PMID: 7888601Nov 1, 1994Paper

Effect of 'unstirred' water layer in the intestine on the rate and extent of absorption after oral administration

Biopharmaceutics & Drug Disposition
W L Chiou

Abstract

The presence of an aqueous diffusion layer or 'unstirred' water layer adjacent to the intestinal membrane has long been regarded as a potential barrier for intestinal absorption of compounds. Theoretical analyses were performed in the present study to quantitatively determine the effect of this layer on the rate and extent of absorption of passively absorbed compounds with different membrane absorption half-lives (10 to 300 min) in humans, dogs, rabbits, rats and mice. Diffusion half-lives across this (40 microns thick) layer were estimated to be 5.8, 2.5, 1.1, 0.65 and 0.32 min, respectively, in the distended intestine of the above five species. These half-lives are reduced by about 5-fold when the intestine is about 80% 'flat' in fasting state. The results of extensive analysis indicate that the presence of such a layer is generally expected to have a relatively mild or insignificant effect on the rate of absorption and an insignificant effect on the extent of absorption. The study also indicates that an aqueous layer of 708 microns has practically no effect on the extent of absorption of progesterone, a highly lipophilic compound, in rats. For prediction of or correlation with the fraction of oral dose absorbed after oral ad...Continue Reading

References

May 1, 1992·Journal of Pharmaceutical Sciences·W L ChiouM H Abdel-Hameed
Aug 1, 1991·Pharmaceutical Research·P J SinkoG L Amidon
Nov 1, 1990·The Journal of Clinical Investigation·M D LevittD G Levitt
Mar 1, 1988·The American Journal of Physiology·S E AndersonP M Cala
Aug 1, 1980·Journal of Pharmacokinetics and Biopharmaceutics·W L Hayton
Jun 1, 1986·Pharmaceutical Research·J B Dressman

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Citations

Aug 15, 2002·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Ta C WuWin L Chiou
Nov 7, 2002·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Ta C WuWin L Chiou
Jan 1, 1997·Annual Review of Entomology·M J Lehane
Apr 1, 2009·Expert Opinion on Drug Metabolism & Toxicology·Kiyohiko Sugano
Jan 20, 1998·Drug and Chemical Toxicology·M M Doherty, K S Pang
May 20, 1998·Journal of Pharmaceutical Sciences·R E OliverM Rowland
Nov 11, 2008·International Journal of Pharmaceutics·Kiyohiko Sugano
Apr 14, 2016·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Sarit Cohen RabbieJoseph F Standing
Aug 1, 1996·Journal of Pharmacokinetics and Biopharmaceutics·W L Chiou
Oct 3, 2018·Therapeutic Delivery·Nikhitha K ShanmukhanSamuel Gideon
Aug 26, 2018·Angewandte Chemie·Andreas F B RäderHorst Kessler
May 21, 2003·American Journal of Veterinary Research·Randal K Buddington, Christiane Malo

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