PMID: 41036Oct 1, 1979

An in vitro model for assessing drug availability from lipophilic vehicles

The Journal of Pharmacy and Pharmacology
N A ArmstrongC K Wong

Abstract

An apparatus for studying the rate of release of a solute from a water-immiscible solvent into an acidic, aqueous liquid, followed by permeation through a simulated lipid membrane, is described. The object was to imitate the absorption of a drug after oral administration in a soft gelatin capsule. Rate constants of transfer were determined for a series of substituted benzoic acids, using octanol and isopropyl myristate as solvents. The quantity of solute in the acidic phase did not correlate with the solvent-water distribution coefficient, but was linearly related to the rate constant for transfer from solvent to water. A dynamic system was therefore postulated, rather than one in which the two phases are in equilibrium. In vivo studies on two of the solutes confirmed the in vitro observations. No simple relationship could be derived between blood concentrations and any in vitro parameter, but the rank order of magnitude of the blood concentrations fitted the postulated dynamic mechanism.

References

Aug 21, 2003·International Journal of Pharmaceutics·A A AttamaC O Onugu
Jan 28, 2017·ACS Chemical Neuroscience·Nathan T RodebergR Mark Wightman
Jun 1, 1984·The Journal of Pharmacy and Pharmacology·N A ArmstrongW K Pugh
Dec 1, 1980·The Journal of Pharmacy and Pharmacology·K C JamesL M Sanders
Jun 1, 1984·The Journal of Pharmacy and Pharmacology·N A ArmstrongW K Pugh

Related Concepts

Isopropyl myristate
Microbial Anatomical Capsule Structure
Pharmaceutical Vehicles
Phenylacetic Acids
Octanols
Acids
Lipids
Solute
Membranes, Artificial
Structure of Organ Capsule

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