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GASTRO RETENTIVE DRUG DELIVERY
SYSTEM (GRDDS)
Presented by:-
Aniket Dinkar Khairnar,
M Pharm (Pharmaceutics),
2022MPP002.
Supervised by:
Dr. D. Madhuri,
Associate Professor,
Dept. of Pharmacy.
CENTRAL UNIVERSITY OF RAJASTHAN
DEPARTMENT OF PHARMACY
1
CONTENT
• INTRODUCTION
• GRDDS APPROACHES
• ADVANTAGES
• CANDIDATES FOR GRDDS
• GASTRO RETENTIVE TECHNOLOGY
• GRDDS TYPES
• APLICATIONS
• CONCLUSION
• REFERENCE
2
Gastroretentive Drug Delivery is an approach to prolong gastric residence
time, thereby targeting site-specific drug release in the upper
gastrointestinal tract (GIT) for local or systemic effects
INTRODUCTION:
3
Osmotically
controlled
Swelling
System
4
ADVANTAGES:
Delivery of drugs with narrow absorption window in the stomach and
small intestine region
Longer residence time in the stomach could be advantageous for local
action in stomach
Reduced Frequency of Dosing with improved patient compliance
Minimize the Fluctuation of drug concentrations
Site specific drug delivery
Drugs that are poorly soluble at the alkaline pH 5
CANDIDATES FOR GRDDS:
Drugs acting locally in the stomach
Drugs that are poorly soluble at the alkaline pH
Drugs with a narrow window of absorption
Drugs with less half life
6
GASTRO RETENTIVE TECHNOLOGY:
j
u
h
7
A) Floating Drug Delivery:
FDDS have a bulk density lower than gastric fluid and thus remain
buoyant in stomach for longer period of time while floating drug will be
release slowly at a desire rate.
These are further Divided into following
1)Effervescent
 Gas generating systems.
 Volatile liquid containing systems.
 Inflatable gastrointestinal delivery systems.
 Intragastric osmotically controlled drug delivery
8
2) Non Effervescent
 Hydrodynamically balanced systems (HBS)
 Hollow Microspheres
 Colloidal Gel Barrier System
 Microporous Membrane System
 Alginate Beads
9
Effervescent System :
1 ) Gas generating systems :
 These buoyant delivery systems utilize
effervescent reactions between
Carbonate/bicarbonate salts and
citric/tartaric acid to liberate CO2, which
gets entrapped in the jellified.
hydrocolloid layer of the systems
 Thus decreasing its specific gravity and
making it to float over gastric content.
10
2 ) Inflatable gastrointestinal delivery
systems
 In these systems an inflatable
chamber is incorporated, which
contains liquid ether that gasifies at
body temperature to cause the
chamber to inflate in the stomach.
11
Non Effervescent
1 ) Hollow Microspheres
 Hollow microspheres loaded with drugs in their other
polymer shelf were prepared by simple solvent
evaporation or solvent diffusion / evaporation methods.
to prolong the gastric retention time (GRT) of the
dosage form.
Polymer Used : polycarbonate,
cellulose acetate, calcium
alginate, Eudragit S, agar and low
methoxylated pectin
12
2 ) Hydrodynamically balanced systems (HBS)
 These system contain drug with gel-
forming hydrocolloids meant to remain
buoyant on the stomach.
 When the capsule containing drug-
hydrocolloid mixture comes in contact
with gastric fluid, the capsule shell
dissolves and the mixture swells to
form a gelatinous barrier content.
Polymers: HPMC, hydroxyethyl cellulose
(HEC), hydroxypropyl cellulose (HPC),
sodium carboxymethyl cellulose (NaCMC),
polycarbophil, polyacrylate, polystyrene
13
B ) Bioadhesive Drug Delivery
 The drug is incorporated with bio/ Muco-adhesive
agents, enabling the Device to adhere to the stomach
walls, Thus resisting gastric emptying.
Polymer Used : Chitosan ,Polyacrylic
acid, Carbopol , Sodium alginate ,
HPMC , Hydroxypropyl cellulose
(HPC)
14
C ) Swellable System
 It should expand for gastric retention
Should be Collapsed after lag time
 Swellable System Also called ‘ PLUG
SYSTEM’
 Size of the formulation more than Pyloric
sphincter
Polymer Used : HPMC , Polyethylene Oxide ,
Hydroxyethyl Cellulose
15
D ) High Density System
 The Dosage Form Should Have (density 2.5 to
3.0 g/ml) To Withstand Peristaltic Movement
and Remained Intact In GIT as Result GI
Transit Time Prolonged
Diluent : Barium Sulphate , Zinc
Oxide, Titanium Dioxide, Iron Powder
16
E ) Magnetic Systems
This approach to enhance the GRT is based on the simple principle
that the dosage form contains a small internal magnet, and a
magnet placed on the abdomen over the position of the stomach.
 Although magnetic system seems to work, the external
magnet must be positioned with a degree of precision
that might compromise patient compliance.
Diluent Used : (Fe2O3 )
17
APPLICATIONS
 Local activity of drugs : Ranitidine,Amoxicilin,Levofloxacin
 Low solubility at alkaline pH : Ofloxacin, Cinnarizine
 Narrow absorption window : Riboflavin, Cilostazol
 Fluctuation of drug concentration : Ciprofloxacin,
Clarithromycin
 Narrow absorption window : Riboflavin,Cilostazol, Pregabalin
18
CONCLUSION :
 GRDDS have great potential to improve the therapeutic efficacy
of drugs.
 GRDDS may need to focus on a combination approach of to
achieve better product quality.
 The goal of any DDS is to provide a therapeutic amount of drug
to the proper site in the body .
 To achieve and maintain the desired plasma concentration of the
drug for a particular period of time.
 Incomplete release of the drug, shorter residence times of dosage
forms in the upper GIT leads to lower oral bio-availability.
19
References :
1) Mandal UK, Chatterjee B, Senjoti FG. Gastro-retentive drug delivery
systems and their in vivo success: A recent update. Asian journal of
pharmaceutical sciences. 2016 Oct 1;11(5):575-84
2) Vinchurkar K, Sainy J, Khan MA, Mane S, Mishra DK, Dixit P.
Features and Facts of a Gastroretentive Drug Delivery System-A
Review. Turk J Pharm Sci. 2022 Aug 31;19(4):476-487
3) Streubel A, Siepmann J, Bodmeier R. Gastroretentive drug delivery
systems. Expert opinion on drug delivery. 2006 Mar 1;3(2):217-33.
20
21

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GRDDS presentation.pptx

  • 1. GASTRO RETENTIVE DRUG DELIVERY SYSTEM (GRDDS) Presented by:- Aniket Dinkar Khairnar, M Pharm (Pharmaceutics), 2022MPP002. Supervised by: Dr. D. Madhuri, Associate Professor, Dept. of Pharmacy. CENTRAL UNIVERSITY OF RAJASTHAN DEPARTMENT OF PHARMACY 1
  • 2. CONTENT • INTRODUCTION • GRDDS APPROACHES • ADVANTAGES • CANDIDATES FOR GRDDS • GASTRO RETENTIVE TECHNOLOGY • GRDDS TYPES • APLICATIONS • CONCLUSION • REFERENCE 2
  • 3. Gastroretentive Drug Delivery is an approach to prolong gastric residence time, thereby targeting site-specific drug release in the upper gastrointestinal tract (GIT) for local or systemic effects INTRODUCTION: 3
  • 5. ADVANTAGES: Delivery of drugs with narrow absorption window in the stomach and small intestine region Longer residence time in the stomach could be advantageous for local action in stomach Reduced Frequency of Dosing with improved patient compliance Minimize the Fluctuation of drug concentrations Site specific drug delivery Drugs that are poorly soluble at the alkaline pH 5
  • 6. CANDIDATES FOR GRDDS: Drugs acting locally in the stomach Drugs that are poorly soluble at the alkaline pH Drugs with a narrow window of absorption Drugs with less half life 6
  • 8. A) Floating Drug Delivery: FDDS have a bulk density lower than gastric fluid and thus remain buoyant in stomach for longer period of time while floating drug will be release slowly at a desire rate. These are further Divided into following 1)Effervescent  Gas generating systems.  Volatile liquid containing systems.  Inflatable gastrointestinal delivery systems.  Intragastric osmotically controlled drug delivery 8
  • 9. 2) Non Effervescent  Hydrodynamically balanced systems (HBS)  Hollow Microspheres  Colloidal Gel Barrier System  Microporous Membrane System  Alginate Beads 9
  • 10. Effervescent System : 1 ) Gas generating systems :  These buoyant delivery systems utilize effervescent reactions between Carbonate/bicarbonate salts and citric/tartaric acid to liberate CO2, which gets entrapped in the jellified. hydrocolloid layer of the systems  Thus decreasing its specific gravity and making it to float over gastric content. 10
  • 11. 2 ) Inflatable gastrointestinal delivery systems  In these systems an inflatable chamber is incorporated, which contains liquid ether that gasifies at body temperature to cause the chamber to inflate in the stomach. 11
  • 12. Non Effervescent 1 ) Hollow Microspheres  Hollow microspheres loaded with drugs in their other polymer shelf were prepared by simple solvent evaporation or solvent diffusion / evaporation methods. to prolong the gastric retention time (GRT) of the dosage form. Polymer Used : polycarbonate, cellulose acetate, calcium alginate, Eudragit S, agar and low methoxylated pectin 12
  • 13. 2 ) Hydrodynamically balanced systems (HBS)  These system contain drug with gel- forming hydrocolloids meant to remain buoyant on the stomach.  When the capsule containing drug- hydrocolloid mixture comes in contact with gastric fluid, the capsule shell dissolves and the mixture swells to form a gelatinous barrier content. Polymers: HPMC, hydroxyethyl cellulose (HEC), hydroxypropyl cellulose (HPC), sodium carboxymethyl cellulose (NaCMC), polycarbophil, polyacrylate, polystyrene 13
  • 14. B ) Bioadhesive Drug Delivery  The drug is incorporated with bio/ Muco-adhesive agents, enabling the Device to adhere to the stomach walls, Thus resisting gastric emptying. Polymer Used : Chitosan ,Polyacrylic acid, Carbopol , Sodium alginate , HPMC , Hydroxypropyl cellulose (HPC) 14
  • 15. C ) Swellable System  It should expand for gastric retention Should be Collapsed after lag time  Swellable System Also called ‘ PLUG SYSTEM’  Size of the formulation more than Pyloric sphincter Polymer Used : HPMC , Polyethylene Oxide , Hydroxyethyl Cellulose 15
  • 16. D ) High Density System  The Dosage Form Should Have (density 2.5 to 3.0 g/ml) To Withstand Peristaltic Movement and Remained Intact In GIT as Result GI Transit Time Prolonged Diluent : Barium Sulphate , Zinc Oxide, Titanium Dioxide, Iron Powder 16
  • 17. E ) Magnetic Systems This approach to enhance the GRT is based on the simple principle that the dosage form contains a small internal magnet, and a magnet placed on the abdomen over the position of the stomach.  Although magnetic system seems to work, the external magnet must be positioned with a degree of precision that might compromise patient compliance. Diluent Used : (Fe2O3 ) 17
  • 18. APPLICATIONS  Local activity of drugs : Ranitidine,Amoxicilin,Levofloxacin  Low solubility at alkaline pH : Ofloxacin, Cinnarizine  Narrow absorption window : Riboflavin, Cilostazol  Fluctuation of drug concentration : Ciprofloxacin, Clarithromycin  Narrow absorption window : Riboflavin,Cilostazol, Pregabalin 18
  • 19. CONCLUSION :  GRDDS have great potential to improve the therapeutic efficacy of drugs.  GRDDS may need to focus on a combination approach of to achieve better product quality.  The goal of any DDS is to provide a therapeutic amount of drug to the proper site in the body .  To achieve and maintain the desired plasma concentration of the drug for a particular period of time.  Incomplete release of the drug, shorter residence times of dosage forms in the upper GIT leads to lower oral bio-availability. 19
  • 20. References : 1) Mandal UK, Chatterjee B, Senjoti FG. Gastro-retentive drug delivery systems and their in vivo success: A recent update. Asian journal of pharmaceutical sciences. 2016 Oct 1;11(5):575-84 2) Vinchurkar K, Sainy J, Khan MA, Mane S, Mishra DK, Dixit P. Features and Facts of a Gastroretentive Drug Delivery System-A Review. Turk J Pharm Sci. 2022 Aug 31;19(4):476-487 3) Streubel A, Siepmann J, Bodmeier R. Gastroretentive drug delivery systems. Expert opinion on drug delivery. 2006 Mar 1;3(2):217-33. 20
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