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A relationship between diffusional transport in lipid membranes and a lipophilic-eutectic parameter.
1Philadelphia College of Pharmacy and Science, PA 19104.
Journal of Theoretical Biology
|December 7, 1986
Summary
A new theoretical model estimates lipophilicity using the lipophilic-eutectic coefficient (Le). This parameter correlates well with transdermal and intestinal absorption, offering a simpler alternative to partition coefficients.
Area of Science:
- Pharmacokinetics
- Physical Chemistry
- Biophysics
Background:
- Passive diffusional transport is crucial for drug absorption.
- Estimating lipophilicity is key to predicting absorption.
- Current methods like partition coefficients can be analytically demanding.
Purpose of the Study:
- To develop a theoretical model for passive diffusional transport.
- To introduce and validate the lipophilic-eutectic coefficient (Le) for estimating lipophilicity.
- To compare Le with traditional methods for predicting absorption.
Main Methods:
- Developed a theoretical model relating passive transport to the lipophilic-eutectic coefficient (Le).
- Utilized melting point depression of a pure substance with a structural impurity.
- Employed cholesterol as a model biological lipid.
Main Results:
- The lipophilic-eutectic coefficient (Le) effectively estimates lipophilicity.
- Le demonstrated a high correlation with transdermal absorption in humans.
- Le showed a high correlation with intestinal absorption in rats.
- Le proved as satisfactory as the partition coefficient for lipophilicity estimation.
Conclusions:
- The lipophilic-eutectic coefficient (Le) is a viable parameter for estimating lipophilicity.
- Le offers a less analytically demanding method compared to partition coefficients.
- This model provides a valuable tool for predicting passive diffusional transport and absorption.