Comparison of Methodologies for Evaluating Regional Intestinal Permeability

  • A. Raoof
  • D. Moriarty
  • D. Brayden
  • O. I. Corrigan
  • I. Cumming
  • J. Butler
  • J. Devane
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 423)


Drugs are most frequently administered orally and any delay or losses during absorption may contribute to variability in drug response and thus to failure in drug therapy.1 How drugs cross the cell membrane was first described by Overton in 1899 which resulted in “Overton’s Law” i.e. permeability coefficients correlate well with oil/water partition coefficients.2 Modern work, however, indicates that the ability of a drug to traverse a biological membrane is difficult to predict from a simple physicochemical measurement (solubility, lipophilicity, pKa, hydrogen bonding capacity, molecular size or weight) and that other biological factors such as stomach-emptying rate, intestinal motility, the composition (pH profile, volume, enzymes and food) of the intestinal lumen and intrinsic membrane permeability can further limit the bioavailability of drugs.3 Recently, factors related to drug formulation such as particle size and shape, degradation and dissolution of the dosage form have been found to influence the absorption kinetics of drugs.4,5


Large Intestine Transepithelial Electrical Resistance Marker Compound Sodium Pentobarbitone Absorption Surface Area 
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Copyright information

© Plenum Press, New York 1997

Authors and Affiliations

  • A. Raoof
    • 1
  • D. Moriarty
    • 1
  • D. Brayden
    • 1
  • O. I. Corrigan
    • 2
  • I. Cumming
    • 1
  • J. Butler
    • 1
  • J. Devane
    • 1
  1. 1.IVIVR Cooperative Working GroupElan Corp. PlcAthloneIreland
  2. 2.IVIVR Cooperative Working GroupTrinity CollegeDublinIreland

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