Bioavailability Enhancement Through Gastrointestinal Retention

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Chapter: Biopharmaceutics and Pharmacokinetics : Bioavailability and Bioequivalence

Gastro-retentive drug delivery systems (GRDDS) are designed on the basis of delayed gastric emptying and CR principles.


BIOAVAILABILITY ENHANCEMENT THROUGH GASTROINTESTINAL RETENTION

Gastro-retentive drug delivery systems (GRDDS) are designed on the basis of delayed gastric emptying and CR principles, and are intended to restrain and localize the drug delivery device in the stomach or within the upper parts of the small intestine until the entire drug is released. Excipients that are bioadhesive or that swell on hydration when incorporated in an oral dosage form, can promote gastro-retention and absorption by –

·            Increased contact with epithelial surfaces

·            Prolonging residence time in the stomach

·            Delaying intestinal transit.

Cellulose ethers, gums of natural origin, and synthetic acrylic acid polymers have been evaluated for such purposes. The range of materials available and their differing viscoelastic and rheological behaviours mean that it is possible, by judicious admixture, to develop delivery units with balanced properties so that adhesion, density, hydration, drug release rate, etc. can be tailored to the drug in question and the physiological characteristics of the target delivery site.

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