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GRDDS

Gastro Retentive Drug Delivery Systems (GRDDS) are designed to increase the gastric residence time and sustain the release of drugs in the stomach or upper gastrointestinal tract. There are several approaches to achieve this, including floating systems (which float on the gastric contents), high density systems (which sink to the bottom of the stomach), inflatable systems (which expand in size), and gastroadhesive systems (which adhere to the stomach walls). GRDDS provide benefits such as reduced dosing frequency, improved drug absorption for drugs that are better absorbed in the upper GI tract, and more sustained drug delivery. However, they may also cause gastric irritation for some drugs and are not suitable for drugs that are unstable in acidic conditions.

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41 views17 pages

GRDDS

Gastro Retentive Drug Delivery Systems (GRDDS) are designed to increase the gastric residence time and sustain the release of drugs in the stomach or upper gastrointestinal tract. There are several approaches to achieve this, including floating systems (which float on the gastric contents), high density systems (which sink to the bottom of the stomach), inflatable systems (which expand in size), and gastroadhesive systems (which adhere to the stomach walls). GRDDS provide benefits such as reduced dosing frequency, improved drug absorption for drugs that are better absorbed in the upper GI tract, and more sustained drug delivery. However, they may also cause gastric irritation for some drugs and are not suitable for drugs that are unstable in acidic conditions.

Uploaded by

Nivetha
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Gastro Retentive Drug

Delivery System (GRDDS)


Gastric emptying time

GIT emptying time


Introduction:
o Conventional oral drug delivery system is complicated by limited GRT
(Gastric Residence Time).
o Rapid GI trasit prevent complete drug release in absorption zone and
reduce the efficiency of dose.
o To overcome these limitations, GRDDS approach has proposed to
increase gastric residence time.
Definition:
It is one of the site specific drug delivery system at stomach, obtained
by retaining dosage form into the stomach and drug is being released at
sustained manner to specific site either in stomach or intestine.
Ways To Retain The Formulation In Stomach

Floating High density system


Inflatable Gastroadhesive system
Floating:
• Tablet density < Gastric contents density.
• Hence, tablet remain buoyant i.e., floats on gastric contents.
• There is always some gastric content even after gastric emptying.
• Hence, tablet remains in the stomach for a prolonged period.
Advantages:
• Poorly soluble in water/ alkaline pH.
• Drugs which are unstable in intestinal fluids.
• Primarily absorbed from stomach.
• Narrow window of absorption.

Disadvantage:
• Formulation must be take with full glass of water – 250ml.
High density system:
• Tablet density > Gastric content density.
• Tablet density should be more than 3g/cm3.
• Hence, tablet remain at the bottom of stomach.
• Capable to withstand peristaltic movement of stomach.
• Hence, tablet remain in the stomach for a prolonged period.
• Prepared by coating/ mixing drug with heavy inert material like
Barium sulphate, Titanium dioxide.
Disadvantage:
• High amount of drug required.
• In some patients, formulation can’t
withstand peristaltic movement.
Inflatable:
• Size of the formulation will be increased inside the stomach.
• Tablet size becomes more than size of pyrolic sphincter.
• Inflatable chamber are used for this purpose.
Eg: Liquid ether filled in inflatable chamber.
• The swelled tablet should be porous, then only the remaining gastric
contents will pass into intestine.
• After desired period, the tablet will be collapsed.
• Since it plugs the pyloric sphincter, also called as plug system.
Disadvantage:
• If gastric emptying takes place, before the swelling of tablet, then
formulation will fail.
Gastroadhesive system:
• Formulation contains = Drug + Mucoadhesive polymers.
• Mucoadhesive polymer is responsible for adhesion.
Eg: Chitosan, Carbopol, Sodium alginate, HPMC K4M.
• Tablet is adhesive to the stomach walls.
• Withstand the both: peristaltic movement, gastric emptying.
Disadvantage:
• Mucous in the stomach walls is in a state of constant
renewal results in unpredictable adherence.
• Chance to adhere to esophagus.
• Very difficult to ensure that tablet is adhere to stomach.
• This approach is not widely used.
Advantages of GRDDS:
• Reduced dosing frequency
• Improve drug absorption
• Sustained and desired rate of drug delivery can be achieved
• Targeted therapy for local upper GIT infections, disease and disorder
• Suitable for drugs with shorter half life
• Suitable for drugs with narrow absorption window in intestine
• Ease of administration
• Possibility of bioavailablility improvement
Disadvantages of GRDDS:
• High chance of gastric irritation ~ stomach burning. Eg: NSAIDs
• Not suitable for drugs which are unstable in acidic pH. Eg: insulin
• Drugs undergo significant 1st pass metabolism. Eg: nifedipine
• Not suitable for limited acid soluble drugs. Eg: phenytoin
• Requires high level of fluid in stomach for floating and to work
efficiently.
• Peristaltic movements, gastric emptying varies patient to patients,
hence, if formulation is not proper, therapeutic failure may elicit.
Application of GRDDS:
• Sustained drug delivery: suitable for drugs with shorter half life,
prolonged release can be achieved, desired rate of drug release also
achieved.
• Useful for drugs having poor bioavailability when compare to non-
GRDDS.
• Suitable for peptic ulcer treatment.
• Absorption enhancement can be achieved.
• Reduces the fluctuations of drug concentration.
THANK YOU

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