Absorption of drugs from the gastrointestinal tract

ABSORPTION OF DRUGS FROM THE GASTROINTESTINAL TRACT

  • Before a drug can be absorbed, it must dissolve in the aqueous contents of the gut. Thus, the actual amount of the drug present in a dose is only one of the factors that will affect the amount of drug actually absorbed or available.
  • Factors affecting absorption include
    • Molecular size of the drug and its concentration
    • Degree of ionizationĀ (depends on the pKa of the drug and pH of the medium)
    • Lipid solubility of the neutral or nonionized form of the drug.
    • Chemical or physical interaction with co-administered preparations and food constituents
    • Pharmaceutical preparation and dosage form, especially their disintegration rate and dissolution rateĀ 
    • Gastric motility and secretion as well as gastric emptying
    • Intestinal motility and secretion as well as intestinal transit time
    • Fluid volume within the gastrointestinal tract
    • Osmolality of the intestinal contents
    • Intestinal blood and lymph flow
    • Disruption of the functional and structural integrity of the gastric and intestinal epithelium
    • Drug biotransformation within the intestinal lumen by microflora or within the mucosa by host enzymes
    • Volume and surface area of the absorbing surface. Stomach has a relatively small surface area compared to the duodenum. Hence absorption is more in the duodenum.
    • Presence of food in the stomach. Normally in full stomach there is a delay in absorption because the drug gets diluted in the stomach contents.
Last modified: Wednesday, 25 April 2012, 5:45 AM