Research paper
Drug absorption sites in the gastrointestinal tract and dosage forms for site-specific delivery

https://doi.org/10.1016/0378-5173(96)85200-8Get rights and content

Abstract

The authors firstly review the literature dealing with drug absorption sites in the gastrointestinal tract. Descriptions are given of the methods used in determining the location of these sites, and the advantages and disavantages of each method are critically discussed. The results obtained concerning the absorption sites of the drugs used in the in vivo methods studied are given in a tabular form and several factors influencing drug absorption are briefly reported. Mechanisms of drug absorption in the human body and their influence on absorption sites are examined. Finally, there is a discussion of various dosage forms which are used for targetting drug absorption to specific sites.

References (181)

  • S.S. Davis

    The design and evaluation of controlled release systems for the gastrointestinal tract

    J. Controlled Release

    (1985)
  • J.T. Doluisio et al.

    Drug absorption I: an in situ rat gut technique yelding realistic absorption rates

    J. Pharm. Sci.

    (1969)
  • J.T. Doluisio et al.

    Drug absorption III: effect of membrane storage on the kinetics of drug absorption

    J. Pharm. Sci.

    (1970)
  • J.B. Dressman et al.

    Gastrointestinal parameters that influence oral medications

    J. Pharm. Sci.

    (1993)
  • J.H. Eldridge et al.

    Biodegradable microspheres as a vaccine delivery system

    Mol. Immunol.

    (1991)
  • G. Fiese et al.

    Further investigations into the absorption of dextrometorphan from the rat's stomach

    J. Pharm. Sci.

    (1969)
  • D.I. Friedman et al.

    Intestinal absorption mechanism of dipeptide angiotensin converting enzyme inhibitors of the lysyl-proline type: lisinopril and SQ 29,852

    J. Pharm. Sci.

    (1989)
  • D.I. Friedman et al.

    Characterization of the intestinal transport parameters for small peptide drugs

    J. Controlled Release

    (1990)
  • C.H. Gleiter et al.

    Colonoscopy in the investigation of drug absorption in healthy volunteers

    Gastrointestinal Endoscopy

    (1985)
  • R. Gröning et al.

    Dosage forms with controlled gastrointestinal passage -studies on the absorption of nitrofuratoin

    Int. J. Pharm.

    (1989)
  • D. Harris et al.

    GI transit of potential bioadhesive formulations in man: a scintigraphic study

    J. Controlled Release

    (1990)
  • D. Harris et al.

    GI transit potential bioadhesive systems in the rat

    J. Controlled Release

    (1990)
  • A.K. Hilton et al.

    In vitro and in vivo evaluation of an oral sustained-release floating dosage form of amoxycillin trihydrate

    Int. J. Pharm.

    (1992)
  • N.F.H. Ho et al.

    Biophysical model approaches to mechanistic transepithelial studies of peptides

    J. Controlled Release

    (1990)
  • M. Ichikawa et al.

    A new multiple-unit oral floating dosage system. II: in vivo evaluation of floating and sustained-release characteristics with p-aminobenzoic acid and isosorbide dinitrate as model drugs

    J. Pharm. Sci.

    (1991)
  • H.M. Ingani et al.

    Conception and in vivo investigation of peroral sustained release floating dosage forms with enhanced gastrointestinal transit

    Int. J. Pharm.

    (1987)
  • J.S. Kim et al.

    Absorption of ACE inhibitors from small intestine and colon

    J. Pharm. Sci.

    (1994)
  • I. Komiya et al.

    Quantitative mechanistic studies in simultaneous fluid flow and intestinal absorption using steroids as model solutes

    Int. J. Pharm.

    (1980)
  • B. Krevsky et al.

    Colonic transit scintigraphy

    Gastroenterology

    (1986)
  • K.H. Antonin

    Other methods in studying colonic drug absorption

  • P. Artursson et al.

    Selective paracellular permeability in two models of intestinal absorption: cultured monolayers of human intestinal epithelial cells and rat intestinal segments

    Pharm. Res.

    (1993)
  • M. Ashford et al.

    Targeting drugs to the colon: delivery systems for oral administration

    J. Drug Targeting

    (1994)
  • R. Balasubramanian et al.

    Pharmacokinetics of acrivastine after oral and colonic administration

    J. Clin. Pharmacol.

    (1989)
  • Banker, G.S., Br. Patent 1,428,426...
  • H. Bechgaard et al.

    Gut reaction to tablets and capsules. 2. Physiological factors and controlled-release dosage forms

    Pharm. J.

    (1982)
  • V. Bohner et al.

    Paracellular transport and other mechanisms involved in intestinal peptide absorption

  • J. Brennan et al.

    The comparative bioavailability of captopril after colonic infusion and oral administration in healthy volunteers

    Clin. Pharmacol. Ther.

    (1991)
  • D. Brockmeier et al.

    Absorption of glibenclamide from different sites of the gastro-intestinal tract

    Eur. J. Clin. Pharmacol.

    (1985)
  • D. Brockmeier

    In vitro/in vivo correlation of dissolution using moments of dissolution and transit times

    Acta Pharm. Technol.

    (1986)
  • D. Brockmeier et al.

    Kinetics of piretanide absorption from the gastrointestinal tract

    Meth. Find. Exp. Clin. Pharmacol.

    (1986)
  • D. Brockmeier et al.

    The absorption of piretanide from the gastro-intestinal tract is site-dependent

    Eur. J. Clin. Pharmacol.

    (1986)
  • H. Brondsted et al.

    Hydrogels for site-specific drug delivery to the colon: in vitro and in vivo degradation

    Pharm. Res.

    (1992)
  • R. Cargill et al.

    Controlled gastric emptying. I. Effects of physical properties on gastric residence times of nondisintegrating geometric shapes in beagle dogs

    Pharm. Res.

    (1988)
  • W.G. Chamblis

    The forgotten dosage form: enteric-coated tablets

    Pharm. Technol.

    (1983)
  • K.K.C. Chan et al.

    Site-differential gastrointestinal absorption of benazepril hydrochloride in healthy volunteers

    Pharm. Res.

    (1994)
  • W.L. Chiou

    Effect of ‘unstirred’ water layer in the intestine on the rate and extent of absorption after oral absorption

    Biopharm. Drug. Dispos.

    (1994)
  • C.S. Cook et al.

    Absorption and disposition of new antiarrhythmic agent bidisomide in man

    Pharm. Res.

    (1993)
  • C. Crevoisier et al.

    Facteurs physico-chimiques susceptibles d'influencer l'absorption gastro-intestinale après dissolution des principes actifs

    Pharm. Acta Helv.

    (1976)
  • L. d'Agay-Abensour et al.

    Absolute bioavailability of an aqueous solution of l-deamino-8-Darginine vasopressin from different regions of the gastrointestinal tract in man

    Eur. J. Clin. Pharmacol.

    (1993)
  • S.S. Davis et al.

    Transit of pharmaceutical dosage forms through the small intestine

    Gut

    (1986)
  • Cited by (302)

    • Mechanical strength and gastric residence time of expandable fibrous dosage forms

      2022, International Journal of Pharmaceutics
      Citation Excerpt :

      Such dosage forms enable the release of drug into the stomach for prolonged time, and hence better control of drug absorption time and drug concentration in blood. This in turn enables improved efficacy, safety, and convenience of many prevailing drug therapies (Davis et al., 1986b; Davis et al., 1988; Rouge et al., 1996; Davis, 2005; Streubel et al., 2006). The concepts mostly examined for gastric retention are the mucoadhesive, floating, and expandable dosage forms.

    View all citing articles on Scopus
    View full text