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SEMINAR ON
GASTRO-RETENTIVE DRUG DELIVERY SYSTEM
Presented by: PAWAN DHAMALA
1ST M.PHARM
(Department of pharmaceutics)
Sub: DRUG DELIVERY SYSTEM
 INRODUCTION
 PRINCIPLE
 ADVANTAGE
 DISADVANTAGE
 LIMITATION
 APPROACHES
 CONCLUSION
 REFERENCES
INTRODUCTION
• Oral drug delivery is widely used in
pharmaceutical field to treat the diseases.
• Some drugs are absorbed at specific site only
,these require release at that specific site.
• Gastro retentive drug delivery(GRDDS) is one
of the site specific drug delivery for the delivery
of the drugs at stomach.
• It is obtained by retaining dosage form into
stomach and drug is being released at
controlled manner at specific site
• Drugs acting locally in the stomach. E.g.
Antacids and drugs for H. Pylori viz., Misoprostol.
• Drugs that are primarily absorbed in the stomach.
E.g. Amoxicillin
• Drugs that is poorly soluble at alkaline pH. E.g.
Furosamide, Diazepam, Verapamil, etc.
• Drugs with a narrow absorption window. E.g.
Cyclosporine, Levodopa, Methotrexate etc
.
GRDDS
• Drugs which are absorbed rapidly
from the GI tract. E.g.
Metronidazole, tetracycline.
• Drugs that degrade in the colon.
E.g. Ranitidine, Metformin.
• Drugs that disturb normal colonic
microbes E.g. antibiotics against
Helicobacter pylori
ADVANTAGES
• Enhanced bioavailability.
• Sustained drug delivery/reduced frequency of
Dosing.
• Targeted therapy for local ailments in the upper
GIT.
• Reduced fluctuations of drug concentration.
• Improved selectivity in receptor activation
• Reduced counter-activity of the body
 Relatively small absorptive surface
area (0.01 sqm vs 100 sq m for GIT).
 Movement affects muco adhesive
systems.
 Less permeable than the small
intestine.
 Salivation and swallowing.
 Taste of the drug.
 Not applicable for unconsciouspatient.
 .
• Not suitable for drugs that have
solubility or stability problem in GIT.
• Drugs which are irritant to gastric
mucosa are also not suitable.
• These systems do not offer significant
advantages over the conventional dosage
forms for drugs, which are absorbed
throughout GIT.
 Bio-adhesive systems, cannot prevail longer
due to high turn-over rate of mucus layer and
presence of soluble mucin.`
 For swelling systems, it is necessary that the
formulation should not exit before the
appropriates welling.
 For High density systems, High amount of
drug is required.
` • High-density systems. (HDS)
• Floating systems. (FS)
• Swelling and expanding systems.
(SS)
• Mucoadhesive & Bioadhesive
systems. (AS)
• Gastro retentive drug delivery systems have
emerged as a current approache of controlled
delivery of drugs that exhibit an absorption
window.
• All these drug delivery systems have their
own advantages and drawbacks.
• To design a successful GRDDS, it is
necessary to take into consideration the
physicochemical properties of the drug,
physiological events in the GIT, formulation
strategies, and correct combination of drug
and excipients.
 Hardness Friability
 Drug
 Content
 Diameter
 Weight
 Variation
 Evaluation of GRDDS
 Dissolution
 medium : 0.1 N HCl
 Temp. : 37 ± 0.5°C
 RPM : 50-100
 Sample analysis :
 UV
 Dissolution Study
 In-vitro
 Mucoadhesion
 Apparatus : USP
 type VI (rotating
 cylinder apparatus)
 Evaluation of GRDDS
 Medium : 0.1 N HCl
 Evaluation of GRDDS
 Temp. : 37 ± 0.5°C
 RPM : 100
 Lag time :
 Measurement : 0.1 N HCl at pH 1.2
 Temp. : 37 ± 0.5°C
 Apparatus : USP Type II dissolution
apparatus
 A tablet is placed in a beaker containing
100 –200 ml dissolution medium & the time
for a tablet to emerge on to the surface of the
dissolution medium is known as lag time .
 Floating Time
 After achieving lag time, the time taken for a tablet
to remain float on the surface of the dissolution
medium is called floating time.
 Water uptake :
 Apparatus : USP type II dissolution apparatus
 Medium : Water
 Temp. : 37 ± 0.5°C
 RPM : 50
 WU (%) = Wt. of swollen tab. – Initial wt. of tab.
Initial wt. of tab. × 100
 Evaluation of GRDDS

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Seminar on Gastro-Retentive Drug Delivery Systems

  • 1. SEMINAR ON GASTRO-RETENTIVE DRUG DELIVERY SYSTEM Presented by: PAWAN DHAMALA 1ST M.PHARM (Department of pharmaceutics) Sub: DRUG DELIVERY SYSTEM
  • 2.  INRODUCTION  PRINCIPLE  ADVANTAGE  DISADVANTAGE  LIMITATION  APPROACHES  CONCLUSION  REFERENCES
  • 3. INTRODUCTION • Oral drug delivery is widely used in pharmaceutical field to treat the diseases. • Some drugs are absorbed at specific site only ,these require release at that specific site. • Gastro retentive drug delivery(GRDDS) is one of the site specific drug delivery for the delivery of the drugs at stomach. • It is obtained by retaining dosage form into stomach and drug is being released at controlled manner at specific site
  • 4. • Drugs acting locally in the stomach. E.g. Antacids and drugs for H. Pylori viz., Misoprostol. • Drugs that are primarily absorbed in the stomach. E.g. Amoxicillin • Drugs that is poorly soluble at alkaline pH. E.g. Furosamide, Diazepam, Verapamil, etc. • Drugs with a narrow absorption window. E.g. Cyclosporine, Levodopa, Methotrexate etc .
  • 5. GRDDS • Drugs which are absorbed rapidly from the GI tract. E.g. Metronidazole, tetracycline. • Drugs that degrade in the colon. E.g. Ranitidine, Metformin. • Drugs that disturb normal colonic microbes E.g. antibiotics against Helicobacter pylori
  • 6. ADVANTAGES • Enhanced bioavailability. • Sustained drug delivery/reduced frequency of Dosing. • Targeted therapy for local ailments in the upper GIT. • Reduced fluctuations of drug concentration. • Improved selectivity in receptor activation • Reduced counter-activity of the body
  • 7.  Relatively small absorptive surface area (0.01 sqm vs 100 sq m for GIT).  Movement affects muco adhesive systems.  Less permeable than the small intestine.  Salivation and swallowing.  Taste of the drug.  Not applicable for unconsciouspatient.
  • 8.  . • Not suitable for drugs that have solubility or stability problem in GIT. • Drugs which are irritant to gastric mucosa are also not suitable. • These systems do not offer significant advantages over the conventional dosage forms for drugs, which are absorbed throughout GIT.
  • 9.  Bio-adhesive systems, cannot prevail longer due to high turn-over rate of mucus layer and presence of soluble mucin.`  For swelling systems, it is necessary that the formulation should not exit before the appropriates welling.  For High density systems, High amount of drug is required.
  • 10. ` • High-density systems. (HDS) • Floating systems. (FS) • Swelling and expanding systems. (SS) • Mucoadhesive & Bioadhesive systems. (AS)
  • 11. • Gastro retentive drug delivery systems have emerged as a current approache of controlled delivery of drugs that exhibit an absorption window. • All these drug delivery systems have their own advantages and drawbacks. • To design a successful GRDDS, it is necessary to take into consideration the physicochemical properties of the drug, physiological events in the GIT, formulation strategies, and correct combination of drug and excipients.
  • 12.  Hardness Friability  Drug  Content  Diameter  Weight  Variation
  • 13.  Evaluation of GRDDS  Dissolution  medium : 0.1 N HCl  Temp. : 37 ± 0.5°C  RPM : 50-100  Sample analysis :  UV  Dissolution Study
  • 14.  In-vitro  Mucoadhesion  Apparatus : USP  type VI (rotating  cylinder apparatus)  Evaluation of GRDDS  Medium : 0.1 N HCl  Evaluation of GRDDS  Temp. : 37 ± 0.5°C  RPM : 100
  • 15.  Lag time :  Measurement : 0.1 N HCl at pH 1.2  Temp. : 37 ± 0.5°C  Apparatus : USP Type II dissolution apparatus  A tablet is placed in a beaker containing 100 –200 ml dissolution medium & the time for a tablet to emerge on to the surface of the dissolution medium is known as lag time .
  • 16.  Floating Time  After achieving lag time, the time taken for a tablet to remain float on the surface of the dissolution medium is called floating time.  Water uptake :  Apparatus : USP type II dissolution apparatus  Medium : Water  Temp. : 37 ± 0.5°C  RPM : 50  WU (%) = Wt. of swollen tab. – Initial wt. of tab. Initial wt. of tab. × 100  Evaluation of GRDDS