it float on the chyme.
- 15. NON- EFFERVESCENT SYSTEMS 1.HYDRODYNAMICALLY BALANCED SYSTEMS: Hydrodynamically Balanced Systems (HBS) use gel-forming hydrocolloids like HPMC and HEC to enhance gastric retention time (GRT) and drug absorption. The drug is in a capsule that dissolves in water, forming a gelatinous barrier that keeps the dosage form buoyant in the stomach. Continuous erosion allows water penetration, maintaining hydration and buoyancy.
- 16. 2. HOLLOW MICROSPHERE Hollowmicrospheres are drug-loaded spheres formed by emulsifying a polymer-drug solution in an aqueous phase with polyvinyl alcohol, creating an oil-in-water emulsion that forms the microspheres.
- 17. 3. Alginate Bead Alginatebeads are prepared by dropping an alginate solution into a calcium chloride solution, forming calcium alginate. The beads are then freeze-dried in liquid nitrogen at -40°C for 24 hours, creating a porous system that remains buoyant for up to 12 hours.
- 19. EVALUATION PARAMETERS Pre-compression test: oSize and shape o Particle size o Density o Specific gravity o Flow property Post-compression test: o Thickness and diameter o Hardness and friability o Weight variation test o Floating time o content uniformity test o Dissolution test o Mucoadhesive test
- 20. IN VITRO TEST oFloating lag time o Floating time o Dissolution time o Swelling index o Mucoadhesive test o Desnsity IN VIVO TEST o Radiology o Scitigraphy o Gastroscopy o Magnetic marker monitoring o Ultrasonography
- 21. MARKTED FORMULATION Sr. No.Brand Name Drug Remark Company 1. Cifran OD Ciprofloxacin Gas generating floating system Rambaxy 2. Oflin OD Ofloxacin Gas generating floating system Rambaxy 3. Cytotec Misoprolol Bilayer floating system Pharmacia, USA 4. Topalkan Al-Mg antacid Floating liquid Pierre Fabre Drug
- 22. APPLICATIONS o Enhanced bioavailability. oSustained drug delivery. o Site specific drug delivery system. o Absorption enhancement. o Minimized adverse activity at colon. o Reduced fluctuation of drug concentration.
- 23. CONCLUSIONS FDDS is apromising approach for gastric retention, improving drug delivery to target sites. Conventional dosage forms face issues like incomplete drug release and short residence time in the upper GIT, reducing bioavailability. This has led to the development of controlled and novel drug delivery systems to enhance drug therapy effectiveness.
- 24. REFERENCE ○ N. K.Jain, Progress in Controlled & Novel Drug Delivery Systems, 1st edition 2004, CBS Publishers, page no.76-86. ○ International Journal of Pharma and Bio Sciences GASTRORETENTIVE DRUG DELIVERY SYSTEM – A REVIEW by RIZWANA KHAN* Institute of Pharmacy Bundelkhand University, Jhansi , U. P., India. ○ S. P. Vyas & R. K. Khar, Controlled drug delivery- concepts and advances, Vallabha Prakashan publishers, page no. 197- 217. ○ A seminar report on FLOATING DRUG DELIVERY SYSTEM, by SHRUSHTI RAMESH KAMBLE.
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