Studies on the reliability of a bihyperbolic functional absorption model. I. Ring-substituted anilines
- 1 December 1986
- journal article
- research article
- Published by Springer Nature in Journal of Pharmacokinetics and Biopharmaceutics
- Vol. 14 (6) , 615-633
- https://doi.org/10.1007/bf01067967
Abstract
The present study reviews and checks the rearranged master lines of the functional bihyperbolic absorption model proposed by Plá-Delfina and Moreno, by examining the correlations between absorption rate constants experimentally found in the small intestine and in the colon of the rat, and two types of partition constants for a series of ring-substituted anilines, of low to medium molecular weight. Evidence is given which demonstrates the reliability of the bihyperbolic equation for the small intestine data, showing the importance of the type of substitution in the absorption rate of compounds; for the colonic data, the collapsed, monohyperbolic form of this equation (i.e., the Wagner-Sedman equilibrium model) applies, independent of the nature and position of the group substituents in the aniline molecule. This means that, as the bihyperbolic model equation predicts, aqueous pore diffusion is a crucial factor, as important as membrane permeation, in absorption in the small intestine, whereas in the colon only this latter route is operative. The perspectives opened by the application of the model to gastrointestinal absorption studies are also discussed.Keywords
This publication has 24 references indexed in Scilit:
- Intestinal absorption-partition relationships: A tentative functional nonlinear modelJournal of Pharmacokinetics and Biopharmaceutics, 1981
- Propranolol absorption in different regions of the rat gastrointestinal tract in situ: implications for sustained release formulationsJournal of Pharmacy and Pharmacology, 1980
- An experimental assessment of the Wagner-Sedman extraction theory for the intestinal absorption of antibacterial sulfonamidesJournal of Pharmacokinetics and Biopharmaceutics, 1980
- Calculation of the gastric absorption rate constants of 5-substituted barbiturates through theR m values or substituent ΔR m constants in reversed-phase partition chromatographyJournal of Pharmacokinetics and Biopharmaceutics, 1975
- Use of chromatographicR m values as a possible approach to calculation of the absorption rate constants for some related drugsJournal of Pharmacokinetics and Biopharmaceutics, 1973
- Clearance concepts in pharmacokineticsJournal of Pharmacokinetics and Biopharmaceutics, 1973
- Quantitaton of rate of gastrointestinal and buccal absorption of acidic and basic drugs based on extraction theoryJournal of Pharmacokinetics and Biopharmaceutics, 1973
- Linear free energy relations between partitioning solvent systemsThe Journal of Organic Chemistry, 1971
- Drug Absorption III: Effect of Membrane Storage on the Kinetics of Drug AbsorptionJournal of Pharmaceutical Sciences, 1970
- Drug Absorption I: An In Situ Rat Gut Technique Yielding Realistic Absorption RatesJournal of Pharmaceutical Sciences, 1969